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Sample records for hydrochloride 10mg tablets

  1. DEVELOPMENT AND BIOEQUIVALENCE STUDY OF OLANZAPINE 10mg TABLETS

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    Ravindra Waykar et al

    2012-09-01

    Full Text Available Generic drugs are lower-cost versions of patent-expired original brand-name medications. According to guidelines of regulatory agencies of the Canada, US and European Union, a generic drug must be “identical, or bioequivalent to a brand name drug in dosage form, safety, strength, route of administration, quality, performance characteristics and intended use”. Bioequivalence is decreed when the ratio of the generic to the reference compound for the area-under-the-curve and maximum plasma concentration (Cmax fall within a 0.80–1.25 range. The present study was to develop Olanzapine Tablets and compare pharmacokinetic profile of Zyprexa 10 mg film-coated tablets, Zyprexa Velotabs 10 mg orodispersible tablets and Olanzapine 10mg tablets. Multi media dissolution studies in 0.1N HCl, pH 4.5 acetate buffer and pH 6.8 phosphate buffer were carried out for Reference (Zyprexa Velotab 10 mg and Zyprexa 10 mg and test product (i.e. Olanzapine 10 mg. A single centre, open-label, single-dose, randomised, 3-way crossover bioequivalence study, performed under fasting conditions. Based on the results obtained, it can be concluded that the test olanzapine (Treatment A is bioequivalent to both references Zyprexa Velotab (Treatment B and Zyprexa (Treatment C following a 10 mg dose under fasting conditions. All formulations were well tolerated, with no major side effects and no relevant differences in safety profiles were observed between the preparations, particularly with respect to the number and pattern of adverse event.

  2. Preference for rizatriptan 10-mg wafer vs. eletriptan 40-mg tablet for acute treatment of migraine.

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    Láinez, M J A; Evers, S; Kinge, E; Allais, G; Allen, C; Rao, N A; Massaad, R; Lis, K

    2006-03-01

    Preference is a composite, patient-oriented endpoint incorporating efficacy, tolerability, formulation, and convenience of medications. The objective of this study was to compare patient preference for rizatriptan 10-mg wafer vs. eletriptan 40-mg tablet for acute treatment of migraine. In this multicentre, open-label, two-period, crossover study, out-patients were randomly assigned to treat the first of two moderate to severe migraines with rizatriptan or eletriptan and the second with the alternate therapy. Patients completed diary assessments at baseline and up to 24 h after taking study medication. At the last visit, patients completed a psychometrically validated preference questionnaire. A total of 372 patients (mean age 38 years, 85% female) treated two migraine attacks, and 342 patients (92%) expressed a preference for treatment. Significantly more (P rizatriptan 10-mg wafer [61.1%; 95% confidence interval (CI) 55.7, 66.3] to eletriptan 40-mg tablet (38.9%; 95% CI 33.7, 44.3). The most common reason given for preference of either treatment was speed of headache relief. At 2 h, 80% and 69% of patients reported that rizatriptan and eletriptan, respectively, was convenient or very convenient to take (mean convenience score 1.99 vs. 2.31, respectively; P rizatriptan 10-mg wafer to the eletriptan 40-mg tablet for acute treatment of migraine. The single most important reason for preference was speed of relief, consistent with results from previous preference studies.

  3. Single dose bioequivalence study of two brands of olanzapine 10 mg tablets in Iranian healthy volunteers.

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    Zakeri-Milani, P; Islambulchilar, Z; Ghanbarzadeh, S; Valizadeh, H

    2013-07-01

    This single dose, randomized, open label, 2-period and crossover study in healthy Iranian adult volunteers was conducted to compare the bioavailability of 2 branded formulations of olanzapine 10 mg tablets. 24 volunteers received one tablet of each olanzapine 10 mg formulation. Drugs were administered after a 12 h overnight fast in each of 2 treatment days which separated by a 2-week washout period. Serial blood samples were collected over a period of 72 h. Plasma was analyzed using a validated high performance liquid chromatography method with ultraviolet detection in the range of 2-24 ng/mL with a lower limit of quantitation of 1.25 ng/mL. A non-compartmental method was employed to determine the pharmacokinetic properties (Cmax, Tmax, AUC0-t, AUC0-∞ and T1/2) to test to bioequivalence. Cmax, AUC0-t and AUC0-∞ were used to test the bioequivalence after log-transformation of plasma data. The mean (SD) Cmax, AUC0-t and AUC0-∞ for the test formulation were 15.82 (3.15) ng/mL, 447.19 (100.64) ng.h/L and 570.75 (130.55) ng.h/L respectively. Corresponding values for the test formulation were 15.72 (4.25) ng/mL, 440.37 (98.75) ng.h/mL and 558.66 (129.57) ng.h/mL. For test formulation vs. the reference formulation, the 90% CIs of the least squares mean test/reference ratios of Cmax, AUC0-t and AUC0-∞ were 97.6-110.0%, 96.4-109.4% and 97.3-109.2%. In these volunteers, based on the FDA regulatory definition, results from the pharmacokinetic analysis suggested that the test and reference formulations of olanzapine 10 mg tablets were bioequivalent.

  4. Pharmacokinetic profile of rizatriptan 10-mg tablet and 10-mg orally disintegrating tablet administered with or without water in healthy subjects: an open-label, randomized, single-dose, 3-period crossover study.

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    Swan, Suzanne K; Alcorn, Harry; Rodgers, Anthony; Hustad, Carolyn M; Ramsey, Karen E; Woll, Susan; Skobieranda, Franck

    2006-02-01

    This open-label, 3-period crossover study compared the plasma concentration profiles of rizatriptan tablet, orally disintegrating tablet with water (ODTc), and ODT without water (ODTs) in 24 healthy volunteers aged 18 to 45 years. At each period, subjects received a single dose of either 10-mg rizatriptan tablet, 10-mg rizatriptan ODTs, or 10-mg rizatriptan ODTc. The authors hypothesized that ODTc has a greater geometric mean AUC(0-2h) than ODTs and that ODTc has a greater geometric mean AUC(0-1h) than tablet. A secondary end point was to compare the time of occurrence of the maximum rizatriptan plasma concentration (t(max)) of each dosing method. ODTc had a statistically significantly greater geometric mean AUC(0-2h) compared with ODTs (33.84 h x ng/mL vs 18.83 h x ng/mL; P rizatriptan tablet (17.07 h x ng/mL vs 13.32 h x ng/mL). The median t(max) was 0.67 hours for ODTc and tablet and 1.33 hours for ODTs. ODTc showed a slightly, but not significantly, faster rate of absorption compared with tablet. ODTs with water had a faster rate of absorption than ODTc. Future studies are needed to determine whether this pharmacokinetic difference produces differential efficacy in a clinical setting.

  5. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride effervescent tablets. 520.1242e Section 520.1242e Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242e Levamisole hydrochloride...

  6. Comparison of rizatriptan 5 mg and 10 mg tablets and sumatriptan 25 mg and 50 mg tablets.

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    Kolodny, A; Polis, A; Battisti, W P; Johnson-Pratt, L; Skobieranda, F

    2004-07-01

    This randomized, double-blind, two-attack, placebo-controlled, crossover study explored the efficacy and tolerability of rizatriptan 10 mg compared with sumatriptan 50 mg as well as rizatriptan 5 mg compared with sumatriptan 25 mg in the acute treatment of migraine. Following randomization to one of six possible treatment sequences, patients (n = 1447) treated two sequential attacks, of moderate or severe intensity, separated by at least 5 days. Patients assessed pain severity, migraine-associated symptoms, and functional disability at 0.5, 1, 1.5, and 2 h post treatment. Compared with placebo, all treatments were effective. On the primary endpoint of time to pain relief, rizatriptan 10 mg was not statistically different from sumatriptan 50 mg [odds ratio (OR) 1.10, P = 0.161], and rizatriptan 5 mg was statistically superior to sumatriptan 25 mg (OR 1.22, P = 0.007). In general, rizatriptan 10 mg and 5 mg treatment resulted in improvement compared with the corresponding doses of sumatriptan on measures of pain severity, migraine symptoms, and functional disability and the 5-mg dose reached statistical significance on almost all measures. All treatments were generally well tolerated.

  7. 78 FR 2416 - Notice of Issuance of Final Determination Concerning Rybix® (Tramadol Hydrochloride) Tablets

    Science.gov (United States)

    2013-01-11

    ... (Tramadol Hydrochloride) Tablets AGENCY: U.S. Customs and Border Protection, Department of Homeland Security... (tramadol hydrochloride) tablets. Based upon the facts presented, CBP has concluded in the final determination that India is the country of origin of the Rybix (tramadol hydrochloride) tablets for purposes of...

  8. Simultaneous Spectrophotometric Determination of Drotaverine Hydrochloride and Paracetamol in Tablet

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    Mahaparale Sonali; Telekone R; Raut R; Damle S; Kasture P

    2010-01-01

    Two simple, accurate and reproducible spectrophotometric methods; Q analysis and first order derivative method have been described for the simultaneous estimation of drotaverine hydrochloride and paracetamol in combined tablet dosage form. Absorption maxima of drotaverine hydrochloride and paracetamol in distilled water were found to be 303.5 nm and 243.5 nm respectively. Beer′s law was obeyed in the concentration range 5-50 µg/ml for drotaverine and 5-60 µg/ml for paracetamo...

  9. Bioequivalence studies for two different strengths of montelukast in healthy volunteers: 10 mg film-coated tablets and 5 mg chewable tablets.

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    Pedroso, P; Almeida, S; Filipe, A; Neves, R I; Boudreault, S; Jiménez, C

    2013-09-01

    In order to assess the bioequivalence of 2 different formulations of montelukast, a pivotal trial for the montelukast 10 mg film-coated tablets formulation and a pivotal trial for the montelukast 5 mg chewable tablets formulation were conducted.For the 10 mg study, 34 healthy subjects were enrolled in a single centre, randomised, single-dose, open-label, 2-way crossover study, with a minimum washout period of 7 days, while for the 5 mg study, 42 healthy subjects were included in another study with a similar design. For both studies, plasma samples were collected up to 24 h post-dosing and drug levels were determined by reverse liquid chromatography and detected by tandem mass spectrometry detection.Pharmacokinetic parameters used for bioequivalence assessment, area under the concentration-time curve from time zero to time of last non-zero concentration (AUC0-t) and from time zero to infinity (AUC0-inf) and maximum observed concentration (Cmax), were determined from the drug concentration data using non-compartmental analysis.In the 10 mg study, the 90% confidence intervals obtained by analysis of variance were 99.62-120.51% for Cmax, 102.25-117.37% for AUC0-t and 101.96-116.67% for AUC0-inf, which were within the predefined acceptable range of 80.00-125.00%.In the 5 mg study, the 90% confidence intervals were 91.14-98.46% for Cmax, 93.02-98.42% for AUC0-t and 93.09-98.63% for AUC0-inf, which were within the predefined acceptable range of 80.00-125.00%.Bioequivalence between formulations was concluded both in terms of rate and extent of absorption for both strengths.

  10. Spectrophotometric simultaneous estimation of ranitidine hydrochloride and ondansetron hydrochloride from tablet formulation

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    Pillai S

    2007-01-01

    Full Text Available Three simple, accurate, economical and reproducible UV spectrophotometric methods for simultaneous estimation of two component drug mixture of ranitidine hydrochloride and ondansetron hydrochloride from combined tablet dosage form have been developed. First developed method involves formation and solving of simultaneous equations at 267.2 nm and 314.4 nm. Second method was developed making use of first order derivative spectroscopy using 340.8 nm and 276.0 nm as zero crossing points for estimation of ranitidine hydrochloride and ondansetron hydrochloride respectively. Third method is based on two wavelength calculation, wavelengths selected for estimation of ranitidine hydrochloride were 266.1 nm and 301.8 nm and for ondansetron hydrochloride 305.7 nm and 319.2 nm. The results of analysis have been validated statistically and by recovery studies.

  11. FORMULATION AND EVALUATION OF FLOATING TABLETS OF TIZANIDINE HYDROCHLORIDE

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    Adimoolam Senthil

    2011-08-01

    Full Text Available The objective of the present investigation was to develop floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34–40% and short biological half life (4.2 h. Tizanidine hydrochloride floating tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropylmethylcellulose (HPMC K4M and K15M. Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility throughout the length of the gastrointestinal tract. Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in-vitro drug release characteristics in 12 hours. Drug release from floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there was no drug and excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. The optimized formulation (F9 released 75% of drug at the end of 10 hours by in-vitro release study.

  12. Spectrophotometric estimation of pioglitazone hydrochloride in tablet dosage form

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    Basniwal Pawan

    2008-01-01

    Full Text Available Two simple, rapid, and precise methods - linear regression equation (LRE and standard absorptivity - were developed and validated for the estimation of pioglitazone hydrochloride in tablet dosage form. The maximum absorbance (lmax of pioglitazone hydrochloride was found to be 269.8 nm in methanol:water:hydrochloric acid (250:250:1. Beer-Lambert law was obeyed in the concentration range of 10-50 µg/ml, and the standard absorptivity was found to be 253.97 dl/g/cm. Both the methods were validated for linearity, accuracy, precision (days, analysts, and instrument variation, and robustness (solvent composition. The numerical values for all parameters lie within the acceptable limits. Pioglitazone hydrochloride was estimated in the range of 99.58-99.97% by LRE method and 100.25-100.75% by standard absorptivity method. At 99% confidence limit, the F-test value for the methods was found to be 1.8767.

  13. Simultaneous spectrophotometric determination of drotaverine hydrochloride and paracetamol in tablet.

    Science.gov (United States)

    Mahaparale, Sonali; Telekone, R S; Raut, R P; Damle, S S; Kasture, P V

    2010-01-01

    Two simple, accurate and reproducible spectrophotometric methods; Q analysis and first order derivative method have been described for the simultaneous estimation of drotaverine hydrochloride and paracetamol in combined tablet dosage form. Absorption maxima of drotaverine hydrochloride and paracetamol in distilled water were found to be 303.5 nm and 243.5 nm respectively. Beer's law was obeyed in the concentration range 5-50 mug/ml for drotaverine and 5-60 mug/ml for paracetamol. In Q analysis method, two wavelengths were selected at isobestic point (277 nm) and lambda(max) of paracetamol (243.5 nm). In first order derivative method, zero crossing point for drotaverine hydrochloride and paracetamol were selected at 303.5 nm and 243.5 nm, respectively. The results of two methods were validated statistically and recovery studies were found to be satisfactory.

  14. Simultaneous spectrophotometric determination of drotaverine hydrochloride and paracetamol in tablet

    Directory of Open Access Journals (Sweden)

    Mahaparale Sonali

    2010-01-01

    Full Text Available Two simple, accurate and reproducible spectrophotometric methods; Q analysis and first order derivative method have been described for the simultaneous estimation of drotaverine hydrochloride and paracetamol in combined tablet dosage form. Absorption maxima of drotaverine hydrochloride and paracetamol in distilled water were found to be 303.5 nm and 243.5 nm respectively. Beer′s law was obeyed in the concentration range 5-50 µg/ml for drotaverine and 5-60 µg/ml for paracetamol. In Q analysis method, two wavelengths were selected at isobestic point (277 nm and λmax of paracetamol (243.5 nm. In first order derivative method, zero crossing point for drotaverine hydrochloride and paracetamol were selected at 303.5 nm and 243.5 nm, respectively. The results of two methods were validated statistically and recovery studies were found to be satisfactory.

  15. FORMULATION AND DISSOLUTION STUDY OF DILTIAZEM HYDROCHLORIDE IMMEDIATE RELEASE TABLETS

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    BRAHMAIAH BONTHAGARALA

    2014-08-01

    Full Text Available Objective: The main aim and objective of the work is to formulate immediate release tablets using different direct compression vehicles (DCV’S in different ratios. Methods: In the present study, design of oral immediate release tablets of Diltiazem hydrochloride by direct compression technique was carried out. Results: The main motive is to compare the dissolution profile of these formulations and conclude the best formulation which release drug at a faster rate . To determine the best fit dissolution profile for the dosage forms. Diltiazem hydrochloride tablets were formulated by using microcrystalline cellulose (diluent, potato starch, acacia (binder and magnesium stearate (lubricant. The granules were compressed into tablets and were subjected to dissolution studies. The dissolution profile of the formulation F2 was found to have better dissolution rate compared to others. Conclusion: The Invitro dissolution studies of all the formulations were conducted and the results were obtained, it was concluded that formulation F2 was the best with fast release of drug compared to others.

  16. Modulation of venlafaxine hydrochloride release from press coated matrix tablet

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    Gohel M

    2008-01-01

    Full Text Available The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 3 2 full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion. The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets.

  17. Modulation of venlafaxine hydrochloride release from press coated matrix tablet.

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    Gohel, M C; Soni, C D; Nagori, S A; Sarvaiya, K G

    2008-01-01

    The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 3(2) full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion). The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets.

  18. FORMULATION DEVELOPMENT OF ISOXSUPRINE HYDROCHLORIDE MODIFIED RELEASE MATRIX TABLETS

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    Ketan Patel

    2012-01-01

    Full Text Available The objective of the present investigation was to study the effect of critical formulation parameters affecting release of isoxsuprine hydrochloride from matrix tablets using combination of polyethylene oxide (PEO and dicalcium phosphate (DCP. The powder blend consisting of drug and excipients was analyzed for angle of repose, Carr’s index and Hausner’s ratio. The tablets were prepared by direct compression method. To assess the compressional behavior of the drug-excipient blend, the tablets were analyzed for friability and crushing strength. The in vitro drug release study was carried out in distilled water. The powder blend exhibited satisfactorily flow as measured by angle of repose, Carr’s index and Hausner’s ratio. The formulation ingredients showed satisfactory tableting properties (friability <1%, crushing strength ≥ 4 kgf. The drug release was modified on addition of PEO and DCP. Addition of 5 to 25% DCP in the formulation of matrix tablets caused apparent difference in the drug dissolution in distilled water. However, the difference was insignificant as analyzed by analysis of variance (ANOVA and similarity factor ( f2. The drug release from the tablets was best explained by Weibull model. Unified Weibull model was evolved to predict drug release from the formulated batches. The findings of this investigation can be extended to industry to cut down the cost of formulation and to by-pass the existing patents employing hydrophilic matrixing agents, at least for selective drugs.

  19. Development and evaluation of microporous osmotic tablets of diltiazem hydrochloride.

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    Bathool, Afifa; Gowda, D V; Khan, Mohammed S; Ahmed, Ayaz; Vasudha, S L; Rohitash, K

    2012-04-01

    Microporous osmotic tablet of diltiazem hydrochloride was developed for colon targeting. These prepared microporous osmotic pump tablet did not require laser drilling to deliver the drug to the specific site of action. The tablets were prepared by wet granulation method. The prepared tablets were coated with microporous semipermeable membrane and enteric polymer using conventional pan coating process. The incorporation of sodium lauryl sulfate (SLS), a leachable pore-forming agent, could form in situ delivery pores while coming in contact with gastrointestinal medium. The effect of formulation variables was studied by changing the amounts of sodium alginate and NaCMC in the tablet core, osmogen, and that of pore-forming agent (SLS) used in the semipermeable coating. As the amount of hydrophilic polymers increased, drug release rate prolonged. It was found that drug release was increased as the concentration of osmogen and pore-former was increased. Fourier transform infrared spectroscopy and Differential scanning calorimetry results showed that there was no interaction between drug and polymers. Scanning electron microscopic studies showed the formation of pores after predetermined time of coming in contact with dissolution medium. The formation of pores was dependent on the amount of pore former used in the semipermeable membrane. in vitro results showed acid-resistant, timed release at an almost zero order up to 24 hours. The developed osmotic tablets could be effectively used for prolonged delivery of Diltiazem HCl.

  20. Development and evaluation of microporous osmotic tablets of diltiazem hydrochloride

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    Afifa Bathool

    2012-01-01

    Full Text Available Microporous osmotic tablet of diltiazem hydrochloride was developed for colon targeting. These prepared microporous osmotic pump tablet did not require laser drilling to deliver the drug to the specific site of action. The tablets were prepared by wet granulation method. The prepared tablets were coated with microporous semipermeable membrane and enteric polymer using conventional pan coating process. The incorporation of sodium lauryl sulfate (SLS, a leachable pore-forming agent, could form in situ delivery pores while coming in contact with gastrointestinal medium. The effect of formulation variables was studied by changing the amounts of sodium alginate and NaCMC in the tablet core, osmogen, and that of pore-forming agent (SLS used in the semipermeable coating. As the amount of hydrophilic polymers increased, drug release rate prolonged. It was found that drug release was increased as the concentration of osmogen and pore-former was increased. Fourier transform infrared spectroscopy and Differential scanning calorimetry results showed that there was no interaction between drug and polymers. Scanning electron microscopic studies showed the formation of pores after predetermined time of coming in contact with dissolution medium. The formation of pores was dependent on the amount of pore former used in the semipermeable membrane. in vitro results showed acid-resistant, timed release at an almost zero order up to 24 hours. The developed osmotic tablets could be effectively used for prolonged delivery of Diltiazem HCl.

