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Sample records for rebamipide 100-mg tablets

  1. Implementation of Quality by Design for Formulation of Rebamipide Gastro-retentive Tablet.

    Science.gov (United States)

    Ha, Jung-Myung; Seo, Jeong-Woong; Kim, Su-Hyeon; Kim, Ju-Young; Park, Chun-Woong; Rhee, Yun-Seok; Park, Eun-Seok

    2017-11-01

    The purpose of the present study was to develop a rebamipide (RBM) gastro-retentive (GR) tablet by implementing quality by design (QbD). RBM GR tablets were prepared using a sublimation method. Quality target product profile (QTPP) and critical quality attributes (CQAs) of the RBM GR tablets were defined according to the preliminary studies. Factors affecting the CQAs were prioritized using failure mode and effects analysis (FMEA). Design space and optimum formulation were established through a mixture design. The validity of the design space was confirmed using runs within the area. The QTPP of the RBM GR tablets was the orally administered GR tablet containing 300 mg of RBM taken once daily. Based on the QTPP, dissolution rate, tablet friability, and floating property were chosen as CQAs. According to the risk assessment, the amount of sustained-release agent, sublimating material, and diluent showed high-risk priority number (RPN) values above 40. Based on the RPN, these factors were further investigated using mixture design methodology. Design space of formulations was depicted as an overlaid contour plot and the optimum formulation to satisfy the desired responses was obtained by determining the expected value of each response. The similarity factor (f2) of the release profile between predicted response and experimental response was 89.463, suggesting that two release profiles are similar. The validity of the design space was also confirmed. Consequently, we were able to develop the RBM GR tablets by implementing the QbD concept. These results provide useful information for development of tablet formulations using the QbD.

  2. Bioequivalence of a single 400-mg dose of imatinib 100-mg oral tablets and a 400-mg tablet in healthy adult Korean volunteers.

    Science.gov (United States)

    Lee, Hae Won; Seong, Sook Jin; Park, Sung Min; Lee, Joomi; Gwon, Mi-Ri; Kim, Hyun-Ju; Lim, Sung Mook; Lim, Mi-Sun; Kim, Woomi; Yang, Dong Heon; Yoon, Young-Ran

    2015-06-01

    Imatinib mesylate (IM) is a selective tyrosine kinase inhibitor for the treatment of chronic myeloid leukemia and gastrointestinal stromal tumors. A new once-daily 400-mg film-coated tablet of imatinib has been developed by a pharmaceutical company in Korea. The present study was designed to assess and compare the PK parameters, bioavailability, and bioequivalence of the new imatinib 400-mg formulation (test) versus the conventional 100-mg formulation (reference) administered as a single 400-mg dose in healthy adult male volunteers. This randomized, open-label, single-dose, two-way crossover study was conducted in healthy Korean male volunteers. Eligible subjects were randomly assigned in a 1 : 1 ratio to receive 400 mg of the test (one 400-mg tablet) or reference (four 100-mg tablets) formulation, followed by a 2-week washout period and administration of the alternate formulation. Serial blood samples were collected at 0 (predose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24, 48, and 72 hours after administration. Plasma imatinib concentrations were determined using liquid chromatography coupled with tandem mass spectrometry. The formulations were to be considered bioequivalent if the 90% confidence intervals (CIs) of the adjusted geometric mean ratios for Cmax, AUC(0-t), and AUC(0-∞)ž were within the predetermined range of 0.80 - 1.25. In total, 35 subjects completed the study. No serious adverse event was reported during the study. The 90% CIs of the adjusted geometric mean ratios of the test formulation to the reference formulation for C(max), AUC(0-t) and AUC(0-∞)ž of imatinib were all within the bioequivalence criteria range of 0.8 - 1.25. The test formulation of imatinib met the Korean regulatory requirements for bioequivalence. Both imatinib formulations were well-tolerated in all subjects.

  3. Bioequivalence of 2 Formulations of Sildenafil Oral Soluble Film 100 mg and Sildenafil Citrate (Viagra) 100 mg Oral Tablets in Healthy Male Volunteers.

    Science.gov (United States)

    Dadey, Eric

    Sildenafil citrate tablets (VIAGRA; Pfizer Inc) have been used since 1998 as an oral therapy for the treatment of erectile dysfunction. However, in some cases, patients may have difficulty in swallowing tablets, and the need to use water to aid in the oral administration of the tablets has the potential to interrupt the sexual encounter, reduce spontaneity, and therefore decrease the quality of the experience. Two oral soluble film (OSF) formulations of sildenafil were developed using MonoSol Rx's proprietary PharmFilm technology. Both films were formulated to dissolve rapidly on the tongue, thereby releasing the drug into the oral cavity, whereupon it is swallowed without the use of water. From a patient perspective, it is anticipated that the film formulations of sildenafil citrate will provide a more compliant and discreet dosage form. The purpose of this clinical study was to compare the bioequivalence of the 2 sildenafil OSF 100 mg formulations (MonoSol Rx, LLC) with the sildenafil citrate 100 mg tablets. The design was a single-dose, randomized, open-label, 3-period, 6-sequence, 3-treatment, single-center, crossover study conducted in 18 healthy, nonsmoking male volunteers under fasting conditions, with each treatment period separated by a 7-day washout period. Plasma sildenafil concentrations were measured predose and then periodically to 24 hours after dosing. The 90% confidence intervals for plasma sildenafil AUC0-t, AUC0-∞, and Cmax for both sildenafil OSF formulations as compared with sildenafil citrate tablets were all within the 80%-125% range, indicating bioequivalence of both film formulations to sildenafil citrate tablets. Overall, the demonstrated bioequivalence coupled with the performance advantages of an OSF dosage form (ie, rapid dissolution in the mouth, can be taken without water, and can be dosed discreetly) suggest that the sildenafil OSF may provide an attractive alternative to sildenafil citrate oral tablets.

  4. Rebamipide suppresses diclofenac-induced intestinal permeability via mitochondrial protection in mice.

    Science.gov (United States)

    Diao, Lei; Mei, Qiao; Xu, Jian-Ming; Liu, Xiao-Chang; Hu, Jing; Jin, Juan; Yao, Qiang; Chen, Mo-Li

    2012-03-14

    To investigate the protective effect and mechanism of rebamipide on small intestinal permeability induced by diclofenac in mice. Diclofenac (2.5 mg/kg) was administered once daily for 3 d orally. A control group received the vehicle by gavage. Rebamipide (100 mg/kg, 200 mg/kg, 400 mg/kg) was administered intragastrically once a day for 3 d 4 h after diclofenac administration. Intestinal permeability was evaluated by Evans blue and the FITC-dextran method. The ultrastructure of the mucosal barrier was evaluated by transmission electron microscopy (TEM). Mitochondrial function including mitochondrial swelling, mitochondrial membrane potential, mitochondrial nicotinamide adenine dinucleotide-reduced (NADH) levels, succinate dehydrogenase (SDH) and ATPase activities were measured. Small intestinal mucosa was collected for assessment of malondialdehyde (MDA) content and myeloperoxidase (MPO) activity. Compared with the control group, intestinal permeability was significantly increased in the diclofenac group, which was accompanied by broken tight junctions, and significant increases in MDA content and MPO activity. Rebamipide significantly reduced intestinal permeability, improved inter-cellular tight junctions, and was associated with decreases in intestinal MDA content and MPO activity. At the mitochondrial level, rebamipide increased SDH and ATPase activities, NADH level and decreased mitochondrial swelling. Increased intestinal permeability induced by diclofenac can be attenuated by rebamipide, which partially contributed to the protection of mitochondrial function.

  5. Bioequivalence study of a new sildenafil 100 mg orodispersible film compared to the conventional film-coated 100 mg tablet administered to healthy male volunteers

    Science.gov (United States)

    Radicioni, Milko; Castiglioni, Chiara; Giori, Andrea; Cupone, Irma; Frangione, Valeria; Rovati, Stefano

    2017-01-01

    A new orodispersible film formulation of the phosphodiesterase type 5 inhibitor, sildenafil, has been developed to examine the advantages of an orally disintegrating film formulation and provide an alternative to the current marketed products for the treatment of erectile dysfunction. The pharmacokinetics of the sildenafil 100 mg orodispersible film (IBSA) was compared to that of the conventional marketed 100 mg film-coated tablet (Viagra®) after single-dose administration to 53 healthy male volunteers (aged 18–51 years) in a randomized, open, two-way crossover bioequivalence study. Each subject received a single oral dose of 100 mg of sildenafil as test or reference formulation administered under fasting conditions at each of the two study periods according to a randomized crossover design. There was a washout interval of ≥7 days between the two administrations of the investigational medicinal products. Blood samples for pharmacokinetic analysis were collected up to 24 h post-dosing. The primary objective was to compare the rate (peak plasma concentration; Cmax) and extent (area under the curve [AUC] from administration to last observed concentration time; AUC0–t) of sildenafil absorption after single-dose administration of test and reference. Secondary endpoints were observed to describe the plasma pharmacokinetic profiles of sildenafil and its metabolite N-desmethyl-sildenafil relative bioavailability and safety profile after single-dose administration. The mean sildenafil and N-desmethyl-sildenafil plasma concentration–time profiles up to 24 h after single-dose administration of sildenafil 100 mg orodispersible film and film-coated tablet were nearly superimposable. The bioequivalence test was fully satisfied for sildenafil and N-desmethyl-sildenafil in terms of rate and extent of bioavailability. Adverse events occurred at similar rates for the two formulations and were of mild-to-moderate severity. The results suggest that the new orodispersible film

  6. Effect of combination tablets containing amlodipine 10 mg and irbesartan 100 mg on blood pressure and cardiovascular risk factors in patients with hypertension

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    Yagi S

    2015-01-01

    Full Text Available Shusuke Yagi,1 Akira Takashima,1 Minoru Mitsugi,2 Toshihiro Wada,2 Junko Hotchi,1 Ken-ichi Aihara,3 Tomoya Hara,1 Masayoshi Ishida,1 Daiju Fukuda,4 Takayuki Ise,1 Koji Yamaguchi,1 Takeshi Tobiume,1 Takashi Iwase,1 Hirotsugu Yamada,1 Takeshi Soeki,1 Tetsuzo Wakatsuki,1 Michio Shimabukuro,4 Masashi Akaike,5 Masataka Sata11Department of Cardiovascular Medicine, Graduate School of Health Biosciences, University of Tokushima, Tokushima, 2Department of Internal Medicine, Shikoku Central Hospital, Shikokuchuo, 3Department of Medicine and Bioregulatory Sciences, 4Department of Cardio-Diabetes Medicine, 5Department of Medical Education, Graduate School of Health Biosciences, University of Tokushima, Tokushima, JapanBackground: Hypertension is one of the major risk factors for cardiovascular and cerebrovascular disease and mortality. Patients who receive insufficient doses of antihypertensive agents or who are poorly adherent to multidrug treatment regimens often fail to achieve adequate blood pressure (BP control. The aim of this study was to determine the efficacy of an angiotensin II receptor blocker (ARB and calcium channel blocker (CCB combination tablet containing a regular dose of irbesartan (100 mg and a high dose of amlodipine (10 mg with regard to lowering BP and other risk factors for cardiovascular disease.Methods: We retrospectively evaluated data from 68 patients with essential hypertension whose treatment regimen was changed either from combination treatment with an independent ARB and a low-dose or regular-dose CCB or from a combination tablet of ARB and a low-dose or regular-dose CCB to a combination tablet containing amlodipine 10 mg and irbesartan 100 mg, because of incomplete BP control. Previous treatments did not include irbesartan as the ARB.Results: The combination tablet decreased systolic and diastolic BP. In addition, it significantly decreased serum uric acid, low-density lipoprotein cholesterol, and increased high

  7. 78 FR 69856 - Determination That BANZEL (Rufinamide) Tablet, 100 Milligrams, Was Not Withdrawn From Sale for...

    Science.gov (United States)

    2013-11-21

    ...] Determination That BANZEL (Rufinamide) Tablet, 100 Milligrams, Was Not Withdrawn From Sale for Reasons of Safety... Drug Administration (FDA) has determined that BANZEL (rufinamide) tablet, 100 milligrams (mg), was not... abbreviated new drug applications (ANDAs) for rufinamide tablet, 100 mg, if all other legal and regulatory...

  8. Bioequivalence study of a new sildenafil 100 mg orodispersible film compared to the conventional film-coated 100 mg tablet administered to healthy male volunteers

    Directory of Open Access Journals (Sweden)

    Radicioni M

    2017-04-01

    Full Text Available Milko Radicioni,1 Chiara Castiglioni,1 Andrea Giori,2 Irma Cupone,3 Valeria Frangione,4 Stefano Rovati4 1CROSS Research S.A., Phase I Unit, Arzo, Switzerland; 2IBSA Farmaceutici Italia, Lodi, Italy; 3Bouty S.p.A., Strada Padana Superiore, Cassina De’ Pecchi, Italy; 4IBSA Institut Biochimique S.A., Pambio-Noranco, Switzerland Abstract: A new orodispersible film formulation of the phosphodiesterase type 5 inhibitor, sildenafil, has been developed to examine the advantages of an orally disintegrating film formulation and provide an alternative to the current marketed products for the treatment of erectile dysfunction. The pharmacokinetics of the sildenafil 100 mg orodispersible film (IBSA was compared to that of the conventional marketed 100 mg film-coated tablet (Viagra® after single-dose administration to 53 healthy male volunteers (aged 18–51 years in a randomized, open, two-way crossover bioequivalence study. Each subject received a single oral dose of 100 mg of sildenafil as test or reference formulation administered under fasting conditions at each of the two study periods according to a randomized crossover design. There was a washout interval of ≥7 days between the two administrations of the investigational medicinal products. Blood samples for pharmacokinetic analysis were collected up to 24 h post-dosing. The primary objective was to compare the rate (peak plasma concentration; Cmax and extent (area under the curve [AUC] from administration to last observed concentration time; AUC0–t of sildenafil absorption after single-dose administration of test and reference. Secondary endpoints were observed to describe the plasma pharmacokinetic profiles of sildenafil and its metabolite N-desmethyl-sildenafil relative bioavailability and safety profile after single-dose administration. The mean sildenafil and N-desmethyl-sildenafil plasma concentration–time profiles up to 24 h after single-dose administration of sildenafil 100 mg

  9. Preventive efficacy and safety of rebamipide in nonsteroidal anti-inflammatory drug-induced mucosal toxicity.

    Science.gov (United States)

    Kim, Jeong Ho; Park, Soo-Heon; Cho, Chul-Soo; Lee, Soo Teik; Yoo, Wan-Hee; Kim, Sung Kook; Kang, Young Mo; Rew, Jong Sun; Park, Yong-Wook; Lee, Soo Kon; Lee, Yong Chan; Park, Won; Lee, Don-Haeng

    2014-07-01

    The use of proton pump inhibitors or misoprostol is known to prevent the gastrointestinal complications of nonsteroidal anti-inflammatory drugs (NSAIDs). Rebamipide is known to increase the mucosal generation of prostaglandins and to eliminate free oxygen radicals, thus enhancing the protective function of the gastric mucosa. However, it is unknown whether rebamipide plays a role in preventing NSAID-induced gastropathy. The aim of this study was to determine the effectiveness of rebamipide compared to misoprostol in preventing NSAID-induced gastrointestinal complications in patients requiring continuous NSAID treatment. We studied 479 patients who required continuous NSAID treatment. The patients were randomly assigned to groups that received 100 mg of rebamipide three times per day or 200 μg of misoprostol three times per day for 12 weeks. The primary endpoint of the analysis was the occurrence rate of gastric ulcers, as determined by endoscopy after 12 weeks of therapy. Of the 479 patients in the study, 242 received rebamipide, and 237 received misoprostol. Ultimately, 44 patients (18.6%) withdrew from the misoprostol group and 25 patients (10.3%) withdrew from the rebamipide group. There was a significant difference in withdrawal rate between the two groups (p=0.0103). The per protocol analysis set was not valid because of the dropout rate of the misoprostol group; thus, the intention to treat (ITT) analysis set is the main set for the efficacy analysis in this study. After 12 weeks, the occurrence rate of gastric ulcers was similar in the rebamipide and misoprostol groups (20.3% vs 21.9%, p=0.6497) according to ITT analysis. In addition, the therapeutic failure rate was similar in the rebamipide and misoprostol groups (13.6% vs 13.1%, p=0.8580). The total severity score of the gastrointestinal symptoms was significantly lower in the rebamipide group than in the misoprostol group (p=0.0002). The amount of antacid used was significantly lower in the rebamipide

  10. Optimization of Forced Degradation Using Experimental Design and Development of a Stability-Indicating Liquid Chromatographic Assay Method for Rebamipide in Bulk and Tablet Dosage Form

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    Sandeep SONAWANE

    2016-09-01

    Full Text Available A novel stability-indicating RP-HPLC assay method was developed and validated for quantitative determination of rebamipide in bulk and tablet dosage form. Rebamipide (drug and drug product solutions were exposed to acid and alkali hydrolysis, thermal stress, oxidation by hydrogen peroxide and photodegradation. Experimental design has been used during forced degradation to determine significant factors responsible for degradation and to obtain optimal degradation conditions. In addition, acid and alkali hydrolysis was performed using a microwave oven. The chromatographic method employed the HiQ sil C-18HS (250 × 4.6 mm; 5 μm column with mobile phase consisting of 0.02 M potassium phosphate (pH adjusted to 6.8 and methanol (40:60, v/v and the detection was performed at 230 nm. The procedure was validated for specificity, linearity, accuracy, precision and robustness. There was no interference observed of excipients and degradation products in the determination of the active pharmaceutical ingredient. The method showed good accuracy and precision (intra and inter day and the response was linear in a range from 0.5 to 5 μg mL−1. The method was found to be simple and fast with less trial and error experimentation by making use of experimental design. Also, it proved that microwave energy can be used to expedite hydrolysis of rebamipide.

  11. Protection of cultured mammalian cells by rebamipide

    International Nuclear Information System (INIS)

    Antoku, Shigetoshi; Aramaki, Ryoji; Tanaka, Hisashi; Kusumoto, Naotoshi.

    1997-01-01

    Rebamipide which is used as a drug for gastritis and stomach ulcer has large capability for OH radical scavenging. It is expected that rebamipide has protective effect against ionizing radiations. The present paper deals with protective effect of rebamipide for cultured mammalian cells exposed to ionizing radiations. As rebamipide is insoluble in water, three solvents were used to dissolve. Rebamipide dissolved in dimethyl sulfoxide (DMSO), dimethyl formamide (DMFA) and 0.02 N NaOH was added to the cells in Eagle's minimum essential medium (MEM) supplemented with 10% fetal calf serum and the cells were irradiated with X-rays. After irradiation, the cells were trypsinized, plated in MEM with 10% fetal calf serum and incubated for 7 days in a CO 2 incubator to form colonies. Rebamipide dissolved in 0.02 N NaOH exhibited the protective effect expected its OH radical scavenging capability. However, the protective effect of rebamipide dissolved in DMSO was about half of that expected by its radical scavenging capability and that of rebamipide dissolved in DMFA was not observed. Uptake of rebamipide labeled with 14 C increased with increasing contact time with rebamipide. These rebamipide mainly distributed in nucleus rather than cytoplasm. (author)

  12. Protection of cultured mammalian cells by rebamipide

    Energy Technology Data Exchange (ETDEWEB)

    Antoku, Shigetoshi; Aramaki, Ryoji [Kyushu Univ., Fukuoka (Japan). Faculty of Medicine; Tanaka, Hisashi; Kusumoto, Naotoshi

    1997-06-01

    Rebamipide which is used as a drug for gastritis and stomach ulcer has large capability for OH radical scavenging. It is expected that rebamipide has protective effect against ionizing radiations. The present paper deals with protective effect of rebamipide for cultured mammalian cells exposed to ionizing radiations. As rebamipide is insoluble in water, three solvents were used to dissolve. Rebamipide dissolved in dimethyl sulfoxide (DMSO), dimethyl formamide (DMFA) and 0.02 N NaOH was added to the cells in Eagle`s minimum essential medium (MEM) supplemented with 10% fetal calf serum and the cells were irradiated with X-rays. After irradiation, the cells were trypsinized, plated in MEM with 10% fetal calf serum and incubated for 7 days in a CO{sub 2} incubator to form colonies. Rebamipide dissolved in 0.02 N NaOH exhibited the protective effect expected its OH radical scavenging capability. However, the protective effect of rebamipide dissolved in DMSO was about half of that expected by its radical scavenging capability and that of rebamipide dissolved in DMFA was not observed. Uptake of rebamipide labeled with {sup 14}C increased with increasing contact time with rebamipide. These rebamipide mainly distributed in nucleus rather than cytoplasm. (author)

  13. Bioavailability of everolimus administered as a single 5 mg tablet versus five 1 mg tablets: a randomized, open-label, two-way crossover study of healthy volunteers.

    Science.gov (United States)

    Thudium, Karen; Gallo, Jorge; Bouillaud, Emmanuel; Sachs, Carolin; Eddy, Simantini; Cheung, Wing

    2015-01-01

    The mammalian target of rapamycin (mTOR) inhibitor everolimus has a well-established pharmacokinetics profile. We conducted a randomized, single-center, open-label, two-sequence, two-period crossover study of healthy volunteers to assess the relative bioavailability of everolimus administered as one 5 mg tablet or five 1 mg tablets. Subjects were randomized 1:1 to receive everolimus dosed as one 5 mg tablet or as five 1 mg tablets on day 1, followed by a washout period on days 8-14 and then the opposite formulation on day 15. Blood sampling for pharmacokinetic evaluation was performed at prespecified time points, with 17 samples taken for each treatment period. Primary variables for evaluation of relative bioavailability were area under the concentration-time curve from time zero to infinity (AUCinf) and maximum blood concentration (Cmax). Safety was assessed by reporting the incidence of adverse events (AEs). Twenty-two participants received everolimus as one 5 mg tablet followed by five 1 mg tablets (n=11) or the opposite sequence (n=11). The Cmax of five 1 mg tablets was 48% higher than that of one 5 mg tablet (geometric mean ratio, 1.48; 90% confidence interval [CI], 1.35-1.62). AUCinf was similar (geometric mean ratio, 1.08; 90% CI, 1.02-1.16), as were the extent of absorption and the distribution and elimination kinetics. AEs, all grade 1 or 2, were observed in 54.5% of subjects. Although the extent of absorption was similar, the Cmax of five 1 mg tablets was higher than that of one 5 mg tablet, suggesting these formulations lead to different peak blood concentrations and are not interchangeable at the dose tested.

  14. Using a single tablet daily to treat latent tuberculosis infection in Brazil: bioequivalence of two different isoniazid formulations (300 mg and 100 mg) demonstrated by a sensitive and rapid high-performance liquid chromatography-tandem mass spectrometry method in a randomised, crossover study.

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    Daher, André; Pitta, Luciana; Santos, Tereza; Barreira, Draurio; Pinto, Douglas

    2015-06-01

    The recommended treatment for latent tuberculosis (TB) infection in adults is a daily dose of isoniazid (INH) 300 mg for six months. In Brazil, INH was formulated as 100 mg tablets. The treatment duration and the high pill burden compromised patient adherence to the treatment. The Brazilian National Programme for Tuberculosis requested a new 300 mg INH formulation. The aim of our study was to compare the bioavailability of the new INH 300 mg formulation and three 100 mg tablets of the reference formulation. We conducted a randomised, single dose, open label, two-phase crossover bioequivalence study in 28 healthy human volunteers. The 90% confidence interval for the INH maximum concentration of drug observed in plasma and area under the plasma concentration vs. time curve from time zero to the last measurable concentration "time t" was 89.61-115.92 and 94.82-119.44, respectively. The main limitation of our study was that neither adherence nor the safety profile of multiple doses was evaluated. To determine the level of INH in human plasma, we developed and validated a sensitive, simple and rapid high-performance liquid chromatography-tandem mass spectrometry method. Our results showed that the new formulation was bioequivalent to the 100 mg reference product. This finding supports the use of a single 300 mg tablet daily strategy to treat latent TB. This new formulation may increase patients' adherence to the treatment and quality of life.

  15. Using a single tablet daily to treat latent tuberculosis infection in Brazil: bioequivalence of two different isoniazid formulations (300 mg and 100 mg demonstrated by a sensitive and rapid high-performance liquid chromatography-tandem mass spectrometry method in a randomised, crossover study

    Directory of Open Access Journals (Sweden)

    André Daher

    2015-06-01

    Full Text Available The recommended treatment for latent tuberculosis (TB infection in adults is a daily dose of isoniazid (INH 300 mg for six months. In Brazil, INH was formulated as 100 mg tablets. The treatment duration and the high pill burden compromised patient adherence to the treatment. The Brazilian National Programme for Tuberculosis requested a new 300 mg INH formulation. The aim of our study was to compare the bioavailability of the new INH 300 mg formulation and three 100 mg tablets of the reference formulation. We conducted a randomised, single dose, open label, two-phase crossover bioequivalence study in 28 healthy human volunteers. The 90% confidence interval for the INH maximum concentration of drug observed in plasma and area under the plasma concentration vs. time curve from time zero to the last measurable concentration “time t” was 89.61-115.92 and 94.82-119.44, respectively. The main limitation of our study was that neither adherence nor the safety profile of multiple doses was evaluated. To determine the level of INH in human plasma, we developed and validated a sensitive, simple and rapid high-performance liquid chromatography-tandem mass spectrometry method. Our results showed that the new formulation was bioequivalent to the 100 mg reference product. This finding supports the use of a single 300 mg tablet daily strategy to treat latent TB. This new formulation may increase patients’ adherence to the treatment and quality of life.

  16. Anti-inflammatory effects of rebamipide according to Helicobacter pylori status in patients with chronic erosive gastritis: a randomized sucralfate-controlled multicenter trial in China-STARS study.

    Science.gov (United States)

    Du, Yiqi; Li, Zhaoshen; Zhan, Xianbao; Chen, Jie; Gao, Jun; Gong, Yanfang; Ren, Jianlin; He, Liping; Zhang, Zhijian; Guo, Xiaozhong; Wu, Jianshen; Tian, Zibin; Shi, Ruihua; Jiang, Bo; Fang, Dianchun; Li, Youming

    2008-11-01

    The aim of the study was to investigate the effects of rebamipide on symptom, histology, endogenous prostaglandin, and mucosal oxygen free radicals in chronic erosive gastritis (CEG) patients by using sucralfate as a control. The trial also examined whether Helicobacter pylori infection would affect rebamipide-induced protection. A total of 453 endoscopy-confirmed CEG patients from 11 hospitals in China were enrolled in the study. They randomly received either rebamipide (100 mg t.i.d) or sucralfate (1.0 t.i.d) for 8 weeks with a ratio of 3:1. Per-protocol analysis (n = 415) showed the accumulated symptom score in the rebamipide group dropped from 5.54 +/- 0.97 to 0.80 +/- 0.47 after 8 weeks (P < 0.001 versus control). The endoscopic inflammation score in rebamipide group also decreased from 2.65 +/- 0.09 to 0.60 +/- 0.10, which showed better effects than sucralfate. It was shown a significant improvement (P < 0.01) in prostaglandin E2 (PGE(2)) contents in rebamipide-treated subjects mucosa (225.4 +/- 18.3 pg/g versus 266.7 +/- 14.7 pg/g) compared with that in sucralfate group after 8 weeks of treatment. Malondialdehyde (MDA) contents were significantly depressed both in the trial and control group. When Helicobacter pylori infection was considered, no statistically difference was found in the effect of rebamipide on either symptom or inflammation scores. In conclusion, Rebamipide demonstrated a stronger suppressive effect on the mucosal inflammation in chronic erosive gastritis than sucralfate. The gastroprotection induced by rebamipide is not influenced by H. pylori infection, which indicates its usage in the treatment of H. pylori-associated CEG.

  17. Additive Effects of Rebamipide Plus Proton Pump Inhibitors on the Expression of Tight Junction Proteins in a Rat Model of Gastro-Esophageal Reflux Disease.

    Science.gov (United States)

    Gweon, Tae-Geun; Park, Jong-Hyung; Kim, Byung-Wook; Choi, Yang Kyu; Kim, Joon Sung; Park, Sung Min; Kim, Chang Whan; Kim, Hyung-Gil; Chung, Jun-Won

    2018-01-15

    The aim of this study was to investigate the effects of rebamipide on tight junction proteins in the esophageal mucosa in a rat model of gastroesophageal reflux disease (GERD). GERD was created in rats by tying the proximal stomach. The rats were divided into a control group, a proton pump inhibitor (PPI) group, and a PPI plus rebamipide (PPI+R) group. Pantoprazole (5 mg/kg) was administered intraperitoneally to the PPI and PPI+R groups. An additional dose of rebamipide (100 mg/kg) was administered orally to the PPI+R group. Mucosal erosions, epithelial thickness, and leukocyte infiltration into the esophageal mucosa were measured in isolated esophagi 14 days after the procedure. A Western blot analysis was conducted to measure the expression of claudin-1, -3, and -4. The mean surface area of mucosal erosions, epithelial thickness, and leukocyte infiltration were lower in the PPI group and the PPI+R group than in the control group. Western blot analysis revealed that the expression of claudin-3 and -4 was significantly higher in the PPI+R group than in the control group. Rebamipide may exert an additive effect in combination with PPI to modify the tight junction proteins of the esophageal mucosa in a rat model of GERD. This treatment might be associated with the relief of GERD symptoms.

  18. COMPARISON OF HYDROCORTISONE 10 MG TABLETS: TABLET HARDNESS OPTIMISED FOR ADULT USE HAS NEGATIVE CONSEQUENCES FOR PAEDIATRIC USE.

    Science.gov (United States)

    Saimbi, Sarina; Madden, Valerie; Stirling, Heather; Yahyouche, Asma; Batchelor, Hannah

    2016-09-01

    Children's medicines are not always readily available as an age appropriate product and manipulation of adult products is often required. Recently the commercial manufacturing process for 10 mg hydrocortisone tablets has changed and the compression force increased due to tablets fracturing on removal from the blister pack. However, this change led to parents of children requiring hydrocortisone reporting that the tablets were more difficult to manipulate.This study evaluated 10 mg hydrocortisone tablets for their suitability for manipulation in order to deliver an appropriate dose to children (2 mg dose). The physical properties of tablets with the old and new compression force were compared as well as the accuracy of obtaining the paediatric dose. The tablets compared were hydrocortisone Auden 10 mg tablets (Brand A, PL16876/002)-these are the newer, harder tablets- and hydrocortisone 10 mg tablets (Brand B, PL17507/0097). Tablet physical properties including friability (Copley FRV200) and tablet hardness (Copley TBF1000) were compared. The accuracy of split doses (halve and quarter tablets) were recorded on a Sartorius analytical balance. The accuracy of the 2 mg paediatric dosing was assessed by crushing the tablet, adding 10 mL of water and extracting 2 mL. The concentration was measured using UV analysis (Jenway Genova Plus) according to a calibration curve (wavelength=246 nm). Two devices were used to crush the tablets: a spoon onto a plate and a commercially available crushing device (Apothecary Ezy Crush Pill Crusher With Ergo Grip). As anticipated Brand A tablets were harder (51.85 ±5.1 N) compared to Brand B (30.99±4.1 N). Brand A tablets passed the friability testing with Auden tablets which are known to be harder tablets and therefore more force is required to crush these. Some of the experimental work within this project was conducted by Andrew Hackett and Kameron Paul-Thaper whilst at the University of Birmingham on work

  19. Rebamipide delivered by brushite cement enhances osteoblast and macrophage proliferation.

    Directory of Open Access Journals (Sweden)

    Michael Pujari-Palmer

    Full Text Available Many of the bioactive agents capable of stimulating osseous regeneration, such as bone morphogenetic protein-2 (BMP-2 or prostaglandin E2 (PGE2, are limited by rapid degradation, a short bioactive half-life at the target site in vivo, or are prohibitively expensive to obtain in large quantities. Rebamipide, an amino acid modified hydroxylquinoline, can alter the expression of key mediators of bone anabolism, cyclo-oxygenase 2 (COX-2, BMP-2 and vascular endothelial growth factor (VEGF, in diverse cell types such as mucosal and endothelial cells or chondrocytes. The present study investigates whether Rebamipide enhances proliferation and differentiation of osteoblasts when delivered from brushite cement. The reactive oxygen species (ROS quenching ability of Rebampide was tested in macrophages as a measure of bioactivity following drug release incubation times, up to 14 days. Rebamipide release from brushite occurs via non-fickian diffusion, with a rapid linear release of 9.70% ± 0.37% of drug per day for the first 5 days, and an average of 0.5%-1% per day thereafter for 30 days. Rebamipide slows the initial and final cement setting time by up to 3 and 1 minute, respectively, but does not significantly reduce the mechanical strength below 4% (weight percentage. Pre-osteoblast proliferation increases by 24% upon exposure to 0.4 uM Rebamipide, and by up to 73% when Rebamipide is delivered via brushite cement. Low doses of Rebamipide do not adversely affect peak alkaline phosphatase activity in differentiating pre-osteoblasts. Rebamipide weakly stimulates proliferation in macrophages at low concentrations (118 ± 7.4% at 1 uM, and quenches ROS by 40-60%. This is the first investigation of Rebamipide in osteoblasts.

  20. Notes from the field: national shortage of isoniazid 300 mg tablets.

    Science.gov (United States)

    2012-12-21

    On November 16, 2012, the Illinois State tuberculosis (TB) program notified CDC's Division of Tuberculosis Elimination of a national shortage of 300 mg tablets of the antituberculosis medication isoniazid (INH). Subsequently, other state TB programs (e.g., California, Indiana, Maryland, New York, Virginia, and Wisconsin) reported difficulty obtaining INH 300 mg tablets. Other programs (e.g., San Diego) have experienced difficulties obtaining at least one of the commercially available anti-TB preparations containing the combination of rifampin and INH (IsonaRif [VersaPharm]).

  1. Efficacy and Safety of Rebamipide in Prevention of NSAID-Gastropathy

    Directory of Open Access Journals (Sweden)

    Serhiy Tkach

    2017-03-01

    Full Text Available Background: Nonsteroidal anti-inflammatory drugs (NSAID are one of the most widely used drugs in medical practice. However, all medical benefits of NSAID are paid for by increased risk of developing numerous side effects. One of the most clinically significant side effects is a NSAID-induced gastrointestinal lesion that develops in, on average, 30% of NSAID users, even with the absence of ulceration; NSAID-induced ulcers and bleeding cause 61% of deaths related to side effects of these medicines. The main aim of this study was to compare the incidence of erosive and ulcerative lesions of the gastroduodenal zone as a result of patients receiving diclofenac on the background of concomitant prophylactic use of proton pump inhibitor (PPI omeprazole or rebamipide. Materials and Methods: To achieve this goal we have conducted a randomized comparative study, which included 118 patients aged from 25 to 65 years (mean age, 45±18 years with osteoarthritis (94 patients and rheumatoid arthritis (24 patients, who had taken a once-daily dose of 100mg diclofenac (Dikloberl over 1 month. Depending on the treatment, all patients were randomized into 3 groups by using the computer method of random numbers. Within 1 month, patients of Group 1 (n=42 received additionally a once-daily dose of 20mg omeprazole (Omez, and patients of Group 2 (n=46 - rebamipide at a dose of 100mg three times a day. Patients of Group 3 (n=30 received only diclofenac. The primary endpoint was the cumulative incidence of development of erosions and ulcers in the gastroduodenal zone, which was determined after the treatment according to data from the endoscopy. The secondary endpoint was the incidence of development of dyspeptic symptoms and side effects. Results: During 1 month of continuous reception of diclofenac, peptic ulcers of stomach and duodenum were found in 2/4.8% and 2/4.8% patients of Group 1 and in 3/6.5% and 2/4.3% patients of Group 2, respectively. In the control group

  2. Study of the 50 mg Propylthiouracil tablets stability

    International Nuclear Information System (INIS)

    Valdes Bendoyro, Maria Olga; Garcia Penna, Caridad Margarita; Lugones Fernandez, Juan

    2010-01-01

    Authors developed a stability study of 50 mg Propylthiouracil tablets and determination of its expiry date. This study was conducted by fixed life methods and of accelerated stability by high-performance liquid chromatography, validated in Drugs Research and Development Center. Fixed life study was conducted during 24 months at room temperature; whereas the accelerated stability study was conducted exposing the product to light influence, humidity and temperature; during 3 months a analysis was performed for the two first ones and over 6 months in the case of temperature study. Propylthiouracil formula (50 mg tablets) fulfilled the quality specifications described in Pharmacopeia. Results of stability study by fixed life after 24 months showed that thr product maintain the parameter determining its quality during this period, and in the accelerated studies there was not a significant degradation of product. Two years was the expity date established in above mentioned conditions

  3. Resolution of persistent corneal erosion after administration of topical rebamipide

    Directory of Open Access Journals (Sweden)

    Kashima T

    2012-08-01

    Full Text Available Tomoyuki Kashima,1,2 Hideo Akiyama,1 Fumihide Miura,2 Shoji Kishi11Department of Ophthalmology, Gunma University School of Medicine, Maebashi, Japan; 2Department of Ophthalmology, Saku Central Hospital, Saku, JapanAbstract: Rebamipide is an antiulcer agent used to treat gastric ulcer and gastritis. Biological effects of rebamipide include cytoprotection, wound healing, and anti-inflammatory properties that are known to be universal for a variety of tissues in addition to gastrointestinal mucosa. The therapeutic effects of rebamipide eye drops are due to its ability to increase corneal and conjunctival mucin-like substances and improve corneal and conjunctival injury in vivo. In this paper, we report a case of Sjögren's syndrome with complete disappearance of corneal erosion after administration of rebamipide eye drops. This was observed even though corneal erosion had not improved for 6 months after punctal occlusion surgery. The patient was a 33-year-old female, diagnosed with Sjögren's syndrome by a salivary gland biopsy. The corneal and conjunctival surfaces were filled with dense erosions, which did not improve with topical drugs. Punctal plugs were applied several times; however, the plugs were repeatedly shed. All four puncta of both eyelids were surgically occluded, and both corneal and conjunctival erosion was clearly improved. However, the erosion in the inferior cornea of both eyes had not improved for 6 months after surgery. We used the newly approved topical rebamipide for treatment of this patient. The corneal erosion gradually improved and completely disappeared 4 weeks after administration of the drug. Dry eye sensation disappeared at the same time. Both membrane-associated mucin and secreted mucin in the ocular surface are thought to be essential for maintenance of the tear film. Induction of mucin from ocular surface epithelium could be an effective treatment in cases of dry eye caused by mucin deficiency. Through its various

  4. Specifications development for "Karbatril" codenamed tablets

    Directory of Open Access Journals (Sweden)

    L. I. Kucherenko

    2017-08-01

    Full Text Available Introduction. According to current legislation of Ukraine the specifications of tablets include the following indicators: description, identification, average weight, disintegration and assay. The aim of the study. The development of specifications and project of quality control methods for "Karbatril" codenamed tablets. Materials and methods. During the study we analyzed 6 series of tablets "Karbatril." For the description, identification, determination of the average mass, disintegration, active ingredients quantify of "Karbatril" codenamed tablets we used appropriate methods and instruments. Results and discussion. Tablets "Karbatril" were analyzed for the following parameters: - Overview - Tablets white or nearly white; - Average weight - during the study the average weight of 6 series of obtained tablets ranged from 339,0 mg to 369,9 mg according to SPU from 337,0 mg to 373,0 mg; - Disintegration – according to SPU the disintegration for tablet without shell shall not exceed 15 min. Analyzed tablets disintegrated in the period from 5 to 10 minutes; - Identification and quantification of the active ingredients of tablets were conducted using modified HPLC methods. During the identification obtained chromatograms show compliance with SPU. In quantitative determination of the active ingredients content in "Karbatril" codenamed tablets we found carbamazepine from 148.18 mg to 150.19 mg, thiotriazoline - from 98.93 mg to 99.71 mg. This data is consistent to SPU which regulates content of carbamazepine - 150 mg ± 7,5%, thiotriazoline - 100 mg ± 10%. Conclusions. This study has developed specification for "Karbatril" codenamed tablets and also methods of HPLC qualitative and quantitative determination of active ingredients. In the specification the following parameters are included: description, identification, average weight, disintegration and assay. The study drafted quality control methods which are planned to be later offered to the

  5. 21 CFR 520.1720a - Phenylbutazone tablets and boluses.

    Science.gov (United States)

    2010-04-01

    ... Section 520.1720a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES...-mg or 1-g tablets, or 2- or 4-g boluses, in dogs and horses. (2) Nos. 000010 and 059130 for use of 100- or 200-mg or 1-g tablets in dogs and horses. (3) Nos. 000856 and 061623 for use of 100-mg or 1-g...

  6. An Evaluation of Theraphy with Fluconazole 150 mg Tablets Compared to Fluconazole 150 mg Tablets Plus Dermoxen Lenitiva Cream in The Time to Reduce Simptomatology in Women with Vulvovaginal Candidiasis

    Directory of Open Access Journals (Sweden)

    Davide Carati

    2014-06-01

    Full Text Available Aim of the study. Authors investigated first of all the time to onset of first relief of symptoms. Secondary measures included the time to overall relief of symptoms and the reoccurrence rate over the first 45 days after the first visit. Methods. A randomized, open-label, parallel study evaluated 47 women with moderate to severe symptoms of Vulvo Vaginal Candidiasis (VVC. Patients were divided into two groups of treatment: group 1 followed a therapy with Fluconazole 150 mg tablets, while group 2 had a therapy based on Fluconazole 150 mg tablets coadjuvated by Dermoxen Lenitiva cream. Results. The time at which 50% of patients experienced first relief of symptoms was 24.6 hours for Group 1, while for Group 2 it was 12.4 hours (P<0.05. There were significant differences between the two groups in respect to the time of first relief of symptoms and reoccurrence of infection within 45 days of treatment. Conclusions. Combined treatment with Fluconazole 150 mg tablets and by Dermoxen Lenitiva cream provides statistically significant improvement in the time of first relief of symptoms, complete relief of symptoms and relapse time in the treatment of VVC compared to fluconazole 150 mg tablets only.

  7. Topical rebamipide improves the ocular surface in mild lagophthalmos

    Directory of Open Access Journals (Sweden)

    Itakura M

    2013-07-01

    Full Text Available Mariko Itakura,1 Hirotaka Itakura,1,2 Tomoyuki Kashima,2 Hideo Akiyama,2 Shoji Kishi21Department of Ophthalmology, Maebashi Red Cross Hospital, Maebashi, Japan; 2Department of Ophthalmology, Gunma University, School of Medicine, Maebashi, JapanAbstract: Administration of topical rebamipide improves the ocular surface in dry eye. We consecutively studied seven eyes in seven cases (three males and four females with mild lagophthalmos (three cases after eyelid surgery, two cases of incomplete facial nerve palsy, and two cases of senile ectropion during the treatment of corneal disorders with rebamipide eye drops four times daily for 2 weeks. The fluorescein corneal staining (FCS score, tear film break-up time (TBUT, Schirmer's test, and decimal visual acuity were examined. Ocular symptoms were examined and scored by questioning each patient before and after administration of the drug. In all seven eyes, inferior corneal erosion decreased or disappeared within 2 weeks after administration of topical rebamipide. The FCS score was significantly improved (P < 0.05. The TBUT was significantly extended from 2.9 ± 0.5 seconds to 5.2 ± 0.4 seconds (P < 0.05. The scores of ocular symptoms, such as eye pain, dryness, blurred vision, and foreign body sensations, were significantly improved (P < 0.05.Topical rebamipide was effective for corneal disorders in mild lagophthalmos. This drug may provide a novel approach to treat lagophthalmos.Keywords: dry eye, ectropion, eyelid surgery, facial nerve palsy, lagophthalmos, rebamipide

  8. Preparation of venlafaxine hydrochloride sustained-release tablets

    Directory of Open Access Journals (Sweden)

    GUO Lingling

    2013-08-01

    Full Text Available To prepare venlafxine hydrochloride sustained-release tablets.Hydroxypropylmethyl cellulose(HPMC and methyl cellulose(MC were used as main materials to prepare sustained-release tablets of velafaxine hydrochloride and the influence of important factors on in vitro release curves of venlafaxine hydrochloride sustained-release tablets was investigated.Results:The optimal prescription included 100 mg HPMC,25 mg MC,and 2.5% glidant in one tablet prepared with 30kN.The tablets were prepared with the method of wet granulation by NO.16 mesh sieve.The tablets exhibited good sustained-release property in phosphate buffered solution (pH=6.8.The as-prepared venlafxine hydrochloride sustained-release tablets have good sustained-release property.

  9. Pharmacokinetic comparison using two tablets of an evogliptin/metformin XR 2.5/500 mg fixed dose combination vs. 1 tablet each of evogliptin 5 mg and metformin XR 1,000 mg
.

    Science.gov (United States)

    Yoon, Sumin; Rhee, Su-Jin; Park, Sang-In; Yoon, Seo Hyun; Cho, Joo-Youn; Jang, In-Jin; Lee, SeungHwan; Yu, Kyung-Sang

    2017-06-01

    The aim of this study was to compare the pharmacokinetic (PK) characteristics of evogliptin and metformin following the administration of 2 evogliptin/metformin extended-release (XR) 2.5/500 mg FDC tablets with the coadministration of separate evogliptin 5-mg and metformin XR 1,000-mg tablets (separate formulations). A randomized, two-period, two-sequence crossover study was conducted. Subjects were randomly assigned to receive 2 FDC tablets or the individual tablets, followed by a 14-day washout period and the administration of the alternate treatment. Blood samples were collected predose and up to 72 hours postdose for each period. PK parameters including Cmax and AUClast were calculated. The geometric mean ratios (GMRs) and the 90% confidence intervals (CIs) between FDC and the separate formulations were calculated for the Cmax and AUClast of evogliptin and metformin. 33 subjects completed the study. The GMR (90% CI) values of Cmax and AUClast for evogliptin were 1.011 (0.959 - 1.066) and 1.010 (0.977 - 1.043), respectively. The GMR (90% CI) values of Cmax and AUClast for metformin were 0.892 (0.827 - 0.963) and 0.893 (0.841 - 0.947), respectively. There was no significant difference between the FDC and separate formulations regarding the occurrence of adverse events. All drug-related adverse events were considered to be mild and resolved without any treatment. Two FDC tablets of evogliptin/metformin XR 2.5/500 mg showed a similar PK profile to the separate formulations of evogliptin 5 mg and metformin XR 1,000 mg. All of the 90% CIs of GMR satisfied the regulatory bioequivalence criteria of 0.800 - 1.250.
.

  10. Stability of a formulation of zidovudine 300 mg tablets

    International Nuclear Information System (INIS)

    Ibannez Calvo, Sergio; Garcia Penna, Caridad Margarita; Leon Rodriguez, Rafael

    2010-01-01

    Authors developed a validation of analytical method by high-performance liquid applicable to stability study of Zidovudine (300 mg tablets). The validated analytical method was linear, specific and exact. Above mentioned study was developed determing its expiry date. This study was conducted by fixed life and of accelerated stability methods by high-performance liquid chromatography, validated in Drugs Research and Development Center (Havana, Cuba). Fixed life study was conducted during 24 months at room temperature whereas the accelerated stability study was conducted exposing the product to light influence and humidity during three months and to temperature during 6 months. Zidovudine formula (300 mg tablets) fulfilled the quality specifications described in Pharmacopeia. After 24 months results of stability study by fixed life showed that product maintained the parameters determining its quality during that period and in accelerated studies there was not a significant degradation of product. Two years was established as expiry date in above mentioned conditions

  11. Formulation development and optimization of Lamivudine 300 mg and Tenofovir Disoproxil Fumarate (TDF 300 mg FDC tablets by D-optimal mixture design

    Directory of Open Access Journals (Sweden)

    Prosper Tibalinda

    2016-12-01

    Full Text Available The usage of fixed dose combination (FDC tablets of Lamivudine and Tenofovir Disoproxil Fumarate (TDF is increasing due to increased incidences of HIV/Hepatitis B and HIV/TB co-infections. This is likely to increase the financial crisis due to limited resources for funding procurement of ready-made products from the pharmaceuticals manufacturing leading countries. Therefore, production of local oral tablets containing Lamivudine and TDF FDC is inevitable. Lamivudine 300 mg/TDF 300 mg tablets were developed and optimized by D-optimal mixture design and produced by direct compression technique. Twenty trial formulations with independent variables, including PVP-CL 1–12.00%, PVP-K30 1–10.00%, starch-1500 2.5–12.5% and Avicel-PH102 2–19.25% were prepared by direct compression technique. The formulations were assessed on assay, dissolution, friability, weight variation and disintegration time. It was found that assay ranged from 98.13–101.95% for Lamivudine, 98.25–102.84 for TDF, both were within the in-house assay specification of 95 to 105%. Dissolution at single point was above 80% for Lamivudine 93.96–100.55% and 95.85–103.15% for TDF, disintegration time was between 1.92–66.33 min and friability 0.06–12.56%. Out of twenty formulation trials, eight formulations had all parameters in proven acceptable range. On optimization, one formulation with independent variables, PVP-CL 5.67%, PVP-K30 1.00%, Starch-1500 5.76% was selected. The optimized formulation was comparable to the reference product on the market with similarity factor (f2 and difference factor (f1 within the acceptable range for both Lamivudine and TDF.

  12. REBAMIPIDE: EFFECTIVE DRUG PREVENTION OF NSAID ENTEROPATHY IS POSSIBLE

    Directory of Open Access Journals (Sweden)

    E. V. Moroz

    2016-01-01

    Full Text Available Prevention of gastrointestinal tract (GIT complications is the most important element for the rational use of nonsteroidal anti-inflammatory drugs (NSAIDs and low-dose aspirin (LDA. Proton pump inhibitors (PPIs have long been the only medication to prevent these complications. However, PPIs are only effective in preventing and treating upper GIT diseases (NSAID gastropathy rather than small intestinal injury (NSAID enteropathy. Rebamipide has emerged as a novel agent to protect the gastrointestinal mucosa today. The effect of the drug differs from that of PPIs: it is a typical gastroand enteroprotector that enhances the synthesis of endogenous prostaglandins and possesses a significant anti-inflammatory potential. Rebamipide has long been widely used by doctors inJapan,South Korea, andChinaas an effective and safe agent for the treatment of many diseases of the digestive system. There is a strong evidence base for the efficacy of rebamipide in preventing and treating NSAID gastropathy and NSAID enteropathy (including LDA-induced injuries. Controlled studies have found that the drug is not inferior to the classic gastroprotective agent misoprostol, significantly outperforming the latter in its tolerability. This review describes the mechanism of action of rebamipide and main clinical trials of its therapeutic effect in NSAID gastropathy and NSAID enteropathy. 

  13. Rebamipide inhibits gastric cancer growth by targeting survivin and Aurora-B

    International Nuclear Information System (INIS)

    Tarnawski, A.; Pai, R.; Chiou, S.-K.; Chai, J.; Chu, E.C.

    2005-01-01

    Rebamipide accelerates healing of gastric ulcers and gastritis but its actions on gastric cancer are not known. Survivin, an anti-apoptosis protein, is overexpressed in stem, progenitor, and cancer cells. In gastric cancer, increased and sustained survivin expression provides survival advantage and facilitates tumor progression and resistance to anti-cancer drugs. Aurora-B kinase is essential for chromosome alignment and mitosis progression but surprisingly its role in gastric cancer has not been explored. We examined in human gastric cancer AGS cells: (1) survivin expression, (2) localization of survivin and Aurora-B (3) cell proliferation, and (4) effects of specific survivin siRNA and/or rebamipide (free radical scavenging drug) on survivin and Aurora-B expression and cell proliferation. Survivin and Aurora-B are strongly expressed in human AGS gastric cancer cells and co-localize during mitosis. Survivin siRNA significantly reduces AGS cell viability. Rebamipide significantly downregulates in AGS cell survivin expression, its association with Aurora-B and cell proliferation. Rebamipide-induced downregulation of survivin is at the transcription level and does not involve ubiquitin-proteasome pathway

  14. Effectiveness and relevant factors of 2% rebamipide ophthalmic suspension treatment in dry eye.

    Science.gov (United States)

    Ueda, Kaori; Matsumiya, Wataru; Otsuka, Keiko; Maeda, Yoshifumi; Nagai, Takayuki; Nakamura, Makoto

    2015-06-06

    Rebamipide with mucin secretagogue activity was recently approved for the treatment of dry eye. The efficacy and safety in the treatment of rebamipide were shown in two pivotal clinical trials. It was the aim of this study to evaluate the effect of 2% rebamipide ophthalmic suspension in patients with dry eye and analyze relevant factors for favorable effects of rebamipide in clinical practice. This was a retrospective cohort study of 48 eyes from 24 patients with dry eye treated with 2% rebamipide ophthalmic suspension. Dry eye-related symptom score, tear film break-up time (TBUT), fluorescein ocular surface staining score (FOS) and the Schirmer test were used to collect the data from patients at baseline, and at 2, 4, 8, and 12 week visits. To determine the relevant factors, multiple regression analyses were then performed. Mean dry eye-related symptom score showed a significant improvement from the baseline (14.5 points) at 2, 4, 8 and 12 weeks (9.80, 7.04, 7.04 and 7.83 points, corrected P value treatment. For ocular symptoms, three parameters (foreign body sensation, dry eye sensation and ocular discomfort) showed significant improvements at all visits. The multiple regression analyses showed that the fluorescein conjunctiva staining score was significantly correlated with the changes of dry eye-related symptom score at 12 weeks (P value = 0.017) and dry eye-related symptom score was significantly correlated with independent variables for the changes of FOS at 12 weeks (P value = 0.0097). Two percent rebamipide ophthalmic suspension was an effective therapy for dry eye patients. Moreover the fluorescein conjunctiva staining score and dry eye-related symptom score might be good relevant factors for favorable effects of rebamipide.

  15. Effect of binders on 500mg metformin hydrochloride tablets produced by wet granulation

    Directory of Open Access Journals (Sweden)

    LUCIANA CATIA BLOCK

    2009-12-01

    Full Text Available Metformin hydrochloride (MH is an oral hypoglycemic agent and a high-dose drug that has poor flow and compression properties. In this study, the feasibility of developing adequate, low cost 500mg tablets of metformin hydrochloride by wet granulation was tested with several binders (Starch / PVP K30®; Starch 1500® /PVP K30®, PVP K30® and PVP K90® in a simple tablet press of the type used in small pharmaceutical laboratories. The drug powder was tested for ability to flow, by determining Carr’s Index (CI and the Hausner ratio (HR. Differential scanning calorimetry and thermogravimetric analysis were carried out on isolated MH and 1:1 (w/w binary mixtures with the excipients. The size distribution, friability, flow properties and drug content of the granules were analyzed, as were the hardness, friability, disintegration, dissolution and uniformity of the dosage form. The drug powder showed CI > 22% and HR > 1.25, characteristic of a poor flow powder, and no significant incompatibilities with the excipients. All the granules showed adequate flow properties and were suitable for pressing into tablets, all of which complied with pharmacopeial specifications. The starch /PVP K30® and starch 1500® /PVP K30® mixtures were best for producing 500 mg MH tablets. Keywords: Metformin hydrochloride. Tablets. Wet granulation. Binders.

  16. Preventive Effect of Rebamipide Gargle on Chemoradiotherpy-Induced Oral Mucositis in Patients with Oral Cancer: a Pilot Study

    Directory of Open Access Journals (Sweden)

    Takashi Yasuda

    2011-11-01

    Full Text Available Objectives: To assess the efficacy and safety of rebamipide in preventing chemoradiotherapy-induced oral mucositis in patients with oral cancer.Material and Methods: Patients with oral cancer treated with chemoradiotherapy (daily radiotherapy plus docetaxel hydrate once a week were enrolled for this study. They were assigned in a double-blind fashion to receive either rebamipide gargle or placebo on the days of chemoradiotherapy. Oral mucositis was assessed using the WHO grading system. The primary endpoint of this study was the incidence of grade 3 - 4 mucositis after exposure to 40 Gy radiation (4 weeks. The secondary endpoint was the effect of rebamipide gargle on tumour response to chemoradiotherapy.Results: Twenty-four patients were randomly assigned to receive rebamipide gargle (n = 12 or placebo-gargle (n = 12 during chemoradiotherapy. The number of patients with severe mucositis (WHO ≥ 3 was higher in the placebo group than in the rebamipide group (83.3% vs. 33.3%, P = 0.036. In addition, no effect of rebamipide gargle on tumour response to chemoradiotherapy was recognized compared with the placebo group.Conclusions: For patients with oral cancer undergoing chemoradiotherapy, rebamipide gargle may contribute to decrease the severity of oral mucositis.

  17. A pilot study of rebamipide-gargle for chemoradiotherapy-induced mucositis in oral cancer patients

    International Nuclear Information System (INIS)

    Yasuda, Takashi; Chiba, Hiroshige; Satomi, Takafumi; Matsuo, Akira; Kaneko, Tadayoshi; Miyamatsu, Hironobu

    2008-01-01

    Mucositis induced by chemoradiotherapy is one of the serious side effects of cancer therapy for oral cancer. It is caused by toxic free radicals (activated oxygen) produced by these therapeutic modalities. Rebamipide is a novel anti-ulcer drug which possesses various cytoprotective activities such as free radical scavenging, induction of prostaglandin-E and acceleration of ulcer healing. We report the results of a pilot study on rebamipide-gargle for inhibition of mucositis induced by chemo-radiotherapy. The present study was conducted on 13 patients (7 men and 6 women; age range 53-88) with oral cancer. They received radiotherapy (30-60 Gy) for the oro-facial area and chemotherapy (docetaxel: 11 cases; tegafur-uracil (UFT): 1 case; radiotherapy alone: 1 case) with simultaneous addition of 1% rebamipide-gargle treatment (10-15 times/day) to prevent the onset of mucositis. Informed consent was obtained prior to entry. Nine cases had grade 1-2 according to the World Health Organization (WHO) criteria, and 4 patients were classified as grade 3-4. No adverse reactions that could be caused by the rebamipide gargle were observed. These results suggested that rebamipide gargle could inhibit the occurrence of stomatitis induced by chemoradiotherapy. (author)

  18. Antianginal efficacy of the combination of felodipine-metoprolol 10/100 mg compared with each drug alone in patients with stable effort-induced angina pectoris

    DEFF Research Database (Denmark)

    Emanuelsson, H; Egstrup, K; Nikus, K

    1999-01-01

    OBJECTIVE: The primary objective of this randomized, double-blind, parallel group trial was to compare the antianginal and antiischemic efficacy of a combination tablet of felodipine-metoprolol 10/100 mg once daily with both drugs given separately once daily in patients with stable effort......-daily treatment with either felodipine-metoprolol 10/100 mg, felodipine 10 mg, or metoprolol 100 mg. The duration of active double-blind treatment was 4 weeks. There were 3 primary efficacy variables in the study; time until end of exercise, time until onset of chest discomfort, and time until 1-mm ST depression...... during a standardized exercise test. RESULTS: The number of patients randomized was 397. There was a statistically significant improvement in time until end of exercise with felodipine-metoprolol 10/100 mg compared with metoprolol 100 mg (P =.04) and felodipine 10 mg compared with metoprolol 100 mg ( P...

  19. Comparison of the pharmacokinetics of a new 30 mg modified-release tablet formulation of metoclopramide for once-a-day administration versus 10 mg immediate-release tablets: a single and multiple-dose, randomized, open-label, parallel study in healthy male subjects.

    Science.gov (United States)

    Bernardo-Escudero, Roberto; Alonso-Campero, Rosalba; Francisco-Doce, María Teresa de Jesús; Cortés-Fuentes, Myriam; Villa-Vargas, Miriam; Angeles-Uribe, Juan

    2012-12-01

    The study aimed to assess the pharmacokinetics of a new, modified-release metoclopramide tablet, and compare it to an immediate-release tablet. A single and multiple-dose, randomized, open-label, parallel, pharmacokinetic study was conducted. Investigational products were administered to 26 healthy Hispanic Mexican male volunteers for two consecutive days: either one 30 mg modified-release tablet every 24 h, or one 10 mg immediate-release tablet every 8 h. Blood samples were collected after the first and last doses of metoclopramide. Plasma metoclopramide concentrations were determined by high-performance liquid chromatography. Safety and tolerability were assessed through vital signs measurements, clinical evaluations, and spontaneous reports from study subjects. All 26 subjects were included in the analyses [mean (SD) age: 27 (8) years, range 18-50; BMI: 23.65 (2.22) kg/m², range 18.01-27.47)]. Peak plasmatic concentrations were not statistically different with both formulations, but occurred significantly later (p 0.05)]. One adverse event was reported in the test group (diarrhea), and one in the reference group (headache). This study suggests that the 30 mg modified-release metoclopramide tablets show features compatible with slow-release formulations when compared to immediate-release tablets, and is suitable for once-a-day administration.

  20. Ficus deltoidea Standardization: Analytical Methods for Bioactive Markers in Deltozide Tablet 200 MG

    International Nuclear Information System (INIS)

    Hazlina Ahmad Hassali; Zainah Adam; Rosniza Razali

    2016-01-01

    Standardization of herbal materials based on their chemical and biological profile is an important prerequisite for development of herbal product. The phyto pharmaceutical product that has been developed by Medical Technology Division, Malaysian Nuclear Agency is DELTOZIDE TABLET 200 MG containing 200 mg of spray-dried aqueous extract of Ficus deltoidea var kunstleri leaf as the active ingredient. Ficus deltoidea Jack or locally known as Mas Cotek is a South East Asian native plant traditionally used to treat several diseases. Pharmacological data showed that this plant exhibited good antioxidant, anti-diabetic and anti-inflammatory properties. It is important to establish the chemical profiles and determine the phytochemicals content of this plant as it is popularly used in traditional medicines. Thus, the present study reports on the comprehensive phytochemicals evaluation of bioactive markers from this extract for the development of DELTOZIDE TABLET 200 MG . Characterization of extract using LCMS/ MS Triple TOF System showed the presence of major constituents representing vitexin, isovitexin, gallic acid, catechinic, api genin, epicatechin and caffeoylquinic acid along with other minor constituents. The extract was standardized by ultra-high performance liquid chromatography (UHPLC) using two pharmacologically active markers, vitexin and isovitexin. Furthermore, qualitative determination of phytochemicals showed the presence of important phyto-constituents namely anthraquinones, terpenoids, flavonoids, tannins, phlobatannins, alkaloids, saponins, cardiac glycosides, steroids and phenols in the aqueous extract of Ficus deltoidea. Quantitative determination of phytochemicals revealed that the amount of total phenolic content (TPC; Gallic acid as standard) and total flavonoid content (TFC; Quercetin as standard) were 126.67±3.98 mg GAE/ g extract and 9.08±0.36 mg QE/ g extract respectively. The generated data provides some explanation for its wide usage in

  1. Formulation and evaluation of rifampicin sustained release tablets using juice of Citrus limetta as bio-retardant.

    Science.gov (United States)

    Gaur, K Pawan; Soam, Kulwant; Gupta, S K; Dabral, Prashant

    2012-03-01

    The advantages of biopolymers over synthetic polymers are low cost, natural origin, free from side effects, biocompatible, bio-acceptable, environmental friendly processing, local availability, better patient tolerance as well as public acceptance. Sustained release tablets containing rifampicin was prepared by adding 100 mg polymer and 50 mg Drug and Granules. Same procedure was followed with 3% and 5% of polymer for preparation of sustained release tablets. Additional Tablets of 100 mg, 200 mg and 400 mg were prepared using 5% of the polymer. The results indicated that the selected biopolymer had a good release retardant property thus it can be concluded that the selected biopolymer can be utilized as low cost natural biocompatible and biodegradable agent.

  2. Formulation and evaluation of rifampicin sustained release tablets using juice of Citrus limetta as bio-retardant

    Directory of Open Access Journals (Sweden)

    K Pawan Gaur

    2012-01-01

    Full Text Available The advantages of biopolymers over synthetic polymers are low cost, natural origin, free from side effects, biocompatible, bio-acceptable, environmental friendly processing, local availability, better patient tolerance as well as public acceptance. Sustained release tablets containing rifampicin was prepared by adding 100 mg polymer and 50 mg Drug and Granules. Same procedure was followed with 3% and 5% of polymer for preparation of sustained release tablets. Additional Tablets of 100 mg, 200 mg and 400 mg were prepared using 5% of the polymer. The results indicated that the selected biopolymer had a good release retardant property thus it can be concluded that the selected biopolymer can be utilized as low cost natural biocompatible and biodegradable agent.

  3. Tablet splitting and weight uniformity of half-tablets of 4 medications in pharmacy practice.

    Science.gov (United States)

    Tahaineh, Linda M; Gharaibeh, Shadi F

    2012-08-01

    Tablet splitting is a common practice for multiple reasons including cost savings; however, it does not necessarily result in weight-uniform half-tablets. To determine weight uniformity of half-tablets resulting from splitting 4 products available in the Jordanian market and investigate the effect of tablet characteristics on weight uniformity of half-tablets. Ten random tablets each of warfarin 5 mg, digoxin 0.25 mg, phenobarbital 30 mg, and prednisolone 5 mg were weighed and split by 6 PharmD students using a knife. The resulting half-tablets were weighed and evaluated for weight uniformity. Other relevant physical characteristics of the 4 products were measured. The average tablet hardness of the sampled tablets ranged from 40.3 N to 68.9 N. Digoxin, phenobarbital, and prednisolone half-tablets failed the weight uniformity test; however, warfarin half-tablets passed. Digoxin, warfarin, and phenobarbital tablets had a score line and warfarin tablets had the deepest score line of 0.81 mm. Splitting warfarin tablets produces weight-uniform half-tablets that may possibly be attributed to the hardness and the presence of a deep score line. Digoxin, phenobarbital, and prednisolone tablet splitting produces highly weight variable half-tablets. This can be of clinical significance in the case of the narrow therapeutic index medication digoxin.

  4. Variability in the 3,4-methylenedioxymethamphetamine content of 'ecstasy' tablets in the UK.

    Science.gov (United States)

    Wood, David Michael; Stribley, Vasoulla; Dargan, Paul Ivor; Davies, Susannah; Holt, David W; Ramsey, John

    2011-09-01

    Toxicity, such as hyperpyrexia, associated with the use of 3,4-methylenedioxymethamphetamine (MDMA; 'ecstasy') appears to be related to serum MDMA concentrations. However, there does not appear to be a similar association with the number of tablets ingested, suggesting variation in the tablet content of MDMA. Although work has shown this variation in other areas of the world, no studies have reported on the variation of MDMA content in UK ecstasy tablets. Ecstasy tablets seized from individuals attending nightclubs were analysed qualitatively to determine if they contained MDMA and quantitatively to determine the MDMA content per tablet. The mean amount of MDMA hydrochloride in 101 seized ecstasy tablets was 58.7±22.9 mg per tablet, with a range of 20 mg to 131 mg per tablet. The majority (96.0%) of tablets contained less than 100 mg MDMA per tablet. There appeared to be a bimodal distribution of MDMA content at approximately 20-40 mg per tablet and 60-80 mg per tablet. There is variability in the MDMA content of ecstasy tablets in the UK. This variability could potentially put users at increased risk of acute harm due to inadvertent excess ingestion of MDMA, as they are unaware of the differences in the MDMA content. Repeat sampling and quantification of MDMA content of ecstasy tablets in the UK will allow better education of users about the potential harms associated with the variability in the MDMA content. In addition, it will provide information to allow the monitoring of changes in not only the MDMA content, but also other adulterants, in ecstasy tablets.

  5. Effects of food on the pharmacokinetics of gemigliptin/metformin sustained-release 50/1,000 mg (25/500 mg x 2 tablets) fixeddose combination tablet in healthy male volunteers.

    Science.gov (United States)

    Choi, Hee Youn; Noh, Yook-Hwan; Kim, Yo Han; Kim, Mi Jo; Lee, Shi Hyang; Kim, Jeong-Ae; Kim, Bogyeong; Lim, Hyeong-Seok; Bae, Kyun-Seop

    2014-05-01

    For patient convenience, a gemigliptin/metformin sustainedrelease fixed-dose combination (FDC) tablet was developed. This study was conducted to investigate the effects of food on the pharmacokinetic (PK) profile of the FDC tablets. This was an open-label, randomized, single dose, 2-period, 2-sequence crossover study in 24 healthy male volunteers. The FDC tablets (25/500 mg × 2 tablets) were administered in high-fat fed and fasted states on separate occasions, and each subject was randomly allocated to each sequence with a 7-day washout period. PK blood samplings were conducted from predose to 48 hours after dosing. Tolerability assessments were performed throughout the study. Nine adverse events (AEs) of mild intensity were reported from 8 subjects after study drug administration, and the AE frequency was similar between treatments. No serious AEs were reported. The PK parameters of gemigliptin and metformin were compared between fasting and fed states. For gemigliptin, the geometric mean ratios (GMRs) (fed : fasted state) of the Cmax and AUClast were 0.886 (90% confidence interval (CI) 0.781 - 1.006) and 1.021 (90% CI 0.949 - 1.099), respectively. For metformin, the GMRs of the Cmax and AUClast were 0.811 (90% CI 0.712 - 0.923) and 1.144 (90% CI 1.013 - 1.291), respectively. A prolonged tmax for metformin was observed. These results are similar to the effects of food on each component. The FDC tablet may have a similar PK profile as that of individual drugs and is generally tolerable when administered with food. These results indicate that the FDC tablet can be administered in the same dosing regimen as each component, especially that of metformin sustained-release.

  6. The critical role of NIR spectroscopy and statistical process control (SPC) strategy towards captopril tablets (25 mg) manufacturing process understanding: a case study.

    Science.gov (United States)

    Curtivo, Cátia Panizzon Dal; Funghi, Nathália Bitencourt; Tavares, Guilherme Diniz; Barbosa, Sávio Fujita; Löbenberg, Raimar; Bou-Chacra, Nádia Araci

    2015-05-01

    In this work, near-infrared spectroscopy (NIRS) method was used to evaluate the uniformity of dosage units of three captopril 25 mg tablets commercial batches. The performance of the calibration method was assessed by determination of Q value (0.9986), standard error of estimation (C-set SEE = 1.956), standard error of prediction (V-set SEP = 2.076) as well as the consistency (106.1%). These results indicated the adequacy of the selected model. The method validation revealed the agreement of the reference high pressure liquid chromatography (HPLC) and NIRS methods. The process evaluation using the NIRS method showed that the variability was due to common causes and delivered predictable results consistently. Cp and Cpk values were, respectively, 2.05 and 1.80. These results revealed a non-centered process in relation to the average target (100% w/w), in the specified range (85-115%). The probability of failure was 21:100 million tablets of captopril. The NIRS in combination with the method of multivariate calibration, partial least squares (PLS) regression, allowed the development of methodology for the uniformity of dosage units evaluation of captopril tablets 25 mg. The statistical process control strategy associated with NIRS method as PAT played a critical role in understanding of the sources and degree of variation and its impact on the process. This approach led towards a better process understanding and provided the sound scientific basis for its continuous improvement.

  7. Industrial production of MgH2 and its application

    International Nuclear Information System (INIS)

    Uesugi, H.; Sugiyama, T.; Nii, H.; Ito, T.; Nakatsugawa, I.

    2011-01-01

    Research highlights: → Tablet and powder Mg were hydrogenated in a 50 kg batch furnace based on thermal equilibrium method. → Compression of Mg tablet improved the hydrogenation yield. → Hydrolysis of MgH 2 using citric acid generated hydrogen under 373 K. → A MgH 2 -hydrogen reactor utilizing hydraulic head pressure was developed. → - Abstract: A process for the industrial production of magnesium hydride (MgH 2 ) based on a thermal equilibrium method and its application to portable hydrogen sources is proposed. Mg powders and tablets compressed with mechanically ground Mg ribbons were successfully hydrogenated in a 50-kg-batch furnace. The resultant MgH 2 showed a hydrogen yield of around 96% with good reproducibility. The compression ratio of Mg tablets was found to be an important factor in the hydrogenation yield. A hydrolysis technique using citric acid as an additive was employed to generate hydrogen under 373 K. Increasing the concentration of citric acid and the temperature accelerated the hydrolysis reactivity. A hydrogen reactor utilizing hydraulic head pressure was developed. It generated hydrogen continuously for 1 h at a flow rate of 100 ml min -1 with hydrolysis of 5 g of tablet-form MgH 2 . The conversion yield was around 70%, regardless of the flow rate.

  8. Rebamipide ophthalmic suspension for the treatment of dry eye syndrome: a critical appraisal

    Directory of Open Access Journals (Sweden)

    Kashima T

    2014-05-01

    Full Text Available Tomoyuki Kashima,1 Hirotaka Itakura,1,2 Hideo Akiyama,1 Shoji Kishi11Department of Ophthalmology, Gunma University, School of Medicine, Maebashi, Gunma, Japan; 2Department of Ophthalmology, Maebashi Red Cross Hospital, Maebashi, Gunma, JapanAbstract: Rebamipide was initially developed and approved for use in treating gastric ulcers and lesions associated with gastritis. Discovery of its ability to increase gastric mucin led to investigations of its effect on ocular surface mucin and the subsequent development for use in dry eye patients. Investigations have confirmed that rebamipide increases corneal and conjunctival mucin-like substances along with improving corneal and conjunctival injury. Clinically, rebamipide ophthalmic suspensions can effectively treat tear deficiency and mucin-caused corneal epithelial damage, and can restore the microstructure responsible for tear stability. Topical rebamipide has also been shown to be effective in treating other ocular surface disorders such as lagophthalmos, lid wiper epitheliopathy, and persistent corneal erosion. Rebamipide’s ability to modify epithelial cell function, improve tear stability, and suppress inflammation in the absence of any known major side effects suggest that it may be a beneficial first drug of choice for severe dry eye treatment and other ocular surface disorders. This review summarizes the history and development of this innovative dry eye treatment from its initial use as an effective stomach medication to its current use in the treatment of dry eye in Japan.Keywords: quinolinone derivative, tear deficiency, ocular surface disorder, mucin secretion, Mucosta

  9. Bioequivalence of generic alendronate sodium tablets (70 mg to Fosamax® tablets (70 mg in fasting, healthy volunteers: a randomized, open-label, three-way, reference-replicated crossover study

    Directory of Open Access Journals (Sweden)

    Zhang Y

    2017-07-01

    Full Text Available Yifan Zhang,1 Xiaoyan Chen,1 Yunbiao Tang,2 Youming Lu,1 Lixia Guo,1 Dafang Zhong1 1State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 2Department of Pharmacy, The General Hospital of Shenyang Military Region, Shenyang, People’s Republic of China Purpose: The aim of this study was to evaluate the bioequivalence of a generic product 70 mg alendronate sodium tablets with the reference product Fosamax® 70 mg tablet. Materials and methods: A single-center, open-label, randomized, three-period, three-sequence, reference-replicated crossover study was performed in 36 healthy Chinese male volunteers under fasting conditions. In each study period, the volunteers received a single oral dose of the generic or reference product (70 mg. Blood samples were collected at pre-dose and up to 8 h after administration. The bioequivalence of the generic product to the reference product was assessed using the US Food and Drug Administration (FDA and European Medicines Agency (EMA reference-scaled average bioequivalence (RSABE methods. Results: The average maximum concentrations (Cmax of alendronic acid were 64.78±43.76, 56.62±31.95, and 60.15±37.12 ng/mL after the single dose of the generic product and the first and second doses of the reference product, respectively. The areas under the plasma concentration–time curves from time 0 to the last timepoint (AUC0–t were 150.36±82.90, 148.15±85.97, and 167.11±110.87 h·ng/mL, respectively. Reference scaling was used because the within-subject standard deviations of the reference product (sWR for Cmax and AUC0–t were all higher than the cutoff value of 0.294. The 95% upper confidence bounds were -0.16 and -0.17 for Cmax and AUC0–t, respectively, and the point estimates for the generic/reference product ratio were 1.08 and 1.00, which satisfied the RSABE acceptance criteria of the FDA. The 90% CIs for Cmax and AUC0–t were 90.35%–129

  10. Captopril 25 mg tablets stability assessment in different primary packing materials

    Directory of Open Access Journals (Sweden)

    Flávia Costa Mendes Paiva

    2017-11-01

    Full Text Available Introduction: Packaging is used to provide protection and information, from the production to the administration of a formulation. It is essential to define the primary packaging, for keeping the therapeutic efficacy of drugs, safety of users and for protecting drugs from instability. Objectives: The main objective of this study was to assess the stability of captopril 25 mg tablets in different primary packaging materials. Method: The characterization (IR, DSC and physical tests of the packaging materials used for captopril was carried out prior to the manufacture of tablets. Tablets were also characterized by physical-chemical analysis, comparative dissolution profile and stability studies. Results: The characterization of packaging materials was crucial for understanding the behavior of captopril when packed in each material. Materials with significant barrier, as blisters PVC/PVdC 90 g.m-² and hard aluminum and PVC/PE/PVdC and hard aluminum showed satisfactory results in a second stage, S2. On the contrary, lower barrier materials as blisters PVC/PVdC 40 g.m-² and hard aluminum did not present dissolution analysis S2. Conclusions: The aluminum strip presented the best results. And the batch in glass bottle, although packaged in excellent material, was disapproved in accelerated stability.

  11. Biopharmaceutic Risk Assessment of Brand and Generic Lamotrigine Tablets.

    Science.gov (United States)

    Vaithianathan, Soundarya; Raman, Siddarth; Jiang, Wenlei; Ting, Tricia Y; Kane, Maureen A; Polli, James E

    2015-07-06

    The therapeutic equivalence of generic and brand name antiepileptic drugs has been questioned by neurologists and the epilepsy community. A potential contributor to such concerns is pharmaceutical quality. The objective was to assess the biopharmaceutic risk of brand name Lamictal 100 mg tablets and generic lamotrigine 100 mg tablets from several manufacturers. Lamotrigine was characterized in terms of the Biopharmaceutics Classification System (BCS), including aqueous solubility and Caco-2 permeability. A panel of pharmaceutical quality tests was also performed on three batches of Lamictal, three batches of Teva generic, and one batch of each of four other generics: appearance, identity, assay, impurity, uniformity of dosage units, disintegration, dissolution, friability, and loss on drying. These market surveillance results indicate that all brand name and generic lamotrigine 100 mg tablets passed all tests and showed acceptable pharmaceutical quality and low biopharmaceutic risk. Lamotrigine was classified as a BCS class IIb drug, exhibiting pH-dependent aqueous solubility and dissolution. At pH 1.2 and 4.5, lamotrigine exhibited high solubility, whereas lamotrigine exhibited low solubility at pH 6.8, including non-sink dissolution. Lamotrigine showed high Caco-2 permeability. The apparent permeability (Papp) of lamotrigine was (73.7 ± 8.7) × 10(-6) cm/s in the apical-to-basolateral (AP-BL) direction and (41.4 ± 1.6) × 10(-6) cm/s in the BL-AP direction, which were higher than metoprolol's AP-BL Papp of (21.2 ± 0.9) × 10(-6) cm/s and BL-AP Papp of (34.6 ± 4.6) × 10(-6) cm/s. Overall, lamotrigine's favorable biopharmaceutics from a drug substance perspective and favorable quality characteristics from a tablet formulation perspective suggest that multisource lamotrigine tablets exhibit a low biopharmaceutic risk.

  12. Prophylactic effect of rebamipide on aspirin-induced gastric lesions and disruption of tight junctional protein zonula occludens-1 distribution.

    Science.gov (United States)

    Suzuki, Takahiro; Yoshida, Norimasa; Nakabe, Nami; Isozaki, Yutaka; Kajikawa, Hirokazu; Takagi, Tomohisa; Handa, Osamu; Kokura, Satoshi; Ichikawa, Hiroshi; Naito, Yuji; Matsui, Hirofumi; Yoshikawa, Toshikazu

    2008-03-01

    Aspirin and nonsteroidal anti-inflammatory agents are known to induce gastroduodenal complications such as ulcer, bleeding, and dyspepsia. In this study, we examined the prophylactic effect of rebamipide, an anti-ulcer agent with free-radical scavenging and anti-inflammatory effect, on acidified aspirin-induced gastric mucosal injury in rats. In addition, we investigated the mucosal barrier functions disrupted by aspirin. Oral administration of acidified aspirin resulted in linear hemorrhagic erosions with increasing myeloperoxidase activity and thiobarbituric acid-reactive substance concentrations in the gastric mucosa. Rebamipide suppressed these acidified aspirin-induced gastric lesions and inflammatory changes significantly, and its protective effect was more potent in the case of repeated (twice daily for 3 days) treatment than single treatment before aspirin administration. Immunostaining of zonula occludens (ZO)-1, one of the tight junctional proteins, was strengthened in rat gastric mucosa after repeated administration of rebamipide. In addition, aspirin induced the increasing transport of fluorescine isothiocyanate-labeled dextrans with localized disruption and decreased expression of ZO-1 protein on rat gastric mucosal cell line RGM-1. Rebamipide effectively prevented aspirin-induced permeability changes and disruption of ZO-1 distribution. These results suggest that rebamipide protects against aspirin-induced gastric mucosal lesions by preserving gastric epithelial cell-to cell integrity in addition to the anti-inflammatory effects.

  13. Desarrollo de una formulación de tabletas revestidas de secnidazol 500 mg Development of a formulation of coated secnidazole tablets 500 mg

    Directory of Open Access Journals (Sweden)

    Iverlis Díaz Polanco

    2008-04-01

    Full Text Available Se describe el desarrollo de una formulación de tabletas revestidas de secnidazol 500 mg. Durante el desarrollo de esta se evaluaron 2 métodos: la granulación seca y la granulación húmeda. En el revestimiento de las tabletas se empleó un sistema hidroalcohólico con el preparado comercial Policoat YS 1-7003 (Opadry®. Los lotes sometidos a ensayos de estabilidad fueron elaborados a escala piloto, por la vía de granulación húmeda, lo que demostró la factibilidad del proceso de fabricación a esta escala. Las tabletas revestidas presentaron adecuadas propiedades físico-mecánicas y tecnológicas y estas fueron envasadas en frascos de polietileno de alta densidad y en sobres termoconformados de polivinilcloruro/aluminio. La estabilidad química y microbiológica de las tabletas de secnidazol fue estudiada durante 24 meses; los resultados demostraron que estas cumplían con los requisitos establecidos durante este periodoThe development of a formulation of coated Secnidazole tablets 500mg was described. During its development, 2 methods were evaluated: dry granulation and humid granulation. A hydroalcoholic system was used with the Policoat YS 1-7003 (Opadry® commercial preparation for coating the tablets. The batches subjected to stability assays were made at pilot scale by humid granulation, which showed the feasibility of the manufacturing process at this scale. The coated tablets had adequate physicomechanical and technological properties and they were packed in polyethylene flasks of high density and in polyvinyl chloride/aluminium thermoconformed envelopes. The chemical and microbiological stability of the secnidazole tablets were studied during 24 months. The results demonstrated that these tablets met the requirements established during this period

  14. Preparation and In-Vitro Evaluation of Sustained Release Matrix Diclofenac Sodium Tablets Using HPMC KM 100 and Gums

    Directory of Open Access Journals (Sweden)

    Zafar Iqbal, Raza Khan, Fazli Nasir, Jamshaid Ali Khan, Lateef Ahmad, Abad Khan, Yaser Shah

    2010-12-01

    Full Text Available Objectives: The impact of hydroxypropylmethyl cellulose(HPMC K 100M alone and in combination with the guar gum,xanthan gum and gum tragacanth on the release of the diclofenac sodium matrix tablets were evaluated.Materials and Methods: The granules were prepared using wet granulation method and compressed into tablets using different ratio of drug and gum ratio. The physical properties of the tablets were within acceptable pharmacopeial limits.The release profiles of the matrix tablets were evaluated in vitro,using USP dissolution apparatus II (paddle method.Results: The formulations containing HPMC K 100M drug ratio1:1.3 and 1:1.6 and formulations containing HPMC, gum and drug with different ratio also sustained the release of diclofenac sodium for 12 hours. The mechanism of drug release from the matrix tablets was studied using Zero order, First order, Higuchi and Korsmeyer’s models using regression coefficient method. The stability of the selected formulations was evaluated at 40˚C and 70% RH for 6 months.Conclusions: HPMC K100M alone and in combination with natural gums as the retarding material retarded the release upto 12 hours and showed little deviation from the theoretical release pattern.