  1. 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

  2. Stability Indicating HPLC Method for Simultaneous Quantification of Trihexyphenidyl Hydrochloride, Trifluoperazine Hydrochloride and Chlorpromazine Hydrochloride from Tablet Formulation

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    P. Shetti

    2010-01-01

    Full Text Available A new, simple, precise, rapid, selective and stability indicating reversed-phase high performance liquid chromatographic (HPLC method has been developed and validated for simultaneous quantification of trihexyphenidyl hydrochloride, trifluoperazine hydrochloride and chlorpromazine hydrochloride from combined tablet formulation. The method is based on reverse-phase using C-18 (250×4.6 mm, 5 μm particle size column. The separation is achieved using isocratic elution by methanol and ammonium acetate buffer (1% w/v, pH 6.5 in the ratio of 85:15 v/v, pumped at flow rate 1.0 mL/min and UV detection at 215 nm. The column is maintained at 30 °C through out the analysis. This method gives baseline resolution. The total run time is 15 min. Stability indicating capability is established buy forced degradation experiment. The method is validated for specificity, accuracy, precision and linearity as per International conference of harmonisation (ICH. The method is accurate and linear for quantification of trihexyphenidyl hydrochloride, trifluoperazine hydrochloride and Chlorpromazine hydrochloride between 5 - 15 μg/mL, 12.5- 37.5 μg/mL and 62.5 - 187.5 μg/mL respectively.

  3. Spectrophotometric estimation of betahistine hydrochloride in tablet formulations

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    Amit Kumar

    2010-01-01

    Full Text Available Aim: The study aims to develop simple, sensitive, rapid, accurate and precise spectrophotometric method for estimation of Betahistine hydrochloride in tablet dosage forms. Materials and Methods: For method I and II, in a series of 10 ml volumetric flask, aliquots of standard drug solution (100 μg/ml in double distilled water were transferred and diluted with same so as to give several dilutions in concentration range of 15-90 μg/ml and 10-80 μg/ml respectively of betahistine hydrochloride. To 5 ml of each dilution taken in a separating funnel, (5 ml of methyl orange for method I and 5 ml of bromo phenol blue for method II reagent and 5 ml of chloroform was added. Reaction mixture was shaken gently for 5 min and allowed to stand so as to separate aqueous and chloroform layer. Absorbance maxima measured at 421.6 nm and 412 nm for method I and II respectively. Results: The recovery studies were found close to 100 % that indicates accuracy and precision of the proposed methods. The statistical analysis was carried out and results of which were found satisfactory. Standard deviation values were found low that indicated reproducibility of the proposed methods. Conclusion: Based on results the developed methods could be used for routine estimation of betahistine hydrochloride from tablet formulations.

  4. 21 CFR 520.1242b - Levamisole hydrochloride tablet or oblet (bolus).

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride tablet or oblet (bolus). 520.1242b Section 520.1242b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242b Levamisole hydrochloride tablet...

  5. Verapamil hydrochloride release characteristics from new copolymer zwitterionic matrix tablets.

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    Kostova, Bistra; Kamenska, Elena; Ivanov, Ivo; Momekov, George; Rachev, Dimitar; Georgiev, George

    2008-01-01

    The aim of this study was to synthesize stable copolymer (vinyl acetate-co-3-dimethyl[methacryloyloxyethyl] ammonium propane sulfinate) zwitterionic latex with different compositions for the first time by emulsifier-free emulsion copolymerization. Throughout the course of the study, a proposal was made for the explanation of the relationship between the "overshooting" phenomenon (a swelling kinetics with a maximum) and the specific self-association of the zwitterionic copolymers. The zwitterionic monomer unit mole fraction, pH, and ionic strength effects on this relationship, on the swelling kinetics of the zwitterionic copolymers, and on the sustained verapamil hydrochloride release from the model tablets were established by the study's authors.

  6. Formulation and Evaluation of Multilayered Tablets of Pioglitazone Hydrochloride and Metformin Hydrochloride

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    Y. Ankamma Chowdary

    2014-01-01

    Full Text Available In the treatment of type 2 diabetes mellitus a continuous therapy is required which is a more complex one. As in these patients there may be a defect in both insulin secretion and insulin action exists. Hence, the treatment depends on the pathophysiology and the disease state. In the present study, multilayered tablets of pioglitazone hydrochloride 15 mg and metformin hydrochloride 500 mg were prepared in an attempt for combination therapy for the treatment of type 2 diabetes mellitus. Pioglitazone HCl was formulated as immediate release layer to show immediate action by direct compression method using combination of superdisintegrants, namely, crospovidone and avicel PH 102. Crospovidone at 20% concentration showed good drug release profile at 2 hrs. Metformin HCl was formulated as controlled release layer to prolong the drug action by incorporating hydrophilic polymers such as HPMC K4M by direct compression method and guar gum by wet granulation method in order to sustain the drug release from the tablets and maintain its integrity so as to provide a suitable formulation. The multilayered tablets were prepared after carrying out the optimization of immediate release layer and were evaluated for various precompression and postcompression parameters. Formulation F13 showed 99.97% of pioglitazone release at 2 hrs in 0.1 N HCl and metformin showed 98.81% drug release at 10 hrs of dissolution in 6.8 pH phosphate buffer. The developed formulation is equivalent to innovator product in view of in vitro drug release profile. The results of all these evaluation tests are within the standards. The procedure followed for the formulation of these tablets was found to be reproducible and all the formulations were stable after accelerated stability studies. Hence, multilayered tablets of pioglitazone HCl and metformin HCl can be a better alternative way to conventional dosage forms.

  7. FORMULATION AND EVALUATION OF EXTENDED RELEASE TABLETS OF TRAMADOL HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Chilvalvar Sapnil

    2013-10-01

    Full Text Available The objective of this research work was to develop extended release tablets (Twice in a day of Tramadol Hydrochloride using different Hydrophilic polymers like HPMC K15M, HPMC K4M, Metalose 60SH50, Carbopol 971P, Sodium alginate, Xanthan gum by direct compression method. Various amounts of polymers was used in the twenty four proposed formulations (F1 to F24 for the study of release rate retardant effect at 10 %, 15 %, 20 %, 25 % of total weight of tablet matrix respectively. Then the tablets were evaluated in terms of their physical parameters (weight variation, hardness, friability and thickness, drug content and in-vitro release studies. All the formulations showed compliance with pharmacopoeial standards. The in-vitro dissolution study were conducted using USP dissolution apparatus type-II (paddle method in 900 ml 0.1 N HCl for first 2 h and remaining 10 h performed in 6.8 pH phosphate buffer at 100 rpm for a total period of 12 h. Based on the dissolution data comparison with innovator product, formulation F14 was found as the best formulation. The drug release of formulation F14 followed First Order kinetic model and the mechanism was found to be non-Fickian/anomalous according to Korsmeyer-Peppas equation.

  8. Application of near-infrared reflectance spectrometry to the analytical control of pharmaceuticals: ranitidine hydrochloride tablet production.

    Science.gov (United States)

    Dreassi, E; Ceramelli, G; Corti, P; Perruccio, P L; Lonardi, S

    1996-02-01

    The possibility of applying near-infrared reflectance spectrometry to the control of the production cycle of ranitidine hydrochloride tablets was investigated. The results were good for the identification of ranitidine hydrochloride drug substance, mixtures for tablets, cores and coated tablets. The determination of the compound and of its water content also gave satisfactory results.

  9. Effects of automated external lubrication on tablet properties and the stability of eprazinone hydrochloride.

    Science.gov (United States)

    Yamamura, Takahiro; Ohta, Tomoaki; Taira, Toshinari; Ogawa, Yutaka; Sakai, Yasuyuki; Moribe, Kunikazu; Yamamoto, Keiji

    2009-03-31

    We investigated the advantages of an external lubrication technique for tableting. A newly developed external lubricating system was applied to tableting in a rotary tablet press using magnesium stearate. The resulting tablets were compared with tablets produced by the conventional internal lubrication method, in which lubricant is blended before tableting. As a model API, we chose eprazinone hydrochloride, because it is easily hydrolyzed by alkaline lubricant. The amount of lubricant required to prevent sticking with external lubrication was only 1/13th of that required with internal lubrication. External lubrication increased tablet crushing strength by 40%, without prolonging tablet disintegration time, and improved the residual ratio of eprazinone hydrochloride in tablets stored under stress conditions for 4 weeks by 10%. The distribution of lubricant on the surface of externally lubricated tablets was observed by scanning electron microscopy after the preparation by focused ion beam milling. The lubricant had formed a layer on the tablet surface. At the central part of the tablet surface, this layer was much thinner than at the edges, and remained extremely thin even when there was excess magnesium stearate. This is the first report to describe the distribution of lubricant on the surface of externally lubricated tablets.

  10. A study of compressibility and compactibility of directly compressible tableting materials containing tramadol hydrochloride.

    Science.gov (United States)

    Mužíková, Jitka; Kubíčková, Alena

    2016-09-01

    The paper evaluates and compares the compressibility and compactibility of directly compressible tableting materials for the preparation of hydrophilic gel matrix tablets containing tramadol hydrochloride and the coprocessed dry binders Prosolv® SMCC 90 and Disintequik™ MCC 25. The selected types of hypromellose are Methocel™ Premium K4M and Methocel™ Premium K100M in 30 and 50 % concentrations, the lubricant being magnesium stearate in a 1 % concentration. Compressibility is evaluated by means of the energy profile of compression process and compactibility by the tensile strength of tablets. The values of total energy of compression and plasticity were higher in the tableting materials containing Prosolv® SMCC 90 than in those containing Disintequik™ MCC 25. Tramadol slightly decreased the values of total energy of compression and plasticity. Tableting materials containing Prosolv® SMCC 90 yielded stronger tablets. Tramadol decreased the strength of tablets from both coprocessed dry binders.

  11. Simultaneous Estimation of Gemcitabine Hydrochloride and Capecitabine Hydrochloride in Combined Tablet Dosage Form by RP-HPLC Method

    Directory of Open Access Journals (Sweden)

    V. Rajesh

    2011-01-01

    Full Text Available A new reverse phase high performance liquid chromatography (RP-HPLC method has been developed for the simultaneous estimation of gemcitabine hydrochloride and capecitabine hydrochloride in combined tablet dosage form. An inertsil ODS-3 C-18 column having dimensions of 250×4.6 mm and particle size of 5 µm, with mobile phase containing a mixture of acetonitrile : water : triethyelamine in the ratio of (70 : 28 : 2v/v was used. The pH of mobile phase was adjusted to 4.0 with ortho-phosphoric acid. The flow rate was 1 mL/min and the column effluents were monitored at 260 nm. The retention time for gemcitabine hydrochloride and capecitabine hydrochloride was found to be 2.76 and 2.3 min respectively. The proposed method was validated in terms of linearity, accuracy, precision, limit of detection, limit of quantitation and robustness. The method was found to be linear in the range of 10-50 µg/mL and 4-24 µg/mL for gemcitabine hydrochloride and capecitabine hydrochloride, with regression coefficient r = 0.999 and r = 0.999, respectively.

  12. Design and development of polyethylene oxide based matrix tablets for verapamil hydrochloride

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    S Vidyadhara

    2013-01-01

    Full Text Available In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of verapamil hydrochloride. Verapamil hydrochloride was formulated as oral controlled release matrix tablets by using the polyethylene oxides (Polyox WSR 303. The aim of this study was to investigate the influence of polymer level and type of fillers namely lactose (soluble filler, swellable filler (starch 1500, microcrystalline cellulose and dibasic calcium phosphate (insoluble fillers on the release rate and mechanism of release for verapamil hydrochloride from matrix tablets prepared by direct compression process. Higher polymeric content in the matrix decreased the release rate of drug. On the other hand, replacement of lactose with anhydrous dibasic calcium phosphate and microcrystalline cellulose has significantly retarded the release rate of verapamil hydrochloride. Biopharmaceutical evaluation of satisfactory formulations were also carried out on New Zealand rabbits and parameters such as maximum plasma concentration, time to reach peak plasma concentration, area under the plasma concentration time curve (0-t and area under first moment curve (0-t were determined. In vivo pharmacokinetic study proves that the verapamil hydrochloride from matrix tablets showed prolonged release and were be able to sustain the therapeutic effect up to 24 h.

  13. RP-HPLC estimation of venlafaxine hydrochloride in tablet dosage forms

    Directory of Open Access Journals (Sweden)

    Baldania S

    2008-01-01

    Full Text Available A simple, specific, accurate, and precise reverse phase high performance liquid chromatographic method was developed and validated for the estimation of venlafaxine hydrochloride in tablet dosage forms. A Phenomenex Gemini C-18, 5 µm column having 250 x 4.6 mm i.d. in isocratic mode, with mobile phase containing methanol: 0.05 M potassium dihydrogen orthophosphate (70:30, v/v; pH 6.2 was used. The flow rate was 1.0 ml/min and effluents were monitored at 226 nm. Carbamazepine was used as an internal standard. The retention time of venlafaxine hydrochloride and carbamazepine were 3.7 min and 5.3 min, respectively. The method was validated for specificity, linearity, accuracy, precision, limit of quantification, limit of detection, robustness and solution stability. Limit of detection and limit of quantification for estimation of venlafaxine hydrochloride were found to be 100 ng/ml and 300 ng/ml, respectively. Recoveries of venlafaxine hydrochloride in tablet formulations were found to be in the range of 99.02-101.68%. Proposed method was successfully applied for the quantitative determination of venlafaxine hydrochloride in tablet dosage forms.

  14. HPLC Method for the Determination of Tamsulosin Hydrochloride in Sustained Release Tablets

    Institute of Scientific and Technical Information of China (English)

    齐美玲; 王鹏; 耿颖姝; 顾峻岭

    2003-01-01

    The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performed on a Diamonsil BDS C18 column with a mobile phase consisting of a mixture of acetonitrile, methanol and 0.5% phosphoric acid solution (20∶30∶50,V/V/V) at a flow rate of 1.0 mL/min. UV detection was made at 274 nm. The linear range for tamsulosin hydrochloride was 0.81-8.10 μg/mL. The mean recovery was 99.8% (SR=0.7%, n=9), and the precision was found to be 0.45% (n=9). The proposed method can be used for routine analysis of tamsulosin hydrochloride in sustained release tablets.

  15. Formulation Development and Characterization of Meclizine Hydrochloride Sublimated Fast Dissolving Tablets.

    Science.gov (United States)

    Vemula, Sateesh Kumar; Vangala, Mohan

    2014-01-01

    The intention of present research is to formulate and develop the meclizine hydrochloride fast dissolving tablets using sublimation method to enhance the dissolution rate. In this study an attempt was made to fasten the drug release from the oral tablets by incorporating the superdisintegrants and camphor as sublimating agent. The prepared fast dissolving tablets were subjected to precompression properties and characterized for hardness, weight variation, friability, wetting time, water absorption ratio, and disintegration time. From in vitro release studies, the formulation F9 exhibited fast release profile of about 98.61% in 30 min, and disintegration time 47 sec when compared with other formulations. The percent drug release in 30 min (Q 30) and initial dissolution rate for formulation F9 was 98.61 ± 0.25%, 3.29%/min. These were very much higher compared to marketed tablets (65.43 ± 0.57%, 2.18%/min). The dissolution efficiency was found to be 63.37 and it is increased by 1.4-fold with F9 FDT tablets compared to marketed tablets. Differential scanning calorimetry and Fourier transform infrared spectroscopy studies revealed that there was no possibility of interactions. Thus the development of meclizine hydrochloride fast dissolving tablets by sublimation method is a suitable approach to improve the dissolution rate.

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

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    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.

  17. Development and evaluation of buccoadhesive tablet for selegiline hydrochloride based on thiolated polycarbophil.

    Science.gov (United States)

    Wasnik, Mangesh N; Godse, Rutika D; Nair, Hema A

    2014-05-01

    Selegiline hydrochloride (SHCl), a monoamine oxidase B inhibitor, is used as an adjunct in the therapy of Parkinson's disease. This study is concerned with the preparation and evaluation of mucoadhesive buccal tablet for controlled systemic delivery of SHCl. Buccal absorption of selegiline can bypass its first-pass metabolism and improve bioavailability accompanied by greatly reduced metabolite formation, which is potentially of enhanced therapeutic value in patients with Parkinson's disease. Polycarbophil-cysteine (PCP-cys) conjugate, which is a thiolated derivative of the mucoadhesive polymer polycarbophil, was synthesized by 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride-mediated amide bond coupling. Tablets of SHCl based on native and thiolated polycarbophil were prepared. The prepared tablets were evaluated for drug content, swelling behavior, mucoadhesive strength, in vitro drug release, ex vivo permeation and in vitro cytotoxicity. PCP-cys tablets showed enhanced mucoadhesion and retarded drug release compared to polycarbophil tablets. Permeation data of SHCl from matrices prepared using the PCP-cys polymer revealed a significantly higher value of apparent permeability in comparison to polycarbophil, which supported the information in literature that thiolation imparts permeation enhancing properties to mucoadhesive polymers. In vitro cytotoxicity studies on PCP-cys using L-929 mouse fibroblast cell line indicated that conjugation with cysteine does not impart any apparent toxicity to polycarbophil. The results from the study indicate that the buccal delivery of SHCl using thiolated polycarbophil tablet could provide a way for improved therapy of Parkinson's disease.

  18. Abnormal dissolutions of chlorpromazine hydrochloride tablets in water by paddle method under a high agitation condition.

    Science.gov (United States)

    Aoyagi, Nobuo; Rimando, Annie Policarpio; Izutsu, Kenichi; Katori, Noriko; Kojima, Shigeo

    2003-09-01

    All sugar-coated tablets of chlorpromazine hydrochloride except for those produced by one manufacture showed concave dissolution profiles in water by paddle method at 100 rpm but not at 50 rpm. The study was undertaken to clarify the agitation-dependent abnormal dissolutions. The strange dissolutions were also observed in water at different ionic strengths but not in buffer solutions of pH 1.2, 4.0 and 6.8. When monitored, the pH's of water in dissolution vessels for the abnormal tablets increased with time at 100 rpm and some of them exceeded pH 8 but did not at 50 rpm. The solubility of chlorpromazine hydrochloride decreased with the increase of pH which was too low to dissolve the whole amount of drug contained in a tablet at pH 8. The elevation of pH seemed to be mainly brought about by dissolution of calcium carbonate popularly used for sugar-coated tablets, because larger amount of calcium ion was dissolved out from the abnormal tablets at 100 rpm than from a normal tablet and from them at 50 rpm. These findings indicate that the concave dissolution profiles should be caused by the decrease of drug solubility with increase in pH of water, probably because of dissolution of calcium carbonate. We should pay attention to the change in pH of water which may differ depending on the agitation speed of dissolution tests.

  19. FORMULATION AND EVALUATION OF S-(--AMLODIPINE BESYLATE AND NEBIVOLOL HYDROCHLORIDE TABLETS

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    Shaikh S.A

    2010-06-01

    Full Text Available The objective of the present study was to develop a tablet formulation of S-(-- amlodipine besylate chiral separation drug and nebivolol hydrochloride for better management of hypertension, while reducing or avoiding undesirable adverse effects, which are often associated with administration of a racemic mixture of amlodipine. The composition containing the optically pure S-(-- isomer of amlodipine 2.5 mg has calcium channel blocking activity and, nebivolol hydrochloride 5 mg has beta-receptor blocking activity.The study was also carried out to design a suitable dissolution medium for S-(- - amlodipine besylate and nebivolol hydrochloride. Amlodipine besylate and nebivolol hydrochloride had maximum solubility in pH 1.2 and thus pH 1.2 was selected as the most suitable media for S-(- - amlodipine besylate and nebivolol hydrochloride dissolution studies. The RSD below 2% indicated insignificant batch-to-batch variation. The accelerated stability study of the optimized formulation was performed as the ICH guidelines. The results indicated no change in optical rotation of S-(- - amlodipine besylate. Hence, combination of two drugs can be formulated into the tablet by wet granulation technique having satisfactory release profile.

  20. FORMULATION AND EVALUATION OF MOUTH DISSOLVING TABLETS OF METFORMIN HYDROCHLORIDE

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    Shaikh T.H.

    2012-06-01

    Full Text Available Metformin HCl is a biguanide antihyperglycemic agent used for treating non-insulin-dependent diabetes mellitus (NIDDM. It improves glycemic control by decreasing hepatic glucose production, decreasing glucose absorption and increasing insulin-mediated glucose uptake. In the present study an attempt has been made to prepare fast dissolving tablets of Metformin HCl in the oral cavity with enhanced dissolution rate. The tablets were prepared with three superdisintegrants e.g:, Croscarmellose sodium, Sodium starch glycolate and Crospovidone. The blend was examined for angle of repose, bulk density, tapped density, compressibility index and hausners ratio. The tablets were evaluated for hardenss, friability, disintegration time, dissolution rate,drug content, and were found to be within 1 min. It was concluded that the mouth dissolving tablets with proper hardness, rapidly disintegrating with enhanced dissolution can be made using selected superdisintegrants.

  1. Formulation Development and Optimization of Matrix Tablet of Tramadol Hydrochloride.

    Science.gov (United States)

    Deb, Pulak; Singha, Jubaraj; Chanda, Indranil; Chakraborty, Prithviraj

    2017-01-01

    The aim of the present investigation is to formulate and optimize oral sustained release matrix tablet of highly water soluble drug Tramadol HCl and to evaluate the effect of varying concentration of hydrophilic and hydrophobic polymer on drug release, based on a survey done on the recent patents of Tramadol HCl (US7374781, CA 2479252) and sustained release matrix tablets. The tablets were prepared by double granulation process, by melt granulation and wet granulation technique using Carnauba wax (CW) and HPMC K100 as release retardant. Pre and post compression factors were evaluated and all the parameters were found within the limit. The drug release data were subjected to different models in order to evaluate release kinetics and mechanism of drug release. The prepared formulations showed drug release in the range 100±2% in 6hrs, 7hrs, 8hrs and 9hrs and upto 12 hrs respectively. The optimized tablet having 25% CW and 20% HPMC showed sustained drug release pattern. Hydrophilic matrix of HPMC alone could not control the Tramadol release effectively for 12 h whereas when combined with CW could slow down the release of drug and can be successfully employed for formulating sustained-release matrix tablets. Similarity factor, f2 shows the test and reference profile are identical. Double granulation technique with CW and HPMC K100 proved as a better technique for sustaining the drug release from the matrix tablet. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  2. A randomized, crossover design study of sevelamer carbonate powder and sevelamer hydrochloride tablets in chronic kidney disease patients on haemodialysis

    OpenAIRE

    Fan, Stanley; Ross, Calum; Mitra, Sandip; Kalra, Philip; Heaton, Jeremy; Hunter, John; Plone, Melissa; Pritchard, Nick

    2009-01-01

    Background. Sevelamer carbonate is an improved, buffered form of sevelamer hydrochloride developed for the treatment of hyperphosphataemia in CKD patients. Sevelamer carbonate formulated as a powder for oral suspension presents a novel, patient-friendly alternative to tablet phosphate binders. This study compared the safety and efficacy of sevelamer carbonate powder with sevelamer hydrochloride tablets in CKD patients on haemodialysis. Methods. This was a multi-centre, open-label, randomized,...

  3. 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.

  4. Comparative bioequivalence studies of tramadol hydrochloride sustained-release 200 mg tablets

    OpenAIRE

    Suhas, Khandave; Satish ,Sawant; Santosh ,Joshi; Bansal,Yatish Kumar; Sonal Sushil Kadam,

    2010-01-01

    Suhas S Khandave1, Satish V Sawant1, Santosh S Joshi1, Yatish K Bansal2, Sonal S Kadam21Accutest Research Laboratories (I) Private Limited, Koparkhirne, Navi Mumbai, Maharashtra, India; 2Ipca Laboratories Limited, Kandivli Mumbai, Maharashtra, IndiaBackground: Tramadol hydrochloride is available as 50 mg immediate-release (IR) and 100 mg, 200 mg, and 300 mg sustained-release (SR) tablets. The recommended dose of tramadol is 50–100 mg IR tablets every 4–6 hours. The tramado...

  5. RP-HPLC estimation of imipramine hydrochloride and diazepam in tablets

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    D Srikantha

    2015-01-01

    Full Text Available A simple and rapid reversed phase-high performance liquid chromatographic method was developed for simultaneous determination of imipramine hydrochloride and diazepam in pharmaceutical formulations. The elution was done in isocratic mode utilizing a mobile phase consisting of methanol:water:0.1M sodium acetate (30:50:20 v/v/v on Chromosil C18 column with a flow rate of 1.0 ml/min and with detection at 243 nm. The measured retention time was 3.33±0.02 min for imipramine hydrochloride and 4.64±0.02 min for diazepam. Linearity was measured in the range 25-150 μg/ml for imipramine hydrochloride (r 2 =0.999 and in the range 5-30 μg/ml for diazepam (r 2 =0.9994, respectively. The limits of detection and quantitation were 0.03 and 0.1 μg/ml for imipramine hydrochloride and 0.02 and 0.07 μg/ml for diazepam. Satisfactory validation was also obtained from recovery (100.95-101.52% for imipramine hydrochloride and 99.47-100.33% for diazepam studies, intraday and interday precision (<2% and robustness results. The reported method was the first study of these drugs in combination and could be employed for routine quantitative determination of imipramine hydrochloride and diazepam in tablets.

  6. Formulation and evaluation of bilayer tablet for bimodal release of venlafaxine hydrochloride

    OpenAIRE

    2015-01-01

    The aim of the present research was to develop a bilayer tablet of venlafaxine hydrochloride for bimodal drug release. In the present investigation authors have tried to explore fenugreek mucilage (FNM) for bioadhesive sustained release layer. The attempt has been made to combine FNM with well studied bioadhesive polymers like hydroxy propyl methyl cellulose (HPMC), Carbopol, and Xanthan Gum. The formulations were evaluated for swelling Index, ex vivo bioadhesion, water uptake studies, in vit...

  7. Formulation and evaluation of S-(--Amlodipine besylate and nebivolol hydrochloride tablets

    Directory of Open Access Journals (Sweden)

    S A Shaikh

    2010-01-01

    The study was also carried out to design a suitable dissolution medium for S-(- - amlodipine besylate and nebivolol hydrochloride. Amlodipine besylate and nebivolol hydrochloride had maximum solubility in pH 1.2 and thus pH 1.2 was selected as the most suitable media for S-(- - amlodipine besylate and nebivolol hydrochloride dissolution studies. The RSD below 2% indicated insignificant batch-to-batch variation. The accelerated stability study of the optimized formulation was performed as the ICH guidelines. The results indicated no change in optical rotation of S-(- - amlodipine besylate. Hence, combination of two drugs can be formulated into the tablet by wet granulation technique having satisfactory release profile.

  8. Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets.

    Science.gov (United States)

    Uzunović, Alija; Vranić, Edina

    2007-08-01

    Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time. It is hydrophobic, and there are many reports in the literature concerning its adverse effect on dissolution rates. The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg. The uniformity content was also checked. During the drug formulation development, several samples were designed for choice of the formulation. For this study, two formulations containing 0,77 and 1,1% of magnesium stearate added in the manufacture of cores were chosen. Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves. The data were analyzed using pharmacopeial test for similarity of dissolution profiles ( f2 equation), previously proposed by Moore and Flanner. Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties. The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response.

  9. TASTE MASKING AND FORMULATION OF ONDANSETRON HYDROCHLORIDE MOUTH DISSOLVING TABLETS

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    Shyam Raj Subedi, Bhupendra Kumar Poudel

    2015-05-01

    Full Text Available This study was done to mask the bitter taste of ondansetron HCl using complexing agent, a polacrilex resin: Tulsion 335 and subsequently forming mouth dissolving tablet using superdisintegrants: Croscarmellose sodium and sodium starch glycollate. A preliminary screening was done. Batch process, a most preferential method for drug loading with ion exchange resins was selected. The process was optimized for drug: resin ratio to get maximum drug loading. A ratio of drug: resin at 1:3 was selected. Taste evaluation was carried out by selecting volunteers. Drug resin complex (DRC was evaluated for drug release. The resultant DRC was formulated by direct compression into mouth dissolving tablet using microcrystalline cellulose PH 102, as diluent and croscarmalose sodium and sodium starch glycolate as superdisintegrants and aspartame was used as sweetening agent to enhance palatability. Thirteen formulations were developed by using superdisintegrants: croscarmellose sodium and sodium starch glycolate. Concentration of superdisintegrants ranged from 0.75-9.24 %. The formulated tablet had satisfactory disintegration time and dissolution profile. Optimization was carried out using central composite design. The disintegration and dissolution times were tallied with marketed ondansetron HCl tablets. From the results, it was deduced that the most effective concentration for desired disintegration was of croscarmellose sodium and sodium starch glycollate respectively at concentration above 5%. Therefore, it can be concluded that the intensely bitter taste of ondansetron HCl can be masked by using tulsion 335 and mouth dissolving ondansetron HCl can be successfully prepared by adding aforementioned superdisintegrants. This sort of mouth dissolving ondansetron HCl can be used in controlling vomiting in paediatric and geriatric patients and also for pregnancy induced vomiting.

  10. Bioequivalence Study of Donepezil Hydrochloride Tablets in Healthy Male Volunteers

    OpenAIRE

    Supanimit Teekachunhatean; Sukit Roongapinun; Nutthiya Hanprasertpong; Siriluk Aunmuang; Noppamas Rojanasthien

    2012-01-01

    The objective of this study was to investigate the bioequivalence of two formulations of 5 mg donepezil HCL tablets: Tonizep as the test and Aricept as the reference. The two products were administered as a single oral dose according to a randomized two-phase crossover with a 3-week washout period in 20 healthy Thai Male volunteers. After drug administration, serial blood samples were collected over a period of 216 hours. Plasma donepezil concentrations were measured by high performance liqui...

  11. Formulation and evaluation of floating matrix tablets of diltiazem hydrochloride

    Directory of Open Access Journals (Sweden)

    Vinay D Gaikwad

    2012-01-01

    Full Text Available This study was performed to design floating tablets of diltiazem as a model drug for prolongation of gastric residence time. A simple visible spectrophotometric method was employed for the estimation of diltiazem at 236 nm and Beer′s law is obeyed in the concentration range of 2-20 mg/ml. Preformulation studies were carried out to optimize the ratios required for various grades of HPMC-SCMC and HPMC- Carbopol P934. Total 10 formulations (five each were prepared using HPMC (K4M. The prepared floating tablets were evaluated for hardness, weight variation, thickness, friability, drug content uniformity, buoyancy lag time, total floating time, water uptake (swelling index, and in vitro dissolution studies. SEM and stability studies were carried out only for best release formulations (A1 and B1. Among the five formulations with HPMC K4M and A1-A4 showed drug release ranging from 99.89 to 77.52%. Similarly five formulations with HPMC K4M and Carbopol P934 (B1-B4 showed drug release ranging from 97.9 to 80.35% in 0.1 N HCl dissolution medium. Formulations A1 and B1 gave maximum drug release upto 100% within 12 hrs. SEM for A1 and B1 formulations revealed that surface was smooth upto 4 hrs after that swelling and porosity of tablet increased indicating the diffusion and erosion mechanism of release.

  12. Development and Characterization of Novel Floating-Mucoadhesive Tablets Bearing Venlafaxine Hydrochloride

    Directory of Open Access Journals (Sweden)

    Raghvendra Misra

    2016-01-01

    Full Text Available The present investigation is concerned about the development of floating bioadhesive drug delivery system of venlafaxine hydrochloride which after oral administration exhibits a unique combination of floating and bioadhesion to prolong gastric residence time and increase drug bioavailability within the stomach. The floating bioadhesive tablets were prepared by the wet granulation method using different ratios of hydroxypropyl methyl cellulose (HPMC K4MCR and Carbopol 934PNF as polymers. Sodium bicarbonate (NaHCO3 and citric acid were used as gas (CO2 generating agents. Tablets were characterized for floating properties, in vitro drug release, detachment force, and swelling index. The concentration of hydroxypropyl methyl cellulose and Carbopol 934PNF significantly affects the in vitro drug release, floating properties, detachment force, and swelling properties of the tablets. The optimized formulation showed the floating lag time 72±2.49 seconds and duration of floating 24.50±0.74 hr. The in vitro release studies and floating behavior were studied in simulated gastric fluid (SGF at pH 1.2. Different drug release kinetics models were also applied. The in vitro drug release from tablets was sufficiently sustained (more than 18 hr and the Fickian transports of the drug from the tablets were confirmed. The radiological evidence suggests that the tablets remained buoyant and altered position in the stomach of albino rabbit and mean gastric residence time was prolonged (more than > 6 hr.

  13. Mathematical Model-Based Accelerated Development of Extended-release Metformin Hydrochloride Tablet Formulation.

    Science.gov (United States)

    Chen, W; Desai, D; Good, D; Crison, J; Timmins, P; Paruchuri, S; Wang, J; Ha, K

    2016-08-01

    A computational fluid dynamic (CFD) model was developed to predict metformin release from a hydroxypropylmethylcellulose (HPMC) matrix-based extended-release formulation that took into consideration the physical and chemical properties of the drug substance, composition, as well as size and shape of the tablet. New high dose strength (1000 mg) tablet geometry was selected based on the surface area/volume (SA/V) approach advocated by Lapidus/Lordi/Reynold to obtain the desired equivalent metformin release kinetics. Maintaining a similar SA/V ratio across all extended-release metformin hydrochloride (Met XR) tablet strengths that had different geometries provided similar simulations of dissolution behavior. Experimental dissolution profiles of three lots of high-strength tablets agreed with the simulated release kinetics. Additionally, a pharmacokinetic absorption model was developed using GastroPlus™ software and known physicochemical, pharmacokinetic, and in vitro dissolution properties of metformin to predict the clinical exposure of the new high strength (1000 mg) tablet prior to conducting a human clinical bioequivalence study. In vitro metformin release kinetics were utilized in the absorption model to predict exposures in humans for new 1000-mg Met XR tablets, and the absorption model correctly projected equivalent in vivo exposure across all dose strengths. A clinical bioequivalence study was pursued based on the combined modeling results and demonstrated equivalent exposure as predicted by the simulations.

  14. FORMULATION AND EVALUATION OF SUSTAINED RELEASE TABLET OF DILTIAZEM HYDROCHLORIDE BY MELT GRANULATION TECHNOLOGY

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    Birajdar Ganesh

    2013-07-01

    Full Text Available The objective behind present study was to formulate and evaluate sustained release tablet of Diltiazem hydrochloride by using different polymers by melt granulation technology and to study the effect of various concentrations of polymers on release rate from tablet. Tablets were prepared using bees wax, carnauba wax, paraffin wax as release ratardent polymers. The drug and excipient compatibility study was done by FTIR method using KBr pellet method. The granules prepared by melt granulation technique evaluated for characterization such as bulk density, tapped density, hausners ratio, angle of repose, cars index all granules shows good flow property. The tablet of Diltiazem HCL evaluated for characterization such as hardness, friability, weight variation and content uniformity all tablets shows sufficient hardness and friability shows that tablets are having sufficient strength. All results were satisfactory. The in vitro drug release studies for the prepared formulation were conducted for a period of 12 h using an EDT 08LX dissolution tester USP Type - II apparatus (rotating paddle set at 100 rpm and a temperature of 37 ± 0.5°C formulation was placed in the 900 ml of the medium. For first 2 h tablet was placed in 1.2 pH acidic medium which was replaced with 7.4 pH phosphate buffer for remaining 10 h. From the dissolution study and comparative graph it was concluded that increase in concentration of wax shows decrease in drug release from tablet. Batch F3 shows 99.84 % drug release at 12 h. In vitro release data of optimized formulations (Batch F3 was fitted to various kinetic models like zero order, first order, Higuchi, korsmeyer-peppas and pass Higuchi model as it has highest r2 value (0.955 among all models.

  15. Formulation and evaluation of once daily minocycline hydrochloride extended release matrix tablets

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    Keny R

    2009-01-01

    Full Text Available The present study was aimed to develop once daily extended release matrix tablets of minocycline hydrochloride, using hydroxypropylmethylcellulose either alone or in combination with ethyl cellulose as the matrix material in different proportions. The formulated tablets were also compared with a marketed product. The results of the dissolution study indicate that formulations FC-IV, FC-V and FC-VI showed maximum drug release upto 24 h, whereas the marketed product was found to extend the release only up to 14 h. Incase of formulations containing combination of hydroxypropylmethylcellulose and ethyl cellulose (FC-I to FC-IX, the release of the drug was found to be dependent on the relative proportions of hydroxypropylmethylcellulose and ethyl cellulose used in the tablet matrix. Mathematical treatment of the in vitro drug release data suggests that, all the formulations best fitted into first order release kinetics. Drug release from the matrix occurred by combination of two mechanisms, diffusion of drug from tablet matrix and erosion of tablet surface, which was reflected from Higuchi′s model and Erosion plot.

  16. Spectrophotometric and HPLC methods for simultaneous estimation of pseudoephedrine hydrochloride and loratadine from tablets

    Directory of Open Access Journals (Sweden)

    Singhvi I

    2006-01-01

    Full Text Available Two simple, accurate, economical and reproducible UV spectrophotometric and one HPLC method for simultaneous estimation of two-component drug mixture of pseudoephedrine hydrochloride and loratadine in combined tablet dosage form have been developed. The first developed method employs multiwavelength spectroscopy using seven mixed standards and 257.0 nm and 283.0 nm as two wavelengths for estimation. The second method involves first derivative spectroscopy using 308.6 nm and 263.0 nm as zero crossing points for pseudoephedrine hydrochloride and loratadine respectively. For both spectrophotometric methods, 0.2 M hydrochloric acid was used as solvent. Linearity was observed in concentration range of 0-40 mg/ml of loratadine and 0-800 mg/ml of pseudoephedrine hydrochloride. Developed HPLC method is reverse-phase chromatographic method using Inertsil C 18 column and methanol:ammonium acetate buffer in ratio of 80:20 pH 7.5 as mobile phase. Nimesulide was used as internal standard for HPLC method. For HPLC method, linearity was observed in concentration range of 0-200 mg/ml of loratadine and 100-2000 mg/ml of pseudoephedrine hydrochloride. Results of analysis were validated statistically and by recovery studies.

  17. Application of new membrane selective electrodes for the determination of drotaverine hydrochloride in tablets and plasma.

    Science.gov (United States)

    El-Saharty, Y S; Metwaly, F H; Refaat, M; El-Khateeb, S Z

    2006-06-07

    The construction and electrochemical response characteristics of poly vinyl chloride (PVC) membrane sensors for the determination of drotaverine hydrochloride were described. The sensors are based on the use of the ion association complexes of drotaverine cation with sodium phosphotungestate (Dro-PTA) or ammonium reineckate (Dro-R) counter anions as ion exchange sites in the PVC matrix. The performance characteristics of these sensors, which were evaluated according to IUPAC recommendations, reveal a fast, stable and linear response for drotaverine over the concentration range 10(-5) to 10(-2) M with cationic slopes of 49.55 and 51.36 mV per concentration decade. The direct potentiometric determination of drotaverine hydrochloride using the proposed sensors gave average recoveries of 99.95+/-0.71 and 100.04+/-0.60 for Dro-PTA and Dro-R, respectively. The sensors are used for determination of drotaverine hydrochloride in tablets, in its mixture with caffeine and paracetamol and in plasma. Validation of the method shows suitability of the proposed sensors for use in the quality control assessment of drotaverine hydrochloride. The developed method was found to be simple, accurate and precise when compared with a reported HPLC method.

  18. Properties of lipophilic matrix tablets containing phenylpropanolamine hydrochloride prepared by hot-melt extrusion.

    Science.gov (United States)

    Liu, J; Zhang, F; McGinity, J W

    2001-09-01

    The objective of the present study was to investigate the influence of formulation factors on the physical properties of hot-melt extruded granules and compressed tablets containing wax as a thermal binder/retarding agent, and to compare the properties of granules and tablets with those prepared by a high-shear melt granulation (MG) method. Powder blends containing phenylpropanolamine hydrochloride, Precirol and various excipients were extruded in a single-screw extruder at open-end discharge conditions. The extrudates were then passed through a 14-mesh screen to form granules. The extrusion conditions and the optimum amount of wax to function as the thermal binder were dependent on the properties of the filler excipients. At the same wax level, drug release from tablets decreased in the order of using microcrystalline cellulose (MCC), lactose and Emcompress as the filler excipient. The observed differences in the dissolution properties of the tablets were due to the differences in the solubility, swellability and density of the filler excipients. Replacing Precirol with Sterotex K, a higher melting point wax, resulted in slightly increased dissolution rates, when the extrusion was performed at the same temperature conditions. Hot-melt extruded granules were observed to be less spherical than high-shear melt granules and showed lower values of bulk/tap densities. However, tablets containing MCC or lactose granules prepared by hot-melt extrusion (HME) exhibited higher hardness values. Slower drug release rates were found for tablets containing MCC by HME compared with MG. Analysis of the hot-melt extruded granules showed better drug content uniformity among granules of different size ranges compared with high-shear melt granules, resulting in a more reproducible drug release from the corresponding tablets.