  15. Clinical efficacy and safety of a new 1000-mg suspension versus twice-daily 500-mg tablets of MPFF in patients with symptomatic chronic venous disorders: a randomized controlled trial.

    Science.gov (United States)

    Carpentier, Patrick; van Bellen, Bonno; Karetova, Debora; Hanafiah, Harunarashid; Enriquez-Vega, Elizabeth; Kirienko, Alexander; Dzupina, Andrej; Sabovic, Miso; Reina Gutierrez, Lourdes; Subwongcharoen, Somboom; Tüzün, Hasan; Maggioli, Arnaud

    2017-10-01

    Chronic venous disorders (CVD) is estimated to affect 30% to 50% of women and 10% to 30% of men. The most widely prescribed treatment for CVD worldwide is micronized purified flavonoid fraction 500 mg (MPFF). The aim of this clinical trial was to develop a new once daily 1000-mg oral suspension of MPFF. In an international, randomized, double-blind, parallel-group study, symptomatic individuals classified CEAP C0s to C4s were randomized in either treatment arm and treated for 8 weeks. Lower limb symptoms (discomfort, pain and heaviness) were assessed using Visual Analog Scales (VAS), and quality of life (QoL) was measured with the CIVIQ-20 Questionnaire. A total of 1139 patients were included in the study. Both MPFF treatment regimens were well tolerated and associated with a significant reduction in lower limb symptoms. A non-inferiority of MPFF 1000-mg oral suspension once daily compared to MPFF 500-mg tablet twice daily (P1000 mg and -3.37 cm for MPFF 500 mg), leg pain (-3.27 cm for MPFF 1000 mg and -3.31 cm for MPFF 500 mg) and leg heaviness (-3.41 cm for MPFF 1000 mg and -3.46 cm for MPFF 500 mg). The patients' QoL was improved by about 20 points on the CIVIQ scale in both groups (19.33 points for MPFF 1000 mg and 20.28 points for MPFF 500 mg). MPFF 1000-mg oral suspension and MPFF 500-mg tablets treatments were associated with similar reductions in lower limb symptoms and QoL improvement. The new once daily MPFF1000-mg oral suspension has a similar safety profile to two tablets of MPFF 500 mg, with the advantage of one daily intake, potentially associated with improved patient adherence and easier CVD management.

  16. In vitro disintegration studies of weekly generic alendronate sodium tablets (70 mg) available in the US.

    Science.gov (United States)

    Dansereau, Richard J; Crail, Debbie J; Perkins, Alan C

    2009-02-01

    Bisphosphonates as a class have the potential to cause upper gastrointestinal irritation. Although the generic alendronate sodium tablets are bioequivalent to the branded product, a potential concern is that the pharmaceutical attributes of the various generic formulations my affect the potential for local irritation and tolerability. The in vitro disintegration times were determined using the method described in the US Pharmacopeia 30 (USP 30). The disintegration of three generic alendronate sodium tablets 70 mg available in the United States was compared to that of the branded product. The mean disintegration times of the generic alendronate sodium tablets ranged from 9 to 10 s for the Barr lots to 108 s for the Watson lot. The disintegration time of the branded product (Fosamax) was 53 s. The three Barr lots and one Teva lot had rapid disintegration times which were similar to the disintegration standards (disintegrating tablets. Since there is no established disintegration time for alendronate sodium tablets there can be no assurance that the generic tablets are equivalent to the branded product in terms of esophageal exposure. However, the in vitro disintegration times have not been correlated with in vivo disintegration performance. Copies of generic alendronate sodium tablets are approved based on the results of single-dose bioavailability studies in healthy subjects and this is not considered adequate to establish similar disintegration characteristics.

  17. Conjunctival Goblet Cell Density Following Cataract Surgery With Diclofenac Versus Diclofenac and Rebamipide: A Randomized Trial.

    Science.gov (United States)

    Kato, Kumiko; Miyake, Kensaku; Kondo, Nagako; Asano, Sayaka; Takeda, Junko; Takahashi, Akiko; Takashima, Yuko; Kondo, Mineo

    2017-09-01

    To determine the effects of topical diclofenac or betamethasone with concomitant application of topical rebamipide on the conjunctival goblet cell density in eyes after cataract surgery. Randomized clinical trial. Eighty patients who were scheduled for cataract surgery. Patients were randomized into 4 groups according to the postoperative topical drugs to be given; Group A, diclofenac alone; Group B, diclofenac and rebamipide; Group C, betamethasone alone; and Group D, betamethasone and rebamipide. Impression cytology was performed before and at 1 month after the surgery, and the mean density of goblet cells was determined. The mean (± SD) density of goblet cells before the surgery in Group A was 257.0 ± 188.7 cells/mm 2 , and it decreased significantly to 86.5 ± 76.7 cells/mm 2 at 1 month after the surgery (P = .002). In Group B, the goblet cell density was not statistically different between before (238.5 ± 116.6 cells/mm 2 ) and at 1 month after the surgery (211.3 ± 184.4 cells/mm 2 , P = .55). In Groups C and D, the mean density of goblet cells was decreased at 1 month after the surgery, but the decreases were not significant (P = .11 and P = .52, respectively). After cataract surgery with postoperative topical diclofenac, the conjunctival goblet cell density was significantly reduced, and this reduction was blocked by the concomitant use of topical rebamipide. These results suggest that the concomitant use of topical rebamipide with nonsteroidal anti-inflammatory drugs is beneficial, especially in cases with postoperative dry eyes. Copyright © 2017 The Author(s). Published by Elsevier Inc. All rights reserved.

  18. Topical rebamipide improves lid wiper epitheliopathy

    OpenAIRE

    Itakura, Hirotaka; Kashima, Tomoyuki; Itakura, Mariko; Akiyama, Hideo; Kishi, Shoji

    2013-01-01

    Hirotaka Itakura,1,2 Tomoyuki Kashima,2 Mariko Itakura,1 Hideo Akiyama,2 Shoji Kishi2 1Department of Ophthalmology, Maebashi Red Cross Hospital, 2Department of Ophthalmology, Gunma University, School of Medicine, Maebashi, Japan Abstract: Administration of topical rebamipide increases the mucin level of tear film and improves the ocular surface in short break-up time type of dry eye. Lid wiper epitheliopathy (LWE) is a disorder of the marginal conjunctiva of the upper eyelid with dry eye sym...

  19. Tablet splitting: is it worthwhile? Analysis of drug content and weight uniformity for half tablets of 16 commonly used medications in the outpatient setting.

    Science.gov (United States)

    Helmy, Sally A

    2015-01-01

    Tablet splitting is a well-established medical practice in clinical settings for multiple reasons, including cost savings and ease of swallowing. However, it does not necessarily result in weight-uniform half tablets. To (a) investigate the effect of tablet characteristics on weight and content uniformity of half tablets, resulting from splitting 16 commonly used medications in the outpatient setting and (b) provide recommendations for safe tablet-splitting prescribing practices. Ten random tablets from each of the selected medications were weighed and split by 5 volunteers (2 men and 3 women aged 25-44 years) using a knife. The selected medications were mirtazapine 30 mg, bromazepam 3 mg, oxcarbazepin 150 mg, sertraline 50 mg, carvedilol 25 mg, bisoprolol fumarate 10 mg, losartan 50 mg, digoxin 0.25 mg, amiodarone HCl 200 mg, metformin HCl 1,000 mg, glimepiride 4 mg, montelukast 10 mg, ibuprofen 600 mg, celecoxib 200 mg, meloxicam 15 mg, and sildenafil citrate 50 mg. The resulting half tablets were evaluated for weight and drug content uniformity in accordance with proxy United States Pharmacopeia (USP) specification (95%-105% for digoxin and 90%-110% for the other 15 drugs). Weight and drug content uniformity were assessed by comparing weight or drug content of the half tablets with one-half of the mean weight or drug content for all whole tablets in the sample. The percentages by which the weight and drug content of each whole tablet or half tablet differed from sample mean values were calculated. Other relevant physical characteristics of the 16 products were measured. A total of 52 of 320 half tablets (16.2%) and 48 of 320 half tablets (15.0%) fell outside of the proxy USP specification for weight and drug content, respectively. Bromazepam, carvedilol, bisoprolol, losartan, digoxin, and meloxicam half tablets failed the weight and content uniformity test; however, the half tablets for the rest of the medications passed the test. Mean percent weight loss after

  20. Actual use of and adherence to ibuprofen 400 mg tablet dosing instructions in a simulated OTC environment
.

    Science.gov (United States)

    Meeves, Suzanne; Leyva, Rina; Richardson, Clark; Wilson, Brenda; Savastano, David M

    2017-07-01

    Evaluate adherence of US consumers to proposed label directions for a new 400 mg ibuprofen formulation. In this single-arm, open-label, multicenter, 30-day study simulating an over-the-counter (OTC)-like environment, US analgesic consumers reviewed proposed product packaging for a new 400 mg ibuprofen formulation and made a purchase decision. Purchasers used the product as needed and recorded use over 30 days. Outcomes included the percentage of participants who exhibited correct or acceptable product use for the primary endpoint (not exceeding 1,200 mg/day > 2 times during the study) or secondary endpoint (not exceeding 400 mg/dose > 2 times during the study) and adherence to the labeled dosing interval of 6 - 8 hours. Primary endpoint success was met if the lower bound of the 95% confidence interval (CI) was ≥ 85%. Of 685 purchasers providing use data, correct or acceptable use behavior occurred in 95.2% (95% CI: 93.6%, 96.8%) regarding total daily dose and in 84.4% (95% CI: 81.7%, 87.1%) regarding the number of tablets taken per dosing occasion. Most participants (87.3%) never used > 1,200 mg/day or took > 1 tablet/dose (78.1%). Nearly 43% of subjects re-dosed within 6 hours of the previous dose; of these, ~ 82% re-dosed between the 4- and 6-hour time intervals. Adverse events were consistent with prior ibuprofen 200 mg experience. This study provides evidence that a majority of US consumers would be able to use OTC ibuprofen 400 mg tablets in a manner consistent with product labeling. Misuse rates were low and unlikely to generate an excess risk of clinically important adverse events.
.

  1. Histological observation of goblet cells following topical rebamipide treatment of the human ocular surface: A case report

    OpenAIRE

    KASE, SATORU; SHINOHARA, TOSHIYA; KASE, MANABU

    2014-01-01

    The topical administration of rebamipide (Mucosta?), an antiulcer agent, clinically increases the mucin level of tear film. The aim of this study was to report the histological changes of goblet cells following the topical administration of rebamipide to a patient with nevus of the lacrimal caruncle. A 62-year-old male exhibited a pigmented nodule located in the lacrimal caruncle in the left eye. An excisional biopsy and subsequent surgical resection were conducted at the caruncle, prior to a...

  2. A fixed-dose combination tablet of gemigliptin and metformin sustained release has comparable pharmacodynamic, pharmacokinetic, and tolerability profiles to separate tablets in healthy subjects.

    Science.gov (United States)

    Park, Sang-In; Lee, Howard; Oh, Jaeseong; Lim, Kyoung Soo; Jang, In-Jin; Kim, Jeong-Ae; Jung, Jong Hyuk; Yu, Kyung-Sang

    2015-01-01

    In type 2 diabetes mellitus, fixed-dose combination (FDC) can provide the complementary benefits of correction of multiple pathophysiologic defects such as dysfunctions in glycemic or metabolic control while improving compliance compared with separate tablets taken together. The objective of the study reported here was to compare the pharmacodynamic (PD), pharmacokinetic (PK), and tolerability profiles of gemigliptin and extended-release metformin (metformin XR) between FDC and separate tablets. A randomized, open-label, single-dose, two-way, two-period, crossover study was conducted in 28 healthy male volunteers. Two FDC tablets of gemigliptin/metformin 25/500 mg or separate tablets of gemigliptin (50 mg ×1) and metformin XR (500 mg ×2) were orally administered in each period. Serial blood samples were collected up to 48 hours post-dose to determine dipeptidyl peptidase 4 (DPP-4) activity using spectrophotometric assay and concentrations of gemigliptin and metformin using tandem mass spectrometry. Geometric mean ratios (GMRs) of FDC to separate tablet formulations and their 90% confidence intervals (CIs) were calculated to compare the PD and PK parameters between the two formulations. Tolerability was assessed throughout the study. The plasma DPP-4 activity-time curves of the FDC and the separate tablets almost overlapped, leading to a GMR (90% CI) of the FDC to separate tablets for the plasma DPP-4 activity and its maximum inhibition of 1.00 (0.97-1.04) and 0.92 (0.82-1.05), respectively. Likewise, all of the GMRs (90% CIs) of FDC to separate tablets for the area under the plasma concentration-time curve and maximum plasma concentration of gemigliptin and metformin fell entirely within the conventional bioequivalence range of 0.80-1.25. Both the FDC and separate tablets were well tolerated. The PD, PK, and tolerability profiles of gemigliptin and metformin XR in FDC and separate tablets were found to be comparable. The FDC tablet of gemigliptin and metformin

  3. Estudio de estabilidad de tabletas de propiltiouracilo 50 mg Study of the 50 mg Propylthiouracil tablets stability

    Directory of Open Access Journals (Sweden)

    María Olga Valdés Bendoyro

    2010-03-01

    Full Text Available Se desarrolló el estudio de estabilidad de las tabletas de propiltiouracilo 50 mg y se determinó su fecha de vencimiento. Este estudio se realizó por los métodos de vida de estante y de estabilidad acelerada mediante cromatografía líquida de alta eficiencia, validados en el Centro de Investigación y Desarrollo de Medicamentos. El estudio de vida de estante se desarrolló por un periodo de 24 meses a temperatura ambiente; mientras que el estudio de estabilidad acelerada se efectuó sometiendo el producto a la influencia de la luz, la humedad y la temperatura; se realizó el análisis durante 3 meses, para los 2 primeros y durante 6 meses para el estudio de la temperatura. La formulación de propiltiouracilo tabletas 50 mg cumplió con las especificaciones de calidad descritas en la farmacopea. Los resultados del estudio de estabilidad por vida de estante después de transcurridos los 24 meses indicaron que el producto mantenía los parámetros que determinan su calidad durante ese tiempo, y en los estudios acelerados no se observó degradación significativa del producto. Se estableció 2 años como fecha de vencimiento en las condiciones señaladas.Autors developed a stability study of 50 mg Propylthiouracil tablets and determination of its expiry date. This study was conducted by fixed life methods and of accelerated stability by high-performance liquid chromatography, validated in Drugs Research and Development Center. Fixed life study was conducted during 24 months at room temperature; whereas the accelerated stability study was conducted exposing the product to light influence, humidity and temperature; during 3 months a analysis was performed for the two first ones and over 6 months in the case of temperature study. Propylthiouracil formula (50 mg tablets fulfilled the quality specifications described in Pharmacopeia. Results of stability study by fixed life after 24 monhts showed that thr product maintain the parameter determining

  4. Evaluation of crushed ticagrelor tablet doses: recovery following crushing and naso-gastric tube passage ex vivo.

    Science.gov (United States)

    Crean, Barry; Finnie, Cindy; Crosby, Anna

    2013-06-01

    Orally available ticagrelor in combination with low-dose aspirin (75-100 mg/day) is indicated for adult patients with acute coronary syndromes. However, patients with swallowing difficulties may be unable to consume the currently available 90-mg tablet. It is hypothesized that ticagrelor could be given to this patient cohort as a crushed dose administered either orally or via a naso-gastric (NG) tube. To investigate the potential use of crushed ticagrelor tablets (90- and 180-mg doses) for oral dose or NG tube administration. Ticagrelor tablets (90 or 180 mg [two 90-mg tablets]) were prepared to emulate oral and NG tube administration by similar methods. For the oral dose, ticagrelor tablets were crushed using a mortar and pestle and transferred to a dosing cup. 100 mL of water was added to the mortar, stirred, and the contents were transferred to the dosing cup and stirred to form a suspension. At this stage, where the suspension would normally be administered to a patient, it was collected for high performance liquid chromatography (HPLC) analysis. The mortar was then flushed with 100 mL of water, and the contents were again transferred to the dosing cup, stirred, and collected for HPLC analysis. For the NG dose, polyvinylchloride, polyurethane, and silicone size CH10 NG tubes were used. The tablets were crushed using a mortar and pestle, diluted with 50 mL of water, and stirred. At this stage, where the suspension would normally be administered to a patient through an NG tube using a syringe, it was collected for HPLC analysis. The mortar was then flushed with two additional 50 mL aliquots of water and the contents were passed through the NG tube. HPLC analysis examined the recoverability of ticagrelor in each of the dose suspensions and flushes and the stability of the suspension when held in a syringe for up to 2 h. One or two crushed 90-mg ticagrelor tablets, prepared for either oral or NG tube administration, delivers a mean dose of ≥97% of the original

  5. Mechanism by Which Magnesium Oxide Suppresses Tablet Hardness Reduction during Storage.

    Science.gov (United States)

    Sakamoto, Takatoshi; Kachi, Shigeto; Nakamura, Shohei; Miki, Shinsuke; Kitajima, Hideaki; Yuasa, Hiroshi

    2016-01-01

    This study investigated how the inclusion of magnesium oxide (MgO) maintained tablet hardness during storage in an unpackaged state. Tablets were prepared with a range of MgO levels and stored at 40°C with 75% relative humidity for up to 14 d. The hardness of tablets prepared without MgO decreased over time. The amount of added MgO was positively associated with tablet hardness and mass from an early stage during storage. Investigation of the water sorption properties of the tablet components showed that carmellose water sorption correlated positively with the relative humidity, while MgO absorbed and retained moisture, even when the relative humidity was reduced. In tablets prepared using only MgO, a petal- or plate-like material was observed during storage. Fourier transform infrared spectrophotometry showed that this material was hydromagnesite, produced when MgO reacts with water and CO2. The estimated level of hydromagnesite at each time-point showed a significant negative correlation with tablet porosity. These results suggested that MgO suppressed storage-associated softening by absorbing moisture from the environment. The conversion of MgO to hydromagnesite results in solid bridge formation between the powder particles comprising the tablets, suppressing the storage-related increase in volume and increasing tablet hardness.

  6. Evaluation of the disintegration properties of commercial famotidine 20 mg orally disintegrating tablets using a simple new test and human sensory test.

    Science.gov (United States)

    Harada, Tsutomu; Narazaki, Ryuichi; Nagira, Shinsuke; Ohwaki, Takayuki; Aoki, Shigeru; Iwamoto, Kiyoshi

    2006-08-01

    The purpose of this study was to demonstrate the usefulness and broad-applicability of a simple disintegration test method for orally disintegrating tablets (ODT). Eight types of commercial famotidine 20 mg orally disintegrating tablets with different physical properties (formulation, manufacturing method, tablet weight, shape, diameter, thickness, etc.), were used. Disintegration times of these tablets were evaluated employing human sensory test, conventional disintegration test, and the new proposed disintegration test. The human sensory test was performed in 5 healthy volunteers. In the conventional disintegration test, the disintegration apparatus described in the Japanese Pharmacopeia (JP 1(st)) was used. Our proposed new test which is characterized by a rotating shaft with a low weight (10, 15 g) and rotation speed (10, 25, 50 rpm) was evaluated using tablets with and without storage under severe conditions (60 degrees C/75%RH for 1 week). The disintegration times of famotidine 20 mg orally disintegrating tablets in human sensory test varied from 9 to 32 s. In contrast, disintegration times in the conventional test were prolonged to over 300 s. Disintegration times in the new proposed test were close to those in human sensory test. Especially, when the new test was conducted with 15 or 10 g weight and 25 rpm, the slope (human sensory test vs. new proposed test) was almost 1. We were able to demonstrate that the new proposed test was useful to estimate the actual human disintegration time.

  7. Formulation of Peperomia pellucida (L Kunth extract tablet by modified filler

    Directory of Open Access Journals (Sweden)

    Nanang Yunarto

    2013-07-01

    Full Text Available AbstrakLatar belakang: Peperomia pelusida telah banyak digunakan dalam pengobatan tradisional. Pada saat ini, bentuk-bentuk yang ada masih konvensional seperti jus dan infusum, karena itu, perlu dirumuskan lebih praktis dan berat seragam seperti bentuk tablet. Tujuan dari penelitian ini adalah untuk mendapatkan formula optimum pelusida tablet ekstrak P. pellucida. Metode: P. pelusida ekstrak tablet yang diproduksi dengan variasi selulosa mikrokristalin (MCC PH 101 - laktosa dengan metode granulasi basah dalam tiga formula, formula I (100% MCC PH 101, II (laktosa 100%, dan III (MCC PH 101: laktosa = 50%: 50%. Butiran dievaluasi karakteristik fisik termasuk laju aliran, penyerapan air, dan kompaktibilitas untuk mendapatkan formula optimum dengan menggunakan desain simplex lattice dan jumlah respon. Formula yang digunakan untuk membuat tablet dan diuji karakteristik fisik (keseragaman bobot, kekerasan, dan kerapuhan dan waktu hancur. Hasil: Laktosa secara signifikan dipengaruhi oleh laju alirannya, sedangkan MCC PH 101 - laktosa dengan metode granulasi basah dalam tiga formula, formula I (100% MCC PH 10PH 101 dipengaruhi penyerapan kompaktibilitas dan air. Berdasarkan karakteristik fisik granul dan jumlah responsnya, kombinasi formula MCC PH 101 80% dan laktosa 20% dapat disimpulkan menjadi yang paling optimal untuk tablet filler. Formula tablet ini yang memiliki karakteristik fisik terbaik dengan berat 620,84 ± 1,04 mg, kekerasan 8,54 ± 0,68 kg, kerapuhan 0,26% ± 0,04 dan waktu hancur 4,58 ± 0,17 menit.Kesimpulan: Proporsi MCC PH 101 80% dan laktosa 20% merupakan formula optimum terbaik dan memenuhi persyaratan karakteristik fisik tablet. (Health Science Indones 2013;1:32-6 Key words: formulasi, extract P. pellucida, optimalAbstractBackground: Peperomia pellucida has been widely used in traditional medicine. Recently, its existing forms are still conventional such as juice and infusum; therefore, it needs to be formulated more practically and

  8. The accuracy, precision and sustainability of different techniques for tablet subdivision: breaking by hand and the use of tablet splitters or a kitchen knife.

    Science.gov (United States)

    van Riet-Nales, Diana A; Doeve, Myrthe E; Nicia, Agnes E; Teerenstra, Steven; Notenboom, Kim; Hekster, Yechiel A; van den Bemt, Bart J F

    2014-05-15

    Tablets are frequently subdivided to lower the dose, to facilitate swallowing by e.g. children or older people or to save costs. Splitting devices are commonly used when hand breaking is difficult or painful. Three techniques for tablet subdivision were investigated: hand breaking, tablet splitter, kitchen knife. A best case drug (paracetamol), tablet (round, flat, uncoated, 500 mg) and operator (24-year student) were applied. Hundred tablets were subdivided by hand and by three devices of each of the following types: Fit & Healthy, Health Care Logistics, Lifetime, PillAid, PillTool, Pilomat tablet splitter; Blokker kitchen knife. The intra and inter device accuracy, precision and sustainability were investigated. The compliance to (adapted) regulatory requirements was investigated also. The accuracy and precision of hand broken tablets was 104/97% resp. 2.8/3.2% (one part per tablet considered; parts right/left side operator). The right/left accuracies of the splitting devices varied between 60 and 133%; the precisions 4.0 and 29.6%. The devices did not deteriorate over 100-fold use. Only hand broken tablets complied with all regulatory requirements. Health care professionals should realize that tablet splitting may result in inaccurate dosing. Authorities should undertake appropriate measures to assure good function of tablet splitters and, where feasible, to reduce the need for their use. Copyright © 2014 The Authors. Published by Elsevier B.V. All rights reserved.

  9. Evaluation of dacryocystorhinostomy using optical coherence tomography and rebamipide ophthalmic suspension

    Directory of Open Access Journals (Sweden)

    Fujimoto M

    2014-08-01

    Full Text Available Masahiro Fujimoto,1 Ken Ogino,1 Chika Miyazaki,1,2 Miou Hirose,1,3 Hiroko Matsuyama,1,4 Takeshi Moritera,1,5 Nagahisa Yoshimura1 1Department of Ophthalmology and Visual Sciences, Kyoto University Graduate School of Medicine, Kyoto, Japan; 2Department of Ophthalmology, Hyogo Prefectural Tsukaguchi Hospital, Hyogo, Japan; 3Department of Ophthalmology, Hyogo Prefectural Amagasaki Hospital, Hyogo, Japan; 4Department of Ophthalmology, National Hospital Organization Himeji Medical Center, Hyogo, Japan; 5Moritera Eye Clinic, Shiga, Japan Purpose: To evaluate the surgical outcome of dacryocystorhinostomy (DCR by measuring the tear meniscus, using optical coherence tomography and rebamipide ophthalmic suspension. Methods: Patients with nasolacrimal obstruction and chronic dacryocystitis who were scheduled for an endonasal DCR underwent tear meniscus examinations before and 2 months after surgery. Vertical scans of the inferior menisci were performed before and at 1, 3, 5, 7, and 10 minutes after the instillation of rebamipide ophthalmic suspension. The tear menisci areas were measured with imaging software. Ten young adults without epiphora formed the control group.Results: Anatomical success was achieved on 22 sides of 21 patients. The patients’ postoperative tear menisci were significantly smaller than the preoperative menisci at all points during the test, and the response to volume loading in the postoperative patients was corrected to nearly that of the young, healthy adults. Nevertheless, the postoperative meniscus area tended to be larger than that of the young adults at all points.Conclusion: The reduced tear meniscus area after DCR reflected the success of the surgical procedure. However, incomplete recovery of the meniscus after the test might suggest a residual disorder of the lacrimal drainage system after DCR. Keywords: dacryocystorhinostomy, tear meniscus, rebamipide, optical coherence tomography

  10. Respiratory outcomes following 100 mg/kg v. 200 mg/kg of poractant ...

    African Journals Online (AJOL)

    In keeping with current evidence, the initial dose of poractant alpha was increased from 100 mg/kg to 200 mg/kg. e outcomes of newborns requiring treatment with surfactant before and aer this change were reviewed. Methods. Electronic clinical records were reviewed of infants admitted to ACH who received surfactant ...

  11. Soy isoflavone tablets reduce osteoporosis risk factors and obesity in middle-aged Japanese women.

    Science.gov (United States)

    Mori, Mari; Aizawa, Toru; Tokoro, Minoru; Miki, Tomohiro; Yamori, Yukio

    2004-12-01

    1. This study examines whether the supplementation of isoflavones (ISO) exerts beneficial effects on the bone mineral density (BMD) measured by dual energy X-ray absorptiometry (DEXA). 2. Eighty-one healthy Japanese pre- and postmenopausal women were randomly assigned to the following two groups taking either ISO (100 mg) tablets (ISO group) or placebo tablets (P group) containing vitamins C (25 mg) and E (5 mg) daily for 24 weeks in a double-blind placebo controlled parallel design. 3. Seventy women completed the intervention study (34 on ISO, 36 on P), only ISO group was proven to increase significantly BMD (P osteoporosis and obesity and, thus to overall health promotion in menopausal women.

  12. REBAMIPIDE: EFFECTIVE DRUG PREVENTION OF NSAID ENTEROPATHY IS POSSIBLE

    OpenAIRE

    E. V. Moroz; A. E. Karateev

    2016-01-01

    Prevention of gastrointestinal tract (GIT) complications is the most important element for the rational use of nonsteroidal anti-inflammatory drugs (NSAIDs) and low-dose aspirin (LDA). Proton pump inhibitors (PPIs) have long been the only medication to prevent these complications. However, PPIs are only effective in preventing and treating upper GIT diseases (NSAID gastropathy) rather than small intestinal injury (NSAID enteropathy). Rebamipide has emerged as a novel agent to protect the gast...

  13. In vitro disintegration and dissolution studies of once-weekly copies of alendronate sodium tablets (70 mg) and in vivo implications.

    Science.gov (United States)

    Dansereau, Richard J; Crail, Debbie J; Perkins, Alan C

    2008-04-01

    The aim of this study was to evaluate the in vitro disintegration and dissolution of 26 alendronic acid tablets (70 mg) on the market in Canada, Germany, the Netherlands, and the United Kingdom compared to the branded product (Fosamax). The disintegration and dissolution times were determined using the methods described in the United States Pharmacopeia 30 (USP 30). The disintegration of four orally disintegrating tablets (non-bisphosphonates) and branded film-coated risedronate sodium tablets were included for comparison. The mean disintegration times of the alendronic acid tablets ranged from 14 s for Pharmachemie (Netherlands) to 342 s (5.7 min) for Betapharm (Germany). The mean disintegration time of the branded product tablets ranged from 43 to 78 s. Six of the 26 companies market alendronic acid tablets with very rapid disintegration times which are similar to those of orally disintegrating tablets (non-bisphosphonates). The alendronic acid tablets with very rapid mean disintegration times are as follows: Pharmachemie (Netherlands), 14 s; Novopharm (Canada), 13-24 s; GRY-Pharma (Germany), 21 s; Juta Pharma (Germany), 30 s; APS/Teva (United Kingdom), 26 and 37 s; and Teva (UK), 14-29 s. Since there is no established disintegration time for alendronic acid tablets there can be no assurance that the copy tablets are equivalent to the branded product in terms of esophageal drug exposure. However, the in vitro disintegration times have not been correlated with in vivo disintegration and performance. The dissolution of all the bisphosphonate tablets was rapid with greater than 80% dissolved in 15 min and all products conformed to the USP 30 specification. The dissolution of all alendronic acid tablets was rapid and complete and conformed to the established USP 30 specifications which should ensure adequate drug absorption from the copy products. However, copies of alendronic acid tablets are approved based on the results of single-dose bioavailability studies in

  14. Bioequivalence of a fixed-dose repaglinide/metformin combination tablet and equivalent doses of repaglinide and metformin tablets
.

    Science.gov (United States)

    Cho, Hea-Young; Ngo, Lien; Kim, Sang-Ki; Choi, Yoonho; Lee, Yong-Bok

    2018-06-01

    This study was conducted to determine whether a fixed-dose combination (FDC) tablet of repaglinide/metformin (2/500 mg) is equivalent to coadministration of equivalent doses of individual (EDI) tablets of repaglinide (2 mg) and metformin (500 mg) in healthy Korean male subjects. This study was conducted as an open-label, randomized, single-dose, two-period, two-sequence crossover design in 50 healthy Korean male subjects who received an FDC tablet or EDI tablets. Plasma concentrations of repaglinide and metformin were determined for up to 24 hours using a validated UPLC-MS/MS method. Bioequivalence was assessed according to current guidelines issued by the U.S. Food and Drug Administration (FDA) and Korean legislation. Tolerability was also evaluated throughout the study via subject interview, vital signs, and blood sampling. Point estimates (90% CIs) for AUC0-t, AUC0-∞, and Cmax based on EDI tablets were 110.07 (102.25 - 118.49), 109.90 (101.70 - 118.39), and 112.60 (101.49 - 124.85), respectively, for repaglinide. They were 95.18 (89.62 - 101.05), 95.00 (89.74 - 100.65), and 98.44 (92.72 - 104.50), respectively, for metformin. These results satisfied the bioequivalence criteria of 80.00 - 125.00% proposed by the FDA and Korean legislation. Results of pharmacokinetic analysis suggested that repaglinide and metformin in FDC tablets were bioequivalent to EDI tablets of repaglinide (2 mg) and metformin (500 mg) in healthy Korean male subjects. Both formulations appeared to be well tolerated.
.

  15. 21 CFR 520.1510 - Nitenpyram tablets.

    Science.gov (United States)

    2010-04-01

    ... and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... order of a licensed veterinarian. (d) Conditions of use—(1) Dogs—(i) Amount—(A) One 11.4-mg tablet for dogs weighing less than 25 pounds (lb) or one 57-mg tablet for dogs weighing more than 25 lb, as needed...

  16. Influence of dissolution media pH and USP1 basket speed on erosion and disintegration characteristics of immediate release metformin hydrochloride tablets.

    Science.gov (United States)

    Desai, Divyakant; Wong, Benjamin; Huang, Yande; Tang, Dan; Hemenway, Jeffrey; Paruchuri, Srinivasa; Guo, Hang; Hsieh, Daniel; Timmins, Peter

    2015-01-01

    To investigate the influence of the pH of the dissolution medium on immediate release 850 mg metformin hydrochloride tablets. A traditional wet granulation method was used to manufacture metformin hydrochloride tablets with or without a disintegrant. Tablet dissolution was conducted using the USP apparatus I at 100 rpm. In spite of its pH-independent high solubility, metformin hydrochloride tablets dissolved significantly slower in 0.1 N HCl (pH 1.2) and 50 mM pH 4.5 acetate buffer compared with 50 mM pH 6.8 phosphate buffer, the dissolution medium in the USP. Metformin hydrochloride API compressed into a round 1200 mg disk showed a similar trend. When basket rotation speed was increased from 100 to 250 rpm, the dissolution of metformin hydrochloride tablets was similar in all three media. Incorporation of 2% w/w crospovidone in the tablet formulation improved the dissolution although the pH-dependent trend was still evident, but incorporation of 2% w/w croscarmellose sodium resulted in rapid pH-independent tablet dissolution. In absence of a disintegrant in the tablet formulation, the dissolution was governed by the erosion-diffusion process. Even for a highly soluble drug, a super-disintegrant was needed in the formulation to overcome the diffusion layer limitation and change the dissolution mechanism from erosion-diffusion to disintegration.

  17. Development and Validation Dissolution Analytical Method of Nimesulide beta-Cyclodextrin 400 mg Tablet

    Directory of Open Access Journals (Sweden)

    Carlos Eduardo Carvalho Pereira

    2016-10-01

    Full Text Available The nimesulide (N-(4-nitro-2-phenoxyphenylmethanesulfonamide belongs to the class of non-steroidal anti-inflammatory drugs (NSAIDs and category II of the biopharmaceutical classification, The complexation of nimesulide with b-cyclodextrin is a pharmacological strategy to increase the solubility of the drug The objective of this study was to develop and validate an analytical methodology for dissolving the nimesulide beta-cyclodextrin 400 mg tablet and meets the guidelines of ANVISA for drug registration purposes. Once developed, the dissolution methodology was validated according to the RE of parameters no.  899/2003. In the development of the method it was noted that the duration of the dissolution test was 60 minutes, the volume and the most suitable dissolution medium was 900 mL of aqueous solution of sodium lauryl sulfate 1% (w/ v. It was also noted that rotation of 100 rpm and the paddle apparatus was the most appropriate to evaluate the dissolution of the drug. Spectrophotometric methodology was used to quantify the percentage of dissolved drug. The wavelength was 390 nm using the quantification. The validation of the methodology, system suitability parameters, specificity/selectivity, linearity, precision, accuracy and robustness were satisfactory and proved that the developed dissolution methodology was duly executed. DOI: http://dx.doi.org/10.17807/orbital.v8i5.827

  18. Formulation and in vitro evaluation of fast dissolving tablets of metoprolol tartrate

    Directory of Open Access Journals (Sweden)

    Mangesh Machhindranath Satpute

    2013-12-01

    Full Text Available The demand for fast dissolving tablets has been growing during the last decade, especially for elderly and children who have swallowing difficulties. In the present work, fast dissolving tablets of metoprolol tartrate, were prepared using sodium starch glycolate, sodium croscarmellose and crospovidone as superdisintegrants, by the direct compression method. The tablets prepared were evaluated for various parameters including weight variation, hardness, friability, in vitro dispersion time, drug-polymer interaction, drug content water absorption ratio, wetting time, in vitro drug release, FTIR and DSC studies. The tablets prepared by the direct compression method had a weight variation in the range of 145 mg to 152 mg, which is below ± 7.5%, a hardness of 3.6 kg/cm² to 4.5 kg/cm², percentage friability of 0.46% to 0.73%, in vitro dispersion time of 18 s to 125 s, drug content uniformity of between 98.12% and 100.03%, a water absorption ratio of 67% to 87%, wetting time of 32 sec. to 64 sec., and an in vitro drug release of 53.92% - 98.82% within 15 min. The IR spectral analysis and DSC study showed no drug interaction with formulation additives of the tablet, and the formulations indicated no significant changes in hardness, friability, drug content or in vitro drug release. Fast dissolving tablets of metoprolol tartrate have enhanced dissolution and will lead to improved bioavailability and more effective therapy.

  19. Improving the hardness of dry granulated tablets containing sodium lauryl sulfate.

    Science.gov (United States)

    Moore, Francis; Okelo, Geoffrey; Colón, Ivelisse; Kushner, Joseph

    2010-11-15

    The impact of the addition of a wetting agent, the surfactant sodium lauryl sulfate (SLS), on the tablet hardness of a dry granulated, solid oral dosage form was investigated. In three batches, SLS was added concurrently with: (1) a poorly soluble, highly hydrophobic active pharmaceutical ingredient (API) and the other excipients prior to the initial blending step, (2) magnesium stearate prior to roller compaction, or (3) magnesium stearate prior to tableting. A fourth batch, which did not contain SLS, served as a control. The maximum hardness of 100 mg, 1/4″-SRC tablets for the four batches--SLS added initially, prior to roller compaction, prior to tableting, and no SLS--were 61±3, 71±3, 89±5, and 86±3N, respectively, suggesting reduced processing of SLS improves tablet hardness by ∼50%. Dissolution of the tablets in 900 ml of simulated gastric fluid with paddles at 75 rpm showed that: (1) there was no impact on the insertion point of SLS into the process on API dissolution, and (2) that the presence of SLS improved dissolution by 5% compared to the control tablets. Adding SLS just prior to tableting can improve tablet hardness and yield similar dissolution performance relative to SLS addition prior to the initial blending step. Copyright © 2010 Elsevier B.V. All rights reserved.

  20. Relative bioavailability of a newly developed 5-mg levomethadone hydrochloride IR tablet (L-Polamidon® 5 mg tablets) in comparison with the 5-mg levomethadone hydrochloride oral solution (L-Polamidon® solution for substitution) as reference product.

    Science.gov (United States)

    Blume, Henning H; Wedemeyer, Ralf-Steven; Donath, Frank; Roscher, Katrin; Elvert, Gerd; Wagner, Daniel; Bley, Oliver; Vuia, Alexander; Todorova-Sanjari, Marina; Villalobos, Ramon; Schug, Barbara

    2015-04-01

    To establish the relative bioavailability (rBA) between two p.o. 5-mg levomethadone hydrochloride formulations, i.e., L-Polamidon® 5 mg tablets (test) vs. L-Polamidon® solution for substitution (reference). To assess the safety and tolerability of both formulations. A total of 33 healthy male subjects, aged 29 ± 6 years (BMI: 23.9 ± 2.5 kg/m2) completed this single center, open-label, randomized, 2-period cross-over study with single dose administrations under fasting conditions and coadministration with naltrexone for safety reasons. Administrations of both investigational products were separated by a washout period of at least 2 weeks, i.e., 13 treatmentfree days. The total dose for each subject was 2 x 5 mg resulting in 10 mg levomethadone hydrochloride. For pharmacokinetic evaluation, blood samples were withdrawn until 72 hours postdose. A validated non-stereoselective liquid chromatography-tandem mass spectroscopy method (LC-MS/MS) was applied for the determination of levomethadone in plasma. The lower limit of quantitation was 0.100 ng/mL. Adverse events were descriptively analyzed in the study population. The geometric means of the parameters related with the extent of total exposure of levomethadone, i.e., AUC(0-tlast) and AUC(0-∞), were 244.422 ng x h/mL and 332.999 ng x h/mL for test and 246.837 ng x h/mL and 329.467 ng×h/mL for reference, respectively. The geometric means of the peak exposure for levomethadone, i.e., Cmax, were 8.923 ng/mL for test and 8.635 ng/mL for reference. The point estimates (PEs) of the Test/Reference (T/R) adjusted geometric mean ratios of AUC(0-last), AUC(0-∞), and C(max) were 99.20%, 101.42%, and 104.11%, respectively, and all of them showed 90%-confidence intervals (CIs) within the range of 80.00 - 125.00% as suggested by regulatory requirements for bioequivalence assessment In total, 21 subjects experienced 55 AEs during the study, the most frequently reported AE, i.e., headache, accounted for 13 out of the total

  1. A randomised comparison of oral desmopressin lyophilisate (MELT) and tablet formulations in children and adolescents with primary nocturnal enuresis

    DEFF Research Database (Denmark)

    Lottmann, H; Froeling, F; Alloussi, S

    2007-01-01

    (MELT) vs. tablet treatment, and the efficacy, safety, compliance and ease of use associated with each formulation. In total, 221 patients aged 5-15 years who were already receiving desmopressin tablets were randomised 1 : 1 to receive desmopressin treatment in the order MELT/tablet (n = 110) or tablet....../MELT (n = 111) for 3 weeks each. Each formulation was administered in bioequivalent doses (0.2/0.4 mg tablets identical with 120/240 microg MELT). Following treatment, patients were questioned regarding treatment preference. Diary card data and 100 mm Visual Analogue Scale scores were also recorded....... RESULTS: Overall, patients preferred the MELT formulation to the tablet (56% vs. 44%; p = 0.112). This preference was age dependent (p = 0.006); patients aged

  2. A double-blind comparison of slow-release and standard tablet formulations of fentiazac in the treatment of patients with tendinitis and bursitis.

    Science.gov (United States)

    Ginsberg, F; Famaey, J P

    1985-01-01

    Two double-blind studies were carried out to compare the effectiveness and tolerance of a slow-release tablet formulation of 300 mg fentiazac, given once daily, with the standard tablet formulations of 100 mg, given 4-times daily, or 200 mg, given twice daily. A total of 60 patients suffering from acute bicipital tendinitis and/or subdeltoid bursitis was studied, 15 patients on the slow-release and 15 on one of the two standard tablets in each of the two trials. Patients were assessed on entry and at Days 7 and 14 of treatment. The results in both studies showed that there was significant improvement in tenderness, pain on movement, overall pain and in the range of movement after treatment, there being no significant difference between those receiving the slow-release form or the standard tablets. Tolerance was good in all groups and only a few minor or moderate side-effects, mainly of a gastro-intestinal type, were reported.

  3. [Titration comparative study of TOPINA Tablets in patients with localization related epilepsy: double-blind comparative study by rapid and slow titration methods].

    Science.gov (United States)

    Kaneko, Sunao; Inoue, Yushi; Sasagawa, Mutsuo; Kato, Masaaki

    2012-04-01

    To compare the tolerability and efficacy of two titration methods (rapid and slow titration) for TOPINA Tablets with different dosages and periods of escalation, a double-blind comparative study was conducted in patients with localization-related epilepsy. A total of 183 patients were randomized to either rapid titration (initial dosage 100 mg/day increased by 100-200 mg at weekly intervals) or to slow titration (initial dosage 50 mg/day increased in 50 mg/day increments at weekly intervals). TOPINA Tablets were administered for 12 weeks to the maximum dosage of 400 mg/day. The incident of adverse events leading to treatment interruptions or withdrawals was 18.9% in rapid titration and 14.8% in slow titration, with no statistical significance (p = 0.554). The incident of adverse events and adverse reactions of slow titration was slightly lower than that of rapid titration. The common adverse events and adverse reactions reported in the two titration methods were comparable and were well tolerated. On the other hand, the efficacy of slow titration, percent reduction in seizure rate and responder rate, was comparable with that of rapid titration. In conclusion, there were no significant differences of therapeutic response to TOPINA Tablets between the two titration methods.

  4. MgO monolayer epitaxy on Ni (100)

    Science.gov (United States)

    Sarpi, B.; Putero, M.; Hemeryck, A.; Vizzini, S.

    2017-11-01

    The growth of two-dimensional oxide films with accurate control of their structural and electronic properties is considered challenging for engineering nanotechnological applications. We address here the particular case of MgO ultrathin films grown on Ni (100), a system for which neither crystallization nor extended surface ordering has been established previously in the monolayer range. Using Scanning Tunneling Microscopy and Auger Electron Spectroscopy, we report on experiments showing MgO monolayer (ML) epitaxy on a ferromagnetic nickel surface, down to the limit of atomic thickness. Alternate steps of Mg ML deposition, O2 gas exposure, and ultrahigh vacuum thermal treatment enable the production of a textured film of ordered MgO nano-domains. This study could open interesting prospects for controlled epitaxy of ultrathin oxide films with a high magneto-resistance ratio on ferromagnetic substrates, enabling improvement in high-efficiency spintronics and magnetic tunnel junction devices.

  5. Investigation of the effect of the rebamipide mouthwash on the crisis of the stomatitis induced by the cancer chemotherapy and/or radiotherapy

    International Nuclear Information System (INIS)

    Kawata, Keishi; Hanawa, Takehisa; Hanawa, Kazumi

    2001-01-01

    Stomatitis is well-known as one of the undesirable side effects induced by high and/or multiple dosing of cytotoxic drugs such as 5-fluorouracil (5-FU). Stomatitis causes pain in the oral cavity, impaired swallowing or loss of appetite, and finally, lowering of the quality of life (QOL) of patients. In this study, we attempted to apply a new mouthwash containing rebamipide (REB) which is known as the anti-activated oxygen agent. Rebamipide mouthwash (REB-M) showed the effectiveness to the crisis of the stomatitis during the cancer chemotherapy and/or radiotherapy. (author)

  6. A fixed-dose combination tablet of gemigliptin and metformin sustained release has comparable pharmacodynamic, pharmacokinetic, and tolerability profiles to separate tablets in healthy subjects

    Directory of Open Access Journals (Sweden)

    Park SI

    2015-02-01

    Full Text Available Sang-In Park,1,* Howard Lee,1,2,* Jaeseong Oh,1 Kyoung Soo Lim,3 In-Jin Jang,1 Jeong-Ae Kim,4 Jong Hyuk Jung,4 Kyung-Sang Yu1 1Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, 2Department of Transdisciplinary Studies, Graduate School of Convergence Science and Technology, Seoul National University, Clinical Trials Center, Seoul National University Hospital, Seoul, 3Department of Clinical Pharmacology and Therapeutics, CHA University School of Medicine and CHA Bundang Medical Center, Seongnam, 4LG Life Sciences, Ltd, Seoul, Republic of Korea *These authors contributed equally to this work Background: In type 2 diabetes mellitus, fixed-dose combination (FDC can provide the complementary benefits of correction of multiple pathophysiologic defects such as dysfunctions in glycemic or metabolic control while improving compliance compared with separate tablets taken together. The objective of the study reported here was to compare the pharmacodynamic (PD, pharmacokinetic (PK, and tolerability profiles of gemigliptin and extended-release metformin (metformin XR between FDC and separate tablets.Methods: A randomized, open-label, single-dose, two-way, two-period, crossover study was conducted in 28 healthy male volunteers. Two FDC tablets of gemigliptin/metformin 25/500 mg or separate tablets of gemigliptin (50 mg ×1 and metformin XR (500 mg ×2 were orally administered in each period. Serial blood samples were collected up to 48 hours post-dose to determine dipeptidyl peptidase 4 (DPP-4 activity using spectrophotometric assay and concentrations of gemigliptin and metformin using tandem mass spectrometry. Geometric mean ratios (GMRs of FDC to separate tablet formulations and their 90% confidence intervals (CIs were calculated to compare the PD and PK parameters between the two formulations. Tolerability was assessed throughout the study.Results: The plasma DPP-4 activity

  7. Evaluation of two novel tablet formulations of artemether-lumefantrine (Coartem) for bioequivalence in a randomized, open-label, two-period study.

    Science.gov (United States)

    Lefèvre, Gilbert; Bhad, Prafulla; Jain, Jay Prakash; Kalluri, Sampath; Cheng, Yi; Dave, Hardik; Stein, Daniel S

    2013-09-08

    Artemether-lumefantrine (Coartem; AL) is a standard of care for malaria treatment as an oral six-dose regimen, given twice daily over three days with one to four tablets (20/120 mg) per dose, depending on patient body weight. In order to reduce the pill burden at each dose and potentially enhance compliance, two novel fixed-dose tablet formulations (80/480 mg and 60/360 mg) have been developed and tested in this study for bioequivalence with their respective number of standard tablets. A randomized, open-label, two-period, single-dose, within formulation crossover bioequivalence study comparing artemether and lumefantrine exposure between the novel 80/480 mg tablet and four standard tablets, and the novel 60/360 mg tablet and three standard tablets, was conducted in 120 healthy subjects under fed conditions. Artemether, dihydroartemisinin, and lumefantrine were measured in plasma by HPLC/UPLC-MS/MS. Pharmacokinetic (PK) parameters were determined by non-compartmental analyses. Adjusted geometric mean AUClast for artemether were 345 and 364 ng·h/mL (geometric mean ratio (GMR) 0.95; 90% CI 0.89-1.01) and for lumefantrine were 219 and 218 μg·h/mL (GMR 1.00; 90% CI 0.93-1.08) for 80/480 mg tablet versus four standard tablets, respectively. Corresponding Cmax for artemether were 96.8 and 99.7 ng/mL (GMR 0.97; 90% CI 0.89-1.06) and for lumefantrine were 8.42 and 8.71 μg/mL (GMR 0.97; 90% CI 0.89-1.05). For the 60/360 mg tablet versus three standard tablets, adjusted geometric mean AUClast for artemether were 235 and 231 ng·h/mL (GMR 1.02; 90% CI 0.94-1.10), and for lumefantrine were 160 and 180 μg·h/mL (GMR 0.89; 90% CI 0.83-0.96), respectively. Corresponding Cmax for artemether were 75.5 and 71.5 ng/mL (GMR 1.06; 90% CI 0.95-1.18), and for lumefantrine were 6.64 and 7.61 μg/mL (GMR 0.87; 90% CI 0.81-0.94), respectively. GMR for Cmax and AUClast for artemether and lumefantrine for all primary comparisons were within the bioequivalence acceptance criteria (0

  8. Double-layer Tablets of Lornoxicam: Validation of Quantification ...

    African Journals Online (AJOL)

    Double-layer Tablets of Lornoxicam: Validation of Quantification Method, In vitro Dissolution and Kinetic Modelling. ... Satisfactory results were obtained from all the tablet formulations met compendial requirements. The slowest drug release rate was obtained with tablet cores based on PVP K90 (1.21 mg%.h-1).

  9. Efficacy of On-Demand Therapy Using 20-mg Vonoprazan for Mild Reflux Esophagitis.

    Science.gov (United States)

    Umezawa, Mariko; Kawami, Noriyuki; Hoshino, Shintaro; Hoshikawa, Yoshimasa; Koizumi, Eriko; Takenouchi, Nana; Hanada, Yuriko; Kaise, Mitsuru; Iwakiri, Katsuhiko

    2018-01-01

    The study aimed to evaluate the efficacy of on-demand therapy using 20-mg vonoprazan for mild reflux esophagitis (RE). On-demand therapy by taking one 20-mg tablet of vonoprazan only when reflux symptoms occurred was performed for 24 weeks using 30 patients with mild RE who were receiving maintenance therapy with proton pomp inhibitors (PPIs). The presence or absence of RE, degree of overall satisfaction with the treatment, score of symptoms, and fasting gastrin level before breakfast were examined before and after on-demand therapy. The number of tablets taken during the 24-week period was also noted. One of the 30 patients dropped out of on-demand therapy 1 week after its initiation. Remission was maintained in 25 (86.2%) of the 29 patients (all 10 [100%] Los Angeles classification grade A patients and 15 (78.9%) of the 19 grade B patients). However, 4 grade B patients exhibited grade B relapse. There were no differences in the degree of overall satisfaction, score of symptoms or the gastrin level between PPI and on-demand therapies. The number of vonoprazan tablets taken during the observation period was 33 tablets (median)/24 weeks. On-demand therapy using 20-mg vonoprazan tablets is an effective alternative maintenance therapy for mild RE. © 2018 S. Karger AG, Basel.

  10. Preparation and evaluation of enteric coated tablets of hot-melt extruded lansoprazole.

    Science.gov (United States)

    Alsulays, Bader B; Kulkarni, Vijay; Alshehri, Sultan M; Almutairy, Bjad K; Ashour, Eman A; Morott, Joseph T; Alshetaili, Abdullah S; Park, Jun-Bom; Tiwari, Roshan V; Repka, Michael A

    2017-05-01

    The objective of this work was to use hot-melt extrusion (HME) technology to improve the physiochemical properties of lansoprazole (LNS) to prepare stable enteric coated LNS tablets. For the extrusion process, we chose Kollidon ® 12 PF (K12) polymeric matrix. Lutrol ® F 68 was selected as the plasticizer and magnesium oxide (MgO) as the alkalizer. With or without the alkalizer, LNS at 10% drug load was extruded with K12 and F68. LNS changed to the amorphous phase and showed better release compared to that of the pure crystalline drug. Inclusion of MgO improved LNS extrudability and release and resulted in over 80% drug release in the buffer stage. Hot-melt extruded LNS was physically and chemically stable after 12 months of storage. Both formulations were studied for compatibility with Eudragit ® L100-55. The optimized formulation was compressed into a tablet followed by coating process utilizing a pan coater using L100-55 as an enteric coating polymer. In a two-step dissolution study, the release profile of the enteric coated LNS tablets in the acidic stage was less than 10% of the LNS, while that in the buffer stage was more than 80%. Drug content analysis revealed the LNS content to be 97%, indicating the chemical stability of the enteric coated tablet after storage for six months. HME, which has not been previously used for LNS, is a valuable technique to reduce processing time in the manufacture of enteric coated formulations of an acid-sensitive active pharmaceutical ingredient as compared to the existing methods.

  11. In vitro release kinetics of Tolmetin from tabletted Eudragit microparticles.

    Science.gov (United States)

    Pignatello, R; Consoli, P; Puglisi, G

    2000-01-01

    In a previous paper the preparation has been described, by three different techniques, of microparticles made of Eudragit RS 100 and RL 100 containing a NSAI agent, Tolmetin. Freely flowing microparticles failed to affect significantly the in vitro drug release, which displayed a similar dissolution profile after micro-encapsulation to the free drug powder. Microparticles were then converted into tablets and the effect of compression on drug delivery, as well as that of the presence of co-additives, was studied in the present work. Furthermore, microparticles were also prepared by adding MgO to the polymer matrix, to reduce the sensitivity of the drug to pH changes during its dissolution. Similarly, magnesium stearate was also used for microparticle formation as a droplet stabilizer, in order to reduce particle size and hinder rapid drug release. A mathematical evaluation, by using two semi-empirical equations, was applied to evaluate the influence of dissolution and diffusion phenomena upon drug release from microparticle tablets.

  12. 21 CFR 520.1200 - Ivermectin, fenbendazole, and praziquantel tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ivermectin, fenbendazole, and praziquantel tablets... Ivermectin, fenbendazole, and praziquantel tablets. (a) Specifications. Each chewable tablet contains either: (1) 68 micrograms (µg) ivermectin, 1.134 grams fenbendazole, and 57 milligrams (mg) praziquantel; or...

  13. Bioavailability of syrup and tablet formulations of cefetamet pivoxil.

    Science.gov (United States)

    Ducharme, M P; Edwards, D J; McNamara, P J; Stoeckel, K

    1993-12-01

    Two studies examining the bioavailability of cefetamet pivoxil in healthy male subjects were conducted. In the first, the bioavailabilities of the 250-mg (M250) and M500 tablet formulations of cefetamet pivoxil to be marketed were compared with that of a tablet used in clinical trials. All products were given with food at a dose of 500 mg. In the second study, the bioavailability of the syrup formulation was evaluated under both fasting and nonfasting conditions and compared with that of the M500 tablet formulation given with food. The absolute bioavailabilities of the M500 and M250 tablets (55.0% +/- 8.0% and 55.7% +/- 7.0%, respectively) were not significantly different from that of the clinical-trial formulation (49.8% +/- 8.5%). The newer tablet formulations exhibited faster absorption as evidenced by higher peak concentrations (3.8 [M500] and 3.9 [M250] mg/liter compared with 3.2 mg/liter for the clinical-trial formulation), a shorter time to peak concentration, and a shorter mean absorption time. The syrup formulation was found to have significantly lower absolute bioavailability (37.9% +/- 6.0%) compared with that of the M500 tablet (58.4% +/- 9.0%) when both were given with food. Food had no significant effect on the bioavailability of the syrup, which averaged 34.0% +/- 8.6% under fasting conditions, although absorption was delayed by food (mean absorption time increased from 2.2 to 3.9 h). This contrasts with the results of previous studies documenting significant increases in tablet bioavailability with food. Despite the lower bioavailability of the syrup, unbound-cefetamet concentrations are expected to remain above the MICs for 90% of the strains tested for susceptible organisms for approximately 10 h of the usual 12-h dosing interval with both syrup and tablet formulations of cefetamet pivoxil given with food.

  14. Cladribine tablets for relapsing-remitting multiple sclerosis

    DEFF Research Database (Denmark)

    Rammohan, Kottil; Giovannoni, Gavin; Comi, Giancarlo

    2012-01-01

    BACKGROUND: In the phase III CLARITY study, treatment with cladribine tablets at cumulative doses of 3.5 or 5.25mg/kg over 96 weeks led to significant reductions in annualized relapse rates (ARR) versus placebo in patients with relapsing-remitting multiple sclerosis. Further post hoc analyses...... of CLARITY study data were conducted to determine the efficacy of cladribine tablets across patient subgroups stratified by baseline characteristics. METHODS: Relapse rates over the 96-week CLARITY study were analyzed in cohorts stratified by demographics; disease duration; treatment history and disease...... activity at baseline. RESULTS: In the intent-to-treat population (n=437, 433 and 456 in the placebo, cladribine 3.5 and 5.25mg/kg groups, respectively), treatment with cladribine tablets 3.5 and 5.25mg/kg led to consistent improvements in ARR versus placebo in patients stratified by gender; age (≤40...

  15. Pharmacokinetics of pediatric lopinavir/ritonavir tablets in children when administered twice daily according to FDA weight bands

    NARCIS (Netherlands)

    Bastiaans, D.E.T.; Forcat, S.; Lyall, H.; Cressey, T.R.; Hansudewechakul, R.; Kanjanavanit, S.; Noguera-Julian, A.; Konigs, C.; Inshaw, J.R.; Chalermpantmetagul, S.; Saidi, Y.; Compagnucci, A.; Harper, L.M.; Giaquinto, C.; Colbers, A.P.; Burger, D.M.

    2014-01-01

    BACKGROUND: Lopinavir/ritonavir (LPV/r) pediatric tablets (100/25 mg) are approved by the United States Food and Drug Administration (FDA) and European Medicines Agency (EMA) as part of combination antiretroviral therapy. Dosing is based on body weight bands or body surface area under FDA approval

  16. Formulation development and optimization of sustained release matrix tablet of Itopride HCl by response surface methodology and its evaluation of release kinetics.

    Science.gov (United States)

    Bose, Anirbandeep; Wong, Tin Wui; Singh, Navjot

    2013-04-01

    The objective of this present investigation was to develop and formulate sustained release (SR) matrix tablets of Itopride HCl, by using different polymer combinations and fillers, to optimize by Central Composite Design response surface methodology for different drug release variables and to evaluate drug release pattern of the optimized product. Sustained release matrix tablets of various combinations were prepared with cellulose-based polymers: hydroxy propyl methyl cellulose (HPMC) and polyvinyl pyrolidine (pvp) and lactose as fillers. Study of pre-compression and post-compression parameters facilitated the screening of a formulation with best characteristics that underwent here optimization study by response surface methodology (Central Composite Design). The optimized tablet was further subjected to scanning electron microscopy to reveal its release pattern. The in vitro study revealed that combining of HPMC K100M (24.65 MG) with pvp(20 mg)and use of LACTOSE as filler sustained the action more than 12 h. The developed sustained release matrix tablet of improved efficacy can perform therapeutically better than a conventional tablet.

  17. Product development of pumpkin tablet

    Directory of Open Access Journals (Sweden)

    Kamgoed, T.

    2007-05-01

    Full Text Available The development of pumpkin tablet was studied and the drying conditions of pumpkin using a double drum dryer were optimized. The study factors were drying agents (maltodextrin D.E.13-16 andtapioca flour at different levels (3 and 5%, drying temperatures (130 and 140oC and drum dryer speeds (4 and 5 rpm. The results showed that the optimal conditions were using 3% maltodextrin D.E.13-16, dryingtemperature of 130oC and drum dryer speed of 4 rpm. The moisture, fat, bulk density, reducing sugars and granulometric retention of the obtained pumpkin powder were 3.39%, 1.42%, 1.004 g/ml, 12.63% and 0.67%, respectively and L*, a* and b* values were 73.85, -0.60 and 35.23, respectively. A study of suitable amount of icing sugar using different contents for tablet production (0, 10, 20, 30 and 40% was performedand showed that using 20% icing sugar was the most acceptable. The obtained pumpkin tablet was subjected to chemical, physical and microbiological analysis. The ash, moisture, protein, fat, fiber and carbohydratecontents were 1.87, 3.60, 3.34, 1.00, 2.26 and 87.99%, respectively. The reducing sugars and β-carotene contents were 5.44±0.61% and 3.79±0.57 mg/100g, respectively. The Aw, hardness and solubility were 0.56,3.25 kgf and 25.00 %, respectively. The L*, a* and b* values were 79.85, 0.28 and 23.64, respectively. The total microbial count and the yeast and mould count were <10 CFU/g. The shelf life of the pumpkin tabletwas at least 4 months at room temperature (35±2oC.

  18. Tetracycline treatment of type III prostatitis nanobacteria infection of 100 cases report

    Science.gov (United States)

    Guo, Junyi; Li, Chongxian; Wu, Baisuo; Hao, Shaojun; Ming, Aimin; Zhang, Xinji; Li, Wenjun; Zhang, Zhengchen

    2018-04-01

    To investigate the efficacy of tetracycline treatment of nanobacterial infection in 100 cases of type III prostatitis. randomly divided into treatment group and control group with double blind method, the treatment group was given Tetracycline Tablets 250mg, oral, 2 times a day; the control group were treated with Levofloxacin Tablets 0.lg, oral, 2 times a day; observation of curative effect of two groups of patients after 1 months of treatment. after the treatment group patients NIH-CPSI score and pain, urinary symptoms and quality of life scores were significantly lower than that of control group (Pprostate fluid and cultured positive cases of nanobacterial numbers were 21 (21%) and 100 cases (100%), the positive rate of nanobacteria in observation group was significantly lower than the control group (Pprostatitis.

  19. [Effect of food thickener on disintegration and dissolution of magnesium oxide tablets].

    Science.gov (United States)

    Tomita, Takashi; Goto, Hidekazu; Yoshimura, Yuya; Tsubouchi, Yoshiko; Nakanishi, Rie; Kojima, Chikako; Yoneshima, Mihoko; Yoshida, Tadashi; Tanaka, Katsuya; Sumiya, Kenji; Kohda, Yukinao

    2015-01-01

    It has been reported that magnesium oxide tablets are excreted in a non-disintegrated state in the stool of patients when the tablets are administered after being immersed in a food thickener. Therefore we examined whether immersion in a food thickener affects the pharmacological effect in patients taking magnesium oxide tablets, and whether immersion affects its disintegration and solubility. The mean dosage (1705 mg/d) was higher for patients who took tablets after immersion in a food thickener than for those who took non-immersed tablets (1380 mg/d). The disintegration time and dissolution rate of the immersed tablets were lower than those of non-immersed tablets in vitro. Furthermore, components that constitute the food thickener and differences in composition concentrations differentially affect the disintegration and solubility of magnesium oxide tablets. This suggests that commercially available food thickeners are likely to be associated with changes in the degradation of magnesium oxide tablets, and they therefore should be carefully used in certain clinical situations.

  20. A Pharmacokinetic Bioequivalence Study Comparing Pirfenidone Tablet and Capsule Dosage Forms in Healthy Adult Volunteers.

    Science.gov (United States)

    Pan, Lin; Belloni, Paula; Ding, Han Ting; Wang, Jianshuang; Rubino, Christopher M; Putnam, Wendy S

    2017-09-01

    Pirfenidone film-coated tablets were developed to offer an alternative to the marketed capsule formulation. This study assessed the bioequivalence of the tablet and capsule formulations under fed and fasted states. A Phase I, open-label, randomized, four-treatment-period, four-sequence, crossover pharmacokinetics study (NCT02525484) was conducted. Each subject received an 801-mg single dose of pirfenidone as three 267-mg capsules or one 801-mg tablet under fasted and fed conditions. Pirfenidone plasma C max , AUC 0-t and AUC 0-∞ were used to assess bioequivalence. Forty-four subjects were randomized to treatment. The 801-mg tablet in the fasted state met bioequivalence criteria [90% confidence intervals (CI) 80.00-125.00%] for the GLSM ratios of natural log-transformed C max , AUC 0-t and AUC 0-∞ . Under fed conditions, the 801-mg tablet met the bioequivalence criteria for AUC 0-t and AUC 0-∞ , but slightly exceeded the bioequivalence criteria for the C max (90% CI of 108.26-125.60%). The tablet C max was approximately 17% higher than that of the capsules. In the fed state, the tablet C max , and both AUC 0-t and AUC 0-∞ were reduced by 39% and 17%, respectively, relative to the fasted state. The tablet and capsules had acceptable tolerability profiles. The pirfenidone 801-mg tablet met bioequivalence criteria when compared with three 267-mg capsules in the fasted state. The tablet C max was slightly higher relative to capsules in the fed state, but this is not expected to have a clinically meaningful impact on the benefit-risk profile of pirfenidone. This work was supported by F. Hoffmann-La Roche Ltd.

  1. Single Layer Extended Release Two-in-One Guaifenesin Matrix Tablet: Formulation Method, Optimization, Release Kinetics Evaluation and Its Comparison with Mucinex® Using Box-Behnken Design.

    Science.gov (United States)

    Morovati, Amirhosein; Ghaffari, Alireza; Erfani Jabarian, Lale; Mehramizi, Ali

    2017-01-01

    Guaifenesin, a highly water-soluble active (50 mg/mL), classified as a BCS class I drug. Owing to its poor flowability and compressibility, formulating tablets especially high-dose one, may be a challenge. Direct compression may not be feasible. Bilayer tablet technology applied to Mucinex®, endures challenges to deliver a robust formulation. To overcome challenges involved in bilayer-tablet manufacturing and powder compressibility, an optimized single layer tablet prepared by a binary mixture (Two-in-one), mimicking the dual drug release character of Mucinex ® was purposed. A 3-factor, 3-level Box-Behnken design was applied to optimize seven considered dependent variables (Release "%" in 1, 2, 4, 6, 8, 10 and 12 h) regarding different levels of independent one (X 1 : Cetyl alcohol, X 2 : Starch 1500 ® , X 3 : HPMC K100M amounts). Two granule portions were prepared using melt and wet granulations, blended together prior to compression. An optimum formulation was obtained (X 1 : 37.10, X 2 : 2, X 3 : 42.49 mg). Desirability function was 0.616. F2 and f1 between release profiles of Mucinex® and the optimum formulation were 74 and 3, respectively. An n-value of about 0.5 for both optimum and Mucinex® formulations showed diffusion (Fickian) control mechanism. However, HPMC K100M rise in 70 mg accompanied cetyl alcohol rise in 60 mg led to first order kinetic (n = 0.6962). The K values of 1.56 represented an identical burst drug releases. Cetyl alcohol and starch 1500 ® modulated guaifenesin release from HPMC K100M matrices, while due to their binding properties, improved its poor flowability and compressibility, too.

  2. Formulation and Evaluation of Fast-Disintegrating Sublingual Tablets of Atropine Sulfate: the Effect of Tablet Dimensions and Drug Load on Tablet Characteristics.

    Science.gov (United States)

    Aodah, Alhussain; Bafail, Rawan S; Rawas-Qalaji, Mutasem

    2017-07-01

    In this study, we formulated and evaluated the effects of tablet dimensions and drug load on the characteristics of atropine sulfate (AS) fast-disintegrating sublingual tablets (FDSTs). We aim to develop AS FDSTs as an alternative non-invasive and portable dosage form for the emergency treatment of organophosphate (OP) toxicity. AS autoinjector, AtroPen®, is the only self-administered dosage form available as an antidote for-out-of-hospital emergency use, but it is associated with several limitations and drawbacks. Seven FDST formulations of two tablet sizes, 150 mg (A) and 50 mg (B), and of several AS loads, 0 mg (A1, B1), 2 mg (A2, B2), 4 mg (B3), and 8 mg (B4a, B4b), were formulated and manufactured by direct compression. AS FDST characteristics were evaluated using USP and non-USP tests. Results were statistically compared at p < 0.05. All FDSTs passed the USP content uniformity and friability tests, disintegrated and released AS in ≤30 and 60 s. B1 and B2 were significantly harder than A1 and A2. Water uptake of A1 was significantly the highest. However, B1 and B2 had shorter disintegration and wetting times and higher amounts of AS dissolved than did A1 and A2 (p < 0.05). Increasing AS negatively affected FDST tensile strength (p < 0.05 for B4a) and water uptake (p < 0.05 for B3, B4a and B4b), however, without affecting AS dissolution. Formulation of AS up to 16% into smaller FDSTs was successful. Smaller FDSTs were harder and disintegrated more quickly. These AS FDSTS have the potential for further in vivo testing to evaluate their OP antidote potential.

  3. Methylene blue MMX® tablets for chromoendoscopy. Bioavailability, colon staining and safety in healthy volunteers undergoing a full colonoscopy.

    Science.gov (United States)

    Di Stefano, A F D; Radicioni, M M; Vaccani, A; Fransioli, A; Longo, L; Moro, L; Repici, A

    2018-06-01

    Methylene blue-MMX® tablets are proposed as an aid for detection and visualisation of adenomas and carcinomas in patients undergoing colonoscopy, by improving their detection rate and highlighting the presence of the intestinal dysplastic lesions. Single total doses of 100 and 200 mg were administered to healthy volunteers undergoing a bowel cleansing preparation and a full colonoscopy to investigate the colonic staining. The pharmacokinetics of methylene blue and the safety after exposure to the tablets were also investigated. With 200 mg, the best staining, assessed as the sum of acceptable and good staining, was achieved in the ascending colon and rectosigmoid (75% subjects each), the transverse and the descending colon (approximately 63% each). Absence of staining or overstaining were reported for no colonic region of interest in any subject. Similar results were observed in the 100mg dose group. Methylene blue blood concentrations reached a peak (C max ) in a median time (T max ) of 12 h with 100mg and 16 h with 200 mg. AUC 0-t was 10.7 ± 6.7 μg/mLxh after 100mg and 25.2 ± 7.4 μg/mLxh after 200 mg. Half-life ranged between 9 and 22 h after the lower dose and between 6 and 26 h after the higher dose. The cumulative excretion was about 28% after 100mg and about 39% after 200 mg. The overall frequency of adverse events was 39%, but only one was related to the product: abnormal transaminases. The most frequent adverse event was a transient polyuria (17%). One serious adverse event (gastrointestinal haemorrhage) led the subject to study discontinuation and hospitalisation and another subject withdrew the study due to one adverse event (haematemesis). Either event was not related to methylene blue. Copyright © 2017. Published by Elsevier Inc.

  4. Chemoinformetrical evaluation of dissolution property of indomethacin tablets by near-infrared spectroscopy.

    Science.gov (United States)

    Otsuka, Makoto; Tanabe, Hideaki; Osaki, Kazuo; Otsuka, Kuniko; Ozaki, Yukihiro

    2007-04-01

    The purpose of this study was to use near-infrared spectrometry (NIR) with chemoinformetrics to predict the change of dissolution properties in indomethacin (IMC) tablets during the manufacturing process. A comparative evaluation of the dissolution properties of the tablets was performed by the diffused reflectance (DRNIR) and transmittance (TNIR) NIR spectroscopic methods. Various kinds of IMC tablets (200 mg) were obtained from a powder (20 mg of IMC, 18 mg of microcrystalline cellulose, 160 mg of lactose, and 2 mg of magnesium stearate) under various compression pressures (60-398 MPa). Dissolution tests were performed in phosphate buffer, and the time required for 75% dissolution (T75) and mean dissolution time (MDT) were calculated. DRNIR and TNIR spectra were recorded, and the both NIR spectra used to establish a calibration model for predicting the dissolution properties by principal component regression analysis (PCR). The T75 and MDT increased as the compression pressure increased, since tablet porosity decreased with increasing pressure. Intensity of the DRNIR spectra of the compressed tablets decreased as the compression pressure increased. However, the intensity of TNIR spectra increased along with the pressure. The calibration models used to evaluate the dissolution properties of tablets were established by using PCR based on both DRNIR and TNIR spectra of the tablets. The multiple correlation coefficients of the relationship between the actual and predictive T75 by the DRNIR and TNIR methods were 0.831 and 0.962, respectively. It is possible to predict the dissolution properties of pharmaceutical preparations using both DRNIR and TNIR chemoinformetric methods. The TNIR method was more accurate for predictions of the dissolution behavior of tablets than the DRNIR method. (c) 2007 Wiley-Liss, Inc.

  5. Lithium ion implantation effects in MgO (100)

    NARCIS (Netherlands)

    van Huis, MA; Fedorov, AV; van Veen, A; Labohm, F; Schut, H; Mijnarends, PE; Kooi, BJ; De Hosson, JTM; Triftshauser, W; Kogel, G; Sperr, P

    2001-01-01

    Single crystals of MgO (100) were implanted with 10(16) (6)Li ions cm(-2) at an energy of 30 keV. After ion implantation the samples were annealed isochronally in air at temperatures up to 1200K. After implantation and after each annealing step, the defect evolution was monitored with optical

  6. Development and analytical characterization of a new antiparasitic fenbendazole compound tablet and pharmacokinetic investigations after its oral administration to dogs.

    Science.gov (United States)

    Dai, Cunchun; Qu, Shaoqi; Zhang, Ruili; Zhao, Li; Li, Yuwen; Zhu, Jiajia; Wang, Chunmei; Guo, Hui; Hao, Zhihui

    2018-02-01

    The objective of this study was to prepare a new compound fenbendazole tablet containing 29.7 % fenbendazole, 1.50 % praziquantel and 0.059 % ivermectin for oral administration. The tablets were successfully prepared using mannitol as filler agent, polyvinyl polypyrrolidone as disintegrant, 5 % povidone (PVAK30) as a binder agent and magnesium stearate as lubricant. The appearance, hardness, fragility, time limit of disintegration and fenbendazole dissolution at 45 min all met the technical standards of the Ministry of Agriculture for the People's Republic of China. We used high performance liquid chromatography and electrospray-mass spectrometry for drug detection. Oral administration of 100 mg/kg fenbendazole, 5 mg/kg praziquantel and 0.2 mg/kg ivermectin using a non-compartmental model defined peak plasma concentrations (Cmax) of 495, 826, 73 ng/mL, and 218 ng/mL for the metabolite oxfendazole, respectively. The area under the curve (AUClast) values for these drugs were 4653, 1045, 1971 and 5525 h×ng/mL, respectively. This study enriches the pharmacokinetic data of compound fenbendazole tablets using dogs as a model system. The new tablet formulation was assimilated quickly and systemically and this study will be beneficial for the clinical application of parasite treatments in dogs.

  7. High-amylose sodium carboxymethyl starch matrices: development and characterization of tramadol hydrochloride sustained-release tablets for oral administration.

    Science.gov (United States)

    Nabais, Teresa; Leclair, Grégoire

    2014-01-01

    Substituted amylose (SA) polymers were produced from high-amylose corn starch by etherification of its hydroxyl groups with chloroacetate. Amorphous high-amylose sodium carboxymethyl starch (HASCA), the resulting SA polymer, was spray-dried to obtain an excipient (SD HASCA) with optimal binding and sustained-release (SR) properties. Tablets containing different percentages of SD HASCA and tramadol hydrochloride were produced by direct compression and evaluated for dissolution. Once-daily and twice-daily SD HASCA tablets containing two common dosages of tramadol hydrochloride (100mg and 200 mg), a freely water-soluble drug, were successfully developed. These SR formulations presented high crushing forces, which facilitate further tablet processing and handling. When exposed to both a pH gradient simulating the pH variations through the gastrointestinal tract and a 40% ethanol medium, a very rigid gel formed progressively at the surface of the tablets providing controlled drug-release properties. These properties indicated that SD HASCA was a promising and robust excipient for oral, sustained drug-release, which may possibly minimize the likelihood of dose dumping and consequent adverse effects, even in the case of coadministration with alcohol.

  8. Determinación cuantitativa por electroforesis capilar de zona de mangiferina en tabletas VIMANG® 300 mg Quantitative determination through capillary zone electrophoresis of mangiferin in 300 mg VIMANG® tablets

    Directory of Open Access Journals (Sweden)

    Harold Curiel Hernández

    2011-09-01

    Full Text Available La mangiferina se seleccionó como marcador en el control de calidad del ingrediente farmacéutico activo VIMANG® y sus formulaciones, que se han empleado como suplemento nutricional, cosmético y fitomedicamento. El trabajo tuvo como objetivo la validación del método electroforesis capilar para la determinación cuantitativa de mangiferina en la formulación farmacéutica tabletas VIMANG® 300 mg. Se evaluaron la especificidad, linealidad, exactitud y precisión. Los resultados obtenidos demostraron que el método fue específico, al no existir interferencias de los excipientes o sus productos de degradación. La linealidad mostró un coeficiente de correlación de 0,9979 en el intervalo de concentraciones estudiado. Los coeficientes de variación para la repetibilidad y la precisión intermedia fueron menores de 2 %. La exactitud mostró un recobrado del 100,20 % que no difiere significativamente de 100 %. En conclusión, el método validado es específico, lineal, preciso y exacto, y constituye una alternativa ventajosa al método cromatografía líquida de alta resolución establecido con anterioridad en el laboratorio.Mangiferin was selected as marker in the quality control of active principle VIMANG® and its formulations, which have been used as nutritional supplement, cosmetic, and phytomedication. This paper was aimed at validating the capillary electrophoresis method for the quantitative analysis of mangiferin in the pharmaceutical formulation 300 mg VIMANG® tablets. The specificity, linearity, accuracy and precision were assessed. The results showed the method specificity owing to lack of interference by the excipients or their degradation products. Linearity showed a correlation coefficient of 0.9979 in the studied concentration range. The variation coefficients for repeatability and intermediate precision were less than 2 %. Accuracy reached a recovery rate of 100.20 % that is not statistically different from 100 %. It may be

  9. Development of midazolam sublingual tablets: in vitro study.

    Science.gov (United States)

    Odou, P; Barthelemy, C; Robert, H

    1998-01-01

    Midazolam is a benzodiazepine with short elimination half-life, used as induction or continuous agent for general anesthesia. At present, only injectable solution is available from French hospital pharmacies. The aim of the study is the development of 5 mg midazolam sublingual tablets to realize a short general anesthesia without intravenous or intramuscular injection. Incorporation of citric acid in the tablet formulation leads to an increase of dissolution rates of active drug, but a decrease of diffusion through lipid membranes is observed with 10 mg of citric acid when using the Dibbern's Resomat three phases apparatus. One explanation of this result is that midazolam (pKa = 6.1) in presence of 10 mg of citric acid is ionised. The ionised form, more hydrophilic, cannot cross the artificial lipid membrane and therefore the diffusion decreases. On the other hand, the decrease of diffusion's rate, when pH increases, is explained by the precipitation of midazolam at pH higher than 6. A compromise between dissolution and diffusion results leads us to choose the sublingual formulation containing 5 mg of citric acid per tablet.

  10. Effect of Rebamipide on the Premalignant Progression of Chronic Gastritis: A Randomized Controlled Study.

    Science.gov (United States)

    Han, Xue; Jiang, Kui; Wang, Bangmao; Zhou, Lu; Chen, Xin; Li, Shu

    2015-10-01

    Chronic gastritis frequently progresses into precancerous intestinal metaplasia and intraepithelial neoplasia lesions. Rebamipide is a free radical scavenger and we assessed its efficacy on clinical symptoms, gastric mucosal lesions, pathologic grade, and immunohistochemistry in chronic gastritis patients. 178 eligible patients were randomized into treatment and control groups. Both groups followed an optimized lifestyle for 26 weeks, but the treatment group was additionally medicated with rebamipide 0.1 g three times per day. Upper gastrointestinal endoscopy was performed in all patients to evaluate the severity of gastritis by the Modified Lanza Scoring (MLS) and histological changes were evaluated by the Updated Sydney System Score (USSS). Gastric mucosa immunohistochemistry in the treatment group was performed using the intestinal metaplasia markers caudal type homeobox transcription factor 2 (CDX2) and trefoil factor 3 (TFF3) detection. There were significant outcome differences between the treatment and control groups regarding the clinical symptom scores (2.62 ± 1.86 vs. 1.55 ± 1.61, P = 0.0001), gastric mucosal lesion scores (0.57 ± 1.05 vs. 0.16 ± 0.90, P = 0.002), and inflammation (P gastritis patients and decreased the expression rates of CDX2 and TFF3 in gastric cells.

  11. Quality Enhancement by Inclusion Complex Formation of Simvastatin Tablets

    Directory of Open Access Journals (Sweden)

    Emőke Rédai

    2013-08-01

    Full Text Available Introduction: Simvastatin is an inhibitor of hydroxy-methyl-glutaryl-coenzyme A reductase, used in the treatment of hypercholesterolemia. To enhance its bioavailability by inclusion complexation, as host molecule randommethyl-β-cyclodextrin had been used. After evaluating the complexes we chose the kneading product in 1:2 molar ratio for incorporation of 10 mg simvastatin tablets. Materials and methods: We prepared homogenous mixtures of the inclusion complex and some excipients. The tablets were prepared by direct compression. The tablets were evaluated in regard to: weight uniformity, thickness, diameter, hardness, friability, disintegration and dissolution profile. Results: Weights are in the range of 196-208 mg, diameter 6.83-6.86 mm, height 3.86-4.01 mm, hardness 78.3-113.1 N, friability 0.75- 1.19 %, disintegration above 15 minutes. The dissolved amounts of simvastatin from the tablets are higher compared to the dissolution of pure simvastatin, but lower than the dissolution of the complex itself. Excipients, like disintegrants and lubricants greatly influence the dissolution properties of the tablets. Conclusions: According to our results, tablets containing inclusion complex of simvastatin exhibit better solubility, according to the dissolved amount of simvastatin, than pure drug alone. Proper physical parameters of the tablets are obtained by application of 5 % Primellose

  12. Development of tablets containing semipurified extract of guaraná (Paullinia cupana

    Directory of Open Access Journals (Sweden)

    Traudi Klein

    2012-12-01

    Full Text Available This study evaluated the technological feasibility of producing a semipurified extract of guaraná (Paullinia cupana Kunth, Sapindaceae in tablet form, using a direct-compression process. Maltodextrin and gum arabic were used to produce the extract microparticles, in order to protect the microparticles against such factors as temperature, oxidation, and humidity. Using pharmacopoeial methodologies, technological and physicochemistry tests (determination of residual moisture, of bulk and tapped density, Hausner ratio, compressibility and compactibility index, appearance, mean weight, hardness, friability, disintegration time, determination of EPA amount in tablets and in vitro release profile were conducted. The formulation containing 200 mg of microparticles, 170 mg microcrystalline cellulose, and 10 mg lactose gave the best results in terms of hardness (116 N, friabilility (0.28%, mean weight (0.3821 g, and disintegration time (25 min for a tablet designed for oral administration. The results met pharmacopoeial specifications, and the tablets are suitable for oral administration.