  19. Controlled release of metformin hydrochloride and repaglinide from sandwiched osmotic pump tablet.

    Science.gov (United States)

    Qin, Chao; He, Wei; Zhu, Chunli; Wu, Mengmeng; Jin, Zhu; Zhang, Qiang; Wang, Guangji; Yin, Lifang

    2014-05-15

    The marketed compound tablet of metformin hydrochloride (MH) and repaglinide (RG) exhibits perfect multidrug therapeutic effect of type 2 diabetes. However, due to the short half life of the drugs, the tablet has to be administered 2 to 3 times a day, causing inconvenience to patient and fluctuations of plasma concentration. Here, a sandwiched osmotic pump tablet was developed to deliver the two drugs simultaneously at zero-order rate, in which MH and RG were loaded in different layers separated by a push layer. The osmotic pump tablet was prepared by a combination of three tableting procedure and film coating method. The factors including type and amount of propellant, osmotic active agents, amount of porogenic agent, coating weight, orifice diameter were optimized. The pharmacokinetic study was performed in beagle dogs, and the drug concentration in plasma samples was assayed by HPLC-MS/MS method. Simultaneous, controlled release of MH and RG in the first 12 and 8h was achieved from the optimized formulation. A significantly decreased Cmax, prolonged Tmax and satisfactory bioavailability of the osmotic pump tablet were obtained, and a good in vivo-in vitro correlation of the two drugs was also established. In summary, the sandwiched osmotic pump tablet released the MH and RG simultaneously at zero-order rate, and exhibited significant sustained release effect in vivo and good in vivo-in vitro correlation. The designed controlled release system for MH and RG proposed a promising replacement for the marked compound product in the therapy of type 2 diabetes.

  20. SIMULTANEOUS ESTIMATION & VALIDATION OF PARACETAMOL, PHENYLEPHRINE HYDROCHLORIDE AND CHLORPHENIRAMINE MALEATE IN TABLETS BY SPECTROPHOTOMETRIC METHOD

    Directory of Open Access Journals (Sweden)

    R. SAWANT, R. JOSHI, P. LANKE L. BHANGALE

    2013-09-01

    Full Text Available The present work describes two methods for simultaneous estimation of phenylephrine hydrochloride and chlorpheniramine maleate in pure and solid dosage forms. First method employs the application of simultaneous equation and second, is a multi-wavelength spectrophotometric analysis method. Both methods utilize 0.1N NaOH as solvent. Simultaneous equation develops using 256.8 nm, 236.8 nm and 222.4 nm as the max of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate respectively. Calibration curves were linear over the concentration ranges of 0-35 μg/mL for all drugs. The results demonstrated that the procedure is accurate, precise and reproducible (relative standard deviation < 1 %, while being simple, cheap and less time consuming, and hence can be suitably applied for simultaneous determination of three drugs in laboratory prepared mixtures and in commercial tablet preparation.

  1. Simultaneous spectrophotometric estimation of imipramine hydrochloride and chlordiazepoxide in tablets

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    Patel Sejal

    2009-01-01

    Full Text Available A binary mixture of imipramine HCl and chlordiazepoxide was determined by three different spectrophotometric methods. The first method involved determination of imipramine HCl and chlordiazepoxide using the simultaneous equations and the second method involved absorbance ratio method. Imipramine has absorbance maxima at 251 nm, chlordiazepoxide has absorbance maxima at 264.5 nm and isoabsorptive point is at 220 nm in methanol. Linearity was obtained in the concentration ranges of 1-25 and 1-10 μg/ml for Imipramine HCL and Chlordiazepoxide, respectively. The third method involved determination of these two drugs using the first-derivative spectrophotometric technique at 219 and 231.5 nm over the concentration ranges of 1-20 and 2-24 μg/ml with mean accuracies 99.46±0.78 and 101.43±1.20%, respectively. These methods were successively applied to pharmaceutical formulations because no interferences from the tablet excipients were found. The suitability of these methods for the quantitative determination of the compounds was proved by validation.

  2. Formulation Development and Evaluation of Fast Disintegrating Tablet of Cetirizine Hydrochloride: A Novel Drug Delivery for Pediatrics and Geriatrics

    Science.gov (United States)

    Sharma, Deepak; Singh, Mankaran; Kumar, Dinesh; Singh, Gurmeet

    2014-01-01

    Recent developments in fast disintegrating tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets. The objective of the present study was to prepare the fast disintegrating tablet of Cetirizine Hydrochloride for allergic and respiratory disorders. As precision of dosing and patient's compliance become important prerequisite for a long-term treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient's acceptability. Hence, the present investigation was undertaken with a view to develop a fast disintegrating tablet of Cetirizine Hydrochloride which offers a new range of products having desired characteristics and intended benefits. Superdisintegrants such as Sodium Starch Glycolate were optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were prepared by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time and uniformity of content. Optimized formulation was evaluated by in vitro dissolution test, drug excipient compatibility and accelerated stability study. It was concluded that fast disintegrating tablets of Cetirizine Hydrochloride were formulated successfully with desired characteristics which disintegrated rapidly, provide rapid onset of action, and enhance the patient convenience and compliance. PMID:26556203

  3. Formulation Development and Evaluation of Fast Disintegrating Tablet of Cetirizine Hydrochloride: A Novel Drug Delivery for Pediatrics and Geriatrics

    Directory of Open Access Journals (Sweden)

    Deepak Sharma

    2014-01-01

    Full Text Available Recent developments in fast disintegrating tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets. The objective of the present study was to prepare the fast disintegrating tablet of Cetirizine Hydrochloride for allergic and respiratory disorders. As precision of dosing and patient's compliance become important prerequisite for a long-term treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient’s acceptability. Hence, the present investigation was undertaken with a view to develop a fast disintegrating tablet of Cetirizine Hydrochloride which offers a new range of products having desired characteristics and intended benefits. Superdisintegrants such as Sodium Starch Glycolate were optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were prepared by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time and uniformity of content. Optimized formulation was evaluated by in vitro dissolution test, drug excipient compatibility and accelerated stability study. It was concluded that fast disintegrating tablets of Cetirizine Hydrochloride were formulated successfully with desired characteristics which disintegrated rapidly, provide rapid onset of action, and enhance the patient convenience and compliance.

  4. Spectrophotometric Quantitative Estimation and Validation of Nimesulide and Drotaverine Hydrochloride in Tablet Dosage form

    OpenAIRE

    Prasad R. K.; Sharma R

    2010-01-01

    Three simple, sensitive and accurate UV spectrophotometric methods, I; first order derivative spectrophotometric, II; area under curve and III; multi-component method, has been developed for the estimation of drotaverine hydrochloride and nimesulide in tablets dosage form. Beers’ law was obeyed in the concentration range 5-35 µgml-1 and 10-50 µgml-1 for drotaverine (λmax = 230.5 nm) and nimesulide (λmax = 331.5 nm) respectively in methanol. All the three methods allowed rapid analysis of bina...

  5. Development and validation of simultaneous spectrophotometric methods for drotaverine hydrochloride and aceclofenac from tablet dosage form.

    Science.gov (United States)

    Shah, S A; Shah, D R; Chauhan, R S; Jain, J R

    2011-05-01

    Two simple spectrophotometric methods have been developed for simultaneous estimation of drotaverine hydrochloride and aceclofenac from tablet dosage form. Method I is a simultaneous equation method (Vierodt's method), wavelengths selected are 306.5 and 276 nm. Method II is the absorbance ratio method (Q-Analysis), which employs 298.5 nm as λ(1) and 276 nm as λ(2) (λmax of AF) for formation of equations. Both the methods were found to be linear between the range of 8-32 μg/ml for drotaverine and 10-40 μg/ml for aceclofenac. The accuracy and precision were determined and found to comply with ICH guidelines. Both the methods showed good reproducibility and recovery with % RSD in the desired range. The methods were found to be rapid, specific, precise and accurate and can be successfully applied for the routine analysis of drotaverine and aceclofenac in their combined tablet dosage form.

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

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    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

  7. FORMULATION AND EVALUATION OF FLOATING MATRIX TABLET OF RANITIDINE HYDROCHLORIDE

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    Himanshu D. Ravat

    2012-05-01

    Full Text Available Ranitidine HCl is used for the H2 receptor antagonist. It is an absorption window limited drug, whosesolubility decreases with increase in the pH and has a short half life of 2-3 h. Therefore the presentinvestigation is concerned with the development of the floating matrix tablets, which after oraladministration were designed to prolong the gastric residence time and thus to increase thebioavailability of the drug and its half life. Ranitidine HCl showed maximum absorption at wavelength324 nm in 0.1N HCl. Drug-polymer compatibility studies by DSC give conformation about their purityand showed no interaction between drug and selected polymers. Various formulations were developedby using release rate controlling and gel forming polymers like HPMC K4 M, and Polyethylene oxideWSR 303 in single by direct compression method with the incorporation of sodium bicarbonate as gasgenerating agent. All the formulations had floating lag time below 4 minutes and constantly floated ondissolution medium for more than 12 h. Swelling studies indicated significant water uptake andcontributed in drug release. From all the developed formulations, batch F5 and F6 prolonged the drugrelease for longer period of time, they were nominated as best formulations. The best formulationsfollowed power law kinetics while the drug release mechanism was found to be diffusion through andpolymer relaxation. The best formulations were found to be stable during stability studies for one month.Thus, best formulations satisfied physico-chemical parameters, floating time, swelling index and in vitrodrug release profile requirements for a floating drug delivery system.

  8. Six sigma: process of understanding the control and capability of ranitidine hydrochloride tablet.

    Science.gov (United States)

    Chabukswar, Ar; Jagdale, Sc; Kuchekar, Bs; Joshi, Vd; Deshmukh, Gr; Kothawade, Hs; Kuckekar, Ab; Lokhande, Pd

    2011-01-01

    The process of understanding the control and capability (PUCC) is an iterative closed loop process for continuous improvement. It covers the DMAIC toolkit in its three phases. PUCC is an iterative approach that rotates between the three pillars of the process of understanding, process control, and process capability, with each iteration resulting in a more capable and robust process. It is rightly said that being at the top is a marathon and not a sprint. The objective of the six sigma study of Ranitidine hydrochloride tablets is to achieve perfection in tablet manufacturing by reviewing the present robust manufacturing process, to find out ways to improve and modify the process, which will yield tablets that are defect-free and will give more customer satisfaction. The application of six sigma led to an improved process capability, due to the improved sigma level of the process from 1.5 to 4, a higher yield, due to reduced variation and reduction of thick tablets, reduction in packing line stoppages, reduction in re-work by 50%, a more standardized process, with smooth flow and change in coating suspension reconstitution level (8%w/w), a huge cost reduction of approximately Rs.90 to 95 lakhs per annum, an improved overall efficiency by 30% approximately, and improved overall quality of the product.

  9. Formulation of taste masked oro-dispersible tablets of ambroxol hydrochloride

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    Venkatesh D

    2008-01-01

    Full Text Available Ambroxol hydrochloride (HCL is a potent mucolytic capable of inducing bronchial secretion. It is used in the treatment of asthma, bronchitis, and cough. But it is a very bitter drug and slightly soluble in water. Thus, in the work under taken, an attempt was made to mask the taste and to formulate into a oro-dispersible tablet by complexation with ion exchange resins, which also acts as super disintegrating agents. Since, these tablets can be swallowed in the form of dispersion, it is suitable dosage form for pediatric and geriatric patients. Cation exchange resins like Indion-204 and Indion-234 were utilized for the sorption of drug. Drug-resinates were prepared in drug to resin ratio of 1:5 and 1:6. The prepared tablets were evaluated for general appearance, content uniformity, hardness, friability, taste evaluation, mouth feel, wetting time, in vitro and in vivo disintegration time, and in vitro dissolution studies. Tablets with both the resins have shown quick disintegrating features, i.e., within 20 s, which is very characteristic of oro-dispersible tablets. Also, the dispersion not showing any bitter taste, indicate the capability of ion exchange resins used, both as taste masking and super disintegrating agents. Almost more than 90 percent of drug was released from both the formulations within 1 h. Further formulations were subjected to stability testing for 3 months at temperatures 25±5°C/60±5%RH and 40±5°C/75±5%RH. Both tablets have shown no appreciable changes with respect to taste, disintegration, and dissolution profiles.

  10. Simultaneous chemometric determination of pyridoxine hydrochloride and isoniazid in tablets by multivariate regression methods.

    Science.gov (United States)

    Dinç, Erdal; Ustündağ, Ozgür; Baleanu, Dumitru

    2010-08-01

    The sole use of pyridoxine hydrochloride during treatment of tuberculosis gives rise to pyridoxine deficiency. Therefore, a combination of pyridoxine hydrochloride and isoniazid is used in pharmaceutical dosage form in tuberculosis treatment to reduce this side effect. In this study, two chemometric methods, partial least squares (PLS) and principal component regression (PCR), were applied to the simultaneous determination of pyridoxine (PYR) and isoniazid (ISO) in their tablets. A concentration training set comprising binary mixtures of PYR and ISO consisting of 20 different combinations were randomly prepared in 0.1 M HCl. Both multivariate calibration models were constructed using the relationships between the concentration data set (concentration data matrix) and absorbance data matrix in the spectral region 200-330 nm. The accuracy and the precision of the proposed chemometric methods were validated by analyzing synthetic mixtures containing the investigated drugs. The recovery results obtained by applying PCR and PLS calibrations to the artificial mixtures were found between 100.0 and 100.7%. Satisfactory results obtained by applying the PLS and PCR methods to both artificial and commercial samples were obtained. The results obtained in this manuscript strongly encourage us to use them for the quality control and the routine analysis of the marketing tablets containing PYR and ISO drugs.

  11. Development and validation of RP-HPLC method for the estimation of ivabradine hydrochloride in tablets

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    Seerapu Sunitha

    2010-01-01

    Full Text Available A simple, sensitive, precise and robust reverse-phase high-performance liquid chromatographic method for analysis of ivabradine hydrochloride in pharmaceutical formulations was developed and validated as per ICH guidelines. The separation was performed on SS Wakosil C18AR, 250Χ4.6 mm, 5 μm column with methanol:25 mM phosphate buffer (60:40 v/v, adjusted to pH 6.5 with orthophosphoric acid, added drop wise, as mobile phase. A well defined chromatographic peak of Ivabradine hydrochloride was exhibited with a retention time of 6.55±0.05 min and tailing factor of 1.14 at the flow rate of 0.8 ml/min and at ambient temperature, when monitored at 285 nm. The linear regression analysis data for calibration plots showed good linear relationship with R=0.9998 in the concentration range of 30-210 μg/ml. The method was validated for precision, recovery and robustness. Intra and Inter-day precision (% relative standard deviation were always less than 2%. The method showed the mean % recovery of 99.00 and 98.55 % for Ivabrad and Inapure tablets, respectively. The proposed method has been successfully applied to the commercial tablets without any interference of excipients.

  12. Ultraviolet spectrophotometric method for analytical determination of mianserin hydrochloride in coated tablets and comparison with LC

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    Letícia Lenz Sfair

    2015-12-01

    Full Text Available abstract Ultraviolet spectrophotometric (UV and Liquid Chromatographic (LC methods for the determination of mianserin hydrochloride in pharmaceutical formulation were developed and validated. The various parameters, such as specificity, linearity, precision and accuracy were studied according to International Conference on Harmonization (ICH, 2005. For UV method, mianserin hydrochloride was determinate at 278 nm using HCl 0.1 M as the solvent. The response was linear in the concentration range of 20.0 - 140.0 µg/mL (r = 0.9998. Precision data evaluated by relative standard deviation was lower than 2%. The UV method was simple, rapid and low cost. Chromatographic analyses were performed in an Ace C18 column and the mobile phase was composed of methanol, 50 mM monobasic potassium phosphate buffer and 0.3% triethylamine solution adjusted to pH 7.0 with phosphoric acid 10% (85:15. LC method was specific, linear, precise, exact and robust. The results confirmed that the both methods are valid and useful to the routine quality control of mianserin hydrochloride in coated tablets. Statistical analysis by Student´s t-test showed no significant difference between the results obtained by UV and LC methods.

  13. [Simultaneous determination of ibuprofen and pseudoephedrin hydrochloride and chlorpheniramine maleate in the compound buluoweimanamin tablets by HPLC].

    Science.gov (United States)

    Yin, San-fu; Qiu, Zong-yin

    2010-07-01

    An HPLC method was developed to determinate Ibuprofen and Pseudoephedrine Hydrochloride and Chlorpheniramine Maleate in Compound BuluoWeimaNamin Tablets. Using HPLC with Kromasil C18 column, and acetonitrile -0.5% SDS- phosphate (580:420:1) as the mobile phase. The wavelength for detection was 262 nm. Better linearities and good correlation coefficients were obtained: the concentration ranges of ibuprofen, pseudoephedrine hydrochloride and chlorpheniramine maleate were over 2.062-14.434 microg (r=0.9999), 0.296-2.072l microg (r=0.9999), and 0.0204~0.1428 microg (r=0.9998), respectively. The recoveries of ibuprofen, pseudoephedrine hydrochloride and chlorpheniramine maleate were 99.98% (RSD=0.52%), 99.72 (RSD=0.82%) and 99.545 (RSD=0.76%), respectively. The method was convenient, accurate and specific. It can be used as a method to control quality of Compound Buluoweimanamin Tablets.

  14. RP-HPLC and HPTLC methods for the estimation of nebivolol hydrochloride in tablet dosage form

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    Patel L

    2007-01-01

    Full Text Available Two simple, specific, accurate and precise methods, namely, reverse phase high performance liquid chromatography and high performance thin layer chromatography were developed for estimation of nebivolol hydrochloride in tablet dosage form. For the HPLC method, Lichrospher 100 C-18, 5 µm column consisting of 200x4.6 mm i.d. in isocratic mode, with mobile phase containing 50 mM KH 2 PO 4 buffer (pH 3.0±0.1:acetonitrile: (45:55 v/v was used. The flow rate was 1.0 ml/min and effluent was monitored at 282 nm. The retention time was found to be 3.76±0.02 min. For the high performance thin layer chromatographic method a Camag system comprising of Linnomat V automatic sample applicator, Hamilton syringe, Camag TLC Scanner-3, Camag Win CAT software with stationary phase precoated silica gel 60F 254 and mobile phase consisting of ethyl acetate:toluene:methanol: ammonium hydroxide (1:6:2:0.1 v/v/v/v were used. The detection of spot was carried out at 282 nm. The R f value was found to be 0.33±0.02. The methods were validated in terms of linearity, accuracy and precision. The linearity curves were found to be linear over 10-150 µg/ml for high performance thin layer chromatography and 100-600 ng/spot for high performance thin layer chromatography. The limit of detection and limit of quantification for high performance thin layer chromatography were found to be 2.0 and 10 µg/ml, respectively, and for the high performance thin layer chromatography, 30 and 100 ng/spot, respectively. The proposed methods were successfully used for estimation of nebivolol hydrochloride in tablet dosage form.

  15. A simple colorimetric method for estimation of tramadol hydrochloride in pure and tablet dosage forms

    Directory of Open Access Journals (Sweden)

    Scaria P Thomas

    2016-01-01

    Full Text Available Objective: The objective of this study was to develop and validate a simple method for estimation of tramadol hydrochloride (TH in pure and pharmaceutical dosage forms using a colorimeter. Materials and Methods: TH on reaction with Eriochrome Black T in the presence of acetate buffer at pH 3.5 forms a colored complex. This complex was extracted with a fixed volume of chloroform. The optical density of this colored complex was measured against reagent blank using a colorimeter at 520 nm. Results: Beer′s law was obeyed with a good correlation coefficient (0.999 in the concentration range of 2.5 μg/ml to 10 μg/ml. Drug content estimation and recovery studies carried out on commercial tablet dosage forms demonstrated the accuracy of the method and that excipients do not cause interference. Precision and robustness were measured and found to be acceptable (% relative standard deviation <2%. Conclusion: The proposed method can be used for the rapid determination of TH content in tablets at a health-care provider level using already available staff and equipment.

  16. Design and development of controlled porosity osmotic tablet of diltiazem hydrochloride

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    Sadhana R Shahi

    2012-01-01

    Full Text Available The present work aims towards the design and development of extended release formulation of freely water-soluble drug diltiazem hydrochloride (DLTZ based on osmotic technology by using controlled porosity approach. DLTZ is an ideal candidate for a zero-order drug delivery system because it is freely water-soluble and has a short half-life (2-3 h. Sodium chloride (Osmogen was added to the core tablet to alter the solubility of DLTZ in an aqueous medium. Cellulose acetate (CA and sorbitol were used as semipermeable membrane and pore former, respectively. The effect of different formulation variables namely concentration of osmogen in the core tablet, % pore former, % weight gain, pH of the dissolution medium and agitation intensity on the in vitro release was studied. DLTZ release was directly proportional to % pore former and inversely proportional to % weight gain. The optimized formulation (F8 delivered DLTZ independent of pH and agitation intensity for 12 h at the upper level concentration of % pore former (25% w/w and middle level concentration of % weight gain (6% w/w. The comparative study of elementary osmotic pump (EOP and controlled porosity osmotic pump revealed that it superior than conventional EOP and also easier and cost effective to formulate.