  13. Limited Effect of Rebamipide in Addition to Proton Pump Inhibitor (PPI) in the Treatment of Post-Endoscopic Submucosal Dissection Gastric Ulcers: A Randomized Controlled Trial Comparing PPI Plus Rebamipide Combination Therapy with PPI Monotherapy

    OpenAIRE

    Nakamura, Kazuhiko; Ihara, Eikichi; Akiho, Hirotada; Akahoshi, Kazuya; Harada, Naohiko; Ochiai, Toshiaki; Nakamura, Norimoto; Ogino, Haruei; Iwasa, Tsutomu; Aso, Akira; Iboshi, Yoichiro; Takayanagi, Ryoichi

    2016-01-01

    Background/Aims The ability of endoscopic submucosal dissection (ESD) to resect large early gastric cancers (EGCs) results in the need to treat large artificial gastric ulcers. This study assessed whether the combination therapy of rebamipide plus a proton pump inhibitor (PPI) offered benefits over PPI monotherapy. Methods In this prospective, randomized, multicenter, open-label, and comparative study, patients who had undergone ESD for EGC or gastric adenoma were randomized into groups recei...

  14. Development and validation of NIR-chemometric methods for chemical and pharmaceutical characterization of meloxicam tablets.

    Science.gov (United States)

    Tomuta, Ioan; Iovanov, Rares; Bodoki, Ede; Vonica, Loredana

    2014-04-01

    Near-Infrared (NIR) spectroscopy is an important component of a Process Analytical Technology (PAT) toolbox and is a key technology for enabling the rapid analysis of pharmaceutical tablets. The aim of this research work was to develop and validate NIR-chemometric methods not only for the determination of active pharmaceutical ingredients content but also pharmaceutical properties (crushing strength, disintegration time) of meloxicam tablets. The development of the method for active content assay was performed on samples corresponding to 80%, 90%, 100%, 110% and 120% of meloxicam content and the development of the methods for pharmaceutical characterization was performed on samples prepared at seven different compression forces (ranging from 7 to 45 kN) using NIR transmission spectra of intact tablets and PLS as a regression method. The results show that the developed methods have good trueness, precision and accuracy and are appropriate for direct active content assay in tablets (ranging from 12 to 18 mg/tablet) and also for predicting crushing strength and disintegration time of intact meloxicam tablets. The comparative data show that the proposed methods are in good agreement with the reference methods currently used for the characterization of meloxicam tablets (HPLC-UV methods for the assay and European Pharmacopeia methods for determining the crushing strength and disintegration time). The results show the possibility to predict both chemical properties (active content) and physical/pharmaceutical properties (crushing strength and disintegration time) directly, without any sample preparation, from the same NIR transmission spectrum of meloxicam tablets.

  15. Pharmacokinetics of diclofenac potassium after oral administration of sachets and tablets

    Directory of Open Access Journals (Sweden)

    A Martso

    2008-01-01

    Results. There is evidence that patients tolerate both its sachets and tablets equally well, as confirmed by subjective and objective observations. There are neither marked side effects nor considerable changes in laboratory tests and in the values of vital functions. Diclofenac potassium as early-action tablets (50 and 100 mg exerts a very good analgesic effect in treating migraine since the plasma concentration of the drug peaks on an average of an hour of administration (range 0,33-2 hours and the analgesic effect developed following 60-90 min. Conclusion. By comparing the rate of absorption, it may be concluded that diclofenac potassium as sachets will produce a much rapider analgesic effect. Thus, the high solubility of diclofenac potassium and its very good absorbability (as sachets in particular make the drug a superior analgesic that has a rapid analgesic activity.

  16. Formulation and in-vitro evaluation of directly compressed controlled release matrices of Losartan Potassium using Ethocel Grade 100 as rate retarding agent.

    Science.gov (United States)

    Khan, Kamran Ahmad; Khan, Gul Majid; Zeeshan Danish, Muhammad; Akhlaq; Khan, Haroon; Rehman, Fazal; Mehsud, Saifullah

    2015-12-30

    Current study was aimed to develop 200mg controlled release matrix tablets of Losartan Potassium using Ethocel 100 Premium and Ethocel 100 FP Premium as rate controlling polymer. In-vitro studies were performed according to USP Method-I in phosphate buffer (PH 6.8) using pharma test dissolution apparatus. The temperature of the dissolution medium was kept constant at 37±0.5°C at 100rpm. Flow properties, physical quality control tests, effect of polymer size and drug-to-polymers ratios were studied using different kinetics models such as 1st-order, zero-order, Hixon Crowell model, Highuchi model and Power law. Difference factor f1 and similarity factor f2 were applied for dissolution profiles against Cardaktin® tablets used as a reference formulation. The matrices with polymer ethocel 100 FP Premiums have prolonged the drug release rate as compared to polymer ethocel 100 Premiums. The n values matrices with polymer ethocel grade 100 ranged from 0.603 to 0.857 indicating that the drug release occurred by anomalous non fickian diffusion kinetics while then value of reference Cardaktin® tablet was measured as 0.125 indicating that these tablets do not follow power law. The dissolution profiles of test formulations were different than that of reference Cardaktin®. This suggests the polymer Ethocel grade 100 can be proficiently incorporated in fabrication and development of once a day controlled release matrix tablets. Copyright © 2015. Published by Elsevier B.V.

  17. Optimized furosemide taste masked orally disintegrating tablets

    Directory of Open Access Journals (Sweden)

    Mohamed Abbas Ibrahim

    2017-11-01

    Full Text Available Optimized orally disintegrating tablets (ODTs containing furosemide (FUR were prepared by direct compression method. Two factors, three levels (32 full factorial design was used to optimize the effect of taste masking agent (Eudragit E100; X1 and superdisintegarant; croscarmellose sodium (CCS; X2 on tablet properties. A composite was prepared by mixing ethanolic solution of FUR and Eudragit E100 with mannitol prior to mixing with other tablet ingredients. The prepared ODTs were characterized for their FUR content, hardness, friability and wetting time. The optimized ODT formulation (F1 was evaluated in term of palatability parameters and the in vivo disintegration. The manufactured ODTs were complying with the pharmacopeia guidelines regarding hardness, friability, weight variation and content. Eudragit E100 had a very slightly enhancing effect on tablets disintegration. However, the effects of both Eudragit E100 (X1 and CCS (X2 on ODTs disintegration time (Y1 were insignificant (p > 0.05. Moreover, X1 exhibited antagonistic effect on the dissolution after 5 and 30 min (D5 and D30, respectively, but only its effect on D30 is significant (p = 0.0004. Furthermore, the optimized ODTs formula showed good to acceptable taste in term of palatability, and in vivo disintegration time of this formula was about 10 s.

  18. Design and in vivo evaluation of oxycodone once-a-day controlled-release tablets

    Directory of Open Access Journals (Sweden)

    Kim JY

    2015-01-01

    Full Text Available Ju-Young Kim,1,* Sung-Hoon Lee,2,3,* Chun-Woong Park,4 Yun-Seok Rhee,5 Dong-Wook Kim,6 Junsang Park,3 Moonseok Lee,3 Jeong-Woong Seo,2 Eun-Seok Park2 1College of Pharmacy, Woosuk University, Wanju-gun, Republic of Korea; 2School of Pharmacy, Sungkyunkwan University, Suwon, Republic of Korea; 3GL Pharmtech, Seongnam, Republic of Korea; 4College of Pharmacy, Chungbuk National University, Cheongju, Republic of Korea; 5College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju, Republic of Korea; 6Department of Pharmaceutical Engineering, Cheongju University, Cheongju, Republic of Korea *These authors contributed equally to this work Abstract: The aim of present study was to design oxycodone once-a-day controlled-release (CR tablets and to perform in vitro/in vivo characterizations. Release profiles to achieve desired plasma concentration versus time curves were established by using simulation software and reported pharmacokinetic parameters of the drug. Hydroxypropyl methylcellulose (HPMC 100,000 mPa·s was used as a release modifier because the polymer was found to be resistant to changes in conditions of the release study, including rotation speed of paddle and ion strength. The burst release of the drug from the CR tablets could be suppressed by applying an additional HPMC layer as a physical barrier. Finally, the oxycodone once-a-day tablet was comprised of two layers, an inert HPMC layer and a CR layer containing drug and HPMC. Commercial products, either 10 mg bis in die (bid [twice a day] or once-a-day CR tablets (20 mg were administered to healthy volunteers, and calculated pharmacokinetic parameters indicated bioequivalence of the two different treatments. The findings of the present study emphasize the potential of oxycodone once-a-day CR tablets for improved patient compliance, safety, and efficacy, which could help researchers to develop new CR dosage forms of oxycodone. Keywords

  19. Modulation of microenvironmental pH for dual release and reduced in vivo gastrointestinal bleeding of aceclofenac using hydroxypropyl methylcellulose-based bilayered matrix tablet.

    Science.gov (United States)

    Kang, Won-Ho; Nguyen, Hien Van; Park, Chulhun; Choi, Youn-Woong; Lee, Beom-Jin

    2017-05-01

    This study was designed to develop a once-daily controlled-release matrix tablet of aceclofenac 200mg (AFC-CR) with dual release characteristics and to investigate the role of an alkalizer in enhancing drug solubility and reducing the occurrence of gastroduodenal mucosal lesions. Two formulation approaches were employed, namely a monolithic matrix tablet and a bilayered tablet. In vitro dissolution studies of AFC-CR tablets were carried out in simulated intestinal fluid (pH6.8 buffer). The in vivo pharmacokinetic studies and drug safety of the immediate-release reference tablet Airtal® 100mg (Daewoong Co., Korea) and the optimized AFC-CR tablet were compared in beagle dogs under fasted condition. The optimally selected AFC-CR formulation displayed the desired dual release characteristics in simulated intestinal fluid with satisfactory micromeritic properties. The swelling action of the optimal matrix tablet, which was visualized by near-infrared (NIR) chemical imaging, occurred rapidly following hydration. Incorporation of sodium carbonate (Na 2 CO 3 ) was found to enhance the release rate of the AFC-CR bilayered tablets at early stages and increase the microenvironmental pH (pH M ). A pharmacokinetic study in beagle dogs indicated a higher drug plasma concentration and a sustained-release pattern for the AFC-CR tablet compared to the Airtal® tablet. AFC-CR was also superior to Airtal® in terms of in vivo drug safety, since no beagle dog receiving AFC-CR experienced gastrointestinal bleeding. The significant enhancement of drug safety was attributed to the size reduction and the increase of pH M of drug particles by means of incorporation of the alkalizer. These findings provide a scientific rationale for developing a novel controlled-release matrix tablet with enhanced patient compliance and better pain control. Copyright © 2017 Elsevier B.V. All rights reserved.

  20. Preparation and in-vitro in-vivo evaluation of sustained release matrix diclofenac sodium tablets using PVP-K90 and natural gums.

    Science.gov (United States)

    Iqbal, Zafar; Khan, Raza; Nasir, Fazli; Khan, Jamshaid Ali; Rashid, Abdur; Khan, Abbas; Khan, Abad

    2011-10-01

    Conventional dosage form is nowadays mostly replaced by sustained release formulation in order to increase drug efficacy and patient compliance. The sustained release properties of the PVP K90 alone and in combination with guar gum, xanthan gum and gum tragacanth were evaluated using diclofenac sodium (100 mg/tablet) as a model drug. Tablets were processed using wet granulation method and evaluated for sustained drug release properties. The drug release from the formulations was studied in relationship with Commercially available Diclofenac Sodium SR, used as a reference tablets and results were expressed as similarity (f1) and differential factor (f2). The tablets prepared using PVP K90 160 mg/tablet sustained the release of diclofenac sodium for 12 hours. Formulations where the PVP K90 was partially replaced with different gums also sustained the release of drug for 12 hours. The release of the drug from these formulations mainly followed Higuchi model and super case-II and Non-Fickian diffusion. The in-vivo drug release was studied in healthy human volunteers using non-blinded cross over, two period design using Diclofenac Sodium SR Tablets as a reference drug. The relative bioavailability of the formulation containing PVP K90 and gum tragacanth was 0.91. The studies showed that the use of the PVP K90 in combination with gum tragacanth both in-vitro and in-vivo sustained the release of the drug.

  1. Dose Uniformity of Scored and Unscored Tablets: Application of the FDA Tablet Scoring Guidance for Industry.

    Science.gov (United States)

    Ciavarella, Anthony B; Khan, Mansoor A; Gupta, Abhay; Faustino, Patrick J

    world. Tablets are often split to modify dose strength, make swallowing easier, and reduce cost to the consumer. To better address product quality for this widely used practice, the U.S. Food and Drug Administration (FDA) published a Guidance for Industry that addresses tablet splitting. The guidance provides testing criteria for scored tablets, which is a part of the FDA review process for drugs. The model drugs selected for this study were amlodipine and gabapentin, which have different sizes, shapes, and tablet scores. Whole and split amlodipine tablets were tested for drug content because of a concern that the low-dose strength may cause greater variability. Whole and split gabapentin tablets were tested for weight variation because of their higher dosage strength of 600 mg. All whole tablets met the acceptance criteria for the Uniformity of Dosage Units based on the guidance recommendations. When unscored amlodipine tablets were split by a splitter, all formulations did not meet the acceptance criteria. When fully scored gabapentin tablets were split by hand and by splitter, they met the acceptance criteria. The findings of this FDA study indicated physical characteristics such as size, shape, and tablet score can affect the uniformity of split tablets. © PDA, Inc. 2016.

  2. NO and NO{sub 2} adsorption on subsurface doped MgO (100) and BaO (100) surfaces. A density functional study

    Energy Technology Data Exchange (ETDEWEB)

    Añez, Rafael, E-mail: ranez@ivic.gob.ve [Laboratorio de Química Física y Catálisis Computacional, Centro de Química, Instituto Venezolano de Investigaciones Científicas, Apartado 21827, Caracas (Venezuela, Bolivarian Republic of); Sierraalta, Aníbal [Laboratorio de Química Física y Catálisis Computacional, Centro de Química, Instituto Venezolano de Investigaciones Científicas, Apartado 21827, Caracas (Venezuela, Bolivarian Republic of); Soto, Lenin J. Díaz [Pontifícia Universidade Católica do Rio de Janeiro, Departamento de Física, 22451-900 Rio de Janeiro, RJ (Brazil); Instituto de Química, Universidade Federal do Rio de Janeiro, Cidade Universitária, CT Bloco A sala 412, Rio de Janeiro, RJ 21949-900 (Brazil)

    2017-05-15

    Highlights: • Subsurface doped BaO(100) and MgO(100) surfaces. • NO and NO{sub 2} adsorption on doped BaO(100) and MgO(100) surfaces. • Surface distortion produced by the doped improves the interaction with the surface. • NO and NO{sub 2} adsorption energies displayed good correlation with the transferred charge. - Abstract: A periodic DFT approach was used to study the energetic, electronic and structural changes produced by the V, Fe and Ni sub layer doped of the MgO (100) and BaO (100) surfaces and the effect of these changes over the adsorption of NO and NO{sub 2}. Results indicate that the higher capacity of donating charge of the transition metal atoms improves the ability of the surfaces to transfer charge to the molecules. The charge transferred goes to NO and NO{sub 2} antibonding orbitals which makes them more reactive hence the interaction becomes stronger. A good lineal correlation between the charge transferred and the calculated adsorption energy was found, that is, as the charge transferred increases the adsorption energy increases. The interaction between the NO or NO{sub 2} molecule on doped surfaces not only depends of the charge transferred, surface structural changes produced by the doping with transition metal atoms increase the adsorption energy specially on the BaO (100) surface where the surface structural changes were more noticeable. Calculated stretching frequency of a NO in a η{sup 1} –N configuration indicates that this is the most stable specie found for the adsorption of NO on terraces of the MgO (100) surface around 77 K and that the sub layer Ni doped BaO (100) surface could be a promising material for the decomposition of NO{sub 2}.

  3. Paracetamol 325 mg/tramadol 37.5 mg effect on pain during needle electromyography: a double-blind crossover clinical trial.

    Science.gov (United States)

    Kalantar, Seyed Sadeq; Abbasi, Mehrshad; Faghihi-Kashani, Sara; Majedi, Hossein; Ahmadi, Mona; Agah, Elmira; Tafakhori, Abbas

    2016-12-01

    Needle insertion during electromyography (EMG) may cause varying levels of pain that could lead to inaccurate assessment and premature termination of the procedure. The aim of this study is to compare paracetamol 325 mg/tramadol 37.5 mg with placebo in relieving pain before EMG. This is a randomized, crossover, placebo-controlled, double-blind clinical trial; forty-four healthy individuals, including 27 males with a mean age of 35.3 years (range 18-59 years), entered this study. The needles were inserted unilaterally 2 h after administration of two analgesic tablets of paracetamol 325 mg/tramadol 37.5 mg or two placebo tablets. The pain was scored through a 100-mm visual analog scale (VAS) immediately and 2 h after the procedure. The side effects were also recorded. Within a week, the procedure was repeated on the other upper limb, changing the treatment and placebo. The immediate and 2-h VAS scores were notably lower after administration of treatment compared to placebo (immediate pain: 17.5 ± 12.8 vs. 32.1 ± 16.0, P pain: 1.6 ± 5.6 vs. 5.8 ± 7.9, P = 0. 002). There was a higher prevalence of side effects when treatment was used (48 vs. 9 %, P pain. Further application of this medication in patients with neuromuscular disorders would warrant additional clinical trials, particularly considering the adverse events.

  4. Comparative investigations of tablet crushing force testers

    DEFF Research Database (Denmark)

    Sonnergaard, Jørn; Jensen, C.G.; Poulsen, L.

    2005-01-01

    The performance of 16 tablet breaking force testers was evaluated in terms of accuracy, reproducibility and repeatability. Three tablet formulations with different plastic or brittle deformation mechanisms and with target breaking forces of 50, 100 and 150 N were tested. Statistically significant...... by the concept of components of variance was 5-7 % depending on the model tablet excipient. The standard deviation within testers (repeatability) was affected by the type of model formulation showing increasing variability with increasing brittleness of the compressed material. No specific effect of altering...

  5. A Pilot Stability Study of Dehydroepiandrosterone Rapid-dissolving Tablets Prepared by Extemporaneous Compounding.

    Science.gov (United States)

    Rush, Steven D; Vernak, Charlene; Zhao, Fang

    2017-01-01

    Dehydroepiandrosterone supplementation is used to treat a variety of conditions. Rapid-dissolving tablets are a relatively novel choice for compounded dehydroepiandrosterone dosage forms. While rapid-dissolving tablets offer ease of administration, there are uncertainties about the physical and chemical stability of the drug and dosage form during preparation and over long-term storage. This study was designed to evaluate the stability of dehydroepiandrosterone rapid-dissolving tablets just after preparation and over six months of storage. The Professional Compounding Centers of America rapid-dissolving tablet mold and base formula were used to prepare 10-mg strength dehydroepiandrosterone rapid-dissolving tablets. The formulation was heated at 100°C to 110°C for 30 minutes, released from the mold, and cooled at room temperature for 30 minutes. The resulting rapid-dissolving tablets were individually packaged in amber blister packs and stored in a stability chamber maintained at 25°C and 60% relative humidity. The stability samples were pulled at pre-determined time points for evaluation, which included visual inspection, tablet weight check, United States Pharmacopeia disintegration test, and stability-indicating high-performance liquid chromatography. The freshly prepared dehydroepiandrosterone rapiddissolving tablets exhibited satisfactory chemical and physical stability. Time 0 samples disintegrated within 40 seconds in water kept at 37°C. The high-performance liquid chromatographic results confirmed that the initial potency was 101.9% of label claim and that there was no chemical degradation from the heating procedure. Over six months of storage, there were no significant changes in visual appearance, physical integrity, or disintegration time for any of the stability samples. The high-performance liquid chromatographic results also indicated that dehydroepiandrosterone rapid-dissolving tablets retained >95% label claim with no detectable degradation

  6. 78 FR 66009 - Determination That INVEGA (Paliperidone) Extended-Release Tablet, 12 Milligrams, Was Not...

    Science.gov (United States)

    2013-11-04

    ...] Determination That INVEGA (Paliperidone) Extended-Release Tablet, 12 Milligrams, Was Not Withdrawn From Sale for... Food and Drug Administration (FDA) has determined that INVEGA (paliperidone) extended-release tablet...-release tablet, 12 mg, if all other legal and regulatory requirements are met. FOR FURTHER INFORMATION...

  7. Validación de un método espectrofotométrico para la cuantificación de principio activo en tabletas de nifedipino 10 mg Validation of a spectrophotometric method for quantification of the active principle in 10 mg Nifedipine tablets

    Directory of Open Access Journals (Sweden)

    Yalexmi Ramos Rodríguez

    2008-12-01

    Full Text Available Se realizó la validación de una técnica espectrofotométrica para la cuantificación del principio activo en tabletas de nifedipino 10 mg con el empleo de etanol al 96 % como solvente. Se determinaron los parámetros de linealidad, exactitud, precisión intermedia, repetibilidad, especificidad y robustez. Se comprobó que el método es lineal, exacto y preciso en un rango de 85 a 115 %, lo que demuestra la fiabilidad del método y su posibilidad de empleo en el control de la calidad de la forma terminada.The validation of a spectrophotometric method for the determination of active principle in tablets of nifedipine 10 mg is presented in this work. The linearity, precision, exactitude, specificity and robustness of the method were evaluated. The method employed was linear, exact and precise in the interval of 85 % to 115%. This proves that the method can be used in the tablets' quality control.

  8. Influence of polymeric subcoats on the drug release properties of tablets powder-coated with pre-plasticized Eudragit L 100-55.

    Science.gov (United States)

    Sauer, Dorothea; Watts, Alan B; Coots, Lonique B; Zheng, Weijia C; McGinity, James W

    2009-02-09

    The aim of the study was to investigate the properties of sodium valproate tablets that were dry powder-coated with pre-plasticized Eudragit L 100-55. Polyethylene glycol 3350 (PEG 3350) was used as primer to facilitate initial coating powder adhesion. Solubility parameters were employed to determine the wetting properties of the PEG 3350 primer. Additional PEG 3350 within the powder coating formulation was required to enable powder adhesion to the tablet cores. The application of a subcoat of either Eudragit E PO or Eudragit RL PO facilitated adhesion of the enteric polymer to the tablet cores and reduced the amount PEG 3350 required in the coating formulation. Since reduction of the PEG 3350 content produced less water-vapor permeable films, the enteric coating level necessary to control the drug release was decreased. PEG 3350 and Methocel K4M were incorporated in both Eudragit E PO and Eudragit RL PO subcoating formulations as pore forming agents. The influence of the pore forming excipients on physicochemical properties of free powder-cast films was investigated. The miscibility of the PEG 3350 and Methocel K4M in the film coating was correlated with their ability to function as pore forming agent.

  9. Comparative study of 250 mg/day terbinafine and 100 mg/day itraconazole for the treatment of cutaneous sporotrichosis.

    Science.gov (United States)

    Francesconi, Glaucia; Francesconi do Valle, Antonio Carlos; Passos, Sonia Lambert; de Lima Barros, Mônica Bastos; de Almeida Paes, Rodrigo; Curi, André Luiz Land; Liporage, José; Porto, Cássio Ferreira; Galhardo, Maria Clara Gutierrez

    2011-05-01

    Itraconazole is currently used for the treatment of cutaneous sporotrichosis. Terbinafine at a daily dose of 250 mg has been successfully applied to the treatment of cutaneous sporotrichosis. To compare the efficacy of 250 mg/day terbinafine and 100 mg/day itraconazole for the treatment of cutaneous sporotrichosis. A bidirectional cohort study was conducted on 55 patients receiving 250 mg/day terbinafine and 249 patients receiving 100 mg/day itraconazole. The latter patients were matched for age and clinical form to the terbinafine group at a ratio of 5:1. Sporothrix schenckii was isolated by culture from all patients (age range: 18-70 years), who were submitted to the standard care protocol consisting of clinical and laboratory evaluation and periodic visits. Cure was observed in 51 (92.7%) patients of the terbinafine group and 229 (92%) of the itraconazole group within a similar mean period of time (11.5 and 11.8 weeks, respectively). An increase in the terbinafine dose to 500 mg was necessary in two patients due to the lack of a response, and one patient presented recurrence. In the itraconazole group, two patients required a dose increase and three presented recurrence. Adverse events were equally frequent among patients receiving terbinafine (n = 4, 7.3%) and itraconazole (n = 19, 7.6%) and were generally mild without the need for drug discontinuation, except for two patients of the itraconazole group. Terbinafine administered at a daily dose of 250 mg is an effective and well-tolerated option for the treatment of cutaneous sporotrichosis.

  10. Improvement in erection hardness and intercourse success with first dose of sildenafil citrate 100 mg

    Directory of Open Access Journals (Sweden)

    Mulhall JP

    2013-11-01

    Full Text Available John P Mulhall,1 Dana L Creanga,2 Vera J Stecher31Urology Service, Department of Surgery, Memorial Sloan Kettering Cancer Center, New York, NY, USA; 2Consultant to Pfizer Inc., New York, NY, USA; 3Medical Affairs, Primary Care Business Unit, Pfizer Inc., New York, NY, USAPurpose: To determine, in men with erectile dysfunction (ED, the extent of improvement in erection hardness and in the rate of successful sexual intercourse (SSI during the final intercourse attempt using sildenafil 50 mg compared with the subsequent initial attempt after a dose increase to 100 mg.Patients and methods: This post hoc analysis used data from two randomized, double-blind, placebo-controlled studies of flexible-dose sildenafil for the treatment of men with ED, who were given sildenafil 50 mg or matching placebo, to be taken as needed before sexual intercourse. After 2 weeks, those with no tolerability concerns were titrated up to 100 mg, forming the subgroup of this analysis. The main outcome measures were event log data, including an Erection Hardness Score (EHS and a question on SSI (“Did your erection last long enough for you to have successful sexual intercourse?”, for each attempt at sexual intercourse, analyzed by study and treatment group (sildenafil or placebo. Statistical comparisons were conducted by using the Fisher's exact test.Results: In both studies, the sildenafil group had a larger proportion of EHS4 (completely hard and fully rigid erections (P < 0.001 and SSI (P < 0.005 compared with the placebo group, both before and after the dose increase. Between the final 50 mg sildenafil dose and the initial 100 mg sildenafil dose, the outcomes improved and significantly so in the larger study.Conclusion: The improved efficacy with sildenafil 100 mg versus 50 mg, which occurs rapidly, suggests that patients should be encouraged to use 100 mg if they are unable to achieve completely hard and fully rigid erections or SSI with the 50 mg dose

  11. Pharmaceutical equivalence of gabapentin tablets with various extragranular binders Pharmaceutical equivalence of gabapentin tablets with various extragranular binders

    Directory of Open Access Journals (Sweden)

    SWATI C. JAGDALE

    2010-06-01

    Full Text Available Gabapentin is a high-dose drug widely used as an oral anti-epilepticagent. Due to high crystalline and has poor compaction properties it is difficult to form tablets by direct compression. The aim of this study was to develop gabapentin tablets, pharmaceutically equivalent to the reference product Neurontin (marketed in USA. Gabapentin 800mg tablets were produced by wet granulation by keeping intragranular binder as well as its concentration constant and by changing with various extragranular binders with its concentration (A = PVPK 30, B = HPMC 15 cps, C = Kollidon VA 64, D =Klucel EXF.The tablet having no weight, thickness and hardness variation and having appropriate, friability as well as disintegration profile were coated with a 3% film coating solution .Seven formulations F1 (A in lower concentration F2 (A in higher concentration, F3 (B in lower concentration and F4 (B in higher concentration, F5 (C in lower concentration, F6 (C in higher concentration, F7 (D in lower concentration were formulated. Among them F6 demonstrated adequate hardness, friability, disintegration, uniformity of content, and total drug dissolution after 45minutes. The dissimilarity factor (f1 is 5.93 and the similarity factor (f2 is 67.85. So F6 was found to be equivalent to Neurontin.Gabapentin is widely used as an oral anti-epileptic agent. However, owing to its high crystallinity and poor compaction properties, it is difficult to form tablets of this drug by direct compression. The aim of this study was to develop gabapentin tablets, pharmaceutically equivalent to the brand-name pioneer product Neurontin® (marketed in USA. Gabapentin 800mg tablets were produced by wet granulation with a constant concentration of intragranular binder and a varying concentration of extragranular binders (A = polyvinylpyrrolidone K30, B = hydroxypropylmethylcellulose 15 cps, C = Kollidon VA64, D =Klucel EXF. The tablets that did not vary in weight, thickness or hardness and had

  12. Cimetidine Pharmacodynamics and Pharmacokinetics in Healthy Subjects: A Comparison of Tablets and Suspension

    Directory of Open Access Journals (Sweden)

    ABR Thomson

    1994-01-01

    Full Text Available The objective of this study was to compare the effect of cimetidine 200 mg tablet with that of cimetidine suspension (200 mg/10 mL, a 20 mL suspension of 800 mg magnesium hydroxide and 912 mg aluminum hydroxide, and matching placebo on intragastric pH of healthy volunteers. There were 13 males and seven females, mean age 23 years (range 20 to 32 and mean weight 72 kg (range 55 to 89. The intragastric pH of each subject was measured over 6 h starting immediately before dosing on each of five study days. Cimetidine plasma levels were measured for 6 h after dosing on each of the cimetidine study days. Cimetidine tablet and suspension were superior to placebo tablet or suspension or to the magnesium hydroxide/aluminum hydroxide suspension in the area under the pH time curve from 0 to 6 h, percentage time pH of at least 3.5, change from pretreatment pH area under the pH time curve (0 to 6 h and maximum increase in pH. Mean plasma cimetidine levels were significantly and positively correlated to mean intragastric pH for both cimetidine tablets and cimetidine suspension. Comparing cimetidine concentration (Cmax and lower percentage time plasma cimetidine concentration was at least 0.5 μg/mL (the minimum therapeutic level. These pharmacokinetic variations between cimetidine suspension and tablets may have partially explained the pharmacodynamic differences of the lower area under the pH time curve (0 to 6 h. The results indicate that both cimetidine tablets and cimetidine suspension significantly increase intragastric pH relative to the magnesium hydroxide/aluminum hydroxide suspension, placebo tablets or placebo suspension. Based on the assumption that elevation of intragastric pH is an important factor for alleviation of the symptoms and for the healing of peptic disorders, the results of this study suggest that both cimetidine tablets and cimetidine suspension should be effective treatment.

  13. Comparative study of thermoluminescent properties of LiF: Mg, Cu, P, LiF: Mg, Ti and TLD-100 irradiated with X-rays

    International Nuclear Information System (INIS)

    Azorin, J.; Rivera, T.; Gonzalez, P.; Ortega, X.; Ginjaume, M.

    2000-01-01

    The thermoluminescent properties (Tl) of LiF: Mg, Cu, P, and LiF: Mg, Ti, were investigated both developed in Mexico and comparing them with the properties of TLD-100 when they are exposure to X-rays. The Tl curve of LiF: Mg, Cu, P exhibited two peaks at 200 and 300 Centigrade. Its response Tl in function of dose resulted linear in the interval of 0.5 Gy until 5 Gy and its sensitivity to X-ray was around 25 times greater that of the TLD-100. Also it was measured the Tl response of the three materials in function of photon energy. The results showed that LiF: Mg, Cu, P has potential to be used as X-ray dosemeter. (Author)

  14. Relative bioavailability of methadone hydrochloride administered in chewing gum and tablets

    DEFF Research Database (Denmark)

    Christrup, Lona Louring; Angelo, H.R.; Bonde, J.

    1990-01-01

    Methadone administered in chewing gum in doses of 16.7-22.6 mg to seven patients in a study using an open balanced cross-over design, was compared with 20 mg of methadone given perorally as tablets. There was no significant difference in the AUC/D obtained after administration of chewing gum...... and tablets (p>0.05). It is concluded that the chewing gum formulation should be considered for further testing with respect to suppression of abstinence syndrome in narcotic addicts....

  15. Relative bioavailability of methadone hydrochloride administered in chewing gum and tablets.

    Science.gov (United States)

    Christrup, L L; Angelo, H R; Bonde, J; Kristensen, F; Rasmussen, S N

    1990-01-01

    Methadone administered in chewing gum in doses of 16.7-22.6 mg to seven patients in a study using an open balanced cross-over design, was compared with 20 mg of methadone given perorally as tablets. There was no significant difference in the AUC/D obtained after administration of chewing gum and tablets (p greater than 0.05). It is concluded that the chewing gum formulation should be considered for further testing with respect to suppression of abstinence syndrome in narcotic addicts.

  16. Is online information on ecstasy tablet content safe?

    Science.gov (United States)

    Vrolijk, Ruben Q; Brunt, Tibor M; Vreeker, Annabel; Niesink, Raymond J M

    2017-01-01

    In recent years, the prevalence of ecstasy use has increased in most European countries. Users can acquire information on ecstasy tablet composition through the internet. This study compares online information from two websites, Pillreports and Partyflock, to the validated Dutch Drugs Information and Monitoring System (DIMS) database, and aims to measure its accuracy and potential danger or value. The drug-related information posted on Pillreports.net and Partyflock.nl between 1 January 2014 and 31 December 2015 was investigated for accuracy and several information characteristics such as picture inclusion and dose range inclusion. In total, 471 informatory statements on ecstasy tablet content were analysed relative to the Dutch ecstasy market. Informatory statements on the content of specific ecstasy tablets were scored as 'too high' or 'too low' if their concentrations deviated > 10 mg from the entries in the DIMS database within a 12-week time-frame, and scored as 'dangerous' if their concentration was > 40 mg too low. Unreported substances were scored as 'dangerous' if listed as an illegal or dangerous substance in the DIMS database and if present in relevant quantities. Also scored were the report characteristics 'picture inclusion', 'spread inclusion' and 'website source', which were tested for their association with report safety/danger. On average, reports on ecstasy tablets from Pillreports and Partyflock show concentrations which are 10.6 mg too high [95% confidence interval (CI) = 6.7-14.4]. Qualitatively, 39.7% of the reports scored as 'too high' (95% CI = 35.2-44.4), 17.6% scored as 'too low' (95% CI = 14.0-21.2) and 15.5% had 'unreported substances' (95% CI = 12.3-18.9), resulting overall in 15.3% of the reports being scored as 'dangerous' (95% CI = 11.9-18.5). The report characteristic 'spread inclusion' associated inversely with report danger [Exp(b) = 0.511, 95% CI = 0.307-0.850, P = 0.01]. Information from the popular

  17. Determination of Letrozole in Tablet Formulations by Reversed ...

    African Journals Online (AJOL)

    Determination of Letrozole in Tablet Formulations by Reversed Phase High Performance Liquid Chromatography. ... The assay values for the two branded letrozole tablets tested were 99.2 and 100.2 %, respectively with % relative standard deviation (RSD) of 0.781 and 0.568, respectively. The bench top stability data of the ...

  18. Bioequivalence of 250 mg lysine clonixinate tablets after a single oral dose in a healthy female Mexican population under fasting conditions.

    Science.gov (United States)

    Marcelín-Jiménez, G; Angeles, A C P; García, A; Morales, M; Rivera, L; Martín-Del-Campo, A

    2010-05-01

    To evaluate the bioequivalence between two 250 mg-tablets of lysine clonixinate, Dorixina Forte (Siegfried Rhein, México) as reference product, and Prestodol (Farmaceúticos Rayere, S.A., México) as test formulation. 26 healthy adult female Mexican volunteers received a single oral dose of 250-mg lysine clonixinate under fasting conditions. The drug was administered following a randomized, two-period, two-sequence, cross-over design. Twelve serial blood samples were collected up to 8 h after dosing, and clonixin (CLX) was measured by ultra-performance liquid chromatography (UPLC) coupled with tandem mass spectrometry. Decimal logarithm values of Cmax and area under the curve (AUC) were used to construct a classic confidence interval at 90% (90% CI). Bioequivalence was established if 90% CI of mean ratios (test/reference) fall within the 0.8-1.25 range. Volunteers formed a homogeneous population in terms of age (27.2 +/- 6.3 years), weight (55.9 +/- 6.5 kg), height (1.6 +/- 0.04 m), and body mass index (BMI) (22.91 +/- 2.03 kg/m(2)). Reference formulation exhibited the following pharmacokinetics: C(max) (32.39 +/- 8.32 microg/ml); t(max) (0.64 +/- 0.2 h); AUC0-8h (48.92 +/- 16.51 microg x h/ml); t1/2 (1.3 +/- 0.24 h); CLapp (5.64 +/- 1.99 l/h), and Vdapp (10.22 +/- 2.9 l). Concerning bioequivalence, 90% CI were: C(max) (82.32 - 98.79), AUC0-t (94.59-106.29), and AUC(0-inf) (94.61-106.42), with a statistical power of > 0.90 at every tested interval. This single-dose study found that both 250-mg immediate-release tablets of lysine clonixinate met the Mexican regulatory criteria for bioequivalence in these volunteers.

  19. Formulation and Study of Some Controlled Release Tablets with Pentoxifylline Based on Hydroxypropylcellulose Matrix Obtained by Wet Granulation Method with PEG 6000

    Directory of Open Access Journals (Sweden)

    Gabriel Hancu

    2011-01-01

    Full Text Available In this work three formulations of modified release tablets
    containing pentoxifylline 400 mg/tablet were obtained. Hydroxypropylcellulose (HPC in di®erent ratios was used as hydrophilic matrix agent. The pentoxifylline inclusion in the matrix has been carried out by water granulation, using PEG 6000 as binder. Tablets were obtained with a single station
    tablet machine (Korsch, using standard pressure, and obtaining tablets with 13 mm diameter, 800 mg weight and 400 mg pentoxifylline per tablet. The weight uniformity, friability, hardness, thickness and disintegration of tablets were determined according to the stipulations of the 2001 Supplement of the Romanian Pharmacopoeia Xth edition. The experimental formulations with 400 mg pentoxifylline/tablet were studied by comparing them to the industrial reference product, Trental 400 mg (Aventis Pharma and in according
    to the stipulations of Romanian Pharmacopoeia Xth edition, USP 27 and European Pharmacopoeia 5th edition. Every determination was performed using 20 tablets. We followed the comparison between dissolution profiles of slow release tablets containing pentoxifylline based on hydrophilic matrix. The dissolution studies were performed using the method from USP 24, using the paddle apparatus, and water as medium of dissolution at 37+/-0,5 Celsius degrees, at a rotation speed of 50 rpm. The determination was performed by spectrofotometric as say in UV at 274 nm. It was noticeable that regarding the weight uniformity, friability, hardness, thickness and disintegration the proposed formulations are comparable with the industrial reference product (Trental, 400 mg and are in agreement with the stipulations of the Romanian Pharmacopoeia Xth edition and European Pharmacopoeia 5th edition. The analysis of dissolution profiles showed that all formulations exhibit slow release.

  20. Effect of antacids in didanosine tablet on bioavailability of isoniazid.

    OpenAIRE

    Gallicano, K; Sahai, J; Zaror-Behrens, G; Pakuts, A

    1994-01-01

    The antacids in two didanosine placebo tablets had no significant effect on the plasma pharmacokinetics of a single oral dose of 300 mg of isoniazid administered to 12 healthy volunteers. These results suggest that isoniazid bioavailability will be unaffected by the antacids in didanosine tablets when the two medications are administered simultaneously to human immunodeficiency virus-seropositive patients.

  1. Effect of antacids in didanosine tablet on bioavailability of isoniazid.

    Science.gov (United States)

    Gallicano, K; Sahai, J; Zaror-Behrens, G; Pakuts, A

    1994-04-01

    The antacids in two didanosine placebo tablets had no significant effect on the plasma pharmacokinetics of a single oral dose of 300 mg of isoniazid administered to 12 healthy volunteers. These results suggest that isoniazid bioavailability will be unaffected by the antacids in didanosine tablets when the two medications are administered simultaneously to human immunodeficiency virus-seropositive patients.

  2. Evaluation of Certain Pharmaceutical Quality Attributes of Lisinopril Split Tablets

    Directory of Open Access Journals (Sweden)

    Khairi M. S. Fahelelbom

    2016-10-01

    Full Text Available Tablet splitting is an accepted practice for the administration of drugs for a variety of reasons, including dose adjustment, ease of swallowing and cost savings. The purpose of this study was to evaluate the physical properties of lisinopril tablets as a result of splitting the tablets either by hand or with a splitting device. The impact of the splitting technique of lisinopril (Zestril® tablets, 20 mg on certain physical parameters such as weight variation, friability, disintegration, dissolution and drug content were studied. Splitting the tablets either by hand or with a splitter resulted in a minute but statistically significant average weight loss of <0.25% of the tablet to the surrounding environment. The variability in the weight of the hand-split tablet halves was more pronounced (37 out of 40 tablet halves varied by more than 10% from the mean weight than when using the tablet splitter (3 out of 40 tablet halves. The dissolution and drug content of the hand-split tablets were therefore affected because of weight differences. However, the pharmacopoeia requirements for friability and disintegration time were met. Hand splitting of tablets can result in an inaccurate dose and may present clinical safety issues, especially for drugs with a narrow therapeutic window in which large fluctuations in drug concentrations are undesirable. It is recommended to use tablets with the exact desired dose, but if this is not an option, then a tablet splitter could be used.

  3. Lithium ion implantation effects in MgO(100)

    Energy Technology Data Exchange (ETDEWEB)

    Huis, M.A. van; Fedorov, A.V.; Veen, A. van; Labohm, F.; Schut, H.; Mijnarends, P.E. [Interfaculty Reactor Inst., Delft Univ. of Technology, Delft (Netherlands); Kooi, B.J.; Hosson, J.T.M. de [Rijksuniversiteit Groningen (Netherlands). Materials Science Centre

    2001-07-01

    Single crystals of MgO(100) were implanted with 10{sup 16} {sup 6}Li ions cm{sup -2} at an energy of 30 keV. After ion implantation the samples were annealed isochronally in air at temperatures up to 1200K. After implantation and after each annealing step, the defect evolution was monitored with optical absorption spectroscopy and depth-sensitive Doppler Broadening positron beam analysis (PBA). A strong increase in the S-parameter is observed in the implantation layer at a depth of approximately 100 nm. The high value of the S-parameter is ascribed to positron annihilation in small lithium precipitates. The results of 2D-ACAR and X-TEM analysis show evidence of the presence of lithium precipitates. The depth distribution of the implanted {sup 6}Li atoms was monitored with neutron depth profiling (NDP). It was observed that detrapping and diffusion of {sup 6}Li starts at an annealing temperature of 1200K. (orig.)

  4. Lithium ion implantation effects in MgO(100)

    International Nuclear Information System (INIS)

    Huis, M.A. van; Fedorov, A.V.; Veen, A. van; Labohm, F.; Schut, H.; Mijnarends, P.E.; Kooi, B.J.; Hosson, J.T.M. de

    2001-01-01

    Single crystals of MgO(100) were implanted with 10 16 6 Li ions cm -2 at an energy of 30 keV. After ion implantation the samples were annealed isochronally in air at temperatures up to 1200K. After implantation and after each annealing step, the defect evolution was monitored with optical absorption spectroscopy and depth-sensitive Doppler Broadening positron beam analysis (PBA). A strong increase in the S-parameter is observed in the implantation layer at a depth of approximately 100 nm. The high value of the S-parameter is ascribed to positron annihilation in small lithium precipitates. The results of 2D-ACAR and X-TEM analysis show evidence of the presence of lithium precipitates. The depth distribution of the implanted 6 Li atoms was monitored with neutron depth profiling (NDP). It was observed that detrapping and diffusion of 6 Li starts at an annealing temperature of 1200K. (orig.)

  5. Tramadol and acetaminophen tablets for dental pain.

    OpenAIRE

    Medve, R. A.; Wang, J.; Karim, R.

    2001-01-01

    The purpose of this work was to compare the efficacy and time to analgesia of a new tramadol/acetaminophen combination tablet to those of tramadol or acetaminophen (APAP) alone. A meta-analysis was performed of 3 separate single-dose, double-blind, parallel-group trials in patients with moderate or severe pain following extraction of 2 or more third molars. Patients in each study were evenly randomized to a single dose of tramadol/APAP (75 mg/650 mg), tramadol 75 mg, APAP 650 mg, ibuprofen 40...

  6. Pharmacokinetics of hydrocodone extended-release tablets formulated with different levels of coating to achieve abuse deterrence compared with a hydrocodone immediate-release/acetaminophen tablet in healthy subjects.

    Science.gov (United States)

    Darwish, Mona; Bond, Mary; Tracewell, William; Robertson, Philmore; Yang, Ronghua

    2015-01-01

    A hydrocodone extended-release (ER) formulation employing the CIMA(®) Abuse-Deterrence Technology platform was developed to provide resistance against rapid release of hydrocodone when tablets are comminuted or taken with alcohol. This study evaluated the pharmacokinetics of three hydrocodone ER tablet prototypes with varying levels of polymer coating to identify the prototype expected to have the greatest abuse deterrence potential based on pharmacokinetic characteristics that maintain systemic exposure to hydrocodone comparable to that of a commercially available hydrocodone immediate-release (IR) product. In this four-period crossover study, healthy subjects aged 18-45 years were randomized to receive a single intact, oral 45-mg tablet of one of three hydrocodone ER prototypes (low-, intermediate-, or high-level coating) or an intact, oral tablet of hydrocodone IR/acetaminophen (APAP) 10/325 mg every 6 h until four tablets were administered, with each of the four treatments administered once over the four study periods. Dosing periods were separated by a minimum 5-day washout. Naltrexone 50 mg was administered to block opioid receptors. Blood samples for pharmacokinetic assessments were collected predose and through 72 h postdose. Parameters assessed included maximum observed plasma hydrocodone concentration (C(max)), time to C(max) (t(max)), and area under the concentration-time curve from time 0 to infinity (AUC(0-∞)). Mean C(max) values were 49.2, 32.6, and 28.4 ng/mL for the low-, intermediate-, and high-level coating hydrocodone ER tablet prototypes, respectively, and 37.3 ng/mL for the hydrocodone IR/APAP tablet; respective median t(max) values were 5.9, 8.0, 8.0, and 1.0 h. Total systemic exposure to hydrocodone (AUC(0-∞)) was comparable between hydrocodone ER tablet prototypes (640, 600, and 578 ng·h/mL, respectively) and hydrocodone IR/APAP (581 ng·h/mL). No serious adverse events or deaths were reported. The most common adverse events included

  7. Gravimetric Analysis of Bismuth in Bismuth Subsalicylate Tablets: A Versatile Quantitative Experiment for Undergraduate Laboratories

    Science.gov (United States)

    Davis, Eric; Cheung, Ken; Pauls, Steve; Dick, Jonathan; Roth, Elijah; Zalewski, Nicole; Veldhuizen, Christopher; Coeler, Joel

    2015-01-01

    In this laboratory experiment, lower- and upper-division students dissolved bismuth subsalicylate tablets in acid and precipitated the resultant Bi[superscript 3+] in solution with sodium phosphate for a gravimetric determination of bismuth subsalicylate in the tablets. With a labeled concentration of 262 mg/tablet, the combined data from three…

  8. Technological development of 40mg furosemide tablets: equivalence and bioavaibility study in dogs Desenvolvimento tecnológico da furosemida comprimido (40mg: estudo da equivalência e biodisponibilidade em cães

    Directory of Open Access Journals (Sweden)

    Ednaldo Q. Lima

    2007-11-01

    Full Text Available Furosemide (40mg was administered to 20 street dogs, 10 males and 10 females, in two different pharmaceutical forms: (1 compressed furosemide 40mg formulated at the Federal University of Pernambuco (UFPE-tablet, and (2 a commercial formulation with equal bioequivalence produced by the Laboratory for Pharmaceutical Technology of Pernambuco State (LAFEPE, the LAFEPE-furosemide. The study aimed to evaluate the kinetics of dissolution of the UFPE-tablet in order to analyze the behavior of bioavailability of the best formulation for veterinary use. The plasmatic concentrations of furosemide for the determination of parameters of pharmacological kinetics were analyzed by high-performance liquid chromatographic method (HPLC. The in vitro study accomplished through physiochemical analyses demonstrated that the formulas of the furosemide tablets attained the pharmaceutical requirements in agreement with USP 23 and the Brazilian Pharmacopoeia. The evaluation accomplished in dogs with UFPE-tablets given in only dose demonstrated uniformity in blood levels indicating stability in maintenance of the pharmaceutical formulation and efficiency in absorption of the active compound. These values are not significantly different in relation to the 5% confidence limit. Regarding maximum concentration (Tmax time and global bioavaibility assessed by AUC means, there were no considerable differences as well. UFPE-furosemide displayed 743.492µg/mL.h as AUC average value whereas LAFEPE-furosemide had an average of 537.284µg/mL.h.Furosemida (40mg foi administrada a 20 cães de rua (cães SRD, 10 machos e 10 fêmeas, em duas formas farmacêuicas distintas: (1 furosemida comprimido 40mg formulada na Universidade Federal de Pernambuco (UFPE-comprimido e (2 uma formulação comercial bioequivalente produzida pelo Laboratório de Tecnologia Farmacêutica do Estado de Pernambuco (LAFEPE-furosemida. O estudo objetivou avaliar a cinética de dissolução do UFPE-comprimido para

  9. Bioequivalence of a new liquid formulation of benazepril compared with the reference tablet product.

    Science.gov (United States)

    Kelers, K; Devi, J L; Anderson, G A; Zahra, P; Vine, J H; Whittem, T

    2013-08-01

    To compare the bioequivalence and 'switchability' of two formulations of benazepril (tablet and liquid) after oral administration. Randomised cross-over design, followed by parallel comparison. Twelve mixed-breed dogs were administered either a tablet (Group A) or liquid formulation (Group B) of benazepril orally at 0.45 mg/kg daily for 4 days. With no washout period, the dogs then received the alternative treatment at the same dose for a further 4 days. Blood samples taken prior to treatment and serially after treatment were analysed for plasma concentrations of benazepril and benazeprilat and the activity and concentration of angiotensin-converting enzyme (ACE). The calculated percentage inhibition of ACE was defined as the primary outcome variable. No statistically significant differences were found between groups A and B for any variable evaluated. The mean (± SD) percentage of ACE inhibition was 85.5 ± 7.04% for the liquid formulation and 85.9 ± 6.66% for the tablet formulation. The mean of the ratios was 1.00 (80% confidence interval 0.96-1.04). No evaluated effect term (sequence, formulation or period) had any statistical effect on any outcome variable. This study supports a conclusion that, based on pharmacodynamic response, the liquid formulation of benazepril is bioequivalent to the reference tablet formulation. Further, the lack of a sequence effect supports the switchability of these two formulations. © 2013 Australian Veterinary Association.

  10. A newly developed lubricant, chitosan laurate, in the manufacture of acetaminophen tablets.

    Science.gov (United States)

    Bani-Jaber, Ahmad; Kobayashi, Asuka; Yamada, Kyohei; Haj-Ali, Dana; Uchimoto, Takeaki; Iwao, Yasunori; Noguchi, Shuji; Itai, Shigeru

    2015-04-10

    To study the usefulness of chitosan laurate (CS-LA), a newly developed chitosan salt, as a lubricant, lubrication properties such as the pressure transmission ratio and ejection force were determined at different concentrations of CS-LA in tableting. In addition, tablet properties such as the tensile strength, disintegration time, and dissolution behavior, were also determined. When CS-LA was mixed at concentrations of 0.1%-3.0%, the pressure transmission ratio was increased in a concentration-dependent manner, and the value at a CS-LA concentration of 3% was equal to that of magnesium stearate (Mg-St), a widely used lubricant. Additionally, a reduction in the ejection force was observed at a concentration from 1%, proving that CS-LA has good lubrication performance. A prolonged disintegration time and decreased tensile strength, which are known disadvantages of Mg-St, were not observed with CS-LA. Furthermore, with CS-LA, retardation of dissolution of the drug from the tablets was not observed. Conjugation of CS with LA was found to be quite important for both lubricant and tablet properties. In conclusion, CS-LA should be useful as an alternative lubricant to Mg-St. Copyright © 2015 Elsevier B.V. All rights reserved.

  11. Relative bioavailability of rifampicin, isoniazid and ethambutol from a combination tablet vs. concomitant administration of a capsule containing rifampicin and a tablet containing isoniazid and ethambutol.

    Science.gov (United States)

    Schall, R; Müller, F O; Duursema, L; Groenewoud, G; Hundt, H K; Middle, M V; Mogilnicka, E M; Swart, K J

    1995-11-01

    Twenty male volunteers who were slow metabolisers of isoniazid, completed this single-blind, single-dose, randomised, cross-over study to compare the bioavailability of rifampicin (CAS 13292-46-1), isoniazid (CAS 54-85-3) and ethambutol (CAS 1070-11-7) from Myrin tablets (test preparation) with the bioavailability of these drugs from a combination of capsules containing rifampicin and tablets containing isoniazid and ethambutol (reference). There were 2 treatment periods and on clinic days volunteers were given either the reference (300 mig rifampicin plus 200 mg isoniazid and 600 mg ethambutol HCl), or the test preparation (300 mg rifampicin, 150 mg isoniazid and 600 mg ethambutol HCl). Serial blood samples were drawn from the volunteers and rifampicin, isoniazid and ethambutol assays were performed. The results of this study indicate that the test preparation is equivalent to the reference with respect to both the rate and the extent of absorption of rifampicin, isoniazid (after adjustment for the different doses of isoniazid and ethambutol).

  12. Formulation studies for mirtazapine orally disintegrating tablets.

    Science.gov (United States)

    Yıldız, Simay; Aytekin, Eren; Yavuz, Burçin; Bozdağ Pehlivan, Sibel; Ünlü, Nurşen

    2016-01-01

    Orally disintegrating tablets (ODTs) recently have gained much attention to fulfill the needs for pediatric, geriatric, and psychiatric patients with dysphagia. Aim of this study was to develop new ODT formulations containing mirtazapine, an antidepressant drug molecule having bitter taste, by using simple and inexpensive preparation methods such as coacervation, direct compression and to compare their characteristics with those of reference product (Remereon SolTab). Coacervation method was chosen for taste masking of mirtazapine. In vitro characterization studies such as diameter and thickness, weight variation, tablet hardness, tablet friability and disintegration time were performed on tablet formulations. Wetting time and in vitro dissolution tests of developed ODTs also studied using 900 mL 0.1 N HCl medium, 900 mL pH 6.8 phosphate buffer or 900 mL pH 4.5 acetate buffer at 37 ± 0.2 °C as dissolution medium. Ratio of Eudragit® E-100 was chosen as 6% (w/w) since the dissolution profile of A1 (6% Eudragit® E-100) was found closer to the reference product than A2 (4% Eudragit® E-100) and A3 (8% Eudragit® E-100). Group D, E and F formulations were presented better results in terms of disintegration time. Dissolution results indicated that Group E and F formulations showed optimum properties in all three dissolution media. Formulations D1, D4, D5, E3, E4, F1 and F5 found suitable as ODT formulations due to their favorable disintegration times and dissolution profiles. Developed mirtazapine ODTs were found promising in terms of showing the similar characteristics to the original formulation.

  13. (Gynazole-1® Compared to Fluconazole 150 mg Tablets (Diflucan® in the Time to Relief of Symptoms in Patients With Vulvovaginal Candidiasis

    Directory of Open Access Journals (Sweden)

    Larry S. Seidman

    2005-01-01

    Full Text Available Background. It is estimated that as many as 13 million cases of vulvovaginal infection occur in the United States annually, the majority of which are the result of Candida albicans infection. The symptoms of vulvovaginal infections are often painful and distressing to the patient. The objective of this study was to compare the time to symptomatic relief of vulvovaginal candidiasis (VVC with butoconazole nitrate 2% Site Release® vaginal cream (Gynazole-1® and oral fluconazole 150 mg tablets (Diflucan®.

  14. Design and Evaluation of an Oral Floating Matrix Tablet of ...

    African Journals Online (AJOL)

    Purpose: To develop floating matrix tablets of salbutamol sulphate using ethyl cellulose and acrycoat S-100 as polymers, and sodium bicarbonate, citric acid and tartaric acid as gas generating agents. Methods: Twenty four formulations were prepared and segregated into four major categories, A to D. The floating tablets ...

  15. Pharmacokinetics of colon-specific pH and time-dependent flurbiprofen tablets.

    Science.gov (United States)

    Vemula, Sateesh Kumar; Veerareddy, Prabhakar Reddy; Devadasu, Venkat Ratnam

    2015-09-01

    Present research deals with the development of compression-coated flurbiprofen colon-targeted tablets to retard the drug release in the upper gastro intestinal system, but progressively release the drug in the colon. Flurbiprofen core tablets were prepared by direct compression method and were compression coated using sodium alginate and Eudragit S100. The formulation is optimized based on the in vitro drug release study and further evaluated by X-ray imaging and pharmacokinetic studies in healthy humans for colonic delivery. The optimized formulation showed negligible drug release (4.33 ± 0.06 %) in the initial lag period followed by progressive release (100.78 ± 0.64 %) for 24 h. The X-ray imaging in human volunteers showed that the tablets reached the colon without disintegrating in the upper gastrointestinal tract. The C max of colon-targeted tablets was 12,374.67 ng/ml at T max 10 h, where as in case of immediate release tablets the C max was 15,677.52 ng/ml at T max 3 h, that signifies the ability of compression-coated tablets to target the colon. Development of compression-coated tablets using combination of time-dependent and pH-sensitive approaches was suitable to target the flurbiprofen to colon.

  16. Orodispersible tablets containing taste-masked solid lipid pellets with metformin hydrochloride: Influence of process parameters on tablet properties.

    Science.gov (United States)

    Petrovick, Gustavo Freire; Kleinebudde, Peter; Breitkreutz, Jörg

    2018-01-01

    Compaction of multiparticulates into tablets, particularly into orodispersible tablets (ODTs), is challenging. The compression of pellets, made by solid lipid extrusion/spheronization processes, presents peculiar difficulties since solid lipids usually soften or melt at relatively low temperature ranges and due to applied mechanical forces. Until now, there are no reports in literature about the development of ODTs based on solid lipid pellets. To investigate the feasibility of producing such tablets, a design of experiment (DoE) approach was performed to elucidate the influence of compression force and amount of two co-processed excipients (Ludiflash ® and Parteck ® ODT) on properties of the tablets (friability, tensile strength, and disintegration time). ODTs (15 mm, flat-faced) with solid lipid pellets (250-1000 µm in diameter) containing 500 mg of metformin HCl, presenting immediate drug release profile and taste-masked properties, were targeted. During compression, a strong lamination of the tablets containing Parteck ® ODT was observed. This phenomenon was prominently observed when high compression forces (≥5 kN) and high excipient amounts (≥40%; w/w) were used. On the other hand, the DoE focused on tablets with Ludiflash ® showed better results regarding the production of ODTs. A positive influence of the compression force on the tensile strength and disintegration time of the tablets, regarding specifications of the Ph. Eur., was observed. The increase in the amount of this excipient resulted in fast disintegrating tablets, however, a negative influence on the tensile strength was noticed. After optimization of the parameters and formulation, based on the DoE results and considering the Ph. Eur. specifications for tablets, ODTs based on lipid pellets containing metformin HCl presenting immediate release profile (85% drug release in less than 30 min) and taste-masked properties (determined by an electronic tongue) were successfully

  17. Formulation, Characterization and Physicochemical Evaluation of Ranitidine Effervescent Tablets

    Directory of Open Access Journals (Sweden)

    Abolfazl Aslani

    2013-08-01

    Full Text Available Purpose: The aim of this study was to design, formulate and physicochemically evaluate effervescent ranitidine hydrochloride (HCl tablets since they are easily administered while the elderly and children sometimes have difficulties in swallowing oral dosage forms. Methods: Effervescent ranitidine HCl tablets were prepared in a dosage of 300 mg by fusion and direct compression methods. The powder blend and granule mixture were evaluated for various pre-compression characteristics, such as angle of repose, compressibility index, mean particle size and Hausner's ratio. The tablets were evaluated for post-compression features including weight variation, hardness, friability, drug content, dissolution time, carbon dioxide content, effervescence time, pH, content uniformity and water content. Effervescent systems with appropriate pre and post-compression qualities dissolved rapidly in water were selected as the best formulations. Results: The results showed that the flowability of fusion method is more than that of direct compression and the F5 and F6 formulations of 300 mg tablets were selected as the best formulations because of their physicochemical characteristics. Conclusion: In this study, citric acid, sodium bicarbonate and sweeteners (including mannitol, sucrose and aspartame were selected. Aspartame, mint and orange flavors were more effective for masking the bitter taste of ranitidine. The fusion method is the best alternative in terms of physicochemical and physical properties.

  18. Vandetanib (100 mg) in patients with locally advanced or metastatic hereditary medullary thyroid cancer.

    Science.gov (United States)

    Robinson, Bruce G; Paz-Ares, Luis; Krebs, Annetta; Vasselli, James; Haddad, Robert

    2010-06-01

    Vandetanib is a once-daily oral inhibitor of vascular endothelial growth factor receptor-2 and epidermal growth factor receptor tyrosine kinases that also inhibits rearranged during transfection kinase activity. Vandetanib (300 mg/d) has previously demonstrated antitumor activity in patients with advanced hereditary medullary thyroid cancer (MTC). This study investigated the efficacy and safety of 100 mg/d vandetanib in patients with advanced hereditary MTC. Eligible patients with unresectable, measurable, locally advanced, or metastatic hereditary MTC received 100 mg/d vandetanib. Upon disease progression, eligible patients could enter postprogression treatment with 300 mg/d vandetanib until a withdrawal criterion was met. The primary objective was to assess the objective response rate by response evaluation criteria in solid tumors. The study comprised 19 patients (13 males, six females; mean age 45 yr). Confirmed objective partial responses were observed in three patients, yielding an objective response rate of 16% (95% confidence interval 3.4-39.6). Stable disease lasting 24 wk or longer was reported in a further 10 patients (53%); the disease control rate was therefore 68% (95% confidence interval 43.4-87.4). Serum levels of calcitonin and carcinoembryonic antigen showed a sustained 50% or greater decrease from baseline in 16% (three of 19) and 5% (one of 19) of patients, respectively. Adverse events were predominantly grade 1 or 2 and consistent with previous vandetanib monotherapy studies. Vandetanib at a once-daily dose of 100 mg has clinically relevant antitumor activity in patients with locally advanced or metastatic hereditary MTC and an overall acceptable safety profile.

  19. Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl.

    Science.gov (United States)

    El Nabarawi, Mohamed A; Teaima, Mahmoud H; Abd El-Monem, Rehab A; El Nabarawy, Nagla A; Gaber, Dalia A

    2017-01-01

    To prolong the residence time of dosage forms within the gastrointestinal tract until all drug is released at the desired rate is one of the real challenges for oral controlled-release drug delivery systems. This study was designed to develop a controlled-release floating matrix tablet and floating raft system of Mebeverine HCl (MbH) and evaluate different excipients for their floating behavior and in vitro controlled-release profiles. Oral pharmacokinetics of the optimum matrix tablet, raft system formula, and marketed Duspatalin ® 200 mg retard as reference were studied in beagle dogs. The optimized tablet formula (FT-10) and raft system formula (FRS-11) were found to float within 34±5 sec and 15±7 sec, respectively, and both remain buoyant over a period of 12 h in simulated gastric fluid. FT-10 (Compritol/HPMC K100M 1:1) showed the slowest drug release among all prepared tablet formulations, releasing about 80.2% of MbH over 8 h. In contrast, FRS-11 (Sodium alginate 3%/HPMC K100M 1%/Precirol 2%) had the greatest retardation, providing sustained release of 82.1% within 8 h. Compared with the marketed MbH product, the C max of FT-10 was almost the same, while FRS-11 maximum concentration was higher. The t max was 3.33, 2.167, and 3.0 h for marketed MbH product, FT-10, and FRS-11, respectively. In addition, the oral bioavailability experiment showed that the relative bioavailability of the MbH was 104.76 and 116.01% after oral administration of FT-10 and FRS-11, respectively, compared to marketed product. These results demonstrated that both controlled-released floating matrix tablet and raft system would be promising gastroretentive delivery systems for prolonging drug action.

  20. In vitro quality evaluation of leading brands of ciprofloxacin tablets available in Bangladesh.

    Science.gov (United States)

    Uddin, Md Sahab; Mamun, Abdullah Al; Hossain, Md Saddam; Asaduzzaman, Md; Sarwar, Md Shahid; Rashid, Mamunur; Herrera-Calderon, Oscar

    2017-05-30

    Ciprofloxacin is a broad-spectrum antibiotic that acts against a number of bacterial infections. The study was carried out to examine the in vitro quality control tests for ten leading brands of ciprofloxacin hydrochloride 500 mg tablet formulation, registered in Bangladesh by Directorate General of Drug Administration. The quality control parameters of ten different brands of ciprofloxacin hydrochloride 500 mg tablets were determined by weight variation, friability, hardness, disintegration, dissolution and assay tests. All the tablets were evaluated for conformity with United States Pharmacopoeia-National Formulary (USP-NF) and British Pharmacopoeia (BP) standards. Among ten brands of tablets Brand C had lower mean weight variation of 1.59% and Brand E had highest mean weight variation of 3.32%. For friability test Brand F had lowest mean friability (0.27%) and Brand G had highest mean friability (0.54%). Among ten brands mean lowest and highest hardness were founded in Brand G (4.49 kg/cm 2 ) and Brand F (7.13 kg/cm 2 ) respectively. The disintegration time for ten brands of ciprofloxacin tablet obtained were in the subsequent order: Brand G (8.19 min) leading brands of this tablet met the quality control parameters as per pharmacopoeial specifications except dissolution test for four brands (Brand J, Brand H, Brand I, and Brand F).

  1. Epitaxial (100)-oriented Mo/V superlattice grown on MgO(100) by dcMS and HiPIMS

    International Nuclear Information System (INIS)

    Shayestehaminzadeh, S.; Magnusson, R.L.; Gislason, H.P.; Olafsson, S.

    2013-01-01

    Epitaxial (100)-oriented Mo/V superlattices have been grown by High Power Impulse Magnetron Sputtering (HiPIMS) and dc Magnetron Sputtering (dcMS) on single-crystalline MgO(100) substrates at growth temperatures ranging from 30 °C to 600 °C. Superlattice bilayer period of Mo/V around 12/12 monolayers and 15 repeat periods was studied. This study aims to investigate the effect of the HiPIMS process on reducing the growth temperature of Mo/V superlattices using the high energy ionized Mo, V species in the HiPIMS plasma. In one case, the Mo layer was only grown with the HiPIMS process and V layer grown using the dcMS process while in another both layers were grown with the HiPIMS process. The as-deposited films were characterized by X-ray reflection and diffraction techniques. The dcMS process was found to give superior superlattice growth at high growth temperatures while a mixed Mo HiPIMS and V dcMS process gives better result at lower growth temperatures (300 °C). Room temperature growth reveals that neither the mixed Mo HiPIMS and V dcMS process nor the pure HiPIMS for both materials can produce better result compared to the pure dcMS process, which gives a relatively better result. - Highlights: • Epitaxial (100)-oriented Mo/V superlattices have been grown by HiPIMS and dcMS on MgO(100) for various temperatures. • The study was aimed to investigate the effect of ionized HiPIMS process onlowering the growth temperature. • The dcMS process was found to give superior superlattice growth at high growth temperature. • The mixed Mo HiPIMS and V dcMS process gives best result at lower growth temperatures

  2. Validating the Accuracy of Reaction Time Assessment on Computer-Based Tablet Devices.

    Science.gov (United States)

    Schatz, Philip; Ybarra, Vincent; Leitner, Donald

    2015-08-01

    Computer-based assessment has evolved to tablet-based devices. Despite the availability of tablets and "apps," there is limited research validating their use. We documented timing delays between stimulus presentation and (simulated) touch response on iOS devices (3rd- and 4th-generation Apple iPads) and Android devices (Kindle Fire, Google Nexus, Samsung Galaxy) at response intervals of 100, 250, 500, and 1,000 milliseconds (ms). Results showed significantly greater timing error on Google Nexus and Samsung tablets (81-97 ms), than Kindle Fire and Apple iPads (27-33 ms). Within Apple devices, iOS 7 obtained significantly lower timing error than iOS 6. Simple reaction time (RT) trials (250 ms) on tablet devices represent 12% to 40% error (30-100 ms), depending on the device, which decreases considerably for choice RT trials (3-5% error at 1,000 ms). Results raise implications for using the same device for serial clinical assessment of RT using tablets, as well as the need for calibration of software and hardware. © The Author(s) 2015.

  3. A new experimental design method to optimize formulations focusing on a lubricant for hydrophilic matrix tablets.

    Science.gov (United States)

    Choi, Du Hyung; Shin, Sangmun; Khoa Viet Truong, Nguyen; Jeong, Seong Hoon

    2012-09-01

    A robust experimental design method was developed with the well-established response surface methodology and time series modeling to facilitate the formulation development process with magnesium stearate incorporated into hydrophilic matrix tablets. Two directional analyses and a time-oriented model were utilized to optimize the experimental responses. Evaluations of tablet gelation and drug release were conducted with two factors x₁ and x₂: one was a formulation factor (the amount of magnesium stearate) and the other was a processing factor (mixing time), respectively. Moreover, different batch sizes (100 and 500 tablet batches) were also evaluated to investigate an effect of batch size. The selected input control factors were arranged in a mixture simplex lattice design with 13 experimental runs. The obtained optimal settings of magnesium stearate for gelation were 0.46 g, 2.76 min (mixing time) for a 100 tablet batch and 1.54 g, 6.51 min for a 500 tablet batch. The optimal settings for drug release were 0.33 g, 7.99 min for a 100 tablet batch and 1.54 g, 6.51 min for a 500 tablet batch. The exact ratio and mixing time of magnesium stearate could be formulated according to the resulting hydrophilic matrix tablet properties. The newly designed experimental method provided very useful information for characterizing significant factors and hence to obtain optimum formulations allowing for a systematic and reliable experimental design method.

  4. Multiple-unit tablet of probiotic bacteria for improved storage stability, acid tolerability, and in vivo intestinal protective effect

    Directory of Open Access Journals (Sweden)

    Park HJ

    2016-04-01

    Full Text Available Hee Jun Park,1 Ga Hyeon Lee,1 Joonho Jun,1 Miwon Son,1 Myung Joo Kang2 1Dong-A Pharmaceutical Co. Ltd., Yongin, Gyeonggi, 2College of Pharmacy, Dankook University, Cheonan, Chungnam, Korea Abstract: The aim of this study was to formulate probiotics-loaded pellets in a tablet form to improve storage stability, acid tolerability, and in vivo intestinal protective effect. Bacteria-loaded pellets primarily prepared with hydroxypropyl methylcellulose acetate succinate were compressed into tablets with highly compressible excipients and optimized for flow properties, hardness, and disintegration time. The optimized probiotic tablet consisted of enteric-coated pellets (335 mg, microcrystalline cellulose (Avicel PH102, 37.5 mg, and porous calcium silicate (25 mg and allowed whole survival of living bacteria during the compaction process with sufficient tablet hardness (13 kp and disintegration time (14 minutes. The multiple-unit tablet showed remarkably higher storage stability under ambient conditions (25°C/60% relative humidity over 6 months and resistance to acidic medium compared to uncoated strains or pellets. Repeated intake of this multiple-unit tablet significantly lowered plasma level of endotoxin, a pathogenic material, compared to repeated intake of bare probiotics or marketed products in rats. These results, therefore, suggest that the multiple-unit tablet is advantageous to better bacterial viability and gain the beneficial effects on the gut flora, including the improvement of intestinal barrier function. Keywords: probiotics, multiple-unit tablet, bacterial viability, acid resistance, intestinal barrier function

  5. Graphite Furnace Atomic Absorption Elemental Analysis of Ecstasy Tablets

    OpenAIRE

    French, Holly E.; Went, Michael J.; Gibson, Stuart J.

    2013-01-01

    Abstract: Six metals (Cu, Mg, Ba, Ni, Cr, Pb) were determined in two separate batches of seized ecstasy\\ud tablets by graphite furnace atomic absorption spectroscopy (GFAAS) following digestion with nitric\\ud acid and hydrogen peroxide. Large intra-batch variations were found as expected for tablets produced\\ud in clandestine laboratories. For example, nickel in batch 1 was present in the range 0.47-13.1 ppm and\\ud in batch 2 in the range 0.35-9.06 ppm. Although batch 1 had significantly high...

  6. [Tablets and tablet production - with special reference to Icelandic conditions].

    Science.gov (United States)

    Skaftason, Jóhannes F; Jóhannesson, Thorkell

    2013-04-01

    Modern tablet compression was instituted in England in 1844 by William Brockedon (1787-1854). The first tablets made according to Brockedon´s procedures contained watersoluble salts and were most likely compressed without expedients. In USA a watershed occurred around 1887 when starch (amylum maydis) was introduced to disperse tablets in aqueous milieu in order to corroborate bioavailability of drugs in the almentary canal. About the same time great advances in tablet production were introduced by the British firm Burroughs Wellcome and Co. In Denmark on the other hand tablet production remained on low scale until after 1920. As Icelandic pharmacies and drug firms modelled themselves mostly upon Danish firms tablet production was first instituted in Iceland around 1930. The first tablet machines in Iceland were hand-driven. More efficent machines came after 1945. Around 1960 three sizeable tablet producers were in Iceland; now there is only one. Numbers of individual tablet species (generic and proprietary) on the market rose from less than 10 in 1913 to 500 in 1965, with wide variations in numbers in between. Tablets have not wiped out other medicinal forms for peroral use but most new peroral drugs have been marketed in the form of tablets during the last decades.

  7. VERIFICATION HPLC METHOD OF QUANTITATIVE DETERMINATION OF AMLODIPINE IN TABLETS

    Directory of Open Access Journals (Sweden)

    Khanin V. A

    2014-10-01

    a volume of 100.0 ml. Preparation of the working standard solution sample amlodipine besylate. 50.0 mg of amlodipine RCC dissolved in methanol and dilute with the same solvent to 50.0 ml. 5.0 ml of this solution argue with methanol to volume 100.0 ml. Before the major controlled trials validated the existence of documents certifying the suitability vykorystovanoho equipment, raw materials and chemicals. Validation of the methodology was carried out in accordance with the requirements of SPhU. Results & discussion. Linearity methods defined within 80-120% of nominal concentrations. The linearity of the methods supported by the entire range of concentrations studied (b=0.9845, Sb=0,01473, a=1.5282, Sa=1.4956, S0=0.5486, r=0.9992. It is proved that the validated method characterized by sufficient convergence and accuracy over the entire range of concentrations (ΔZ=1.03, δ%=0.09. Conclusion. During verification methods of quantitative determination of amlodipine besylate tablets were studied characteristics validated HPLC method: accuracy, linearity, precision, specificity, and internal laboratory precision. Validation technique characteristics do not exceed the critical value of error (1.6% and characterized by qualitative analytical indicators. This technique can be correctly reproduced in the laboratory conditions, and is independent of the excipients.

  8. COMPARATIVE ANALYSIS OF FIVE BRANDS OF LISINOPRIL TABLETS IN YEMENI MARKET

    Directory of Open Access Journals (Sweden)

    Gamil Q. Othman

    2014-12-01

    Full Text Available Background: In poor countries such as Yemen, the cost of drugs is a factor affecting the patient’s decision to buy it and generic medicines are introduced as cheaper alternatives to the high cost brands. Thus, this study aimed to identify the physicochemical similarity of five products of tablets comprising much Lisinopril (antihypertensive taken from various pharmacies where retail medications are rendered to the Yemeni market. Methods: In this study, the researcher has conducted an assessment to the quality and physicochemical uniformity of five various products of Lisinopril tablets. The uniformity of weight, friability, crushing strength, disintegration and dissolution tests and chemical test of the tablets were evaluated as major factors. Results: Results showed that all five products of the Lisinopril 5 mg tablets were compatible to the standards of British Pharmacopoeia (BP in terms of uniformity of weight (91.04 – 137.4%, the crushing strength/hardness test (3.93 – 7.92% and the friability test (0.18 – 0.29%. All the products have showed good results about the disintegration time (15 sec – 7 min and 5 sec and dissolution test (96.67 – 103.7%. The active content of products ranged from 102.8 – 108%. Conclusion: The five brands of Lisinopril 5mg tablets, which were analyzed, have matched the BP quality standards and were physically and chemically consistent. Thus, cheap generic medicine can be used as alternative for innovator products.

  9. A study on friability, hardness and fiber content analysis of fiber enriched milk tablet

    Science.gov (United States)

    Suzihaque, M. U. H.; Irfan, M. H.; Ibrahim, U. K.

    2017-06-01

    This study was performed to analyze the friability, hardness and fiber content of fiber enriched milk tablet derived from five different local fiber sources such as carrot, spinach, dragon fruit, mango and watermelon. Cow milk was mixed to complement with the tablet as a protein source. The powder were spray dried at 100°C, 120°C and 140°C and freeze dried at -60°C. The mixture of fruits and milk were made into equal ratio with the addition of 15 maltodextrin as a carrier. Tablets formed were used for friability and hardness test while dried powder were used for fiber content analysis. Dragon fruit tablet dried at 140°C have the highest friability with 11. 42 of weight loss. The second highest friability was spinach tablet dried at 100°C and 120°C drying temp erature with 9.30 and 9.28 respectively. The lowest friability was exhibited by carrot, mango and watermelon tablet at 100°C and dragon fruit at 120°C while carrot and spinach at 140°C. In contras t, none of the freeze dried tablets showed any weight loss hence they are not friable. For hardness test, all of the freeze dried showed to have higher tensile strength than spray dried, where carrot showed to be the highest at 2.27 Newton and the lowest were spray dried mango at 0.16 Newton. In fiber content analysis, freeze dried mango have the highest fiber content followed by freeze dried carrot and 140°C s pray dried carrot. It can be concluded that the higher the spray dry temperature, the more friable is the tablet. While, high friability leads to lower hardness of tablets. In terms of fiber content, the higher the spray dry temperature, the lower the fiber content found.

  10. Hardness and microstructure of Al-10.0 wt% Zn-4.0 wt% Mg alloy

    International Nuclear Information System (INIS)

    Iqbal, M.; Shaikh, M.A.; Ahmad, W.; Ali, K.L.

    1996-01-01

    Al-Zn-Mg alloys are widely used in industries as these have excellent physical and mechanical properties. However some aspects of the effect of heat treatment on these alloys are not yet clear. In order to understand the precipitation phenomena in these alloys, microstructure of a locally prepared alloy Al-10.0 wt% Zn-4.0 wt% Mg heat treated under different conditions has been examined in scanning electron microscope/electron probe micro analyser. Precipitates MgZn/sub 2/, MgZn/sub 4/ and Mg/sub 2/Zn/sub 11/ have been observed and these are caused by heat treatment. Correlation between these precipitates and Vickers's hardness has also been studied. In the present paper results of this investigation have been presented and discussed. (author)

  11. The comparison of hyaluronic acid vaginal tablets with estradiol vaginal tablets in the treatment of atrophic vaginitis: a randomized controlled trial.

    Science.gov (United States)

    Ekin, Murat; Yaşar, Levent; Savan, Kadir; Temur, Muzaffer; Uhri, Mehmet; Gencer, Işıl; Kıvanç, Esra

    2011-03-01

    To compare the effectiveness of the vaginal tablets of hyaluronic acid and estrodiol for the treatment of atrophic vaginitis. Forty-two postmenopausal women with symptoms of atrophic vaginitis were randomized to take vaginal tablets of 25 μg estradiol (n = 21) (group I) or 5 mg hyaluronic acid sodium salt (n = 21) (group II) for 8 weeks. The symptoms of atrophic vaginitis were evaluated by a self-assessed 4-point scale of composite score and the degree of epithelial atrophy was determined as, none, mild, moderate and severe. Vaginal pH and maturation index were measured and compared in both the groups. The symptoms were relieved significantly in both the groups (P Hyaluronic acid vaginal tablets can be used in patients with atrophic vaginitis who do not want to or can not take local estrogen treatment.

  12. Morphology evolution of thin Ni film on MgO(100) substrate

    International Nuclear Information System (INIS)

    Lin, C.; Xu, Y.H.; Naramoto, H.; Wei, P.; Kitazawa, S.; Narumi, K.

    2002-01-01

    Thin Ni films with various thicknesses were deposited onto the MgO(100) single crystal substrate at 400 deg. C. The morphology measured by atomic force microscope shows an apparent correlation with the thickness. The initial 10 A film is composed of small round Ni islands. In the 25 A film, pinholes with narrow size distribution occur, which show local periodic distribution in some regions when the thickness of the film reaches 75 A. The driving force for such a structure is attributed to the elastic strain energy. When the film is about 100 A thick, the pinholes begin to disappear, due to filling by the late-coming atoms and covering of upper islands. (author)

  13. A bioequivalence study of two tamsulosin sustained-release tablets in Indonesian healthy volunteers.

    Science.gov (United States)

    Prasaja, Budi; Harahap, Yahdiana; Lusthom, Windy; Setiawan, Evy C; Ginting, Mena B; Hardiyanti; Lipin

    2011-06-01

    The bioavailability of two 0.4 mg tamsulosin sustained-release film-coated tablet formulations was compared; using generic tablets (Prostam(®)) as test formulation and the originator product as reference formulation. Twenty-four subjects were included in this single-dose, open-label, randomized two-way crossover design following an overnight fasting. A one-week wash-out period was applied. Blood samples were drawn up to 72 h following drug administration. Plasma concentration of tamsulosin was determined by liquid chromatography-tandem mass spectrometry method with TurboIonSpray mode. Pharmacokinetic parameters AUC(0-t,) AUC(0-∞), C (max) and t (½) were determined and used for bioequivalence evaluation after log-transformation, whereas t (max) ratios were evaluated non-parametrically. The estimated point and 90% confidence intervals (CI) for AUC(0-t,) AUC(0-∞), C (max) and t (½) were 109.55% (96.41-124.49%), 109.94% (96.85-124.81%), 105.87% (92.88-120.67%) and 100.00% (90.56-110.43%), respectively. These results indicated that the two formulations of tamsulosin were bioequivalent; therefore they may be prescribed interchangeably.

  14. A Study on the Use of Primolut-N Tablet as a Contraceptive in the ...

    African Journals Online (AJOL)

    Objective: This study investigated into the use of Primolut-N tablet which contains norethisterone (5 mg), popularly called 'N-tablet' by users, as a pre-coital contraceptive by women in the Kumasi metropolis of Ghana. Methods: Clients who called at any of the Twenty (20) selected Pharmacies in residential areas within the ...

  15. PROFIL DISOLUSI DAN PENETAPAN KADAR TABLET MELOKSIKAM INOVATOR DAN GENERIK BERMEREK DENGAN KCKT (KROMATOGRAFI CAIR KINERJA TINGGI

    Directory of Open Access Journals (Sweden)

    D. Mutiatikum

    2012-07-01

    Full Text Available Abstract. The determination of meloxicam and the dissolution test has been done. Drug dissolution test is an approach to evaluate drug release characteristics of product (Tablets/capsules in vitro. The tests are conducted for various durations from 5,10,15,20,25,30,40,50 and 60 minutes with appropriate sampling. The method of dissolution test and assay of meloxicam accords with British Pharmacopoeia 2007. A control  experiment wih HPLC was performed simoultaneously. The dissolution test of meloxicam at 30 minutes in tablet A is 97.79% and tablet B is 87.78% meet the requirement of the British Pharmacopoeia 2007. The content of meloxicam are in tablet A is 100.26%, tablet B is 104.07%. Both of its meet the requirement of British Pharmacopoeia 2007. The content of meloxicam are in tablet A is 100.26%, tablet B is 104.07%. Both of its meet the requirement of British Pharmacopoeia 2007.Key Words : Meloksikam, KCKT

  16. To Study Capping or Lamination Tendency of Tablets Through Evaluation of Powder Rheological Properties and Tablet Mechanical Properties of Directly Compressible Blends.

    Science.gov (United States)

    Dudhat, Siddhi M; Kettler, Charles N; Dave, Rutesh H

    2017-05-01

    Air entrapment efficiency of the powders is one of the main factors leading to occurrence of capping or lamination tendency of tablets manufactured from the directly compressible powder blends. The purpose of the current research was to study this underlying cause leading to occurrence of capping or lamination of tablets through evaluation of powder rheological properties. Powder blends were prepared by addition of 0% w/w to 100% w/w of individual active pharmaceutical ingredient (API) [two model API: acetaminophen (APAP) and ibuprofen (IBU)] with microcrystalline cellulose without and with 0.5% w/w Magnesium Stearate as lubricant. Powder rheological properties were analyzed using FT4 Powder Rheometer for dynamic, bulk, and shear properties. Tablet mechanical properties of the respective blends were studied by determining the ability of the material to form tablet of specific strength under applied compaction pressure through tabletability profile. The results showed that powder rheometer distinguished the powder blends based on their ability to relieve entrapped air along with the distinctive flow characteristics. Powder blend prepared with increasing addition of APAP displayed low powder permeability as compared to IBU blends with better powder permeability, compressibility and flow characteristics. Also, lubrication of the APAP blends did not ease their ability to relieve air. Tabletability profiles revealed the potential occurrence of capping or lamination in tablets prepared from the powder blends with high APAP content. This study can help scientist to understand tableting performance at the early-developmental stages and can avoid occurrence capping and lamination of tablets.

  17. Marine Corps Counterterrorism: Determining Medical Supply Needs for the Chemical Biological Incident Response Force

    Science.gov (United States)

    2004-03-04

    80.33 6505009269197 Ipecac Syrup USP 7% 30ml 1 BT 0.01 0.30 $0.93 0.01 0.3 $0.93 6505001326904 Isoniazid Tablets USP 300 Mg 100s...Administer Appropriate Medication 6505000648724 Acetazolamide Sodium Sterile USP 500mg Vial 0.5 VI 29 6505001009985 Aspirin Tablets USP 0.324gm 100s...6505012149062 Ibuprofen Tablets USP 800 Mg 500 Tablets Per Bottle 1 EA 7 6515013448487 Injector Tube Reusable 1ml & 2ml Ndl Units 1 EA

  18. TabletGaze: Unconstrained Appearance-based Gaze Estimation in Mobile Tablets

    OpenAIRE

    Huang, Qiong; Veeraraghavan, Ashok; Sabharwal, Ashutosh

    2015-01-01

    We study gaze estimation on tablets, our key design goal is uncalibrated gaze estimation using the front-facing camera during natural use of tablets, where the posture and method of holding the tablet is not constrained. We collected the first large unconstrained gaze dataset of tablet users, labeled Rice TabletGaze dataset. The dataset consists of 51 subjects, each with 4 different postures and 35 gaze locations. Subjects vary in race, gender and in their need for prescription glasses, all o...

  19. Determination of Modafinil in Tablet Formulation Using Three New Validated Spectrophotometric Methods

    International Nuclear Information System (INIS)

    Basniwal, P.K.; Jain, D.; Basniwal, P.K.

    2014-01-01

    In this study, three new UV spectrophotometric methods viz. linear regression equation (LRE), standard absorptivity (SA) and first order derivative (FOD) method were developed and validated for determination of modafinil in tablet form. The Beer-Lamberts law was obeyed as linear in the range of 10-50 μg/ mL and all the methods were validated for linearity, accuracy, precision and robustness. These methods were successfully applied for assay of modafinil drug content in tablets in the range of 100.20 - 100.42 %, 100.11 - 100.58 % and 100.25 - 100.34 %, respectively with acceptable standard deviation (less than two) for all the methods. The validated spectrophotometric methods may be successfully applied for assay, dissolution studies, bio-equivalence studies as well as routine analysis in pharmaceutical industries. (author)

  20. Correlation between the viscoelastic properties of the gel layer of swollen HPMC matrix tablets and their in vitro drug release.

    Science.gov (United States)

    Hamed, Rania; Al Baraghthi, Tamadur; Sunoqrot, Suhair

    2016-11-21

    Drug release from hydroxypropyl methylcellulose (HPMC) hydrophilic matrix tablets is controlled by drug diffusion through the gel layer of the matrix-forming polymer upon hydration, matrix erosion or combination of diffusion and erosion mechanisms. In this study, the relationship between viscoelastic properties of the gel layer of swollen intact matrix tablets and drug release was investigated. Two sets of quetiapine fumarate (QF) matrix tablets were prepared using the high viscosity grade HPMC K4M at low (70 mg/tablet) and high (170 mg/tablet) polymer concentrations. Viscoelastic studies using a controlled stress rheometer were performed on swollen matrices following hydration in the dissolution medium for predetermined time intervals. The gel layer of swollen tablets exhibited predominantly elastic behavior. Results from the in vitro release study showed that drug release was strongly influenced by the viscoelastic properties of the gel layer of K4M tablets, which was further corroborated by results from water uptake studies conducted on intact tablets. The results provide evidence that the viscoelastic properties of the gel layer can be exploited to guide the selection of an appropriate matrix-forming polymer, to better understand the rate of drug release from matrix tablets in vitro and to develop hydrophilic controlled-release formulations.

  1. A Liquid Chromatography-Tandem Mass Spectrometry Method for Evaluation of Two Brands of Enalapril 20 mg Tablets in Healthy Human Volunteers

    Directory of Open Access Journals (Sweden)

    Wael Abu Dayyih

    2017-01-01

    Full Text Available Enalapril is an angiotensin-converting enzyme inhibitor used for treatment of hypertension and chronic heart disease. Enalaprilat is its active metabolite responsible for the activity. This study aimed to develop and validate a method for enalapril and enalaprilat analysis and to determine the bioequivalence of two tablet formulae of enalapril. LC-MS/MS bioanalytical method was developed and validated and then applied to evaluate the bioavailability of two enalapril formulae. Antihyperglycemic sitagliptin was used as internal standard (IS. The method was accurate for the within- and between-days analysis, and precise CV% was 85% and the LOD was 0.907 and 0.910 ng/ml for enalapril and enalaprilat, respectively, and LLOQ was 1 ng/ml. The pharmacokinetic parameters Cmax, tmax, AUC0–72, and AUC0–∞ values of enalapril and enalaprilat of the two formulae were calculated and nonsignificant differences were found. A linearity, specific, accurate, and precise method was developed and applied for the analysis of enalapril and enalaprilat in human plasma after oral administration of two formulae of enalapril 20 mg tablets in healthy volunteers. Depending on the statistical analysis it was concluded that the two enalapril formulae were bioequivalent.

  2. PREPARATION AND CHARACTERIZATION OF CHITOSAN TABLETS OF ACECLOFENAC FOR COLON TARGETED DRUG DELIVERY

    OpenAIRE

    UMA DEVI,THIRUGANESH, SURESH

    2013-01-01

    The present study objective was to develop novel colon specific drug delivery systems for aceclofenac using chitosan as a microbially degradable polymeric carrier and to coat the optimized batches with a pH dependent polymeric coating solution containing Eudragit L 100 and S 100 (1:4). Tablets containing four proportions of chitosan were prepared. The tablets were evaluated for physicochemical properties, drug content, dissolution, water uptake & erosion characteristics, in vitro drug rel...

  3. Epitaxial growth of fcc-CoxNi100-x thin films on MgO(110) single-crystal substrates

    International Nuclear Information System (INIS)

    Ohtake, Mitsuru; Nukaga, Yuri; Sato, Yoichi; Futamoto, Masaaki; Kirino, Fumiyoshi

    2009-01-01

    Co x Ni 100-x (x=100, 80, 20, 0 at. %) epitaxial thin films were prepared on MgO(110) single-crystal substrates heated at 300 deg. C by ultrahigh vacuum molecular beam epitaxy. The growth mechanism is discussed based on lattice strain and crystallographic defects. CoNi(110) single-crystal films with a fcc structure are obtained for all compositions. Co x Ni 100-x film growth follows the Volmer-Weber mode. X-ray diffraction analysis indicates that the out-of-plane and the in-plane lattice spacings of the Co x Ni 100-x films are in agreement within ±0.5% with the values of the respective bulk Co x Ni 100-x crystals, suggesting that the strain in the film is very small. High-resolution cross-sectional transmission microscopy shows that an atomically sharp boundary is formed between a Co(110) fcc film and a MgO(110) substrate, where periodical misfit dislocations are preferentially introduced in the film at the Co/MgO interface. The presence of such periodical misfit dislocations relieves the strain caused by the lattice mismatch between the film and the substrate.

  4. Antibacterial Properties of Tebipenem Pivoxil Tablet, a New Oral Carbapenem Preparation against a Variety of Pathogenic Bacteria in Vitro and in Vivo

    Directory of Open Access Journals (Sweden)

    Qi Yao

    2016-01-01

    the sepsis-model mice as compared with the control. Furthermore, the survival rate in the tebipenem pivoxil tablet group was remarkably higher than that in the meropenem group in all the sepsis mouse models tested. In the sepsis model challenged with Staphylococcus aureus ATCC29213, Escherichia coli ATCC25922, Pseudomonas aeruginosa ATCC27853, and Pseudomonas aeruginosa clinical strain, respectively, tebipenem pivoxil tablet (100 mg/kg displayed a better protective effect than tebipenem pivoxil granules (100 mg/kg. Conclusions: In summary, tebipenem pivoxil displays an excellent antibacterial activity against a variety of pathogenic bacteria in vitro. Importantly, tebipenem pivoxil tablet significantly protects the sepsis mice challenged with various pathogenic bacteria, which may provide a potential approach to treating bacterial sepsis in clinic.

  5. Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac

    Directory of Open Access Journals (Sweden)

    Ehab Mostafa Elzayat

    2017-07-01

    Full Text Available The rapid availability of the drug at the site of action followed by maintaining its effect for a long period of time is of great clinical importance. Thus, the purpose of the present study was to prepare and evaluate multi-layered matrix tablets of diclofenac using Eudragit RL/RS blend to achieve both immediate and sustained therapeutic effects. Diclofenac potassium (25 mg was incorporated in an outer immediate release layer to provide immediate pain relief whereas diclofenac sodium (75 mg was incorporated in the inner core to provide extended drug release. Wet granulation was employed to prepare the inner core of the tablets that were further layered with an immediate release drug layer in the perforated pan coater. The in-vitro and in-vivo performance of the developed formulation was compared with the marketed products Voltaren® SR 75 mg and Cataflam® 25 mg. The in-vitro drug release of the prepared formulation showed similarity (f2 = 66.19 to the marketed product. The pharmacokinetic study showed no significant difference (p > 0.05 in AUC0-24 and Cmax between the test and reference formulations. The AUC0-24 values were 105.36 ± 83.3 and 92.87 ± 55.53 μg h/ml whereas the Cmax values were 11.25 ± 6.87 and 12.97 ± 8.45 μg/ml, for the test and reference, respectively. The multi-layered tablets were proved to be bioequivalent with the commercially available tablets and were in agreement with the observed in-vitro drug release results. Stable physical characteristics and drug release profiles were observed in both long term and accelerated conditions stability studies.

  6. Terbutaline depot tablets in childhood asthma. A double-blind controlled study

    DEFF Research Database (Denmark)

    Foged, N; Høst, A; Ljungholm, K

    1985-01-01

    Thirty children 8-13 years old, with perennial asthma and with a reversibility of greater than or equal to 20% in lung function (FEV1) were given a sustained-release preparation of terbutaline sulphate 5 mg twice a day and ordinary tablets 2.5 mg three times a day; each treatment lasted 1 week...

  7. An oral modified-release nifedipine tablet (Adalat LA) and its appearance on double contrast barium enema

    International Nuclear Information System (INIS)

    Bleehen, Robert E.

    2000-01-01

    Adalat LA 30 mg and 60 mg tablets are widely prescribed oral modified release nifedipine preparations with a porous, non-digestible plastic tablet coating which is required in order to effect the osmotically driven slow release mechanism. These tablets may therefore be seen anywhere along the gastrointestinal tract and are passed apparently whole in the faeces. An example of the appearance within the rectum of Adalat LA 30 (Bayer) on double contrast barium enema is shown and the main features described. A review of the literature is given. Recognition of the appearances during the barium enema examination will prompt those performing the procedure to question the drug history where relevant and will reduce the incidence of false-positive reporting. Bleehen, R.E. (2000)

  8. Epitaxial growth of bcc-FexCo100-x thin films on MgO(1 1 0) single-crystal substrates

    International Nuclear Information System (INIS)

    Ohtake, Mitsuru; Nishiyama, Tsutomu; Shikada, Kouhei; Kirino, Fumiyoshi; Futamoto, Masaaki

    2010-01-01

    Fe x Co 100-x (x=100, 65, 50 at%) epitaxial thin films were prepared on MgO(1 1 0) single-crystal substrates heated at 300 deg. C by ultra-high vacuum molecular beam epitaxy. The film structure and the growth mechanism are discussed. FeCo(2 1 1) films with bcc structure grow epitaxially on MgO(1 1 0) substrates with two types of variants whose orientations are rotated around the film normal by 180 deg. each other for all compositions. Fe x Co 100-x film growth follows the Volmer Weber mode. X-ray diffraction analysis indicates the out-of-plane and the in-plane lattice spacings are in agreement with the values of respective bulk Fe x Co 100-x crystals with very small errors less than ±0.4%, suggesting the strains in the films are very small. High-resolution cross-sectional transmission electron microscopy shows that periodical misfit dislocations are preferentially introduced in the film at the Fe 50 Co 50 /MgO interface along the MgO[1 1-bar 0] direction. The presence of such periodical dislocations decreases the large lattice mismatch of about -17% existing at the FeCo/MgO interface along the MgO[1 1-bar 0] direction.

  9. Development and Optimum Composition of Locally Developed Potable Water Treatment Tablets

    Directory of Open Access Journals (Sweden)

    Josiah Oladele BABATOLA

    2009-07-01

    Full Text Available Current high level of energy cost and operational cost of membrane technologies and couple with difficulties in obtaining chemicals for potable water treatment give rooms for development of local substance and low cost adsorbents for water treatment. This paper presents a follow-up study on an earlier work in which some water treatment Tablets were produced and tested. The current work was directed at establishing the optimum composition of the tablets. Alum, calcium hypochlorite and lime were combined in proportion and made into pastes and tablets. Residual chlorine contents of the tablets were determined. The quality of stream water samples treated with the tablets was measured by chlorine content, pH and turbidity removal. It is concluded that the best composition is one part alum, two parts hypochlorite and three parts lime and this produced treated water pH of 7.8, chlorine residual of 5.0 mg/l and settled water turbidity 3.0 NTU. The product is aimed for use in rural communities to reduce rampaging death from water borne diseases.

  10. Evaluation of the Discrepancy between the European Pharmacopoeia Test and an Adopted United States Pharmacopoeia Test Regarding the Weight Uniformity of Scored Tablet Halves: Is Harmonization Required?

    Science.gov (United States)

    Zaid, Abdel Naser; Ghoush, Abeer Abu; Al-Ramahi, Rowa'; Are'r, Mohammed

    2012-01-01

    The aim of this study was to evaluate whether there exists any discrepancy between the European Pharmacopoeia (Ph. Eur.) and adopted United States Pharmacopeia (USP) tests concerning the weight uniformity measurements of tablet halves after splitting. The USP method does not contain provisions to evaluate split tablets, so here we adopt their whole tablet weight uniformity method. Twenty-nine different commercial scored tablets (local and imported) were divided. The split units were individually weighed and the relative standard deviation (RSD) for each product was calculated and then evaluated according to both the adopted USP and the Ph. Eur. tests of weight uniformity. Twenty out of the 29 products tested failed the USP test, while 14 of them failed the Ph. Eur. test. Nine products passed both the USP and Ph. Eur. tests. Six products passed the Ph. Eur. test but failed the USP test, with all of these products having an RSD greater than 6%. The correlation coefficient between the weight and content of split halves for three randomly selected products-corotenol 100 mg, corotenol 50 mg, and lorazepam 2.5 mg-was found to be 0.986, 0.998, and 0.72, respectively. A clear difference can be seen between outcomes obtained by the two compendial tablet splitting methods with regard to weight uniformity. Results from the USP test showed that tighter measures are needed to pass the test. Our results argue that the Ph. Eur. should revise the existing weight uniformity test on scored tablets to include the RSD parameter in it. The USP should include this adopted test as a specific test for scored tablet halves, not just whole tablets. Manufacturers in some cases will need to improve the quality of the produced scored tablets in order to pass the USP test, especially those with low therapeutic indices. Finally, harmonization between the pharmacopoeias regarding the weight uniformity testing of split tablets is warranted. The aim of this study was to evaluate whether there

  11. 75 FR 48352 - Determination That MOTRIN (Ibuprofen) Tablets and Four Other Drug Products Were Not Withdrawn...

    Science.gov (United States)

    2010-08-10

    ... DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and Drug Administration [Docket No. FDA-2010-N-0391] Determination That MOTRIN (Ibuprofen) Tablets and Four Other Drug Products Were Not Withdrawn From Sale for... Applicant NDA 17-463 MOTRIN (ibuprofen) Tablets, 300 milligrams (mg), McNeil Consumer Healthcare, 7050 Camp...

  12. An in vitro analysis of disintegration times of different formulations of olanzapine orodispersible tablet: a preliminary report.

    Science.gov (United States)

    Hobbs, David; Karagianis, Jamie; Treuer, Tamas; Raskin, Joel

    2013-12-01

    Orodispersible tablets (ODTs) are tablet or wafer forms of medication that disintegrate in the mouth, aided only by saliva. ODTs rely on different fast dissolve/disintegration manufacturing technologies. Disintegration time differences for several olanzapine ODT forms were investigated. Risperdal M-Tab(®) was included as a non-olanzapine ODT comparator. Eleven olanzapine ODT examples and orodispersible risperidone strengths were evaluated in vitro for formulation composition, manufacturing method, disintegration and dissolution characteristics, and formulation differences in comparison with freeze dried Zydis(®) ODT. Automated dissolution test equipment captured ODT dissolution rates by measuring real-time release of active ingredient. A high-speed video camera was used to capture tablet disintegration times in warm simulated saliva. The main outcome measure was the disintegration and dissolution characteristics of the ODT formulations. The ODT manufacturing method was associated with time to disintegrate; the fastest were freeze dried tablets, followed by soft compressed tablets and then hard/dense tablets. Olanzapine Zydis(®) was the only ODT that completely disintegrated in less than 4 s for all strengths (5, 10, 15, and 20 mg), followed by 5-mg Prolanz FAST(®) (12 s) and then risperidone ODT 4 mg (40 s). Reasons for slow dissolution of the olanzapine generics may include low product potency, excipient binding, excipient solubility, active ingredient particle size and incomplete disintegration. Differences in the formulation and manufacturing process of olanzapine ODTs appear to have a strong influence on the disintegration time of the active compound; differences that may potentially impact their use in clinical practice.

  13. Bioequivalence and food effect assessment for vildagliptin/metformin fixed-dose combination tablets relative to free combination of vildagliptin and metformin in Japanese healthy subjects.

    Science.gov (United States)

    Mita, Sachiko; Chitnis, Shripad D; Kulmatycki, Kenneth; Salunke, Atish; He, Yan-Ling; Zhou, Wei; Suzuki, Hikoe

    2016-04-01

    To assess the bioequivalence of vildagliptin/metformin fixeddose combination (FDC) tablets (50/250 mg and 50/500 mg) to free combinations of vildagliptin and metformin and the effect of food on the pharmacokinetics (PK) of vildagliptin and metformin following administration of 50/500 mg FDC tablets. Two openlabel, randomized, single-center, singledose, 2-period crossover studies were conducted in Japanese healthy male volunteers. Participants were administered vildagliptin/ metformin FDC tablets (study I: 50/250 mg, study II: 50/500 mg) or their free combinations under fasted condition. Food effect (standard Japanese breakfast: fat, 20 - 30% with ~ 600 kcal in total) was assessed during an additional period in study II (50/500 mg). PK parameters (AUC, C(max), t(max), t(1/2)) were calculated for vildagliptin and metformin. In both studies, vildagliptin/metformin FDC tablets were bioequivalent to their respective free combinations. Administration of FDC tablets after meals had no effect on vildagliptin PK parameters. The rate of absorption of metformin decreased when administered under fed condition, as reflected by a prolonged t(max) (3 hours in fasted state vs. 4 hours in fed state) and decrease in C(max) by 26%, however, the extent of absorption (AUC(last)) was similar to that in the fasted state. Vildagliptin/metformin FDC tablets were bioequivalent to their free combinations. Food decreased the C(max) of metformin by 26%, while AUC(last) was unchanged, consistent with previous reports. No food effect was observed on the C(max) or AUC(last) of vildagliptin. Thus, food had no clinically relevant effects on the PK of metformin or vildagliptin.

  14. Amorphous Formulation and in Vitro Performance Testing of Instantly Disintegrating Buccal Tablets for the Emergency Delivery of Naloxone.

    Science.gov (United States)

    Alqurshi, Abdulmalik; Kumar, Zahrae; McDonald, Rebecca; Strang, John; Buanz, Asma; Ahmed, Shagufta; Allen, Elizabeth; Cameron, Peter; Rickard, James A; Sandhu, Verity; Holt, Chris; Stansfield, Rebecca; Taylor, David; Forbes, Ben; Royall, Paul G

    2016-05-02

    The aim of this study was to develop a freeze-dried buccal tablet for the rapid delivery of naloxone in opioid overdose. The tablet composition was optimized to produce an amorphous matrix, which was confirmed by the absence of peaks associated with crystallinity observed by differential scanning calorimetry and powder X-ray diffraction. Tablets with high gelatin content lacked adequate porosity. Mannitol was added to the formulation to bridge and intercalate gelatin's tight polymer aggregates, however sodium bicarbonate was also required to prevent crystallization within the tablets. A linear reduction in mannitol's recrystallization enthalpy was observed with increasing sodium bicarbonate concentration (ΔrecryH = -20.3[NaHCO3] + 220.9; r(2) = 0.9, n = 18). The minimum sodium bicarbonate concentration for full inhibition of mannitol crystallization was 10.9% w/w. Freeze-dried tablets with lower amounts of sodium bicarbonate possessed a crystalline fraction that PXRD identified as mannitol hemihydrate from the unique peak at 9.7° 2θ. Mannitol's greater affinity for both ions and residual water rather than its affinity for self-association was the mechanism for the inhibition of crystallization observed here. The optimized tablet (composition mannitol 24% w/w (4.26 mg), gelatin 65% w/w (11.7 mg), sodium bicarbonate 11% w/w (1.98 mg), and naloxone 800 μg) formed predominantly amorphous tablets that disintegrated in less than 10 s. Optimized tablets were chemically and physically stable over 9 months storage at 25 °C. As speed of drug liberation is the critical performance attribute for a solid dosage form designed to deliver drug in an emergency, a novel imaging based in vitro disintegration assay for buccal tablets was developed. The assay was optimized with regard to conditions in the buccal cavity: i.e., temperature 33-37 °C, volume of medium (0.1-0.7 mL), and use of mucin-containing biorelevant medium. The disintegration assay was sensitive to temperature

  15. Determination of Venlafaxine and Modafinil in Individual Tablet ...

    African Journals Online (AJOL)

    Admin

    Methods: The compounds were analyzed on Waters symmetry C18 column (4.6 mm x ... 5µm) using a mobile phase consisting of a mixture of ammonium acetate buffer ... equivalent of 25 mg (1 tablet) of active ingredient .... phosphate buffers with organic modifiers, viz, .... liquid–liquid extraction and high-performance liquid.

  16. Estabilidad de las tabletas de clorodiazepóxido 10 mg

    Directory of Open Access Journals (Sweden)

    Vivian Tolosa Cubela

    1998-04-01

    Full Text Available Se estudió la estabilidad de las tabletas de clorodiazepóxido 10 mg que fueron elaboradas con un almidón modificado (GECLYN-ER2 de bajo costo en sustitución de la gelatina, aglutinante tradicional. Se emplearon como métodos analíticos para la cuantificación e identificación de clorodiazepóxido: cromatografía líquida de alta resolución, cromatografía en capa delgada y espectrofotometría. Los resultados obtenidos para las tabletas expuestas en condiciones variables de temperatura, humedad y de vida en estante confirman la factibilidad del empleo de este almidón, modificado para la fabricación de las tabletas de clorodiazepóxido 10 mg.The stability of chlordiazepoxide 10 mg tablets, which were made with low cost modified starch (GECLYN-ER2 to substitute gelatine, the traditional agglutinant, was studied. The following analytical methods were used for the quantification and identification of chlordiazipoxide: high pressure liquid chromatography thin layer chromatography, and spectrophotometry. The results attained for the tablets exposed to different conditions of temperature, humidity and shelf life confirmed the feasibility of this starch that was modified to make chlordiazepoxide 10 mg tablets.

  17. Model surface studies of metal oxides: Adsorption of water and methanol on ultrathin MgO films on Mo(100)

    International Nuclear Information System (INIS)

    Wu, M.; Estrada, C.A.; Corneille, J.S.; Goodman, D.W.

    1992-01-01

    Model surface studies of magnesium oxide have been carried out using surface sensitive techniques. Ultrathin MgO films have been synthesized under ultrahigh vacuum (UHV) conditions by thermally evaporating Mg onto Mo(100) in the presence of oxygen. Low-energy electron diffraction (LEED) studies indicate that the MgO films grow epitaxially with the (100) face of MgO oriented parallel to Mo(100). The MgO films, prepared under optimum synthesis conditions, have essentially one-to-one stoichiometry, are nearly free from pointlike surface defects, and have properties essentially identical to those of bulk, single-crystal MgO. Adsorption of water and methanol onto the MgO films has been studied using high-resolution electron energy-loss spectroscopy (HREELS) and temperature programmed desorption (TPD). In order to circumvent the difficulty associated with intense multiple surface optical phonon (Fuchs--Kliewer modes) losses, a new approach to acquisition of HREELS data has been demonstrated. This new approach enables the direct observation of weak loss features due to excitation of the adsorbates without serious interference from multiple phonon losses. Our HREELS studies show that water and methanol undergo heterolytic dissociation, leading to the formation of hydroxyl and methoxy species, respectively

  18. Why do adult women in Vietnam take iron tablets?

    Directory of Open Access Journals (Sweden)

    Zhao Yun

    2006-06-01

    Full Text Available Abstract Background Conducting iron supplementation programs has been a major strategy to reduce iron deficiency anemia in pregnancy. However, only a few countries have reported improvements in the anemia rate at a national level. The strategies used for control of nutrition problems need regular review to maintain and improve their effectiveness. The objective of this study was to analyze the factors in compliance with taking iron tablets, where daily doses of iron (60 mg and folic acid (400 μg were distributed in rural Vietnamese communes. Methods A cross sectional survey was conducted in Nghe An province, Vietnam in January, 2003. The study population was adult women aged less than 35 years who delivered babies between August 1st 2001 and December 1st 2002 (n = 205, of which 159 took part in the study. Data for the study were collected from a series of workshops with community leaders, focus group discussions with community members and a questionnaire survey. Results Improvements in the rate of anemia was not given a high priority as one of the commune's needs, but the participants still made efforts to continue taking iron tablets. Two major factors motivated the participants to continue taking iron tablets; their experience of fewer spells of dizziness (50%, and their concern for the health of their newborn baby (54%. When examining the reasons for taking iron tablets for at least 5–9 months, the most important factor was identified as 'a frequent supply of iron tablets' (OR = 11.93, 95% CI: 4.33–32.85. Conclusion The study found that multiple poor environmental risk factors discouraged women from taking iron tablets continuously. The availability (frequent supply of iron tablets was the most effective way to help adult women to continue taking iron tablets.

  19. The effect of a vaginal suppository formulation of dill (Anethum graveolens) in comparison to clotrimazole vaginal tablet on the treatment of vulvovaginal candidiasis.

    Science.gov (United States)

    Saghafi, Nafiseh; Karjalian, Maryam; Ghazanfarpour, Masumeh; Khorsand, Imaneh; Rakhshandeh, Hassan; Mirteimouri, Masumeh; Babakhanian, Masoudeh; Khadivzadeh, Talat; Najafzadeh, Mohammad Javad; Ghorbani, Ahmad; Pourali, Leila; Bahman, Sara

    2018-03-19

    The goal of this study was to compare the effect of Anethum graveolens (dill) vaginal suppositories and 100mg clotrimazole vaginal tablets on vulvovaginal Candidiasis. This study was a single centre, single-blind, randomised, placebo-controlled trial, in which 60 women with microbiology-confirmed vulvovaginal candidiasis were randomly assigned to dill and clotrimazole groups. At the end of the study, the estimated prevalence of leucorrhoea, burning, and itching was 23%, 23% and 20% in dill users, respectively. This figure was 20%, 10% and 16.7% for the clotrimazole group, respectively. The difference between the two groups was not significant. 13% of suppository patients, compared with 10% of clotrimazole-treatment patients, had a positive culture, which was not significant (p = .68). According to findings, 2% dill vaginal suppositories were as effective as clotrimazole vaginal tablets in reducing both clinical and microbiological symptoms of Candidiasis. Studies with larger sample sizes are required to confirm current findings. Impact statement What is already known on the subject? Based on results from in vivo and in vitro animal studies, dill (Anethum graveolens) has anti-candida activity. What do the results of this study add? It appears that 2% dill vaginal suppositories were as effective as 100mg clotrimazole vaginal tablets in reducing both the clinical and microbiological symptoms. What are the implications of these findings for clinical practice and further research? Obstetricians and gynaecologists can offer dill as a useful alternative to chemical drugs, especially in women who are often interested in herbal medicine, or in women who are resistant or are not allowed to use antifungal drugs.

  20. Comparison of desmopressin (DDAVP tablet and intranasal spray in the treatment of central diabetes insipidus

    Directory of Open Access Journals (Sweden)

    "Bagher Larijani

    2005-07-01

    Full Text Available Desmoperssin is the drug of choice for treatment of central diabetes insipidus and most commonly it is used as intranasal spray. In this study, efficacy and side effects of oral desmopressin was compared with the intranasal spray. This study was before -after clinical trial on 14 outpatients (9 F, 5 M, age 14 -50 Y with central diabetes insipidus who had been treated with intranasal spray of desmopressin previously. Weight, pulse rate and blood pressure (sitting -standing, biochemical profile, serum electrolytes, 24h urine volume, specific gravity of urine and LFT was measured before and after 1 month study. Starting dose for each patient was one oral tablet of DDAVP (0.1 mg per 8 hours. Paired Samples T-Test was used for data analysis. No clinically significant changes were found as regard to weight, pulse rate, blood pressure, blood chemistry, electrolyte and urinalysis. Single reported adverse effect was headache (43% in tablet group and dyspnea (7% in spray group. Both dosage forms were able to control diurnal polyuria and nocturnal polyuria. The antidiuretic dose - equivalence ratio for intranasal to oral desmopressin was 1: 18. Spray was superior in terms of rapid onset of action and duration of antidiuretic action in 100% and 78% of cases (not significant, respectively. Tablets were more available and much more easily consumed as reported by patients, in 86% (P=0.0006. Treatment with tablets offers a good alternative to the intranasal route, especially in patients with chronic rhinitis or common cold and similar conditions.

  1. Efficacy of Cladribine Tablets in high disease activity subgroups of patients with relapsing multiple sclerosis: A post hoc analysis of the CLARITY study.

    Science.gov (United States)

    Giovannoni, Gavin; Soelberg Sorensen, Per; Cook, Stuart; Rammohan, Kottil W; Rieckmann, Peter; Comi, Giancarlo; Dangond, Fernando; Hicking, Christine; Vermersch, Patrick

    2018-04-01

    In the CLARITY (CLAdRIbine Tablets treating multiple sclerosis orallY) study, Cladribine Tablets significantly improved clinical and magnetic resonance imaging (MRI) outcomes (vs placebo) in patients with relapsing-remitting multiple sclerosis. Describe two clinically relevant definitions for patients with high disease activity (HDA) at baseline of the CLARITY study (utility verified in patients receiving placebo) and assess the treatment effects of Cladribine Tablets 3.5 mg/kg compared with the overall study population. Outcomes of patients randomised to Cladribine Tablets 3.5 mg/kg or placebo were analysed for subgroups using HDA definitions based on high relapse activity (HRA; patients with ⩾2 relapses during the year prior to study entry, whether on DMD treatment or not) or HRA plus disease activity on treatment (HRA + DAT; patients with ⩾2 relapses during the year prior to study entry, whether on DMD treatment or not, PLUS patients with ⩾1 relapse during the year prior to study entry while on therapy with other DMDs and ⩾1 T1 Gd+ or ⩾9 T2 lesions). In the overall population, Cladribine Tablets 3.5 mg/kg reduced the risk of 6-month-confirmed Expanded Disability Status Scale (EDSS) worsening by 47% vs placebo. A risk reduction of 82% vs placebo was seen in both the HRA and HRA + DAT subgroups (vs 19% for non-HRA and 18% for non-HRA + DAT), indicating greater responsiveness to Cladribine Tablets 3.5 mg/kg in patients with HDA. There were consistent results for other efficacy endpoints. The safety profile in HDA patients was consistent with the overall CLARITY population. Patients with HDA showed clinical and MRI responses to Cladribine Tablets 3.5 mg/kg that were generally better than, or at least comparable with, the outcomes seen in the overall CLARITY population.

  2. Determinação de 3,4-metilenodioximetanfetamina (MDMA em comprimidos de Ecstasy por cromatografia líquida de alta eficiência com detecção por fluorescência (CLAE-DF Determination of 3,4-methylenedioxymethamphetamine (MDMA in Ecstasy tablets by high performance liquid chromatography with fluorescence detection (HPLC-FD

    Directory of Open Access Journals (Sweden)

    José Luiz da Costa

    2009-01-01

    Full Text Available This paper describes the development and validation of simple and selective analytical method for determination of 3.4-methylenedioxymethamphetamine (MDMA in Ecstasy tablets, using high performance liquid chromatography with fluorescence detection. Analysis was performed in a reversed phase column (LiChrospher 100 C18, 150 x 4.6 mm, 5 µm, isocratic elution with phosphate buffer 25 mmol/L pH 3.0 and acetonitrile (95:5, v/v. The method presents adequate linearity, selectivity, precision and accuracy. MDMA concentration in analyzed tablets showed a remarkable variability (from 8.5 to 59.5 mg/tablet although the tablet weights were uniform, indicating poor manufacturing control thus imposing additional health risks to the users.

  3. Formulation of Dipyridamole Sustained Release Tablet Using Floating System

    Directory of Open Access Journals (Sweden)

    Lenny Mauilida Valentina

    2011-06-01

    Full Text Available Dipyridamole is a drug for prevention of postoperative thromboembolic complication of heart valve replacement and long term therapy of angina pectoris will be well absorbed in stomach. To maintain therapeutic plasma concentration in long time and to increase bioavalaibility is needed a sustained release dosage form having the long residence time in the stomach. The objective of this research was to make floating sustained release tablet of dipyridamole conforming to the requirement that was set up by dipyridamol therapeutic concentration. Tablets were made by wet granulation method using aquadest as a liquid binder, HPMC K4M, Ac-di-sol, Avicel PH 102, talk, and Mg stearat. Dissolution assay was carried out using type 2 release tester at rotation speed of 50 rpm in medium 900 mL HCl 0.1 N at 37 ± 0.5 °C for 8 hours. The formulation containing of 50 mg dipirydamole, HPMC K4M (30%, Ac-di-sol (20%, Avicel PH 102 (37%, talk (2%, and Mg stearat (1% released 59.61 ± 6.73% and 89.34 ± 5.87% of dipyridamole respectively after 4 and 8 hours that conformed to the requirement.

  4. Perpendicular magnetic tunnel junction with tunneling magnetoresistance ratio of 64% using MgO (100) barrier layer prepared at room temperature

    International Nuclear Information System (INIS)

    Ohmori, Hideto; Hatori, Tomoya; Nakagawa, Shigeki

    2008-01-01

    MgO (100) textured films can be prepared by reactive facing targets sputtering at room temperature without postdeposition annealing process when they were deposited on (100) oriented Fe buffer layers. This method allows fabrication of perpendicular magnetic tunnel junction (p-MTJ) with MgO (100) tunneling barrier layer and rare-earth transition metal (RE-TM) alloy thin films as perpendicularly magnetized free and pinned layers. The 3-nm-thick MgO tunneling barrier layer in p-MTJ multilayer prepared on glass substrate revealed (100) crystalline orientation. Extraordinary Hall effect measurement clarified that the perpendicular magnetic components of 3-nm-thick Fe buffer layers on the two ends of MgO tunneling barrier layer were increased by exchange coupling with RE-TM alloy layers. The RA of 35 kΩ μm 2 and tunneling magnetoresistance ratio of 64% was observed in the multilayered p-MTJ element by current-in-plane-tunneling

  5. Solubility and release of fenbufen intercalated in Mg, Al and Mg, Al, Fe layered double hydroxides (LDH): The effect of Eudragit S 100 covering

    International Nuclear Information System (INIS)

    Arco, M. del; Fernandez, A.; Martin, C.; Rives, V.

    2010-01-01

    Following different preparation routes, fenbufen has been intercalated in the interlayer space of layered double hydroxides with Mg 2+ and Al 3+ or Mg 2+ , Al 3+ and Fe 3+ in the layers. Well crystallized samples were obtained in most of the cases (intercalation was not observed by reconstruction of the MgAlFe matrix), with layer heights ranging between 16.1 and 18.8 A. The presence of the LDH increases the solubility of fenbufen, especially when used as a matrix. The dissolution rate of the drug decreases when the drug is intercalated, and is even lower in those systems containing iron; release takes place through ionic exchange with phosphate anions from the solution. Preparation of microspheres with Eudragit S 100 leads to solids with an homogeneous, smooth surface with efficient covering of the LDH surface, as drug release was not observed at pH lower than 7. - Graphical abstract: LDHs containing Mg, Al, Fe increase fenbufen solubility, release takes place through ionic exchange with phosphate anions from the medium. Spherical solids with homogeneous, smooth surface are formed when using Eudragit S 100, efficiently covering the LDH surface. Display Omitted

  6. Weight loss during therapy with olanzapine orally disintegrating tablets: two case reports.

    Science.gov (United States)

    Kozumplik, Oliver; Uzun, Suzana; Jakovljević, Miro

    2009-03-01

    The aim of this article is to report weight loss in patients with schizophrenia after switching from olanzapine standard oral tablet (SOT) to olanzapine orally disintegrating tablets (ODT). In the first case report, the patient was switched to olanzapine ODT in daily dosage of 20 mg, while in the second case report, the patient was switched to olanzapine ODT in daily dosage of 15 mg, and weight loss was similar (14 kg vs. 15 kg). Switching patients from olanzapine SOT to olanzapine ODT treatment resulted in significant weight loss that was maintained during 12 months in both case reports. Further controlled clinical investigations are necessary to evaluate change in weight during treatment with olanzapine ODT, and to improve our understanding of this change.

  7. A Comparative Study of the Pharmacokinetics of Conventional and ...

    African Journals Online (AJOL)

    ... a commercial brand of aceclofenac immediate release tablet (Zerodol® 100 mg). Methods: Each of two groups of twelve fasting volunteers received either the reference standard (Zerodol 100 mg tablets) or the test formulation (200 mg aceclofenac) orally once, using a cross-over design with a one week wash-out period.

  8. Rapid voltammetric monitoring of melatonin in the presence of tablet excipients

    International Nuclear Information System (INIS)

    Ball, Andrew T.; Patel, Bhavik Anil

    2012-01-01

    Melatonin is an important neurohormonal chemical that is responsible for regulating sleep. Melatonin dietary supplements are available and utilised to counteract the effects of jet-lag or to aid sleep. Voltammetric detection with a boron-doped diamond electrode was utilised for the rapid monitoring of individual melatonin tablets. Melatonin was oxidised at a potential of +0.8 V vs. Ag|AgCl. Voltammetric measurements were carried out without the need of excessive sample preparation steps such as filtration. However dicalcium phosphate and carboxymethyl cellulose were shown to alter the electrochemical response. Calibration responses were linear over a concentration of 2–4 mg/25 ml of melatonin and a limit of detection of 0.06 mg/25 ml was observed. Volammetric recordings were only stable for one measurement, but the electrode surface could be replenished following a single wipe of an ethanol soaked lens cloth. This new assay was capable of analysing individual melatonin tablets within a total analysis time of 2.5 min. Overall this approach provides the basis for rapid electrochemical monitoring of pharmaceutical and dietary tablets without the need for extensive sample preparation.

  9. Quality control and stability study of 100 mg/ml paracetamol oral drops

    International Nuclear Information System (INIS)

    Garcia Penna, Caridad M.; Montes de Oca Porto, Yanet; Salomon Izquierdo, Suslebys

    2013-01-01

    Paracetamol is an effective analgesic and antipyretic drug of the non-steroidal anti-inflammatory drug group. Paracetamol oral drops are indicated for use in infant population aged up to 5 years to relieve fever, headache, toothache and symptomatic relief of common cold. To validate two analytical methods for the quality control and the stability study and to study the stability of 100 mg/ml Paracetamol oral drops made in Cuba

  10. A single dose, randomized, open-label, cross-over bioequivalence study of sildenafil citrate tablets in healthy Chinese volunteers
.

    Science.gov (United States)

    Li, Dai; Wang, Yu-Lu; Xu, Su-Mei; Li, Dan; Li, Xiao-Min; Pan, Jing; Xu, Ping-Sheng

    2017-02-01

    The present study was designed to evaluate the bioequivalence of a newly developed sildenafil citrate tablet 50 mg (Jinge®, Test) and a marketed counterpart (Viagra®, 100 mg, Reference) in healthy adult male Chinese volunteers. This single-dose, randomized, open-label, four-period, and two-treatment self-crossover study included two parts: fasting and postprandial studies. In each part of the study, the subjects were randomly assigned to receive test or reference products (100 mg sildenafil) in a 1 : 1 ratio, and then received the alternative products, following a 1-week washout period. Plasma sildenafil concentrations were analyzed by liquid chromatography-tandem mass spectrometry. Tolerability was assessed during the entire study period. 32 healthy volunteers (aged 19 - 30) were enrolled in the study; 31 volunteers completed the fasting study, while 32 volunteers completed the postprandial study. The test formulation was bioequivalent to the marketed formulation as the 90% CIs for the ratio of geometric means of Cmax (fasting: 98.79 - 119.61%; fed: 94.47 - 119.65%), AUClast (fasting: 98.70 - 109.71%; fed: 96.39 - 112.89%), and AUC∞ (fasting: 98.45 - 108.87%; fed: 96.36 - 112.74%) were within equivalence limits (80 - 125%) under both fasting and postprandial conditions. When sildenafil was given with high-fat meals, mean Cmax was reduced by 23%, and median tmax ranged from 0.75 to 1.50 hours (p ≤ 0.05). However, both AUClast and AUC∞ were comparable between fasting and postprandial conditions. No serious adverse events were found among the subjects. This study confirmed that test and reference sildenafil citrate tablets were bioequivalent under fasting and postprandial conditions.
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  11. Erosive potential of vitamin and vitamin+mineral effervescent tablets.

    Science.gov (United States)

    Wegehaupt, Florian J; Lunghi, Nancy; Hogger, Vanessa M G; Attin, Thomas

    2016-01-01

    The extrinsic sources for erosion-causing acids are primarily acidic beverages and foodstuffs. Effervescent tablets also contain organic acids (e.g. citric, tartaric, malic) in order to form carbon dioxide by contact with water – with the help of the carbonate salts of the tablets. To adequately inform patients about the possible erosive potential of effervescent tablets, this study was undertaken in order to investigate the erosive potential of effervescent tablets (ET), containing either a combination of vitamins and minerals or vitamins only, commercially available in Switzerland. One hundred and ninety-two bovine enamel samples were prepared and allocated to 16 groups (A–H and 1–8; n = 12/group). Samples were eroded (120 s/erosive cycle) in freshly prepared solutions (200 ml/12 samples) comprised of tap water and a supplement as follows: none (control groups, A and 1); vitamin+mineral ET: Qualite and Prix (B), Optisana (C), Well and Active (D), Actilife All in One (E), Berocca (F), Isostar (G) and Qualite and Prix Mg + Vit C (H); vitamin ET: Actilife-Multivitamin (2), Sunlife Vitamin C (3), Optisana Vitamin C (4), Optisana Multivitamin (5), Well and Active Multivitamin (6), Kneipp Vitamin C+Zink (7) and Sunlife Multivitamin (8). Enamel loss was measured using profilometry after 10 and 20 erosive cycles. For the vitamin+mineral ET, no loss was observed in groups B–E. Significantly highest enamel loss (mean ± SD) after 20 cycles was observed for Isostar (5.26 ± 0.76 µm) and Qualite and Prix Mg + Vit C (5.12 ± 0.67 µm). All vitamine ET showed erosive enamel loss. Significantly highest loss was observed for Sunlife Multivitamin (8.45 ± 1.08 µm), while the lowest loss was observed for Actilife-Multivitamin (5.61 ± 1.08 µm) after 20 cycles. Some of the tested effervescent tablets showed a considerable erosive potential and patients should be informed accordingly.

  12. Capmul MCM/Solutol HS15-Based Microemulsion for Enhanced Oral Bioavailability of Rebamipide.

    Science.gov (United States)

    Kim, Ki Taek; Lee, Jae-Young; Park, Ju-Hwan; Cho, Hyun-Jong; Yoon, In-Soo; Kim, Dae-Duk

    2017-04-01

    Rebamipide (RBP) is a potent anti-ulcer and anti-oxidative agent, which is a BCS class IV drug with a low oral bioavailability of less than 10%. Thus, the systemic absorption of RBP into the blood circulation is an essential prerequisite for exerting its pharmacological activities after oral dosing. Herein, we report on microemulsion (ME) systems for the enhancement of oral RBP bioavailability. In this study, MEs consisting of Capmul MCM (oil), Solutol HS15 (surfactant), and ethanol (co-surfactant) were prepared by the construction of pseudo-ternary phase diagram. The RBP-loaded MEs had spherical nano-sized droplets with narrow size distribution and neutral zeta potential. Moreover, the prepared MEs significantly enhanced the dissolution and oral bioavailability of RBP with no discernible intestinal toxicity. These results suggest that the present ME system could be further developed as an alternative oral formulation for RBP.

  13. Esophageal transit and in vivo disintegration of branded risedronate sodium tablets and two generic formulations of alendronic acid tablets: a single-center, single-blind, six-period crossover study in healthy female subjects.

    Science.gov (United States)

    Perkins, Alan C; Blackshaw, P Elaine; Hay, Peter D; Lawes, Simon C; Atherton, Clare T; Dansereau, Richard J; Wagner, Leigh K; Schnell, Dan J; Spiller, Robin C

    2008-05-01

    Delayed esophageal transit or disintegration of oral bisphosphonate tablets before they enter the stomach may be of concern with respect to iatrogenic complications among patients receiving longterm treatment. Different formulations of generic bisphosphonate tablets meeting regulatory requirements may have substantial differences in pharmaceutical attributes from the branded product that may result in different characteristics during esophageal transit. The primary objective of this study was to evaluate and compare esophageal transit times and in vivo disintegration of 3 bisphosphonate formulations, one branded and the others generic, that are commercially available in Canada and the United Kingdom. This was a single-center, randomized, singleblind, 6-period crossover study in healthy postmenopausal women aged >50 years. Each subject received a single oral dose of a branded risedronate sodium 35-mg tablet and 2 generic formulations of alendronic acid 70-mg tablets (Novopharm Limited, Toronto, Canada, and Teva UK Limited, Morley, United Kingdom) in both the erect and semisupine (45 degrees ) positions. Although the products are labeled to be taken in the erect position, the semisupine position was included to simulate dosing in bedridden patients. Subjects took tablets with 30 mL of water in the morning after an overnight fast. The tablets were radiolabeled with technetium-99m ion-exchange resins to enable visualization and measurement of esophageal transit time and disintegration using a gamma camera. Dynamic scintigraphic images were obtained for a total of 10 minutes: 2 images per second for the first 30 seconds and 1 image every 15 seconds for 9.5 minutes. This was a mechanistic study and tolerability was not assessed. The study was conducted in 20 healthy white female subjects with a mean age of 62 years (range, 51-77 years). The effect of body position was statistically significant (P = 0.043), with the estimated hazard ratio (HR) of 0.74 indicating longer

  14. UJI DISOLUSI DAN PENETAPAN KADAR TABLET LORATADIN INOVATOR DAN GENERIK BERMEREK

    Directory of Open Access Journals (Sweden)

    Mariana Raini

    2012-09-01

    Full Text Available Antihistamines Loratadin available in tablet form, as loratadin tablets innovator, branded generic preparations. Socializing generic drugs need information about quality of these drugs, to ensure that the quality of generic drugs not lower or similar to its innovator drugs. The impact of economic crisis caused the price of very expensive drugs. The information quality of generic drugs is expected to increase the use of generic drugs by health practitioners and public. It is necessary for the laboratory data that are qualityparameters, such as dissolution profiles, dissolution testing and determinationof drug dosage levels. Dissolution test method anddetermination of levelsconducted in accordanceto the requirements of the USP (United State of Pharmacopeia. Loratadin dissolution test resultsof tablets A, B and Cin accordancewith the requirements of the USP. Loratadin contentin tablet Ais 103, 73%, B=99,62% and C=100,21%. Loratadin levels in all of these tablets meet the requirements of the USP.   Key words: innovator,branded generic drug, dissolution, content

  15. [Troubleshooting of bioinequivalence of compound valsartan tablets].

    Science.gov (United States)

    Shao, Da; Zhang, Yi-Fan; Zhan, Yan; Chen, Xiao-Yan; Zhong, Da-Fang

    2014-04-01

    The study aims to evaluate the bioequivalence of valsartan hydrochlorothiazide tablets, and to investigate the potential cause of bioinequivalence. This was a single-center study with an open, randomized double-way crossover design. Test and reference preparations containing 160 mg of valsartan and 25 mg of hydrochlorothiazide were given to 36 healthy male volunteers. Plasma concentrations of valsartan and hydrochlorothiazide were determined simultaneously by LC-MS/MS. The pharmacokinetic parameters and relative bioavailability were calculated, while the bioequivalence between test and reference preparations were evaluated. The dissolution profiles of test and reference preparations in four different mediums were determined via dissolution test and HPLC. The similarity was investigated according to the similarity factors (f2). The F(o-t) and F(0-infinity) were (139.4 +/- 65.2)% and (137.5 +/- 61.2)% for valsartan of test preparations. It led to get the conclusion that test and reference preparations were not bioequivalent for valsartan. A significant difference was observed between test and reference tablets in the valsartan dissolution test of pH 1.2 hydrochloric acid solution. The key factor of the bioinequivalence might be that dissolution of valsartan in acid medium has marked difference between two preparations.

  16. Angular circulation speed of tablets in a vibratory tablet coating pan.

    Science.gov (United States)

    Kumar, Rahul; Wassgren, Carl

    2013-03-01

    In this work, a single tablet model and a discrete element method (DEM) computer simulation are developed to obtain the angular circulation speed of tablets in a vibratory tablet coating pan for range of vibration frequencies and amplitudes. The models identify three important dimensionless parameters that influence the speed of the tablets: the dimensionless amplitude ratio (a/R), the Froude number (aω2/g), and the tablet-wall friction coefficient, where a is the peak vibration amplitude at the drum center, ω is the vibration angular frequency, R is the drum radius, and g is the acceleration due to gravity. The models predict that the angular circulation speed of tablets increases with an increase in each of these parameters. The rate of increase in the angular circulation speed is observed to decrease for larger values of a/R. The angular circulation speed reaches an asymptote beyond a tablet-wall friction coefficient value of about 0.4. Furthermore, it is found that the Froude number should be greater than one for the tablets to start circulating. The angular circulation speed increases as Froude number increases but then does not change significantly at larger values of the Froude number. Period doubling, where the motion of the bed is repeated every two cycles, occurs at a Froude number larger than five. The single tablet model, although much simpler than the DEM model, is able to predict the maximum circulation speed (the limiting case for a large value of tablet-wall friction coefficient) as well as the transition to period doubling.

  17. Evaluation of disintegration properties of orally rapidly disintegrating tablets using a novel disintegration tester.

    Science.gov (United States)

    Kondo, Keita; Niwa, Toshiyuki; Danjo, Kazumi

    2012-01-01

    This report describes a new disintegration tester that can determine not only the disintegration time of orally rapidly disintegrating tablets (ODT), but also the disintegration behavior and mechanism. Using the tester, the disintegration properties of the tablets prepared in a previous study were examined. The purpose of this study is to confirm the utility of the tester as an instrument for evaluating the disintegration properties of ODT and determine relations among time, behavior and mechanism of the disintegration. Results demonstrated that in vitro disintegration time in the tester is similar to that in the commercial disintegration tester for ODT and is highly correlated with oral disintegration time. Observations of disintegration process revealed that a difference in disintegration behavior between tablets compressed at 50-75 MPa and 100 MPa; the disintegration behavior of the tablets were designated immediate disintegrating type and gradual disintegrating type, respectively. The dynamic swelling profile and water absorption profile indicated that the disintegration mechanism of the tablets involved wicking action induced by swelling of the disintegrant; the disintegration time was closely related to the initial rates of swelling and water absorption. Furthermore, the mechanism of water absorption of tablets compressed at 50-75 MPa and 100 MPa shows anomalous diffusion and case-II transport, respectively. The shift in this mechanism is consistent with differences in disintegration time and behavior between the tablets. These findings suggest that information on disintegration properties obtained by our tester is useful for understanding of disintegration phenomena of ODT.

  18. Performance of tablet disintegrants: impact of storage conditions and relative tablet density.

    Science.gov (United States)

    Quodbach, Julian; Kleinebudde, Peter

    2015-01-01

    Tablet disintegration can be influenced by several parameters, such as storage conditions, type and amount of disintegrant, and relative tablet density. Even though these parameters have been mentioned in the literature, the understanding of the disintegration process is limited. In this study, water uptake and force development of disintegrating tablets are analyzed, as they reveal underlying processes and interactions. Measurements were performed on dibasic calcium phosphate tablets containing seven different disintegrants stored at different relative humidities (5-97%), and on tablets containing disintegrants with different mechanisms of action (swelling and shape recovery), compressed to different relative densities. Disintegration times of tablets containing sodium starch glycolate are affected most by storage conditions, which is displayed in decreased water uptake and force development kinetics. Disintegration times of tablets with a swelling disintegrant are only marginally affected by relative tablet density, whereas the shape recovery disintegrant requires high relative densities for quick disintegration. The influence of relative tablet density on the kinetics of water uptake and force development greatly depends on the mechanism of action. Acquired data allows a detailed analysis of the influence of storage conditions and mechanisms of action on disintegration behavior.

  19. Tabletted guar gum microspheres of piroxicam for targeted adjuvant therapy for colonic adenocarcinomas.

    Science.gov (United States)

    Vats, Anima; Pathak, Kamla

    2012-11-01

    In recent years, nonsteroidal anti-inflammatory drugs have been found to be cogent as an adjuvant therapeutic agent in mitigating colorectal cancer. Thus, this present investigation was aimed to formulate an oral, targeted tablet of piroxicam microspheres for sustained and targeted adjuvant therapy for colonic adenocarcinomas. Crosslinked guar gum microspheres of piroxicam were directly compressed into matrix tablet and coated with Eudragit S100. The optimized tablet that displayed 0% release in simulated gastric fluid, 15% in simulated intestinal fluid and 97.1% in simulated colonic fluid underwent roentgenographic study in rabbits to check its safe transit to the colon. x-ray images revealed intactness of the tablet until it reached the colon where the tablet matrix eroded. The designed, conceptual formulation emerged as potential carrier for targeted adjuvant therapy of piroxicam.

  20. Assessment of pharmaceutical quality of furosemide tablets from multinational markets.

    Science.gov (United States)

    Qureshi, S A; McGilveray, I J

    1998-11-01

    This report describes results of a collaborative study in which samples of the 40-mg strength of furosemide tablets were evaluated following a common protocol based on British (BP), European (Ph. Eur.), and US Pharmacopoeial (USP) specifications. Several tests, including identification, uniformity of mass, and dissolution, were performed. In total, excluding Lasix lots, results for 162 lots obtained from 115 manufacturers or suppliers were submitted. Also, 23 laboratories identified and submitted data for 34 lots of Lasix products available in their countries. There were no reported abnormalities in the physical test requirements of the products analyzed. The summaries (n, mean, and 95% CI) of the assay results for the "standard sample" (a common sample), Lasix lots from participating countries, and for all other furosemide products, respectively, are as follows: 30, 99.8%, 96-104; 33, 100.0%, 94-106; and 162, 99.6, 94-105. About half (approximately 62%) of the reported uniformity of mass results based on tablet weights were in the range 150-175 mg/tablet. However, there appears to be notable variability in tablet weights that would result in significant differences in the ratios (0.14 to 0.40) of active ingredient to excipient. The reported disintegration times ranged from 0 (instantaneous) to 18 min, with most less than 1 min. The drug dissolution testing was conducted with phosphate buffer at pH 5.8 (USP recommended). Another test was conducted with acetate buffer at pH 4.6 (noncompendial). There appears to be remarkable similarity in overall percentage of drug release from the three types of products (standard sample, Lasix lots, and other products). Although apparently there is a very wide spread in dissolution characteristics of the products tested, the analyses of variance did not detect differences among the products tested and, to this extent, would not indicate differences in bioavailability characteristics for most of these products. It is observed that

  1. Aspirin administered to women at 100 mg every other day produces less platelet inhibition than aspirin administered at 81 mg per day: implications for interpreting the women's health study.

    Science.gov (United States)

    Swaim, Lisa; Hillman, Robert S

    2009-07-01

    We aimed to determine the relative level of platelet inhibition achieved with low-dose aspirin (81 mg daily) compared with a very low-dose (100 mg every other day). The Womens Health Study (WHS) found that a dose of 100 mg every other day of aspirin provided protection against stroke as primary prophylaxis, but not myocardial infarction. In the United States, the most commonly prescribed dose of aspirin for primary prophylaxis is 81 mg per day. As a result, it is important to know whether these doses are equivalent before extrapolating the results of the WHS to women in the U.S. To achieve this goal, we have studied the effects of these two dosing regimens on platelet function in healthy women meeting the WHS inclusion criteria using a randomized design. We enrolled 49 healthy female volunteers and used a sequential, crossover design to compare the two regimens. The participants received a 17-day course of each aspirin-dosing regimen separated by a 7-day washout period. The degree of platelet inhibition was measured on days 14-17 of each dosing regimen using a point-of-care platelet function assay utilizing arachidonic acid to activate platelets (VerifyNow-Aspirin). Participants platelet response, expressed as Aspirin Response Unit (ARU) attained a significantly greater level of platelet inhibition on days 14-17 while taking aspirin 81 mg daily compared to aspirin 100 mg every other day (31.3% vs. 12.7%, P or=550 ARU, a value correlated with clinical outcomes in several studies, with the 100 mg every other day regimen (72.0% vs. 6.4% with 81 mg daily, P day regimen also resulted in more day-to-day variability in platelet function (P = 0.0002). We found significantly less inhibition of platelet function with the dose used in the WHS than the usual U.S. dose. We observed that the degree of platelet inhibition was significantly less with aspirin 100 mg every other day compared with aspirin 81 mg daily, suggesting that results of the Women's Health Study may have

  2. Preparation and evaluation of diclofenac sodium orally disintegrating tablets

    Directory of Open Access Journals (Sweden)

    Iancu Valeriu

    2016-06-01

    Full Text Available Orally disintegrating tablets (ODTs are dosage forms which disintegrate in mouth within seconds without need of water. This type of quality in dosage form can be attained by addition of different varieties of excipients. Pharmaburst™ 500 is a co-processed excipient system which allows rapid disintegration and low adhesion to punches. The aim of the present study was to develop and evaluate 25 mg diclofenac sodium ODTs (orodispersible tablets batches by direct compression method at different compression forces 10 kN (F1 and 20 kN (F2 and directly compressible excipients used in different ratio (Avicel PH 102, magnesium stearate and coprocessed excipient Pharmaburst™ 500, 70% and 80% w/w. The obtained batches were analyzed for appearance, tablet thickness, uniformity of weight, hardness, friability, disintegration time, and non-compendial methods (wetting time. Co-processed Pharmaburst™ 500 excipient 70% used for sodium diclofenac ODT obtaining determined good results for quality control tests evaluation.

  3. PENYULUHAN DAN PEMBERIAN TABLET ASAM FOLAT BAGI IBU-IBU USIA REPRODUKTIF DI DESA ABIANSEMAL, BADUNG

    Directory of Open Access Journals (Sweden)

    DESAK MADE WIHANDANI

    2012-09-01

    Full Text Available ABSTRACT Folat deficiency that happened during early period of pregnancy, has known as one of the factor that cause fetal abnormalities. That why it is important for pregnant women to get information about the rule of folic acid in preventing fetal abnormalities. From 93 women within reproductive age, 6 of them were pregnant. Pregnant women were given 30 tablets of 0,4 mg folic acid taken once a day, and the less 87 women who were not in pregnant state received 10 tablets of folic acid to be taken once a day. PENYULUHAN DAN PEMBERIAN TABLET ASAM FOLAT BAGI IBU-IBU USIA REPRODUKTIF DI DESA ABIANSEMAL, BADUNG DESAK MADE WIHANDANI, NYOMAN AGUS BAGIADA DAN WAYAN SURUDARMA Bagian Biokimia Fakultas Kedokteran Universitas Udayana ABSTRACT Folat deficiency that happened during early period of pregnancy, has known as one of the factor that cause fetal abnormalities. That why it is important for pregnant women to get information about the rule of folic acid in preventing fetal abnormalities. From 93 women within reproductive age, 6 of them were pregnant. Pregnant women were given 30 tablets of 0,4 mg folic acid taken once a day, and the less 87 women who were not in pregnant state received 10 tablets of folic acid to be taken once a day.

  4. Seaweed tablet: a natural source of iodine

    International Nuclear Information System (INIS)

    Briones, Annabelle V.; Ambal, Wilhelmina O.; Monroyo, Evangelina C.; Bonifacio, Teresita S.; Sison, Fe M.

    1997-01-01

    Species of seaweeds namely: Halymenia durvillaei, Laurencia flexilis and Sargassum gigantifolium were processed into dried form and formulated as tablet. Prior to tablet formulation, the seaweeds were assayed for iodine and trace elements. The seaweeds that exhibited significance values of iodine and trace elements were further analyzed for the presence of heavy metals followed by acute oral toxicity test (LD 50 ). Among the seaweeds evaluated, H. durvilaei was found to contain high level of iodine (0.255% w/w) and magnesium (1.65% w/w) with sufficient amount of zinc (25.69 ppm) and phosporous (11.68 ppm). Analysis of heavy metals showed minute amount of mercury (0.0055 ppm), cadmium (0.67 ppm) and lead (1.80 ppm). The median lethal dose (LD 50 ) of H. durvillaei administered orally in Swiss male mice is 119.1489 ± 4.9873 g/kg. Tablet formulation was based on the U.S. recommended daily allowance of 0.15 mg. of iodine per adult and children. The final product was comparable to imported Kelp pills (available in the local market) in terms of physical properties and iodine content. (Author)

  5. Investigation of LiF, Mg and Ti (TLD-100) Reproducibility.

    Science.gov (United States)

    Sadeghi, M; Sina, S; Faghihi, R

    2015-12-01

    LiF, Mg and Ti cubical TLD chips (known as TLD-100) are widely used for dosimetry purposes. The repeatability of TL dosimetry is investigated by exposing them to doses of (81, 162 and 40.5 mGy) with 662keV photons of Cs-137. A group of 40 cubical TLD chips was randomly selected from a batch and the values of Element Correction Coefficient (ECC) were obtained 4 times by irradiating them to doses of 81 mGy (two times), 162mGy and 40.5mGy. Results of this study indicate that the average reproducibility of ECC calculation for 40 TLDs is 1.5%, while these values for all chips do not exceed 5%.

  6. A comparison of oral misoprostol and vaginal prostaglandin e2 tablets for induction of labour at term

    International Nuclear Information System (INIS)

    Munzar, Z.

    2015-01-01

    To compare the efficacy and safety of oral misoprostol with prostaglandin E2 vaginal tablets for ripening of cervix and induction of labour at term. Study Design: A non blinded, randomised, controlled trial. Place and Duration of Study: Department of Obstetrics and Gynaecology, Pakistan Air Force Hospital, Air Headquarters Islamabad from July 2005 to January 2006. Patients and Methods: Hundred pregnant women with a singleton live pregnancy, at term (37-42 weeks) with cephalic presentation were selected for induction of labour for various indications having a Bishop's score of < or =5. These women were randomly allocated to receive either 100 micro gm of misoprostol rally repeated four hourly to a maximum of four doses or a 3mg PGE2 tablet vaginally repeated six hourly to a maximum of two doses. Main outcomes measured: Cervical score before and after oral misoprostol and prostaglandin E2 vaginal tablets, vaginal birth within 24 hours of first prostaglandin dose, no of patients having failed induction, caesarean sections (all), caesarean section for fetal distress and uterine hyperstimulation with associated changes in fetal heart rate. Results: Over the period of one year 100 women were recruited for the study, 50 to the misoprostol group and 50 to the vaginal prostaglandin E2 group. There was no significant differences between the two treatment groups in the primary outcomes: improvement in bishops score in both the groups, no of patients with failed induction in both the groups misoprostol 2/50 (4%) v PGE2 3/50 (6%) , vaginal birth achieved in 24 hours (misoprostol 27/50 (54%) v PGE2 29/50 (58%), caesarean sections 14/50 (28%) v 12/50(24%) caesarean section for fetal distress 4/50((8%) v 5/50(9%); uterine hyperstimulation with fetal heart rate changes 2/50 ((4%) v none in the PGE2 group.). Neonatal outcomes were not significantly different in the two groups. Conclusion: Oral misoprostol in strength of 100 micro gm has similar efficacy to vaginal PGE2 tablets

  7. Development and optimization of carvedilol orodispersible tablets: enhancement of pharmacokinetic parameters in rabbits

    Science.gov (United States)

    Aljimaee, Yazeed HM; El-Helw, Abdel-Rahim M; Ahmed, Osama AA; El-Say, Khalid M

    2015-01-01

    Background Carvedilol (CVD) is used for the treatment of essential hypertension, heart failure, and systolic dysfunction after myocardial infarction. Due to its lower aqueous solubility and extensive first-pass metabolism, the absolute bioavailability of CVD does not exceed 30%. To overcome these drawbacks, the objective of this work was to improve the solubility and onset of action of CVD through complexation with hydroxypropyl-β-cyclodextrin and formulation of the prepared complex as orodispersible tablets (ODTs). Methods Compatibility among CVD and all tablet excipients using differential scanning calorimetry and Fourier transform infrared spectroscopy, complexation of CVD with different polymers, and determination of the solubility of CVD in the prepared complexes were first determined. A Box-Behnken design (BBD) was used to study the effect of tablet formulation variables on the characteristics of the prepared tablets and to optimize preparation conditions. According to BBD design, 15 formulations of CVD-ODTs were prepared by direct compression and then evaluated for their quality attributes. The relative pharmacokinetic parameters of the optimized CVD-ODTs were compared with those of the marketed CVD tablet. A single dose, equivalent to 2.5 mg/kg CVD, was administered orally to New Zealand white rabbits using a double-blind, randomized, crossover design. Results The solubility of CVD was improved from 7.32 to 22.92 mg/mL after complexation with hydroxypropyl-β-cyclodextrin at a molar ratio of 1:2 (CVD to cyclodextrin). The formulated CVD-ODTs showed satisfactory results concerning tablet hardness (5.35 kg/cm2), disintegration time (18 seconds), and maximum amount of CVD released (99.72%). The pharmacokinetic data for the optimized CVD-ODT showed a significant (Ptablet. Conclusion The optimized CVD-ODTs showed improved oral absorption of CVD and a subsequent acceleration of clinical effect, which is favored for hypertensive and cardiac patients. PMID

  8. MRI outcomes with cladribine tablets for multiple sclerosis in the CLARITY study.

    Science.gov (United States)

    Comi, Giancarlo; Cook, Stuart D; Giovannoni, Gavin; Rammohan, Kottil; Rieckmann, Peter; Sørensen, Per Soelberg; Vermersch, Patrick; Hamlett, Anthony C; Viglietta, Vissia; Greenberg, Steven J

    2013-04-01

    We herein provide a comprehensive assessment of magnetic resonance imaging (MRI) outcomes from CLARITY, a 96-week, double-blind study demonstrating significant clinical and MRI improvements in patients with relapsing-remitting multiple sclerosis (RRMS) treated with cladribine tablets. Patients with RRMS were randomized 1:1:1 to annual short-course therapy with cladribine tablets cumulative dose 3.5 or 5.25 mg/kg or placebo. MRI endpoints included mean number of T1 gadolinium-enhancing (Gd+), active T2 and combined unique (CU) lesions/patient/scan. MRI-measured disease activity was significantly reduced in both cladribine tablets groups versus placebo. The proportion of patients with no active lesions at study end was: T1 Gd+ lesions: 86.8 and 91.0 versus 48.3 % (p tablet groups when data were stratified by baseline disease characteristics. For example, the percentage of patients who remained lesion-free over the study was significantly greater in cladribine tablet groups than in the placebo group for all lesion types regardless of relapse category at baseline (p MRI-measured disease activity was greatly reduced by both doses of cladribine tablets, with consistent effect across clinically relevant patient populations. These findings add to our scientific understanding of the neurological impact of this therapeutic modality in patients with RRMS.

  9. Tablet Use within Medicine

    Science.gov (United States)

    Hogue, Rebecca J.

    2013-01-01

    This paper discusses the scholarly literature related to tablet computer use in medicine. Forty-four research-based articles were examined for emerging categories and themes. The most studied uses for tablet computers include: patients using tablets to complete diagnostic survey instruments, medical professionals using tablet computers to view…

  10. Comparison of interface structure of BCC metallic (Fe, V and Nb) films on MgO (100) substrate

    Energy Technology Data Exchange (ETDEWEB)

    Du, J.L. [State Key Laboratory of Nuclear Physics and Technology, School of Physics, Peking University, Beijing 100871 (China); Zhang, L.Y. [State Key Laboratory for Mechanical Behavior of Materials, Xi’an Jiaotong University, Xi’an, 710049 (China); Fu, E.G., E-mail: efu@pku.edu.cn [State Key Laboratory of Nuclear Physics and Technology, School of Physics, Peking University, Beijing 100871 (China); Ding, X., E-mail: dingxd@mail.xjtu.edu.cn [State Key Laboratory for Mechanical Behavior of Materials, Xi’an Jiaotong University, Xi’an, 710049 (China); Yu, K.Y., E-mail: kyyu@cup.edu.cn [Department of Materials Science and Engineering, China University of Petroleum, Beijing 102249 (China); Wang, Y.G. [State Key Laboratory of Nuclear Physics and Technology, School of Physics, Peking University, Beijing 100871 (China); Wang, Y.Q.; Baldwin, J.K. [Experimental Physical Sciences Directorate, Los Alamos National Laboratory, Los Alamos, NM 87544 (United States); Wang, X.J. [State Key Laboratory of Advanced Optical Communication Systems and Networks, Peking University, Beijing 100871 (China); Xu, P. [Department of Chemistry, Harbin Institute of Technology, Harbin, Heilongjiang, 150001 (China)

    2017-07-15

    Highlights: • The difference of BCC metal/MgO(100) interface configuration with various lattice mismatches is identified by experiments and simulations in terms of dislocations and work of separation. • The strength of bonds along interface is found to be the fundamental factor to determine the interface configurations between BCC metal and MgO substrate. • The combination of experiments and simulations shows that the O-atop model is the actual match type between BCC metal and MgO substrate. - Abstract: This study systematically investigates the interface structure of three body-centered-cubic (BCC) metallic (Fe, V and Nb) films grown on MgO(100) substrates through experiments and simulations. Orientation relationships of their interfaces with the different lattice mismatches exhibit cube-on-cube configurations. The misfit dislocations at these three interfaces exhibit different characteristics. High resolution TEM (HRTEM), combined with first principle calculations, demonstrates the O-atop match type between metal atoms and MgO substrates for the first time. The fundamental mechanism in determining the interface configuration is discussed in terms of the work of separation and delocalization of atomic charge density.

  11. Impairment of the in vitro Release of Carbamazepine from Tablets

    Directory of Open Access Journals (Sweden)

    Alija Uzunović

    2010-08-01

    Full Text Available Carbamazepine belongs to the class II biopharmaceutical classification system (BCS which is characterized by a high per-oral dose, a low aqueous solubility and a high membrane permeability. The bioavailability of such a drug is limited by the dissolution rate. The present study deals with the formulations of immediate release tablets of poorly soluble carbamazepine. As model tablets for this investigation, two formulations (named “A” and “B” formulations of carbamazepine tablets labeled to contain 200 mg were evaluated. The aim of this study was to establish possible differences in dissolution profile of these two formulations purchased from the local market.The increased crystallinity together with enlarged particle size, enhanced aggregation and decreased wettability of the drug, resulted in insufficient dissolution rate for formulation “B’.’ From the dissolution point of view, this formulation was inferior to the formulation “A, due to the solubilization effect.

  12. Formulation and evaluation of diclofenac potassium fast-disintegrating tablets and their clinical application in migraine patients.

    Science.gov (United States)

    Comoglu, Tansel; Dogan, Aysegul; Comoglu, Selcuk; Basci, Nursabah

    2011-03-01

    The aim of this study was to prepare fast-disintegrating tablets (FDTs) of diclofenac potassium with sufficient integrity as well as a pleasant taste, using two different fillers and binders: Tablettose 70(®) and Di-Pac(®). Tablets were made with direct compression method. Tablet properties such as porosity, hardness, and disintegration time were determined. Diclofenac potassium determinations were carried out using a validated spectrophotometric method for the analysis of drug. Furthermore, in vivo experiments were carried out to compare the analgesic effect and the time to relieve migraine headache between the commercial tablets and FDTs of diclofenac potassium against placebo. Results showed that FDTs of diclofenac potassium with durable structure and desirable taste can be prepared using both fillers and binders but tablets prepared with Di-Pac had a better taste so the tablet formulation containing Di-Pac was chosen for in vivo experiments. Placebo controlled in vivo trial demonstrated that 50 mg diclofenac potassium, administered as a single dose of FDTs or commercial tablets, was effective in relieving the pain and both of them were superior to placebo.

  13. In vivo anti-psoriatic activity, biodistribution, sub-acute and sub-chronic toxicity studies of orally administered methotrexate loaded chitin nanogel in comparison with methotrexate tablet.

    Science.gov (United States)

    Panonnummal, Rajitha; Jayakumar, R; Anjaneyan, Gopikrishnan; Sabitha, M

    2018-04-15

    The anti-psoriatic efficacy of orally administered methotrexate loaded chitin nanogel (MCNG) was evaluated (two doses- 2.715 mg/kg and 5.143 mg/kg) and compared against orally administered methotrexate tablet MTX (5.143 mg/kg). MCNG at both dose levels of 2.715 mg/kg and 5.143 mg/kg exhibited significant anti-psoriatic activity which is very much comparable with MTX, caused normalization of histological features and inflammatory score associated with induced psoriasis. Biodistribution studies revealed the presence of drug in serum and in vital organs at all the three cases with highest amount in MCNG at 5.143 mg/kg dose, followed by MTX tablet and are lowest in MCNG at 2.715 mg/kg dose. MCNG at the highest dose of 5.143 mg/kg caused liver, lung and kidney toxicities on sub acute toxicity studies and MTX tablet was found to be toxic on liver and lung on sub chronic toxicity studies. MCNG 2.715 mg/kg was found to be safe on both sub acute and sub chronic administrations, suggesting that it can provide sufficient serum and tissue level of methotrexate necessary to clear psoriatic lesions, without inducing systemic toxicity and expected to be a better alternative for orally administered conventional methotrexate tablet for patients who need systemic medications for psoriasis. Copyright © 2018. Published by Elsevier B.V.

  14. A new tablet brittleness index.

    Science.gov (United States)

    Gong, Xingchu; Sun, Changquan Calvin

    2015-06-01

    Brittleness is one of the important material properties that influences the success or failure of powder compaction. We have discovered that the reciprocal of diametrical elastic strain at fracture is the most suitable tablet brittleness indices (TBIs) for quantifying brittleness of pharmaceutical tablets. The new strain based TBI is supported by both theoretical considerations and a systematic statistical analysis of friability data. It is sufficiently sensitive to changes in both tablet compositions and compaction parameters. For all tested materials, it correctly shows that tablet brittleness increases with increasing tablet porosity for the same powder. In addition, TBI increases with increasing content of a brittle excipient, lactose monohydrate, in the mixtures with a plastic excipient, microcrystalline cellulose. A probability map for achieving less than 1% tablet friability at various combinations of tablet tensile strength and TBI was constructed. Data from marketed tablets validate this probability map and a TBI value of 150 is recommended as the upper limit for pharmaceutical tablets. This TBI can be calculated from the data routinely obtained during tablet diametrical breaking test, which is commonly performed for assessing tablet mechanical strength. Therefore, it is ready for adoption for quantifying tablet brittleness to guide tablet formulation development since it does not require additional experimental work. Copyright © 2015 Elsevier B.V. All rights reserved.

  15. Investigation of LiF, Mg and Ti (TLD-100 Reproducibility

    Directory of Open Access Journals (Sweden)

    Sadeghi M.

    2015-12-01

    Full Text Available LiF, Mg and Ti cubical TLD chips (known as TLD-100 are widely used for dosimetry purposes. The repeatability of TL dosimetry is investigated by exposing them to doses of (81, 162 and 40.5 mGy with 662keV photons of Cs-137. A group of 40 cubical TLD chips was randomly selected from a batch and the values of Element Correction Coefficient (ECC were obtained 4 times by irradiating them to doses of 81 mGy (two times, 162mGy and 40.5mGy. Results of this study indicate that the average reproducibility of ECC calculation for 40 TLDs is 1.5%, while these values for all chips do not exceed 5%.

  16. Dissolution of Intact, Divided and Crushed Circadin Tablets: Prolonged vs. Immediate Release of Melatonin

    Directory of Open Access Journals (Sweden)

    Hui Ming Chua

    2016-01-01

    Full Text Available Circadin 2 mg prolonged-release tablet is the only licensed melatonin product available in the UK. Circadin is indicated for patients with primary insomnia aged 55 and over, but is more widely used “off-label” to treat sleep disorders especially in the paediatric population. Children and older people often have difficulty swallowing tablets and dividing the tablet is sometimes required to ease administration. The aim of this study was to measure the release profile of melatonin from Circadin tablets when divided or crushed, and compare this with release from intact tablets. Dissolution testing was also performed for unlicensed melatonin products for comparison. Dissolution tests were performed using the pharmacopoeial paddle apparatus, with melatonin release analyzed by high performance liquid chromatography. Melatonin content, hardness, friability, and disintegration of the products were also evaluated. The prolonged release of melatonin from Circadin tablets was unlike that of any other product tested. When divided into halves, Circadin preserved most of the prolonged-release characteristic (f2 = 58, whereas quarter-cut and crushed tablet had a more immediate melatonin release profile. Circadin is significantly less expensive and should be preferred to unlicensed medicines which are not pharmaceutically equivalent and offer less quality assurance.

  17. Study of drug release and tablet characteristics of silicone adhesive matrix tablets.

    Science.gov (United States)

    Tolia, Gaurav; Li, S Kevin

    2012-11-01

    Matrix tablets of a model drug acetaminophen (APAP) were prepared using a highly compressible low glass transition temperature (T(g)) polymer silicone pressure sensitive adhesive (PSA) at various binary mixtures of silicone PSA/APAP ratios. Matrix tablets of a rigid high T(g) matrix forming polymer ethyl cellulose (EC) were the reference for comparison. Drug release study was carried out using USP Apparatus 1 (basket), and the relationship between the release kinetic parameters of APAP and polymer/APAP ratio was determined to estimate the excipient percolation threshold. The critical points attributed to both silicone PSA and EC tablet percolation thresholds were found to be between 2.5% and 5% w/w. For silicone PSA tablets, satisfactory mechanical properties were obtained above the polymer percolation threshold; no cracking or chipping of the tablet was observed above this threshold. Rigid EC APAP tablets showed low tensile strength and high friability. These results suggest that silicone PSA could eliminate issues related to drug compressibility in the formulation of directly compressed oral controlled release tablets of poorly compressible drug powder such as APAP. No routinely used excipients such as binders, granulating agents, glidants, or lubricants were required for making an acceptable tablet matrix of APAP using silicone PSA. Copyright © 2012 Elsevier B.V. All rights reserved.

  18. A New Application of Lipid Nanoemulsions as Coating Agent, Providing Zero-Order Hydrophilic Drug Release from Tablets

    Directory of Open Access Journals (Sweden)

    Nicolas Anton

    2012-01-01

    Full Text Available The objective of the present investigation was to evaluate potential of nanoemulsions as a coating material for the tablets. The nanoemulsion of size less than 100 nm was prepared using a simple and low-energy spontaneous emulsification method. Conventional tablets containing theophylline as a model hydrophilic drug were prepared. The theophylline tablets were coated with the nanoemulsion using a fluid bed coater. The effect of different levels of the nanoemulsion coating on the theophylline release was evaluated. The theophylline tablets containing different levels of the nanoemulsion coating could be successfully prepared. Interestingly, the coating of tablet with the nanoemulsion resulted in zero-order release of theophylline from the tablets. The noncoated theophylline tablets release the entire drug in less than 2 minutes, whereas nanoemulsion coating delayed the release of theophylline from tablets. This investigation establishes the proof of concept for the potential of nanoemulsions as a coating material for tablets.