  17. Development and validation of simultaneous spectrophotometric methods for drotaverine hydrochloride and aceclofenac from tablet dosage form

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    S A Shah

    2011-01-01

    Full Text Available Two simple spectrophotometric methods have been developed for simultaneous estimation of drotaverine hydrochloride and aceclofenac from tablet dosage form. Method I is a simultaneous equation method (Vierodt′s method, wavelengths selected are 306.5 and 276 nm. Method II is the absorbance ratio method (Q-Analysis, which employs 298.5 nm as λ1 and 276 nm as λ2 (λmax of AF for formation of equations. Both the methods were found to be linear between the range of 8-32 μg/ml for drotaverine and 10-40 μg/ml for aceclofenac. The accuracy and precision were determined and found to comply with ICH guidelines. Both the methods showed good reproducibility and recovery with % RSD in the desired range. The methods were found to be rapid, specific, precise and accurate and can be successfully applied for the routine analysis of drotaverine and aceclofenac in their combined tablet dosage form.

  18. FORMULATION AND IN-VITRO EVALUATION OF TRAMADOL HYDROCHLORIDE FLOATING TABLETS

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    Narendra Palla

    2013-04-01

    Full Text Available Tramadol hydrochloride is a synthetic opioid used as a centrally acting analgesic and effective in both experimental and clinical pain. The half-life of the drug is about 5.5 hours and oral dose is 50 to 100 mg every 4 to 6 hours. To reduce the frequency of administration and to improve patient compliance, a sustained-release formulation of tramadol is desirable. The directly compressible floating tablets of Tramadol HCl were formulated using varying amounts of carbopol-934, HPMC K100M, and Hibiscus rosa-sinensis polymers along with other requisite excipients. Sodium bicarbonate was incorporated as a gas-generating agent. The concentration of the polymers increased gradually to attain the optimised formulation. In-vitro drug release profile and floatational characteristics of the formulations were determined. The studies indicated successful formulation of gastroretentive compressed matrices with excellent sustained release and hydrodynamic balance. From FTIR studies no interaction was found between the Tramadol HCl and polymers. Comparison of the dissolution profiles of the optimized formulation, with optimal composition of HPMC: Hibiscus rosa sinensis; 100:100, with that of marketed formulation indicated analogy of drug release performance with each other. The optimized formulation F10 was found to exhibit first–order kinetics which shows the diffusion along with polymer relaxation and polymer erosion of drug from the tablet.

  19. Formulation And Evaluation Of Bilayer Tablet for Bimodal Release of Venlafaxine Hydrochloride

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    Munira eMomin

    2015-07-01

    Full Text Available The aim of the present research was to develop a bilayer tablet of venlafexine hydrochloride for bimodal drug release. In the present investigation authors have tried to explore Fenugreek Mucilage (FNM for bioadhesive sustained release layer. The attempt has been made to combine FNM with well studied bioahesive polymers like Hydroxy Propyl Methyl Cellulose, Carbopol and Xanthan Gum. The formulations were evaluated for swelling Index, ex-vivo bioadhesion, water uptake studies, in-vitro drug release and dissolution kinetics was studied. Substantial bioadhesion force (2.4±0.023 gms and tablet adhesion retention time (24±2 hrs was observed with FNM and HPMC combination at 80:20 ratio. The dissolution kinetics followed the Higuchi model (R2 =0.9913 via a non-Fickian diffusion controlled release mechanism after the initial burst. The 32 full factorial design was employed in the present study. The type of polymers used in combination with FNM (X1 and percent polymer replaced with FNM (X2 were taken as independent formulations variables. The selected responses, bioadhesion force (0.11-0.25±0.023gm, amount of drug released in 10 h, Y10 (78.20–95.78±1.24 % and bioadhesive strength, (19-24±2hrs presented good correlation with the selected independent variables. Statistical analysis (ANOVA of the optimized bilayer formulations showed no significant difference in the cumulative amount of drug release after 15 min, but significant difference (p < 0.05 in the amount of drug released after 1 hr till 12 h from optimized formulations was observed. The natural mucilage like FNM could be successfully incorporated into tablet with only 20% replacement with HPMC and it showed good bioadhesiveness and sustained drug release.

  20. [Simultaneous determination of five cold medicine ingredients in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets by pH/organic solvent double-gradient high performance liquid chromatography].

    Science.gov (United States)

    Xuan, Xueyi; Huang, Lina; Pan, Xiaoling; Li, Ning

    2013-02-01

    A pH/organic solvent double-gradient mode in reversed-phase high performance liquid chromatography (HPLC) has been established as a new approach to the simultaneous determination of acetaminophen, caffeine, salicylamide, pseudoephedrine hydrochloride and triprolidine hydrochloride in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets. Through the optimization of the organic solvent gradient mode and pH/organic solvent double-gradient mode, the optimum double-gradient HPLC system of the five cold medicine ingredients has been built. The determination was carried out on a Diamonsiol C18 column (250 mm x 4.6 mm, 5 microm). The mobile phase consisted of methanol, 0.05 mol/L ammonium acetate solution and 0.08 mol/L acetic acid solution. The column temperature was set at 30 degrees C. The flow rate was 1.0 mL/min. The sample was measured at multiple wavelengths: 0-6 min, 280 nm; 6-7 min, 257 nm; 7-14 min, 280 nm; 14 min, 233 nm. The separation of the five cold medicine ingredients in the tablets was achieved in 25.5 min. The linear ranges of acetaminophen, pseudoephedrine hydrochloride, caffeine, salicylamide and triprolidine hydrochloride were 0.055 -0.998 g/L, 0.053-0.946 g/L, 0.007-0.129 g/L, 0.035-0.622 g/L and 0.002-0.039 g/L, respectively, with their correlation coefficients greater than 0.999 0. The detection limits (S/N = 3) were 0.09, 6, 0.02, 0.128 and 0.02 mg/L, respectively. Their mean recoveries were 97.9%-102.8%. The advantage of the method is the simultaneous determination of acidic, neutral and basic compounds. It also can improve the column efficiency of the analyte, compress the half-peak width and reduce the trailing. The optimized and validated method can be used for the simultaneous determination of the five cold medicine ingredients in the tablets.

  1. Formulation and dissolution kinetics study of hydrophilic matrix tablets with tramadol hydrochloride and different co-processed dry binders.

    Science.gov (United States)

    Komersová, Alena; Lochař, Václav; Myslíková, Kateřina; Mužíková, Jitka; Bartoš, Martin

    2016-12-01

    The aim of this study is to present the possibility of using of co-processed dry binders for formulation of matrix tablets with drug controlled release. Hydrophilic matrix tablets with tramadol hydrochloride, hypromellose and different co-processed dry binders were prepared by direct compression method. Hypromelloses Methocel™ K4M Premium CR or Methocel™ K100M Premium CR were used as controlled release agents and Prosolv® SMCC 90 or Disintequik™ MCC 25 were used as co-processed dry binders. Homogeneity of the tablets was evaluated using scanning electron microscopy and energy dispersive X-ray microanalysis. The release of tramadol hydrochloride from prepared formulations was studied by dissolution test method. The dissolution profiles obtained were evaluated by non-linear regression analysis, release rate constants and other kinetic parameters were determined. It was found that matrix tablets based on Prosolv® SMCC 90 and Methocel™ Premium CR cannot control the tramadol release effectively for >12h and tablets containing Disintequik™ MCC 25 and Methocel™ Premium CR >8h. Copyright © 2016 Elsevier B.V. All rights reserved.

  2. Development and Evaluation of Sustained Release Tablet of Betahistine Hydrochloride Using Ion Exchange Resin Tulsion T344

    OpenAIRE

    Wagh, Vijay D.; Pawar, Nilesh

    2012-01-01

    An attempt was made to sustain the release of Betahistine hydrochloride by complexation technique using strong cation-exchange resin, Tulsion T344. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, swelling time, ratio of drug : resin, and temperature. The resinate was evaluated for micromeritic properties and characterized using XRPD and IR. For resinate sustained release tablets were formulated using hydoxypropyl methylcellulose K100M. The tab...

  3. Comparative bioequivalence studies of tramadol hydrochloride sustained-release 200 mg tablets

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    Suhas S Khandave

    2010-11-01

    Full Text Available Suhas S Khandave1, Satish V Sawant1, Santosh S Joshi1, Yatish K Bansal2, Sonal S Kadam21Accutest Research Laboratories (I Private Limited, Koparkhirne, Navi Mumbai, Maharashtra, India; 2Ipca Laboratories Limited, Kandivli Mumbai, Maharashtra, IndiaBackground: Tramadol hydrochloride is available as 50 mg immediate-release (IR and 100 mg, 200 mg, and 300 mg sustained-release (SR tablets. The recommended dose of tramadol is 50–100 mg IR tablets every 4–6 hours. The tramadol SR 200 mg tablet is a better therapeutic option, with a reduced frequency of dosing, and improved patient compliance and quality of life. The present study evaluated the bioequivalence of a generic tramadol SR 200 mg tablet.Methods: A comparative in vitro dissolution study was performed on the test and reference products, followed by two separate single-dose bioequivalence studies under fasting and fed conditions and one multiple-dose bioequivalence study under fasting conditions. These bioequivalence studies were conducted in healthy human subjects using an open-label, randomized, two-treatment, two-period, two-sequence, crossover design. The oral administration of the test and reference products was done on day 1 for both the single-dose studies and on days 1–5 for the multiple-dose study in each study period as per the randomization code. Serial blood samples were collected at predefined time points in all the studies. Analysis of plasma concentrations of tramadol and O-desmethyltramadol (the M1 metabolite was done by a validated liquid chromatography-mass spectrometry analytical method. The standard acceptance criterion of bioequivalence was applied on log-transformed pharmacokinetic parameters for tramadol and its M1 metabolite.Results: The ratios for geometric least-square means and 90% confidence intervals were within the acceptance range of 80%–125% for log-transformed primary pharmacokinetic parameters for tramadol and its M1 metabolite in all the three studies

  4. SIMULTANEOUS ESTIMATION AND VALIDATION OF PARACETAMOL, CHLORPHENIRAMINE MALEATE AND PHENYLEPHRINE HYDROCHLORIDE IN BULK AND TABLET DOSAGE FORM BY USING DIFFERENT SPECTROPHOTOMETRIC METHOD

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    Hapse Sandip Appasaheb

    2013-10-01

    Full Text Available A simple, precise, accurate and economic simultaneous UV spectrophotometric method has been developed for the estimation of Paracetamol, Chlorpheniramine Maleate and Phenylephrine Hydrochloride in combination in bulk mixture and tablet. The estimation was based upon measurement of absorbance at absorbance maxima of 258 nm, 262 nm and 239 nm for Paracetamol, Chlorpheniramine Maleate and Phenylephrine Hydrochloride in methanol, respectively in bulk mixture and tablet. The Beer Lambert's law obeyed in the concentration range 4-24 μg/ml, for Paracetamol, Chlorpheniramine Maleate and Phenylephrine Hydrochloride respectively. The estimation of bulk mixture and tablet was carried out by simultaneous equation, Q-analysis and area under curve method for estimation of Paracetamol, Chlorpheniramine Maleate and Phenylephrine Hydrochloride. Recovery study was performed to confirm the accuracy of the methods. The methods were validated as per ICH guidelines.

  5. 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 (100 mg 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.

  6. Formulation and evaluation of taste mask pellets of granisetron hydrochloride as oro dispersible tablet

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    Nilesh Choudhary

    2015-09-01

    Full Text Available Orally disintegrating systems have carved a niche amongst the oral drug delivery systems due to the highest compliance of the patients, especially the geriatrics and pediatrics. In addition, patients suffering from dysphagia, motion sickness, repeated emesis and mental disorders prefer these medications because they cannot swallow large quantity of water. Further, drugs exhibiting satisfactory absorption from the oral mucosa or intended for immediate pharmacological action can be advantageously formulated in these dosage forms. However, the requirements of formulating these dosage forms with mechanical strength sufficient to withstand the rigors of handling and capable of disintegrating within a few seconds on contact with saliva are inextricable. The purpose of this research was to mask the bitter taste of granisetron hydrochloride. To mask the taste Kollicoat(r Smartseal 30D was used as coating polymer for pellet coating. The coated pellets of the drug was directly compressed with different superdisintegrant as AC-Di-Sol, Explotab and Kollidon CL in different concentration 5.0-7.5% w/w into an ODT. The prepared tablets were evaluated for hardness, friability, weight variation, wetting time, wet absorption ratio, in-vitro disintegration time and in vitro dissolution studies. Tablets exhibited quick disintegration characteristics with Kollidon CL in concentration 7.5% w/w i.e., within 20 seconds, which is characteristic of orally disintegrating dosage forms. More than 98% of drug was released from the formulations within 15 minutes. Formulations subjected to stability testing as per the ICH guidelines for 3 months, indicated stability with no change in taste, hardness, drug content, disintegration time and dissolution profiles. Thus, the results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated dosage forms in the oral cavity.

  7. Development and evaluation of buccoadhesive propranolol hydrochloride tablet formulations: effect of fillers.

    Science.gov (United States)

    Akbari, Jafar; Nokhodchi, Ali; Farid, Djavad; Adrangui, Massoud; Siahi-Shadbad, Mohammad Reza; Saeedi, Majid

    2004-02-01

    The buccal mucosa has been investigated for local and systemic delivery of therapeutic peptides and other drugs that are subjected to first-pass metabolism or are unstable within the rest of the gastrointestinal tract. Propranolol hydrochloride (propranolol HCl) is subjected to first-pass effect, therefore formulation of buccal-adhesive dosage form can circumvent this effect. The effect of lactose (a soluble excipient) and dicalcium phosphate (DCP) (an insoluble excipient) on dissolution rate, kinetic of release and adhesion force of buccal-adhesive tablets of propranolol HCl were evaluated. Each tablet composed of 80 mg propranolol HCl, 80 mg hydroxypropylmethylcellulose (HPMC) K4M, polycarbophil AA1 and lactose or DCP with different ratios. The results showed that the presence of the fillers increased dissolution rate of the drug. The release data also showed that the effect of lactose on the dissolution rate was greater than the DCP. Kinetic release of propranolol HCl from buccal-adhesive matrices was affected by the different ratios of polymers and fillers. The fillers reduced the bioadhesion force and this effect was more considerable in formulation containing DCP. In order to determine the mode of release, the data were analyzed based on the equation Q =kt(n). The results showed that an increase in the concentration of HPMC K4M resulted in a reduction in the value of n. The value of n was not significantly affected by an increase in the concentration of lactose or DCP. The values of n in this study were calculated to be between 0.461 and 0.619, indicating both diffusional release and erosional mechanism.

  8. Highly sensitive and selective spectrophotometric and spectrofluorimetric methods for the determination of ropinirole hydrochloride in tablets

    Science.gov (United States)

    Aydoğmuş, Zeynep

    2008-06-01

    Three sensitive, selective, accurate spectrophotometric and spectrofluorimetric methods have been developed for the determination of ropinirole hydrochloride in tablets. The first method was based on measuring the absorbance of drug solution in methanol at 250 nm. The Beer's law was obeyed in the concentration range 2.5-24 μg ml -1. The second method was based on the charge transfer reaction of drug, as n-electron donor with 7,7,8,8-tetracyanoquinodimethane (TCNQ), as π-acceptor in acetonitrile to give radical anions that are measured at 842 nm. The Beer's law was obeyed in the concentration range 0.6-8 μg ml -1. The third method was based on derivatization reaction with 4-chloro-7-nitrobenzofurazan (NBD-Cl) in borate buffer of pH 8.5 followed by measuring the fluorescence intensity at 525 nm with excitation at 464 nm in chloroform. Beer's law was obeyed in the concentration range 0.01-1.3 μg ml -1. The derivatization reaction product of drug with NBD-Cl was characterized by IR, 1H NMR and mass spectroscopy. The developed methods were validated. The following analytical parameters were investigated: the molar absorptivity ( ɛ), limit of detection (LOD, μg ml -1) and limit of quantitation (LOQ, μg ml -1), precision, accuracy, recovery, and Sandell's sensitivity. Selectivity was validated by subjecting stock solution of ropinirole to acidic, basic, oxidative, and thermal degradation. No interference was observed from common excipients present in formulations. The proposed methods were successfully applied for determination of drug in tablets. The results of these proposed methods were compared with each other statistically.

  9. 盐酸利托君片在中国健康人体的生物等效性%Bioequivalence of ritodrine hydrochloride tablets in Chinese healthy volunteers

    Institute of Scientific and Technical Information of China (English)

    张佳丽; 吴华; 潘世芬; 王鹤尧

    2012-01-01

    目的 评价2种国产盐酸利托君片在中国健康人体的生物等效性.方法 22名健康女性受试者随机交叉单剂量口服盐酸利托君片试验药物或对照药物,各10 mg.用高效液相色谱-串联质谱法测定血浆中盐酸利托君浓度;用DAS2.0软件计算药代动力学参数,并对2种药物进行生物等效性评价.结果 试验药物和对照药物的主要药代动力学参数:Cmax分别为(5.71±1.83)和(5.61±2.03)ng·mL-1;Tmax分别为(0.54±0.45)和(0.46 ±0.24) h;t1/2分别为(3.64±3.99)和(4.25±4.02)h;AUC0-t分别为(12.31±5.20)和(12.01±5.42)h·ng·mL-1.AUC0-t、AUC0-∞、Cmax的90%可信区间分别为95.8%~111.6%、92.3% ~ 118.9%和95.4% ~ 108.2%.试验药物相对于对照药物的生物利用度F为(105.3±19.96)%.结论 试验药物和对照药物生物等效.%Objective To evaluate the bioequivalence of two preparations of ritodrine hydrochloride tablets. Methods A single oral dose of 10 mg test and reference ritodrine hydrochloride tablets were given to 22 female healthy volunteers in a randomized crossover study. The concentrations of ritodrine hydrochloride were determined by HPLC - MS /MS method. The pharmacokinetic paramters and relative bioavailability were calculated by DAS 2. 0 software, then the bioequivalence was judged. Results The main pharmacokinetic parameters of two preparations were as follows; CmaXwere (5.71 ±1.83), (5.61 ±2.03) ng · mL-1, Tmax were (0. 54 ±0. 45), (0. 46 ±0. 24) h, t1/2were(3. 64 ±3. 99), (4. 25 ±4.02) h, AUC0_t were(12. 31 ±5.20), (12.01 ±5.42) h · ng · mL -1, respectively. The relative bioavailability of test tablets was (105. 3 ± 19. 96) % . The 90% Cis for the ratios of AUC0_t, Cmax were 95. 8% - 111. 6% , 95.4% - 108. 2% , respectively. Conclusion The results demonstrated that the two preparations were bioequivalent.

  10. Development and evaluation of modified release wax matrix tablet dosage form for tramadol hydrochloride

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    Paresh Ramesh Mahaparale

    2015-01-01

    Full Text Available The objective of this study was to develop modified release dosage forms of tramadol hydrochloride using wax matrix system by melt granulation method. The effect of various waxes, concentration of waxes, effect of excipients on the release profile of drug from wax matrix system was studied. Release retardant effect was observed in the order of hydrogenated vegetable oil (HVO > compritol >precirol. This may be due to more lipophilicity imparted by HVO than any other waxy substances. It was also observed that as ratio of drug: Wax was increased, it sustained release of drug for more time. This may be due to proper embedment/entrapment of drug in sufficient wax matrix system. In case of excipients, release retardant effect was found in order of dicalcium phosphate (DCP > microcrystalline cellulose (MCC > lactose. DCP is insoluble which helps in release retardation of drug. MCC is hydrophilic swellable polymer which showed release of drug by swelling. Lactose is soluble excipient which get dissolved and formed channels for entry of dissolution medium and release of drug occurred by erosion mechanism. Wax matrix tablets were found to be stable.

  11. Derivative emission spectrofluorimetry for the simultaneous determination of guaifenesin and phenylephrine hydrochloride in pharmaceutical tablets.

    Science.gov (United States)

    Maher, Hadir M; Alshehri, Mona M; Al-taweel, Shorog M

    2015-05-01

    Rapid, simple and sensitive derivative emission spectrofluorimetric methods have been developed for the simultaneous analysis of binary mixtures of guaifenesin (GUA) and phenylephrine hydrochloride (PHE). The methods are based upon measurement of the native fluorescence intensity of the two drugs at λex = 275 nm in methanolic solutions, followed by differentiation using first (D1) and second (D2) derivative techniques. The derivative fluorescence intensity-concentration plots were rectilinear over a range of 0.1-2 µg/mL for both GUA and PHE. The limits of detection were 0.027 (D1, GUA), 0.025 (D2, GUA), 0.031 (D1, PHE) and 0.033 (D2, PHE) µg/mL and limits of quantitation were 0.089 (D1, GUA), 0.083 (D2, GUA), 0.095 (D1, PHE) and 0.097 (D2, PHE) µg/mL. The proposed derivative emission spectrofluorimetric methods (D1 and D2) were successfully applied for the determination of the two compounds in binary mixtures and tablets with high precision and accuracy. The proposed methods were fully validated as per ICH guidelines. Copyright © 2014 John Wiley & Sons, Ltd.