  19. Hardness, function, emotional well-being, satisfaction and the overall sexual experience in men using 100-mg fixed-dose or flexible-dose sildenafil citrate.

    Science.gov (United States)

    Ströberg, P; Kaminetsky, J C; Park, N C; Goldfischer, E R; Creanga, D L; Stecher, V J

    2010-01-01

    The prescribing information for sildenafil citrate (VIAGRA, Pfizer, New York, NY, USA) recommends flexible dosing (50 mg initially, adjusted to 100 or 25 mg based on effectiveness and tolerability) in most men with erectile dysfunction (ED). In many men, however, 100 mg may be the most appropriate initial dose because it would reduce the need for titration and could prevent discouragement and treatment abandonment should 50 mg be insufficient. Results of two previously published double-blind, placebo-controlled sildenafil trials of similar design except for a fixed-dose vs flexible-dose regimen were analyzed. Relative to the flexible-dose, approximately one-third more men were satisfied with an initial and fixed dose of 100 mg. In addition, tolerability was similar, and improvements from baseline in outcomes on validated, ED-specific, patient-reported questionnaires were either similar (erectile function and the percentage of completely hard and fully rigid erections) or greater (emotional well-being and the overall sexual experience). The similarity in outcomes is not surprising given that almost 90% of the men in the flexible-dose trial titrated to 100 mg after 2 weeks. These data suggest prescription of an initial dose of 100 mg for men with ED, except in those for whom it is inappropriate.

  20. Desktop 3D printing of controlled release pharmaceutical bilayer tablets.

    Science.gov (United States)

    Khaled, Shaban A; Burley, Jonathan C; Alexander, Morgan R; Roberts, Clive J

    2014-01-30

    Three dimensional (3D) printing was used as a novel medicine formulation technique for production of viable tablets capable of satisfying regulatory tests and matching the release of standard commercial tablets. Hydroxypropyl methylcellulose (HPMC 2208) (Methocel™ K100M Premium) and poly(acrylic acid) (PAA) (Carbopol(®) 974P NF) were used as a hydrophilic matrix for a sustained release (SR) layer. Hypromellose(®) (HPMC 2910) was used as a binder while microcrystalline cellulose (MCC) (Pharmacel(®) 102) and sodium starch glycolate (SSG) (Primojel(®)) were used as disintegrants for an immediate release (IR) layer. Commercial guaifenesin bi-layer tablets (GBT) were used as a model drug (Mucinex(®)) for this study. There was a favourable comparison of release of the active guaifenesin from the printed hydrophilic matrix compared with the commercially available GBT. The printed formulations were also evaluated for physical and mechanical properties such as weight variation, friability, hardness and thickness as a comparison to the commercial tablet and were within acceptable range as defined by the international standards stated in the United States Pharmacopoeia (USP). All formulations (standard tablets and 3D printed tablets) showed Korsmeyer-Peppas n values between 0.27 and 0.44 which indicates Fickian diffusion drug release through a hydrated HPMC gel layer. Copyright © 2013 Elsevier B.V. All rights reserved.

  1. Hydrogen dissociation and incorporation on Mg{sub 17}Al{sub 12}(100) surface: A density functional theory study

    Energy Technology Data Exchange (ETDEWEB)

    Ning, Hua [Guangxi Key Laboratory for Relativistic Astrophysics, Guangxi Colleges and Universities Key Laboratory of Novel Energy Materials and Related Technology, College of Physics Science and Technology, Guangxi University, Nanning 530004 (China); Guangxi Collaborative Innovation Center of Structure and Property for New Energy and Materials, School of Material Science and Engineering, Guilin University of Electronic Technology, Guilin 541004 (China); Zhou, Zhiyan; Zhang, Ziyan [Guangxi Key Laboratory for Relativistic Astrophysics, Guangxi Colleges and Universities Key Laboratory of Novel Energy Materials and Related Technology, College of Physics Science and Technology, Guangxi University, Nanning 530004 (China); Zhou, Wenzheng; Li, Guangxu [Guangxi Key Laboratory for Relativistic Astrophysics, Guangxi Colleges and Universities Key Laboratory of Novel Energy Materials and Related Technology, College of Physics Science and Technology, Guangxi University, Nanning 530004 (China); Guangxi Collaborative Innovation Center of Structure and Property for New Energy and Materials, School of Material Science and Engineering, Guilin University of Electronic Technology, Guilin 541004 (China); Guo, Jin, E-mail: guojin@gxu.edu.cn [Guangxi Key Laboratory for Relativistic Astrophysics, Guangxi Colleges and Universities Key Laboratory of Novel Energy Materials and Related Technology, College of Physics Science and Technology, Guangxi University, Nanning 530004 (China); Guangxi Collaborative Innovation Center of Structure and Property for New Energy and Materials, School of Material Science and Engineering, Guilin University of Electronic Technology, Guilin 541004 (China)

    2017-02-28

    Highlights: • Hydrogen adsorption, dissociation, and penetration on (in) Mg{sub 17}Al{sub 12} (100) surface are studied. • Hydrogen molecules are dissociated on the surface with barrier of 0.63 eV. • The maximum barrier energy for atomic hydrogen penetration into the subsurface is ∼0.7 eV. • The hybridization between the s orbital of H and the s orbitals of Mg is major. - Abstract: Hydrogen adsorption, dissociation, and penetration on (in) Mg{sub 17}Al{sub 12} (100) surface are studied extensively by DFT total-energy calculations. The adsorption geometries, dissociation barriers, various diffusion pathways, penetrative processes, and electronic structures were investigated. Results show that the atomic and molecular hydrogen forms prefer to be adsorbed on the Mg3-Mg3 bridge sites (C sites). Hydrogen molecules are dissociated on the surface with the minimum barrier energy of 0.63 eV. There are two stages in the process of hydrogen incorporation, which are hydrogen diffusion on the surface and the penetration from the surface into the subsurface. Two possible pathways of atomic hydrogen penetration from surface into subsurface are found. The calculations of electronic structures show that the hybridization between the s orbital of H and the s orbitals of Mg is major. The Mg-Mg bond on the outmost surface is shortened from 4.48 Å to 3.30 Å after the hydrogen adsorption on C sites, showing the strong interaction between Mg and H atoms.

  2. MRI outcomes with cladribine tablets for multiple sclerosis in the CLARITY study

    DEFF Research Database (Denmark)

    Comi, Giancarlo; Cook, Stuart D; Giovannoni, Gavin

    2013-01-01

    We herein provide a comprehensive assessment of magnetic resonance imaging (MRI) outcomes from CLARITY, a 96-week, double-blind study demonstrating significant clinical and MRI improvements in patients with relapsing-remitting multiple sclerosis (RRMS) treated with cladribine tablets. Patients...... with RRMS were randomized 1:1:1 to annual short-course therapy with cladribine tablets cumulative dose 3.5 or 5.25 mg/kg or placebo. MRI endpoints included mean number of T1 gadolinium-enhancing (Gd+), active T2 and combined unique (CU) lesions/patient/scan. MRI-measured disease activity was significantly...... reduced in both cladribine tablets groups versus placebo. The proportion of patients with no active lesions at study end was: T1 Gd+ lesions: 86.8 and 91.0 versus 48.3 % (p ...

  3. Bioequivalence study of two losartan tablet formulations with special emphasis on cardiac safety.

    Science.gov (United States)

    Khandave, Suhas S; Sawant, Satish V; Sahane, Rakhi V; Murthi, Vivekanand; Dhanure, Shivanand S; Surve, Pradeep G

    2012-05-01

    To study the bioequivalence of Losartan Potassium Tablets 50 mg manufactured by Micro Labs Ltd. India to Cozaar® Tablets 50 mg, manufactured by Merck Sharp and Dohme Ltd., UK in normal healthy adult subjects under fasting condition along with the comparative safety evaluation of both treatments. The in vitro dissolution studies were carried out on 12 units each of test and reference products using the paddle method and dissolution media like water, 0.1 N hydrochloric acid with pH 1.2, pH 4.5 acetate buffer and pH 6.8 phosphate buffer. An open label, randomized, two-treatment, two-period, two-sequence, crossover bioequivalence study with a washout period of 7 days was conducted in 60 healthy Indian male subjects. Serial blood samples were collected after drug administration in each study period. Plasma concentrations of losartan and losartan acid were determined using a validated LC-MS-MS method. The pharmacokinetic parameters of losartan and losartan acid were determined using a non compartmental model. Occurrence of adverse events, change in systolic blood pressure, diastolic blood pressure, heart rate and QT interval from the baseline to 3.50 h post dose were studied and compared between the two treatments as safety parameters. The in vitro study proved the essential similarity of both the formulations as evident from the similarity factor of > 50% in all the dissolution media. The ratios for geometric least square means and 90% confidence intervals were within the acceptance criteria of 80% to 125% for log transformed C(max), AUC(0-t) and AUC(0-∞) for losartan. No statistically significant difference between the two treatments was observed for either of the safety parameters. The test product Losartan Potassium tablets 50 mg manufactured by Micro Labs Limited, India was bioequivalent to Cozaar® tablets 50 mg, manufactured by Merck Sharp and Dohme Ltd., UK in terms of rate and extent of absorption. Both treatments were well tolerated and had similar non

  4. Formulation and evaluation of a novel matrix-type orally disintegrating Ibuprofen tablet.

    Science.gov (United States)

    Tayebi, Hoda; Mortazavi, Seyed Alireza

    2011-01-01

    Orally disintegrating tablets (ODTs) are capable of turning quickly into a liquid dosage form in contact with the saliva, thus possessing the advantages of both the solid dosage forms particularly stability and liquid dosage forms specially ease of swallowing and pre-gastric absorption of drug. The aim of this study was to prepare a novel matrix-type buccal fast disintegrating ibuprofen tablet formulation using special polymers, water soluble excipients, super-disintegrants and quickly soluble granules. For this purpose different tablet formulations of ibuprofen were prepared. The amount of ibuprofen in each formulation was 100 mg. Eight groups of formulation were prepared (A-H series), accounting for a total number of 45 formulations. Formulations prepared were examined in terms of different physicochemical tests including powder/granule flowability, appearance, thickness, uniformity of weight, hardness, friability and disintegration time. Results of formulation F22a (in series F), was found to be acceptable, making it the chosen formulation for further studies. Then, by adding various flavorants and sweeteners to this formulation, complementary series of formulations, named G and H, were prepared. Following the comparison of their taste with each other through asking 10 volunteers, the most suitable formulation regarding the taste, being formulation F22s, was chosen as the ultimate formulation. This formulation had PVP, ibuprofen and croscarmellose as the intra-granular components and xylitol and saccharin as the extra-granular ingredients. Formulation F22s was found to be acceptable in terms of physicochemical tests conducted, showing quick disintegration within the buccal cavity, appropriate hardness and rather low friability. Hence formulation F22s was selected as the final formulation.

  5. 75 FR 14444 - Determination That DIDREX (Benzphetamine Hydrochloride) Tablets, 25 Milligrams, Were Not...

    Science.gov (United States)

    2010-03-25

    ... subsidiary of Pfizer Inc. Benzphetamine HCl 25-mg tablets are indicated in the management of exogenous obesity as a short-term (a few weeks) adjunct in a regimen of weight reduction based on caloric...

  6. When color fails: illicit blue tablets containing anabolic androgen steroids.

    Science.gov (United States)

    Favretto, Donata; Castagna, Franca; Maietti, Sergio; Boscolo-Berto, Rafael; Ferrara, Santo Davide

    2013-09-01

    The necessity of specific, confirmatory tests in the identification of seized illicit products was highlighted by the analysis of eighteen heart shaped, blue tablets confiscated by Police at a street control in the North East of Italy. The tablets responded as amphetamines to a preliminary color test (Marquis); a subsequent, confirmatory assay by gas chromatography-mass spectrometry revealed the presence of two anabolic androgen steroids (AAS), methandienone and methyltestosterone, in concentration of 1.7 and 1.5mg respectively per tablet; no trace of amphetamine-like or nitrogen containing compounds was found. The observed orange coloration was due to the reaction of concentrated sulphuric acid, contained in the Marquis reagent, with the Δ(4) C-3 keto group of steroids. The two AAS, banned under the world antidoping code, are not considered as psychoactive drugs of abuse in most countries, although their trafficking may entangle severe public health concerns. Copyright © 2013 Elsevier B.V. All rights reserved.

  7. Pharmaceutical equivalence of metformin tablets with various binders

    Directory of Open Access Journals (Sweden)

    L. C. Block

    2009-01-01

    Full Text Available

    Metformin hydrochloride is a high-dose drug widely used as an oral anti-hyperglycemic agent. As it is highly crystalline and has poor compaction properties, it is difficult to form tablets by direct compression. The aim of this study was to develop adequate metformin tablets, pharmaceutically equivalent to the reference product, Glucophage® (marketed as Glifage® in Brazil. Metformin 500mg tablets were produced by wet granulation with various binders (A = starch, B = starch 1500®, C = PVP K30®, D = PVP K90®. The tablets were analyzed for their hardness, friability, disintegration, dissolution, content uniformity and dissolution profile (basket apparatus at 50 rpm, pH 6.8 phosphate buffer. The 4 formulations, F1 (5% A and 5% C, F2 (5% B and 5% C, F3 (10% C and F4 (5% D, demonstrated adequate uniformity of content, hardness, friability, disintegration and total drug dissolution after 30 minutes (F1, F2 and F4, and after 60 minutes (F3. The drug release time profiles fitted a Higuchi model (F1, F2 and F3, similarly to the pharmaceutical reference, or a zero order model (F4. The dissolution efficiency for all the formulations was 75%, except for F3 (45%. F1 and F2 were thus equivalent to Glifage®. Keywords: dissolution; metformin; tablet; binder; pharmaceutical equivalence

  8. [Application of β-cyclodextrin in the formulation of ODT tablets containing ibuprofen].

    Science.gov (United States)

    Zimmer, Łukasz; Kasperek, Regina; Poleszak, Ewa

    2014-01-01

    Oral disintegrating tablet (ODT) dissolves or disintegrates in saliva and then it is swallowed. Diluent in direct compression formulation has a dual role: it increases bulk of the dosage form and it promotes binding of the constituent particles of the formulation. Hence, selection of diluent is important in tablets produced by direct compression method. The aim of this work was to exame feasibility of preparing and optimizing oral disintegrating tablet formulation using β-cyclodextrin as a diluent. 400 mg round tablets were prepared by direct compression method on single punch tablet press using flat plain-face. 60% β-CD and MCC (microcrystalline cellulose - MCC-Vivapur 102) were used at different proportions for all the formulations. 5% of Kollidon CL was added as superdisintegrant. The eight formulations prepared were assessed for weight variation, thickness, disintegration time, hardness and dissolution rate according to FP IX. A dissolution test was performed at 37ºC using the paddle method at 50 rpm with 900 mL phosphate buffer (pH 6.8) as a dissolution medium. The content of ibuprofen sodium was found inside the ± 5% of the theoretical value. Hardness values of presented tablets were in the range 0.11-0.15 kG/mm2. Friability of the tablets lower than 1% indicates that the developed formulations can be processed and handled without excessive care. Disintegration time was in the range of 86 to 161 s. The results confirm the good mechanical properties of tablets containing β-CD. A composition with 20% β-CD and 40% MCC fulfilled a maximum requisite of an optimum formulation. These properties were similar to Ludiflash, the formulation used for comparison purposes. In the present study, higher concentration of β cyclodextrin was found to improve the hardness of tablets without increasing the disintegration time.

  9. Oral Disintegration Tablets of Stavudine for HIV Management: A New Technological Approach.

    Science.gov (United States)

    Sankar, V; Ramakrishna, B; Devi, P Shalini; Karthik, S

    2012-11-01

    Stavudine oral disintegration tablets were formulated to minimize the bitter taste and to reduce the first-pass hepatic metabolism. The various precompression parameters like the angle of repose, bulk density, compressibility index and Hausner's ratio were determined for the powder blend. In this study, 14 formulations of stavudine oral disintegration tablet were prepared by direct compression method. The tablets were evaluated for weight variation, percentage friability, disintegration time, hardness, wetting time and water absorption ratio. The in vitro dissolution study results of the batch S1 (stavudine+crospovidone+sodium starch glycollate) are encouraging as highest dissolution rate (99.2% in 100 min) and lowest time of disintegration (56 s) was achieved. The in vivo drug release studies were carried out in rabbits and the relative bioavailability of formulation S1 was found to be 2.83 times greater than that of conventional tablets.

  10. Development of modified-release tablets of zolpidem tartrate by biphasic quick/slow delivery system.

    Science.gov (United States)

    Mahapatra, Anjan Kumar; Sameeraja, N H; Murthy, P N

    2015-06-01

    Zolpidem tartrate is a non-benzodiazepine analogue of imidazopyridine of sedative and hypnotic category. It has a short half-life with usual dosage regimen being 5 mg, two times a day, or 10 mg, once daily. The duration of action is considered too short in certain circumstances. Thus, it is desirable to lengthen the duration of action. The formulation design was implemented by preparing extended-release tablets of zolpidem tartrate using the biphasic delivery system technology, where sodium starch glycolate acts as a superdisintegrant in immediate-release part and hydroxypropyl methyl cellulose as a release retarding agent in extended-release core. Tablets were prepared by direct compression. Both the core and the coat contained the drug. The pre-compression blends were evaluated for angle of repose, bulk density, and compressibility index. The tablets were evaluated for thickness, hardness, weight variation test, friability, and in vitro release studies. No interaction was observed between zolpidem tartrate and excipients from the Fourier transform infrared spectroscopy and differential scanning calorimetry analysis. The results of all the formulations prepared were compared with reference product Stilnoct®. Optimized formulations showed release patterns that match the United States Pharmacopeia (USP) guidelines for zolpidem tartrate extended-release tablets. The mechanism of drug release was studied using different mathematical models, and the optimized formulation has shown Fickian diffusion. Accelerated stability studies were performed on the optimized formulation.

  11. Hardness, function, emotional well-being, satisfaction and the overall sexual experience in men using 100-mg fixed-dose or flexible-dose sildenafil citrate

    Science.gov (United States)

    Ströberg, P; Kaminetsky, J C; Park, N C; Goldfischer, E R; Creanga, D L; Stecher, V J

    2010-01-01

    The prescribing information for sildenafil citrate (VIAGRA, Pfizer, New York, NY, USA) recommends flexible dosing (50 mg initially, adjusted to 100 or 25 mg based on effectiveness and tolerability) in most men with erectile dysfunction (ED). In many men, however, 100mg may be the most appropriate initial dose because it would reduce the need for titration and could prevent discouragement and treatment abandonment should 50 mg be insufficient. Results of two previously published double-blind, placebo-controlled sildenafil trials of similar design except for a fixed-dose vs flexible-dose regimen were analyzed. Relative to the flexible-dose, approximately one-third more men were satisfied with an initial and fixed dose of 100mg. In addition, tolerability was similar, and improvements from baseline in outcomes on validated, ED-specific, patient-reported questionnaires were either similar (erectile function and the percentage of completely hard and fully rigid erections) or greater (emotional well-being and the overall sexual experience). The similarity in outcomes is not surprising given that almost 90% of the men in the flexible-dose trial titrated to 100mg after 2 weeks. These data suggest prescription of an initial dose of 100mg for men with ED, except in those for whom it is inappropriate. PMID:20596083

  12. Latent structure analysis in the pharmaceutical process of tablets prepared by wet granulation.

    Science.gov (United States)

    Uehara, Naoto; Hayashi, Yoshihiro; Mochida, Hiroshi; Otoguro, Saori; Onuki, Yoshinori; Obata, Yasuko; Takayama, Kozo

    2016-01-01

    Granule characteristics are some of the important intermediate qualities that determine tablet properties. However, the relationships between granule and tablet characteristics are poorly understood. The aim of this study was to elucidate relationships among formulation factors, granule characteristics, and tablet properties using a non-linear response surface method (RSM) incorporating a thin-plate spline interpolation (RSM-S) and a Bayesian network (BN). Tablets containing lactose (Lac), cornstarch (CS), and microcrystalline cellulose (MCC) were prepared by wet granulation. Ten formulations were prepared by an extreme vertices design. The angle of repose (Y 1 ), compressibility (Y 2 ), cohesion force (Y 3 ), internal friction angle (Y 4 ), and mean particle size (Y 5 ) were measured as granule characteristics. Tensile strength (TS) and disintegration time (DT) were measured as tablet properties. RSM-S results showed that TS increased with increasing amounts of MCC and Lac. DT decreased with increasing amounts of MCC and CS. The optimal BN models were predicted using four evaluation indices -Y 3 was shown to be the most important factor for TS, whereas Y 2 , Y 3 , and Y 4 were relatively important for predicting DT. Moreover, tablets with excellent tablet properties (i.e. high TS and low DT) were produced by relatively high Y 1 , low Y 2 , high Y 3 , high Y 4 , and middle Y 5 values, and resulted from the middle of MCC, middle-to-low CS, low Lac, and middle-to-low magnesium stearate (Mg-St) amounts. The RSM-S and BN techniques are useful for revealing complex relationships among formulation factors, granule characteristics, and tablet properties.

  13. Safety Evaluation of Crocin (a constituent of saffron Tablets in Healthy Volunteers

    Directory of Open Access Journals (Sweden)

    Amir Houshang Mohamadpour

    2013-01-01

    Full Text Available Objective(s: Crocin is the chemical ingredient primarily responsible for the color of saffron. It has different pharmacological effects such as antioxidant, anticancer and memory improving activities. Crocin tablets were evaluated for short-term safety and tolerability in healthy adult volunteers. Materials and Methods: The study was a randomized, double-blind, placebo-controlled design consisting of one month treatment of crocin tablets. Volunteers who fulfilled inclusion and exclusion criteria were randomized into 2 groups of 22 each (males and females and received 20 mg crocin tablets or placebo. General measures of health were recorded during the study such as hematological, biochemical, hormonal and urinary parameters in pre and post-treatment periods. Results: No major adverse events were reported during the trial. Crocin tablets did not change the above parameters except that it decreased amylase, mixed white blood cells and PTT in healthy volunteers after one month. Conclusion: This clinical safety evaluation showed a relatively safe and normal profile for crocin in healthy volunteers at the given doses within the trial period.

  14. Fosamprenavir or atazanavir once daily boosted with ritonavir 100 mg, plus tenofovir/emtricitabine, for the initial treatment of HIV infection: 48-week results of ALERT

    Directory of Open Access Journals (Sweden)

    Ross Lisa L

    2008-03-01

    Full Text Available Abstract Background Once-daily (QD ritonavir 100 mg-boosted fosamprenavir 1400 mg (FPV/r100 or atazanavir 300 mg (ATV/r100, plus tenofovir/emtricitabine (TDF/FTC 300 mg/200 mg, have not been compared as initial antiretroviral treatment. To address this data gap, we conducted an open-label, multicenter 48-week study (ALERT in 106 antiretroviral-naïve, HIV-infected patients (median HIV-1 RNA 4.9 log10 copies/mL; CD4+ count 191 cells/mm3 randomly assigned to the FPV/r100 or ATV/r100 regimens. Results At baseline, the FPV/r100 or ATV/r100 arms were well-matched for HIV-1 RNA (median, 4.9 log10 copies/mL [both], CD4+ count (mean, 176 vs 205 cells/mm3. At week 48, intent-to-treat: missing/discontinuation = failure analysis showed similar responses to FPV/r100 and ATV/r100 (HIV-1 RNA 3, p = 0.398 [Wilcoxon rank sum test]. Fasting total/LDL/HDL-cholesterol changes-from-baseline were also similar, although week 48 median fasting triglycerides were higher with FPV/r100 (150 vs 131 mg/dL. FPV/r100-treated patients experienced fewer treatment-related grade 2–4 adverse events (15% vs 57%, with differences driven by ATV-related hyperbilirubinemia. Three patients discontinued TDF/FTC because their GFR decreased to Conclusion The all-QD regimens of FPV/r100 and ATV/r100, plus TDF/FTC, provided similar virologic, CD4+ response, and fasting total/LDL/HDL-cholesterol changes through 48 weeks. Fewer FPV/r100-treated patients experienced treatment-related grade 2–4 adverse events.

  15. PEMBERIAN TABLET ASAM FOLAT BAGI IBU-IBU USIA REPRODUKTIF DI DESA ABIANSEMAL, BADUNG

    Directory of Open Access Journals (Sweden)

    Wihandani Desak Made

    2012-09-01

    Full Text Available Abstract Folat deficiency that happened during early period of pregnancy, has known as one of the factor that cause fetal abnormalities. That why it is important for pregnant women to get information about the rule of folic acid in preventing fetal abnormalities. From 93 women within reproductive age, 6 of them were pregnant. Pregnant women were given 30 tablets of 0,4 mg folic acid taken once a day, and the less 87 women who were not in pregnant state received 10 tablets of folic acid to be taken once a day.

  16. Adrenaline (epinephrine) microcrystal sublingual tablet formulation: enhanced absorption in a preclinical model.

    Science.gov (United States)

    Rawas-Qalaji, Mutasem; Rachid, Ousama; Mendez, Belacryst A; Losada, Annette; Simons, F Estelle R; Simons, Keith J

    2015-01-01

    For anaphylaxis treatment in community settings, adrenaline (epinephrine) administration using an auto-injector in the thigh is universally recommended. Despite this, many people at risk of anaphylaxis in community settings do not carry their prescribed auto-injectors consistently and hesitate to use them when anaphylaxis occurs.The objective of this research was to study the effect of a substantial reduction in adrenaline (Epi) particle size to a few micrometres (Epi microcrystals (Epi-MC)) on enhancing adrenaline dissolution and increasing the rate and extent of sublingual absorption from a previously developed rapidly disintegrating sublingual tablet (RDST) formulation in a validated preclinical model. The in-vivo absorption of Epi-MC 20 mg RDSTs and Epi 40 mg RDSTs was evaluated in rabbits. Epi 0.3 mg intramuscular (IM) injection in the thigh and placebo RDSTs were used as positive and negative controls, respectively. Epimean (standard deviation) area under the plasma concentration vs time curves up to 60 min and Cmax from Epi-MC 20 mg and Epi 40 mg RDSTs did not differ significantly (P > 0.05) from Epi 0.3 mg IM injection. After adrenaline, regardless of route of administration, pharmacokinetic parameters were significantly higher (P adrenaline levels). Epi-MC RDSTs facilitated a twofold increase in Epi absorption and a 50% reduction in the sublingual dose. This novel sublingual tablet formulation is potentially useful for the first-aid treatment of anaphylaxis in community settings. © 2014 Royal Pharmaceutical Society.

  17. Compressibility of tableting materials and properties of tablets with glyceryl behenate

    Directory of Open Access Journals (Sweden)

    Mužíková Jitka

    2015-03-01

    Full Text Available The paper studies the compressibility of directly compressible tableting materials with dry binders, spray-dried lactose and microcrystalline cellulose, and glyceryl dibehenate at various concentrations. Compressibility was evaluated by means of the energy profile of compression and tensile strength of tablets. Release rate of the active ingredient, salicylic acid, from the tablets was also examined. In the case of microcrystalline cellulose, a higher concentration of glyceryl dibehenate increased the strength of tablets, while this did not occur in the case of spray-dried lactose. Increasing concentration of glyceryl dibehenate prolonged the release of salicylic acid; however, no statistically significant difference was found compared to the type of the dry binder used

  18. Evaluating tablet computers as a survey tool in rural communities.

    Science.gov (United States)

    Newell, Steve M; Logan, Henrietta L; Guo, Yi; Marks, John G; Shepperd, James A

    2015-01-01

    Although tablet computers offer advantages in data collection over traditional paper-and-pencil methods, little research has examined whether the 2 formats yield similar responses, especially with underserved populations. We compared the 2 survey formats and tested whether participants' responses to common health questionnaires or perceptions of usability differed by survey format. We also tested whether we could replicate established paper-and-pencil findings via tablet computer. We recruited a sample of low-income community members living in the rural southern United States. Participants were 170 residents (black = 49%; white = 36%; other races and missing data = 15%) drawn from 2 counties meeting Florida's state statutory definition of rural with 100 persons or fewer per square mile. We randomly assigned participants to complete scales (Center for Epidemiologic Studies Depression Inventory and Regulatory Focus Questionnaire) along with survey format usability ratings via paper-and-pencil or tablet computer. All participants rated a series of previously validated posters using a tablet computer. Finally, participants completed comparisons of the survey formats and reported survey format preferences. Participants preferred using the tablet computer and showed no significant differences between formats in mean responses, scale reliabilities, or in participants' usability ratings. Overall, participants reported similar scales responses and usability ratings between formats. However, participants reported both preferring and enjoying responding via tablet computer more. Collectively, these findings are among the first data to show that tablet computers represent a suitable substitute among an underrepresented rural sample for paper-and-pencil methodology in survey research. Published 2014. This article is a U.S. Government work and is in the public domain in the USA.

  19. 76 FR 53908 - Determination That OPANA ER (Oxymorphone Hydrochloride) Extended-Release Tablets, 7.5 Milligrams...

    Science.gov (United States)

    2011-08-30

    ... proceedings that could result in the withdrawal of approval of the ANDAs that refer to the listed drug. OPANA... relief of moderate to severe pain in patients requiring continuous, around-the-clock opioid treatment for... withdrawal of OPANA ER (oxymorphone HCl) extended-release tablets, 7.5 mg and 15 mg, from sale. We have also...

  20. Forecasting Medical Materiel Requirements for Contingency Operations

    Science.gov (United States)

    2004-04-09

    Antituberculosis Agents 6505008122579 51479004701 ETHAMBUTOL 400MG TABLET 100S BT Antituberculosis Agents 6505001326904 17236018201 ISONIAZID 300MG TABLET ...the Marine Corps’ BAS AMAL required to treat notional patient stream Figure 6. RSVP output for acetaminophen tablets for a fictitious scenario with...patient requirements. This can be seen in Figure 6 below. Here, RSVP projected in this example, the quantity of acetaminophen tablets needed over six

  1. Evaluation about wettability, water absorption or swelling of excipients through various methods and the correlation between these parameters and tablet disintegration.

    Science.gov (United States)

    Yang, Baixue; Wei, Chen; Yang, Yang; Wang, Qifang; Li, Sanming

    2018-04-06

    To evaluate parameters about wettability, water absorption or swelling of excipients in forms of powders or dosage through various methods systematically and explore its correlation with tablet disintegration. The water penetration and swelling of powders with different proportions of excipients including microcrystalline cellulose (MCC), mannitol, low-substituted hydroxypropyl cellulose (L-HPC), crospolyvinylpyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na), croscarmellose sodium (CCMC-Na) and magnesium stearate (MgSt) were determined by Washburn capillary rise. Both contact angle of water on the excipient compacts and surface swelling volume were measured by sessile drop technique. Moreover, the test about water absorption and swelling of compacts was fulfilled by a modified method. Eventually, the disintegration of tablets with or without loratadine was performed according to the method described in USP. These parameters were successfully identified by the methods above, which proved that excipient wettability or swelling properties varied with the structure of excipients. For example, MgSt could improve the water uptake, while impeded tablet swelling. Furthermore, in the present study it is verified that tablet disintegration was closely related to these parameters, especially wetting rate and initial water absorption rate. The higher wetting rate of water on tablet or initial water absorption rate, the faster swelling it be, resulting in the shorter tablet disintegration time. The methods utilized in the present study were feasible and effective. The disintegration of tablets did relate to these parameters, especially wetting rate and initial water absorption rate.

  2. The efficacy of cladribine tablets in CIS patients retrospectively assigned the diagnosis of MS using modern criteria: Results from the ORACLE-MS study.

    Science.gov (United States)

    Freedman, Mark S; Leist, Thomas P; Comi, Giancarlo; Cree, Bruce Ac; Coyle, Patricia K; Hartung, Hans-Peter; Vermersch, Patrick; Damian, Doris; Dangond, Fernando

    2017-01-01

    Multiple sclerosis (MS) diagnostic criteria have changed since the ORACLE-MS study was conducted; 223 of 616 patients (36.2%) would have met the diagnosis of MS vs clinically isolated syndrome (CIS) using the newer criteria. The objective of this paper is to assess the effect of cladribine tablets in patients with a first clinical demyelinating attack fulfilling newer criteria (McDonald 2010) for MS vs CIS. A post hoc analysis for subgroups of patients retrospectively classified as fulfilling or not fulfilling newer criteria at the first clinical demyelinating attack was conducted. Cladribine tablets 3.5 mg/kg ( n  = 68) reduced the risk of next attack or three-month confirmed Expanded Disability Status Scale (EDSS) worsening by 74% vs placebo ( n  = 72); p  = 0.0009 in patients meeting newer criteria for MS at baseline. Cladribine tablets 5.25 mg/kg ( n  = 83) reduced the risk of next attack or three-month confirmed EDSS worsening by 37%, but nominal significance was not reached ( p  = 0.14). In patients who were still CIS after applying newer criteria, cladribine tablets 3.5 mg/kg ( n  = 138) reduced the risk of conversion to clinically definite multiple sclerosis (CDMS) by 63% vs placebo ( n  = 134); p  = 0.0003. Cladribine tablets 5.25 mg/kg ( n  = 121) reduced the risk of conversion by 75% vs placebo ( n  = 134); p  ORACLE-MS study (NCT00725985).

  3. Epitaxial growth of bcc-Fe{sub x}Co{sub 100-x} thin films on MgO(1 1 0) single-crystal substrates

    Energy Technology Data Exchange (ETDEWEB)

    Ohtake, Mitsuru, E-mail: ohtake@futamoto.elect.chuo-u.ac.j [Faculty of Science and Engineering, Chuo University, 1-13-27 Kasuga, Bunkyo-ku, Tokyo 112-8551 (Japan); Nishiyama, Tsutomu; Shikada, Kouhei [Faculty of Science and Engineering, Chuo University, 1-13-27 Kasuga, Bunkyo-ku, Tokyo 112-8551 (Japan); Kirino, Fumiyoshi [Graduate School of Fine Arts, Tokyo National University of Fine Arts and Music, 12-8 Ueno-koen, Taito-ku, Tokyo 110-8714 (Japan); Futamoto, Masaaki [Faculty of Science and Engineering, Chuo University, 1-13-27 Kasuga, Bunkyo-ku, Tokyo 112-8551 (Japan)

    2010-07-15

    Fe{sub x}Co{sub 100-x} (x=100, 65, 50 at%) epitaxial thin films were prepared on MgO(1 1 0) single-crystal substrates heated at 300 deg. C by ultra-high vacuum molecular beam epitaxy. The film structure and the growth mechanism are discussed. FeCo(2 1 1) films with bcc structure grow epitaxially on MgO(1 1 0) substrates with two types of variants whose orientations are rotated around the film normal by 180 deg. each other for all compositions. Fe{sub x}Co{sub 100-x} film growth follows the Volmer Weber mode. X-ray diffraction analysis indicates the out-of-plane and the in-plane lattice spacings are in agreement with the values of respective bulk Fe{sub x}Co{sub 100-x} crystals with very small errors less than +-0.4%, suggesting the strains in the films are very small. High-resolution cross-sectional transmission electron microscopy shows that periodical misfit dislocations are preferentially introduced in the film at the Fe{sub 50}Co{sub 50}/MgO interface along the MgO[1 1-bar 0] direction. The presence of such periodical dislocations decreases the large lattice mismatch of about -17% existing at the FeCo/MgO interface along the MgO[1 1-bar 0] direction.

  4. Uranium sandwich targets of 0.1 to 100 mg.cm-2 prepared by electron beam gun evaporation

    International Nuclear Information System (INIS)

    Folger, H.; Klemm, J.

    1978-01-01

    Metallic uranium layers of 0.1 to 100 mg.cm -2 between different backings and protecting layers were prepared for bombardments with heavy ions such as argon, krypton, xenon, lead, or uranium at energies of up to 8 MeV/u at the UNILAC of the GSI. An experimental set-up for the preparation of thick and oxygen-free sandwich targets using a 6 kVA electron beam gun was installed in a high vacuum apparatus. Then deposition and evaporation rates for uranium were investigated as a function of the electron beam gun power. It turned out that reproducible evaporation rates of up to 7 mg.s -1 were achieved when uranium pieces of 20 to 40 grams were used. Specific evaporation rates and vapor pressures for different temperatures were calculated. Some of these data are compared to measured values, especially evaporation rates at the evaporation point. The preparation, composition, and usage of uranium sandwich targets is described in detail. It concerns uranium layers of 0.1 to 100 mg.cm -2 deposited onto backings of carbon, titanium, nickel, gold, or glass. Evaporated films of carbon, titanium, nickel, or gold of 0.01 to 0.2 mg.cm -2 are used to protect the uranium layers from oxidation

  5. The efficacy and safety of clotrimazole vaginal tablet vs. oral fluconazole in treating severe vulvovaginal candidiasis.

    Science.gov (United States)

    Zhou, Xiaofang; Li, Ting; Fan, Shangrong; Zhu, Yuxia; Liu, Xiaoping; Guo, Xuedong; Liang, Yiheng

    2016-07-01

    To compare the efficacy and safety of two doses of clotrimazole vaginal tablet 500 mg with two doses of oral fluconazole 150 mg in treating severe vulvovaginal candidiasis (SVVC), 240 consecutive patients with SVVC were studied at the Department of Obstetrics and Gynaecology of Peking University Shenzhen Hospital between June 2014, and September 2015. Patients were randomly assigned in a 1 : 1 ratio to receive treatment with either two doses of clotrimazole vaginal tablet or two doses of oral fluconazole. The clinical cure rates in the clotrimazole group and the fluconazole group at days 7-14 follow-up were 88.7% (102/115) and 89.1% (98/110) respectively; the clinical cure rates at days 30-35 in the two groups were 71.9% (82/114) and 78.0% (85/109) respectively. The mycological cure rates at days 7-14 follow-up in the two groups were 78.3% (90/115) and 73.6% (81/110) respectively. The mycological cure rates of the patients at days 30-35 in the two groups were 54.4% (62/114) and 56.0% (61/109) respectively (P > 0.05). The adverse events of clotrimazole were mainly local. This study demonstrated that two doses of clotrimazole vaginal tablet 500 mg were as effective as two doses of oral fluconazole 150 mg in the treatment of patients with SVVC and could be an appropriate treatment for this disorder. © 2016 The Authors Mycoses Published by Blackwell Verlag GmbH.

  6. Three-way, three-period, crossover bioequivalence study of single oral dose of three brands of 300 mg phenytoin sodium tablets marketed in India, on healthy Indian human volunteers.

    Science.gov (United States)

    Doshi, Maulik S; Naik, Anuja A; Mehta, Mohit R; Gogtay, Nithya J; Thatte, Urmila M; Menon, Mala D

    2013-10-01

    To compare the bioavailability of two brands of phenytoin sodium tablets available in the Indian market using Eptoin™ as the reference. A randomized, assessor-blind, three-way crossover design study was carried out over a period of 6 months after approval from the Institutional Review Board (IRB). Twenty-two healthy male participants received a single oral 300 mg oral tablet of either of the formulations with a 2-week washout. Blood samples were collected predose and at regular intervals postdose. Plasma phenytoin levels were estimated by high-performance liquid chromatography. Calculation of Cmax, AUC0-t, and AUC0-∞ was done by the linear trapezoidal rule and 90-110% margin (90% confidence interval (CI)) was used to assess bioequivalence. Twenty volunteers completed the study. It was seen that the log-transformed values of Cmax, AUC0-t, and AUC0-∞ of the test formulations were not within the specified limits. Bioinequivalence of available phenytoin brands indicates that switching brands could lead to variations in blood concentrations and thus impact safety and efficacy. If a brand switch is done for any reason, stringent drug-level monitoring is advised.

  7. Theoretical aspects of methyl acetate and methanol activation on MgO(100) and (501) catalyst surfaces with application in FAME production

    Energy Technology Data Exchange (ETDEWEB)

    Man, Isabela-Costinela, E-mail: isabela.man@g.unibuc.ro [University of Bucharest, Faculty of Chemistry, Department of Organic Chemistry, Biochemistry and Catalysis, 4-12 Regina Elisabeta Av., S3, 030018 Bucharest (Romania); Romanian Academy, ‘C.D. Nenitzescu’ Center of Organic Chemistry, 202B Spl. Independentei, 060023 Bucharest (Romania); Soriga, Stefan Gabriel [University Politehnica of Bucharest, Centre for Technology Transfer in the Process Industries, 1, Gh. Polizu Street, Building A, Room A056, RO-011061 Bucharest (Romania); Parvulescu, Vasile [University of Bucharest, Faculty of Chemistry, Department of Organic Chemistry, Biochemistry and Catalysis, 4-12 Regina Elisabeta Av., S3, 030018 Bucharest (Romania)

    2017-01-15

    Highlights: • Energetics of C−O and C−H bond dissociation and formation of MeOAc on MgO(100) indicate that the bond formations are favorable. • Energetics of C−O and C−H bond dissociation and formation of MeOAc on MgO(501) indicate that the C−O bond dissociation and C−H bond formations are favorable. • The coadsorbed MeOH facilitate O−H bond dissociation of MeOH compared to isolated molecule. • Provide further understanding of reactivity of MgO surfaces with application in transesterification and interesterification reactions. - Abstract: Density functional theory (DFT) calculations were carried out to study the activation of methyl acetate and methanol on MgO(100) and MgO(501) surfaces and integrated in the context of transesterification, interesterification and glycerolysis reactions used in biodiesel industry. First results indicate the importance of including of dispersion forces in the calculations. On MgO(100) the reverse reactions steps of C−O and C−H dissociations and on MgO(501) the same reverse reaction step of C−H dissociations of methyl acetate are energetically favorable, while the dissociation of C−O bond into methoxide and acetate fragments on the edge of MgO(501) was found to be exothermic with a low activation energy. For methanol, the dissociation of O−H bond on MgO(100) surface in the presence of the second coadsorbed methanol molecule becomes more energetically favoured compared to the isolated molecule, due to the fact that the methoxide fragment is stabilized by intermolecular hydrogen bonding. This is reflected by the decrease of the activation energy of the forward reaction step and the increase of the activation energy of the backward reaction step, increasing the probability to have dissociated molecules among the undissociated ones. These results represent a step forward for better understanding from atomistic point of view the paths of these reactions on these surfaces for the corresponding catalytic

  8. Colon specific CODES based Piroxicam tablet for colon targeting: statistical optimization, in vivo roentgenography and stability assessment.

    Science.gov (United States)

    Singh, Amit Kumar; Pathak, Kamla

    2015-03-01

    This study was aimed to statistically optimize CODES™ based Piroxicam (PXM) tablet for colon targeting. A 3(2) full factorial design was used for preparation of core tablet that was subsequently coated to get CODES™ based tablet. The experimental design of core tablets comprised of two independent variables: amount of lactulose and PEG 6000, each at three different levels and the dependent variable was %CDR at 12 h. The core tablets were evaluated for pharmacopoeial and non-pharmacopoeial test and coated with optimized levels of Eudragit E100 followed by HPMC K15 and finally with Eudragit S100. The in vitro drug release study of F1-F9 was carried out by change over media method (0.1 N HCl buffer, pH 1.2, phosphate buffer, pH 7.4 and phosphate buffer, pH 6.8 with enzyme β-galactosidase 120 IU) to select optimized formulation F9 that was subjected to in vivo roentgenography. Roentgenography study corroborated the in vitro performance, thus providing the proof of concept. The experimental design was validated by extra check point formulation and Diffuse Reflectance Spectroscopy revealed absence of any interaction between drug and formulation excipients. The shelf life of F9 was deduced as 12 months. Conclusively, colon targeted CODES™ technology based PXM tablets were successfully optimized and its potential of colon targeting was validated by roentgenography.

  9. Métodos analíticos necesarios para el desarrollo de tabletas de metformina 500 mg Analytical methods needed for Metformin 500mg tablets development

    Directory of Open Access Journals (Sweden)

    Caridad M. García Peña

    2009-12-01

    cada uno de los casos en el intervalo de concentraciones establecido.Metformin hydrochloride is a biguanide-derivative used in non-dependent insulin diabetes mellitus reducing the blood glucose concentration without increases insulin secretion, and it is considered a anti-hyperglycemia agent and not a hypoglycemia one. Technological development requires of a reliable analytical methods allowing drug quantification in different stages of research. The aim of present paper was the analytical method validation, reported in USA Pharmacopeia (USP 31,2008 by UV-spectrophotometry and the adaptation of abovementioned method reported in the same pharmacopeia, for analysis of compound related in determination of active principle in end product, by high-performance liquid chromatography validated for quality control and study of Metformin (500-mg tablets stability. In validated techniques by chromatographic spectrophtometric methods we determined performance parameter, specificity, linearity, accuracy, and precision. Calibration curves for each method was performed in intervals of 60to 140%, where they were linear with correlation coefficients equal to 0.9994 and 0.99903, respectively. Statistical test for interceptor and slope was considered as non-significant. We achieved recoveries of 100.01 and 99.1, respectively during interval of study concentrations, and the Cochran (G and Student's (t tests were not significant. Variation coefficients in studies of repetition were equal to 1.4 and 0.8, respectively for the 6 assayed replica, whereas in average precision analysis, Fischer and Student tests were not significant. Results allow concluding that both methods fulfill the established requirements as acceptable for each of cases during the concentration interval established.

  10. 21 CFR 520.622a - Diethylcarbamazine citrate tablets.

    Science.gov (United States)

    2010-04-01

    ... Section 520.622a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES..., and 400 milligram tablets for prevention of heartworm disease in dogs and as an aid in the treatment of ascarid infections in dogs and cats. (2) See 053501 in § 510.600(c) of this chapter for use of 100...

  11. Development and evaluation of controlled-release buccoadhesive verapamil hydrochloride tablets

    Directory of Open Access Journals (Sweden)

    Emami J.

    2008-05-01

    Full Text Available Background and purpose of the study: Verapamil hydrochloride is a calcium channel blocker which is used in the control of supraventricular arrhythmia, hypertension and myocardial infraction. There are considerable inter-individual variations in serum concencentration of verpamil due to variation in the extent of hepatic metabolism. In this study controlled-release buccoadhesive tablets of verapamil hydrochloride (VPH were prepared in order to achieve constant plasma concentrations, to improve the bioavailability by the avoidance of hepatic first-pass metabolism, and to prevent frequent administration. Materials and methods: Tablets containing fixed amount of VPH were prepared by direct compression method using polymers like carbomer (CP, hydroxypropylmethyl cellulose (HPMC and sodium carboxymethyl cellulose (NaCMC in various combination and ratios and evaluated for thickness, weight variation, hardness, drug content uniformity, swelling, mucoadhesive strength, drug release and possible interaction between ingredients. Results: All tablets were acceptable with regard to thickness, weight variation, hardness, and drug content. The maximum bioadhesive strength was observed in tablets formulated with a combination of CP-NaCMC followed by CP-HPMC and NaCMC-HPMC.  Decreasing the content of CP in CP-HPMC tablets or NaCMC in CP-NaCMC or NaCMC-HPMC systems resulted in decrease in detachment forces. Lower release rates were observed by lowering the content of CP in CP-HPMC containing formulations or NaCMC in tablets which contained CP-NaCMC or NaCMC-HPMC. The release behavior was non-Fickian controlled by a combination of diffusion and chain relaxation mechanisms and best fitted zero-order kinetics. Conclusion: The buccoadhesive VPH tablets containing 53% CP and 13.3% HPMC showed suitable release kinetics (n = 0.78, K0 zero order release = 4.11 mg/h, MDT = 5.66 h and adhesive properties and did not show any interaction between polymers and drug based on

  12. Prediction of effects of punch shapes on tableting failure by using a multi-functional single-punch tablet press

    Directory of Open Access Journals (Sweden)

    Takashi Osamura

    2017-09-01

    Full Text Available We previously determined “Tableting properties” by using a multi-functional single-punch tablet press (GTP-1. We proposed plotting “Compactability” on the x-axis against “Manufacturability” on the y-axis to allow visual evaluation of “Tableting properties”. Various types of tableting failure occur in commercial drug production and are influenced by the amount of lubricant used and the shape of the punch. We used the GTP-1 to measure “Tableting properties” with different amounts of lubricant and compared the results with those of tableting on a commercial rotary tableting machine. Tablets compressed with a small amount of lubricant showed bad “Manufacturability”, leading to sticking of powder on punches. We also tested various punch shapes. The GTP-1 correctly predicted the actual tableting results for all punch shapes. With punches that were more likely to cause tableting failure, our system predicted the effects of lubricant quantity in the tablet formulation and the occurrence of sticking in the rotary tableting machine.

  13. Analytical method validation for quality control and the study of the 50 mg Propylthiouracil stability

    International Nuclear Information System (INIS)

    Valdes Bendoyro, Maria Olga; Garcia Penna, Caridad Margarita; Fernandez, Juan Lugones; Garcia Borges, Lisandra; Martinez Espinosa, Vivian

    2010-01-01

    A high-performance liquid chromatography analytical method was developed and validated for the quality control and stability studies of 50 mg Propylthiouracil tablets. Method is based in active principle separation through a 100 RP-18 RP-18 (5 μm) (250 x 4 mm) Lichrospher chromatography with UV detection to 272 nm, using a mobile phase composed by a ungaseous mixture of a 0.025 M buffer solution-monobasic potassium phosphate to pH= 4,6 ad acetonitrile in a 80:20 ratio with a flux speed of 0,5 mL/min. Analytical method was linear, precise, specific and exact in the study concentrations interval

  14. Physicochemical properties of direct compression tablets with spray dried and ball milled solid dispersions of tadalafil in PVP-VA.

    Science.gov (United States)

    Wlodarski, K; Tajber, L; Sawicki, W

    2016-12-01

    The aim of this research was to develop immediate release tablets comprising solid dispersion (IRSDTs) of tadalafil (Td) in a vinylpyrrolidone and vinyl acetate block copolymer (PVP-VA), characterized by improved dissolution profiles. The solid dispersion of Td in PVP-VA (Td/PVP-VA) in a weight ratio of 1:1 (w/w) was prepared using two different processes i.e. spray drying and ball milling. While the former process has been well established in the formulation of IRSDTs the latter has not been exploited in these systems yet. Regardless of the preparation method, both Td/PVP-VA solid dispersions were amorphous as confirmed by PXRD, DSC and FTIR. However, different morphology of particles (SEM) resulted in differences in water apparent solubility and disk intrinsic dissolution rate (DIDR). Both solid dispersions and crystalline Td were successfully made into directly compressible tablets at three doses of Td, i.e. 2.5mg, 10mgand20mg, yielding nine different formulations (D 1 -D 9 ). Each of the lots met the requirements set by Ph.Eur. and was evaluated with respect to appearance, diameter, thickness, mass, hardness, friability, disintegration time and content of Td. IRSDTs performed as supersaturable formulations and had significantly improved water dissolution profiles in comparison with equivalent tablets containing crystalline Td and the marketed formulations. Tablets with both spray dried and ball milled Td/PVP-VA revealed the greatest improvement in dissolution depending on the investigated doses, i.e. 2.5mgand20mg, respectively. Also, dissolution of Td from Td/PVP-VA delivered in different forms occurred in the following order: powders>tablets>capsules. Copyright © 2016 Elsevier B.V. All rights reserved.

  15. Safety and pharmacokinetic profile of fixed-dose ivermectin with an innovative 18mg tablet in healthy adult volunteers.

    Directory of Open Access Journals (Sweden)

    Jose Muñoz

    2018-01-01

    Full Text Available Ivermectin is a pivotal drug for the control of onchocerciasis and lymphatic filariasis, which is increasingly identified as a useful drug for the control of other Neglected Tropical Diseases. Its role in the treatment of soil transmitted helminthiasis through improved efficacy against Trichuris trichiura in combination with other anthelmintics might accelerate the progress towards breaking transmission. Ivermectin is a derivative of Avermectin B1, and consists of an 80:20 mixture of the equipotent homologous 22,23 dehydro B1a and B1b. Pharmacokinetic characteristics and safety profile of ivermectin allow to explore innovative uses to further expand its utilization through mass drug administration campaigns to improve coverage rates. We conducted a phase I clinical trial with 54 healthy adult volunteers who sequentially received 2 experimental treatments using a new 18 mg ivermectin tablet in a fixed-dose strategy of 18 and 36 mg single dose regimens, compared to the standard, weight based 150–200 μg/kg, regimen. Volunteers were recruited in 3 groups based on body weight. Plasma concentrations of ivermectin were measured through HPLC up to 168 hours post treatment. Safety data showed no significant differences between groups and no serious adverse events: headache was the most frequent adverse event in all treatment groups, none of them severe. Pharmacokinetic parameters showed a half-life between 81 and 91 h in the different treatment groups. When comparing the systemic bioavailability (AUC0t and Cmax of the reference product (WA-ref with the other two study groups using fixed doses, we observed an overall increase in AUC0t and Cmax for the two experimental treatments of 18 mg and 36 mg. Body mass index (BMI and weight were associated with t1/2 and V/F, probably reflecting the high liposolubility of IVM with longer retention times proportional to the presence of more adipose tissue. Systemic exposure to ivermectin (AUC0t or Cmax was not

  16. Effect of desvenlafaxine 50 mg and 100 mg on energy and lassitude in patients with major depressive disorder: A pooled analysis.

    Science.gov (United States)

    Lam, Raymond W; Wajsbrot, Dalia B; Meier, Ellen; Pappadopulos, Elizabeth; Mackell, Joan A; Boucher, Matthieu

    2017-09-01

    Nine randomized, double-blind, placebo-controlled studies of major depressive disorder were pooled to evaluate the effects of desvenlafaxine 50- and 100-mg/d on energy and lassitude in adults with major depressive disorder ( n=4279). Changes from baseline to endpoint in 17-item Hamilton Rating Scale for Depression (HAM-D 17 ) Work and Activities, Retardation, and Somatic Symptoms General items, HAM-D 17 psychomotor retardation factor, and Montgomery-Åsberg Depression Rating Scale Lassitude item were analyzed with a mixed model for repeated measures analysis of variance. Associations between residual energy measures and functional impairment, based on the Sheehan Disability Scale, were modeled using stepwise multiple linear regression. Improvement from baseline was significantly greater for both desvenlafaxine doses versus placebo on all energy symptom outcomes at week 8 (all p⩽0.005). Both early improvement in HAM-D 17 psychomotor retardation at week 2 and residual energy symptoms at week 8 were associated with Sheehan Disability Scale total score at week 8 (all p⩽0.001). Among Sheehan Disability Scale remitters and responders, the HAM-D 17 psychomotor retardation score at week 8 was significantly lower with desvenlafaxine (both doses) than placebo. Desvenlafaxine 50 and 100 mg/d significantly improved energy and lassitude symptoms in patients with major depressive disorder. Both early improvement in energy and fewer residual energy symptoms were associated with functional improvement.

  17. Dissolution Behavior and Content Uniformity of An Improved Tablet Formulation Assayed by Spectrofluorometric and RIA Methods

    Directory of Open Access Journals (Sweden)

    Morteza Rafiee-Tehrani

    1990-06-01

    Full Text Available Digoxin 0.25 mg tablets were manufactured by pregranulation of lactose-fcorn starch with 10% corn starch paste and deposition of solvent on pregranules to make digoxin granules. In the preparation of tablet A, granules of lactose-corn Starch was uniformly moistened with a 5% chloroform-ethanol solution (2:lv/vof digoxin by a simple blending. Tablet B was produced by spray granulation system on which the solvent was sprayed on the granules of lactose-corn starch by utilization of a laboratory size fluidized bed drier (Uniglatt . The content uniformity and dissolution of both tablets were determined by the spectrofluorometric and radio¬immunoassay (RIA method modified for the assay of tablet solutious. One available commercially brand of digoxin tablet (C was included in dissolution study for comparison. For the spectrofluorometric method the technique is based on the fluor-ometric measurenent of the dehydration product of the cardiotonic steroid resulting from its reaction with hydrogen peroxide in concentrated hydrochloric acid. For the RIA method, the filtrate was diluted to theoretical concentration of 2.5 ng/ml."nAliquots of this dilution were then assayed for digoxin content using a commercial digoxin125 I RIA kit. Results from both assay methods were extrapolated to the total tablet content and compared with the labeled amount of 20 individual tablets. All tablet assay results were within the USP standards for the content uniformity and"ndissolution of individual. The individual tablet deviations from labeled amount by RIA method were smaller when compared with the spectrofluorometric method.There was no significant difference between the release of digoxin from three products, and thus it is suggested that the Procedure B could be easily applied for manufacturing"nof digoxin tablets in industrial scales.It was also concluded that,the RIA method could be used for the digoxin tablet determination.

  18. Evaluation of the ease of taking mini-tablets compared with other tablet formulations in healthy volunteers.

    Science.gov (United States)

    Hayakawa, Yoshiyuki; Uchida, Shinya; Namiki, Noriyuki

    2016-03-10

    "Mini-tablets" (MTs) are tablets of diameter≤3mm and have been widely studied and developed. However, reports comparing MTs with other tablet formulations are few. We wished to evaluate the ease of taking a MT quantitatively in comparison with an orally disintegrating mini-tablet (ODMT), conventional tablet (CT) and conventional orally disintegrating tablet (ODT). Four types of tablets were prepared. We prepared tablets of two diameters (3mm for MTs and ODMTs vs. 8mm for CTs and ODTs) and two formulations (MTs and CTs vs. ODMTs and ODTs). Our randomized crossover trial in 18 healthy volunteers (8 men and 10 women; mean age, 22.5years) indicated that the visual analog scale (VAS) score for the ease and amount of water required for intake of MTs was significantly lower than those of CTs. An ODMT required the least amount of water and smallest VAS score for the ease of taking a tablet. Our results showed that the advantage of MTs with regard to the ease of taking and decreased amount of water required was exerted for a unit of dosing comprising tablets. These data suggested the usefulness of MTs and the importance of the number of MTs for comfortable consumption by patients. Copyright © 2015. Published by Elsevier B.V.

  19. QUALITY CONTROL OF HYDROCHLOROTHIAZIDE TABLETS MARKETED IN SINOP-MT

    Directory of Open Access Journals (Sweden)

    M. K. Órfão

    2017-10-01

    Full Text Available The thiazide diuretics are of the classes of drugs most frequently used for the treatment of hypertension. Hydrochlorothiazide is the representative of this class and is found in tablet form in doses of 25 and 50 mg. It is marketed in three different categories of drugs: reference, similar and generic. According to the regulator in Brazil, the National Health Surveillance Agency (ANVISA, before pharmaceuticals are released for use, the pharmaceutical industry must meet product quality specifications, but the consumption of counterfeit drugs, contraband or without registration with government laws It is growing in Brazil, which affect the entire drug production chain affecting the health of those who use these medicines. In view of the reported problems about the quality of marketed drugs and being the state of Mato Grosso considered a fake gateway drug, due to its proximity to Bolivia, this study aimed to assess the quality of tablets containing hydrochlorothiazide is already one of the most widely used drugs in the treatment of hypertension in Sinop-MT municipality according local search. Samples from five laboratories that produce hydrochlorothiazide tablets at a dose of 25 mg, and the most market in the municipality of Sinop / MT were analyzed as stablished in the Brazilian Pharmacopoeia. It was found that four of the five samples of drugs in Mato Grosso, performed all the requirements for approval in quality testing, with the exception of a product that has lower hardness values than recommended, which can lead to problems drug presentation as well as directly affect the absorption, bioavailability and action of the therapeutic drug. It was concluded that medicinal products containing hydrochlorothiazide showed adequate quality, ensuring their effectiveness.

  20. Preparation of Porous Hydroxyapatite Tablets and Porous Hydroxyapatite Coatings for Orthopaedic Use

    International Nuclear Information System (INIS)

    Mendez-Gonzalez, M.

    2004-01-01

    Porous hydroxyapatite tablets and coatings on metal substrates were obtained by the addition of polymeric additives and liofilization. Both tablets and coatings were characterized by scanning electron microscopy and x-ray diffraction. Coatings obtained by plasma spraying also exhibited interconnected porous of 100 μm while coatings obtained by laser ablation did not show any porosity. The diffraction patterns of the deposited HA were similar to that of the powder obtained by the precipitation method suggesting that no significant changes occurred during the coating procedure

  1. THE CHOICE OF NITRATE THERAPY IN PATIENTS WITH STABLE ANGINA: COMPARATIVE STUDY OF ISOSORBIDE DINITRATE (IN USUAL TABLETS WITH ISOSORBIDE-5-MONONITRATE (IN VARIOUS PRESENTATIONS

    Directory of Open Access Journals (Sweden)

    V. A. Egoro

    2008-01-01

    Full Text Available Aim. To study efficacy and tolerability of isosorbide-5-mononitrate (IMN in various presentations in comparison with isosorbide dinitrate (IDN in usual tablets in patients with stable angina.Material and Methods. 22 patients (5 women and 17 men with stable angina of II-III functional class were involved into open randomized comparative crossover study. Patients were split in 3 groups and received each of studied drugs during 4 weeks. IDN (Nitrosorbide, Nizpharm, Russia in usual tablets 10 mg prescribed for 3 times a day administration; IMN (Monocinque,Berlin-Chemie, German in tablets 20 mg prescribed for 2 times a day administration. After 1 week therapy the doses of IDN or IMN doubled if it was clinically necessary. Retarded presentation of IMN (Monocinque Retard, Berlin-Chemie, German in capsules 50 mg prescribed once daily. Drug efficacy was evaluated by changes in clinical symptoms, number of angina attacks, demand in short-acting sublingual nitroglycerin as well as physical activity tolerance.Results. After 4 weeks 18 patients completed study, 2 patients dropped out because of protocol nonobservance and 2 patients dropped out because of side effects (headache. IDN therapy in adjusted dose provided antianginal effect in 15 (83,3% patients: a number of angina attacks decreased in 39,6%, short-acting nitroglycerin demand reduced in 47,7%. Monocinque in adjusted dose provided antianginal effect in 16 (88,9% patients: a number of angina attacks decreased in 60%, short-acting nitroglycerin demand reduced in 63%. Monocinque Retard provided good antianginal effect in 18 (100% patients: a number of angina attacks decreased in 72%, short-acting nitroglycerin demand reduced in 84,8%. There were not significant differences in frequency and severity of headache between studied drugs.Conclusion. IMN therapy with both presentations (administrated 1 or 2 times a day was more convenient and effective than IDN (administrated 3 times a day.

  2. Comparison of weekly administration of cisplatin versus three courses of cisplatin 100 mg/m2 for definitive radiochemotherapy of locally advanced head-and-neck cancers

    International Nuclear Information System (INIS)

    Rades, Dirk; Seidl, Daniel; Janssen, Stefan; Bajrovic, Amira; Karner, Katarina; Strojan, Primoz; Schild, Steven E

    2016-01-01

    To compare definitive radiochemotherapy with weekly administration of 30–40 mg/m 2 of cisplatin to 100 mg/m 2 of cisplatin on days 1, 22 and 43 for outcomes and toxicity in patients with squamous cell carcinoma of the head-and-neck. Seventy-five patients receiving radiochemotherapy with weekly cisplatin (30–40 mg/m 2 ) were compared to 58 patients receiving radiochemotherapy with 100 mg/m 2 cisplatin on days 1, 22 and 43. Radiochemotherapy regimen plus seven characteristics (age, gender, performance score, tumor site, T-/N-category, histologic grading) were evaluated for locoregional control (LRC), metastases-free survival (MFS) and overall survival (OS). Radiochemotherapy groups were compared for toxicity. On multivariate analysis, improved LRC was associated with cisplatin 100 mg/m 2 (hazard ratio [HR] 1.57; p = 0.008) and female gender (HR 4.37; p = 0.003). Radiochemotherapy regimen was not significantly associated with MFS on univariate analysis (p = 0.66). On multivariate analysis, better MFS was associated with ECOG performance score 0–1 (HR 5.63; p < 0.001) and histological grade 1–2 (HR 1.81; p = 0.002). On multivariate analysis, improved OS was associated with cisplatin 100 mg/m 2 (HR 1.33; p = 0.023), ECOG performance score 0–1 (HR 2.15; p = 0.029) and female gender (HR 1.98; p = 0.026). Cisplatin 100 mg/m 2 was associated with higher rates of grade ≥3 hematotoxicity (p = 0.004), grade ≥2 renal failure (p = 0.004) and pneumonia/sepsis (p = 0.033). Radiochemotherapy with 100 mg/m 2 of cisplatin every 3 weeks resulted in better LRC and OS than weekly doses of 30–40 mg/m 2 . Given the limitations of a retrospective study, 100 mg/m 2 of cisplatin appears preferable. Since this regimen was associated with considerable acute toxicity, patients require close monitoring

  3. Influence of disintegrants in different substrate physical form on dimensional recovery of multi-component tablet.

    Science.gov (United States)

    Sarkar, Srimanta; Ooi, Shing Ming; Liew, Celine Valeria; Tan, Bing Xun; Heng, Paul Wan Sia

    2014-11-20

    This study investigated the influence of different disintegrants, present in different substrate physical forms, on dimensional recovery of multi-component tablets prepared at different compression pressures. Formulations containing model drug, metformin, (10%, w/w), different disintegrants (10%, w/w), and lactose (80%, w/w) were compressed directly or after granulation using polyvinyl pyrrolidone (1%, w/w) as binder, into tablets (350 mg, 10mm diameter) at 150, 200, and 250 N/mm(2) compression pressures. Tablets were characterized for immediate dimensional recovery (IR) after ejection from the die, latent dimensional recovery (LR) over 24 h, tensile strength, and disintegration. The IR was predominantly contributed by crystalline components whereas LR was brought about by polymeric materials. With increased compression pressure, higher degree of plastic deformation of the polymeric disintegrants resulted in tablet with lower LR and higher tensile strength. Presence of polyvinyl pyrrolidone in the granules contributed considerably to plastic deformation, and the tablets produced had lower LR, higher tensile strength, and longer disintegration time. This study indicated that use of granules as the feed substrate physical form and a prudent selection of components may enable the coating of resultant tablets immediately after compression without the risk of coat damage due to LR. Copyright © 2014 Elsevier B.V. All rights reserved.

  4. Quality assessment of pharmaceutical tablet samples using Fourier transform near infrared spectroscopy and multivariate analysis

    Science.gov (United States)

    Kandpal, Lalit Mohan; Tewari, Jagdish; Gopinathan, Nishanth; Stolee, Jessica; Strong, Rick; Boulas, Pierre; Cho, Byoung-Kwan

    2017-09-01

    Determination of the content uniformity, assessed by the amount of an active pharmaceutical ingredient (API), and hardness of pharmaceutical materials is important for achieving a high-quality formulation and to ensure the intended therapeutic effects of the end-product. In this work, Fourier transform near infrared (FT-NIR) spectroscopy was used to determine the content uniformity and hardness of a pharmaceutical mini-tablet and standard tablet samples. Tablet samples were scanned using an FT-NIR instrument and tablet spectra were collected at wavelengths of 1000-2500 nm. Furthermore, multivariate analysis was applied to extract the relationship between the FT-NIR spectra and the measured parameters. The results of FT-NIR spectroscopy for API and hardness prediction were as precise as the reference high-performance liquid chromatography and mechanical hardness tests. For the prediction of mini-tablet API content, the highest coefficient of determination for the prediction (R2p) was found to be 0.99 with a standard error of prediction (SEP) of 0.72 mg. Moreover, the standard tablet hardness measurement had a R2p value of 0.91 with an SEP of 0.25 kg. These results suggest that FT-NIR spectroscopy is an alternative and accurate nondestructive measurement tool for the detection of the chemical and physical properties of pharmaceutical samples.

  5. Polar catastrophe at the MgO(100)/SnO2(110) interface

    KAUST Repository

    Albar, Arwa

    2016-11-14

    First principles calculations, based on density functional theory, are used to investigate the structural and electronic properties of the epitaxial MgO(100)/SnO2(110) interface of wide band gap insulators. Depending on the interface termination, nonmagnetic metallic and half-metallic interface states are observed. The formation of these states is explained by a polar catastrophe model for nonpolar-polar interfaces. Strong lattice distortions and buckling develop in SnO2, which influence the interface properties as the charge discontinuity is partially screened. Already a single unit cell of SnO2 is sufficient to drive the polar catastrophe scenario. © 2016 The Royal Society of Chemistry.

  6. Skew scattering dominated anomalous Hall effect in Cox(MgO)100-x granular thin films

    KAUST Repository

    Zhang, Qiang

    2017-07-31

    We investigated the mechanism(s) of the anomalous Hall effect (AHE) in magnetic granular materials by fabricating 100-nm-thick thin films of Cox(MgO)100-x with a Co volume fraction of 34≤x100 using co-sputtering at room temperature. We measured the temperature dependence of longitudinal resistivity (ρxx) and anomalous Hall resistivity (ρAHE) from 5 K to 300 K in all samples. We found that when x decreases from 100 to 34, the values of ρxx and ρAHE respectively increased by about four and three orders in magnitude. By linearly fitting the data, obtained at 5 K, of anomalous Hall coefficient (Rs) and of ρxx to log(Rs)~γlog(ρxx), we found that our results perfectly fell on a straight line with a slope of γ= 0.97±0.02. This fitting value of γ in Rsρxxγ clearly suggests that skew scattering dominated the AHE in this granular system. To explore the effect of the scattering on the AHE, we performed the same measurements on annealed samples. We found that although both ρxx and ρAHE significantly reduced after annealing, the correlation between them was almost the same, which was confirmed by the fitted value, γ=0.99±0.03. These data strongly suggest that the AHE originates from the skew scattering in Co-MgO granular thin films no matter how strong the scatterings of electrons by the interfaces and defects is. This observation may be of importance to the development of spintronic devices based on MgO.

  7. How do tablet properties influence swallowing behaviours?

    Science.gov (United States)

    Yamamoto, Shinya; Taniguchi, Hiroshige; Hayashi, Hirokazu; Hori, Kazuhiro; Tsujimura, Takanori; Nakamura, Yuki; Sato, Hideaki; Inoue, Makoto

    2014-01-01

    Behavioural performance of tablet swallowing was evaluated with different tablet conditions in terms of size, number and surface coating. Four different types of tablets were prepared: small or large, and with or without a surface coating. Fourteen normal male adults were instructed to swallow the prepared tablets with 15 ml of water. The number of tablets in one trial was changed from one to three. To evaluate swallowing and tablet transport, electromyographic activity was recorded in the left suprahyoid muscles, and videofluorographic images were examined. All tablet conditions (size, number and surface coating) affected the swallowing performance in terms of total number of swallows, electromyographic burst patterns and location of remaining tablets. Increases in the size and number of tablets increased the number of swallows and electromyographic burst area and duration. In addition, all of these parameters increased while swallowing tablets without a coating compared with tablets with a coating. Location of the remaining tablets was mainly within the mouth. This study only clarified the normal pattern of tablet swallowing under several conditions in healthy subjects, but the results may facilitate comprehensive evaluation and treatment planning in terms of administering medication to dysphagic patients. © 2013 Royal Pharmaceutical Society.

  8. Effect of repeated compaction of tablets on tablet properties and work of compaction using an instrumented laboratory tablet press.

    Science.gov (United States)

    Gamlen, Michael John Desmond; Martini, Luigi G; Al Obaidy, Kais G

    2015-01-01

    The repeated compaction of Avicel PH101, dicalcium phosphate dihydrate (DCP) powder, 50:50 DCP/Avicel PH101 and Starch 1500 was studied using an instrumented laboratory tablet press which measures upper punch force, punch displacement and ejection force and operates using a V-shaped compression profile. The measurement of work compaction was demonstrated, and the test materials were ranked in order of compaction behaviour Avicel PH101 > DCP/Avicel PH101 > Starch > DCP. The behaviour of the DCP/Avicel PH101 mixture was distinctly non-linear compared with the pure components. Repeated compaction and precompression had no effect on the tensile fracture strength of Avicel PH101 tablets, although small effects on friability and disintegration time were seen. Repeated compaction and precompression reduced the tensile strength and the increased disintegration time of the DCP tablets, but improved the strength and friability of Starch 1500 tablets. Based on the data reported, routine laboratory measurement of tablet work of compaction may have potential as a critical quality attribute of a powder blend for compression. The instrumented press was suitable for student use with minimal supervisor input.

  9. Eudragit E100 and Polysaccharide Polymer Blends as Matrices for ...

    African Journals Online (AJOL)

    Purpose: To compare the effects of two states of polymer/polymer blending (dry and aqueous/lyophilized) on the physicomechanical properties of tablets, containing blends of locust bean gum (LB) with Eudragit® E100 (E100) and sodium carboxymethylcellulose (SCMC) as matrices. Methods: LB, SCMC and E100 were ...

  10. Teach yourself visually Fire tablets

    CERN Document Server

    Marmel, Elaine

    2014-01-01

    Expert visual guidance to getting the most out of your Fire tablet Teach Yourself VISUALLY Fire Tablets is the comprehensive guide to getting the most out of your new Fire tablet. Learn to find and read new bestsellers through the Kindle app, browse the app store to find top games, surf the web, send e-mail, shop online, and much more! With expert guidance laid out in a highly visual style, this book is perfect for those new to the Fire tablet, providing all the information you need to get the most out of your device. Abundant screenshots of the Fire tablet graphically rich, touch-based Androi

  11. Comparative evaluation of some commercially available brands of rifampacin tablets

    International Nuclear Information System (INIS)

    Shah, S.N.; Mahmood, K.; Uzair, M.; Rabbani, M.

    2009-01-01

    The objective of this study was to evaluate some commercially available brands of Rifampacin Tablets. In in- vitro release studies of physical parameters of tablet i.e. disintegration, dissolution rate, crushing strength, thickness and diameter, uniformity of weight and assay of the active ingredients of four brands of commercially available Rifampacin tablet i.e. A, B, C and D were performed. For this purpose, Dissolution rate was studied in phosphate buffer at pH 6.0, 6.5 and 7.4 using USP rotating basket at 100 rpm. The data was analyzed by Cube-Root law and calculated dissolution rate constant predicting in vitro behavior of the drug released from these preparations. In this particular case two types of dissolution mechanisms were founded; in first 20 minutes, the fast release phase and after 20 minutes the slow release phase. According to the degree of dissolution of D and B proved to be the best of the available commercial brands. (author)

  12. Modulation of the wettability of excipients by surfactant and its impacts on the disintegration and release of tablets.

    Science.gov (United States)

    Yang, Baixue; Xu, Lu; Wang, Qiuxiao; Li, Sanming

    2016-12-01

    To investigate the modulation of the wettability of excipients by different types of surfactants and its impacts on the disintegration of tablets and drug release. The critical micelle concentration (CMC) of surfactants, including sodium dodecyl sulfate (SDS), sodium dodecyl benzene sulfonate (SDBS), dodecyl trimethyl ammonium bromide (DTAB), cetyltrimethyl ammonium bromide (CTAB) and polysorbate (Tween-20 and Tween-80), was obtained using the platinum ring method. Contact angles of surfactant solutions on the excipient compacts and double-distilled water on the mixture of surfactant and the other excipient (magnesium stearate (MgSt) or sodium alginate (SA)) were measured by the sessile drop technique. Besides, surface free energy of excipients was calculated by the Owens method. Finally, the disintegration of tablets and in vitro dissolution testing were performed according to the method described in USP. The wettability of excipients could be enhanced to different extent with low concentration of surfactant solutions and maintained stable basically after CMC. For MgSt (hydrophobic excipient), the shorter the hydrophobic chain (C 12 , including SDS and DTAB), the better the wettability with the addition of surfactant in the formulation, leading to the shorter disintegration time of tablets and higher drug release rate. In contrast, the wettability of SA (hydrophilic excipient) was reduced by adding surfactant, resulting in the longer disintegration time of tablets and lower release rate. The modulation of the wetting of pharmaceutical excipients by surfactant had changed the disintegration time of tablets and drug release rate to a greater extent.

  13. 100 mg 251Cf activation analysis facility at the Savannah River Laboratory

    International Nuclear Information System (INIS)

    MacMurdo, K.W.; Bowman, W.W.

    1975-01-01

    The 252 Cf Activation Analysis Facility at the Savannah River Laboratory (SRL) is used routinely for multielement analyses of a wide variety of solid and liquid samples (e.g., metal alloys, fly ash and other airborne particles, rocks, and aqueous and nonaqueous solutions). An automated absolute activation analysis technique, developed to use neutron transport codes to calculate multienergy group neutron spectra and fluxes, converts counting data directly into elemental concentrations expressed in parts per million. The facility contains four sources of 252 Cf totaling slightly over 100 mg. A pneumatic ''rabbit'' system permits automatic irradiation/decay/counting regimes to be performed unattended on up to 100 samples. Detection sensitivities of less than or equal to 400 ppb natural uranium and less than or equal to 0.5 nCi/g for 239 Pu are observed. Detection limits for over 65 elements have been determined. Over 40 elements are detectable at the one part per million level or less. Overall accuracies of +- 10 percent are observed for most elements. (auth)

  14. A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets.

    Science.gov (United States)

    Vemula, Sateesh Kumar

    2015-12-01

    A significant plan is executed in the present study to study the effect of double-compression coating on flurbiprofen core mini-tablets to achieve the pulsatile colonic delivery to deliver the drug at a specific time as per the patho-physiological need of the disease that results in improved therapeutic efficacy. In this study, pulsatile double-compression-coated tablets were prepared based on time-controlled hydroxypropyl methylcellulose K100M inner compression coat and pH-sensitive Eudragit S100 outer compression coat. Then, the tablets were evaluated for both physical evaluation and drug-release studies, and to prove these results, in vivo pharmacokinetic studies in human volunteers were conducted. From the in vitro drug-release studies, F6 tablets were considered as the best formulation, which retarded the drug release in the stomach and small intestine (3.42 ± 0.12% in 5 h) and progressively released to the colon (99.78 ± 0.74% in 24 h). The release process followed zero-order release kinetics, and from the stability studies, similarity factor between dissolution data before and after storage was found to be 88.86. From the pharmacokinetic evaluation, core mini-tablets producing peak plasma concentration (C max) was 14,677.51 ± 12.16 ng/ml at 3 h T max and pulsatile colonic tablets showed C max = 12,374.67 ± 16.72 ng/ml at 12 h T max. The area under the curve for the mini and pulsatile tablets was 41,238.52 and 72,369.24 ng-h/ml, and the mean resident time was 3.43 and 10.61 h, respectively. In conclusion, development of double-compression-coated tablets is a promising way to achieve the pulsatile colonic release of flurbiprofen.

  15. Environmental dosimetry system based on LiF : Mg, Ti (TLD-100)

    International Nuclear Information System (INIS)

    Saez Vergara, J.C.

    1990-01-01

    The report presents the various tests carried out to the characterize a thermoluminescence environmental dosimetry systems, using the phosphor LiF:mg,Ti (TLD-100) in chip form. The holder has been specifically designed in order to obtain simplicity in the operation and to assure correct measurements in terms of the new operational quantities in radiation protection (ICRU-1985). Some topics in TLD Environmental Monitoring are discussed (Dark Current, Reference Light, Zero Reading, Free-in-Air or Phantom Calibration, Fading Correction, Transit Dose, etc.), and the proposed solutions are exposed. The tests performed have been designed to conform with the different existing international Standards and Recommendations (ANSI : N545-1975; IEC: Draft 45B-1987, ISO : DP 8034-19849. The data from an European Interlaboratory Programm (EUR-8932) have been used to evaluate the performance : the TLD System presented is among the best systems using TLD-100. The results obtained in the characterization (linearity, repeatability, detection threshold, residue, angular response, stability of stored information, etc.) show the optimum performance of this dosimetric system in its application to environmental gamma dose monitoring. Based on these results, two operational procedures have been developed for the application of this Dosimetric System, specially in Quality Assurance Monitoring Programs around Nuclear Plants in Spain. (author)

  16. The Milky Way: paediatric milk-based dispersible tablets prepared by direct compression - a proof-of-concept study.

    Science.gov (United States)

    Orubu, Samuel E F; Hobson, Nicholas J; Basit, Abdul W; Tuleu, Catherine

    2017-04-01

    Dispersible tablets are proposed by the World Health Organization as the preferred paediatric formulation. It was hypothesised that tablets made from a powdered milk-base that disperse in water to form suspensions resembling milk might be a useful platform to improve acceptability in children. Milk-based dispersible tablets containing various types of powdered milk and infant formulae were formulated. The influence of milk type and content on placebo tablet properties was investigated using a design-of-experiments approach. Responses measured included friability, crushing strength and disintegration time. Additionally, the influence of compression force on the tablet properties of a model formulation was studied by compaction simulation. Disintegration times increased as milk content increased. Compaction simulation studies showed that compression force influenced disintegration time. These results suggest that the milk content, rather than type, and compression force were the most important determinants of disintegration. Up to 30% milk could be incorporated to produce 200 mg 10-mm flat-faced placebo tablets by direct compression disintegrating within 3 min in 5-10 ml of water, which is a realistic administration volume in children. The platform could accommodate 30% of a model active pharmaceutical ingredient (caffeine citrate). © 2016 Royal Pharmaceutical Society.

  17. The effect of Vaccinium uliginosum extract on tablet computer-induced asthenopia: randomized placebo-controlled study.

    Science.gov (United States)

    Park, Choul Yong; Gu, Namyi; Lim, Chi-Yeon; Oh, Jong-Hyun; Chang, Minwook; Kim, Martha; Rhee, Moo-Yong

    2016-08-18

    To investigate the alleviation effect of Vaccinium uliginosum extract (DA9301) on tablet computer-induced asthenopia. This was a randomized, placebo-controlled, double-blind and parallel study (Trial registration number: 2013-95). A total 60 volunteers were randomized into DA9301 (n = 30) and control (n = 30) groups. The DA9301 group received DA9301 oral pill (1000 mg/day) for 4 weeks and the control group received placebo. Asthenopia was evaluated by administering a questionnaire containing 10 questions (responses were scored on a scales of 0-6; total score: 60) regarding ocular symptoms before (baseline) and 4 weeks after receiving pills (DA9301 or placebo). The participants completed the questionnaire before and after tablet computer (iPad Air, Apple Inc.) watching at each visit. The change in total asthenopia score (TAS) was calculated and compared between the groups TAS increased significantly after tablet computer watching at baseline in DA9301 group. (from 20.35 to 23.88; p = 0.031) However, after receiving DA9301 for 4 weeks, TAS remained stable after tablet computer watching. In the control group, TAS changes induced by tablet computer watching were not significant both at baseline and at 4 weeks after receiving placebo. Further analysis revealed the scores for "tired eyes" (p = 0.001), "sore/aching eyes" (p = 0.038), "irritated eyes" (p = 0.010), "watery eyes" (p = 0.005), "dry eyes" (p = 0.003), "eye strain" (p = 0.006), "blurred vision" (p = 0.034), and "visual discomfort" (p = 0.018) significantly improved in the DA9301 group. We found that oral intake of DA9301 (1000 mg/day for 4 weeks) was effective in alleviating asthenopia symptoms induced by tablet computer watching. The study is registered at www.clinicaltrials.gov (registration number: NCT02641470, date of registration December 30, 2015).

  18. Can Tablet Computers Enhance Faculty Teaching?

    Science.gov (United States)

    Narayan, Aditee P; Whicker, Shari A; Benjamin, Robert W; Hawley, Jeffrey; McGann, Kathleen A

    2015-06-01

    Learner benefits of tablet computer use have been demonstrated, yet there is little evidence regarding faculty tablet use for teaching. Our study sought to determine if supplying faculty with tablet computers and peer mentoring provided benefits to learners and faculty beyond that of non-tablet-based teaching modalities. We provided faculty with tablet computers and three 2-hour peer-mentoring workshops on tablet-based teaching. Faculty used tablets to teach, in addition to their current, non-tablet-based methods. Presurveys, postsurveys, and monthly faculty surveys assessed feasibility, utilization, and comparisons to current modalities. Learner surveys assessed perceived effectiveness and comparisons to current modalities. All feedback received from open-ended questions was reviewed by the authors and organized into categories. Of 15 eligible faculty, 14 participated. Each participant attended at least 2 of the 3 workshops, with 10 to 12 participants at each workshop. All participants found the workshops useful, and reported that the new tablet-based teaching modality added value beyond that of current teaching methods. Respondents developed the following tablet-based outputs: presentations, photo galleries, evaluation tools, and online modules. Of the outputs, 60% were used in the ambulatory clinics, 33% in intensive care unit bedside teaching rounds, and 7% in inpatient medical unit bedside teaching rounds. Learners reported that common benefits of tablet computers were: improved access/convenience (41%), improved interactive learning (38%), and improved bedside teaching and patient care (13%). A common barrier faculty identified was inconsistent wireless access (14%), while no barriers were identified by the majority of learners. Providing faculty with tablet computers and having peer-mentoring workshops to discuss their use was feasible and added value.

  19. Comparison of intramuscular olanzapine, orally disintegrating olanzapine tablets, oral risperidone solution, and intramuscular haloperidol in the management of acute agitation in an acute care psychiatric ward in Taiwan.

    Science.gov (United States)

    Hsu, Wen-Yu; Huang, Si-Sheng; Lee, Bo-Shyan; Chiu, Nan-Ying

    2010-06-01

    The purpose of this study was to compare efficacy and safety among intramuscular olanzapine, intramuscular haloperidol, orally disintegrating olanzapine tablets, and oral risperidone solution for agitated patients with psychosis during the first 24 hours of treatment in an acute care psychiatric ward. Forty-two inpatients from an acute care psychiatric ward of a medical center in central Taiwan were enrolled. They were randomly assigned to 1 of the 4 treatment groups (10-mg intramuscular olanzapine, 10-mg olanzapine oral disintegrating tablet, 3-mg oral risperidone solution, or 7.5-mg intramuscular haloperidol). Agitation was measured by using the excited component of the Positive and Negative Syndrome Scale (PANSS-EC), the Agitation-Calmness Evaluation Scale, and the Clinical Global Impression--Severity Scale during the first 24 hours. There were significant differences in the PANSS-EC total scores for the 4 intervention groups at 15, 30, 45, 60, 75, and 90 minutes after the initiation of treatment. More significant differences were found early in the treatment. In the post hoc analysis, the patients who received intramuscular olanzapine or orally disintegrating olanzapine tablets showed significantly greater improvement in PANSS-EC scores than did patients who received intramuscular haloperidol at points 15, 30, 45, 60, 75, and 90 minutes after injection. These findings suggest that intramuscular olanzapine, orally disintegrating olanzapine tablets, and oral risperidone solution are as effective treatments as intramuscular haloperidol for patients with acute agitation. Intramuscular olanzapine and disintegrating olanzapine tablets are more effective than intramuscular haloperidol in the early phase of the intervention. There is no significant difference in effectiveness among intramuscular olanzapine, orally disintegrating olanzapine tablets, and oral risperidone solution.

  20. Tl response of LiF: Mg, Cu, P+Ptfe at X rays of 24, 42 and 100 KeV; Respuesta TL de LiF: Mg, Cu, P+Ptfe a rayos X de 24, 42 y 100 KeV

    Energy Technology Data Exchange (ETDEWEB)

    Gonzalez M, P.R.; Tovar M, V.M. [ININ, 52045 Ocoyoacac, Estado de Mexico (Mexico); Azorin N, J. [UAM-I, 09340 Mexico D.F. (Mexico); Furetta, C. [Universita degli Studi di Roma ' La Sapienza' , Piazzale Aldo Moro 2, 00185 Roma (Italy); Quiroz C, M.C. [Facultad de Medicina, UAEM, 50180 Toluca, Estado de Mexico (Mexico)

    2005-07-01

    In this work the obtained results of the irradiation of thermoluminescent dosemeters (Tl) of LiF: Mg,Cu,P + Ptfe with X rays for the effective radiation energy of 24, 42 and 100 keV, in an interval of Kerma in air in the sinus of the air between 0.05 and 1.0 Gy are presented. The rate of Kerma in air was determined with an ionization chamber PTW-1152, gauged by the Laboratoire Central des Industries Electriques (LCIE). As reference commercial TLD-100 dosemeters was used. The results showed that the studied Tl dosemeters presented a lineal response in the interval of mentioned Kerma. On the other hand the estimated Kerma with the Tl dosemeter in the calibration curves for X rays, were similar to the one measured with the previously gauged ionization chamber. The Tl of LiF: Mg, Cu, P + Ptfe, developed in the ININ, are highly reliable for X-ray dosimetry. (Author)

  1. Development and evaluation of sustained release losartan potassium matrix tablet using kollidon SR as release retardant

    Directory of Open Access Journals (Sweden)

    Shahid Sarwar

    2012-12-01

    Full Text Available The present study was undertaken to develop sustained release (SR matrix tablets of losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method, along with Kollidon SR as release retardant polymer. The amount of losartan potassium remains fixed (100 mg for all the three formulations whereas the amounts of Kollidon SR were 250 mg, 225 mg, and 200 mg for F-1, F-2, and F-3 respectively. The evaluation involves three stages: the micromeritic properties evaluation of granules, physical property studies of tablets, and in-vitro release kinetics studies. The USP apparatus type II was selected to perform the dissolution test, and the dissolution medium was 900 mL phosphate buffer pH 6.8. The test was carried out at 75 rpm, and the temperature was maintained at 37 ºC ± 0.5 ºC. The release kinetics was analyzed using several kinetics models. Higher polymeric content in the matrix decreased the release rate of drug. At lower polymeric level, the rate and extent of drug release were enhanced. All the formulations followed Higuchi release kinetics where the Regression co-efficient (R² values are 0.958, 0.944, and 0.920 for F-1, F-2, and F-3 respectively, and they exhibited diffusion dominated drug release. Statistically significant (PO presente estudo foi realizado para desenvolver (SR matriz de comprimidos de liberação sustentada de losartana, um antagonista da angiotensina II, para o tratamento da hipertensão arterial. Os comprimidos foram preparados pelo método de compressão direta com Kollidon SR como polímero de liberação lenta. A quantidade de losartana potássica permanece fixa (100 mg para todas as três formulações enquanto que as quantidades de Kollidon SR foram de 250 mg, 225 mg e 200 mg para F-1, F-2 e F-3, respectivamente. A avaliação envolve três etapas- propriedades micromeríticas dos grânulos, estudo das propriedades físicas dos comprimidos e

  2. Microstructure of Tablet-Pharmaceutical Significance, Assessment, and Engineering.

    Science.gov (United States)

    Sun, Changquan Calvin

    2017-05-01

    To summarize the microstructure - property relationship of pharmaceutical tablets and approaches to improve tablet properties through tablet microstructure engineering. The main topics reviewed here include: 1) influence of material properties and manufacturing process parameters on the evolution of tablet microstructure; 2) impact of tablet structure on tablet properties; 3) assessment of tablet microstructure; 4) development and engineering of tablet microstructure. Microstructure plays a decisive role on important pharmaceutical properties of a tablet, such as disintegration, drug release, and mechanical strength. Useful information on mechanical properties of a powder can be obtained from analyzing tablet porosity-pressure data. When helium pycnometry fails to accurately measure true density of a water-containing powder, non-linear regression of tablet density-pressure data is a useful alternative method. A component that is more uniformly distributed in a tablet generally exerts more influence on the overall tablet properties. During formulation development, it is highly recommended to examine the relationship between any property of interest and tablet porosity when possible. Tablet microstructure can be engineered by judicious selection of formulation composition, including the use of the optimum solid form of the drug and appropriate type and amount of excipients, and controlling manufacturing process.

  3. Strain relaxation studies of the Fe3O4/MgO (100) heteroepitaxial system grown by magnetron sputtering

    International Nuclear Information System (INIS)

    Balakrishnan, K; Arora, S K; Shvets, I V

    2004-01-01

    Detailed strain relaxation studies of epitaxial magnetite, Fe 3 O 4 , films on MgO(100) substrates grown by magnetron sputtering reveal the accommodation of strain up to 600 nm thickness, a thickness far above the critical thickness (t c ) predicted by theoretical models. The results are in agreement with the suggestion that the excess strain in Fe 3 O 4 /MgO (100) heteroepitaxy is accommodated by the presence of antiphase boundaries. The compressive strain generated by the antiphase boundaries compensates for the tensile strain within the growth islands, allowing the film to remain fully coherent with the substrate. Contrary to earlier findings, magnetization decreases with an increase in the film thickness. This vindicates the view that the structure of the antiphase boundaries depends on the growth conditions

  4. Safety of a benazepril and pimobendan combination tablet in adult healthy dogs.

    Science.gov (United States)

    Kuntz, E A; Strehlau, G; Giraudel, J M; King, J N

    2018-02-01

    The objective of the study was to investigate the safety of a combination tablet of benazepril and pimobendan, Fortekor PLUS ® , in a randomized, blinded, parallel-group design study in healthy adult beagle dogs. The test article, Fortekor PLUS ® tablets, was administered orally twice daily for 6 months at one, two, and four times the highest recommended dosage of 0.5 mg/kg benazepril hydrochloride/0.25 mg/kg pimobendan (four males and four females per group). An additional control group was sham-dosed. Fortekor PLUS ® did not induce any treatment-related effects on body weight, food consumption, neurological, ophthalmologic or physical assessments over the 6-month treatment period. The test article was possibly associated with an increased frequency of occasional vomiting. Fortekor PLUS ® was associated with small, but significant, increases in heart rate and reductions in PR and QT intervals, which were assessed by electrocardiography. These effects were most probably related to reflex tachycardia secondary to reduced systemic blood pressure. Statistically significant changes in some clinical pathology variables were noted after test article administration, but were considered to be of no clinical relevance as values remained within reference ranges and/or were not dose-dependent. No treatment-related macroscopic or microscopic findings were observed. In conclusion, Fortekor PLUS ® tablets were well tolerated in healthy adult dogs when administered at one, two, and four times the highest recommended dosage for 6 months. © 2017 John Wiley & Sons Ltd.

  5. Grasp interaction with tablets

    CERN Document Server

    Wolf, Katrin

    2015-01-01

    This book presents guidelines for a future device type: a tablet that allows ergonomic front- and back-of-device interaction. These guidelines help designers and developers of user interfaces to build ergonomic applications for tablet devices, in particular for devices that enable back-of-device interaction. In addition, manufacturers of tablet devices obtain arguments that back-of-device interaction is a promising extension of the interaction design space and results in increased input capabilities, enriched design possibilities, and proven usability. The guidelines are derived from empirical studies and developed to fit the users’ skills to the way the novel device type is held. Three particular research areas that are relevant to develop design guidelines for tablet interaction are investigated: ergonomic gestures, interaction areas, and pointing techniques.

  6. 75 FR 42455 - Novartis Pharmaceuticals Corp. et al.; Withdrawal of Approval of 27 New Drug Applications and 58...

    Science.gov (United States)

    2010-07-21

    ... Endo Pharmaceuticals NDA 17-255 MPI DTPA Chelate multidose (kit for Medi-Physics, Inc., d/b/a GE... 7.5 mg/750 mg ANDA 40-312 Innofem (estradiol tablets USP), 0.5 Novo Nordisk, Inc., 100 College Rd... Ranbaxy, Inc., U.S. Agent for Ranbaxy Tablets, 1,000 mg Laboratories Limited, 600 College Rd. East...

  7. Effect of Qing Nao tablet on blood stasis model of mice

    Science.gov (United States)

    Kong, Xuejun; Hao, Shaojun; Wang, Hongyu; Liu, Xiaobin; Xie, Guoqi; Li, Wenjun; Zhang, Zhengchen

    2018-04-01

    To investigate the effect of Qing Nao tablet on mouse model of blood stasis syndrome, 60 mice, male and female, were randomly divided into 6 groups, were fed with large, small doses of Qing Nao tablet suspension, Naoluotong saline suspension and the same volume (group 2, 0.1ml/10g), administer 1 times daily, orally for 15 days. Intragastric administration for first days, in addition to the 1 group saline group every day in the hind leg intramuscular saline, the other 5 groups each rat day hind leg muscle injection of dexamethasone 0.8mg/kg intramuscular injection every day, 1 times, 15 days. 1 hour continuous intramuscular injection and intramuscular drug perfusion on the sixteenth day after mice. The eyeball blood, heparin after whole blood viscosity test. Compared with the control group, model group, high and low shear viscosity were significantly increased (Pgroup, high dose group and Qing Nao tablet Naoluotong group can significantly reduce the viscosity at high shear and (Pgroup can significantly reduce high shear and shear viscosity (Pgroup can significantly reduce the low shear viscosity (Pgroup can significantly reduce the low shear viscosity (Pgroup were lower high cut, low shear viscosity and trend The potential (P>0.05). The Qing Nao tablet has a good effect on the model of blood stasis in mice.

  8. Role of various natural, synthetic and semi-synthetic polymers on drug release kinetics of losartan potassium oral controlled release tablets.

    Science.gov (United States)

    Jayasree, J; Sivaneswari, S; Hemalatha, G; Preethi, N; Mounika, B; Murthy, S Vasudeva

    2014-10-01

    The objective of the present work was to formulate and to characterize controlled release matrix tablets of losartan potassium in order to improve bioavailability and to minimize the frequency of administration and increase the patient compliance. Losartan potassium controlled release matrix tablets were prepared by direct compression technique by the use of different natural, synthetic and semisynthetic polymers such as gum copal, gum acacia, hydroxypropyl methyl cellulose K100 (HPMC K100), eudragit RL 100 and carboxy methyl ethyl cellulose (CMEC) individually and also in combination. Studies were carried out to study the influence of type of polymer on drug release rate. All the formulations were subjected to physiochemical characterization such as weight variation, hardness, thickness, friability, drug content, and swelling index. In vitro dissolution studies were carried out simulated gastric fluid (pH 1.2) for first 2 h and followed by simulated intestinal fluid (pH 6.8) up to 24 h, and obtained dissolution data were fitted to in vitro release kinetic equations in order to know the order of kinetics and mechanism of drug release. Results of physiochemical characterization of losartan potassium matrix tablets were within acceptable limits. Formulation containing HPMC K100 and CMEC achieved the desired drug release profile up to 24 h followed zero order kinetics, release pattern dominated by Korsmeyer - Peppas model and mechanism of drug release by nonfickian diffusion. The good correlation obtained from Hixson-Crowell model indicates that changes in surface area of the tablet also influences the drug release. Based on the results, losartan potassium controlled release matrix tablets prepared by employing HPMC K100 and CMEC can attain the desired drug release up to 24 h, which results in maintaining steady state concentration and improving bioavailability.

  9. Brand versus generic dispensing trend for ciprofloxacin 500 mg, levofloxacin 500 mg, and moxifloxacin 400 mg (oral dosage forms) among pharmacies of Karachi, Pakistan.

    Science.gov (United States)

    Zehra, Fatima; Naqvi, Atta Abbas; Tasneem, Sumbul; Ahmad, Rizwan; Ahmad, Niyaz; Shamsi, Adnan Zia; Asghar, Naqiya Ali; Khan, Ghufran Ullah

    2017-01-01

    Pakistan spends 0.7% of its gross domestic product on health. The public sector health-care system provides services to 22% of population thus paving the way for a dominant private sector. Patients in Pakistan mostly pay their medical expenses directly, and 64% of the health expenditures are borne by the household. Expenditure on medicine constitutes 43% of the total household expenditure. A quantitative cross-sectional study was conducted in Karachi, Pakistan, for a month. It was aimed at gathering response from different pharmacies to understand the brand versus generic dispensing trend of ciprofloxacin 500 mg, levofloxacin 500 mg, and moxifloxacin 400 mg oral dosage forms. The study employed convenience sampling and used a survey checklist. The data gathered was entered in SPSS version 22. The mean price per tablet for ciprofloxacin brand and generic was reported at Pakistani Rupees (PKR) 48.44 and PKR 26.85, respectively. The trend for dispensing ciprofloxacin highlighted a split in the market between brand (51%) and generic (49%). For levofloxacin brand and generic, the price per tablet was reported at PKR 36.50 and PKR 36.15 respectively, and despite same price, the market was dominated by generic levofloxacin (92%). Due to a price difference between brand and generic moxifloxacin, i.e., PKR 129.44 and PKR 71.91, respectively, the market was mostly occupied by the generic form (75%). Pricing mechanism must be revisited, and the authorities should take stern actions against any illegitimate price hike. The surging burden of drug expenditure on poorer sections of the society must be addressed by the government on an urgent basis.

  10. Design and characterisation of matrix tablets of highly water soluble drug

    Directory of Open Access Journals (Sweden)

    Vijayalakshmi Prakya

    2012-04-01

    Full Text Available Tramadol HCL is a centrally acting opioid analgesic. Although the drug has a higher plasma half life, the steady state plasma concentration is not achieved with frequent dosing of q.i.d at 6 hour intervals. Therefore, the objective of the present work was to formulate a 100mg strength Tramadol matrix tablets to extend the drug release and thus decrease the dosing frequency and achieve steady state plasma concentration. Initially, preformulation studies were carried out to rule out any incompatibility between the drug and the chosen polymer(s after exposing physical mixtures of the drug and the polymer(s to 40 and deg;C/75% RH for three months. A suitable method was developed for drug estimation at 271nm by a UV double beam spectrophotometer. Next, various batches of tablets were designed using different polymers such as Ethylcellulose, Carnauba wax, HPMC-K100M, Carbopol-974P and Kollidon-SR. Direct compression technique was used except for the formulation containing carnauba wax for which melt granulation was done followed by compression. Formulations F-1 to F-15 contained single polymers in increasing concentrations in drug:polymer ratios of 1:1, 1:2 and 1:3 where it was observed that the drug release extended with increasing polymer concentrations. Carbopol-974P extended drug release better followed by HPMC-K100M and Carnauba wax compared to other polymers. A combination of these polymers was also used at various ratios to get formulations F-16 to F-20 and observed that the polymer combinations controlled drug release better. The type of fillers like lactose and microcrystalline cellulose had no effect on the physiochemical characters as well as on the drug release profiles. The in vitro release data from the best formulation fitted well in Higuchi as well as Peppas model, the and #8216;n and #8217; value, which confirmed that the release mechanism shifted from initial dissolution to later extended diffusion in which both diffusion and erosion

  11. Pharmacokinetic and bioequivalence studies of immediate release diclofenac potassium tablets (50mg) in healthy volunteers.

    Science.gov (United States)

    Ali, Huma; Shoaib, Muhammad Harris; Zafar, Farya; Hanif, Muhammad; Bushra, Rabia; Naz, Asia; Khursheed, Raheela

    2016-09-01

    This study was conducted with the aim to determine the pharmacokinetic and bioequivalence of diclofenac potassium 50 mg test (F4) tablet formulation with reference product (Caflam). Present study was single dose, randomized, two phase cross over design, conducted in 12 healthy Pakistani volunteers and planned in accordance with FDA guidelines. In this study a simple, selective, sensitive and reproducible HPLC procedure was developed and validated for the estimation of diclofenac potassium in plasma. The process was validated in the range of 50 - 0.05 µg.mL-1 and used in bioequivalence trial of two products. Multiple blood samples were collected at various time points (0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12 and 14 hr after treating volunteers with test (F4) and marketed reference brand. Plasma separation and deproteination were carried out with acetonitrile; samples (20µL) were injected using the validated HPLC method. Various pharmacokinetic parameters (compartmental and noncompartmental) were estimated using KineticaTM 4.4.1 (Thermo Electron Corp. USA). Bioequivalence among the products was established by calculating the 90% CI with log and non log transformed data for Cmaxcalc, Tmaxcalc, AUC0-∞, AUCtot and AUClast using two way ANOVA and Schirmann's Two one sided t- test. No significant difference was found between log and non-log data. The 90% confidence interval values using log transformed data for AUC0-∞ (0.997-1.024), AUCtot (1.004-1.031), AUClast (0.997 -1.024), Cmaxcalc (0.994-1.007) and Tmaxcalc (0.996-1.013) for the trial and reference products were found within the FDA acceptable limits of 0.8-1.25. Results were further verified by the Schirmann's one-sided t test. Results showed the bioequivalence of test and reference formulations. Both the products were well tolerated.

  12. Evaluation of a Silver-Embedded Ceramic Tablet as a Primary and Secondary Point-of-Use Water Purification Technology in Limpopo Province, S. Africa.

    Directory of Open Access Journals (Sweden)

    Beeta Ehdaie

    Full Text Available The World Health Organization (WHO recognizes point-of-use water treatment (PoUWT technologies as effective means to improve water quality. This paper investigates long-term performance and social acceptance of a novel PoUWT technology, a silver-infused ceramic tablet, in Limpopo Province, South Africa. When placed in a water storage container, the silver-embedded ceramic tablet releases silver ions into water, thereby disinfecting microbial pathogens and leaving the water safe for human consumption. As a result of its simplicity and efficiency, the silver-embedded ceramic tablet can serve as a stand-alone PoUWT method and as a secondary PoUWT to improve exisitng PoUWT methods, such as ceramic water filters. In this paper, three PoUWT interventions were conducted to evaluate the silver-embedded ceramic tablet: (1 the silver-embedded ceramic tablet as a stand-alone PoUWT method, (2 ceramic water filters stand-alone, and (3 a filter-tablet combination. The filter-tablet combination evaluates the silver-embedded ceramic tablet as a secondary PoUWT method when placed in the lower reservoir of the ceramic water filter system to provide residual disinfection post-filtration. Samples were collected from 79 households over one year and analyzed for turbidity, total silver levels and coliform bacteria. Results show that the silver-embedded ceramic tablet effectively reduced total coliform bacteria (TC and E. coli when used as a stand-alone PoUWT method and when used in combination with ceramic water filters. The silver-embedded ceramic tablet's performance as a stand-alone PoUWT method was comparable to current inexpensive, single-use PoUWT methods, demonstrating 100% and 75% median reduction in E. coli and TC, respectively, after two months of use. Overall, the the filter-tablet combination performed the best of the three interventions, providing a 100% average percent reduction in E. coli over one year. User surveys were also conducted and indicated

  13. 77 FR 25720 - Determination That GRIFULVIN V (Griseofulvin Microcrystalline) Tablets, 250 Milligrams, Was Not...

    Science.gov (United States)

    2012-05-01

    ... been discontinued from marketing for reasons other than safety or effectiveness. ANDAs that refer to... Sale for Reasons of Safety or Effectiveness AGENCY: Food and Drug Administration, HHS. ACTION: Notice... microcrystalline) tablets, 250 milligrams (mg), was not withdrawn from sale for reasons of safety or effectiveness...

  14. [Neurotropic effect of B vitamins in the complex treatment of pain syndrome].

    Science.gov (United States)

    Shavlovskaya, O A

    Combined vitamin preparations in therapeutic doses are used, along with simple analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs), muscle and epidural blockade, for the relief of acute pain. It is recommended to use the B vitamin preparation neuromultivit. The tablet form of this preparation contains vitamin thiamine hydrochloride (100 mg), pyridoxine hydrochloride (200 mg), cyanocobalamin (0.2 mg), and injectable form includes thiamine hydrochloride (100mg), pyridoxine hydrochloride (100 mg), cyanocobalamin (1 mg). The efficacy of neuromultivit in a two stage scheme (intramuscular injections of 2 ml daily for 5-10 days with further injections 2-3 times a week for 2-3 weeks at the initial stage and 1 tablet 3 times a day for 4 weeks at the second stage) was shown.

  15. Bioavailability of oxycodone after administration of a new prolonged-release once-daily tablet formulation in healthy subjects, in comparison to an established twice-daily tablet
.

    Science.gov (United States)

    Scheidel, Bernhard; Maritz, Martina A; Gschwind, Yves J; Steigerwald, Kerstin; Guth, Volker; Kovacs, Peter; Rey, Helene

    2017-11-01

    To evaluate and to compare the bioavailability, the influence of food intake on the bioavailability, and the safety and tolerability of a newly-developed oxycodone once-daily (OOD) prolonged-release tablet with an established oxycodone twice-daily (OTD) prolonged-release tablet after single-dose administration under fasting or fed conditions as well as after multiple-dose administration. Three single-center, open-label, randomized, balanced, two-treatment, two-period, two-sequence crossover studies were conducted. In each study, 36 healthy volunteers were randomized to receive 10 mg oxycodone daily as OOD (oxycodone HCL 10-mg PR tablets XL (Develco Pharma Schweiz AG, Pratteln, Switzerland); administration of 1 tablet in the morning) or as OTD (reference formulation: oxygesic 5-mg tablets (Mundipharma GmbH, Limburg an der Lahn, Germany); administration of 1 tablet in the morning and 1 tablet in the evening). Tablets were administered once daily or twice daily under fasting conditions (study 1) or under fed conditions (study 2) as well as after multiple-dose administration (study 3). A sufficient number of blood samples were taken for describing plasma profiles and for calculation of pharmacokinetic parameters. Plasma concentrations of oxycodone were determined by LC-MS/MS. Safety and tolerability were monitored and assessed in all three studies. Plasma profiles of OOD reveal sustained concentrations of oxycodone over the complete dosing interval of 24 hours. In comparison to the OTD reference formulation, the OOD test formulation showed a slightly slower increase of concentrations within the absorption phase and similar plasma concentrations at the maximum and at the end of the dosing interval (24 hours). Extent of bioavailability (AUC), maximum plasma concentrations (Cmax), and plasma concentrations at the end of the dosing interval (Cτ,ss,24h) of OOD could be classified as comparable to OTD considering 90% confidence intervals (CIs) and acceptance limits of 80

  16. Development of Modified-Release Tablets of Zolpidem Tartrate by Biphasic Quick/Slow Delivery System

    OpenAIRE

    Mahapatra, Anjan Kumar; Sameeraja, N. H.; Murthy, P. N.

    2014-01-01

    Zolpidem tartrate is a non-benzodiazepine analogue of imidazopyridine of sedative and hypnotic category. It has a short half-life with usual dosage regimen being 5 mg, two times a day, or 10 mg, once daily. The duration of action is considered too short in certain circumstances. Thus, it is desirable to lengthen the duration of action. The formulation design was implemented by preparing extended-release tablets of zolpidem tartrate using the biphasic delivery system technology, where sodium s...

  17. The pharmacokinetic profile of a novel fixed-dose combination tablet of ibuprofen and paracetamol

    OpenAIRE

    Tanner, Trevor; Aspley, Sue; Munn, Andrew; Thomas, Tracy

    2010-01-01

    Background Ibuprofen and paracetamol differ in their mode of action and related therapeutic effects, suggesting that combined administration may offer improved analgesia. Reported here are the results of two studies on the pharmacokinetic properties of a novel ibuprofen (200 mg) and paracetamol (500 mg) fixed-dose combination tablet. Methods Both studies were open-label, randomised studies in healthy volunteers: Study 1 was a four-way crossover, single-dose study; Study 2 was a two-way cross-...

  18. What can potassium-iodine tablets help in case of a reactor accident

    International Nuclear Information System (INIS)

    Grueter, H.

    1979-01-01

    Pharmacologic iodine-doses (0.5g KJ orally) stop the radio iodine storage of the thyroid almost immediately and reduce the thyroid dose by 90% up to 2 hrs. after incorporation. So far, the distribution of potassium-iodine tablets among people living near to nuclear power plants seems, in the authors opinion, reasonable. He points out, however, that the thyroid is relatively unsensitive to radiation and that it is difficult to estimate the importance of an isolated protection of this organ as the storage effect of the thyroid can reduce a critical whole body exposure. Furthermore he indicates the psychological effects on the population which cannot be estimated in advance; i.e. it might be dangerous to distribute tablets among the people. (MG) [de

  19. Efficacy and tolerability of tamsulosin 0.4 mg in Asian patients with lower urinary tract symptoms secondary to benign prostatic hyperplasia refractory to tamsulosin 0.2 mg: a randomized placebo controlled trial.

    Science.gov (United States)

    Kim, Jung Jun; Han, Deok Hyun; Sung, Hyun Hwan; Choo, Seol Ho; Lee, Sung Won

    2014-07-01

    To evaluate the efficacy and safety of tamsulosin dose increase to 0.4 mg daily in Asian patients with lower urinary tract symptoms secondary to benign prostatic hyperplasia refractory to tamsulosin 0.2 mg treatment. We carried out a 12-week, single-center, randomized, placebo-controlled trial in 220 patients. Patients treated with 0.2 mg tamsulosin daily without other lower urinary tract symptoms secondary to benign prostatic hyperplasia medication for more than 3 months and refractory to this treatment were enrolled. We defined "refractory" as an International Prostate Symptom Score of 13 or greater and a maximum flow rate of 15 or under despite medication. Patients with a surgical history related to lower urinary tract symptoms secondary to benign prostatic hyperplasia or a postvoid residual of 150 mL or greater were excluded. Eligible patients were randomly assigned to the 0.4 mg group (two tablets of 0.2 mg tamsulosin once daily) or the 0.2 mg group (one tablet of 0.2 mg tamsulosin and one tablet of placebo once daily). International Prostate Symptom Score, maximum flow rate, blood pressure, heart rate, and adverse events were compared between the two groups at 4 weeks and 12 weeks. A total of 220 patients were enrolled and analyzed. There were no differences in baseline characteristics between the two groups. After 12 weeks of medication, the International Prostate Symptom Score was not different between the two groups. However, the improvement in maximum flow rate was greater in the 0.4 mg group than the 0.2 mg group (3.0 ± 0.48 mL/s vs -0.25 ± 0.30 mL/s, P Tamsulosin 0.4 mg appears to be a safe treatment regimen for treating lower urinary tract symptoms secondary to benign prostatic hyperplasia in Asian patients who do not respond to 0.2 mg treatment. Increasing the dose of tamsulosin results in a significant improvement in maximum flow rate without any increase in cardiovascular complications. © 2014 The

  20. A critical review on tablet disintegration.

    Science.gov (United States)

    Quodbach, Julian; Kleinebudde, Peter

    2016-09-01

    Tablet disintegration is an important factor for drug release and can be modified with excipients called tablet disintegrants. Tablet disintegrants act via different mechanisms and the efficacy of these excipients is influenced by various factors. In this review, the existing literature on tablet disintegration is critically reviewed. Potential disintegration mechanisms, as well as impact factors on the disintegration process will be discussed based on experimental evidence. Search terms for Scopus and Web of Science included "tablet disintegration", "mechanism tablet disintegration", "superdisintegrants", "disintegrants", "swelling force", "disintegration force", "disintegration mechanisms", as well as brand names of commonly applied superdisintegrants. References of identified papers were screened as well. Experimental data supports swelling and shape recovery as main mechanisms of action of disintegrants. Other tablet excipients and different manufacturing techniques greatly influence the disintegration process. The use of different excipients, experimental setups and manufacturing techniques, as well as the demand for original research led to a distinct patchwork of knowledge. Broader, more systematic approaches are necessary not only to structure the past but also future findings.

  1. Anthelmintic efficacies of a tablet formula of ivermectin-praziquantel on horses experimentally infected with three Strongylus species.

    Science.gov (United States)

    Bonneau, Stephane; Maynard, Laurence; Tomczuk, Krzysztof; Kok, Dawid; Eun, Hyone-Myong

    2009-09-01

    In this blinded randomized and controlled study, the anthelmintic efficacy of a tablet formula of ivermectin-praziquantel was evaluated in horses experimentally infected with three species of Strongylus larvae. Eighteen previously dewormed horses were inoculated on study day 0 with third-stage larvae of Strongylus vulgaris, Strongylus equinus, and Strongylus edentatus. The horses were randomly allocated to three groups (n = 6): test-drug (tablet formula), positive-control (reference gel), and negative-control (placebo tablet). On day 56, the horses were treated once with the respective drugs. On day 95, the horses were sacrificed, and necropsy examinations were performed to assess the status of the parasite burden (L4 and immature L5) and pathological lesions on selected organs and tissues. By the criteria of worm counts, the test-drug and positive-control showed, respectively, 100% and 97.3% anthelmintic efficacies on S. vulgaris, 100% and 81.4% on S. equinus, and equally 100% on S. edentatus. However, the efficacies on S. equinus and S. edentatus should be taken only as face values considering their respective low worm counts in the placebo group. The S. vulgaris-induced arterial lesions were also reduced in the test-drug and positive-control groups with efficacies of 73.9% and 62.9%, respectively. No adverse reactions were observed with either of the drugs. Our data demonstrate that the Equimax tablet formula was as safe and efficacious as the gel formula anthelmintic on large strongyles in horses.

  2. Linking the pharmacological content of ecstasy tablets to the subjective experiences of drug users.

    Science.gov (United States)

    Brunt, Tibor M; Koeter, Maarten W; Niesink, Raymond J M; van den Brink, Wim

    2012-04-01

    Most studies on the subjective effects of ecstasy are based on the assumption that the substance that was taken is 3,4-methylenedioxymethamphetamine (MDMA). However, many tablets sold as ecstasy contain other substances and MDMA in varying doses. So far, few attempts have been made to take this into account while assessing subjective effects. This study aims to link the pharmacological content of tablets sold as ecstasy to the subjective experiences reported by ecstasy users. Self-reported effects on ecstasy tablets were available from 5,786 drug users who handed in their tablets for chemical analysis at the Drug Information and Monitoring System (DIMS) in the Netherlands. Logistic regression was employed to link the pharmacological content of ecstasy tablets to the self-reported subjective effects and compare effects with MDMA to other substances present. MDMA showed a strong association with desirable subjective effects, unparalleled by any other psychoactive substance. However, the association of MDMA was dose-dependent, with higher doses (>120 mg/tablet) likely to evoke more adverse effects. The novel psychostimulants mephedrone and p-fluoroamphetamine were considered relatively desirable, whereas meta-chlorophenylpiperazine (mCPP) and p-methoxymethamphetamine (PMMA) were strongly associated with adverse subjective effects. Also, 3,4-methylene-dioxyamphetamine (MDA) and benzylpiperazine (BZP) were not appreciated as replacement for MDMA. Linking the pharmacological content of ecstasy sold on the street to subjective experiences contributes to a better understanding of the wide range of subjective effects ascribed to ecstasy and provides a strong rationale for the prolonged endurance of MDMA as the key ingredient of the ecstasy market.

  3. Proton/gamma relative thermoluminescence efficiencies of LiF:Mg,Cu,P+PTFE prepared at ININ and TLD-100H

    International Nuclear Information System (INIS)

    Avila, O.; Gonzalez, P.; Murillo, G.

    2009-10-01

    Properties of LiF:Mg,Cu,P+PTFE dosemeters developed at ININ have been investigated in order to evaluate their performance compared to those of equivalent commercial dosemeters. In this work both LiF:Mg,Cu,P+PTFE and TLD-100H pellets were exposed to low fluence 3 MeV protons and to low dose gamma radiation to evaluate experimental proton/gamma efficiencies. Gamma irradiation was performed using the Vic krad irradiator at ININ at varying doses between 25 and 500 mGy. For proton irradiation the Tandem Van de Graaff accelerator at ININ was used. Dosemeters were placed on a holder inside a scattering chamber where protons impinge on a gold target and scatter in all directions. The holder allows for several angular positions so that dosemeters receive proton fluence between 10 6 and 10 1 0 p/cm 2 . Experimental efficiency values found for LiF:Mg,Cu,P+PTFE and TLD-100H were 0.18 +- 03 and 0.23 +- 0.03, respectively. These results allow to confirm the reliability of the dosemeters developed at ININ. (Author)

  4. Predictive evaluation of pharmaceutical properties of direct compression tablets containing theophylline anhydrate during storage at high humidity by near-infrared spectroscopy.

    Science.gov (United States)

    Otsuka, Yuta; Yamamoto, Masahiro; Tanaka, Hideji; Otsuka, Makoto

    2015-01-01

    Theophylline anhydrate (TA) in tablet formulation is transformed into monohydrate (TH) at high humidity and the phase transformation affected dissolution behavior. Near-infrared spectroscopic (NIR) method is applied to predict the change of pharmaceutical properties of TA tablets during storage at high humidity. The tablet formulation containing TA, lactose, crystalline cellulose and magnesium stearate was compressed at 4.8 kN. Pharmaceutical properties of TA tables were measured by NIR, X-ray diffraction analysis, dissolution test and tablet hardness. TA tablet was almost 100% transformed into TH after 24 hours at RH 96%. The pharmaceutical properties of TA tablets, such as tablet hardness, 20 min dissolution amount (D20) and increase of tablet weight (TW), changed with the degree of hydration. Calibration models for TW, tablet hardness and D20 to predict the pharmaceutical properties at high-humidity conditions were developed on the basis of the NIR spectra by partial least squares regression analysis. The relationships between predicted and actual measured values for TW, tablet hardness and D20 had straight lines, respectively. From the results of NIR-chemometrics, it was confirmed that these predicted models had high accuracy to monitor the tablet properties during storage at high humidity.

  5. Factor analysis in optimization of formulation of high content uniformity tablets containing low dose active substance.

    Science.gov (United States)

    Lukášová, Ivana; Muselík, Jan; Franc, Aleš; Goněc, Roman; Mika, Filip; Vetchý, David

    2017-11-15

    Warfarin is intensively discussed drug with narrow therapeutic range. There have been cases of bleeding attributed to varying content or altered quality of the active substance. Factor analysis is useful for finding suitable technological parameters leading to high content uniformity of tablets containing low amount of active substance. The composition of tabletting blend and technological procedure were set with respect to factor analysis of previously published results. The correctness of set parameters was checked by manufacturing and evaluation of tablets containing 1-10mg of warfarin sodium. The robustness of suggested technology was checked by using "worst case scenario" and statistical evaluation of European Pharmacopoeia (EP) content uniformity limits with respect to Bergum division and process capability index (Cpk). To evaluate the quality of active substance and tablets, dissolution method was developed (water; EP apparatus II; 25rpm), allowing for statistical comparison of dissolution profiles. Obtained results prove the suitability of factor analysis to optimize the composition with respect to batches manufactured previously and thus the use of metaanalysis under industrial conditions is feasible. Copyright © 2017 Elsevier B.V. All rights reserved.

  6. X-ray magnetic circular dichroism study of epitaxial magnetite ultrathin film on MgO(100)

    Energy Technology Data Exchange (ETDEWEB)

    Liu, W. Q.; Xu, Y. B., E-mail: yongbing.xu@york.ac.uk, E-mail: rzhang@nju.edu.cn [York-Nanjing International Center for Spintronics (YNICS), School of Electronics Science and Engineering, Nanjing University, Nanjing 210093 (China); Spintronics and Nanodevice Laboratory, Department of Electronics, University of York, York YO10 5DD (United Kingdom); Song, M. Y.; Lin, J. G. [Center for Condensed Matter Sciences, National Taiwan University, Taipei 106, Taiwan (China); Maltby, N. J.; Li, S. P. [Spintronics and Nanodevice Laboratory, Department of Electronics, University of York, York YO10 5DD (United Kingdom); Samant, M. G.; Parkin, S. S. P. [IBM Research Division, Almaden Research Center, San Jose, California 95120 (United States); Bencok, P.; Steadman, Paul; Dobrynin, Alexey [Diamond Light Source, Didcot OX11 0DE (United Kingdom); Zhang, R., E-mail: yongbing.xu@york.ac.uk, E-mail: rzhang@nju.edu.cn [York-Nanjing International Center for Spintronics (YNICS), School of Electronics Science and Engineering, Nanjing University, Nanjing 210093 (China)

    2015-05-07

    The spin and orbital magnetic moments of the Fe{sub 3}O{sub 4} epitaxial ultrathin film synthesized by plasma assisted simultaneous oxidization on MgO(100) have been studied with X-ray magnetic circular dichroism. The ultrathin film retains a rather large total magnetic moment, i.e., (2.73 ± 0.15) μ{sub B}/f.u., which is ∼70% of that for the bulk-like Fe{sub 3}O{sub 4}. A significant unquenched orbital moment up to 0.54 ± 0.05 μ{sub B}/f.u. was observed, which could come from the symmetry breaking at the Fe{sub 3}O{sub 4}/MgO interface. Such sizable orbital moment will add capacities to the Fe{sub 3}O{sub 4}-based spintronics devices in the magnetization reversal by the electric field.

  7. Pulsed laser deposition of SmFeAsO1-δ on MgO(100) substrates

    Science.gov (United States)

    Haindl, Silvia; Kinjo, Hiroyuki; Hanzawa, Kota; Hiramatsu, Hidenori; Hosono, Hideo

    2018-04-01

    Layered iron oxyarsenides are novel interesting semimetallic compounds that are itinerant antiferromagnets in their ground state with a transition to high-temperature superconductivity upon charge carrier doping. The rare earth containing mother compounds offer rich physics due to different antiferromagnetic orderings: the alignment of Fe magnetic moments within the FeAs sublattice, which is believed to play a role for the superconducting pairing mechanism, and the ordering of the rare-earth magnetic moments at low temperatures. Here, we present thin film preparation and a film growth study of SmFeAsO on MgO(100) substrates using pulsed laser deposition (PLD). In general, the PLD method is capable to produce iron oxyarsenide thin films, however, competition with impurity phase formation narrows the parameter window. We assume that the film growth in an ultra-high vacuum (UHV) environment results in an oxygen-deficient phase, SmFeAsO1-δ. Despite the large lattice misfit, we find epitaxial oxyarsenide thin film growth on MgO(100) with evolving film thickness. Bragg reflections are absent in very thin films although they locally show indications for pseudomorphic growth of the first unit cells. We propose the possibility for a Stranski-Krastanov growth mode as a result of the large in-plane lattice misfit between the iron oxypnictide and the MgO unit cells. A columnar 3-dimensional film growth mode dominates and the surface roughness is determined by growth mounds, a non-negligible parameter for device fabrication as well as in the application of surface sensitive probes. Furthermore, we found evidence for a stratified growth in steps of half a unit cell, i.e. alternating growth of (FeAs)- and (SmO1-δ)+ layers, the basic structural components of the unit cell. We propose a simple model for the growth kinetics of this compound.

  8. Amorphization within the tablet

    DEFF Research Database (Denmark)

    Doreth, Maria; Hussein, Murtadha Abdul; Priemel, Petra A.

    2017-01-01

    , the feasibility of microwave irradiation to prepare amorphous solid dispersions (glass solutions) in situ was investigated. Indomethacin (IND) and polyvinylpyrrolidone K12 (PVP) were tableted at a 1:2 (w/w) ratio. In order to study the influence of moisture content and energy input on the degree of amorphization......, tablet formulations were stored at different relative humidity (32, 43 and 54% RH) and subsequently microwaved using nine different power-time combinations up to a maximum energy input of 90 kJ. XRPD results showed that up to 80% (w/w) of IND could be amorphized within the tablet. mDSC measurements...

  9. Android tablets for dummies

    CERN Document Server

    Gookin, Dan

    2015-01-01

    Learn all you need to know about your Android tablet in one quick and easy reference! It's not a computer and it's not a smartphone-so what in the world is it? Whether you're new to Android or new to tablets altogether, you're about to experience mobile computing like never before with this fun, full-color guide! Inside, longtime and bestselling author Dan Gookin walks you through setting up your Android tablet, navigating the interface, browsing the web, setting up email, connecting to social media, finding plenty of apps, music, books, and movies to indulge your interests-and so much more.

  10. A simple and convenient method for the simultaneous in vitro study of metformin and glimepiride tablets.

    Science.gov (United States)

    Ahmed, Rehan

    2014-11-01

    A simple and convenient method was developed for the simultaneous determination of metformin HCl and glimepiride in tablet dosage form of different pharmaceuticals companies. This method was validated and proved to be applicable for assay determination in intermediate and finished staged. More over a single medium dissolution of metformin HCl and glimepiride was established and the media was evaluated for comparative studies for different formulations. Reverse phase HPLC equipped with UV detector was used for the determination of metformin HCl and glimepiride. A mixture of acetonitrile and ammonium acetate buffer 0.05M pH 3.0 was used as mobile phase at flow rate of 1.0ml/min. Promocil C18 5µ 100Aº 4.6 x 100mm C18 silica column was used and detection was carried out at 270nm. Method was found to be linear over the range of 4ppm to 16ppm for glimepiride and 170ppm to 680ppm for metformin HCl. Regression co-efficient were found to be 0.9949 and 0.9864 for glimepiride and metformin HCl respectively. Dissolution was performed in 500ml 0.2% sodium lauryl sulfate at 37°C for 45min using paddle apparatus. Dissolution of glimepiride was found to be 98.60% and 101.08% in Orinase Met1 tablet and Amaryl M tablet respectively whereas metformin was found 99.41% and 98.59% in Orinase Met 1 tablet and Amaryl M tablet. RSD for all the dissolutions was less than 2.0% after completion.

  11. Magnetic resonance imaging and relaxometry to study water transport mechanisms in a commercially available gastrointestinal therapeutic system (GITS) tablet.

    Science.gov (United States)

    Broadbent, Amber L; Fell, Rob J; Codd, Sarah L; Lightley, Kim A; Konagurthu, Sanjay; Koehler-King, Dory G; Seymour, Joseph D

    2010-09-15

    The hydration of 4 mg Cardura XL (Pfizer), a commercially available gastrointestinal therapeutic system (GITS) tablet, was investigated using magnetic resonance imaging (MRI). A short echo time (T(e)=2.81 ms) technique for MRI of the hydration of a GITS tablet was implemented. From the MR images, signal intensity profiles were generated and interpreted in the context of diffusive and osmotic transport mechanisms. A distinct transition from diffusive to osmotic transport was measured at a timescale relevant to the measured drug release time. Diffusion and osmotic rate coefficients for water in the drug and polymer sweller layers of the tablet were quantified. Spin-lattice T(1) and spin-spin T(2) relaxation times of the water signal from within the tablet were measured as a function of hydration time in order to incorporate the effects of relaxation into interpretation of signal intensity and provide unique information on the distribution of water in different physical and chemical environments within the tablet. Copyright 2010 Elsevier B.V. All rights reserved.

  12. Tablet-Based Functional MRI of the Trail Making Test: Effect of Tablet Interaction Mode

    Directory of Open Access Journals (Sweden)

    Mahta Karimpoor

    2017-10-01

    Full Text Available The Trail Making Test (TMT is widely used for assessing executive function, frontal lobe abilities, and visual motor skills. Part A of this pen-and-paper test (TMT-A involves linking numbers randomly distributed in space, in ascending order. Part B (TMT-B alternates between linking numbers and letters. TMT-B is more demanding than TMT-A, but the mental processing that supports the performance of this test remains incompletely understood. Functional MRI (fMRI may help to clarify the relationship between TMT performance and brain activity, but providing an environment that supports real-world pen-and-paper interactions during fMRI is challenging. Previously, an fMRI-compatible tablet system was developed for writing and drawing with two modes of interaction: the original cursor-based, proprioceptive approach, and a new mode involving augmented reality to provide visual feedback of hand position (VFHP for enhanced user interaction. This study characterizes the use of the tablet during fMRI of young healthy adults (n = 22, with half of the subjects performing TMT with VFHP and the other half performing TMT without VFHP. Activation maps for both TMT-A and TMT-B performance showed considerable overlap between the two tablet modes, and no statistically differences in brain activity were detected when contrasting TMT-B vs. TMT-A for the two tablet modes. Behavioral results also showed no statistically different interaction effects for TMT-B vs. TMT-A for the two tablet modes. Tablet-based TMT scores showed reasonable convergent validity with those obtained by administering the standard pen-and-paper TMT to the same subjects. Overall, the results suggest that despite the slightly different mechanisms involved for the two modes of tablet interaction, both are suitable for use in fMRI studies involving TMT performance. This study provides information for using tablet-based TMT methods appropriately in future fMRI studies involving patients and healthy

  13. Interchangeability and comparative effectiveness between generic and brand montelukast immediate release tablets after a single oral administration in healthy volunteers.

    Science.gov (United States)

    Zaid, Abdel Naser; Mousa, Ayman; Ghazal, Nadia; Bustami, Rana

    2015-01-01

    Montelukast is a leukotriene receptor antagonist. The release of leukotrienes causes narrowing and constricting in the respiratory airways. Blocking the action of these leukotrienes, montelukast can be used for the prophylaxis and treatment of chronic asthma. The aim of this study was to evaluate the interchangeability and comparative effectiveness between a generic and a brand montelukast 10 mg immediate release tablets (Broncast(®) and Singulair(®), respectively) after a single oral dose among Arab Mediterranean volunteers. An open-label, randomized two-period crossover bioequivalence design was conducted in 31 healthy male volunteers with a 1 week washout between each study period and under fasting conditions. The plasma drug concentration was assessed by using a previously validated LC MS/MS method. The ratio between the generic and brand of geometric least squares means was reported for both generic and brand products. Moreover, an in vitro dissolution study was conducted on generic and brand tablets using three different pH media, and similarity and non-similarity factors (f2 and f1) were calculated. The used bioanalytical method was found to be linear within the range 6.098-365.855 ng/mL. The correlation coefficient was close to 0.999 during the course of the study validation. Statistical comparison of the main pharmacokinetic parameters showed the inexistence of any significant difference between generic and the brand. The point estimates (ratios of geometric means) were 111.939, 111.711, and 112.169 % for AUC0-24, AUC0-∞, and Cmax, respectively. The 90 % confidence intervals (CIs) were within the pre-defined limits of 80.00-125.00 % as specified by the FDA and EMA for bioequivalence studies. F2 and f1 were higher than 50 and lower than 15, respectively in all selected pH media. Broncast(®) immediate release film coated tablets (10 mg/tablet) are bioequivalent to Singulair(®) immediate release film coated tablets (10 mg/tablet), with a

  14. Formation of nano-sized pinholes array in thin Ni film on MgO(100) substrate

    Energy Technology Data Exchange (ETDEWEB)

    Lin Chuan; Naramoto, Hiroshi; Xu Yonghua; Kitazawa, Sin-iti; Narumi, Kazumasa; Sakai, Seiji

    2003-10-22

    We have grown thin Ni films with various thicknesses on polished MgO(100) single crystal substrates in an e-gun evaporation system. The morphology of the as-deposited films was characterized with atomic force microscopy. Pinholes with average diameter of 5-10 nm are found in the film with thickness from 1 to 15 nm, and pinholes array was observed in the film 10 nm thick. The origin of such structure formation is discussed in terms of the elastic strain energy.

  15. Multivariate modelling of the tablet manufacturing process with wet granulation for tablet optimization and in-process control

    NARCIS (Netherlands)

    Westerhuis, J.A; Coenegracht, P.M J; Lerk, C.F

    1997-01-01

    The process of tablet manufacturing with granulation is described as a two-step process. The first step comprises wet granulation of the powder mixture, and in the second step the granules are compressed into tablets. For the modelling of the pharmaceutical process of wet granulation and tableting,

  16. Evaluation of the performance characteristics of bilayer tablets: Part II. Impact of environmental conditions on the strength of bilayer tablets.

    Science.gov (United States)

    Kottala, Niranjan; Abebe, Admassu; Sprockel, Omar; Bergum, James; Nikfar, Faranak; Cuitiño, Alberto M

    2012-12-01

    Ambient air humidity and temperature are known to influence the mechanical strength of tablets. The objective of this work is to understand the influence of processing parameters and environmental conditions (humidity and temperature) on the strength of bilayer tablets. As part of this study, bilayer tablets were compressed with different layer ratios, dwell times, layer sequences, material properties (plastic and brittle), first and second layer forces, and lubricant concentrations. Compressed tablets were stored in stability chambers controlled at predetermined conditions (40C/45%RH, 40C/75%RH) for 1, 3, and 5 days. The axial strength of the stored tablets was measured and a statistical model was developed to determine the effects of the aforementioned factors on the strength of bilayer tablets. As part of this endeavor, a full 3 × 2(4) factorial design was executed. Responses of the experiments were analyzed using PROC GLM of SAS (SAS Institute Inc, Cary, North Carolina, USA). A model was fit using all the responses to determine the significant interactions (p < 0.05). Results of this study indicated that storage conditions and storage time have significant impact on the strength of bilayer tablets. For Avicel-lactose and lactose-Avicel tablets, tablet strength decreased with the increasing humidity and storage time. But for lactose-lactose tablets, due to the formation of solid bridges upon storage, an increase in tablet strength was observed. Significant interactions were observed between processing parameters and storage conditions on the strength of bilayer tablets.

  17. 78 FR 43210 - Bracco Diagnostics et al.; Withdrawal of Approval of 52 New Drug Applications and 77 Abbreviated...

    Science.gov (United States)

    2013-07-19

    ...., 235 East 42nd 50 mg, 75 mg, and St., New York, NY 100 mg. 10017. NDA 020239 Kytril (granisetron... Kytril (granisetron Do. HCl) Tablets, EQ 1 mg (base), EQ 2 mg (base). NDA 020336 DynaCirc CR GlaxoSmith...) Abbott Laboratories. Capsules, 100 mg. NDA 021238 Kytril (granisetron Hoffman-La Roche, HCl) Oral...

  18. Desenvolvimento de comprimidos de AAS 500 mg: influência do Amido 1500® na compressão direta Development of AAS 500 mg tablets influenced by direct compression (CD process

    Directory of Open Access Journals (Sweden)

    Osvaldo Albuquerque Cavalcanti

    2002-04-01

    Full Text Available O experimento teve por objetivo demonstrar a viabilidade tecnológica do desenvolvimento de comprimidos de AAS 500 mg (Ácido Acetil Salicílico, empregando processo de compressão direta (CD. O Amido 1500® foi usado como excipiente no desenvolvimento das formulações, visando investigar suas propriedades de compressibilidade, desintegração, agregação e lubrificação. Usando metodologias previstas em Farmacopéias, foram realizados ensaios tecnológicos e físico-químicos. Os resultados evidenciaram que a mistura dos pós apresentou características de fluxo e compressibilidade adequadas ao rol de excipientes para compressão direta disponíveis no mercado. A presença do Amido 1500® também interferiu no tempo de desintegração. Dentre as formulações propostas neste trabalho, a fórmula contendo 6,35% de Amido 1500® foi eleita a mais adequada por apresentar maior proximidade em relação aos produtos disponíveis no mercado brasileiroThe present work aims to show the technologic viability in the development of AAS 500 mg tablets using direct compression (CD process. We employed Starch 1500® as excipient to develop the formulations, trying to investigate its compression, disintegration, aggregation and lubrication properties. Technologic, physical and chemical essays were performed using methodologies anticipated in pharmacology. Results demonstrated that the powder mix showed characteristics of free flux and good compression qualities very important for the excipients of direct compression in the market. Starch 1500® interfered in the disintegration time. The formulation with 6,35% of Starch 1500® proposed in this work obtained a highest proximity between the products in the Brazilian market

  19. Effect of protective coating of aspirin tablets with acrylatemethacrylate copolymers on tablet disintegration times and dissolution rates

    OpenAIRE

    Okor R; Eichie F; Uhumwangho M; Aka-Aha A

    2007-01-01

    Tablets of aspirin (a moisture degradable drug) have been film coated with two analogous Eudragit RL and RS copolymers designated here as A and B which differ only in their cation content in the ratio 2:1 (A:B). A, is therefore more hydrophilic than B. The tablets were film coated with ethanol solutions of these two polymers. Film coating with either A or B significantly reduced the moisture uptake potentials of the tablets but caused an increase in the disintegration times of the tablets and...

  20. Using a Virtual Tablet Machine to Improve Student Understanding of the Complex Processes Involved in Tablet Manufacturing.

    Science.gov (United States)

    Mattsson, Sofia; Sjöström, Hans-Erik; Englund, Claire

    2016-06-25

    Objective. To develop and implement a virtual tablet machine simulation to aid distance students' understanding of the processes involved in tablet production. Design. A tablet simulation was created enabling students to study the effects different parameters have on the properties of the tablet. Once results were generated, students interpreted and explained them on the basis of current theory. Assessment. The simulation was evaluated using written questionnaires and focus group interviews. Students appreciated the exercise and considered it to be motivational. Students commented that they found the simulation, together with the online seminar and the writing of the report, was beneficial for their learning process. Conclusion. According to students' perceptions, the use of the tablet simulation contributed to their understanding of the compaction process.

  1. Relationships between response surfaces for tablet characteristics of placebo and API-containing tablets manufactured by direct compression method.

    Science.gov (United States)

    Hayashi, Yoshihiro; Tsuji, Takahiro; Shirotori, Kaede; Oishi, Takuya; Kosugi, Atsushi; Kumada, Shungo; Hirai, Daijiro; Takayama, Kozo; Onuki, Yoshinori

    2017-10-30

    In this study, we evaluated the correlation between the response surfaces for the tablet characteristics of placebo and active pharmaceutical ingredient (API)-containing tablets. The quantities of lactose, cornstarch, and microcrystalline cellulose were chosen as the formulation factors. Ten tablet formulations were prepared. The tensile strength (TS) and disintegration time (DT) of tablets were measured as tablet characteristics. The response surfaces for TS and DT were estimated using a nonlinear response surface method incorporating multivariate spline interpolation, and were then compared with those of placebo tablets. A correlation was clearly observed for TS and DT of all APIs, although the value of the response surfaces for TS and DT was highly dependent on the type of API used. Based on this knowledge, the response surfaces for TS and DT of API-containing tablets were predicted from only two and four formulations using regression expression and placebo tablet data, respectively. The results from the evaluation of prediction accuracy showed that this method accurately predicted TS and DT, suggesting that it could construct a reliable response surface for TS and DT with a small number of samples. This technique assists in the effective estimation of the relationships between design variables and pharmaceutical responses during pharmaceutical development. Copyright © 2017 Elsevier B.V. All rights reserved.

  2. Touch Screen Tablets and Emergent Literacy

    Science.gov (United States)

    Neumann, Michelle M.; Neumann, David L.

    2014-01-01

    The use of touch screen tablets by young children is increasing in the home and in early childhood settings. The simple tactile interface and finger-based operating features of tablets may facilitate preschoolers' use of tablet application software and support their educational development in domains such as literacy. This article reviews…

  3. Quantitative Appearance Inspection for Film Coated Tablets.

    Science.gov (United States)

    Yoshino, Hiroyuki; Yamashita, Kazunari; Iwao, Yasunori; Noguchi, Shuji; Itai, Shigeru

    2016-01-01

    The decision criteria for the physical appearance of pharmaceutical products are subjective and qualitative means of evaluation that are based entirely on human interpretation. In this study, we have developed a comprehensive method for the quantitative analysis of the physical appearance of film coated tablets. Three different kinds of film coated tablets with considerable differences in their physical appearances were manufactured as models, and their surface roughness, contact angle, color measurements and physicochemical properties were investigated as potential characteristics for the quantitative analysis of their physical appearance. All of these characteristics were useful for the quantitative evaluation of the physical appearances of the tablets, and could potentially be used to establish decision criteria to assess the quality of tablets. In particular, the analysis of the surface roughness and film coating properties of the tablets by terahertz spectroscopy allowed for an effective evaluation of the tablets' properties. These results indicated the possibility of inspecting the appearance of tablets during the film coating process.

  4. Research Article. Kinetics and Mechanism of Drug Release from Loratadine Orodispersible Tablets Developed without Lactose

    Directory of Open Access Journals (Sweden)

    Ciurba Adriana

    2017-03-01

    Full Text Available Objective: The aim of this study is to develop lactose-free orodispersible tablets with loratadine for patients with lactose intolerance. Materials and methods: Seven compositions (F1-F7 of 10 mg loratadine were prepared in form of orally disintegrating tablets, by direct compression, using croscarmellose sodium and pre-gelatinized starch in various concentrations as superdisintegrants, diluted with microcrystalline cellulose and combined with mannitol and maltodextrin as binder agents. The tablets had been studied in terms of their pharmacotechnical characteristics, by determining: the weight uniformity of the tablets, their friability, breaking strength and disintegration time, drug content and the dissolution profile of loratadine. The statistical analyses were performed with GraphPad Prism Software Inc. As dependent variables, both the hardness of the tablets and their disintegration ability differ between batches due to their compositional differences (as independent variables. DDSolver were used for modeling the kinetic of the dissolution processes by fitting the dissolution profiles with time-dependent equations (Zero-order, First-order, Higuchi, Korsmeyer-Peppas, Peppas-Sahlin. Results: All proposed formulas shows rapid disintegration, in less than 15 seconds, and the dissolution loratadine spans a period of about 10 minutes. Akaike index as well as R2 adjusted parameter have demonstrated that the studied dissolution profiles are the best fitted by Zero-order kinetic. Conclusion: In conclusion, association of croscarmellose sodium (7.5% with pre-gelatinized starch (6% as superdisintegrants and mannitol as the binder agent (35%, positively influences the dissolution properties of loratadine from orally fast dispersible tablets.

  5. Comparative bioavailability studies of citric acid and malonic acid based aspirin effervescent tablets

    Directory of Open Access Journals (Sweden)

    Anju Gauniya

    2010-01-01

    Full Text Available Purpose: The present investigation is aimed at comparing the pharmacokinetic profile (Bioavailability of aspirin in tablet formulations, which were prepared by using different effervescent excipients such as citric acid and malonic acid. Materials and Methods: The relative bioavailability and pharmacokinetics of citric acid based aspirin effervescent tablet (Product A and malonic acid based aspirin effervescent tablet (Product B formulations were evaluated for an in-vitro dissolution study and in-vivo bioavailability study, in 10 normal healthy rabbits. The study utilized a randomized, crossover design with a one-week washout period between doses. Blood samples were collected at 0, 1, 2, 4, 6, 8, 12 and 24 hours following a 100 mg/kg dose. Plasma samples were assayed by High Performance Liquid Chromatography. T max , C max , AUC 0-24 , AUC 0- ∞, MRT, K a, and relative bioavailability were estimated using the traditional pharmacokinetic methods and were compared by using the paired t-test. Result: In the present study, Products A and B showed their T max , C max , AUC 0-24 , AUC 0- ∞, MRT, and K a values as 2.5 h, 2589 ± 54.79 ng/ml, 9623 ± 112.87 ng.h/ml, 9586 ± 126.22 ng.h/ml, 3.6 ± 0.10 h, and 0.3698 ± 0.003 h -1 for Product A and 3.0 h, 2054 ± 55.79 ng/ml, 9637 ± 132.87 ng.h/ml, 9870 ± 129.22 ng.h/ml, 4.76 ± 0.10 h, and 0.3812 ± 0.002 h -1 for Product B, respectively. Conclusion: The results of the paired t-test of pharmacokinetics data showed that there was no significant difference between Products A and B. From both the in vitro dissolution studies and in vivo bioavailability studies it was concluded that products A and B had similar bioavailability.

  6. Assessing gastrointestinal motility and disintegration profiles of magnetic tablets by a novel magnetic imaging device and gamma scintigraphy.

    Science.gov (United States)

    Goodman, Kirsteen; Hodges, Lee Ann; Band, Janet; Stevens, Howard N E; Weitschies, Werner; Wilson, Clive G

    2010-01-01

    To validate Magnetic Moment Imaging (MMI) for the investigation of gastrointestinal transit and disintegration of solid dosage forms and to correlate the MMI findings with the corresponding gamma scintigraphic data. Three magnetic tablets (MTs) were investigated using in vitro and in vivo tests. The clinical study was a four-way, crossover study with the following arms: (a) immediate-release tablets administered in fasted state; (b) immediate-release tablets administered after 400mL of Clinutren ISO; (c) enteric-coated tablets administered in the fasted state; and (d) non-disintegrating tablets studied in the lightly fed state (100mL of Clinutren ISO). In both the in vitro and in vivo studies, tablets were detected successfully by MMI and scintigraphy. There was a good correlation between gastric residence times and positional data (in the x, y and y, z-axes). In addition, MMI revealed early swelling behaviour of the tablet matrix. There was excellent agreement for the disintegration times of MT(A) in the fasted arm (scintigraphy 12.0+/-4.4min, MMI 11.8+/-4.4min). In the MT(A)-fed arm, onset times determined by scintigraphy were delayed in three subjects when compared to the corresponding MMI results. Delayed disintegration was observed with MT(A) administered after food (pdisintegration of a magnetic tablet through the gastrointestinal tract. Copyright 2009 Elsevier B.V. All rights reserved.

  7. Development and evaluation of Ketoprofen sustained release matrix tablet using Hibiscus rosa-sinensis leaves mucilage

    Directory of Open Access Journals (Sweden)

    M. Kaleemullah

    2017-07-01

    Full Text Available Currently, the use of natural gums and mucilage is of increasing importance in pharmaceutical formulations as valuable drug excipient. Natural plant-based materials are economic, free of side effects, biocompatible and biodegradable. Therefore, Ketoprofen matrix tablets were formulated by employing Hibiscus rosa-sinensis leaves mucilage as natural polymer and HPMC (K100M as a synthetic polymer to sustain the drug release from matrix system. Direct compression method was used to develop sustained released matrix tablets. The formulated matrix tablets were evaluated in terms of physical appearance, weight variation, thickness, diameter, hardness, friability and in vitro drug release. The difference between the natural and synthetic polymers was investigated concurrently. Matrix tablets developed from each formulation passed all standard physical evaluation tests. The dissolution studies of formulated tablets revealed sustained drug release up to 24 h compared to the reference drug Apo Keto® SR tablets. The dissolution data later were fitted into kinetic models such as zero order equation, first order equation, Higuchi equation, Hixson Crowell equation and Korsmeyer-Peppas equation to study the release of drugs from each formulation. The best formulations were selected based on the similarity factor (f2 value of 50% and more. Through the research, it is found that by increasing the polymers concentration, the rate of drug release decreased for both natural and synthetic polymers. The best formulation was found to be F3 which contained 40% Hibiscus rosa-sinensis mucilage polymer and showed comparable dissolution profile to the reference drug with f2 value of 78.03%. The release kinetics of this formulation has shown to follow non-Fickian type which involved both diffusion and erosion mechanism. Additionally, the statistical results indicated that there was no significant difference (p > 0.05 between the F3 and reference drug in terms of MDT and

  8. Development and evaluation of Ketoprofen sustained release matrix tablet using Hibiscus rosa-sinensis leaves mucilage.

    Science.gov (United States)

    Kaleemullah, M; Jiyauddin, K; Thiban, E; Rasha, S; Al-Dhalli, S; Budiasih, S; Gamal, O E; Fadli, A; Eddy, Y

    2017-07-01

    Currently, the use of natural gums and mucilage is of increasing importance in pharmaceutical formulations as valuable drug excipient. Natural plant-based materials are economic, free of side effects, biocompatible and biodegradable. Therefore, Ketoprofen matrix tablets were formulated by employing Hibiscus rosa-sinensis leaves mucilage as natural polymer and HPMC (K100M) as a synthetic polymer to sustain the drug release from matrix system. Direct compression method was used to develop sustained released matrix tablets. The formulated matrix tablets were evaluated in terms of physical appearance, weight variation, thickness, diameter, hardness, friability and in vitro drug release. The difference between the natural and synthetic polymers was investigated concurrently. Matrix tablets developed from each formulation passed all standard physical evaluation tests. The dissolution studies of formulated tablets revealed sustained drug release up to 24 h compared to the reference drug Apo Keto® SR tablets. The dissolution data later were fitted into kinetic models such as zero order equation, first order equation, Higuchi equation, Hixson Crowell equation and Korsmeyer-Peppas equation to study the release of drugs from each formulation. The best formulations were selected based on the similarity factor ( f 2 ) value of 50% and more. Through the research, it is found that by increasing the polymers concentration, the rate of drug release decreased for both natural and synthetic polymers. The best formulation was found to be F3 which contained 40% Hibiscus rosa-sinensis mucilage polymer and showed comparable dissolution profile to the reference drug with f 2 value of 78.03%. The release kinetics of this formulation has shown to follow non-Fickian type which involved both diffusion and erosion mechanism. Additionally, the statistical results indicated that there was no significant difference (p > 0.05) between the F3 and reference drug in terms of MDT and T50% with p

  9. Ghost tablet in feces.

    Science.gov (United States)

    Iwamuro, Masaya; Morishita, Yosuke; Urata, Haruo; Okada, Hiroyuki

    2017-12-01

    Recently, we encountered a female patient who identified the presence of a ghost tablet in her fecal matter. Interestingly, although the patient was prescribed potassium chloride capsules, elemental composition analysis by energy-dispersive X-ray spectroscopy was unable to detect the presence of either potassium or chloride in the fecal tablet remnant.

  10. 21 CFR 520.812 - Enrofloxacin tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Enrofloxacin tablets. 520.812 Section 520.812 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.812 Enrofloxacin tablets. (a) Specifications. Each tablet contains either 22.7, 68.0, or 136.0 milligrams of enrofloxacin. (b) Sponsor. See No...

  11. Steady-state pharmacokinetics of fluvastatin in healthy subjects following a new extended release fluvastatin tablet, Lescol XL.

    Science.gov (United States)

    Barilla, Denise; Prasad, Pratapa; Hubert, Martine; Gumbhir-Shah, Kavita

    2004-03-01

    This was an open-label, randomized, three-period, three-treatment, multiple dose, crossover study in 12 healthy male and female subjects. This study evaluated single dose and steady-state pharmacokinetics of fluvastatin following single and multiple dose administrations of a new extended release fluvastatin 8 h matrix tablet, Lescol XL 80 mg and 160 mg doses once a day. The study also included a twice a day administration of an immediate release (IR) form of fluvastatin capsule, Lescol, for comparative purposes. All doses were administered for 7 days. The safety and tolerability were also assessed. The pharmacokinetics of fluvastatin were evaluated on days 1 and 7 following each treatment. Fluvastatin systemic exposure was 50% less when administered as Lescol XL 80 mg qd compared with Lescol IR 40 mg bid. Conversely, fluvastatin systemic exposure was 22% higher when administered as Lescol XL 160 mg qd compared with Lescol IR 40 mg bid. Single doses of Lescol XL 80 mg and 160 mg were dose proportional but, deviation (30%) from dose proportionality was observed for the Lescol XL 160 mg at steady-state. There appeared to be moderate (20%-40%) accumulation of serum fluvastatin maximal concentrations and exposure after multiple doses of Lescol XL tablets. Both Lescol XL 80 mg and 160 mg showed delayed absorption and longer apparent elimination half-life compared with fluvastatin IR capsule. Single and multiple doses of fluvastatin were generally well tolerated in this healthy volunteer population. Adverse event profiles were consistent with the published safety profile of the marketed formulations. Aside from one incidence of creatine phosphokinase (CPK) elevation (following Lescol XL 160 mg qd treatment), there were no safety concerns with any of the treatments when administered acutely (7 days). Copyright 2004 John Wiley & Sons, Ltd.

  12. Understanding and optimizing the dual excipient functionality of sodium lauryl sulfate in tablet formulation of poorly water soluble drug: wetting and lubrication.

    Science.gov (United States)

    Aljaberi, Ahmad; Chatterji, Ashish; Dong, Zedong; Shah, Navnit H; Malick, Waseem; Singhal, Dharmendra; Sandhu, Harpreet K

    2013-01-01

    To evaluate and optimize sodium lauryl sulfate (SLS) and magnesium stearate (Mg.St) levels, with respect to dissolution and compaction, in a high dose, poorly soluble drug tablet formulation. A model poorly soluble drug was formulated using high shear aqueous granulation. A D-optimal design was used to evaluate and model the effect of granulation conditions, size of milling screen, SLS and Mg.St levels on tablet compaction and ejection. The compaction profiles were generated using a Presster(©) compaction simulator. Dissolution of the kernels was performed using a USP dissolution apparatus II and intrinsic dissolution was determined using a stationary disk system. Unlike kernels dissolution which failed to discriminate between tablets prepared with various SLS contents, the intrinsic dissolution rate showed that a SLS level of 0.57% was sufficient to achieve the required release profile while having minimal effect on compaction. The formulation factors that affect tablet compaction and ejection were identified and satisfactorily modeled. The design space of best factor setting to achieve optimal compaction and ejection properties was successfully constructed by RSM analysis. A systematic study design helped identify the critical factors and provided means to optimize the functionality of key excipient to design robust drug product.

  13. 'Tablet burden' in patients with metastatic breast cancer.

    Science.gov (United States)

    Milic, Marina; Foster, Anna; Rihawi, Karim; Anthoney, Alan; Twelves, Chris

    2016-03-01

    The implications for patients with cancer, of the 'tablet burden' resulting from increasing use of oral anticancer drugs and medication for co-morbidities have not previously been well explored. We sought to (i) quantify tablet burden in women with metastatic breast cancer (MBC), (ii) establish which groups of drug contribute most to this burden and (iii) gain insight into patients' attitudes towards oral anti-cancer treatment. One hundred patients with MBC anonymously completed a questionnaire describing their medication histories and attitudes towards their tablets. The patients (mean age 60, range 31-95) were all female and taking a median of six tablets (range 0-31) daily; 37 patients were taking >10 tablets. Oral anticancer treatment constituted the category of treatment taken by the highest proportion of patients, followed by symptomatic cancer treatments, proton pump inhibitors and cardiovascular medication. Numerically, however, symptomatic drugs accounted for 44% of all tablets and specific anti-cancer treatment for 15%; medication not directly related to the cancer accounted for the remaining 40% of tablets. A quarter of patients reported inconvenience in taking their tablets, the main reason being tablet size and one third reported forgetting their tablets at least once a week. Nearly two thirds of patients expressing a preference favoured oral anticancer treatment, the commonest reason being greater convenience. Tablet burden is considerable for many patients with MBC and can be problematic. A significant proportion of tablets represent treatment for co-morbidities, the significance of which may be questionable in women with MBC. Copyright © 2015 Elsevier Ltd. All rights reserved.

  14. Tablet telerounding.

    Science.gov (United States)

    Kaczmarek, Bartosz F; Trinh, Quoc-Dien; Menon, Mani; Rogers, Craig G

    2012-12-01

    To evaluate the feasibility of remote rounding using commercially available standard tablets with videoconferencing system and assess patient satisfaction. Thirty-two patients with at least 2 postoperative days of hospital stay after robotic urologic procedures were included in the study. On the first postoperative day, the physician-patient encounter was performed as telerounding with videoconferencing due to the physician's duties scheduled in another affiliated hospital. On the second day, the personal bedside encounter took place. The tablet we used was an iPad2 (Apple, iOS 5.1; Apple, Cupertino, CA) with a videoconferencing application. A telerounding satisfaction survey was fulfilled by all patients on the touchscreen of the tablet. Average time of telerounding encounter was 4.5 minutes (range, 1.0-13.5 minutes), average age of the patient was 57.7 years (range, 19-80 years), and 19 were men (59%). Patients expressed a high level of satisfaction with 91% of patients stating that their care was better using telerounding and 97% of patients stating that telerounding should be a regular part of patient care in the hospital. Additionally, 94% of patients stated that they could easily communicate with their doctor over the telerounding system, 84% of patients agreed that they would feel comfortable with telerounding daily if they were hospitalized again and 81% of patients would prefer telerounding communication with their doctor than be directly seen by another doctor. Tablet telerounding using videoconferencing can be a strong supplementing tool in doctor-patient communication. It is convenient for the physician and increases the patient's hospital stay satisfaction. Copyright © 2012 Elsevier Inc. All rights reserved.

  15. Correlation of ibuprofen bioavailability with gastrointestinal transit by scintigraphic monitoring of 171Er-labeled sustained-release tablets

    International Nuclear Information System (INIS)

    Parr, A.F.; Beihn, R.M.; Franz, R.M.; Szpunar, G.J.; Jay, M.

    1987-01-01

    External gamma scintigraphy was used to monitor the gastrointestinal (GI) transit of radiolabeled sustained-release tablets containing 800 mg ibuprofen in eight fasted healthy volunteers. Ibuprofen serum concentrations were determined from blood samples drawn sequentially over a 24-hr period. Serum concentrations and related parameters were correlated to the position of the dosage form in the GI tract from the scintiphotos. The sustained-release tablets were radiolabeled intact utilizing a neutron activation procedure, by incorporating 0.18% of 170 Er2O3 (enriched to greater than 96% 170 Er) into the bulk formulation. After manufacture of the final dosage forms, the tablets were irradiated in a neutron flux (4.4 x 10(13) n/cm2.sec) for 2 min, converting the stable 170 Er to radioactive 171 Er (t1/2 = 7.5 hr). Each tablet contained 50 microCi of 171 Er at the time of administration. The scintigraphy studies suggested that the greatest proportion of ibuprofen was absorbed from this dosage form while the tablet was in the large bowel. The dosage forms eroded slowly in the small bowel and appeared to lose their integrity in the large bowel. In vitro studies showed only minimal effects of the neutron irradiation procedure on the dosage form performance

  16. Principles of Tablet Computing for Educators

    Science.gov (United States)

    Katzan, Harry, Jr.

    2015-01-01

    In the study of modern technology for the 21st century, one of the most popular subjects is tablet computing. Tablet computers are now used in business, government, education, and the personal lives of practically everyone--at least, it seems that way. As of October 2013, Apple has sold 170 million iPads. The success of tablets is enormous and has…

  17. Comparative pharmacokinetics of two modified-release oral morphine formulations (Reliadol® and Kapanol®) and an immediate-release morphine tablet (Morfin 'DAK') in healthy volunteers

    DEFF Research Database (Denmark)

    Bochner, F.; Somogyi, A.A.; Danz, C.

    1999-01-01

    , its metabolites morphine-6-glucuronide (M6G) and morphine-3-glucuronide (M3G), after ingestion of Reliadol® (2 x 30 mg capsules) compared with Kapanolo (3 x 20 mg) [Glaxo Wellcome Australia Ltd] and an immediate-release morphine tablet (Morfin 'DAK', 30 mg; Nycomed Denmark A/S). Design and Setting...

  18. Using Tablet on Education

    Science.gov (United States)

    Algoufi, Rateeba

    2016-01-01

    Technological advancements in digital devices have made educational methodology to adopt new strategies and procedures to suit the Mobile learning era. Mobile devices such as tablets are growing to be the focus of research studies and educational use around the globe in the present day. With the influence of handy computing tablets in the hands of…

  19. A randomized, double-blind study of hydromorphone hydrochloride extended-release tablets versus oxycodone hydrochloride extended-release tablets for cancer pain: efficacy and safety in Japanese cancer patients (EXHEAL: a Phase III study of EXtended-release HydromorphonE for cAncer pain reLief

    Directory of Open Access Journals (Sweden)

    Inoue S

    2017-08-01

    Full Text Available Satoshi Inoue,1 Yoji Saito,2 Satoru Tsuneto,3 Etsuko Aruga,4 Azusa Ide,1 Yasuyuki Kakurai5 1Clinical Development Department, R&D Division, Daiichi Sankyo, Tokyo,2Department of Anesthesiology, Faculty of Medicine, Shimane University, Shimane, 3Human Health Sciences, Graduate School of Medicine, Kyoto University, Kyoto, 4Department of Palliative Medicine, School of Medicine, Teikyo University, Tokyo, 5Biostatistics and Data Management Department, R&D Division, Daiichi Sankyo, Tokyo, Japan Background: In Japan, there are limited options for switching opioid analgesics. Hydromorphone is an opioid analgesic that is routinely used instead of morphine for cancer pain; however, it is not yet available in Japan. The aim of this study was to assess the efficacy and safety of hydromorphone (DS-7113b extended-release tablets in opioid-naïve patients with cancer pain not relieved by non-opioid analgesics.Subjects and methods: This was a multicenter, randomized, double-blind, parallel-group trial. A double-dummy method was used for blinding. Each randomized subject received either hydromorphone extended-release tablets plus placebo oxycodone hydrochloride extended-release tablets 4 mg/day (n=88 or placebo hydromorphone extended-release tablets plus oxycodone hydrochloride extended-release tablets 10 mg/day (n=93 orally for 7 days (once-daily dosing for hydromorphone and twice-daily dosing for oxycodone. The doses were adjusted as necessary. Efficacy was evaluated by change in visual analog scale (VAS score from baseline to completion of treatment.Results: The between-group difference in least squares mean changes in VAS score from baseline to completion or discontinuation of treatment was −0.4 mm (95% CI −5.9 to 5 mm by analysis of covariance where the baseline VAS score was used as a covariate. The upper limit of the 95% CI was below 10 mm, which was predefined as the noninferiority limit. This verified the noninferiority of hydromorphone tablets

  20. Evaluation of tableting and tablet properties of Kollidon SR: the influence of moisture and mixtures with theophylline monohydrate.

    Science.gov (United States)

    Hauschild, Karsten; Picker-Freyer, Katharina M

    2006-02-01

    The aim of the study was firstly to investigate the influence of moisture on the tableting and tablet properties of Kollidon SR and secondly to investigate the influence of theophylline monohydrate on the tableting behavior and tablet properties produced from binary mixtures with Kollidon SR. In comparison to Kollidon SR, microcrystalline cellulose (MCC) was used. The glass transition temperature (Tg) of the powder over the whole range of RH (0-90%), and in addition, the Tg of tablets of Kollidon SR were measured. Densities and flowability of the powders were analyzed. The tablets were produced at five different maximum relative densities (rho(rel), max) on an instrumented eccentric tableting machine. They were produced at three different relative humidities (RH), 30%, 45%, and 60% RH for the pure substances and binary mixtures with different ratios of drug and excipient were tableted at 45% RH. The tableting properties were analyzed by 3D modeling, force-displacement profiles, and compactibility plots. First, the Tg of the powder decreased with increasing RH and the Tg of the tablet was 4-8 K lower than the powder. The predominant deformation of Kollidon SR is plastic deformation and Kollidon SR showed a higher compactibility than MCC. The parameters of the 3D model showed an extreme change between 45 and 60% RH, and at higher RH more and more particles deformed elastically. This was confirmed by analysis of force-displacement profiles. At 60% RH, the radial tensile strength of the Kollidon SR tablets was half of the radial tensile strength at 45% RH. The reason is a higher relative energy of plastic deformation than for MCC. This results in a better utilization of the energy to deform the powder into a tablet and the exceeding of the glass transition temperature at higher RH. In conclusion, at 60% RH at the same rho(rel, max), tableting and tablet properties of Kollidon SR are extremely changed since plasticity is significantly higher. In the second part of the

  1. Tablet-Aided BehavioraL intervention EffecT on Self-management skills (TABLETS) for Diabetes.

    Science.gov (United States)

    Lynch, Cheryl P; Williams, Joni S; J Ruggiero, Kenneth; G Knapp, Rebecca; Egede, Leonard E

    2016-03-22

    Multiple randomized controlled trials (RCTs) show that behavioral lifestyle interventions are effective in improving diabetes management and that comprehensive risk factor management improves cardiovascular disease (CVD) outcomes. The role of technology has been gaining strong support as evidence builds of its potential to improve diabetes management; however, evaluation of its impact in minority populations is limited. This study intends to provide early evidence of a theory-driven intervention, Tablet-Aided BehavioraL intervention EffecT on Self-management skills (TABLETS), using real-time videoconferencing for education and skills training. We examine the potential for TABLETS to improve health risk behaviors and reduce CVD risk outcomes among a low-income African American (AA) population with poorly controlled type 2 diabetes. The study is a two-arm, pilot controlled trial that randomizes 30 participants to the TABLETS intervention and 30 participants to a usual care group. Blinded outcome assessments will be completed at baseline, 2.5 months (immediate post-intervention), and 6.5 months (follow-up). The TABLETS intervention consists of culturally tailored telephone-delivered diabetes education and skills training delivered via videoconferencing on tablet devices, with two booster sessions delivered via tablet-based videoconferencing at 3 months and 5 months to stimulate ongoing use of the tablet device with access to intervention materials via videoconferencing slides and a manual of supplementary materials. The primary outcomes are physical activity, diet, medication adherence, and self-monitoring behavior, whereas the secondary outcomes are HbA1c, low-density lipoprotein cholesterol (LDL-C), BP, CVD risk, and quality of life. This study provides a unique opportunity to assess the feasibility and efficacy of a theory-driven, tablet-aided behavioral intervention that utilizes real-time videoconferencing technology for education and skills training on self

  2. Dissolution test for glibenclamide tablets

    Directory of Open Access Journals (Sweden)

    Elisabeth Aparecida dos Santos Gianotto

    2007-10-01

    Full Text Available The aim of this work is to develop and validate a dissolution test for glibenclamide tablets. Optimal conditions to carry out the dissolution test are 500 mL of phosphate buffer at pH 8.0, paddles at 75 rpm stirring speed, time test set to 60 min and using equipment with six vessels. The derivative UV spectrophotometric method for determination of glibenclamide released was developed, validated and compared with the HPLC method. The UVDS method presents linearity (r² = 0.9999 in the concentration range of 5-14 µg/mL. Precision and recoveries were 0.42% and 100.25%, respectively. The method was applied to three products commercially available on the Brazilian market.