  12. Preparation and evaluation of microencapsulated fast melt tablets of ambroxol hydrochloride

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    Jacob S

    2009-01-01

    Full Text Available Natural resources in general and plant materials in particular are receiving more attention due to their safety as pharmaceutical excipients. Present work assessed the potential of a natural polysaccharide, pectin to mask the bitter taste of ambroxol hydrochloride, by microencapsulation technique, and its possibility to formulate as a fast disintegrating dosage form. Taste masking is an important developmental challenge in fast dissolving drug delivery system since it dissolves or disintegrates in the patient′s mouth in close proximity to the taste buds. The prepared microspheres by emulsion solvent evaporation technique possessed good sphericity, smooth surface morphology, uniform and narrow size distribution (10-90 μm, when analyzed by scanning electron microscopy, laser diffraction and optical microscopy. Method of preparation has influenced the particle size and drug loading efficiency. Drug-polymer compatibility was confirmed by Fourier transform infrared spectroscopy and thin layer chromatography. DSC and X-ray diffraction studies revealed that the drug was dispersed inside the microspheres in the form of an insoluble matrix. The formation of microspheres was affected by glass transition temperature of the polymer, surfactant, type of plasticizers, volume of internal phase, stirrer speed etc. Fast dissolving tablets were prepared by the modification of melt granulation technique. The resulting granules were found to melt fast at body temperature, have smooth mouth feel and good physical stability. This study demonstrated that pectin could be a right choice in developing patient favored formulations for bitter drugs and can be utilized in fast disintegrating dosage forms as well.

  13. RP-HPLC analytical method development and optimization for quantification of donepezil hydrochloride in orally disintegrating tablet.

    Science.gov (United States)

    Liew, Kai Bin; Peh, Kok Khiang; Fung Tan, Yvonne Tze

    2013-09-01

    An easy, fast and validated RV-HPLC method was invented to quantify donepezil hydrochloride in drug solution and orally disintegrating tablet. The separation was carried out using reversed phase C-18 column (Agilent Eclipse Plus C-18) with UV detection at 268 nm. Method optimization was tested using various composition of organic solvent. The mobile phase comprised of phosphate buffer (0.01M), methanol and acetonitrile (50:30:20, v/v) adjusted to pH 2.7 with phosphoric acid (80%) was found as the optimum mobile phase. The method showed intraday precision and accuracy in the range of 0.24% to -1.83% and -1.83% to 1.99% respectively, while interday precision and accuracy ranged between 1.41% to 1.81% and 0.11% to 1.90% respectively. The standard calibration curve was linear from 0.125 μg/mL to 16 μg/mL, with correlation coefficient of 0.9997±0.00016. The drug solution was stable under room temperature at least for 6 hours. System suitability studies were done. The average plate count was > 2000, tailing factor method was used to assay donepezil hydrochloride in tablet and dissolution study of in-house manufactured donepezil orally disintegrating tablet and original Aricept.

  14. DEVELOPMENT AND VALIDATION OF UV SPECTROSCOPIC METHOD FOR THE DETERMINATION OF METFORMIN HYDROCHLORIDE IN TABLET DOSAGE FORM

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    Reatul Karim et al

    2012-09-01

    Full Text Available A simple, economic, sensitive, precise and accurate UV spectrophotometric method was developed and validated for quantification of Metformin hydrochloride in bulk and in tablet dosage form. Adequate drug solubility and maximum assay sensitivity was found in 0.01N sodium hydroxide at 233nm. Calibration graph constructed at 233nm was linear in concentration range of 1-25μg/ml with correlation coefficient of 0.9998. The method was validated as per ICH guidelines in terms of linearity (within 1-25µg/ml, accuracy (% recovery, precision (inter-day and intraday, specificity and robustness. The limit of detection (LOD and limit of quantification (LOQ were found to be 0.2226µg/ml and 0.6745µg/ml respectively. Therefore, the proposed method is suitable and can be adopted for the determination of Metformin hydrochloride from pharmaceutical dosage form in routine quality control analysis.

  15. Development of alternative methods for the determination of raloxifene hydrochloride in tablet dosage form

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    Fernanda Rodrigues Salazar

    2015-06-01

    Full Text Available Three methods are proposed for the quantitative determination of raloxifene hydrochloride in pharmaceutical dosage form: ultraviolet method (UV high performance liquid chromatography (HPLC and micellar capillary electrophoresis (MEKC. These methods were developed and validated and showed good linearity, precision and accuracy. Also they demonstrated to be specific and robust. The HPLC and MEKC methods were tested in regards to be stability indicating methods and they showed to have this attribute. The UV method used methanol as solvent and optimal wavelength at 284 nm, obeying Lambert-Beer law in these conditions. The chromatographic conditions for the HPLC method included: NST column C18 (250 x 4.6 mm x 5 µm, mobile phase water:acetonitrile:triethylamine (67:33:0,3 v/v, pH 3.5, flow rate 1.0 mL min-1, injection volume 20.0 µl, UV detection 287 nm and analysis temperature 30 °C. The MEKC method was performed on a fused-silica capillary (40 cm effective length x 50 µm i.d. using as background electrolyte 35.0 mmol L-1 borate buffer and 50.0 mmol L-1 anionic detergent sodium dodecyl sulfate (SDS at pH 8.8. The capillary temperature was 32°C, applied voltage 25 kV, UV detection at 280 nm and injection was perfomed at 45 mBar for 4 s, hydrodimanic mode. In this MEKC method, potassium diclofenac (200.0 µg mL-1 was used as internal standard. All these methods were statistically analyzed and demonstrated to be equivalent for quantitative analysis of RLX in tablets and were successfully applied for the determination of the drug.

  16. Determination of ivabradine hydrochloride in Ivabradine Hydrochloride Tablets by HPLC%HPLC法测定盐酸伊伐布雷定片含量

    Institute of Scientific and Technical Information of China (English)

    杨晓莉; 张琼; 李辉

    2012-01-01

    Objective To establish an HPLC method for the determination of ivabradine hydrochloride in Ivabradine Hydrochloride Tablets. Methods The column C18 Inertsil ODS-3(250 mm ×4. 6 mm,5 μm) was used. The mobile phase consisted of buffer phos-phate(pH7. 6)- acetonitrile(60 : 40) ,flow rate was 1. 0 mL o min-1 ,the detection wavelength was set at 286 nm,and the column temperature was 25 ℃. Results The linearity of peak area was good when the sample content was in the range of 2. 32-16. 25 μg(r= 0. 999 9). The average recovery was 101. 3% with RSD 1. 2%(n = 9). Conclusions The method is accurate,reliable and simple,and it can be used in the determination of ivabradine hydrochloride in Ivabradine Hydrochloride Tablets.%目的 建立HPLC法测定盐酸伊伐布雷定片的含量.方法 采用C18 Inertsil ODS-3(250 mm ×4.6 mm,5 μm)色谱柱,流动相为磷酸盐缓冲液(pH7.6)-乙腈(60∶40),流速为1.0 mL·min-1,检测波长为286 nm,柱温25 ℃.结果 盐酸伊伐布雷定线性范围为2.32~16.25 μg,峰面积与进样量线性关系良好(r=0.999 9);平均回收率为101.3%,其RSD为1.2% (n=9).结论 该方法准确、可靠、简便,适用于盐酸伊伐布雷定片的含量测定.

  17. ABSORPTION RATIO METHOD FOR ESTIMATION OF DROTAVERINE HYDROCHLORIDE AND MEFENAMIC ACID IN THEIR COMBINED TABLET DOSAGE FORM

    OpenAIRE

    Sakhare Ram Suresh; Jamkhande Prasad Govindrao

    2012-01-01

    A new, simple, accurate and sensitive UV-spectrophotometric absorption Ratio method has been developed for simultaneous determination of Drotaverine Hydrochloride and Mefenamic Acid in their combined Tablet dosage form. The method is based upon determination of Drotaverine HCl and Mefenamic Acid at 239 nm, and 280nm in Methanol. Drotaverine HCl and Mefenamic Acid at isoabsorptive λmax 239 nm and at 280 nm λmax Mefenamic acid shows linearity in the concentration range of 3-30 μg/ml and 3 -30...

  18. ABSORPTION RATIO METHOD FOR ESTIMATION OF DROTAVERINE HYDROCHLORIDE AND MEFENAMIC ACID IN THEIR COMBINED TABLET DOSAGE FORM

    Directory of Open Access Journals (Sweden)

    Sakhare Ram Suresh

    2012-10-01

    Full Text Available A new, simple, accurate and sensitive UV-spectrophotometric absorption Ratio method has been developed for simultaneous determination of Drotaverine Hydrochloride and Mefenamic Acid in their combined Tablet dosage form. The method is based upon determination of Drotaverine HCl and Mefenamic Acid at 239 nm, and 280nm in Methanol. Drotaverine HCl and Mefenamic Acid at isoabsorptive λmax 239 nm and at 280 nm λmax Mefenamic acid shows linearity in the concentration range of 3-30 μg/ml and 3 -30 μg/ml respectively. The method was validated statistically.

  19. Some variables affecting the characteristics of Eudragit E-sodium alginate polyelectrolyte complex as a tablet matrix for diltiazem hydrochloride.

    Science.gov (United States)

    Yusif, Rehab Mohammad; Abu Hashim, Irhan Ibrahim; El-Dahan, Marwa Salah

    2014-03-01

    Eudragit E (EE)-sodium alginate (SA) polyelectrolyte complexes (PECs) were prepared at pH 4 and 5.8 using sodium alginate of high (SAH) and low viscosity (SAL). The optimum EE-SA complexation mass ratio was determined using viscosity measurements. Interactions between EE and SA in PECs were characterized by Fourier transform infra-red spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Diltiazem hydrochloride (DTZ HCl) tablets were prepared using the prepared EE-SA PECs and their physical mixtures at different ratios as matrices. Tablets were evaluated for swelling characteristics and in vitro drug release. Tablets containing EE-SAH physical mixtures of ratios (1.5:1 and 1:3) as matrices were effective in achieving sustained release of DTZ HCl, where the percent drug released was significantly (p < 0.05) decreased compared to that from tablets either containing the same ratios of EE-SAL physical mixtures or the preformed EE- -SAH and EE-SAL PECs.

  20. Evaluation of dissolution of propranolol hydrochloride tablets%国产盐酸普萘洛尔片溶出评价

    Institute of Scientific and Technical Information of China (English)

    刘海涛; 王俊秋; 余立; 周立春

    2011-01-01

    OBJECTIVE To compare the in vitro dissolution of propranolol hydrochloride tablets from different pharmaceutical factories for giving references of clinical application of propranolol hydrochloride tablets. METHODS The dissolution test was carried out with paddle-rotating method. The content of propranolol hydrochloride was determined by UV spectrophotome-try. The accumulative dissolution percentage was calculated. The similarity factor and the Weibull equation were used to evaluate the dissolution results. RESULTS The dissolution of propranolol hydrochloride tablets from 21 manufactories conformed to the requirements of Chinese Pharmacopoeia(2010 edition). But significant differences were found among propranolol hydrochloride tablets dissolution behaviour. CONCLUSION There was significant difference in dissolution parameters among the propranolol hydrochloride tablets preparations from different manufactories,which should be given attention in clinical application.%目的:考察国内21个厂家生产的盐酸普萘洛尔片的体外溶出度,为提高药品内在质量和临床用药提供参考.方法:采用桨法进行体外溶出度试验,以紫外分光光度法测定盐酸普萘洛尔的含量,计算累积溶出百分率;使用相似因子法和威布尔方程法对结果进行分析和评价.结果:21个厂家盐酸普萘洛尔片的体外溶出度均符合中国药典2010年版中的相关规定,但各厂家产品溶出行为差别较大,产品质量存在差异.结论:不同厂家盐酸普萘洛尔片的溶出参数存在差异,临床用药时应加以注意.

  1. Formulation and evaluation of a sustained-release tablets of metformin hydrochloride using hydrophilic synthetic and hydrophobic natural polymers

    Directory of Open Access Journals (Sweden)

    K J Wadher

    2011-01-01

    Full Text Available Metformin hydrochloride has relatively short plasma half-life, low absolute bioavailability. The need for the administration two to three times a day when larger doses are required can decrease patient compliance. Sustained release formulation that would maintain plasma level for 8-12 h might be sufficient for daily dosing of metformin. Sustained release products are needed for metformin to prolong its duration of action and to improve patient compliances. The overall objective of this study was to develop an oral sustained release metformin hydrochloride tablet by using hydrophilic Eudragit RSPO alone or its combination with hydrophobic natural polymers Gum copal and gum damar as rate controlling factor. The tablets were prepared by wet granulation method. The in vitro dissolution study was carried out using USP 22 apparatus I, paddle method and the data was analysed using zero order, first order, Higuchi, Korsmeyer and Hixson-Crowell equations. The drug release study revealed that Eudragit RSPO alone was unable to sustain the drug release. Combining Eudragit with gum Copal and gum Damar sustained the drug release for more than 12 h. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism of drug release.

  2. Development and validation of a HPTLC method for estimation of duloxetine hydrochloride in bulk drug and in tablet dosage form

    Directory of Open Access Journals (Sweden)

    Dhaneshwar Suneela

    2008-01-01

    Full Text Available Duloxetine hydrochloride is a potent dual reuptake inhibitor of serotonin and norepinephrine used to treat major depressive disorders. The present work describes a simple, precise and accurate HPTLC method for its estimation as bulk and in tablet dosage form. The chromatographic separation was carried out on precoated silica gel 60 F254 aluminium plates using mixture of chloroform:methanol (8:1 v/v as mobile phase and densitometric evaluation of spots was carried out at 235 nm using Camag TLC Scanner-3 with win CAT 1.3.4 version software. The experimental parameters like band size of the spot applied, chamber saturation time, solvent front migration, slit width etc. were critically studied and optimum conditions were evolved. The drug was satisfactorily resolved with Rf value 0.11±0.01. The accuracy and reliability of the proposed method was ascertained by evaluating various validation parameters like linearity (40-200 ng/spot, precision (intra-day RSD 0.46-0.75%, inter-day RSD 0.46-1.59%, accuracy (98.72±0.20 and specificity according to ICH guidelines. The proposed method can analyse ten or more formulation units simultaneously on a single plate and provides a faster and cost-effective quality control tool for routine analysis of duloxetine hydrochloride as bulk drug and in tablet formulation.

  3. Formulation and evaluation of a sustained-release tablets of metformin hydrochloride using hydrophilic synthetic and hydrophobic natural polymers.

    Science.gov (United States)

    Wadher, K J; Kakde, R B; Umekar, M J

    2011-03-01

    Metformin hydrochloride has relatively short plasma half-life, low absolute bioavailability. The need for the administration two to three times a day when larger doses are required can decrease patient compliance. Sustained release formulation that would maintain plasma level for 8-12 h might be sufficient for daily dosing of metformin. Sustained release products are needed for metformin to prolong its duration of action and to improve patient compliances. The overall objective of this study was to develop an oral sustained release metformin hydrochloride tablet by using hydrophilic Eudragit RSPO alone or its combination with hydrophobic natural polymers Gum copal and gum damar as rate controlling factor. The tablets were prepared by wet granulation method. The in vitro dissolution study was carried out using USP 22 apparatus I, paddle method and the data was analysed using zero order, first order, Higuchi, Korsmeyer and Hixson-Crowell equations. The drug release study revealed that Eudragit RSPO alone was unable to sustain the drug release. Combining Eudragit with gum Copal and gum Damar sustained the drug release for more than 12 h. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism of drug release.

  4. FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF RANITIDINE HYDROCHLORIDE USING DIFFERENT SUPERDISINTEGRANT

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    Sharma Dharmendra

    2011-10-01

    Full Text Available Ranitidine HCl is an H2 anhistaminic drug mainly used for treatment of peptic ulcers and is absorbed 50% orally. The drug undergoes hepatic metabolism, so the attempt has been made to administer it as fast dissolving tablet to increases its oral bioavailability. The tablets were prepared by using sublimation method using ammonium bicarbonate as sublimating agent. The tablets were evaluated for hardness, wetting time, dispersion time, disintegrating time. The other tablets prepared by using sodium starch glycolate and cross carmellose sodium as superdisintegrant. It was concluded that the tablets prepared by super disintergrant addition have better disintegrating properties and release profile when compared to the tablets prepared by sublimation method.

  5. Development of a new benazepril hydrochloride chewable tablet and evaluation of its bioequivalence for treatment of heart failure in dogs.

    Science.gov (United States)

    Qian, M; Chen, T; Zhou, D; Zhang, Z; Zhang, Q; Tang, S; Xiao, X

    2016-02-01

    The aim of the study was to develop a new chewable benazepril hydrochloride(BH) tablet, investigate its physical properties, and evaluate its bioequivalence with the branded formulation (Fortekor). A corrective agent was included in the formula to improve its palatability and convenience for administration to dogs. The tablet remained stable in light, heat, and humidity tests, and its physical properties such as hardness, uniformity of content, and dissolution rate were highly consistent with the technical standards. After single and repeated administrations to eight beagles and single dose to 14 mongrel dogs (0.5 mg/kg p.o.), plasma BH and its active metabolite, benazeprilat (BZ), were detected. There was no significant difference in the major pharmacokinetic parameters (Cmax , Tmax, and AUC₀₋₂₄) between the two formulations. The 90% confidence intervals calculated for the ratios of area under the time-concentration curve (AUC₀₋₂₄) were 92.4-116.3% for BH and 89.9-102.3% for BZ, within the accepted range for bioequivalence of 80-125%. The results showed our new chewable tablet is bioequivalent to the commercial product and suitable for addition to the benazepril product family for the treatment of heart failure in dogs.

  6. Generic sustained release tablets of trimetazidine hydrochloride: Preparation and in vitro–in vivo correlation studies

    Directory of Open Access Journals (Sweden)

    Longmei Wang

    2016-06-01

    Full Text Available The aim of the current work was to develop generic sustained-release tablets containing 35 mg trimetazidine dihydrochloride and to establish an in vitro–in vivo correlation that could predict the bioavailability. The marketed sustained release tablet (Vastarel MR used as reference, a sustained-release matrix tablet was prepared using hydroxypropyl methylcellulose (HPMC as matrix by wet granulation and the in vitro dissolution profiles of the self-made tablets were determined in four different dissolution media (0.1 M HCl, pH 4.5 PBS, pH 6.8 PBS and water. A higher similarity between prepared tablets and Vastarel MR was established, with similarity factor (f2 ranging from 60 to 75 in the four media. The in vivo pharmacokinetics was studied in six healthy beagles. Compared with Vastarel MR, the Cmax of self-made tablets was slightly decreased, while the Tmax and MRT0–t were slightly prolonged, but with no significant difference (P > 0.05. The average of relative bioavailability (F was 102.52% based on AUC0–t. For log-transformed AUC0–t and Cmax, the upper confidence limit on the appropriate criterion is <0, indicating these two formulations were population bioequivalent. The in vivo–in vitro correlation coefficient obtained from point-to-point analysis of self-made tablets was 0.9720. In conclusion, the prepared tablets were bioequivalent to the marketed tablets, according to both the in vitro release rate and extent of absorption, and a good in vivo–in vitro correlation was established for the self-made tablets that indicated in vitro dissolution tests could be used as a surrogate for bioavailability studies.

  7. Novel spectrophotometric method for determination of cinacalcet hydrochloride in its tablets via derivatization with 1,2-naphthoquinone-4-sulphonate

    Science.gov (United States)

    2012-01-01

    This study represents the first report on the development of a novel spectrophotometric method for determination of cinacalcet hydrochloride (CIN) in its tablet dosage forms. Studies were carried out to investigate the reaction between CIN and 1,2-naphthoquinone-4-sulphonate (NQS) reagent. In alkaline medium (pH 8.5), an orange red-colored product exhibiting maximum absorption peak (λmax) at 490 nm was produced. The stoichiometry and kinetic of the reaction were investigated and the reaction mechanism was postulated. This color-developing reaction was employed in the development of a simple and rapid visible-spectrophotometric method for determination of CIN in its tablets. Under the optimized reaction conditions, Beer's law correlating the absorbance with CIN concentration was obeyed in the range of 3 - 100 μg/ml with good correlation coefficient (0.9993). The molar absorptivity (ε) was 4.2 × 105 l/mol/cm. The limits of detection and quantification were 1.9 and 5.7 μg/ml, respectively. The precision of the method was satisfactory; the values of relative standard deviations (RSD) did not exceed 2%. No interference was observed from the excipients that are present in the tablets. The proposed method was applied successfully for the determination of CIN in its pharmaceutical tablets with good accuracy and precisions; the label claim percentage was 100.80 - 102.23 ± 1.27 - 1.62%. The results were compared favorably with those of a reference pre-validated method. The method is practical and valuable in terms of its routine application in quality control laboratories. PMID:22305461

  8. Novel spectrophotometric method for determination of cinacalcet hydrochloride in its tablets via derivatization with 1,2-naphthoquinone-4-sulphonate

    Directory of Open Access Journals (Sweden)

    Darwish Ibrahim A

    2012-02-01

    Full Text Available Abstract This study represents the first report on the development of a novel spectrophotometric method for determination of cinacalcet hydrochloride (CIN in its tablet dosage forms. Studies were carried out to investigate the reaction between CIN and 1,2-naphthoquinone-4-sulphonate (NQS reagent. In alkaline medium (pH 8.5, an orange red-colored product exhibiting maximum absorption peak (λmax at 490 nm was produced. The stoichiometry and kinetic of the reaction were investigated and the reaction mechanism was postulated. This color-developing reaction was employed in the development of a simple and rapid visible-spectrophotometric method for determination of CIN in its tablets. Under the optimized reaction conditions, Beer's law correlating the absorbance with CIN concentration was obeyed in the range of 3 - 100 μg/ml with good correlation coefficient (0.9993. The molar absorptivity (ε was 4.2 × 105 l/mol/cm. The limits of detection and quantification were 1.9 and 5.7 μg/ml, respectively. The precision of the method was satisfactory; the values of relative standard deviations (RSD did not exceed 2%. No interference was observed from the excipients that are present in the tablets. The proposed method was applied successfully for the determination of CIN in its pharmaceutical tablets with good accuracy and precisions; the label claim percentage was 100.80 - 102.23 ± 1.27 - 1.62%. The results were compared favorably with those of a reference pre-validated method. The method is practical and valuable in terms of its routine application in quality control laboratories.