  3. Fabrication and interface electrical properties of Fe3O4/MgO/GaAs(100) spin contacts

    NARCIS (Netherlands)

    Wong, P.K.J.; Zhang, W.; Zhang, W.; Xu, Y.B.

    2010-01-01

    Moderately doped n-GaAs(100) substrates (n= 5 x 10 17cm3 ) with In Ohmic back contacts were annealed in the growth chamber with a base pressure of 1 x 10-8 mbar for 60 min at 830 K prior to the film stack growth. MgO layer was then grown by e-beam evaporation at a rate of 2 Amin-1 while the

  4. Emergency CT brain: preliminary interpretation with a tablet device: image quality and diagnostic performance of the Apple iPad.

    LENUS (Irish Health Repository)

    Mc Laughlin, Patrick

    2012-04-01

    Tablet devices have recently been used in radiological image interpretation because they have a display resolution comparable to desktop LCD monitors. We identified a need to examine tablet display performance prior to their use in preliminary interpretation of radiological images. We compared the spatial and contrast resolution of a commercially available tablet display with a diagnostic grade 2 megapixel monochrome LCD using a contrast detail phantom. We also recorded reporting discrepancies, using the ACR RADPEER system, between preliminary interpretation of 100 emergency CT brain examinations on the tablet display and formal review on a diagnostic LCD. The iPad display performed inferiorly to the diagnostic monochrome display without the ability to zoom. When the software zoom function was enabled on the tablet device, comparable contrast detail phantom scores of 163 vs 165 points were achieved. No reporting discrepancies were encountered during the interpretation of 43 normal examinations and five cases of acute intracranial hemorrhage. There were seven RADPEER2 (understandable) misses when using the iPad display and 12 with the diagnostic LCD. Use of software zoom in the tablet device improved its contrast detail phantom score. The tablet allowed satisfactory identification of acute CT brain findings, but additional research will be required to examine the cause of "understandable" reporting discrepancies that occur when using tablet devices.

  5. Pharmacokinetic comparison and bioequivalence evaluation of losartan/ hydrochlorothiazide tablet between Asian Indian and Japanese volunteers.

    Science.gov (United States)

    Kumar, Sudershan; Monif, Tausif; Khuroo, Arshad; Reyar, Simrit; Jain, Rakesh; Singla, Ajay K; Kurachi, Kazuya

    2014-01-01

    To demonstrate the bioequivalence between the test and reference formulations of losartan/hydrochlorothiazide 50 + 12.5 mg tablet and evaluate the effect of ethnicity on pharmacokinetics properties of losartan, losartan carboxylic acid and hydrochlorothiazide on healthy Asian Indian and Japanese volunteers. Randomized, open-label, crossover, bioavailability studies were conducted separately in healthy Asian Indian and Japanese volunteers. One tablet either of test or of reference product was administered after 10 hours of overnight fasting. After dosing, serial blood samples were collected for a period of 48 hours for both the studies. Plasma samples were analyzed for losartan, losartan carboxylic acid and hydrochlorothiazide by a validated liquid chromatographic and mass spectrometric method (LC-MS/MS). The pharmacokinetic parameters AUC0-t, AUC0-∞, Cmax, tmax, and other pharmacokinetics parameters were determined from plasma concentration-time profiles for both test and reference formulations of losartan/hydrochlorothiazide 50 + 12.5 mg tablets. Statistical evaluations were done to evaluate bioequivalence between generic test formulation (EPR0001) and Japanese reference product (Preminent®). Losartan, losartan carboxylic acid and hydrochlorothiazide were well tolerated by subjects in all periods of each study under fasted conditions. No serious adverse events were observed. The ratios of least square means for AUC0-t and Cmax and the affiliated 90% confidence intervals were within acceptance range recommended by PMDA. Marginal differences were observed in pharmacokinetic values of Asian Indian and Japanese volunteers. The results of these bioavailability studies indicate that the test formulation of losartan/hydrochlorothiazide 50 + 12.5 mg (EPR0001) tablets is bioequivalent to marketed Preminent® reference formulation in Asian Indian and Japanese volunteers, when administered under fasting conditions. Both test and reference formulations were well tolerated

  6. The advantages of combination therapy on hypertension: development of immediate release perindopril-indapamide tablet and assessment of bioequivalence studies.

    Science.gov (United States)

    Ölçer, A; Ölçer, M; İnce, I; Karasulu, E

    2016-03-01

    Hypertension has a major associated risk for organ damage and mortality, which is further heightened in patients with prior cardiovascular events, comorbid diabetes mellitus, microalbuminuria and renal impairment. Convers Plus tablet including perindopril erbumine (PE), which is an angiotensin converting enzyme (ACE) inhibitor, and indapamide, which is diuretic, was designed as a combined tablet to succes in the treatment of hypertension. Physico-pharmaceutical properties and characterization studies were evaluated in vitro conditions. Later on in vivo study was planned as a cross-designed, randomized, open-labeled, single-dose, single-center study via peroral route in 24 healthy male subjects. In this study, bioequivalence with primary pharmacokinetical target parameters reference (Bipreterax 4/1.25 mg Tablet-S.A.Servier Benelux N.V.) and test (Convers Plus 4/1.25 mg Tablet-ARGESAN Pharmaceutical Company) tablets have been found bioequivalent. The results of pharmacokinetic parameters for perindopril, perindoprilat and indapamide were found as Cmax = 23.179 µg/mL, tmax = 0.729 h, t1/2 = 1.429 h; AUC0-t = 26.998 µgs/mL, AUC0-inf = 27.117 µgs/mL; Cmax = 1.834 µg/mL, tmax = 8.792 h, t1/2 = 40.699 h; AUC0-t = 54.828 µgs/mL, AUC0-inf = 77.113 µgs/mL; Cmax = 18.994 µg/mL, tmax = 3.417 h, t1/2 = 16.626 h and AUC0-t = 385.829 µgs/mL, AUC0-inf = 410.728 µgs/mL respectively. In conclusion, physico-pharmaceutical properties and results of clinical trials show that Convers Plus tablets have been found as bioequivalent for perindopril, perindoprilat and indapamide in terms of AUC and Cmax, in 90% confidence limits.

  7. Comparison of cortisol exposures and pharmacodynamic adrenal steroid responses to hydrocortisone suspension vs. commercial tablets.

    Science.gov (United States)

    Sarafoglou, Kyriakie; Gonzalez-Bolanos, Maria T; Zimmerman, Cheryl L; Boonstra, Timothy; Yaw Addo, O; Brundage, Richard

    2015-04-01

    The Endocrine Society Clinical Practice Guidelines on congenital adrenal hyperplasia (CAH) recommend against using hydrocortisone suspension based on a study that examined a commercial suspension. Our objective was to examine the absorption of an extemporaneously prepared hydrocortisone suspension and compare it to tablets. Secondary objectives were to evaluate the 17-hydroxyprogesterone and androstenedione adrenal steroid responses. Using a parallel design, 34 children diagnosed with CAH received either suspension (n = 9; median age 1.8 years) or tablets (n = 25; median age 7.5 years). Patients were given their usual morning hydrocortisone formulation and dose; 12 serial blood samples were obtained and the area under the curve (AUC) was calculated. The mg/m(2) dose-normalized cortisol AUCs were no different in the suspension and tablet groups (P = ·06), nor was there a significant difference in the C(max) or T(max) (P = .08 and P = .41, respectively). Although there were no differences in the 17-hydroxyprogesterone change-from-baseline AUCs, baseline concentrations, or the nadir concentrations when comparing suspension and tablet formulations, the androstenedione values were significantly lower as expected in the younger aged suspension group. Our results offer compelling evidence that an extemporaneously prepared hydrocortisone suspension provides comparable cortisol exposures to commercially available tablet formulations in children and can be used to safely and effectively treat CAH. © 2014, The American College of Clinical Pharmacology.

  8. 21 CFR 520.434 - Chlorphenesin carbamate tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Chlorphenesin carbamate tablets. 520.434 Section 520.434 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Chlorphenesin carbamate tablets. (a) Specifications. Each tablet contains 400 milligrams of chlorphenesin...

  9. Stage control of tablets manufacturing

    Directory of Open Access Journals (Sweden)

    L. I. Kucherenko

    2014-08-01

    Full Text Available Today in Ukraine tuberculosis is the wide-spread infectious disease causing the death in most cases; about 700 thousand persons are suffering from it. In Ukraine epidemic of tuberculosis is progressing and spreading. In spite of all protective measures three inhabitants of our country contract tuberculosis per hour, every hour one patient dies and in common about 1.5% of the population is ill with tuberculosis. Isoniazid is antituberculous drug of the first line and it is the most effective one. Chemotherapy of tuberculosis requests long-lasting administration of antituberculous drugs that causes high risk of side effects. To prevent or lessen side effects of antituberculous medicines antioxidants use in complex therapy is perspective. Fulfilled investigations showed efficacy of combining two medical substances – isoniazid andthiotriazolin – in one dosage form. Objective.The aim of our investigation is working out the methods of standardization, in particularquantitative determination of isoniazid andthiotriazolin content in tablet mass by high-performance liquid chromatography (HPLC. Materials and Methods.During in-process investigations combined tableted remedy containing isoniazid andthiotriazolin and proper amount of adjuvants has been developed (it contains active substances isoniazid – 0.2 g,thiotriazolin – 0.05 g and adjuvants up to the 0.4 g of the tablet. During stage control of tablets manufacturingspecial attention is paid to the control of tablet mass quality. Especially it concerns quantitative determination of active substances in it. More and more attention is paid to modern physical-chemical methods of standardization in up-to-date analysis of drug products, such as ultraviolet spectrometry, high-performance liquid chromatography (HPLC etc. In previous scientific investigations we proved the possibility of standardization of active substances artificial compound by HPLC method and optimal conditions of analysis performing

  10. Oral sustained release tablets of zidovudine using binary blends of natural and synthetic polymers.

    Science.gov (United States)

    Emeje, Martins; Olaleye, Olajide; Isimi, Christiana; Fortunak, Joseph; Byrn, Stephen; Kunle, Olobayo; Ofoefule, Sabinus

    2010-01-01

    Oral sustained release matrix tablets of zidovudine (ZDV) were prepared using different types, proportions and blends of carbopol 71G (C71) and a plant gum obtained from Abelmoschus esculentus (AEG). The effect of various formulation factors like polymer proportion, polymer type and pH of the dissolution medium on the in vitro release of the drug was studied, using the half change technique, in 900 ml of dissolution medium, at 100 rpm. Release kinetics were analyzed using Zero-order, Higuchi's square-root and Ritger-Peppas' empirical equations. In vitro release performance as revealed by the time taken for 70% of the drug to be released (t70%), showed that the release rate decreased with increase in polymer proportion. Matrix tablets containing 10 and 20% AEG were found to exhibit immediate-release characteristics. Matrix tablets containing 30% AEG showed t70% value of 204 min and extended the release up to 5 h, while matrix tablets containing 30% carbopol showed t70% value of 234 min and extended the release up to 6 h. Three blends of AEG and C71 at the ratio of 1:2, 2:1 and 1:3 showed t70% values of 132, 312 and 102 min respectively and extended the release up to 8 h. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets followed Fickian and anomalous release. Drug release from matrix tablets of zidovudine containing blends of AEG and C71 demonstrates the advantage of blending a natural and synthetic polymer over single polymer use.

  11. Terahertz Technology: A Boon to Tablet Analysis

    Science.gov (United States)

    Wagh, M. P.; Sonawane, Y. H.; Joshi, O. U.

    2009-01-01

    The terahertz gap has a frequency ranges from ∼0.3 THz to ∼10 THz in the electromagnetic spectrum which is in between microwave and infrared. The terahertz radiations are invisible to naked eye. In comparison with x-ray they are intrinsically safe, non-destructive and non-invasive. Terahertz spectroscopy enables 3D imaging of structures and materials, and the measurement of the unique spectral fingerprints of chemical and physical forms. Terahertz radiations are produced by a dendrimer based high power terahertz source and spectroscopy technologies. It resolves many of the questions left unanswered by complementary techniques, such as optical imaging, Raman and infrared spectra. In the pharmaceutical industries it enables nondestructive, internal, chemical analysis of tablets, capsules, and other dosage forms. Tablet coatings are a major factor in drug bioavailability. Therefore tablet coatings integrity and uniformity are of crucial importance to quality. Terahertz imaging gives an unparalleled certainty about the integrity of tablet coatings and the matrix performance of tablet cores. This article demonstrates the potential of terahertz pulse imaging for the analysis of tablet coating thickness by illustrating the technique on tablets. PMID:20490288

  12. Bioavailability of isoniazid, rifampicin and pyrazinamide (in free combination or fixed-triple formulation) in intermittent antituberculous chemotherapy.

    Science.gov (United States)

    Acocella, G; Luisetti, M; Grassi, G G; Peona, V; Pozzi, E; Grassi, C

    1993-01-01

    A study was carried out in six human volunteers, to assess the blood kinetics of isoniazid, rifampicin and pyrazinamide, administered in a fixed-triple combination intended for use in intermittent chemotherapy of tuberculosis. The formulation employed contained 125 mg of isoniazid (H), 100 mg of rifampicin (R) and 375 mg of pyrazinamide (Z) per tablet; six tablets were administered to every subject, giving a total dosage of 750 mg of isoniazid, 600 mg of rifampicin and 2,250 mg of pyrazinamide. In each subject, the same dose of each drug was administered individually in separate sessions and the results compared. The results indicated that, at the level of dose of the intermittent tablet, no negative interactions between the drugs were observed.

  13. Simultaneous determination of andrographolide, dehydroandrographolide and neoandrographolide in dog plasma by LC-MS/MS and its application to a dog pharmacokinetic study of Andrographis paniculata tablet.

    Science.gov (United States)

    Xu, Fang-fang; Fu, Shu-jun; Gu, Sheng-pan; Wang, Zhi-min; Wang, Zhen-zhong; He, Xin; Xiao, Wei

    2015-05-15

    In this study, a sensitive and rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated to simultaneously determinate andrographolide (AP), dehydroandrographolide (DP), and neoandrographolide (NP) in plasma of beagle dogs after oral administration of Andrographis paniculata tablet (A. paniculata). The analytes and bilobalide (internal standard) were separated on an Agilent ZORBAX XDB-C18 column (50mm×2.1mm, 3.5μm) by using gradient elution consisting of methanol and water at a flow rate of 0.50mL/min in 7min. Multiple reaction monitoring (MRM) mode was performed to quantify data under monitoring precursor-product ion transitions of m/z 348.8→286.9, 330.9→107.9, 479.1→160.8 and 325.0→163.0 for AP, DP, NP and internal standard (IS) at negative ion mode, respectively. This method was developed at linearity ranging from 0.50 to 250ng/mL for AP, 1.00 to 500ng/mL for DP and 0.20 to 100ng/mL for NP. The accuracy of each analyte ranged between 94.8% and 107.1% and the precision was within 14.6%. No significant matrix effect was observed. AP, DP and NP were stable during sample storage, preparation and analytic procedures. Furthermore, this method was successfully applied in the investigation of the pharmacokinetic profile of AP, DP and NP in beagle dogs after oral administration of A. paniculata tablet (49.5mg for AP, 7.0mg for DP, 22.0mg for NP). Biological half-life (t1/2) was 2.08±0.99, 3.13±1.19 and 1.07±0.38h for AP, DP and NP, respectively. The areas under curves (AUC0-t) of AP, DP and NP was 494.50±150.64, 26.01±8.72 and 78.78±18.29ngh/mL, respectively. Copyright © 2015 Elsevier B.V. All rights reserved.

  14. Gastric emptying of enteric-coated tablets

    International Nuclear Information System (INIS)

    Park, H.M.; Chernish, S.M.; Rosenek, B.D.; Brunelle, R.L.; Hargrove, B.; Wellman, H.N.

    1984-01-01

    To evaluate the gastric emptying time of pharmaceutical dosage forms in a clinical setting, a relatively simple dual-radionuclide technique was developed. Placebo tablets of six different combinations of shape and size were labeled with indium-111 DTPA and enteric coated. Six volunteers participated in a single-blind and crossover study. Tablets were given in the morning of a fasting stomach with 6 oz of water containing /sup 99m/Tc pertechnetate and continuously observed with a gamma camera. A scintigraph was obtained each minute. The results suggested that the size, shape, or volume of the tablet used in this study had no significant effect in the rate of gastric emptying. The tablets emptied erratically and unpredictably, depending upon their time of arrival in the stomach in relation to the occurrence of interdigestive myoelectric contractions. The method described is a relatively simple and accurate technique to allow one to follow the gastric emptying of tablets

  15. Iodine tablets and a nuclear accident

    International Nuclear Information System (INIS)

    Paile, W.

    1992-01-01

    Radioactive iodine is one of the major substances released during severe nuclear accidents. Radioactive iodine is easily gasified, and if present in fallout it can enter the lungs, and thereby the circulatory system, with the inhalation of air. Once in a body, radioactive iodine accumulates in the thyroid and may result in tumours in the thyroid and, in extreme cases, impaired thyroid function. Accumulation of radioactive iodine can be prevented by taking non-radioactive, 'cold' iodine as tablets. Iodine tablets dilute the radioactive iodine that has entered the body. A dose of iodine also paralyses the thyroid temporarily by saturating its iodine-carrying capacity. To be useful iodine tablets should be taken immediately when a radioactive emission has occurred. If the tablets are taken too early or too late, they give little protection. Iodine tablets should not be taken just to be on the safe side, since their use may involve harmful side effects. Dosing instructions should also be followed with care. (orig.)

  16. Safety and efficacy of cladribine tablets in patients with relapsing-remitting multiple sclerosis: Results from the randomized extension trial of the CLARITY study.

    Science.gov (United States)

    Giovannoni, Gavin; Soelberg Sorensen, Per; Cook, Stuart; Rammohan, Kottil; Rieckmann, Peter; Comi, Giancarlo; Dangond, Fernando; Adeniji, Abidemi K; Vermersch, Patrick

    2017-08-01

    In the 2-year CLARITY study, cladribine tablets significantly improved clinical and magnetic resonance imaging (MRI) outcomes (vs placebo) in patients with relapsing-remitting multiple sclerosis (MS). To assess the safety and efficacy of cladribine treatment in a 2-year Extension study. In this 2-year Extension study, placebo recipients from CLARITY received cladribine 3.5 mg/kg; cladribine recipients were re-randomized 2:1 to cladribine 3.5 mg/kg or placebo, with blind maintained. A total of 806 patients were assigned to treatment. Adverse event rates were generally similar between groups, but lymphopenia Grade ⩾ 3 rates were higher with cladribine than placebo (Grade 4 lymphopenia occurred infrequently). In patients receiving cladribine 3.5 mg/kg in CLARITY and experiencing lymphopenia Grade ⩾ 3 in the Extension, >90% of those treated with cladribine 3.5 mg/kg and all treated with placebo in the Extension, recovered to Grade 0-1 by study end. Cladribine treatment in CLARITY produced efficacy improvements that were maintained in patients treated with placebo in the Extension; in patients treated with cladribine 3.5 mg/kg in CLARITY, approximately 75% remained relapse-free when given placebo during the Extension. Cladribine tablets treatment for 2 years followed by 2 years' placebo treatment produced durable clinical benefits similar to 4 years of cladribine treatment with a low risk of severe lymphopenia or clinical worsening. No clinical improvement in efficacy was apparent following further treatment with cladribine tablets after the initial 2-year treatment period in this trial setting.

  17. Tl response of LiF: Mg, Cu, P+Ptfe at X rays of 24, 42 and 100 KeV

    International Nuclear Information System (INIS)

    Gonzalez M, P.R.; Tovar M, V.M.; Azorin N, J.; Furetta, C.; Quiroz C, M.C.

    2005-01-01

    In this work the obtained results of the irradiation of thermoluminescent dosemeters (Tl) of LiF: Mg,Cu,P + Ptfe with X rays for the effective radiation energy of 24, 42 and 100 keV, in an interval of Kerma in air in the sinus of the air between 0.05 and 1.0 Gy are presented. The rate of Kerma in air was determined with an ionization chamber PTW-1152, gauged by the Laboratoire Central des Industries Electriques (LCIE). As reference commercial TLD-100 dosemeters was used. The results showed that the studied Tl dosemeters presented a lineal response in the interval of mentioned Kerma. On the other hand the estimated Kerma with the Tl dosemeter in the calibration curves for X rays, were similar to the one measured with the previously gauged ionization chamber. The Tl of LiF: Mg, Cu, P + Ptfe, developed in the ININ, are highly reliable for X-ray dosimetry. (Author)

  18. Iodine prophylaxis following nuclear accidents - a concept how to distribute potassium-iodide tablets out of the central stocks in the event of an accident

    International Nuclear Information System (INIS)

    Portius, U.

    2007-01-01

    With its recommendation ''Iodine prophylaxis following nuclear accidents'' (1996) and its reports of 1997 and 2001 the German Commission on Radiological Protection (SSK) followed the recommendations of the WHO ''Guidelines for iodine prophylaxis following nuclear accidents'' of 1989. The intervention levels were lowered (50 mSv for children/adolescents (up to the age of 18 years) and pregnant women, 250 mSv for adults), the iodine prophylaxis was restricted to persons up to the age of 45 years and the recommended dosage of stable iodine was changed. Due to the lowered reference levels the radius of 25 km around a nuclear power plant that had been the planning radius for the distribution of iodine tablets so far was extended to 100 km. Based on these recommendations the German authorities began to set up new strategies for the provision and distribution of potassium-iodide tablets (iodine tablets). Since 2004, within the radius of 25 km the iodine tablets are pre-distributed to households and/or stored at several points in the municipality for persons up to the age of 45 years. For the new planning radius of 25-100 km iodine tablets are stored in 8 central stocks in Germany for children/adolescents (up to the age of 18 years) and pregnant women. A working group with representatives from federal and Laender authorities has developed a distribution strategy for the distribution out of these central stocks in the event of an accident. It describes a possibility of organising and implementing the distribution of the iodine tablets within the radius of 25-100 km in a nationwide standardised way. (orig.)

  19. Tablets for Learning in Higher Education

    DEFF Research Database (Denmark)

    Godsk, Mikkel

    Based on a small-scale literature review this paper identifies the top 10 affordances of post PC tablets (sometimes referred to as ‘tablet computers’) for higher education in settings where the technology is used for learning. The review shows that the predominant affordances of the technology...... are related to its ability to support engaging, inclusive, and/or collaborative learning, to provide flexibility in place, and to include multimedia and interactive content in teaching practice. However, performing the review also revealed that the notion of tablets for learning is equivocal. As a consequence......, the concepts of tabletcasts and tabletcasting are introduced as one possible framing for future research on tablets as an educational technology....

  20. Lattice-Boltzmann Simulation of Tablet Disintegration

    Science.gov (United States)

    Jiang, Jiaolong; Sun, Ning; Gersappe, Dilip

    Using the lattice-Boltzmann method, we developed a 2D model to study the tablet disintegration involving the swelling and wicking mechanisms. The surface area and disintegration profile of each component were obtained by tracking the tablet structure in the simulation. Compared to pure wicking, the total surface area is larger for swelling and wicking, which indicates that the swelling force breaks the neighboring bonds. The disintegration profiles show that the tablet disintegrates faster than pure wicking, and there are more wetted active pharmaceutical ingredient particles distributed on smaller clusters. Our results indicate how the porosity would affect the disintegration process by changing the wetting area of the tablet as well as by changing the swelling force propagation.

  1. Attitudes towards Smart Phones and Tablets

    Directory of Open Access Journals (Sweden)

    Ali Akbar Ansarin

    2017-07-01

    Full Text Available This paper examines the perceptions of advantages of smart phones and tablets on basic and general English students' language learning, self-sufficiency, and interest using smart phones and tablets at an Iranian university college during one university term. Through a survey administered to 333 basic and general English students and through selective observations and interviews, the following questions were examined: 1 Students' perceived impact of smart phones and tablets on increasing their confidence throughout the course,2  Students’ perceived comfort/enjoyment with smart phones and tablets for the students at the beginning and end of the semester,3 Students' perceived impact of devices through a comparison between pre and post survey measures on improvement of reading comprehension, reading speed, vocabulary and spelling, motivation, and preparing them for class tests and quizzes. Tablets were evaluated more positively than smart phones by the students as a means to increase confidence. Both tablets and smart phones were evaluated positively, both as a means of improving students’ motivation to learn, and as a means to develop reading comprehension, spelling, and vocabulary. However, students’ expectations regarding the impact of such devices on their reading speed, preparation for tests and quizzes, as well as comfort and enjoyment were not met.

  2. Eudragit E100 and Polysaccharide Polymer Blends as Matrices for ...

    African Journals Online (AJOL)

    aqueous/lyophilized) of locust bean gum with Eudragit® E100 and sodium carboxymethylcellulose on swelling and ... Xanthan gum [2,3], guar gum [4,5], gum. Arabic [6,7] ..... tablets based on low density foam powder: effects of formulation and ...

  3. 21 CFR 520.1409 - Methylprednisolone, aspirin tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Methylprednisolone, aspirin tablets. 520.1409... Methylprednisolone, aspirin tablets. (a) Specifications. Each tablet contains 0.5 milligram of methylprednisolone and 300 milligrams of aspirin. (b) Sponsor. See No. 000009 in § 510.600(c) of this chapter. (c) NAS/NRC...

  4. 21 CFR 520.1157 - Iodinated casein tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Iodinated casein tablets. 520.1157 Section 520...) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1157 Iodinated casein tablets. (a) Specifications. Each 1-gram tablet contains 25 milligrams of iodinated casein. (b) Sponsor...

  5. DEVELOPMENT OF SUSTAINED RELEASE TABLETS CONTAINING SOLID DISPERSIONS OF BACLOFEN

    Directory of Open Access Journals (Sweden)

    K. H. Janardhana

    2015-07-01

    Full Text Available Sustained release tablets containing solid dispersions granules of a poorly water soluble drug were prepared to investigate the controlled release of the drug. Baclofen was chosen because of its poor water solubility and short elimination half-life. Poloxamer 188 and PEG 6000 were used as solid dispersion carrier. Free flowing solid dispersion granules were prepared by adsorbing the melt of the drug and carriers onto the surface of an adsorbent, Carbopol 934P followed by direct compression with HPMC K4M and HPMC K100 to obtain an solid dispersion loaded sustained release tablets. FTIR studies confirmed that the compatibility of drug and carriers. Differential scanning calorimetry (DSC and X-ray diffraction (XRD revealed partially amorphous structures of the drug in solid dispersion granules. The solid dispersion granules dissolved completely within 30 min, which was much faster than that of pure drug baclofen. The sustained release of baclofen from the solid dispersion containing tablet was achieved for 2 h in gastric fluid (pH 1.2 and for up to 10 h in intestinal fluid (pH 6.8. A combination of solid dispersion techniques using adsorption and sustained release concepts is a promising approach to control the release rate of poorly water-soluble drugs.

  6. DEVELOPMENT OF SUSTAINED RELEASE TABLETS CONTAINING SOLID DISPERSIONS OF BACLOFEN

    Directory of Open Access Journals (Sweden)

    K. H. Janardhana

    2013-12-01

    Full Text Available Sustained release tablets containing solid dispersions granules of a poorly water soluble drug were prepared to investigate the controlled release of the drug. Baclofen was chosen because of its poor water solubility and short elimination half-life. Poloxamer 188 and PEG 6000 were used as solid dispersion carrier. Free flowing solid dispersion granules were prepared by adsorbing the melt of the drug and carriers onto the surface of an adsorbent, Carbopol 934P followed by direct compression with HPMC K4M and HPMC K100 to obtain an solid dispersion loaded sustained release tablets. FTIR studies confirmed that the compatibility of drug and carriers. Differential scanning calorimetry (DSC and X-ray diffraction (XRD revealed partially amorphous structures of the drug in solid dispersion granules. The solid dispersion granules dissolved completely within 30 min, which was much faster than that of pure drug baclofen. The sustained release of baclofen from the solid dispersion containing tablet was achieved for 2 h in gastric fluid (pH 1.2 and for up to 10 h in intestinal fluid (pH 6.8. A combination of solid dispersion techniques using adsorption and sustained release concepts is a promising approach to control the release rate of poorly water-soluble drugs.

  7. Development of Orodispersible Tablets of Candesartan Cilexetil-β-cyclodextrin Complex

    Directory of Open Access Journals (Sweden)

    Maddukuri Sravya

    2013-01-01

    Full Text Available The aim of this study was to investigate the use of inclusion complexation technique employing β-cyclodextrin in improving the dissolution profile of candesartan cilexetil, a BCS class-II drug, and to formulate the inclusion complex into orodispersible tablets. The inclusion complexes were formed by physical mixing, kneading, coevaporation, and lyophilisation methods. Inclusion complexes were characterized by FTIR, DSC, XRD, NMR, and mass spectral studies. Inclusion complexes prepared using kneading, and lyophilisation techniques in the molar ratio 1 : 5 with β-cyclodextrin were used for formulating orodispersible tablets by direct compression with different superdisintegrants like croscarmellose sodium, crospovidone, sodium starch glycolate, and low substituted hydroxypropyl cellulose in varying concentrations. The directly compressible powder was evaluated for precompression parameters, and the prepared orodispersible tablets were evaluated for postcompression parameters. Drug-excipient compatibility studies showed no interaction, and characterization proved the formation of inclusion complex. In vitro disintegration time was found to be within 3 minutes, and all the formulations showed complete drug release of 100% within 20 minutes. The optimized formulation was found to be stable after 6 months and showed no significant change in drug content. This work proved β-cyclodextrins to be effective solubilizing agent in improving the solubility of poorly water soluble drugs.

  8. Transmission FTIR derivative spectroscopy for estimation of furosemide in raw material and tablet dosage form

    Directory of Open Access Journals (Sweden)

    Máximo Gallignani

    2014-10-01

    Full Text Available A Fourier transform infrared derivative spectroscopy (FTIR-DS method has been developed for determining furosemide (FUR in pharmaceutical solid dosage form. The method involves the extraction of FUR from tablets with N,N-dimethylformamide by sonication and direct measurement in liquid phase mode using a reduced path length cell. In general, the spectra were measured in transmission mode and the equipment was configured to collect a spectrum at 4 cm−1 resolution and a 13 s collection time (10 scans co-added. The spectra were collected between 1400 cm−1 and 450 cm−1. Derivative spectroscopy was used for data processing and quantitative measurement using the peak area of the second order spectrum of the major spectral band found at 1165 cm−1 (SO2 stretching of FUR with baseline correction. The method fulfilled most validation requirements in the 2 mg/mL and 20 mg/mL range, with a 0.9998 coefficient of determination obtained by simple calibration model, and a general coefficient of variation <2%. The mean recovery for the proposed assay method resulted within the (100±3% over the 80%–120% range of the target concentration. The results agree with a pharmacopoeial method and, therefore, could be considered interchangeable.

  9. Evaluación de desempeño del método de ensayo de disolución para tabletas de zidovudina 300 mg producidas en Cuba Performance assessment of dissolution assay method of 300 mg of Zidovudine tablets produced in Cuba

    Directory of Open Access Journals (Sweden)

    Caridad Margarita García Peña

    2010-09-01

    Full Text Available Se validó un método por cromatografía líquida de alta resolución para evaluar la disolución de las tabletas de zidovudina 300 mg producidas en Cuba, con detección ultravioleta a 265 nm. Se evaluaron los parámetros de especificidad, linealidad, precisión e influencia de la filtración. En el estudio de la influencia de la filtración se demostró que a través del filtro de línea, no se absorbe el principio activo, ni se aportan interferencias al filtrado, por lo que se recomienda su empleo. Se demostró la especificidad del método al no observarse interferencias de los excipientes de la formulación, en la determinación del principio activo. La curva de linealidad se realizó en el intervalo de concentraciones estudiadas con un coeficiente de correlación igual a 0,999. El método resultó preciso ya que los valores se encontraron dentro de los límites establecidos. Se realizó además la comparación estadística de los perfiles de disolución de las tabletas producidas en Cuba contra el Retrovir® (medicamento líder, lo cual demostró que existe similitud entre el perfil de liberación de las formulaciones.A high-performance liquid chromatography method was validated to assess the dissolution of 300 mg Zidovudine tablets manufactured in Cuba with 265 nm ultraviolet (UV detection. Filtration specificity, linearity, accuracy parameters were assessed. In influence filtration study it was shown that through the line-filter the active principle it isn't absorbed and without filtrate interferences thus it is recommended its use. It was possible to demonstrate the method specificity due to no interferences of the formula excipients in active principle assessment. Linearity curve was drawed in the interval of study concentrations with a correlation coefficient similar to 0.999. The method was precise since the values were within the established limits. Also, we made a statistical comparison of dissolution profiles of tablets manufactured

  10. Development of modified release 3D printed tablets (printlets) with pharmaceutical excipients using additive manufacturing.

    Science.gov (United States)

    Goyanes, Alvaro; Fina, Fabrizio; Martorana, Annalisa; Sedough, Daniel; Gaisford, Simon; Basit, Abdul W

    2017-07-15

    The aim of this study was to manufacture 3D printed tablets (printlets) from enteric polymers by single filament fused deposition modeling (FDM) 3D printing (3DP). Hot melt extrusion was used to generate paracetamol-loaded filaments from three different grades of the pharmaceutical excipient hypromellose acetate succinate (HPMCAS), grades LG, MG and HG. One-step 3DP was used to process these filaments into enteric printlets incorporating up to 50% drug loading with two different infill percentages (20 and 100%). X-ray Micro Computed Tomography (Micro-CT) analysis revealed that printlets with 20% infill had cavities in the core compared to 100% infill, and that the density of the 50% drug loading printlets was higher than the equivalent formulations loaded with 5% drug. In biorelevant bicarbonate dissolution media, drug release from the printlets was dependent on the polymer composition, drug loading and the internal structure of the formulations. All HPMCAS-based printlets showed delayed drug release properties, and in the intestinal conditions, drug release was faster from the printlets prepared with polymers with a lower pH-threshold: HPMCAS LG > HPMCAS MG > HPMCAS HG. These results confirm that FDM 3D printing makes it possible not only to manufacture delayed release printlets without the need for an outer enteric coating, but it is also feasible to adapt the release profile in response to the personal characteristics of the patient, realizing the full potential of additive manufacturing in the development of personalised dose medicines. Copyright © 2017 Elsevier B.V. All rights reserved.

  11. Skew scattering dominated anomalous Hall effect in Cox(MgO)100-x granular thin films

    KAUST Repository

    Zhang, Qiang; Wen, Yan; Zhao, Yuelei; Li, Peng; He, Xin; Zhang, Junli; He, Yao; Peng, Yong; Yu, Ronghai; Zhang, Xixiang

    2017-01-01

    We investigated the mechanism(s) of the anomalous Hall effect (AHE) in magnetic granular materials by fabricating 100-nm-thick thin films of Cox(MgO)100-x with a Co volume fraction of 34≤x100 using co

  12. Evaluating vertical concentration profile of carbon source released from slow-releasing carbon source tablets and in situ biological nitrate denitrification activity

    Science.gov (United States)

    Yeum, Y.; HAN, K.; Yoon, J.; Lee, J. H.; Song, K.; Kang, J. H.; Park, C. W.; Kwon, S.; Kim, Y.

    2017-12-01

    Slow-releasing carbon source tablets were manufactured during the design of a small-scale in situ biological denitrification system to reduce high-strength nitrate (> 30 mg N/L) from a point source such as livestock complexes. Two types of slow-releasing tablets, precipitating tablet (PT, apparent density of 2.0 g/mL) and floating tablet (FT), were prepared to achieve a vertically even distribution of carbon source (CS) in a well and an aquifer. Hydroxypropyl methylcellulose (HPMC) was used to control the release rate, and microcrystalline cellulose pH 101 (MCC 101) was added as a binder. The #8 sand was used as a precipitation agent for the PTs, and the floating agents for the FTs were calcium carbonate and citric acid. FTs floated within 30 min. and remained in water because of the buoyance from carbon dioxide, which formed during the acid-base reaction between citric acid and calcium carbonate. The longevities of PTs with 300 mg of HPMC and FTs with 400 mg of HPMC were 25.4 days and 37.3 days, respectively. We assessed vertical CS profile in a continuous flowing physical aquifer model (release test, RT) and its efficiency on biological nitrate denitrification (denitrification test, DT). During the RT, PTs, FTs and a tracer (as 1 mg rhodamine B/L) were initially injected into a well of physical aquifer model (PAM). Concentrations of CS and the tracer were monitored along the streamline in the PAM to evaluate vertical profile of CS. During the DT, the same experiment was performed as RT, except continuous injection of solution containing 30 mg N/L into the PAM to evaluate biological denitrification activity. As a result of RT, temporal profiles of CS were similar at 3 different depths of monitoring wells. These results suggest that simultaneous addition of PT and FT be suitable for achieving a vertically even distribution of the CS in the injection well and an aquifer. In DT, similar profile of CS was detected in the injection well, and nitrate was biologically

  13. Tablet surface characterisation by various imaging techniques

    DEFF Research Database (Denmark)

    Seitavuopio, Paulus; Rantanen, Jukka; Yliruusi, Jouko

    2003-01-01

    The aim of this study was to characterise tablet surfaces using different imaging and roughness analytical techniques including optical microscopy, scanning electron microscopy (SEM), laser profilometry and atomic force microscopy (AFM). The test materials compressed were potassium chloride (KCl......) and sodium chloride (NaCl). It was found that all methods used suggested that the KCl tablets were smoother than the NaCl tablets and higher compression pressure made the tablets smoother. Imaging methods like optical microscopy and SEM can give useful information about the roughness of the sample surface...

  14. [The enantioselective pharmacokinetic study of desvenlafaxine sustained release tablet in Chinese healthy male volunteers after oral administration].

    Science.gov (United States)

    Chen, Yin-xia; Du, Jiang-bo; Zhang, Yi-fan; Chen, Xiao-yan; Zhong, Da-fang

    2015-04-01

    A chiral LC-MS/MS method for the simultaneous analysis of desvenlafaxine (DVS) enantiomers in human plasma was developed and applied to a pharmacokinetic study on 12 Chinese healthy volunteers. d6-Desvenlafaxine was used as internal standard (IS). Chromatographic separation was performed on the Astec Chirobiotic V chiral column (150 mm x 4.6 mm, 5 μm). The assay was linear over the concentration range of 0.500-150 ng x mL(-1) for both enantiomers (r2 > 0.99). The method was successfully applied to a stereoselective pharmacokinetic study of 100 mg desvenlafaxine sustained release tablets on 12 Chinese healthy volunteers under fasting conditions. The results showed that the pharmacokinetic parameters were similar to both enantiomers in Chinese healthy volunteers. The AUC(0-t), and C(max) of the two enantiomers were about 1.5 times higher than those of blacks and whites reported in the literature.

  15. Disintegration of sublingual tablets: proposal for a validated test method and acceptance criterion.

    Science.gov (United States)

    Weda, M; van Riet-Nales, D A; van Aalst, P; de Kaste, D; Lekkerkerker, J F F

    2006-12-01

    In the Netherlands the market share of isosorbide dinitrate 5 mg sublingual tablets is dominated by 2 products (A and B). In the last few years complaints have been received from health care professionals on product B. During patient use the disintegration of the tablet was reported to be slow and/or incomplete, and ineffectiveness was experienced. In the European Pharmacopoeia (Ph. Eur.) no requirement is present for the disintegration time of sublingual tablets. The purpose of this study was to compare the in vitro disintegration time of products A and B, and to establish a suitable test method and acceptance criterion. A and B were tested with the Ph. Eur. method described in the monograph on disintegration of tablets and capsules as well as with 3 modified tests using the same Ph. Eur. apparatus, but without movement of the basket-rack assembly. In modified test 1 and modified test 2 water was used as medium (900 ml and 50 ml respectively), whereas in modified test 3 artificial saliva was used (50 ml). In addition, disintegration was tested in Nessler tubes with 0.5 and 2 ml of water. Finally, the Ph. Eur. method was also applied to other sublingual tablets with other drug substances on the Dutch market. With modified test 3 no disintegration could be achieved within 20 min. With the Ph. Eur. method and modified tests 1 and 2 product A and B differed significantly (p disintegration times. These 3 methods were capable of discriminating between products and between batches. The time measured with the Ph. Eur. method was significantly lower compared to modified tests 1 and 2 (p tablets the disintegration time should be tested. The Ph. Eur. method is considered suitable for this test. In view of the products currently on the market and taking into consideration requirements in the United States Pharmacopeia and Japanese Pharmacopoeia, an acceptance criterion of not more than 2 min is proposed.

  16. Taking the classical large audience university lecture online using tablet computer and webconferencing facilities

    DEFF Research Database (Denmark)

    Brockhoff, Per B.

    2011-01-01

    During four offerings (September 2008 – May 2011) of the course 02402 Introduction to Statistics for Engineering students at DTU, with an average of 256 students, the lecturing was carried out 100% through a tablet computer combined with the web conferencing facility Adobe Connect (version 7...

  17. Multiple-dose pharmacokinetic study of proguanil and cycloguanil following 12-hourly administration of 100 mg proguanil hydrochloride.

    Science.gov (United States)

    Jamaludin, A; Mohamad, M; Navaratnam, V; Yeoh, P Y; Wernsdorfer, W H

    1990-09-01

    A pharmacokinetic study with 12-hourly doses of 100 mg proguanil hydrochloride over 15 days has been conducted in six adult male Malaysian volunteers. Steady state for proguanil was established after the fourth dose on Day 2, for the active metabolite cycloguanil as from Day 3 inclusive. The steady state mean peak concentration of proguanil was 1201.6 +/- 132.4 nmol/l, the mean trough concentration 650.0 +/- 58.1 nmol/l. The corresponding values for cycloguanil were 317.0 +/- 44.4 nmol/l (mean peak) and 230.8 +/- 35.1 nmol/l (mean trough). The profiles and peak/trough ratios of proguanil and cycloguanil with 12-hourly dosing offer better prospects for protection against malaria than those obtained with 24-hourly doses of 200 mg proguanil hydrochloride, the current routine in malaria chemoprophylaxis.

  18. Comparison of antiplatelet activity of garlic tablets with cardio-protective dose of aspirin in healthy volunteers: a randomized clinical trial

    Directory of Open Access Journals (Sweden)

    Mojtaba Shafiekhani

    2016-08-01

    Full Text Available Objective: Some of the adverse effects of aspirin including peptic ulcers, gastrointestinal bleeding and aspirin resistance compelled researchers to find a suitable alternative with fewer adverse effects. In this clinical trial, we aimed to find the effective antiplatelet dose of garlic. Materials and Methods: This randomized controlled clinical trial (RCT was conducted on 62 healthy volunteers of 20-50 years old. All volunteers used 80 mg aspirin per day for 1 week and at the end of this time, platelet aggregation (PA induced by 4 agonists acting in aggregation pathway including adenosinediphosphate (20 μmol/l, epinephrine (20 μmol/l, collagen(0.19 mg/ ml and arachidonic acid (0.5mg/ ml was measured by Light Transmittance Aggregometry (LTA in all participants. After one month washout period, volunteers were randomized into 3 groups and each received 1, 2 or 3 garlic tablets (1250 mg a day for 1 month. After one month, PA was examined in all groups. Results: The mean ±SD of the age of all volunteers was 28.60 ± 9.00 years. In addition, 52.00 % of our volunteers were male and 48.00% of them were female. Garlic tablet didnot have significant effect on PA at any dose. However, 30% of volunteers in the group that used 3 garlic tablets/day reported adverse effect (i.e. bleeding. No significant association between sex, age and PA was observed. Conclusion:  In this study, we were unable to determine the effective anti-platelet dose of garlic which that could be equal to that of aspirin anti-platelet activity, as assessed LTA method.

  19. Estabilidad acelerada de tabletas de levodopa-carbidopa (250-25 mg

    Directory of Open Access Journals (Sweden)

    Mirna Fernández Cervera

    2001-08-01

    Full Text Available Se realizó el estudio de estabilidad acelerada de tabletas de levodopa-carbidopa (250-25 mg con el empleo de un método de cromatografía líquida de alta resolución y se comprobó su especificidad para estos fines. Se analizó la influencia de medios degradantes artificiales sobre los productos activos, además del efecto de la humedad sobre la estabilidad del producto, colocándolo en hidrostatos con humedades controladas. Este medicamento, producción nacional, cumplió con las especificaciones de calidad descritas en la USP 23 y mostró una alta estabilidad térmica.An accelerated stability study of levodopa-carbidopa tablets (250-25 mg was made using high-performance liquid chromatography which specificity for these purposes was proved. The influence of the artificial degrading media on the active products was analyzed and also the effect of humidity on the product´s satbility was examined after placing the tablets into hydrostats under controlled humidity levels. This domestically-made drug met the quality standards described in USP 23 and showed high heat stability.

  20. Optical and terahertz measurement techniques for flat-faced pharmaceutical tablets: a case study of gloss, surface roughness and bulk properties of starch acetate tablets

    International Nuclear Information System (INIS)

    Juuti, M; Tuononen, H; Kontturi, V; Peiponen, K-E; Prykäri, T; Alarousu, E; Myllylä, R; Kuosmanen, M; Ketolainen, J

    2009-01-01

    Surface and bulk properties of flat-faced starch acetate tablets were studied. For surface quality inspection optical coherence tomography and recently developed diffractive glossmeter were utilized. Both these optical devices together provide local information on surface roughness and gloss of a tablet over a measured area. The concepts of mean topography and mean gloss profile for surface quality of a tablet are introduced. It was observed that the surface quality of the tablet varies, and compression at high pressure may not guarantee a good surface quality of the tablet. Using novel statistical parameters for gloss and relevant surface roughness parameter, it is possible to get more comprehensive quantitative data on the surface condition of a tablet. THz spectrometer was utilized for detection of THz pulse delay in transmission measurement mode from the tablets. The delay time and thickness ratio of the tablet are consistent with the porosity of the tablet as a function of compression pressure. We suggest that the multimeasurement scheme using three different devices helps tablet makers to better assess bulk and surface quality of their products

  1. Control de la calidad y estudio de estabilidad del paracetamol gotas orales 100 mg/ml Quality control and stability study of 100 mg/ml paracetamol oral drops

    Directory of Open Access Journals (Sweden)

    Caridad M García Peña

    2013-03-01

    Full Text Available Introducción: las gotas orales de Paracetamol, están indicadas a la población infantil hasta los 5 años para el alivio de la fiebre, dolor de cabeza, dolores dentales y proporciona alivio sintomático del resfriado común. Objetivo: validar dos métodos analíticos, para el control de la calidad y el estudio de estabilidad y estudiar la estabilidad de las gotas orales de producción nacional. Métodos: para cuantificar el principio activo para el estudio de estabilidad, la separación se realizó a través de una columna cromatográfica Lichrosorb RP - 18 (5µm (250 x 4 mm, con detección ultravioleta a 243 nm, empleando una fase móvil compuesta por Agua destilada: Metanol (3:1. Mientras que el método para el control de la calidad se utilizó un Espectrofotómetro SPECTRONIC GENESYS 2.Para el estudio de estabilidad, se emplearon los métodos de vida de estante (a temperatura inferior a 30 º C y de estabilidad acelerada (40 ± 2ºC mediante cromatografía líquida de alta eficiencia. Resultados: los resultados obtenidos de los parámetros evaluados en las validaciones se encontraron dentro de los límites establecidos. Los resultados del estudio de estabilidad realizado, demuestran que el producto terminado cumplió con las especificaciones de calidad durante el estudio. Conclusiones: los métodos analíticos por espectrofotometría UV y cromatografía líquida de alta resolución, son válidos para el control de la calidad y estudio de estabilidad de las gotas orales de Paracetamol 100 mg/mL, ya que resultaron lineales, precisos, exactos y específicos. Se demostró la estabilidad física, química y microbiológica del producto por espacio de 12 meses a temperatura inferior a 30 ºC, envasados en frascos de vidrio ámbar por 15 mL, boca 18 mm, calidad hidrolítica III. Además se evidenció que el producto es estable durante 30 días después de abierto el frasco.Introduction: paracetamol is an effective analgesic and antipyretic drug of

  2. A pharmaceutical study on lornoxicam fast disintegrating tablets: formulation and in vitro and in vivo evaluation.

    Science.gov (United States)

    Moutasim, Mohamed Yousif; ElMeshad, Aliaa Nabil; El-Nabarawi, Mohamed Ahmed

    2017-06-01

    Lornoxicam is an anti-inflammatory drug used to relieve rheumatoid arthritis pain, but the low water solubility and bitter taste of the drug present challenges for formulation as fast disintegrating tablets (FDTs). Complexation of the drug with β-cyclodextrin was initially carried out to increase the drug solubility and to mask its bitter taste. Tablets were prepared by direct compression of drug complex (DC), F-Melt, mannitol, crospovidone, and sodium starch glycolate (SSG). FDTs were characterized in terms of disintegration time (DT) and dissolution. A bioequivalence study was carried out using (Zeficam® tablets (Eva Pharma) as reference with the help of human volunteers (n = 4). The chosen formula (F2, DC 24 mg, F-Melt 88.4 mg, and crospovidone 5 mg) exhibited the shortest in vitro (18 s) and in vivo DT (13 s), and the percent drug released after Q6min was 95.90%. Following administration of F2 and Zeficam®, the respective maximum drug plasma concentrations (C max ) were 510 and 532.5 ng/mL, at times (T max ) of 1 and 2.5 h, of mean residence times (MRTs) of 12.25 and 11.35 h and of areas under the plasma curve [AUC(0-24)] of 5080.253 and 4815.775 ng/h/mL. There were significant differences in T max and MRT of both treatments (p < 0.05). Moreover, the volunteers found F2 to be palatable. FDTs could be considered as promising dosage forms for lornoxicam as they exhibited a short in vivo DT and an increased rate of drug release and attained a relative bioavailability of 105.49%. This could offer a fast relief of pain accompanying rheumatoid arthritis.

  3. Real-world dose-relativity, tablet burden, and cost comparison of conversion between sevelamer hydrochloride/carbonate and lanthanum carbonate monotherapies.

    Science.gov (United States)

    Keith, Michael S; Sibbel, Scott; Copley, J Brian; Wilson, Rosamund J; Brunelli, Steven M

    2014-10-01

    Sevelamer hydrochloride/carbonate (SH/C) and lanthanum carbonate (LC) are noncalcium-based phosphate binders used for the management of hyperphosphatemia in patients with end-stage renal disease (ESRD). The objectives of this study were to examine the dose-relativity, tablet burden, and cost difference of bidirectional conversion between SH/C and LC monotherapy in a large cohort of real-world patients with ESRD. This retrospective cohort study included three 30-day preconversion periods (days -90 to -61, -60 to -31, and -30 to -1) followed by three 30-day postconversion periods (days 1 to 30, 31 to 60, and 61 to 90); day 0 was the index date of conversion. The full analysis population (FAP) comprised two cohorts: SH/C to LC (S-L) converters and LC to SH/C (L-S) converters. The SH/C:LC dose-relativity ratio was assessed in the dose-relativity subset, defined as patients whose serum phosphate levels fell within a caliper range of ± 0.5 mg/dL in the final preconversion (days -30 to -1) and postconversion (days 61 to 90) periods. Tablet burden and phosphate binder costs were assessed in the FAP. Phosphate binder costs were based on average wholesale prices. The FAP contained a total of 303 patients, comprising the S-L (128 patients) and L-S (175 patients) converter cohorts. The dose-relativity subset contained 159 patients, 72 from the S-L cohort and 87 from the L-S cohort. The overall mean SH/C:LC dose-relativity ratio was 2.27 (95% CI, 2.04 to 2.52). In SH/C dose strata >800 to 2400, >2400 to 4800, >4800 to 7200, and >7200 mg/d, overall mean dose-relativity ratios were 0.79 (95% CI, 0.57 to 1.10), 1.45 (95% CI, 1.20 to 1.75), 2.05 (95% CI, 1.75 to 2.39), and 3.24 (95% CI, 2.89 to 3.66), respectively. The overall mean tablet burden was 6.6 tablets per day lower with LC monotherapy than with SH/C monotherapy (95% CI, -7.1 to -6.0; P 7800 mg/d was the inflection point at which conversion to LC resulted in mean cost savings. Patients requiring SH/C >7800 mg/d comprised

  4. Challenges in detecting magnesium stearate distribution in tablets.

    Science.gov (United States)

    Lakio, Satu; Vajna, Balázs; Farkas, István; Salokangas, Henri; Marosi, György; Yliruusi, Jouko

    2013-03-01

    Magnesium stearate (MS) is the most commonly used lubricant in pharmaceutical industry. During blending, MS particles form a thin layer on the surfaces of the excipient and drug particles prohibiting the bonding from forming between the particles. This hydrophobic layer decreases the tensile strength of tablets and prevents water from penetrating into the tablet restraining the disintegration and dissolution of the tablets. Although overlubrication of the powder mass during MS blending is a well-known problem, the lubricant distribution in tablets has traditionally been challenging to measure. There is currently no adequate analytical method to investigate this phenomenon. In this study, the distribution of MS in microcrystalline cellulose (MCC) tablets was investigated using three different blending scales. The crushing strength of the tablets was used as a secondary response, as its decrease is known to result from the overlubrication. In addition, coating of the MCC particles by MS in intact tablets was detected using Raman microscopic mapping. MS blending was more efficient in larger scales. Raman imaging was successfully applied to characterize MS distribution in MCC tablets despite low concentration of MS. The Raman method can provide highly valuable visual information about the proceeding of the MS blending process. However, the measuring set-up has to be carefully planned to establish reliable and reproducible results.

  5. A study of the properties of tablets made of directly compressible maltose.

    Science.gov (United States)

    Muzíková, J; Balhárková, J

    2008-01-01

    The paper deals with the study of the strength and disintegration time of tablets made of directly compressible maltose Advantose 100. It studies the differences of the effects of two types of lubricants, magnesium stearate and sodium stearylfumarate, on the above-mentioned properties, and it also tests the mixtures of the substance with microcrystalline cellulose Vivapur 102 in a ratio of 1:1 and with ascorbic and acetylsalicylic acids. The compacts are obtained by using three compression forces, excepting mixtures with active ingredients, where one compression force is used. In the compression forces of 6 and 8 kN, no statistically significant difference was found in the intervention of the lubricants into the strength of the compacts made of Advantose 100, only in the compression force of 10 kN Pruv decreased the strength more than stearate. The mixture of Advantose 100 and Vivapur 102 yielded the strongest tablets, an addition of Pruv to it decreased the strength of compacts more than stearate. The periods of disintegration time of Advantose compacts as well as those of the mixture of dry binders were longer with an addition of Pruv. The compacts with acetylsalicylic acid possessed higher strength and a longer period of disintegration than those with ascorbic acid. There was no statistically significant difference within the type of the lubricant employed, both in the case of Advantose 100 and its mixture with Vivapur 102, between the values of strength of the compacts with acetylsalicylic acid.

  6. Systematic evaluation of common lubricants for optimal use in tablet formulation.

    Science.gov (United States)

    Paul, Shubhajit; Sun, Changquan Calvin

    2018-05-30

    As an essential formulation component for large-scale tablet manufacturing, the lubricant preserves tooling by reducing die-wall friction. Unfortunately, lubrication also often results in adverse effects on tablet characteristics, such as prolonged disintegration, slowed dissolution, and reduced mechanical strength. Therefore, the choice of lubricant and its optimal concentration in a tablet formulation is a critical decision in tablet formulation development to attain low die-wall friction while minimizing negative impact on other tablet properties. Three commercially available tablet lubricants, i.e., magnesium stearate, sodium stearyl fumerate, and stearic acid, were systematically investigated in both plastic and brittle matrices to elucidate their effects on reducing die-wall friction, tablet strength, tablet hardness, tablet friability, and tablet disintegration kinetics. Clear understanding of the lubrication efficiency of commonly used lubricants as well as their impact on tablet characteristics would help future tablet formulation efforts. Copyright © 2018 Elsevier B.V. All rights reserved.

  7. Portable Tablets in Science Museum Learning

    DEFF Research Database (Denmark)

    Gronemann, Sigurd Trolle

    2016-01-01

    Despite the increasing use of portable tablets in learning, their impact has received little attention in research. In five different projects, this media-ethnographic and design-based analysis of the use of portable tablets as a learning resource in science museums investigates how young people...... is identified. It is argued that, paradoxically, museums’ decisions to innovate by introducing new technologies, such as portable tablets, and new pedagogies to support them conflict with many young people’s traditional ideas of museums and learning. The assessment of the implications of museums’ integration...... of portable tablets indicates that in making pedagogical transformations to accommodate new technologies, museums risk opposing didactic intention if pedagogies do not sufficiently attend to young learners’ systemic expectations to learning and to their expectations to the digital experience influenced...

  8. Validated, Ultra Violet Spectroscopy method for the Dissolution study of Mycophenolate mofetil immediate release 500mg tablets

    OpenAIRE

    Surajpal P. Verma; Ozair Alam; Pooja Mullick; Nadeem Siddiqui; Suroor A. Khan

    2008-01-01

    A simple, selective and precise dissolution method was developed and validated for the Mycophenolate mofetil immediate release tablets. The method employed dissolution medium 0.1N HCl (pH1.2) and volume 900ml with USP-II apparatus (Paddle). Detection was made by measuring the absorbance on UV at the [lambda]~max~ 250nm. The method show the linearity in the range of conc. 5[micro]g/ml to 40[micro]g/ml with r^2^=0.999. The method is also validated as per International Conference of Harmonizatio...

  9. The Formulation of Diclofenac Sodium Hydrogel Tablets | Onyechi ...

    African Journals Online (AJOL)

    The dissolution data fitted to Higuchi and Hixson-Crowell equations indicating the existence of diffusion mechanism controlling diclofenac release from the tablets. Keywords: Sustained release, diclofenac sodium hydrogel tablets, Voltarol retard tablets, film coating, dissolution profiles. Nigerian Journal of Pharmaceutical ...

  10. Key Technical Aspects Influencing the Accuracy of Tablet Subdivision.

    Science.gov (United States)

    Teixeira, Maíra T; Sá-Barreto, Lívia C L; Gratieri, Taís; Gelfuso, Guilherme M; Silva, Izabel C R; Cunha-Filho, Marcílio S S

    2017-05-01

    Tablet subdivision is a common practice used mainly for dose adjustment. The aim of this study was to investigate how the technical aspects of production as well as the method of tablets subdivision (employing a tablet splitter or a kitchen knife) influence the accuracy of this practice. Five drugs commonly used as subdivided tablets were selected. For each drug, the innovator drug product, a scored-generic and a non-scored generic were investigated totalizing fifteen drug products. Mechanical and physical tests, including image analysis, were performed. Additionally, comparisons were made between tablet subdivision method, score, shape, diluent composition and coating. Image analysis based on surface area was a useful tool as an alternative assay to evaluate the accuracy of tablet subdivision. The tablet splitter demonstrates an advantage relative to a knife as it showed better results in weight loss and friability tests. Oblong, coated and scored tablets had better results after subdivision than round, uncoated and non-scored tablets. The presence of elastic diluents such as starch and dibasic phosphate dehydrate conferred a more appropriate behaviour for the subdivision process than plastic materials such as microcrystalline cellulose and lactose. Finally, differences were observed between generics and their innovator products in all selected drugs with regard the quality control assays in divided tablet, which highlights the necessity of health regulations to consider subdivision performance at least in marketing authorization of generic products.

  11. Pharmacokinetic and tolerability of i.m. disodium clodronate 200 mg/lidocaine 1%, given twice monthly, in comparison with i.m. disodium clodronate 100 mg/lidocaine 1%, given weekly, in healthy postmenopausal female patients.

    Science.gov (United States)

    Radicioni, Milko; Cremonesi, Giovanni; Baraldi, Enrica; Leuratti, Chiara; Mariotti, Fabrizia

    2013-04-01

    Clodronate is a bisphosphonate effective in the prevention and treatment of osteoporosis in postmenopausal women. Non-adherence to bisphosphonates, however, is a major issue in clinical practice. Simplifying dose regimens may increase compliance. To assess bioequivalence between an intramuscular (i.m.) clodronate 200 mg/lidocaine 1% twice-a-month formulation and a clodronate 100 mg/lidocaine 1% weekly formulation in 32 postmenopausal women. In this double-blind, randomized, two-way crossover study, test and reference formulations were administered in single dose, with a 2-week wash-out between administrations. The primary endpoint was clodronic acid cumulative excretion in the first 24 hours after injection (Xu0-24h). Cumulative excretion in the 72 hours post-dose (Xu0-72h) and maximum excretion rate (Ratemax) were also evaluated. Bioequivalence was assumed if the 90% confidence intervals (CIs) of the geometric means ratios of the dose-normalized parameters were within the 80.00 - 125.00% range. Local tolerability was evaluated. Mean Xu0-24h values were 114.03 ±23.13 mg and 55.22 ±9.73 mg for clodronate 200 mg and 100 mg. The 90% CIs for dose-normalized Xu0-24h, Xu0-72h and Ratemax ere 95 -110%, 94 -107% and 95 - 113%. Local tolerability of both treatments was good. The differences in pain intensity between formulations were not sigificantly different at most assessment times. Headache was the only treatment-related adverse event. Bioequivalence of the two formulations was confirmed in terms of dose-normalized rate and amount of clodronic acid excretion. This result, together with the favorable tolerability of the novel 200 mg formulation, suggests the possibility of reducing the number of i.m. administrations from once-a-week to twice-a-month.

  12. Composition profiling of seized ecstasy tablets by Raman spectroscopy.

    Science.gov (United States)

    Bell, S E; Burns, D T; Dennis, A C; Matchett, L J; Speers, J S

    2000-10-01

    Raman spectroscopy with far-red excitation has been investigated as a simple and rapid technique for composition profiling of seized ecstasy (MDMA, N-methyl-3,4-methylenedioxyamphetamine) tablets. The spectra obtained are rich in vibrational bands and allow the active drug and excipient used to bulk the tablets to be identified. Relative band heights can be used to determine drug/excipient ratios and the degree of hydration of the drug while the fact that 50 tablets per hour can be analysed allows large numbers of spectra to be recorded. The ability of Raman spectroscopy to distinguish between ecstasy tablets on the basis of their chemical composition is illustrated here by a sample set of 400 tablets taken from a large seizure of > 50,000 tablets that were found in eight large bags. The tablets are all similar in appearance and carry the same logo. Conventional analysis by GC-MS showed they contained MDMA. Initial Raman studies of samples from each of the eight bags showed that despite some tablet-to-tablet variation within each bag the contents could be classified on the basis of the excipients used. The tablets in five of the bags were sorbitol-based, two were cellulose-based and one bag contained tablets with a glucose excipient. More extensive analysis of 50 tablets from each of a representative series of sample bags have distribution profiles that showed the contents of each bag were approximately normally distributed about a mean value, rather than being mixtures of several discrete types. Two of the sorbitol-containing sample sets were indistinguishable while a third was similar but not identical to these, in that it contained the same excipient and MDMA with the same degree of hydration but had a slightly different MDMA/sorbitol ratio. The cellulose-based samples were badly manufactured and showed considerable tablet-to-tablet variation in their drug/excipient ratio while the glucose-based tablets had a tight distribution in their drug/excipient ratios

  13. Guargum and Eudragit ® coated curcumin liquid solid tablets for colon specific drug delivery.

    Science.gov (United States)

    S Kumar, Vrinda; Rijo, John; M, Sabitha

    2018-04-15

    Colorectal cancer, also known as bowel cancer, is the uncontrolled cell growth in the colon or rectum (parts of the large intestine), or in the appendix. The colon specific drug delivery would alleviate the systemic side effects and would assure the safe therapy for colonic disorders with minimum dose and duration of therapy. The liquisolid technique refers to solubilisation of drug in a non-volatile solvent combined with inclusion of appropriate carrier and coating agent required for tableting. Colon specific degradation of natural polymer, guar gum and pH dependant degradative (pH-7) property of eudragit L100 restricts the delivery of curcumin in gastric and intestinal pH. Formulated curcumin liquisolid powder was evaluated for the micrometric properties, solubility and by differential thermal analysis, X ray powder diffraction and scanning electron microscopy. Curcumin loaded liquisolid tablet showed more anticancer activity against HCT-15 compared with free curcumin. Bioavailability study of the coated and uncoated liquisolid tablets were performed using Newzealand white rabbits. The present study concludes that liquisolid technique is a promising alternative for improving oral bioavailability and dissolution rate of water insoluble drug and coating liquisolid tablet with colon sensitive polymers showed site specific release of drug in the colon. Copyright © 2018 Elsevier B.V. All rights reserved.

  14. Optimization of the formulation of fast disintegrating tablets

    NARCIS (Netherlands)

    Kamp, Herman Vincent van

    1987-01-01

    Chapter 1 presents general information on tableting and is an introduction to the other chapters. Chapter 2 covers the mechanism of action of tablet disintegrants, in particular modern super disintegrants. The results indicate that when the tablets contain a slightly swelling but hydrophilic

  15. Design and evaluation of nicorandil extended-release tablet

    Directory of Open Access Journals (Sweden)

    Ju-Young Kim

    2015-04-01

    Full Text Available The aim of this study was to design and evaluate extended-release formulations of a model drug, nicorandil, in order to achieve the desired steady-state plasma concentration of drug in vivo. Simulation was employed to estimate optimum dissolution and absorption rate of nicorandil. The dissolution test was employed using pH 1.2, 4.0, 6.8 buffer solution, or water, to measure the in vitro release behaviors of nicorandil formulations. A single dose (15 mg of each formulation was orally administered to four beagle dogs under fasted conditions, and the pharmacokinetic parameters were calculated. The in vitro/in vivo relationship of the extended-release formulation was confirmed using in vitro dissolution profiles and plasma concentrations of drug in beagle dogs. Nicorandil was released completely within 30 min from the immediate-release tablets and released for 24 h from the extended-release tablets. The nicorandil plasma concentration could be modified by adjusting the drug release rate from the extended-release formulation. The release rate of nicorandil was the rate-limiting step in the overall absorption of drug from the extended-release formulations. These results highlight the potential of a nicorandil extended-release formulation in the treatment of angina pectoris.

  16. Preparation of Orally Disintegrating Tablets Containing Powdered Tea Leaves with Enriched Levels of Bioactive Compounds by Means of Microwave Irradiation Technique.

    Science.gov (United States)

    Tanaka, Hironori; Iwao, Yasunori; Izumikawa, Masahiro; Sano, Syusuke; Ishida, Hitoshi; Noguchi, Shuji; Itai, Shigeru

    2016-01-01

    In the present study, a microwave treatment process has been applied to prepare orally disintegrating tablets (ODTs) containing powdered tea leaves with enriched levels of the anti-inflammatory compounds such as chafuroside A (CFA) and chafuroside B (CFB). The use of distilled water as the adsorbed and granulation solvents in this preparation process afforded tablets with a long disintegration time (more than 120 s). The CFA and CFB contents of these tablets did not also change after 4 min of microwave irradiation due to the tablet temperature, which only increased to 100°C. In contrast, the tablet temperature increased up to 140°C after 3 min of microwave irradiation when a 1.68 M Na2HPO4 solution instead of distilled water. Notably, the disintegration time of these tablets was considerably improved (less than 20 s) compared with the microwave-untreated tablets, and there were 7- and 11-fold increases in their CFA and CFB contents. In addition, the operational conditions for the preparation of the tablets were optimized by face-centered composite design based on the following criteria: tablet hardness greater than 13 N, disintegration time less than 30 s and friability less than 0.5%. The requirements translated into X1 (the amount of granulation solvent), X2 (tableting pressure) and X3 (content of the powdered tea leaves) values of 45%, 0.43 kN and 32%, respectively, and the ODTs containing powdered tea leaves prepared under these optimized conditions were found to show excellent tablet properties and contain enriched levels of CFA and CFB.

  17. Effects of plantain and corn starches on the mechanical and disintegration properties of paracetamol tablets.

    Science.gov (United States)

    Akin-Ajani, Olufunke D; Itiola, Oludele A; Odeku, Oluwatoyin A

    2005-10-22

    The effects of plantain starch obtained from the unripe fruit of the plant Musa paradisiaca L. (Musaceae) on the mechanical and disintegration properties of paracetamol tablets have been investigated in comparison with the effects of corn starch BP using a 2(3) factorial experimental design. The individual and combined effects of nature of starch binder (N), concentration of starch binder (C), and the relative density of tablet (RD) on the tensile strength (TS), brittle fracture index (BFI), and disintegration time (DT) of the tablets were investigated. The ranking of the individual effects on TS was RD > C > N, on BFI was C > RD > N and on DT was N > C > RD. The ranking for the interaction effects on TS and DT was N-C > N-RD > C-RD, while that on BFI was N-C > C-RD > N-RD. Changing nature of starch from a "low" (plantain starch) to a "high" (corn starch) level, increasing the concentration of starch binding agent from 2.5% to 10.0% wt/wt, and increasing relative density of the tablet from 0.80 to 0.90, led to increase in the values of TS and DT, but a decrease in BFI. Thus, tablets containing plantain starch had lower tensile strength and disintegration time values than those containing corn starch, but showed better ability to reduce the lamination and capping tendency in paracetamol tablet formulation. The interaction between N and C was significantly (P < .001) higher than those between N and RD and between C and RD. There is therefore the need to carefully choose the nature (N) and concentration (C) of starch used as binding agent in tablet formulations to obtain tablets of desired bond strength and disintegration properties. Furthermore, plantain starch could be useful as an alternative binding agent to cornstarch, especially where faster disintegration is required and the problems of lamination and capping are of particular concern.

  18. Tablet Keiti: Does it Contain Astronomical Instructions?

    DEFF Research Database (Denmark)

    Wieczorek, Rafal

    2010-01-01

    Ethnographic data collected on Easter Island in the late XIX and first half of the XX century suggest that the extant rongorongo tablets contain songs, legends or other chanted traditions. However, we have yet to succeed in relating any one of the rongorongo texts to one of the many legends...... collected by ethnographers. An interesting observation is that, while none of the Rapanuis with whom early visitors to the island were acquainted mentioned anything about astronomy in the context of rongorongo tablets, the only piece of rongorongo texts whose meaning we are certain of is the “calendar...... tablet Mamari”. In the four lines of this tablet, also known as rongorongo text C, we encounter 30 moon glyphs arranged in a pattern that mirrors the Rapa Nui lunar calendar as recorded by early Western visitors. This presentation argues that yet another rongorongo item – tablet Keiti, also known as text...

  19. Development and validation of spectrophotometric method for assay determination and in vitro dissolution studies of sofosbuvir tablets

    International Nuclear Information System (INIS)

    Zaman, B.; Hassan, W.; Noreen, H.

    2017-01-01

    In vitro dissolution of sofosbuvir 400 mg tablets dosage form was performed, using USP dissolution apparatus type-II (paddle type), at 75rpm ± 4 %, and 900mL ± 1%, 0.05 M phosphate buffer pH 6.8 ± 0.05 equilibrated at 37.0 ± 0.5ºC as dissolution medium. Percentage of dissolved sofosbuvir as a function of time was determined using the straight line equation and linear regression using zero order and first order ANOVA based kinetics model. Comparative dissolution studies on two different generic brands A and B was performed comparing the drug release profile with innovator brand Sovaldi 400 mg tablets. The comparison of dissolution profiles was evaluated using model independent approach. The values of similarity factor f2 were (4 and 3) and the difference factor f1 were (64 and 50) for both generic products A and B respectively. A simple and precise spectrophotometric method was developed for estimation of sofosbuvir in dissolution medium based on spectrophotometric detection at wavelength 262 nm. The specific absorbance (A = 1%) of sofosbuvir was 178.5 ± 4% and Beer’s law was obeyed in the concentration ranges 4µg mL−1 to 48µg mL−1. The method was validated appropriately for accuracy, precision, linearity, and specificity, according the guidelines of United State Pharmacopoeia and International Conference on Harmonization. The calibration curve was linear with correlation coefficient (r > 0.9999) and there was no spectral interference from excipients present in the tablets dosage form. This method is precise, rapid and specific for determination of sofosbuvir in tablets dosage form and successfully applied for assay determination and in vitro dissolution studies. (author)

  20. The effect of food on gastrointestinal (GI) transit of sustained-release ibuprofen tablets as evaluated by gamma scintigraphy

    International Nuclear Information System (INIS)

    Borin, M.T.; Khare, S.; Beihn, R.M.; Jay, M.

    1990-01-01

    The GI transit of radiolabeled sustained-release ibuprofen 800-mg tablets in eight healthy, fed volunteers was monitored using external gamma scintigraphy. Ibuprofen serum concentrations were determined from blood samples drawn over 36 hr following dosing. Sustained-release ibuprofen tablets containing 0.18% of 170Er2O3 (greater than 96% 170Er) in the bulk formulation were manufactured under pilot-scale conditions and were radiolabeled utilizing a neutron activation procedure which converted stable 170Er to radioactive 171Er (t1/2 = 7.5 hr). At the time of dosing, each tablet contained 50 mu Ci of 171Er. Dosage form position were reported at various time intervals. In five subjects the sustained-release tablet remained in the stomach and eroded slowly over 7-12 hr, resulting in gradual increases in small bowel radioactivity. In the remaining three subjects, the intact tablet was ejected from the stomach and a gastric residence time of approximately 4 hr was measured. This is in marked contrast to a previous study conducted in fasted volunteers in which gastric retention time ranged from 10 to 60 min. Differences in GI transit between fed and fasted volunteers had little effect on ibuprofen bioavailability. AUC and Tmax were unaltered and Cmax was increased by 24%, which is in agreement with results from a previous, crossover-design food effect study

  1. A chromatographic method validation to quantify tablets Mephenesine of national production

    International Nuclear Information System (INIS)

    Suarez Perez, Yania; Izquierdo Castro, Adalberto; Milian Sanchez, Jana Daria

    2009-01-01

    Authors made validation of an analytical method by high performance liquid chromatography (HPLC) for quantification of Mephenesine in recently reformulated 500 mg tablets. With regard to its application to quality control, validation included the following parameters: linearity, accuracy, precision, and selectivity. Results were satisfactory within 50-150 % rank. In the case of its use in subsequent studies of chemical stability, the selectivity for stability and sensitivity was assessed. Estimated detection and quantification limits were appropriate, and the method was selective versus the possible degradation products. (Author)

  2. Efficacy and safety of milnacipran 100 mg/day in patients with fibromyalgia: results of a randomized, double-blind, placebo-controlled trial.

    Science.gov (United States)

    Arnold, Lesley M; Gendreau, R Michael; Palmer, Robert H; Gendreau, Judy F; Wang, Yong

    2010-09-01

    To assess the efficacy and safety of milnacipran at a dosage of 100 mg/day (50 mg twice daily) for monotherapy treatment of fibromyalgia. A double-blind, placebo-controlled trial was performed to assess 1,025 patients with fibromyalgia who were randomized to receive milnacipran 100 mg/day (n = 516) or placebo (n = 509). Patients underwent 4-6 weeks of flexible dose escalation followed by 12 weeks of stable-dose treatment. Two composite responder definitions were used as primary end points to classify the response to treatment. The 2-measure composite response required achievement of ≥30% improvement from baseline in the pain score and a rating of "very much improved" or "much improved" on the Patient's Global Impression of Change (PGIC) scale. The 3-measure composite response required satisfaction of these same 2 improvement criteria for pain and global status as well as improvement in physical function on the Short Form 36 (SF-36) physical component summary (PCS) score. After 12 weeks of stable-dose treatment, a significantly greater proportion of milnacipran-treated patients compared with placebo-treated patients showed clinically meaningful improvements, as evidenced by the proportion of patients meeting the 2-measure composite responder criteria (P recall pain score, PGIC score, SF-36 PCS and mental component summary scores, average pain severity score on the Brief Pain Inventory, Fibromyalgia Impact Questionnaire total score (all P total score (P = 0.036 versus placebo). Milnacipran was well tolerated by most patients, with nausea being the most commonly reported adverse event (placebo-adjusted rate of 15.8%). Milnacipran administered at a dosage of 100 mg/day improved pain, global status, fatigue, and physical and mental function in patients with fibromyalgia.

  3. Controlled-release tablet formulation of isoniazid.

    Science.gov (United States)

    Jain, N K; Kulkarni, K; Talwar, N

    1992-04-01

    Guar (GG) and Karaya gums (KG) alone and in combination with hydroxy-propylmethylcellulose (HPMC) were evaluated as release retarding materials to formulate a controlled-release tablet dosage form of isoniazid (1). In vitro release of 1 from tablets followed non-Fickian release profile with rapid initial release. Urinary excretion studies in normal subjects showed steady-state levels of 1 for 13 h. In vitro and in vivo data correlated (r = 0.9794). The studies suggested the potentiality of GG and KG as release retarding materials in formulating controlled-release tablet dosage forms of 1.

  4. Pediatric Dispersible Tablets: a Modular Approach for Rapid Prototyping.

    Science.gov (United States)

    Buck, Jonas; Huwyler, Jörg; Kühl, Peter; Dischinger, Angela

    2016-08-01

    The design of pediatric formulations is challenging. Solid dosage forms for children have to meet the needs of different ages, e.g. high number of dosing increments and strengths. A modular formulation strategy offering the possibility of rapid prototyping was applied. Different tablet compositions and the resulting tablet characteristics were investigated for dispersible tablets using customized analytical methods. Fluid bed granules were blended with extragranular components, and compressed to tablets. Disintegration behavior was studied with a Texture Analyzer and a Tensiometer. Methods for determination of disintegration time and water uptake of tablets were developed with a Texture Analyzer, and a Tensiometer, respectively. Twenty-two different tablet formulations were prepared and analyzed with respect to disintegration time, hardness, friability, and viscosity. Multivariate data analysis revealed a high impact of type and amount of viscosity enhancer on the disintegration behavior of tablets. An optimized formulation was selected with a disintegration time of 24 s. Methods providing additional information on the disintegration behavior of dispersible tablets compared to standard pharmacopoeia methods were established. Selecting the right type and level of viscosity enhancer and superdisintegrant was critical for developing pediatric tablets with a disintegration time of less than 30 s but still pleasant mouth feel.

  5. Ispaghula Husk-Based Extended Release Tablets of Diclofenac ...

    African Journals Online (AJOL)

    Purpose: To formulate extended-release tablets of diclofenac sodium based on ispaghula husk. Methods: Tablets with varying proportions of diclofenac sodium and ispaghula husk were formulated by wet granulation technique at a fixed compression force of 10 kN. The formulated tablets were evaluated for ...

  6. The variability of ecstasy tablets composition in Brazil.

    Science.gov (United States)

    Togni, Loraine R; Lanaro, Rafael; Resende, Rodrigo R; Costa, Jose L

    2015-01-01

    The content of ecstasy tablets has been changing over the years, and nowadays 3,4-methylenedioxymethamphetamine (MDMA) is not always present in the tablets. The aim of this study was to investigate the chemical composition in the seized tablets labeled as ecstasy. We analyzed samples from 150 different seizures made by Sao Paulo's State Police by gas chromatography-mass spectrometry. MDMA was present in 44.7% of the analyzed samples, and another twenty different active substances were identified in these tablets, such as caffeine, 2C-B, piperazines, amphetamines, phencyclidine, and others. Methamphetamine was present in 22% of these samples. The results demonstrate a huge shift in the pattern of trafficking of synthetic drugs, where MDMA has been replaced in tablets mostly by illicit psychoactive substances, in a clear attempt to bypass the law. The great variability in the tablets composition may lead to an increased risk of drug poisoning. © 2014 American Academy of Forensic Sciences.

  7. Pharmaceutical and analytical evaluation of triphalaguggulkalpa tablets

    OpenAIRE

    Savarikar, Shreeram S.; Barbhind, Maneesha M.; Halde, Umakant K.; Kulkarni, Alpana P.

    2011-01-01

    Aim of the Study: Development of standardized, synergistic, safe and effective traditional herbal formulations with robust scientific evidence can offer faster and more economical alternatives for the treatment of disease. The main objective was to develop a method of preparation of guggulkalpa tablets so that the tablets meet the criteria of efficacy, stability, and safety. Materials and Methods: Triphalaguggulkalpa tablet, described in sharangdharsanhita and containing guggul and triphala p...

  8. Electronic acquisition of OSCE performance using tablets

    Directory of Open Access Journals (Sweden)

    Hochlehnert, Achim

    2015-10-01

    Full Text Available Background: Objective Structured Clinical Examinations (OSCEs often involve a considerable amount of resources in terms of materials and organization since the scores are often recorded on paper. Computer-assisted administration is an alternative with which the need for material resources can be reduced. In particular, the use of tablets seems sensible because these are easy to transport and flexible to use.Aim: User acceptance concerning the use of tablets during OSCEs has not yet been extensively investigated. The aim of this study was to evaluate tablet-based OSCEs from the perspective of the user (examiner and the student examinee.Method: For two OSCEs in Internal Medicine at the University of Heidelberg, user acceptance was analyzed regarding tablet-based administration (satisfaction with functionality and the subjective amount of effort as perceived by the examiners. Standardized questionnaires and semi-standardized interviews were conducted (complete survey of all participating examiners. In addition, for one OSCE, the subjective evaluation of this mode of assessment was gathered from a random sample of participating students in semi-standardized interviews.Results: Overall, the examiners were very satisfied with using tablets during the assessment. The subjective amount of effort to use the tablet was found on average to be “hardly difficult”. The examiners identified the advantages of this mode of administration as being in particular the ease of use and low rate of error. During the interviews of the examinees, acceptance for the use of tablets during the assessment was also detected.Discussion: Overall, it was found that the use of tablets during OSCEs was well accepted by both examiners and examinees. We expect that this mode of assessment also offers advantages regarding assessment documentation, use of resources, and rate of error in comparison with paper-based assessments; all of these aspects should be followed up on in

  9. Formulation and evaluation of glipizide floating-bioadhesive tablets

    Directory of Open Access Journals (Sweden)

    Jayvadan K. Patel

    2010-10-01

    Full Text Available The purpose of this study was formulation and in vitro evaluation of floating-bioadhesive tablets to lengthen the stay of glipizide in its absorption area. Effervescent tablets were made using chitosan (CH, hydroxypropyl methylcellulose (HPMC, carbopolP934 (CP, polymethacrylic acid (PMA, citric acid, and sodium bicarbonate. Tablets with 5% effervescent base had longer lag time than 10%. The type of polymer had no significant effect on the floating lag time. All tablets floated atop the medium for 23-24 hr. Increasing carbopolP934 caused higher bioadhesion than chitosan (p < 0.05. All formulations showed a Higuchi, non-Fickian release mechanism. Tablets with 10% effervescent base, 80% CH/20% HPMC, or 80% CP/20% PMA seemed desirable.

  10. Breaking of scored tablets : a review

    NARCIS (Netherlands)

    van Santen, E; Barends, D M; Frijlink, H W

    The literature was reviewed regarding advantages, problems and performance indicators of score lines. Scored tablets provide dose flexibility, ease of swallowing and may reduce the costs of medication. However, many patients are confronted with scored tablets that are broken unequally and with

  11. Feasibility of mini-tablets as a flexible drug delivery tool.

    Science.gov (United States)

    Mitra, Biplob; Chang, Jessica; Wu, Sy-Juen; Wolfe, Chad N; Ternik, Robert L; Gunter, Thomas Z; Victor, Michael C

    2017-06-15

    Mini-tablets have potential applications as a flexible drug delivery tool in addition to their generally perceived use as multi-particulates. That is, mini-tablets could provide flexibility in dose finding studies and/or allow for combination therapies in the clinic. Moreover, mini-tablets with well controlled quality attributes could be a prudent choice for administering solid dosage forms as a single unit or composite of multiple mini-tablets in patient populations with swallowing difficulties (e.g., pediatric and geriatric populations). This work demonstrated drug substance particle size and concentration ranges that achieve acceptable mini-tablet quality attributes for use as a single or composite dosage unit. Immediate release and orally disintegrating mini-tablet formulations with 30μm to 350μm (particle size d 90 ) acetaminophen and Compap™ L (90% acetaminophen) at concentrations equivalent to 6.7% and 26.7% acetaminophen were evaluated. Mini-tablets achieved acceptable weight variability, tensile strength, friability, and disintegration time at a reasonable solid fraction for each formulation. The content uniformity was acceptable for mini-tablets of 6.7% formulations with ≤170μm drug substance, mini-tablets of all 26.7% formulations, and composite dosage units containing five or more mini-tablets of any formulation. Results supported the manufacturing feasibility of quality mini-tablets, and their applicability as a flexible drug delivery tool. Copyright © 2017 Elsevier B.V. All rights reserved.

  12. Evaluation of Tablets Divisibility in Pharmacoeconomic Aspects

    Directory of Open Access Journals (Sweden)

    Omer Yemsen

    2013-10-01

    Full Text Available Aim: Divisibility and dose homogeneity in scored tablets which form a part of the drugs those are in tablet forms in Turkey and have an extensive implementation area in drug therapy have a high importance for patient compliance and safety. In this study, it is aimed to evaluate Turkey%u2019s pharmaceutical market about cost differences of dividing scored tablets which has different unit quantities of the same active substance. Material and Method: In Turkey%u2019s pharmaceutical market, to detect cost differences of dividing scored tablets which has different unit quantities of the same active substance, All Drug%u2019s Price List that has been published on Turkish Medicine and Medical Devices Agency%u2019s web site is evaluated by using cost-minimization analysis method. Results: It is determined that the use of scored tablets make a price advantage of about 70%. Discussion: In conclusion, on package leaflets and outer packaging information those are prepared for the use of patients, the warning %u201CDon%u2019t divide, crack or swallow the tablets unless otherwise recommended by your doctor.%u201D should be stated and it is considered that it would be useful if the patient is informed about divisibility by the pharmacist.

  13. Avaliação das propriedades de fluxo dos granulados e dissolução de comprimidos de hidroclorotiazida 50 mg obtidos por granulação úmida Evaluation of the flow and the dissolution of 50 mg hydrochlorothiazide tablets obtained by wet granulation

    Directory of Open Access Journals (Sweden)

    Marco Aurélio Lamolha

    2007-09-01

    Full Text Available O processo de granulação úmida ainda encontra larga aplicabilidade junto à moderna indústria farmacêutica para a produção de comprimidos, pois elimina alguns dos principais problemas atribuídos à compressão direta: a tendência de segregação e as baixas propriedades de fluxo dos pós durante o processo. O presente trabalho avalia e compara através de estudos micromeríticos e análise estatística as características de fluxo de granulados destinados ao desenvolvimento de comprimidos de hidroclorotiazida 50 mg. Foram testados três aglutinantes (pasta de amido e as dispersões aquosas, preparadas a frio, de amido pré-gelatinizado e povidone. Avaliou-se ainda a compatibilidade entre o fármaco e os excipientes empregados, através de estudos termoanalíticos (DSC, e a influência da adição extragranular do superdesintegrante crospovidone nos valores de eficiência de dissolução (%ED dos comprimidos obtidos. Os granulados obtidos apresentaram propriedades de fluxo e compressibilidade boas a excelentes, caracterizadas por: valores de índice de compressibilidade situados entre 5 e 15; proporções de Hausner inferiores a 1,25 e ângulos de repouso entre 30 e 35º. A adição de crospovidone não incrementou os valores de %ED das formulações desenvolvidas, nas condições experimentais empregadas, ainda que tenha reduzido, de forma pouco significativa, os tempos de desintegração das formulações.The wet granulation process still finds large applicability close to the modern pharmaceutical industry for the production of tablets, because it eliminates some of the main attributed problems of the direct compression: the segregation tendency and the low flow properties of the powders during the process. The present work evaluates and it compares through micromeritical studies and statistical analysis the flow characteristics of granulates destined to the development of tablets of hydrochlorothiazide 50 mg. Three binders were

  14. Systematic Study of Au6 to Au12 Gold Clusters on MgO(100) F Centers Using Density-Functional Theory

    DEFF Research Database (Denmark)

    Vilhelmsen, Lasse; Hammer, Bjørk

    2012-01-01

    We present an optimized genetic algorithm used in conjunction with density-functional theory in the search for stable gold clusters and O2 adsorption ensembles in F centers at MgO(100). For Au8 the method recovers known structures and identifies several more stable ones. When O2 adsorption...

  15. Eudragit E100 and Polysaccharide Polymer Blends as Matrices for ...

    African Journals Online (AJOL)

    Methods: LB, SCMC and E100 were blended in their dry (as purchased) state or modified by aqueous blending and subsequent lyophilization, prior to use as matrices in tablets. ... pullulan from Aureobasidium pullulans, 3-(3,4- .... the frozen polymer before sublimation and drying). Subsequently, milling generated a more.

  16. Formulation development and in vitro evaluation of solidified self-microemulsion in the form of tablet containing atorvastatin calcium.

    Science.gov (United States)

    Ali, Kazi Asraf; Mukherjee, Biswajit; Bandyopadhyay, Amal Kumar

    2013-11-01

    The objective of our present study was to prepare solid self-microemulsion in the form of tablet of a poorly water soluble drug, Atorvastatin calcium (ATNC) to increase the solubility, dissolution rate, and minimize the hazards experienced from liquid emulsions. Self-microemulsifying ATNC tablet was formulated mainly by using self-emulsifying base, solidifying agent silicon dioxide and sodium starch glycolate as tablet disintegrant. Self-emulsifying base containing Transcutol P, Gelucire 44/14, and Lutrol F68 with their ratios in the formulation, were best selected by solubility study and ternary phase diagram in different vehicles. Particle size of microemulsion from tablet, physical parameters of the tablet and drug content has been checked. In vitro drug release rate has been carried out in phosphate buffer medium (pH 6.8). Physicochemical characterization of the drug in the optimized formulation has been performed to check drug-excipient incompatibility, if any. Average particle diameter of the emulsions formed from the tablet was found to be below 100 nm in case of formulation F4 and F5, which indicated microemulsions has been formed. In vitro drug release from the formulations F3, F4, and F5 was found to be >90%, indicated the enhancement of solubility of ATNC compared to parent drug. Differential thermal analysis (DTA), Powder X-ray Diffraction (X-RD) and Fourier transform infra red (FTIR) study proved the identity of the drug in the optimized formulation. The tablet form of self-microemulsifying (SME) drug delivery is good for solubility enhancement.

  17. Android Tablet Application Development For Dummies

    CERN Document Server

    Felker, Donn

    2011-01-01

    Get up to speed on the hottest opportunity in the application development arena App development for tablets is a booming business. Android tablets, including the popular Motorola Xoom, are gaining market share at breakneck speed, and this book can have even novice programmers creating great Android apps specifically for tablets quickly and easily. A little Java knowledge is helpful but not essential to get started creating apps. Android expert Donn Felker helps you get the Android environment up and running, use XML to create application menus, create an icon for your app, and submit your app

  18. Validação de método para determinação de 3,4-metilenodioximetanfetamina (MDMA em comprimidos de ecstasy por cromatografia em fase gasosa Validation of a gas-chromatographic method for the determination of 3,4-methylenedioxymethamphetamine(MDMA in ecstasy tablets

    Directory of Open Access Journals (Sweden)

    Silvio Fernandes Lapachinske

    2004-03-01

    Full Text Available O ecstasy é comercializado, de maneira ilegal, normalmente sob a forma de comprimidos, com cores, aspectos, dimensões e logotipos variados. Quimicamente, é a metilenodioximetanfetamina (MDMA, um composto sintético com propriedades estimulante central e alucinogênicas. Devido à grande expansão do abuso de ecstasy, também tem aumentado o número de casos de intoxicações, decorrentes diretamente da droga (MDMA e análogas e/ou de eventuais adulterantes. Algumas substâncias análogas à MDMA, já identificadas em comprimidos de ecstasy são: metilenodioxietilanfetamina (MDEA, metilenodioxianfetamina (MDA, metanfetamina e anfetamina. Como possíveis adulterantes, geralmente são encontradas cafeína e efedrinas. O objetivo deste trabalho foi a validação de um método analítico para quantificar a MDMA em comprimidos ou cápsulas de ecstasy, através da cromatografia em fase gasosa com detector de nitrogênio/fósforo (GC/NPD. Além disso, substâncias análogas à MDMA e adulterantes também foram identificados. O método, que consiste na dissolução direta da amostra em metanol, centrifugação e diluição do sobrenadante, demonstrou ser simples, rápido e eficiente. Os limites de detecção e quantificação para a MDMA foram respectivamente de 1,5 e 3,0 mg/100 mg de comprimido. Amostras de comprimidos e cápsulas apreendidos como sendo ecstasy provenientes de 25 lotes foram analisadas, apresentando considerável variabilidade na composição e na quantidade de MDMA.Ecstasy is illegally commercialized in the form of tablets with different aspects, colors, sizes, and logotypes. Chemically, ecstasy is 3,4-methylenedioxymethamphetamine (MDMA, a synthetic compound with stimulant and hallucinogenic proprieties. Due to the great expansion of ecstasy abuse, the number of cases of intoxications by MDMA, analogs and eventual adulterant compounds has also increased. Some MDMA analog substances, such as 3,4-methylenedioxyethylamphetamine (MDEA

  19. Growth of thin films of TiN on MgO(100) monitored by high-pressure RHEED

    DEFF Research Database (Denmark)

    Pryds, Nini; Cockburn, D.; Rodrigo, Katarzyna Agnieszka

    2008-01-01

    Reflection high-energy electron diffraction (RHEED) operated at high pressure has been used to monitor the initial growth of titanium nitride (TiN) thin films on single-crystal (100) MgO substrates by pulsed laser deposition (PLD). This is the first RHEED study where the growth of TiN films...... electron microscopy. These observations are in good agreement with the three-dimensional Volmer-Weber growth type, by which three-dimensional crystallites are formed and later cause a continuous surface roughening. This leads to an exponential decrease in the intensity of the specular spot in the RHEED...

  20. Development and validation of a dissolution test with reversed-phase liquid chromatography analysis for rupatadine in tablet dosage forms

    Directory of Open Access Journals (Sweden)

    Sérgio Luiz Dalmora

    2010-01-01

    Full Text Available A dissolution test for in vitro evaluation of tablet dosage forms containing 10 mg of rupatadine was developed and validated by RP-LC. A discriminatory dissolution method was established using apparatus paddle at a stirring rate of 50 rpm with 900 mL of deaerated 0.01 M hydrochloric acid. The proposed method was validated yielding acceptable results for the parameters evaluated, and was applied for the quality control analysis of rupatadine tablets, and to evaluate the formulation during an accelerated stability study. Moreover, quantitative analyses were also performed, to compare the applicability of the RP-LC and the LC-MS/MS methods.

  1. ESR accident dosimetry using medicine tablets coated with sugar

    International Nuclear Information System (INIS)

    Kai, A.; Miki, T.; Ikeya, M.

    1990-01-01

    Properties of radiation-induced radicals in medicine tablets were investigated using electron spin resonance (ESR). A sharp ESR signal sensitive to gamma ray irradiation was observed in the sugar coating part of the tablets. The signal has anisotropic g values of g 1 = 2.0009, g 2 = 2.0007 and g 3 = 2.0002. The signal grows linearly with dose at least up to about 20 Gy. No fading was observed at room temperature even when exposed to sunlight. The dose to artificially irradiated tablets was estimated using the signal intensity and a previously determined calibration curve. The signal in sugar coated tablets can be utilised for dose measurements. In particular, the wide distribution of sugar coated tablets allows the use of the tablets as accident dosemeters. (author)

  2. The best 100 free apps for libraries

    CERN Document Server

    Hahn, Jim

    2013-01-01

    Librarian Jim Hahn has carefully culled the over 500,000 available apps down to the 100 that are the absolute best for day-in, day-out library services. The guide covers apps from both Apple and Android devices, including tablets. This guide is intended as an introduction for those with little or no app experience and for those wanting to know more about app uses for information access.

  3. Galileo's Telescopy and Jupiter's Tablet

    Science.gov (United States)

    Usher, P. D.

    2003-12-01

    A previous paper (BAAS 33:4, 1363, 2001) reported on the dramatic scene in Shakespeare's Cymbeline that features the descent of the deity Jupiter. The paper suggested that the four ghosts circling the sleeping Posthumus denote the four Galilean moons of Jupiter. The god Jupiter commands the ghosts to lay a tablet upon the prone Posthumus, but says that its value should not be overestimated. When Posthumus wakens he notices the tablet, which he calls a "book." Not only has the deity's "tablet" become the earthling's "book," but it appears that the book has covers which Posthumus evidently recognizes because without even opening the book he ascribes two further properties to it: rarity, and the very property that Jupiter had earlier attributed, viz. that one must not read too much into it. The mystery deepens when the Jovian gift undergoes a second metamorphosis, to "label." With the help of the OED, the potentially disparate terms "tablet," "book," and "label," may be explained by terms appropriate either to supernatural or worldly beings. "Tablet" may recognize the Mosaic artifact, whereas "book" and "label" are probably mundane references to Galileo's Sidereus Nuncius which appeared shortly before Cymbeline. The message of the Olympian god indicates therefore that the book is unique even as its contents have limited value. The first property celebrates the fact that Galileo's book is the first of its kind, and the second advises that all results except the discovery of Jupiter's moons have been reported earlier, in Hamlet.

  4. A pilot study on quality of artesunate and amodiaquine tablets used in the fishing community of Tema, Ghana.

    Science.gov (United States)

    Affum, Andrews O; Lowor, Samuel; Osae, Shiloh D; Dickson, Adomako; Gyan, Benjamin A; Tulasi, Delali

    2013-06-28

    The ineffectiveness of artesunate and amodiaquine tablets in malaria treatment remains a health burden to WHO and governments of malaria-endemic countries, including Ghana. The proliferation of illegitimate anti-malarial drugs and its use by patients is of primary concern to international and local drug regulatory agencies because such drugs are known to contribute to the development of the malaria-resistant parasites in humans. No data exist on quality of these drugs in the fishing village communities in Ghana although the villagers are likely users of such drugs. A pilot study on the quality of anti-malarial tablets in circulation during the major fishing season at a malarious fishing village located along the coast of Tema in southern Ghana was determined. Blisterpacks of anti-malarial tablets were randomly sampled. The International Pharmacopoeia and Global Pharma Health Fund Minilab protocols were used to assess the quality of anti-malarial tablets per blisterpacks allegedly manufactured by Guilin Pharmaceutical Co Ltd, China (GPCL) and Letap Pharmaceuticals Ltd, Ghana (LPL) and sold in chemical sales outlets at Kpone-on-Sea. Ferric chloride and cobaltous thiocyanate tests confirmed the presence of active ingredients in the tablets. A confirmatory test for the active ingredient was achieved with artesunate (ICRS1409) and amodiaquine (ICRS0209) reference standards. A high performance liquid chromatography analysis confirmed the amount of artesunate found in tablets. Based on the International Pharmacopoeia acceptable range of 96/98 to 102% for genuine artesunate per tablet, 10% [relative standard deviation (RSD): 3.2%] of field-selected artesunate blisterpack per tablets manufactured by GPCL, and 50% (RSD: 5.1%) of a similar package per tablet by LPL, passed the titrimetric test. However, 100% (RSD: 2.2%) of amodiaquine blisterpack per tablet by GPCL were found to be within the International Pharmacopeia acceptable range of 90 to 110% for genuine amodiaquine in

  5. Does the performance of wet granulation and tablet hardness affect the drug dissolution profile of carvedilol in matrix tablets?

    Science.gov (United States)

    Košir, Darjan; Ojsteršek, Tadej; Vrečer, Franc

    2018-06-14

    Wet granulation is mostly used process for manufacturing matrix tablets. Compared to the direct compression method, it allows for a better flow and compressibility properties of compression mixtures. Granulation, including process parameters and tableting, can influence critical quality attributes (CQAs) of hydrophilic matrix tablets. One of the most important CQAs is the drug release profile. We studied the influence of granulation process parameters (type of nozzle and water quantity used as granulation liquid) and tablet hardness on the drug release profile. Matrix tablets contained HPMC K4M hydrophilic matrix former and carvedilol as a model drug. The influence of selected HPMC characteristics on the drug release profile was also evaluated using two additional HPMC batches. For statistical evaluation, partial least square (PLS) models were generated for each time point of the drug release profile using the same number of latent factors. In this way, it was possible to evaluate how the importance of factors influencing drug dissolution changes in dependence on time throughout the drug release profile. The results of statistical evaluation show that the granulation process parameters (granulation liquid quantity and type of nozzle) and tablet hardness significantly influence the release profile. On the other hand, the influence of HPMC characteristics is negligible in comparison to the other factors studied. Using a higher granulation liquid quantity and the standard nozzle type results in larger granules with a higher density and lower porosity, which leads to a slower drug release profile. Lower tablet hardness also slows down the release profile.

  6. [The effects of various factors on the in vitro velocity of drug release from repository tablets. Part 4: Isoniazid (Rimicid) respository tablets (author's transl)].

    Science.gov (United States)

    Tomassini, L; Michailova, D; Naplatanova, D; Slavtschev, P

    1979-12-01

    The authors investigated the release of isoniazid from repository tablets as related to form, processing technology, strength constant and storage for 5 years. On determining the diffusion coefficient (D), the initial dissolution rate (Vo) and the time required for the diffusion of the releasing medium to the middle of the tablet (t1/2), it was found that the difference in release rate between the flat and the biconvex tablets is small. Furthermore, it was stated that the three-layer tablets have very high D and Vo values and very low t1/2 values, for what reason they are unsuited for repository tablets of the composition under investigation. Moreover, it was found that an increase of the strength constant does not affect the D, t1/2 and Vo values, and that the release of isoniazid is retarded only in flat tablets with the highest strength constant. Storage exerts no effect on the drug release from these tablets. The industrial production of these tablets is under way.

  7. Use of hydrophilic and hydrophobic polymers for the development of controlled release tizanidine matrix tablets

    Directory of Open Access Journals (Sweden)

    Tariq Ali

    2014-12-01

    Full Text Available The aim of the present study was to develop tizanidine controlled release matrix. Formulations were designed using central composite method with the help of design expert version 7.0 software. Avicel pH 101 in the range of 14-50% was used as a filler, while HPMC K4M and K100M in the range of 25-55%, Ethylcellulose 10 ST and 10FP in the range of 15 - 45% and Kollidon SR in the range of 25-60% were used as controlled release agents in designing different formulations. Various physical parameters including powder flow for blends and weight variation, thickness, hardness, friability, disintegration time and in-vitro release were tested for tablets. Assay of tablets were also performed as specified in USP 35 NF 32. Physical parameters of both powder blend and compressed tablets such as compressibility index, angle of repose, weight variation, thickness, hardness, friability, disintegration time and assay were evaluated and found to be satisfactory for formulations K4M2, K4M3, K4M9, K100M2, K100M3, K100M9, E10FP2, E10FP9, KSR2, KSR3 & KSR9. In vitro dissolution study was conducted in 900 ml of 0.1N HCl, phosphate buffer pH 4.5 and 6.8 medium using USP Apparatus II. In vitro release profiles indicated that formulations prepared with Ethocel 10 standard were unable to control the release of drug while formulations K4M2, K100M9, E10FP2 & KSR2 having polymer content ranging from 40-55% showed a controlled drug release pattern in the above mentioned medium. Zero-order drug release kinetics was observed for formulations K4M2, K100M9, E10FP2 & KSR2. Similarity test (f2 results for K4M2, E10FP2 & KSR2 were found to be comparable with reference formulation K100M9. Response Surface plots were also prepared for evaluating the effect of independent variable on the responses. Stability study was performed as per ICH guidelines and the calculated shelf life was 24-30 months for formulation K4M2, K100M9 and E10FP2.

  8. Relative bioavailability of diclofenac potassium from softgel capsule versus powder for oral solution and immediate-release tablet formulation.

    Science.gov (United States)

    Bende, Girish; Biswal, Shibadas; Bhad, Prafulla; Chen, Yuming; Salunke, Atish; Winter, Serge; Wagner, Robert; Sunkara, Gangadhar

    2016-01-01

    The oral bioavailability of diclofenac potassium 50 mg administered as a soft gelatin capsule (softgel capsule), powder for oral solution (oral solution), and tablet was evaluated in a randomized, open-label, 3-period, 6-sequence crossover study in healthy adults. Plasma diclofenac concentrations were measured using a validated liquid chromatography-mass spectrometry/mass spectrometry method, and pharmacokinetic analysis was performed by noncompartmental methods. The median time to achieve peak plasma concentrations of diclofenac was 0.5, 0.25, and 0.75 hours with the softgel capsule, oral solution, and tablet formulations, respectively. The geometric mean ratio and associated 90%CI for AUCinf, and Cmax of the softgel capsule formulation relative to the oral solution formulation were 0.97 (0.95-1.00) and 0.85 (0.76-0.95), respectively. The geometric mean ratio and associated 90%CI for AUCinf and Cmax of the softgel capsule formulation relative to the tablet formulation were 1.04 (1.00-1.08) and 1.67 (1.43-1.96), respectively. In conclusion, the exposure (AUC) of diclofenac with the new diclofenac potassium softgel capsule formulation was comparable to that of the existing oral solution and tablet formulations. The peak plasma concentration of diclofenac from the new softgel capsule was 67% higher than the existing tablet formulation, whereas it was 15% lower in comparison with the oral solution formulation. © 2015, The American College of Clinical Pharmacology.

  9. Carbon Break Even Analysis: Environmental Impact of Tablets in Higher Education

    OpenAIRE

    Fadi Safieddine; Imad Nakhoul

    2016-01-01

    With the growing pace of tablets use and the large focus it is attracting especially in higher education, this paper looks at an important aspect of tablets; their carbon footprint. Studies have suggested that tablets have positive impact on the environment; especially since tablets use less energy than laptops or desktops. Recent manufacturers’ reports on the carbon footprint of tablets have revealed that a significant portion, as much as 80%, of the carbon footprint of tablets comes from pr...

  10. Understanding abuse of buprenorphine/naloxone film versus tablet products using data from ASI-MV® substance use disorder treatment centers and RADARS® System Poison Centers.

    Science.gov (United States)

    Butler, Stephen F; Black, Ryan A; Severtson, Stevan Geoffrey; Dart, Richard C; Green, Jody L

    2018-01-01

    The objectives were to examine the abuse prevalence and route-of-administration (ROA) profiles of sublingual buprenorphine/naloxone combination (BNX) film in comparison with the BNX tablet and to identify clinically-relevant subgroups of patients or geographic patterns. Between Q1 2015 through Q3 2015, data were collected from two major surveillance systems: (1) assessment of individuals in substance use disorder (SUD) treatment collected from the National Addictions Vigilance Intervention and Prevention Program (NAVIPPRO®) ASI-MV® system and (2) intentional abuse/misuse exposures in the RADARS® System Poison Center Program. Poisson regression models were tailored to each system's data characteristics by population (all SUD treatment patients, US census) and adjusted for prescription volume. Effects of gender, race, age and US region as well as ROA profile were examined. For the ASI-MV study, 45,695 assessments of unique adults evaluated for substance use problems were collected. The abuse rate unadjusted for prescription volume of BNX tablet formulation was 2.64 cases/100 ASI-MV respondents versus 7.01 cases for the film formulation (RR=0.390, pfilm) (RR=1.25, pfilm abuse (0.0364) were greater than for tablet (0.0161), while prescription-adjusted rates were greater for tablet (0.2114) than for film (0.1703) per 100,000 prescriptions. ASI-MV ROA analyses indicated less abuse of the film by any alternate route, insufflation or injection than the tablet. Poison center data found more injection of tablets than film, although insufflation was not significantly different. On a prescription-adjusted basis, overall abuse of the BNX tablet is greater than that of the sublingual film formulation. For those who continue to abuse BNX, use by alternate ROAs was, in general, lower for the film. Copyright © 2017 Elsevier Inc. All rights reserved.

  11. Development and evaluation of fixed dose bi therapy sublingual tablets for treatment stress hypertension and anxiety

    Directory of Open Access Journals (Sweden)

    Mohamed A El-Nabarawi

    2013-01-01

    Full Text Available Objective: A stress induced rise in the blood pressure. Some believe that patients with hypertension are characterized by a generalized state of increased anxiety. Aim: The purpose of this study is to prepare a fixed dose bi therapy using bisoprolol hemifumarate (BH as antihypertensive drug and buspirone hydrochloride (BuHCl as anxiolytic drug, which can be used to treat both diseases concomitantly. Using sublingual tablets is hopeful to improve the BuHCl poor oral bioavailability and to facilitate administration to patients experiencing problems with swallowing. Materials and Methods: A total of 5mg BH and 10mg BuHCl were selected based on compatibility study. A 3×22 full factorial design was adopted for the optimization of the tablets prepared by direct compression method. The effects of the filler type, the binder molecular weight, and the binder type were studied. The prepared formulae were evaluated according to their physical characters as hardness, friability, disintegration time (new modified method and in vivo disintegration time and wetting properties. In vitro drugs dissolute, permeation through the buccal mucosa and the effect of storage were analyzed by a new valid high pressure liquid chromatography (HPLC method. Bioavailability study of the selected formula study was carried out and followed by the clinical. Results: The optimized tablet formulation showed accepted average weight, hardness, wetting time, friability, content uniformity, disintegration time (less than 3 min. Maximum drug release could be achieved with in 10 min. In addition enhancing drug permeation through the buccal mucosa and, the maximum concentration of the drug that reached the blood was in the first 10 min which means a rapid onset of action and improved the extent of both drug′s absorption. Conclusion: The results revealed that sublingual (F6 tablets containing both drugs would maintain rapid onset of action, and increase bioavailability. BuHCl with BH

  12. An evaluation of total disintegration time for three different doses of sublingual fentanyl tablets in patients with breakthrough pain.

    Science.gov (United States)

    Nalamachu, Srinivas

    2013-12-01

    Breakthrough pain is common among patients with cancer and presents challenges to effective pain management. Breakthrough pain is characterized by rapid onset, severe intensity, and duration typically lasting disintegration time of three different doses of sublingual fentanyl tablets in opioid-tolerant patients. This was a single-center, non-randomized, open-label study. Opioid-tolerant adult patients (N = 30) with chronic pain were assigned to one of three dose groups and self-administered a single 100, 200, or 300 μg sublingual fentanyl tablet (Abstral(®), Galena Biopharma, Portland, OR, USA). Time to complete disintegration was measured by each patient with a stopwatch and independently verified by study personnel. Disintegration time (mean ± SD) for sublingual fentanyl tablets (all doses) was 88.2 ± 55.1 s. Mean disintegration times tended to be slightly longer for the 200 μg (96.7 ± 57.9 s) and 300 μg doses (98.6 ± 64.8 s) compared to the 100 μg dose (69.5 ± 40.5 s). Differences were not statistically significant. Disintegration time was not significantly different between men and women and was not affected by age. Sublingual fentanyl tablets dissolved rapidly (average time <2 min) in all patients, with the higher doses taking slightly more time to dissolve.

  13. Giving Iron Tablets by Health Worker and Pregnant Compliance in Consuming More Than 90 Tablets, in The Slum Urban, in The West Java Province and Yogyakarta

    Directory of Open Access Journals (Sweden)

    Tumaji Tumaji

    2015-03-01

    Full Text Available ABSTRAKLatar Belakang: Angka kematian ibu di Indonesia saat ini masih cukup tinggi dan sangat bervariasi di tingkat provinsi. Provinsi Jawa Barat (Jabar merupakan penyumbang kematian ibu terbesar yaitu 19,8%, sedangkan yang relatif kecil adalah Provinsi Daerah Istimewa Yogyakarta (DIY yaitu 1,1%. Mencegah anemia pada ibu hamil dengan minum tablet besi ≥ 90 selama hamil diharapkan mampu menekan kematian ibu akibat perdarahan. Tujuan: Membandingkan pemberian tablet zat besi oleh tenaga kesehatan dan kepatuhan ibu hamil mengonsumsinya, di daerah kumuh perkotaan di Provinsi Jabar dan DIY. Metode: Penelitian ini merupakan analisis lanjut objek dengan sampel dari data hasil Riskesdas 2010. Hasil: Berdasarkan karakteristik, sebagian besar ibu di Provinsi DIY berpendidikan tingkat menengah, bekerja sebagai wiraswasta/tani/nelayan/buruh. Sedangkan di Provinsi Jabar, sebagian besar hanya berpendidikan rendah dan tidak memiliki pekerjaan. Jumlah kepemilikan asuransi kesehatan di Provinsi DIY relatif lebih banyak dibanding di Provinsi jabar. Berdasarkan cakupan pemberian tablet zat besi, tampak bahwa sebagian besar ibu di Provinsi Jabar maupun DIY mendapatkan tablet zat besi selama kehamilannya (84,7% vs 96,0%. Kondisi ini jauh berbeda ketika dilihat dari persentase ibu hamil yang mengonsumsi tablet zat besi minimal 90 tablet. Terlihat bahwa ibu hamil yang mengonsumsi tablet zat besi ≥ 90 di Provinsi Jabar hanya 12,6% saja. Sebaliknya di Provinsi DIY, konsumsi tablet zat besi ≥ 90 persentasenya cukup tinggi yaitu mencapai 60,0%. Kesimpulan: Cakupan pemberian tablet zat besi di kedua provinsi relatif cukup baik, namun konsumsi tablet zat besi ≥ 90 tablet di Provinsi DIY relatif lebih baik dibanding di Provinsi di Jabar. Saran: disarankan pemerintah Provinsi Jabar melakukan promosi dan penyuluhan yang lebih gencar melalui berbagai media serta melakukan terobosan, misalnya dengan menunjuk orang terdekat dari si ibu hamil untuk menjadi pengawas dan

  14. Teach yourself visually Windows 8 tablets

    CERN Document Server

    McFedries, Paul

    2012-01-01

    A visual guide to all the features of the new Windows 8 Tablet This must-have resource features visually rich, step-by-step instructions that show you how to get the most enjoyment from your Windows 8 tablet. Learn about the exciting new Metro UI, optimized specifically for touch devices. The most popular and commonly used apps and functions are covered too, along with the basics of syncing with a network, setting up e-mail, watching videos, listening to music, and common productivity tasks. This book provides all the guidance needed to enjoy all the best the new Windows 8 tablets have to offe

  15. Understanding the Delamination Risk of a Trilayer Tablet Using Minipiloting Tools.

    Science.gov (United States)

    Tao, Jing; Robertson-Lavalle, Sophia; Pandey, Preetanshu; Badawy, Sherif

    2017-11-01

    A multilayer tablet is one of the formulation options used to mitigate chemical and physical incompatibility between different drug substances. Feasibility studies of multilayer tablets are often conducted using round flat-faced punch tooling. However, the link between different tooling designs and multilayer tablet performance is not well established. This study uses a prototype trilayer tablet and examines tooling design considerations when conducting small-scale studies to gauge the risk of interfacial defects. The impact of tablet weight and dimensions was evaluated to gain understanding of the effect of scale-up/down of tablet size. The factors in tooling selection, including tablet shape, cup depth, and size of embossing were evaluated to gain insight on the impact of tooling design on the interfacial strength of the trilayer tablet. It was found that tablet weight and dimensions can significantly affect the interfacial strength due to their impact on force transmission during compression and the retardation force from the die wall during ejection. Round flat-faced tooling generated trilayer tablets of the strongest interfacial strength compared to typical commercial tablets-oval shaped with concave surfaces. These factors should be accounted for when using round flat compacts to assess the interface risks of a multilayer tablet. Copyright © 2017 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

  16. Værsgo' ta' en tablet. Om brugen af tablets i dansk

    DEFF Research Database (Denmark)

    Lorentzen, Rasmus Fink

    2014-01-01

    Hvordan kan vi udvikle elevernes faglighed ved hjælp af it? Hvad er det i det hele taget vigtigt at lære i en tidssvarende folkeskole, så eleverne bliver klædt på til fremtidens samfund? Og kan iPads bruges til dette? Dette kapitel handler om fagdidaktik og tablets i undervisningen.......Hvordan kan vi udvikle elevernes faglighed ved hjælp af it? Hvad er det i det hele taget vigtigt at lære i en tidssvarende folkeskole, så eleverne bliver klædt på til fremtidens samfund? Og kan iPads bruges til dette? Dette kapitel handler om fagdidaktik og tablets i undervisningen....

  17. Efficacy and safety of 5-grass pollen sublingual immunotherapy tablets in patients with different clinical profiles of allergic rhinoconjunctivitis

    DEFF Research Database (Denmark)

    Malling, Hans-Jørgen; Montagut, A; Melac, M

    2009-01-01

    pollen sublingual tablets of 100 IR (index of reactivity), 300 IR or 500 IR, or placebo starting 4 months before the pollen season. OBJECTIVE: The aim of this complementary analysis was to determine whether 300 IR 5-grass pollen SLIT-tablets is effective in different subtypes of patients who are allergic......BACKGROUND: The optimal dose of grass pollen tablets for sublingual immunotherapy (SLIT) in allergic rhinoconjunctivitis patients was previously established in a multinational, randomized, double-blind, placebo-controlled study in 628 adults. Patients were randomized to receive once-daily 5-grass...... to grass pollen. METHODS: Different subgroups could be identified regarding comorbidities (with or without asthma during the grass-pollen season), sensitization (mono/polysensitization) and symptom severity. An additional exploratory analysis was performed within four subgroups based on pre...

  18. Formulation and Evaluation of Ascorbic acid Tablets by Direct ...

    African Journals Online (AJOL)

    Formulation and Evaluation of Ascorbic acid Tablets by Direct Compression using Microcrystalline Starch as a Direct Compression Excipient. ... Abstract. PURPOSE: To evaluate the tableting properties of microcrystalline starch (MCS) used as a direct ... RESULTS: Mechanical properties of tablets formulated with MCS were

  19. Investigation of excipients’ nature influence on the quality indices of effervescent tablets of acetylsalicylic acid, paracetamol and ascorbic acid

    Directory of Open Access Journals (Sweden)

    О. V. Tryhubchak

    2018-03-01

    Full Text Available The priority objective of pharmaceutical science remains the creation and rational use of medicines. In recent years among these medicines particular attention is paid to the form of sparkling (fast-dissolving, gaseous or effervescent solid dosage forms – tablets, granules, powders, microspheres, capsules, suppositories and others. In the development of effervescent tablets, which are absent in the domestic market, a combination of acetylsalicylic acid, paracetamol and ascorbic acid was selected for experimental studies. The purpose of the work is to study the influence of excipients on the pharmaco-technological properties of effervescent tablets of acetylsalicylic acid, paracetamol and ascorbic acid. Materials and methods. In the course of the experiment, nine excipients from groups of fillers, leavens and binders were investigated. By studying qualitative factors, one of the plans of dispersion analysis was used, namely a three-factorial experiment based on the Hyper-Greek-Latin square. In experiments we used modern equipment for determining the bulk density of powders (ERWEKA GT, Germany, bulk density (ERWEKA SVM 202, Germany, tablet press (Korsh XL-100, Germany, uniformity of the weight of tablets (Mettler Toledo AB54-S, Switzerland, crushing resistance (ERWEKA TBH-525 WTO, Germany, abradability (ERWEKA TAR 200, Germany, disintegration time (ERWEKA ZT 33, Germany. Results. As a result of the statistical processing of experimental results, the influence of excipients on the pharmaco-technological parameters of mass for tableting (bulk density, density after compression, Carr's index, flow ability, slope angle, tableting process, tablet appearance, mass uniformity, abradability, resistance to crushing, disintegration and transparency of the solution were investigated. Conclusions. The influence of nine excipients on the pharmaco-technological characteristics of effervescent tablets of acetylsalicylic acid, paracetamol and ascorbic acid was

  20. Estudio de bioequivalencia de clonazepam, tabletas de 2 mg, en voluntarios sanos colombianos Bioequivalence study of clonazepam 2 mg tablets in colombian healthy volunteers

    Directory of Open Access Journals (Sweden)

    Victoria Eugenia Toro Pareja

    2007-08-01

    Full Text Available Con el fin de determinar la bioequivalencia de dos formulaciones de tabletas de 2 mg de clonazepam: Sedatril®/Clonazepam MK (Tecnoquímicas S. A., Cali, Colombia como producto de prueba y Rivotril® (Roche Químicos e Farmacéuticas S. A., Río de Janeiro, Brasil, como producto de referencia, se realizó un estudio de bioequivalencia en 26 voluntarios sanos. Los productos de prueba y de referencia se administraron en condiciones de ayuno de acuerdo con un diseño cruzado aleatorio de dosis única, con dos secuencias, dos tratamientos y un período de lavado de 28 días. Las muestras de sangre se obtuvieron desde las 0 hasta las 96 horas después de la administración del medicamento. Los niveles plasmáticos de clonazepam se determinaron con un método validado por cromatografía líquida de alta eficiencia con detección ultravioleta (HPLC/UV, siglas en inglés. Los parámetros farmacocinéticos ABC0-96, ABC0-∞, Cmax, Tmax, t1/2, and ke se determinaron de los perfiles plasmáticos concentración-tiempo por el método no compartimental. El test de bioequivalencia se realizó con los datos transformados a logaritmo natural (ln de ABC0-∞and Cmax. Los intervalos de confianza del 90% para la relación producto de prueba/producto de referencia fueron de 87,9% a 103,6% y 84,4% a 104,0%, respectivamente. Estos resultados estuvieron dentro de los rangos de aceptación del 80,0% al 125%, establecidos por la FDA y se concluyó que ambos productos son bioequivalentes. In order to determine the bioequivalence of two formulations of clonazepam 2 mg tablets: Sedatril®/ Clonazepam MK (Tecnoquímicas S. A., Cali, Colombia as a test product and Rivotril® (Roche Químicos e Farmacêuticas S. A., Rio de Janeiro, Brazil as a reference product, a bioavailability study was performed in 26 healthy volunteers. Test and reference products were administered under fasting conditions following a single dose, two-sequences, two treatments, crossover randomized

  1. Bioavailability and stability of erythromycin delayed release tablets.

    Science.gov (United States)

    Ogwal, S; Xide, T U

    2001-12-01

    Erythromycin is available as the free base, ethylsuccinate, estolate, stearate, gluceptate, and lactobionate derivatives. When given orally erythromycin and its derivatives except the estolate are inactivated to some extent by the gastric acid and poor absorption may result. To establish whether delayed release erythromycin tablets meet the bioequivalent requirement for the market. Sectrophotometric analysis was used to determine the dissolution percentage of the tablets in vitro. High performance liquid chromatography and IBM/XT microcomputer was used to determine the bioavailability and pharmacokinetic parameters in vivo. Dissolution percentage in thirty minutes reached 28.9% and in sixty minutes erythromycin was completely released. The parameters of the delayed release tablets were Tlag 2.3 hr, Tmax.4.5 hr, and Cmax 2.123 g/ml Ka 0.38048 hr(-1) T (1/2) 1.8 hr, V*C/F 49.721 AUC 12.9155. The relative bioavailability of erythromycin delayed release tablet to erythromycin capsules was 105.31% The content, appearance, and dissolution bioavailability of delayed release erythromycin tablets conforms to the United States pharmacopoeia standards. The tablets should be stored in a cool and dry place in airtight containers and the shelf life is temporarily assigned two years.

  2. The Disintegration Process in Microcrystalline Cellulose Based Tablets, Part 1: Influence of Temperature, Porosity and Superdisintegrants

    Science.gov (United States)

    Yassin, Samy; Goodwin, Daniel J; Anderson, Andrew; Sibik, Juraj; Wilson, D Ian; Gladden, Lynn F; Zeitler, J Axel

    2015-01-01

    Disintegration performance was measured by analysing both water ingress and tablet swelling of pure microcrystalline cellulose (MCC) and in mixture with croscarmellose sodium using terahertz pulsed imaging (TPI). Tablets made from pure MCC with porosities of 10% and 15% showed similar swelling and transport kinetics: within the first 15 s, tablets had swollen by up to 33% of their original thickness and water had fully penetrated the tablet following Darcy flow kinetics. In contrast, MCC tablets with a porosity of 5% exhibited much slower transport kinetics, with swelling to only 17% of their original thickness and full water penetration reached after 100 s, dominated by case II transport kinetics. The effect of adding superdisintegrant to the formulation and varying the temperature of the dissolution medium between 20°C and 37°C on the swelling and transport process was quantified. We have demonstrated that TPI can be used to non-invasively analyse the complex disintegration kinetics of formulations that take place on timescales of seconds and is a promising tool to better understand the effect of dosage form microstructure on its performance. By relating immediate-release formulations to mathematical models used to describe controlled release formulations, it becomes possible to use this data for formulation design. © 2015 The Authors. Journal of Pharmaceutical Sciences published by Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 104:3440–3450, 2015 PMID:26073446

  3. A Method for Decreasing the Amount of the Drug Remaining on the Surfaces of the Mortar and Pestle after Grinding Small Amount of Tablets.

    Science.gov (United States)

    Kawakami, Miki; Kitada, Rika; Kurita, Takuro; Tokumura, Tadakazu

    2017-01-01

    The aim of the present study was to develop a method for grinding tablets with a mortar and pestle while reducing drug loss because grinding tablets is known to be associated with reductions in tablet weight and loss of the active drug. Seven kinds of tablets were subjected to grinding. The proportion (%) of the amount of the active drug in the powder remaining on the surfaces of the mortar and pestle relative to the total amount of the drug recovered (the recovery percent) was calculated. The recovery percent of the 7 kinds of tablets ranged from 17.2-35.9%, and the tablets' recovery percent decreased as the tablet weight increased. When the grinding was performed with 1 g of lactose monohydrate or 1 g of D-mannitol moistened with water, the recovery percent of the tablets decreased to 2.6-9.9% and 3.8-9.9%, respectively. The effects of the weight of lactose monohydrate on the recovery percent of Allegra ® 60 mg tablets were examined. It was found that at least 0.6 g of lactose monohydrate was required to have a sufficient effect on drug recovery. Therefore, additives that have stronger effects at lower amounts were sought. As a result, calcium monohydrogen phosphate was found to have the strongest effect on drug recovery. The addition of 0.4 g calcium monohydrogen phosphate resulted in the recovery percent of 5.1%, which was significantly lower than that of 15.0% observed after the addition of 0.4 g lactose monohydrate, and lower than the 6.8% of 1 g lactose monohydrate.

  4. Comparison of characteristics of LiF:Mg,Ti e LiF:Mg,Cu,P thermoluminescent dosemeters; Comparacao das caracteristicas dos dosimetros termoluminescentes LiF:Mg,Ti e LiF:Mg,Cu,P

    Energy Technology Data Exchange (ETDEWEB)

    Pereira, M.S.; Filipov, D., E-mail: dfilipov@utfpr.edu.br [Universidade Tecnologica Federal do Parana (UTFPR/DAFIS), Curitiba, PR (Brazil). Departamento Academicao de Fisica; Schelin, H.R. [Instituto de Pesquisa Pele Pequeno Principe (IPPPP), Curitiba, PR (Brazil)

    2014-07-01

    The aim of the current study was to compare the thermoluminescent dosimeters LiF:Mg,Ti (TLD-100) and LiF:Mg,Cu,P (MCP) data, which were acquired by the Federal Technological University - Parana. Tests were realized, for this purpose, such as: sensitivity (only one MCP TLD did not present results within the limit range), linearity (whose MCP result was better than the TLD-100 one), energy dependence (TLD-100 presented lower variation than MCP TLD) and reproducibility (whose TLD-100 results were better than the MCP ones). The results from both dosimeters show that these TLDs attend radiodiagnostic dosimetry criteria, however MCP had more satisfactory results. (author)

  5. Development and Evaluation of Mucoadhesive Chlorhexidine Tablet ...

    African Journals Online (AJOL)

    Purpose: To formulate mucoadhesive chlorhexidine tablets and evaluate their drug release characteristics and mechanism. Methods: Chlorhexidine buccal adhesive tablets were prepared by direct compression using a blend of hydroxypropyl methylcellulose (HPMC) and chitosan as the bioadhesive polymers.

  6. Novel platens to measure the hardness of a pentagonal shaped tablet.

    Science.gov (United States)

    Malladi, Jaya; Sidik, Kurex; Wu, Sutan; McCann, Ryan; Dougherty, Jeffrey; Parab, Prakash; Carragher, Thomas

    2017-03-01

    Tablet hardness, a measure of the breaking force of a tablet, is based on numerous factors. These include the shape of the tablet and the mode of the application of force. For instance, when a pentagonal-shaped tablet was tested with a traditional hardness tester with flat platens, there was a large variation in hardness measurements. This was due to the propensity of vertices of the tablet to crush, referred to as an "improper break". This article describes a novel approach to measure the hardness of pentagonal-shaped tablets using modified platens. The modified platens have more uniform loading than flat platens. This is because they reduce loading on the vertex of the pentagon and apply forces on tablet edges to generate reproducible tablet fracture. The robustness of modified platens was assessed using a series of studies, which included feasibility and Gauge Repeatability & Reproducibility (R&R) studies. A key finding was that improper breaks, generated frequently with a traditional hardness tester using flat platens, were eliminated. The Gauge R&R study revealed that the tablets tested with novel platens generated consistent values in hardness measurements, independent of batch, hardness level, and day of testing, operator and tablet dosage strength.

  7. Enteric coating of ibuprofen tablets (200 mg using an aqueous dispersion system

    Directory of Open Access Journals (Sweden)

    Rabia Bushra

    2010-03-01

    Full Text Available Ibuprofen is a propionic acid derivative that belongs to the class NSAIDs. Major adverse reactions associated with Ibuprofen are related to GIT and include peptic and mucosal ulcers, dyspepsia, severe gastric pain and bleeding, that results in excessive treatment failure. The goal of this study was to develop enteric coated ibuprofen tablets in order to avoid gastric mucosal irritation, diffusion of drug across mucosal lining and to let active ingredient be absorbed easily in small intestine. The formulation was developed and manufactured through the direct compression process, the simplest, easiest and most economical method of manufacturing. Enteric coating was done using an Opadry white subcoating and an aqueous coating dispersion of Acryl-Eze. Enteric coated formulation was subjected to disintegration and dissolution tests by placing in 0.1 M hydrochloric acid for 2 h and then 1 h in phosphate buffer with a pH of 6.8. About 0.04% of drug was released in the acidic phase and 99.05% in the basic medium. These results reflect that ibuprofen can be successfully enteric coated in order to prevent its release in the stomach and facilitate rapid release of the drug in the duodenum, due to the presence of superdisintegrant. Formulating this enteric coated tablets could increase patient compliance by decreasing adverse drug reactions (ADR S associated with Ibuprofen therapy.Ibuprofeno é um derivado do ácido propiônico, que pertence à classe dos fármacos não-esteróides (AINES. As principais reações adversas associadas com o ibuprofeno se referem àquelas do trato gastrintestinal (TGI, como úlceras pépticas e da mucosa, dispepsia, dor gástrica grave e sangramento, que resultam em muitas falhas de tratamento. O objetivo do estudo foi desenvolver comprimidos revestidos de ibuprofeno que impeçam a irritação da mucosa gástrica, difusão do fármaco através da mucosa e permitam, facilmente, a absorção do princípio ativo do intestino

  8. Application of face centred central composite design to optimise compression force and tablet diameter for the formulation of mechanically strong and fast disintegrating orodispersible tablets.

    Science.gov (United States)

    Pabari, Ritesh M; Ramtoola, Zebunnissa

    2012-07-01

    A two factor, three level (3(2)) face centred, central composite design (CCD) was applied to investigate the main and interaction effects of tablet diameter and compression force (CF) on hardness, disintegration time (DT) and porosity of mannitol based orodispersible tablets (ODTs). Tablet diameters of 10, 13 and 15 mm, and CF of 10, 15 and 20 kN were studied. Results of multiple linear regression analysis show that both the tablet diameter and CF influence tablet characteristics. A negative value of regression coefficient for tablet diameter showed an inverse relationship with hardness and DT. A positive value of regression coefficient for CF indicated an increase in hardness and DT with increasing CF as a result of the decrease in tablet porosity. Interestingly, at the larger tablet diameter of 15 mm, while hardness increased and porosity decreased with an increase in CF, the DT was resistant to change. The optimised combination was a tablet of 15 mm diameter compressed at 15 kN showing a rapid DT of 37.7s and high hardness of 71.4N. Using these parameters, ODTs containing ibuprofen showed no significant change in DT (ANOVA; p>0.05) irrespective of the hydrophobicity of the ibuprofen. Copyright © 2012 Elsevier B.V. All rights reserved.

  9. Formulation and Evaluation of Ascorbic acid Tablets by Direct ...

    African Journals Online (AJOL)

    PURPOSE: To evaluate the tableting properties of microcrystalline starch (MCS) used as a direct compression excipient in the formulation of ascorbic acid tablets and to compare with the properties of tablets produced using microcrystalline cellulose (MCC). METHODS: MCS was obtained by partial hydrolysis of cassava ( ...

  10. 21 CFR 520.1660c - Oxytetracycline hydrochloride tablets/boluses.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride tablets/boluses. 520....1660c Oxytetracycline hydrochloride tablets/boluses. (a) Specifications. Each tablet or bolus contains 250, 500, or 1,000 milligrams of oxytetracycline hydrochloride. (b) Sponsors. For sponsors in § 510...

  11. Astronomical Content in Rongorongo Tablet Keiti

    DEFF Research Database (Denmark)

    Wieczorek, Rafal

    2011-01-01

    Th e fi eld of rongorongo research: the study of Easter Island’s native script is in a peculiar state at the moment. While relative progress has been made in structural and statistical analysis in the last decades, at the level of both single glyphs as well as entire texts, little to no advanceme...... has been achieved in the actual decipherment. To shed new light on rongorongo research, a hypothesis regarding the contents of tablet Keiti, one of the 25 obtained artifacts, is proposed. Th e content, as well as the meaning, of all but one of these 25 rongorongo texts is still unknown....... In this publication, an interpretation for the recto side of tablet Keiti is presented. It is argued that the tablet contains astronomical observations or instructions regarding the Rapa Nui lunar calendar, and is similar in content to the only other rongorongo text whose function has been partially ascertained......: tablet Mamari. If the calendrical contents of this artifact were confi rmed, this would be a major boost to our understanding of Oceania’s only native script....

  12. Polyols as filler-binders for disintegrating tablets prepared by direct compaction

    NARCIS (Netherlands)

    Bolhuis, Gerad K.; Rexwinkel, Erik G.; Zuurman, Klaas

    Background: Although polyols are frequently used as tablet excipients in lozenges, chewing tablets, and orodisperse tablets, special directly compressible (DC) forms are recommended as filler-binder in common disintegrating tablets. Aim: In this article, DC types of isomalt, lactitol, mannitol,

  13. Tablets, læring og nye forretningsmodeller

    DEFF Research Database (Denmark)

    Andersen, Pernille Viktoria Kathja

    2011-01-01

    D. 6 oktober satte Netværk om E-Læring (NoEL) i samarbejde med InVIO fokus på Tablet-computing igennem et heldagsarrangement i Aalborg Universitets nye omgivelser på Nyhavnsgade 14. Formålet med dagen var, at stille skarpt på tablet formatet og udforske potentialerne og udfordringerne med særligt...... vægt på iPads til mobillæring og nye forretningsmodeller. Tablet –computing er de seneste år blevet mere og mere udbredt indenfor både uddannelse, arbejdsliv og i fritiden. Ønsket for dagen var derfor at bidrage med diskussion og videndeling omkring, hvad den nye håndholdte touch teknologi kommer til...... at betyde for læring, samarbejde og forretningsmodeller og dermed hvilke nye vilkår tablet computing kan bidrage med indenfor arbejdsliv og uddannelse....

  14. Cyclodextrins as excipients in tablet formulations.

    Science.gov (United States)

    Conceição, Jaime; Adeoye, Oluwatomide; Cabral-Marques, Helena Maria; Lobo, José Manuel Sousa

    2018-04-22

    This paper aims to provide a critical review of cyclodextrins as excipients in tablet formulations, highlighting: (i) the principal pharmaceutical applications of cyclodextrins; (ii) the most relevant technological aspects in pharmaceutical formulation development; and (iii) the actual regulatory status of cyclodextrins. Moreover, several illustrative examples are presented. Cyclodextrins can be used as complexing excipients in tablet formulations for low-dose drugs. By contrast, for medium-dose drugs and/or when the complexation efficiency is low, the methods to enhance the complexation efficiency play a key part in reducing the cyclodextrin quantity. In addition, these compounds are used as fillers, disintegrants, binders and multifunctional direct compression excipients of the tablets. Copyright © 2018 Elsevier Ltd. All rights reserved.

  15. Damage-tolerance strategies for nacre tablets.

    Science.gov (United States)

    Wang, Shengnan; Zhu, Xinqiao; Li, Qiyang; Wang, Rizhi; Wang, Xiaoxiang

    2016-05-01

    Nacre, a natural armor, exhibits prominent penetration resistance against predatory attacks. Unraveling its hierarchical toughening mechanisms and damage-tolerance design strategies may provide significant inspiration for the pursuit of high-performance artificial armors. In this work, relationships between the structure and mechanical performance of nacre were investigated. The results show that other than their brick-and-mortar structure, individual nacre tablets significantly contribute to the damage localization of nacre. Affected by intracrystalline organics, the tablets exhibit a unique fracture behavior. The synergistic action of the nanoscale deformation mechanisms increases the energy dissipation efficiency of the tablets and contributes to the preservation of the structural and functional integrity of the shell. Copyright © 2016 Elsevier Inc. All rights reserved.

  16. Development of Corn Starch-Neusilin UFL2 Conjugate as Tablet Superdisintegrant: Formulation and Evaluation of Fast Disintegrating Tablets

    Directory of Open Access Journals (Sweden)

    Prateek Juneja

    2014-01-01

    Full Text Available In the present study, corn Starch-Neusilin UFL2 conjugates were prepared by physical, chemical, and microwave methods with the aim of using the conjugates as tablet superdisintegrant. Various powder tests, namely, angle of repose, bulk density, tapped density, Hausner’s ratio, Carr’s index, swelling index, and powder porosity were conducted on the samples. The conjugates were characterized by ATR-FTIR, XRD, DSC, and SEM techniques. Heckel and Kawakita models were applied to carry out compression studies for the prepared conjugates. Fast disintegrating tablets of domperidone were prepared using corn starch and corn Starch-Neusilin UFL2 conjugates as tablet superdisintegrants in different concentrations. Conjugates were found to possess good powder flow and tabletting properties. Heckel analysis indicated that the conjugates prepared by microwave method showed the slowest onset of plastic deformation while Kawakita analysis indicated that the conjugates prepared by microwave method exhibited the highest amount of total plastic deformation. The study revealed that the corn Starch-Neusilin UFL2 conjugates possess improved powder flow properties and could be a promising superdisintegrant for preparing fast disintegrating tablet. Also, the results sugessted that the microwave method was found to be most effective for the preparation of corn Starch-Neusilin UFL2 conjugates.

  17. Development of fast disintegrating compressed tablets using amino acid as disintegration accelerator: evaluation of wetting and disintegration of tablet on the basis of surface free energy.

    Science.gov (United States)

    Fukami, Jinichi; Ozawa, Asuka; Yoshihashi, Yasuo; Yonemochi, Etsuo; Terada, Katsuhide

    2005-12-01

    A fast disintegrating compressed tablet was formulated using amino acids, such as L-lysine HCl, L-alanine, glycine and L-tyrosine as disintegration accelerator. The tablets having the hardness of about 4 kgf were prepared and the effect of amino acids on the wetting time and disintegration time in the oral cavity of tablets was examined on the basis of surface free energy of amino acids. The wetting time of the tablets increased in the order of L-lysine HCl, L-alanine, glycine and L-tyrosine, whereas the disintegration time in the oral cavity of the tablets increased in the order of L-alanine, glycine, L-lysine HCl and L-tyrosine. These behaviors were well analyzed by the introduction of surface free energy. When the polar component of amino acid was large value or the dispersion component was small value, faster wetting of tablet was observed. When the dispersion component of amino acid was large value or the dispersion component was small value, faster disintegration of tablet was observed, expect of L-tyrosine tablet. The fast disintegration of tablets was explained by the theory presented by Matsumaru.

  18. Embolic stroke associated with injection of buprenorphine tablets.

    Science.gov (United States)

    Lim, C C Tchoyoson; Lee, Sze Haur; Wong, Yee-Choon; Hui, Francis

    2009-09-15

    Drug users who crush, dissolve, and inject buprenorphine tablets parenterally may be at risk of severe thromboembolic complications or death. We describe patients with neurologic complications after injecting buprenorphine tablets. Brain MRI including diffusion-weighted imaging (DWI) in patients admitted to the neurologic department after injecting buprenorphine tablets were reviewed. Seven men had neurologic complications after buprenorphine tablet injection. In 5 patients, multiple small scattered hyperintense lesions were detected on DWI in the cortex, white matter, and basal ganglia of the cerebral hemisphere; one patient had a single small lesion. The side of MRI abnormality corresponded to the side of needle marks on the neck except in one patient who had bilateral injections. One patient, who denied injecting into the neck, had DWI abnormalities in the middle cerebral artery territory on one side and occlusion of the ipsilateral internal carotid artery. Buprenorphine tablets can be intentionally or inadvertently injected into the carotid artery, causing a characteristic appearance on diffusion-weighted imaging, consistent with embolic cerebral infarction.

  19. Tensile and shear methods for measuring strength of bilayer tablets.

    Science.gov (United States)

    Chang, Shao-Yu; Li, Jian-Xin; Sun, Changquan Calvin

    2017-05-15

    Both shear and tensile measurement methods have been used to quantify interfacial bonding strength of bilayer tablets. The shear method is more convenient to perform, but reproducible strength data requires careful control of the placement of tablet and contact point for shear force application. Moreover, data obtained from the shear method depend on the orientation of the bilayer tablet. Although more time-consuming to perform, the tensile method yields data that are straightforward to interpret. Thus, the tensile method is preferred in fundamental bilayer tableting research to minimize ambiguity in data interpretation. Using both shear and tensile methods, we measured the mechanical strength of bilayer tablets made of several different layer combinations of lactose and microcrystalline cellulose. We observed a good correlation between strength obtained by the tensile method and carefully conducted shear method. This suggests that the shear method may be used for routine quality test of bilayer tablets during manufacturing because of its speed and convenience, provided a protocol for careful control of the placement of the tablet interface, tablet orientation, and blade is implemented. Copyright © 2017 Elsevier B.V. All rights reserved.

  20. SU-E-I-09: Application of LiF:Mg,Cu (TLD-100H) Dosimeters for in Diagnostic Radiology

    Energy Technology Data Exchange (ETDEWEB)

    Sina, S [Radiation Research Center, Shiraz University, Shiraz (Iran, Islamic Republic of); Zeinali, B; Karimipourfard, M; Lotfalizadeh, F; Sadeghi, M [Nuclear Engineering Department, Shiraz University, Shiraz (Iran, Islamic Republic of); Faghihi, R [Radiation Research Center, Shiraz University, Shiraz (Iran, Islamic Republic of); Nuclear Engineering Department, Shiraz University, Shiraz (Iran, Islamic Republic of)

    2014-06-01

    Purpose: Accurate dosimetery is very essential in diagnostic radiology. The goal of this study is to verify the application of LiF:Mg,Cu,P (TLD100H) in obtaining the Entrance skin dose (ESD) of patients undergoing diagnostic radiology. The results of dosimetry performed by TLD-100H, were compared with those obtained by TLD100, which is a common dosimeter in diagnostic radiology. Methods: In this study the ESD values were measured using two types of Thermoluminescence dosimeters (TLD-100, and TLD-100H) for 16 patients undergoing diagnostic radiology (lumbar spine imaging). The ESD values were also obtained by putting the two types of TLDs at the surface of Rando phantom for different imaging techniques and different views (AP, and lateral). The TLD chips were annealed with a standard procedure, and the ECC values for each TLD was obtained by exposing the chips to equal amount of radiation. Each time three TLD chips were covered by thin dark plastic covers, and were put at the surface of the phantom or the patient. The average reading of the three chips was used for obtaining the dose. Results: The results show a close agreement between the dose measuered by the two dosimeters.According to the results of this study, the TLD-100H dosimeters have higher sensitivities (i.e.signal(nc)/dose) than TLD-100.The ESD values varied between 2.71 mGy and 26.29 mGy with the average of 11.89 mGy for TLD-100, and between 2.55 mGy and 27.41 mGy with the average of 12.32 mGy for measurements. Conclusion: The TLD-100H dosimeters are suggested as effective dosimeters for dosimetry in low dose fields because of their higher sensitivities.

  1. SU-E-I-09: Application of LiF:Mg,Cu (TLD-100H) Dosimeters for in Diagnostic Radiology

    International Nuclear Information System (INIS)

    Sina, S; Zeinali, B; Karimipourfard, M; Lotfalizadeh, F; Sadeghi, M; Faghihi, R

    2014-01-01

    Purpose: Accurate dosimetery is very essential in diagnostic radiology. The goal of this study is to verify the application of LiF:Mg,Cu,P (TLD100H) in obtaining the Entrance skin dose (ESD) of patients undergoing diagnostic radiology. The results of dosimetry performed by TLD-100H, were compared with those obtained by TLD100, which is a common dosimeter in diagnostic radiology. Methods: In this study the ESD values were measured using two types of Thermoluminescence dosimeters (TLD-100, and TLD-100H) for 16 patients undergoing diagnostic radiology (lumbar spine imaging). The ESD values were also obtained by putting the two types of TLDs at the surface of Rando phantom for different imaging techniques and different views (AP, and lateral). The TLD chips were annealed with a standard procedure, and the ECC values for each TLD was obtained by exposing the chips to equal amount of radiation. Each time three TLD chips were covered by thin dark plastic covers, and were put at the surface of the phantom or the patient. The average reading of the three chips was used for obtaining the dose. Results: The results show a close agreement between the dose measuered by the two dosimeters.According to the results of this study, the TLD-100H dosimeters have higher sensitivities (i.e.signal(nc)/dose) than TLD-100.The ESD values varied between 2.71 mGy and 26.29 mGy with the average of 11.89 mGy for TLD-100, and between 2.55 mGy and 27.41 mGy with the average of 12.32 mGy for measurements. Conclusion: The TLD-100H dosimeters are suggested as effective dosimeters for dosimetry in low dose fields because of their higher sensitivities

  2. Profil Disolusi Terbanding Tablet Rifampisin Merek Dan Generik

    OpenAIRE

    Nurtanti, Mutiara Poetri; Kusuma, Anjar Mahardian; Siswanto, Agus

    2010-01-01

    Obat generik saat ini masih dipandang sebelah mata oleh masyarakat karena alasan kualitas dari obat generik lebih rendah dibandingkan obat merek. Tujuan penelitian ini untuk mengetahui perbandingan profil disolusi rifampisin tablet merek (A, B, C) dengan tablet rifampisin generik (D, E). Parameter penting dalam menentukan mutu obat dalam bentuk tablet adalah penetapan kekerasan, penetapan waktu hancur dan uji disolusi. Pengambilan sampel dilakukan berdasarkan produk yang beredar di pasaran ya...

  3. Ginger Orally Disintegrating Tablets to Improve Swallowing in Older People.

    Science.gov (United States)

    Hirata, Ayumu; Funato, Hiroki; Nakai, Megumi; Iizuka, Michiro; Abe, Noriaki; Yagi, Yusuke; Shiraishi, Hisashi; Jobu, Kohei; Yokota, Junko; Hirose, Kahori; Hyodo, Masamitsu; Miyamura, Mitsuhiko

    2016-01-01

    We previously prepared and pharmaceutically evaluated ginger orally disintegrating (OD) tablets, optimized the base formulation, and carried out a clinical trial in healthy adults in their 20 s and 50s to measure their effect on salivary substance P (SP) level and improved swallowing function. In this study, we conducted clinical trials using the ginger OD tablets in older people to clinically evaluate the improvements in swallowing function resulting from the functional components of the tablet. The ginger OD tablets were prepared by mixing the excipients with the same amount of mannitol and sucrose to a concentration of 1% ginger. Eighteen healthy older adult volunteers aged 63 to 90 were included in the swallowing function test. Saliva was collected before and 15 min after administration of the placebo and ginger OD tablets. Swallowing endoscopy was performed by an otolaryngologist before administration and 15 min after administration of the ginger OD tablets. A scoring method was used to evaluate the endoscopic swallowing. Fifteen minutes after taking the ginger OD tablets, the salivary SP amount was significantly higher than prior to ingestion or after taking the placebo (pginger OD tablets. Our findings showed that the ginger OD tablets increased the salivary SP amount and improved swallowing function in older people with appreciably reduced swallowing function.

  4. Portable Tablets in Science Museum Learning: Options and Obstacles

    Science.gov (United States)

    Gronemann, Sigurd Trolle

    2017-01-01

    Despite the increasing use of portable tablets in learning, their impact has received little attention in research. In five different projects, this media-ethnographic and design-based analysis of the use of portable tablets as a learning resource in science museums investigates how young people's learning with portable tablets matches the…

  5. 21 CFR 520.1696d - Penicillin V potassium tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Penicillin V potassium tablets. 520.1696d Section... Penicillin V potassium tablets. (a) Specifications. Each tablet contains penicillin V potassium equivalent to 125 milligrams (200,000 units) or 250 milligrams (400,000 units) of penicillin V. (b) Sponsors. See...

  6. The tabletting properties of Stearolac-S | Onyechi | Journal of ...

    African Journals Online (AJOL)

    press was used to determine the unit ejection force of tablets made from the direct compression formulations. The effects of the excipients on tablet hardness, friability, disintegration and dissolution rate were also evaluated. Tablets containing 3 - 4 % w/w STEAROLAC-S gave unit ejection force values comparable to those ...

  7. Statistical evaluation of tablet coating processes: influence of pan design and solvent type

    Directory of Open Access Journals (Sweden)

    Valdomero Pereira de Melo Junior

    2010-12-01

    Full Text Available Partially and fully perforated pan coaters are among the most relevant types of equipment currently used in the process of coating tablets. The goal of this study was to assess the performance differences among these types of equipment employing a factorial design. This statistical approach allowed the simultaneous study of the process variables and verification of interactions among them. The study included partially-perforated and fully-perforated pan coaters, aqueous and organic solvents, as well as hypromellose-based immediate-release coating. The dependent variables were process time, energy consumption, mean weight of tablets and process yield. For the tests, placebo tablets with a mean weight of 250 mg were produced, divided into eight lots of two kilograms each and coated in duplicate, using both partially perforated pan and fully perforated pan coaters. The results showed a significant difference between the type of equipment used (partially and fully perforated pan coaters with regard to process time and energy consumption, whereas no significant difference was identified for mean weight of the coated tablets and process yield.Entre os tipos de equipamentos de maior relevância utilizados atualmente no processo de revestimento de comprimidos estão os de tambor parcial e totalmente perfurados. A proposta desse trabalho foi avaliar as diferenças de desempenho entre esses equipamentos empregando projeto fatorial. Essa abordagem estatística possibilitou o estudo simultâneo das variáveis do processo, permitindo verificar interações entre elas. O trabalho incluiu equipamento com tambor parcialmente perfurado e totalmente perfurado, solventes aquoso e orgânico, assim como revestimento de liberação imediata à base de hipromelose. As variáveis dependentes ou respostas foram tempo de processo, consumo de energia, peso médio e rendimento do processo. Para os ensaios, foram produzidos comprimidos de placebo de 250 mg de peso m

  8. Characterization of the Roman curse tablet

    Science.gov (United States)

    Liu, Wen; Zhang, Boyang; Fu, Lin

    2017-08-01

    The Roman curse tablet, produced in ancient Rome period, is a metal plate that inscribed with curses. In this research, several techniques were used to find out the physical structure and chemical composition of the Roman curse tablet, and testified the hypothesis that whether the tablet is made of pure lead or lead alloy. A sample of Roman Curse Tablet from the Johns Hopkins Archaeological Museum was analyzed using several different characterization techniques to determine the physical structure and chemical composition. The characterization techniques used were including optical microscopy, scanning electron microscopy (SEM), atomic force microscopy (AFM), and differential scanning calorimetry (DSC). Because of the small sample size, X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS) and X-ray fluorescence (XRF) cannot test the sample. Results from optical microscopy and SEM, enlarged images of the sample surface were studied. The result revealed that the sample surface has a rough, non-uniform, and grainy surface. AFM provides three-dimensional topography of the sample surface, studying the sample surface in atomic level. DSC studies the thermal property, which is most likely a lead-alloy, not a pure lead. However, none of these tests indicated anything about the chemical composition. Future work will be required due to the lack of measures finding out its chemical composition. Therefore, from these characterization techniques above, the Roman curse tablet sample is consisted of lead alloy, not pure lead.

  9. Bioequivalence of generic lamotrigine 100-mg tablets in healthy Thai male volunteers: a randomized, single-dose, two-period, two-sequence crossover study.

    Science.gov (United States)

    Srichaiya, Arunee; Longchoopol, Chaowanee; Oo-Puthinan, Sarawut; Sayasathid, Jarun; Sripalakit, Pattana; Viyoch, Jarupa

    2008-10-01

    Lamotrigine is an antiepileptic drug which has been used in the treatment of epilepsy and bipolar disorder. A search of the literature did not find previously published bioequivalence and pharmacokinetic evaluations of lamotrigine in healthy Thai male volunteers. The aim of this study was to compare the pharmacokinetic parameters between 2 brands of lamotrigine in healthy Thai male volunteers. A randomized, single-dose, 2-period, 2-sequence, crossover study design with a 2-week washout period was conducted in healthy Thai males. Subjects were randomized to receive either the test or reference formulation in the first period. All subjects were required to be nonsmokers and without a history of alcohol or drug abuse. Plasma samples were collected over a 120-hour period after 100-mg lamotrigine administration in each period. A validated high-performance liquid chromatography ultraviolet method was used to analyze lamotrigine concentration in plasma. Pharmacokinetic parameters were determined using a noncompartmental method. Bioequivalence between the test and reference products, as defined by the US Food and Drug Administration (FDA), is determined when the ratio for the 90% CIs of the difference in the means of the log-transformed AUC(0-t), AUC(0-infinity), and C(max) of the 2 products are within 0.80 and 1.25. Adverse events were determined by measuring vital signs after dosing. Subjects were also asked if they suffered from undesirable effects such as nausea, vomiting, dizziness, and headache. This bioequivalence study was performed in 24 healthy Thai males (mean [SD] age, 20.5 [1.3] years; range, 19-24 years; weight, 62.5 [7.4] kg; height, 172.8 [6.9] cm; body mass index, 20.9 [2.0] kg/m(2)). The mean (SD) C(max) and T(max) of the test formulation of lamotrigine were 1.7 (0.3) microg/mL and 1.2 (0.9) hours, respectively. The mean (SD) C(max) and T(max) of the reference formulation of lamotrigine were 1.7 (0.3) microg/mL and 1.4 (1.0) hours, respectively. The mean

  10. Spectrofluorimetric determination of aliskiren in tablets and spiked human plasma through derivatization with dansyl chloride.

    Science.gov (United States)

    Aydoğmuş, Zeynep; Sarı, Ferhat; Ulu, Sevgi Tatar

    2012-03-01

    A simple and sensitive method has been developed and validated for the determination of aliskiren (ALS) in its dosage forms and spiked plasma. The method was based on the reaction of the drug with dansyl chloride in the presence of bicarbonate solution of pH 10.5 to give a highly fluorescent derivative which was measured at 501 nm with excitition at 378 nm in dichloromethane. Different experimental parameters affecting the development of the method and stability were carefully studied and optimized. The calibration curves were linear over the concentration ranges of 100-700 and 50-150 ng/mL for standard solution and plasma, respectively. The limits of detection were 27.52 ng/mL in standard solution, 4.91 ng/mL in plasma. The developed method was successfully applied to the analysis the drug in the commercial tablets and spiked plasma samples. The mean recovery of ALS from tablets and plasma was 100.10 and 97.81%, respectively. A proposal of the reaction pathway was presented.

  11. Placing wireless tablets in clinical settings for patient education.

    Science.gov (United States)

    Stribling, Judy C; Richardson, Joshua E

    2016-04-01

    The authors explored the feasibility and possible benefit of tablet-based educational materials for patients in clinic waiting areas. We distributed eight tablets preloaded with diagnosis-relevant information in two clinic waiting areas. Patients were surveyed about satisfaction, usability, and effects on learning. Technical issues were resolved. Thirty-seven of forty patients completed the survey. On average, the patients were satisfied in all categories. Placing tablet-based educational materials in clinic waiting areas is relatively easy to implement. Patients using tablets reported satisfaction across three domains: usability, education, and satisfaction.

  12. Study of the Formulation and Preparation of Chewable Tablets With a Calcium Complex Association and Vitamin D3

    Directory of Open Access Journals (Sweden)

    Emma Creţu

    2010-06-01

    Full Text Available The experimental study objective was the development of
    chewable tablets with the calcium complex association, the minerals and vitamin D3 for children, subject to the rules as stipulated by the Romanian Pharmacopoeia Xth edition. Generating sources of calcium, used as raw materials in the preparation of these tablets are natural products represented by complex mineral rich in calcium - Lactoval (R HiCal (ratio of calcium and phosphorus is 2,2:1, report the same as breast milk and 30% bovine colostrums [1, 3], making the absorption of calcium should be increased. Also, in order to
    fix and better absorb calcium in the body was added to make the preparation of these chewable tablets and vitamin D3.
    Was chosen as a method of preparing direct compression. Excipients for direct compression are diluents-binder-disaggregated. They are unitary excipients or co-processed products, multi-processed excipients together to meet those properties: microcrystalline cellulose (Vivapur 102 Ludipress, lactose (Tablettose 80, Kollidon CL Isomalt DC 100. Was also added to a lubricant (magnesium stearate and sweetener and flavoring to carry out the preparation of tablets and after 30 days as provided Romanian Pharmacopoeia Xth and its 2001 supplement, which comprises: organoleptic control, uniformity of weight, strength, disintegration and their friability. Working method chosen and make the appropriate choice leads to tablets in terms of quality standards officinal.

  13. Long-term effects of cladribine tablets on MRI activity outcomes in patients with relapsing–remitting multiple sclerosis: the CLARITY Extension study

    OpenAIRE

    Comi, Giancarlo; Cook, Stuart; Rammohan, Kottil; Soelberg Sorensen, Per; Vermersch, Patrick; Adeniji, Abidemi K.; Dangond, Fernando; Giovannoni, Gavin

    2018-01-01

    Background The CLARITY and CLARITY Extension studies demonstrated that treatment of relapsing–remitting multiple sclerosis (RRMS) with cladribine tablets (CT) results in significant clinical improvements, compared with placebo. This paper presents the key magnetic resonance imaging (MRI) findings from the CLARITY Extension study. Methods Patients who received a cumulative dose of either CT 3.5 or 5.25 mg/kg in CLARITY were rerandomized to either placebo or CT 3.5 mg/kg in CLARITY Extension. P...

  14. Replacing Smartphones With Mini Tablet Technology: An Evaluation.

    Science.gov (United States)

    Maneval, Rhonda; Mechtel, Marci

    Handheld technology allows students to access point-of-care resources throughout the clinical experience. To assess the viability of replacing student smartphones with tablets, an evaluation project was undertaken. Overall, students were equally dissatisfied with the 2 types of tablets that were evaluated. Students saw the potential usefulness of tablets to manage clinical assignments, interact with the learning management system, and communicate with faculty, but not for retrieving information currently accessible on their phones.

  15. Tablet Computer Literacy Levels of the Physical Education and Sports Department Students

    Directory of Open Access Journals (Sweden)

    Gulten HERGUNER

    2016-04-01

    Full Text Available Education systems are being affected in parallel by newly emerging hardware and new developments    occurring in technology daily. Tablet usage especially is becoming ubiquitous in the teaching‐learning processes in recent years. Therefore, using the tablets effectively, managing them and having a high level of tablet literacy play an important role within the education system. This study aimed at determining the tablet literacy levels of students in the Physical Education and Sports Teaching department at Sakarya University in Turkey, and examining this data with regard to various variables. Some 276 students participated in the study. Findings of the study suggest that the sample has a high tablet literacy level. While no significant difference was found in the tablet literacy  by gender, the students in the 2nd grade are noted to have higher levels of tablet literacy compared to the students in 3rd and 4th grades and tablet owners are more tablet literate when compared to non‐owners. A significant but low level correlation was found between the tablet usage time and tablet literacy.  

  16. Evaluation of LiF:Mg,Ti (TLD-100 for Intraoperative Electron Radiation Therapy Quality Assurance.

    Directory of Open Access Journals (Sweden)

    Raffaele Liuzzi

    Full Text Available Purpose of the present work was to investigate thermoluminescent dosimeters (TLDs response to intraoperative electron radiation therapy (IOERT beams. In an IOERT treatment, a large single radiation dose is delivered with a high dose-per-pulse electron beam (2-12 cGy/pulse during surgery. To verify and to record the delivered dose, in vivo dosimetry is a mandatory procedure for quality assurance. The TLDs feature many advantages such as a small detector size and close tissue equivalence that make them attractive for IOERT as in vivo dosimeters.LiF:Mg,Ti dosimeters (TLD-100 were irradiated with different IOERT electron beam energies (5, 7 and 9 MeV and with a 6 MV conventional photon beam. For each energy, the TLDs were irradiated in the dose range of 0-10 Gy in step of 2 Gy. Regression analysis was performed to establish the response variation of thermoluminescent signals with dose and energy.The TLD-100 dose-response curves were obtained. In the dose range of 0-10 Gy, the calibration curve was confirmed to be linear for the conventional photon beam. In the same dose region, the quadratic model performs better than the linear model when high dose-per-pulse electron beams were used (F test; p<0.05.This study demonstrates that the TLD dose response, for doses ≤10 Gy, has a parabolic behavior in high dose-per-pulse electron beams. TLD-100 can be useful detectors for IOERT patient dosimetry if a proper calibration is provided.

  17. Optimization of fast dissolving etoricoxib tablets prepared by sublimation technique

    OpenAIRE

    Patel D; Patel M

    2008-01-01

    The purpose of this investigation was to develop fast dissolving tablets of etoricoxib. Granules containing etoricoxib, menthol, crospovidone, aspartame and mannitol were prepared by wet granulation technique. Menthol was sublimed from the granules by exposing the granules to vacuum. The porous granules were then compressed in to tablets. Alternatively, tablets were first prepared and later exposed to vacuum. The tablets were evaluated for percentage friability and disintegration time. A 3 2 ...

  18. Validation of ascorbic acid tablets of national production by igh-performance liquid chromatography method

    International Nuclear Information System (INIS)

    Rodriguez Hernandez, Yaslenis; Suarez Perez, Yania; Izquierdo Castro, Idalberto

    2009-01-01

    We validate an analytical method by high-performance liquid chromatography to determine ascorbic acid proportion in vitamin C tablets, which was designed as an alternative method to quality control and to follow-up of active principle chemical stability, since official techniques to quality control of ascorbic acid in tablets are not selective with degradation products. Method was modified according to that reported in USP 28, 2005 for analysis of injectable product. We used a RP-18 column of 250 x 4.6 mm 5 μm with a UV detector to 245 nm. Its validation was necessary for both objectives, considering parameters required for methods of I and II categories. This method was enough linear, exact, and precise in the rank of 100-300 μg/mL. Also, it was selective with remaining components of matrix and with the possible degradation products achieved in stressing conditions. Detection and quantification limits were estimated. When method was validated it was applied to ascorbic acid quantification in two batches of expired tablets and we detected a marked influence of container in active degradation principle after 12 months at room temperature. (Author)

  19. Correlation between stoichiometry and surface structure of the polar MgAl2O4(100) surface as a function of annealing temperature

    DEFF Research Database (Denmark)

    Jensen, Thomas Nørregaard; Rasmussen, Morten Karstoft; Knudsen, Jan

    2015-01-01

    is found to significantly increase as the surface is sputtered and annealed in oxygen at intermediate temperatures ranging from 800-1000 [degree]C. The Al excess is explained by the observed surface structure, where the formation of nanometer sized pits and elongated patches with Al terminated step edges....... The excess of Al and high concentration of octahedral vacancies, very interestingly means, that the top few surface layers of the MgAl2O4(100) adopts a surface structure similar to that of a spinel-like transition Al2O3 film. However, after annealing at a high temperature of 1200 [degree]C, the Al/Mg ratio...... are filled by Mg from the bulk, due to the increased mobility at high annealing temperatures....

  20. Transforming the Classroom With Tablet Technology.

    Science.gov (United States)

    Sargent, Lana; Miles, Elizabeth

    Identifying the most effective models for integrating new technology into the classroom and understanding its effects on educational outcomes are essential for nurse educators. This article describes an educational intervention with tablet technology (iPads) using an innovative case-based learning model in a nursing program. Students reported positive learning outcomes when using the tablet technology for learning course content.