  9. Cathodic adsorptive stripping voltammetry of drotaverine hydrochloride and its determination in tablets and human urine by differential pulse voltammetry.

    Science.gov (United States)

    Zayed, S I M; Issa, Y M

    2009-04-01

    The stripping voltammetric behaviour of drotaverine hydrochloride (DvCl) was studied using a hanging mercury drop electrode (HMDE). The adsorptive stripping response has been evaluated with respect to pH, accumulation time, accumulation potential, scan rate and other variables. Differential pulse DP mode; over the potential range -400 to -1200 mV, is used in the presence of 0.04 M Britton-Robinson buffer pH 2. Cyclic voltammetric study indicates that the reduction process is irreversible and controlled by adsorption. The response of DP technique is linear over the concentration range 21.70-257.34 ng/ml. Limit of detection and limit of quantification were 3.15 and 10.50 ng/ml, respectively. The proposed method was successfully applied for the determination of the drug in commercial tablets and spiked human urine samples.

  10. Clinical application of OxyContin hydrochloride controlled release tablets in treatment of pain suffered from advanced cancer

    Institute of Scientific and Technical Information of China (English)

    Wenwu Wang; Xuenong OuYang; Zongyang Yu; Zhangshu Chen

    2012-01-01

    Objective: The aim of this study was to evaluate the efficacy and adverse reactions of OxyContin hydrochloride controlled release tablets in the treatment of moderate or severe pain in patients with terminal cancer and to observe any improvement on the cancer patients' quality of life. Methods: Sixty-eight patients with moderate or severe cancer pain were treated with OxyContin hydrochloride controlled release tablets. The initial dose was 5 mg/12h, or 1/2 that of the standard morphine regimen. During the course of treatment, the dosage was adjusted according to the patients' condition until the pain completely disappeared or nearly did so. Each patient received a treatment for at least 15 days. At the same time, adverse reactions, the quality of life and scores for the intensity of pain were observed and recorded [1]. Results: The final titrated dosage of OxyContin was as follows: the patients in 30 cases (44.1%) received a dosage of ≤ 30 mg/d, those in 16 cases (23.5%) received a dosage of 31 to 60 mg/d, those in 18 cases (26.5%) received a dosage of 61 to 120 mg/d and those in 4 cases (5.9%) received a dosage of ≥ 120 mg/d. The overall rate of relief from pain was 95.6%, among which the rates of excellent, effective and moderate relief were respectively 39.7%, 48.5% and 7.4%. OxyContin had mild adverse reactions and patients' quality of life was markedly improved. Conclusion: OxyContin is effective in treatment of moderate and severe cancer pain. The adverse reactions of OxyContin are mild, and the drug can significantly improve the quality of life of patients with cancer pain.

  11. Simultaneous determination of salbutamol sulphate and bromhexine hydrochloride in tablets by reverse phase liquid chromatography

    Directory of Open Access Journals (Sweden)

    Pai P. N. S.

    2009-01-01

    Full Text Available A simple reverse phase liquid chromatographic method has been developed and subsequently validated for simultaneous determination of salbutamol sulphate and bromhexine hydrochloride. The separation was carried out using a mobile phase consisting of acetonitrile, methanol and phosphate buffer, pH 4 in the ratio 60:20:20 v/v. The column used was SS Wakosil-II C-18 with a flow rate of 1 ml/min and UV detection at 224 nm. The described method was linear over a concentration range of 10-110 µg/ml and 20-140 µg/ml for the assay of salbutamol sulphate and bromhexine hydrochloride, respectively. The mean recovery was found to be 95-105% for salbutamol sulphate and 96.2-102.1% for bromhexine hydrochloride when determined at five different levels.

  12. Formulation and evaluation of sustained release matrix tablets of pioglitazone hydrochloride using processed Aloe vera mucilage as release modifier

    Directory of Open Access Journals (Sweden)

    Manoj Choudhary

    2015-01-01

    Full Text Available Background: Natural gums and mucilage which hydrates and swells on contact with aqueous media are used as additives in the formulation of hydrophilic drug delivery system. Aim: The purpose of this study was to develop a new monolithic matrix system for complete delivery of Pioglitazone hydrochloride (HCl, in a zero-order manner over an extended time period using processed Aloe vera gel mucilage (PAG as a release modifier. Materials and Methods: The matrices were prepared by dry blending of selected ratios of polymer and ingredients using direct compression technique. Physicochemical properties of dried powdered mucilage of A. vera were studied. Various formulations of pioglitazone HCl and A. vera mucilage were prepared using different drug: Polymer ratios viz., 1:1, 1:2, 1:3, 1:4, 1:5 for PAG by direct compression technique. Results: The formulated matrix tablets were found to have better uniformity of weight and drug content with low statistical deviation. The swelling behavior and in vitro release rate characteristics were also studied. Conclusion: The study proved that the dried A. vera mucilage can be used as a matrix forming material for controlled release of Pioglitazone HCl matrix tablets.

  13. In vitro-in vivo evaluation of fast-dissolving tablets containing solid dispersion of pioglitazone hydrochloride

    Directory of Open Access Journals (Sweden)

    Vinay Pandit

    2012-01-01

    Full Text Available Investigation of in vitro/in vivo behavior of fast-dissolving tablets containing solid dispersions of pioglitazone hydrochloride (PIO is the focus of the present research work. The effect of various hydrophilic polymers on the aqueous solubility of PIO was studied. Poly vinyl pyrrolidine K 30 (PVPK 30 carrier was selected and solid dispersions were prepared by various methods. Evaluation of solid dispersion for percentage yield, drug content, solubility, and Fourier Transform Infrared-indicated kneading method was most appropriate. Furthermore, the dissolution studies exhibited an enhancement in drug dissolution. One-way ANOVA of in vitro data suggested that there was significant (P ≤ 0.05 difference in dissolution profile of PIO solid dispersion when compared with pure drug and commercial product. Infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction performed on solid dispersion indicated lack of physicochemical interaction between the drug and the carrier. The selected formulation is compressed into fast-dissolving tablets which were further evaluated for tablet properties and in vitro drug release. In vivo studies of pure drug, selected formulation, and marketed product were carried out in male Wistar rats and pharmacokinetic parameters were calculated using Kinetica software 2000. The best formulation has shown T max of 1 hour which was highly significant (P < 0.01 when compared with pure drug and marketed formulation. Therefore, the solid dispersions prepared by kneading method using PVPK 30 as hydrophilic carrier can be successfully used for improvement of dissolution of PIO and resulted in faster onset of action as indicated by in vivo studies.

  14. In vitro release kinetics and bioavailability of gastroretentive cinnarizine hydrochloride tablet.

    Science.gov (United States)

    Nagarwal, Ramesh C; Ridhurkar, Devendra N; Pandit, J K

    2010-03-01

    An oral sustained release dosage form of cinnarizine HCl (CNZ) based on gastric floating matrix tablets was studied. The release of CNZ from different floating matrix formulations containing four viscosity grades of hydroxypropyl methylcellulose, sodium alginate or polyethylene oxide, and gas-forming agent (sodium bicarbonate or calcium carbonate) was studied in simulated gastric fluid (pH 1.2). CNZ release data from the matrix tablets were analyzed kinetically using Higuchi, Peppas, Weibull, and Vergnaud models. From water uptake, matrix erosion studies, and drug release data, the overall release mechanism can be explained as a result of rapid hydration of polymer on the surface of the floating tablet and formation of a gel layer surrounding the matrix that controls water penetration into its center. On the basis of in vitro release data, batch HP1 (CNZ, HPMC-K100LV, SBC, LTS, and MgS) was subjected to bioavailability studies in rabbits and was compared with CNZ suspension. It was concluded that the greater bioavailability of HP1 was due to its longer retention in the gastric environment of the test animal. Batch no. HP1 of floating tablet in rabbits demonstrated that the floating tablet CNZ could be a 24-h sustained release formulation.

  15. Formulation and in vitro evaluation of floating tablets of hydroxypropyl methylcellulose and polyethylene oxide using ranitidine hydrochloride as a model drug.

    Science.gov (United States)

    Gharti, Kp; Thapa, P; Budhathoki, U; Bhargava, A

    2012-10-01

    The present study was carried out with an objective of preparation and in vitro evaluation of floating tablets of hydroxypropyl methyl cellulose (HPMC) and polyethylene oxide (PEO) using ranitidine hydrochloride as a model drug. The floating tablets were based on effervescent approach using sodium bicarbonate a gas generating agent. The tablets were prepared by dry granulation method. The effect of polymers concentration and viscosity grades of HPMC on drug release profile was evaluated. The effect of sodium bicarbonate and stearic acid on drug release profile and floating properties were also investigated. The result of in vitro dissolution study showed that the drug release profile could be sustained by increasing the concentration of HPMC K15MCR and Polyox WSR303. The formulation containing HPMC K15MCR and Polyox WSR303 at the concentration of 13.88% showed 91.2% drug release at the end of 24 hours. Changing the viscosity grade of HPMC from K15MCR to K100MCR had no significant effect on drug release profile. Sodium bicarbonate and stearic acid in combination showed no significant effect on drug release profile. The formulations containing sodium bicarbonate 20 mg per tablet showed desired buoyancy (floating lag time of about 2 minutes and total floating time of >24 hours). The present study shows that polymers like HPMC K15MCR and Polyox WSR303 in combination with sodium bicarbonate as a gas generating agent can be used to develop sustained release floating tablets of ranitidine hydrochloride.

  16. Spectrophotometric estimation of ambroxol and cetirizine hydrochloride from tablet dosage form.

    Science.gov (United States)

    Gowekar, N M; Pande, V V; Kasture, A V; Tekade, A R; Chandorkar, J G

    2007-07-01

    Fixed dose combination tablets containing ambroxol HCl and cetirizine HCl are clinically used as mucolytic and antiallergic. Several spectrophotometric and HPLC methods have been reported for simultaneous estimation of these drugs with other drugs. The drugs individually and in mixture obeys Beer's law over conc. range 1.2-4.4 microg/mL for cetirizine HCL and for ambroxol HCL 15-52 microg/mL at all five sampling wavelengths (correlation coeff. well above 0.995). The mean recoveries from tablet by standard addition method were 100.18% (+/-2.4) and 100.66 % (+/-2.31). The present work reports simple, accurate and precise spectrophotometric methods for their simultaneous estimation from tablet dosage form.

  17. Pharmacokinetics and effect of food after oral administration of prolonged-release tablets of ropinirole hydrochloride in Japanese patients with Parkinson's disease.

    Science.gov (United States)

    Hattori, N; Hasegawa, K; Sakamoto, T

    2012-10-01

    Ropinirole hydrochloride, a dopamine receptor agonist with a non-ergot alkaloid structure, is highly selective for the dopamine D(2) /D(3) receptors. This study was conducted to evaluate the steady-state pharmacokinetics, safety and efficacy after repeated oral administration of prolonged-release tablets of ropinirole hydrochloride in the absence of L-dopa preparations in Japanese patients with Parkinson's disease (PD). This was a multicenter, open-label, uncontrolled study. The total duration of participation in the study ranged from 56 to 63 weeks. In the study, the plasma concentrations of ropinirole, its major metabolite SK&F104557 (N-depropyl ropinirole) and another metabolite SK&F89124 (ropinirole hydroxylated at the seventh position of the indole ring) were assessed. Safety based on adverse events, haematology, biochemistry, urinalysis and electrocardiography (ECG) (standard 12-lead ECG) were evaluated, and vital signs (blood pressure/pulse rate) were measured. Efficacy based on the Japanese version of Unified Parkinson's Disease Rating Scale (UPDRS) Parts III (motor) and II [activities of daily living (ADL)] as well as tolerability was evaluated. After repeated oral administration of prolonged-release tablets of ropinirole hydrochloride in Japanese patients with PD, ropinirole, SK&F104557 and low levels of SK&F89124 were detected in plasma. The trough concentrations of ropinirole and the two metabolites increased in proportion to the dose when ropinirole hydrochloride prolonged-release tablets were administered at doses ranging from 2 to 16 mg/day. The plasma exposure to ropinirole and its two metabolites after intake of normal diet was comparable to that in the fasting state. The most common adverse events (10% or more) were somnolence, nausea, constipation, hallucination and nasopharyngitis. Most adverse events were mild or moderate in severity, and with no death. During the treatment period, serious adverse events were reported in five patients. Efficacy

  18. Simultaneous Determination of Sitagliptin Phosphate Monohydrate and Metformin Hydrochloride in Tablets by a Validated UPLC Method.

    Science.gov (United States)

    Malleswararao, Chellu S N; Suryanarayana, Mulukutla V; Mukkanti, Khagga

    2012-01-01

    A novel approach was used to develop and validate a rapid, specific, accurate and precise reverse phase ultra performance liquid chromatographic (UPLC) method for the simultaneous determination of Sitagliptin phosphate monohydrate and Metformin hydrochloride in pharmaceutical dosage forms. The chromatographic separation was achieved on Aquity UPLC BEH C8 100 × 2.1 mm, 1.7 μm, column using a buffer consisting of 10 mM potassium dihydrogen phosphate and 2 mM hexane-1-sulfonic acid sodium salt (pH adjusted to 5.50 with diluted phosphoric acid) and acetonitrile as organic solvent in a gradient program. The flow rate was 0.2 mL min(-1) and the detection wavelength was 210 nm. The limit of detection (LOD) for Sitagliptin phosphate monohydrate and Metformin hydrochloride was 0.2 and 0.06 μg mL(-1), respectively. The limit of quantification (LOQ) for Sitagliptin phosphate monohydrate and Metformin hydrochloride was 0.7 and 0.2 μg mL(-1), respectively. This method was validated with respect to linearity, accuracy, precision, specificity and robustness. The method was also found to be stability-indicating.

  19. 21 CFR 520.2345h - Tetracycline hydrochloride, sodium novobiocin, and prednisolone tablets.

    Science.gov (United States)

    2010-04-01

    ... or one triple-strength tablet for each 18 pounds) every 12 hours for 48 hours. Treatment is to be... longer as needed. (2) Indications for use. Treatment of acute and chronic canine respiratory infections such as tonsillitis, bronchitis, and tracheobronchitis when caused by pathogens susceptible to...

  20. 21 CFR 520.2345g - Tetracycline hydrochloride and sodium novobiocin tablets.

    Science.gov (United States)

    2010-04-01

    ... tablet for each 18 pounds). (2) Indications for use. Treatment of acute or chronic canine respiratory infections such as tonsillitis, bronchitis, and tracheobronchitis when caused by pathogens susceptible to... treatment for at least 48 hours after the temperature has returned to normal and all evidence of infection...

  1. 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...

  2. 75 FR 14444 - Determination That DIDREX (Benzphetamine Hydrochloride) Tablets, 25 Milligrams, Were Not...

    Science.gov (United States)

    2010-03-25

    ... the Drug Price Competition and Patent Term Restoration Act of 1984 (Public Law 98-417) (the 1984... the Drug Efficacy Study Implementation, FDA concluded that benzphetamine HCl 25-mg tablets are... products that have been discontinued from marketing for reasons other than safety or effectiveness....

  3. Design and in vitro/in vivo evaluation of sustained-release floating tablets of itopride hydrochloride

    Directory of Open Access Journals (Sweden)

    Ahmed SM

    2016-12-01

    Full Text Available Sayed M Ahmed,1 Adel Ahmed Ali,2 Ahmed MA Ali,2,3 Omiya A Hassan2,4 1Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, 2Department of Pharmaceutics, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt; 3Department of Pharmaceutics, Faculty of Pharmacy, Taif University, Taif, Kingdom of Saudi Arabia; 4Department of Pharmaceutics, Faculty of Pharmacy, Deraya University, El-Minia Gadida, Egypt Purpose: The aim of the present study was to improve the bioavailability of itopride (ITO and sustain its action by formulating as a floating dosage form. Materials and methods: Sustained-release floating tablets of ITO hydrochloride (HCl were prepared by direct compression using different hydrocolloid polymers such as hydroxypropyl methylcellulose and ethylcellulose and/or methacrylic acid polymers Eudragit RSPM and Carbopol 934P. The floating property was achieved using an effervescent mixture of sodium bicarbonate and anhydrous citric acid (1:1 mol/mol. Hardness, friability, content uniformity, and dissolution rate of the prepared floating tablets were evaluated. The formulation F10 composed of 28.5% Eudragit RSPM, 3% NaHCO3, and 7% citric acid provided sustained drug release. Results: In vitro results showed sustained release of F10 where the drug release percentage was 96.51%±1.75% after 24 hours (P=0.031.The pharmacokinetic results indicated that the area under the curve (AUC0–∞ of the prepared sustained-release floating tablets at infinity achieved 93.69 µg·h/mL compared to 49.89 µg·h/mL for the reference formulation (Ganaton® and the relative bioavailability of the sustained-release formulation F10 increased to 187.80% (P=0.022. Conclusion: The prepared floating tablets of ITO HCl (F10 could be a promising drug delivery system with sustained-release action and enhanced drug bioavailability. Keywords: itopride HCl, oral drug delivery, stability study, bioavailability

  4. Formulation design and optimization of taste-masked mouth-dissolving tablets of Tramadol hydrochloride

    Directory of Open Access Journals (Sweden)

    Patel K

    2010-01-01

    Full Text Available The aim of the present study was to mask the extremely bitter taste of Tramadol HCL, an opioid analgesic, and to formulate a tablet which can rapidly disintegrate in saliva (rapidly disintegrating tablet. The crucial aspect in the formulation of mouth-dissolving tablets is to mask the bitter taste and to minimize the disintegration time. Taste masking was done using sweetening agent and D-mannitol and taste-masked pellets were prepared by extrusion spheronization technique. Prepared pellets were tested for drug content, taste evaluation in oral cavity and molecular property. Pellet shows significant taste masking, confirmed by in vitro taste evaluation; therefore, it was selected for further study. Pellets were evaluated for density, angle of repose, Carr′s index, Hausner′s ratio and sphericity while tablets were evaluated for disintegration and in vitro dissolution. A 3 2 full factorial design and statistical models were applied to optimize the effect of two factors, i.e. superdisintegrant sodium starch glycolate and taste-masking agent (D-mannitol. In this study, response surface methodology was used for designing of the experiment, generation of mathematical models and optimization study. Taste evaluation of pellets in human volunteers revealed considerable taste masking with a degree of bitterness below threshold value (2.0 within 10 s, whereas Tramadol HCl was rated intensely bitter with a score of +4 for 10 s. The size of the pellets varied from 0.895 to 1.423 mm for different batch and found to be a spherical. Disintegration time of different formulations varied from 30 to 60 s. It was observed that the responses, i.e. disintegration time and sphericity were affected by both the factors. The statistical models were validated and can be successfully used to prepare optimized taste-masked mouth-dissolving tablets of Tramadol HCl with adequate disintegration and shape.

  5. A multicentric, open label, randomised, postmarketing efficacy study comparing multidose of lincomycin hydrochloride capsule 500 mg with multidose cefpodoxime proxetil tablet 200 mg in patients with tonsillitis, sinusitis.

    Science.gov (United States)

    Kothadiya, Ajay

    2012-08-01

    Tonsillitis causes considerable short and medium term morbidity, and can be recurrent. Sinusitis can be acute (less than 4 weeks), subacute (4-8 weeks) or chronic (8 weeks or more). To study the comparative efficacy and safety of multidose treatments of lincomycin hydrochloride 500 mg capsules against cefpodoxime proxetil 200 mg tablets on its outcome in the Indian scenario are the aims and objective of the study. A total of 41 tonsillitis, sinusitis cases of either gender aged above 18 years were enrolled in the study. The diagnosis of sonsillitis, sinusitis was made based on examination of symptoms and throat swab. A randomised treatment of either lincomycin hydrochloride 500 mg capsules or cefpodoxime proxetil 200 mg tablets twice daily for five days alongwith other concomitant medications depending on related symptoms was given to 40 patients. At the end of study, all patients were re-evaluated and the response rate was assessed. The most common clinical symptoms were body temperature, headache, throat pain, postnasal discharge, mucopus, odynophagia, sinus tenderness, nasal congestion, pharyngeal congestion and tonsillar congestion. The overall response rate of lincomycin hydrochloride in all the symptoms except headache was more effective than cefpodoxime proxetil. Out of 100% (n = 20) patients in each group, 67.89% in lincomycin and 52.27% in cefpodoxime patients achieved complete relief, in all the clinical symptoms. The study suggests that lincomycin hydrochloride capsules, a conventional antibiotic indicates effective treatment for relief from tonsillitis and sinusitis, as compared to new third generation antibiotic.

  6. Development and validation of a reversed-phase HPLC method for simultaneous estimation of ambroxol hydrochloride and azithromycin in tablet dosage form.

    Science.gov (United States)

    Shaikh, K A; Patil, S D; Devkhile, A B

    2008-12-15

    A simple, precise and accurate reversed-phase liquid chromatographic method has been developed for the simultaneous estimation of ambroxol hydrochloride and azithromycin in tablet formulations. The chromatographic separation was achieved on a Xterra RP18 (250 mm x 4.6 mm, 5 microm) analytical column. A Mixture of acetonitrile-dipotassium phosphate (30 mM) (50:50, v/v) (pH 9.0) was used as the mobile phase, at a flow rate of 1.7 ml/min and detector wavelength at 215 nm. The retention time of ambroxol and azithromycin was found to be 5.0 and 11.5 min, respectively. The validation of the proposed method was carried out for specificity, linearity, accuracy, precision, limit of detection, limit of quantitation and robustness. The linear dynamic ranges were from 30-180 to 250-1500 microg/ml for ambroxol hydrochloride and azithromycin, respectively. The percentage recovery obtained for ambroxol hydrochloride and azithromycin were 99.40 and 99.90%, respectively. Limit of detection and quantification for azithromycin were 0.8 and 2.3 microg/ml, for ambroxol hydrochloride 0.004 and 0.01 microg/ml, respectively. The developed method can be used for routine quality control analysis of titled drugs in combination in tablet formulation.

  7. PREPARATION AND IN VITRO AND IN VIVO EVALUATION OF BUCCOADHESIVE BILAYERED TABLETS OF DILTIAZEM HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    D’souza A

    2012-08-01

    Full Text Available In this study buccoadhesive bilayered tablets of Diltiazem HCl (DTZ were prepared in order to improve the bioavailability by the avoidance of hepatic first-pass metabolism, and to prevent frequent administration. Bilayered Tablets containing fixed amount of Diltiazem HCl (DTZ were prepared by direct compression method using polymers like hydroxyl propyl methyl cellulose (HPMC K4M, HPMC K15M, HPMC K100M in combination with backing layer of ethyl cellulose and evaluated for physicochemical properties, swelling, bioadhesive strength, in vitro permeation studies, in vitro drug release and possible interaction between ingredients. The physicochemical properties, swelling index, surface pH, bioadhesive strength, in vitro drug release and in vitro permeation studies were found to be dependent on the grade and proportion of buccoadhesive material used. The dissolution of Diltiazem HCl from all the prepared tablets into phosphate buffer (pH 6.8 was controlled for 6 hrs and followed non-Fickian release mechanism. Lower release rates were observed for formulations containing higher concentration of higher viscosity grade of HPMC. FTIR and DSC studies revealed the absence of significant interaction between DTZ and the selected bioadhesive materials. In vivo studies of selected formulation in rabbits demonstrated significant enhancement in bioavailability of DTZ relative to orally administered drug.

  8. A stability-indicating high performance liquid chromatographic assay for the simultaneous determination of atenolol and lercanidipine hydrochloride in tablets

    Directory of Open Access Journals (Sweden)

    H O Kaila

    2011-01-01

    Full Text Available A simple, rapid, precise and accurate isocratic reversed phase stability indicating HPLC method was developed and validated for the simultaneous determination of atenolol and lercanidipine hydrochloride in commercial tablets. The chromatographic separation was achieved on phenomenex Gemini C18 (250×4.6 mm, 5 μm column using a mobile phase consisting of acetonitrile and buffer (20 mM potassium dihydrogen phosphate pH 3.5 in the ratio of (55:45, v/v at a flow rate of 1.0 ml/min and UV detection at 235 nm. The linearity of the proposed method was investigated in the range of 40-160 μg/ml (r 2 =0.9995 for atenolol and 8-32 μg/ml (r 2 =0.9993 for lercanidipine. Degradation products produced as a result of stress studies did not interfere with the detection of atenolol and lercanidipine and the assay can thus be considered stability-indicating.

  9. Development and validation of a rapid RP-UPLC method for the simultaneous estimation of bambuterol hydrochloride and montelukast sodium from tablets

    Directory of Open Access Journals (Sweden)

    R Yanamandra

    2012-01-01

    Full Text Available A rapid, simple, sensitive and selective analytical method was developed by using reverse phase ultra performance liquid chromatographic technique for the simultaneous estimation of bambuterol hydrochloride and montelukast sodium in combined tablet dosage form. The developed method is superior in technology to conventional high performance liquid chromatography with respect to speed, resolution, solvent consumption, time, and cost of analysis. Elution time for the separation was 6 min and ultra violet detection was carried out at 210 nm. Efficient separation was achieved on BEH C18 sub-2-μm Acquity UPLC column using 0.025% (v/v trifluoro acetic acid in water and acetonitrile as organic solvent in a linear gradient program. Resolutions between bambuterol hydrochloride and montelukast sodium were found to be more than 31. The active pharmaceutical ingredient was extracted from tablet dosage from using a mixture of methanol, acetonitrile and water as diluent. The calibration graphs were linear for bambuterol hydrochloride and montelukast sodium in the range of 6.25-37.5 μg/ml. The percentage recoveries for bambuterol hydrochloride and montelukast sodium were found to be in the range of 99.1-100.0% and 98.0-101.6%, respectively. The test solution was found to be stable for 7 days when stored in the refrigerator between 2-8Ί. Developed UPLC method was validated as per International Conference on Harmonization specifications for method validation. This method can be successfully employed for simultaneous estimation of bambuterol hydrochloride and montelukast sodium in bulk drugs and formulations.

  10. Comparative bioavailability of two tablet formulations of ranitidine hydrochloride in healthy volunteers.

    Science.gov (United States)

    Bawazir, S A; Gouda, M W; El-Sayed, Y M; Al-Khamis, K I; Al-Yamani, M J; Niazy, E M; Al-Rashood, K A

    1998-05-01

    This investigation was carried out to evaluate the bioavailability of a new tablet formulation of ranitidine HCl (300 mg), Ranid, relative to the reference product, Zantac, (300 mg) tablets. The bioavailability was carried out on 24 healthy male volunteers who received a single dose (300 mg) of the test (T) and the reference (R) products in the fasting state, in a randomized balanced 2-way crossover design. After dosing, serial blood samples were collected for a period of 16 hours. Plasma harvested from blood was analyzed for ranitidine by a sensitive and validated high-performance liquid chromatographic assay. The maximum plasma concentration (Cmax), area under the plasma concentration time curve up to the last measurable concentration (AUC0-t), and to infinity (AUC0-infinity) and the absorption rate (Cmax/AUC0-infinity) were analyzed statistically under the assumption of a multiplicative model. The time to maximum concentration (Tmax) was analyzed assuming an additive model. The parametric confidence intervals (90%) of the mean values of the pharmacokinetic characteristics (AUC0-t, AUC0-infinity), Cmax and Cmax/AUC0-infinity) for T/R ratio were in each case well within the bioequivalence acceptable range of 80-125%. The test formulation was found bioequivalent to the reference formulation by the Schuirmann's two one-sided t-tests and by Wilcoxon Mann Whitney two one-sided tests procedure. Therefore, the 2 formulations were considered to be bioequivalent.

  11. Formulation optimization of hydrodynamically balanced oral controlled release bioadhesive tablets of tramadol hydrochloride.

    Science.gov (United States)

    Singh, Bhupinder; Rani, Ashu; Babita; Ahuja, Naveen; Kapil, Rishi

    2010-01-01

    The directly compressible floating-bioadhesive tablets of tramadol were formulated using varying amounts Carbopol 971P (CP) and hydroxy-propylmethyl cellulose (HPMC), along with other requisite excipients. In vitro drug release profile, floatational characteristics and ex vivo bioadhesive strength using texture analyzer were determined, and systematically optimized using a 3(2) central composite design (CCD). The studies indicated successful formulation of gastroretentive compressed matrices with excellent controlled release, mucoadhesion and hydrodynamic balance. Comparison of the dissolution profiles of the optimized formulation, with optimal composition of CP:HPMC :: 80.0:125.0, with that of the marketed controlled release formulation other indicated analogy of drug release performance with each other. Validation of optimization study using eight confirmatory experimental runs indicated very high degree of prognostic ability of CCD with mean  SEM of â0.06%  0.37. Further, the study successfully unravels the effect of the polymers on the selected response variables.

  12. Fluorescent quantification of terazosin hydrochloride content in human plasma and tablets using second-order calibration based on both parallel factor analysis and alternating penalty trilinear decomposition.

    Science.gov (United States)

    Zou, Hong-Yan; Wu, Hai-Long; OuYang, Li-Qun; Zhang, Yan; Nie, Jin-Fang; Fu, Hai-Yan; Yu, Ru-Qin

    2009-09-14

    Two second-order calibration methods based on the parallel factor analysis (PARAFAC) and the alternating penalty trilinear decomposition (APTLD) method, have been utilized for the direct determination of terazosin hydrochloride (THD) in human plasma samples, coupled with the excitation-emission matrix fluorescence spectroscopy. Meanwhile, the two algorithms combing with the standard addition procedures have been applied for the determination of terazosin hydrochloride in tablets and the results were validated by the high-performance liquid chromatography with fluorescence detection. These second-order calibrations all adequately exploited the second-order advantages. For human plasma samples, the average recoveries by the PARAFAC and APTLD algorithms with the factor number of 2 (N=2) were 100.4+/-2.7% and 99.2+/-2.4%, respectively. The accuracy of two algorithms was also evaluated through elliptical joint confidence region (EJCR) tests and t-test. It was found that both algorithms could give accurate results, and only the performance of APTLD was slightly better than that of PARAFAC. Figures of merit, such as sensitivity (SEN), selectivity (SEL) and limit of detection (LOD) were also calculated to compare the performances of the two strategies. For tablets, the average concentrations of THD in tablet were 63.5 and 63.2 ng mL(-1) by using the PARAFAC and APTLD algorithms, respectively. The accuracy was evaluated by t-test and both algorithms could give accurate results, too.

  13. Programmed delivery of verapamil hydrochloride from tablet in a capsule device

    Directory of Open Access Journals (Sweden)

    Mukesh Lal Sah

    2012-06-01

    Full Text Available The aim of the present work was to develop a programmed drug delivery system which would be able to release the drug after 6 h of lag time by use of hydrophilic polymers. The capsule body was made impermeable by use of formaldehyde vapor treatment, while the cap was untreated. The capsule was filled with two layered tablets (tablet-in-capsule, followed by a sodium bicarbonate:citric acid mixture (SBCM and lactose as bulking agent. Sodium alginate, chitosan, HPMC K15 and chitosan:sodium alginate complex (CSAC were used as the rate modulating layer. Through combined use of HPMC K15 and adjusting the ratio of CSAC, the desired lag time of 6 h was obtained. The effect of the bulking agents on the lag time were also studied and it was found that the lag time was decreased with higher amounts of lactose, and delayed dissolution and decreased lag time was observed at higher amount of effervescent mixture.O objetivo do presente trabalho foi desenvolver sistema de liberação programada de cloridrato de verapamil capaz de liberação imediata do fármaco após 6 h de intervalo de tempo usando polímeros hidrofílicos. O corpo da cápsula foi impermeabilizado por tratamento de vapor de formaldeído, enquanto a tampa não foi submetida ao tratamento. Dois comprimidos foram inseridos na cápsula (comprimidos em cápsula seguido de mistura de bicarbonato de sódio: ácido cítrico e lactose, utilizados como excipientes. O alginato de sódio, a quitosana, o HPMC K15 e o complexo quitosana:alginato de sódio foram utilizados para modular a razão de liberação do fármaco. A combinação entre o HPMC K15 e o ajuste da proporção do complexo quitosana:alginato de sódio permitiu a liberação do fármaco após 6 h. O efeito dos excipientes na liberação do fármaco foi também avaliado. Verificou-se que o tempo de latência foi reduzido na presença de maior quantidade de lactose, enquanto o menor tempo foi observado empregando maior concentração da

  14. 两种盐酸特拉唑嗪片的人体生物等效性研究%Bioequivalence study on two terazosin hydrochloride tablets

    Institute of Scientific and Technical Information of China (English)

    朱蕾蕾; 苏淑芳; 蒋健; 郭丽霞; 詹燕; 裘福荣; 赵彤芳; 叶宇婕; 元唯安; 李安平; 李明花

    2015-01-01

    Objective To evaluate the bioequivalence of domestic and imported terazosin hydrochloride tablets after single oral dose .Methods It was a single center ,randomized ,open ,cross-over trail design ,21 subjects were fasting oral adminis-tered of 2 mg domestic and imported terazosin hydrochloride tablets in different periods ,venous blood 4 ml were collected in different time points before and 60 h after administration ,plasma concentration of terazosin was determined by LC-MS/MS . Results The main pharmacokinetic parameters of domestic and imported terazosin hydrochloride tablets were as follows :t1/2 :(13.2± 2.39)hvs(12.5±1.93)h,tmax :(1.01±0.83)hvs(1.08±0.69)h,Cmax :(40.1±10.6)ng/mlvs(37.3± 9 .57) ng/ml;AUC0- ∞ :(428 ± 82 .1) ng · h/ml vs (426 ± 85 .2) ng · h/ml .The relative bioavailability of domestic terazosin hydrochloride tablets was (101 .2 ± 14 .7)% .90% CI of domestic and imported terazosin hydrochloride tablets AUC0-t and Cmax geometric mean ratio fell between 80% -125% .Conclusion The domestic tablets are bioequivalent to the imported tablets .%目的:评价单剂量口服国产和进口盐酸特拉唑嗪片的人体生物等效性。方法采用单中心、随机、开放、双周期交叉试验设计,21名受试者在不同周期分别空腹口服国产和进口盐酸特拉唑嗪片2mg,于给药前0h及给药后60h内不同时间点采集静脉血4 ml ,采用液-质联用(LC-MS/MS)法测定受试者血浆中特拉唑嗪的浓度。结果国产和进口盐酸特拉唑嗪片的 t1/2分别为(13.2±2.39)和(12.5±1.93) h;tmax分别为(1.01±0.83)和(1.08±0.69) h;Cmax分别为(40.1±10.6)和(37.3±9.57) ng/ml;AUC0-∞分别为(428±82.1)和(426±85.2) ng · h/ml。国产盐酸特拉唑嗪片的相对生物利用度为(101.2±14.7)%。国产与进口盐酸特拉唑嗪片 AUC0-t和Cmax几何均值比的90%置信区间(CI)均落在80%~125%之间。结论国产和进口

  15. 盐酸利多卡因口腔黏附片的处方研究%Study on the Formula of Lidocaine Hydrochloride Buccal Adhesive Tablets

    Institute of Scientific and Technical Information of China (English)

    谢向阳; 李旸; 李银科; 李雪梅; 符旭东

    2012-01-01

    Objective: To prepare the lidocaine hydrochloride buccal adhesive tablets. Method: The buccal adhesive tablets were prepared using different proportions of dextrin, carbomer and CMC-Na. The expansion coefficients, adhesive ability, drug release in vitro and adhesive time in oral cavity were investigated. Result: The formula with dextrin and carbomer in the proportion of 23: 16 was optimal. The tablets prepared by the optimal formula could stick the No. 4 steel ball, reached the maximum expansion coefficient in 1h, 97% drug was released in 2 h, and the adhesive time in oral cavity was about 2 h. Conclusion: The formula of lidocaine hydrochloride buccal adhesive tablets is feasible.%目的:研制盐酸利多卡因口腔黏附片.方法:采用不同配比的糊精和卡波姆制备盐酸利多卡因口腔黏附片,考察其体外膨胀率、黏附力、释药性能和口腔滞留时间.结果:以糊精和卡波姆23:16为比例制得的口腔黏附片较符合要求,能粘住4号钢球,1 h达到最大膨胀率,体外释药2 h释放度为97%,在人口腔中约能滞留2 h.结论:盐酸利多卡因口腔黏附片处方是可行的.

  16. 盐酸氨基葡萄糖片高效液相色谱测定方法的改进%Improvement on Determination of Glucosamine Hydrochloride in Glucosamine Hydrochloride Tablets by HPLC

    Institute of Scientific and Technical Information of China (English)

    吴学军; 金鹏飞; 邹定; 姜文清; 胡欣; 孙春华

    2012-01-01

    Objective To improve an HPLC method for the determination of glucosamine hydrochloride in Glucosamine Hydrochloride Tablets. Methods An Alltima C18 column (250 mm × 4. 6 mm, 5 μm) was used for the separation, with 10 mm ammonium dihydrogen phosphate - acetonitrile (95 : 5) as the mobile phase at the flow rate of 0.5 mL/min. The detection wavelength was 194 nm. Results This method showed good linearity with a correlation coefficient (r) of 0.999 5; the specificity study showed satisfactory resolutions between glucosamine hydrochloride, excipients, forced degradation products and common acid radical negative ions; the precisions and stability were satisfactory with all RSDs below 2% ; and the spiked recovery ranged from 99.52% to 101. 2%. Conclusion This method is superior to the standard method, and could be used for the determination of glucosamine hydrochloride in Glucosamine Hydrochloride Tablets.%目的 改进盐酸氨基葡萄糖片的高效液相色谱测定方法.方法 采用AlhimaC18色谱柱(250mm×4.6mm,5μm),以10mmol/L磷酸二氢铵溶液一乙腈(95:5,V/V)为流动相,流速为0.5 mL/min,检测渡长为194nm.结果 改进方法后,盐酸氨基葡萄糖的线性关系良好,r=0.999 5;方法专属性强,盐酸氨基葡萄糖和辅料、降解产物、常见酸根离子之间都有良好分离度;方法精密度和稳定性良好.RSD均小于2%;加样回收率良好,百分回收率在99.52%-101.2%之间.结论 改进后的方法优于国家食品药品监督管理局注册标准中的方法,可作为盐酸氨基葡萄糖片的含量测定方法.

  17. A novel validated RP-HPLC-DAD method for the simultaneous estimation of Metformin Hydrochloride and Canagliflozin in bulk and pharmaceutical tablet dosage form with forced degradation studies

    Directory of Open Access Journals (Sweden)

    Uttam Prasad Panigrahy

    2015-09-01

    Full Text Available A novel approach was used to develop and validate a rapid isocratic Reversed Phase-High Performance Liquid Chromatographic method for the simultaneous estimation of Metformin Hydrochloride and Canagliflozin in bulk and pharmaceutical tablet dosage form with forced degradation studies. The separation was performed by using Kromasil C18 column (250mm×4.6 mm, 5mm particle size, Waters Alliance e2695 HPLC system with 2998 PDA detector and mobile phase contained a mixture of 0.01M Ammonium acetate (pH adjusted to 3.5 with orthophosphoric acid and Acetonitrile (65:35, v/v. The flow rate was set to 1ml/min with responses measured at 254nm. The retention time of Metformin Hydrochloride and Canagliflozin was 2.440min and 3.713min respectively with resolution of 8.95.Linearity was established in the range of 50-300µg/ml for Metformin Hydrochloride and 5-30µg/ml for Canagliflozin with correlation coefficients (r2=0.999. The percentage recoveries were between (99.45%-100.65% and (99.95%-100.74% for Metformin Hydrochloride and Canagliflozin respectively. Validation parameters were evaluated according to the International Conference on Harmonization (ICH Q2 R1 guidelines. The forced degradation studies were performed by using HCl, NaOH, H2O2, thermal, UV radiation and water. Metformin Hydrochloride and Canagliflozin are more sensitive towards oxidative degradation condition. The developed method was successfully applied for the quantification and hyphenated instrumental analysis.

  18. [Initial Evaluation of the Efficacy and Safety of Tablets Containing Trifluridine and Tipiracil Hydrochloride--Safety Measures Devised by a Multidisciplinary Team Including a Pharmaceutical Outpatient Clinic].

    Science.gov (United States)

    Aimono, Yuka; Kamoshida, Toshiro; Sakamoto, Risa; Nemoto, Masahiko; Saito, Yoshiko; Aoyama, Yoshifumi; Maruyama, Tsunehiko

    2015-07-01

    In May 2014, tablets containing both trifluridine and tipiracil hydrochloride (Lonsurf® tablets) were launched in Japan ahead of other countries, for the treatment of advanced/relapsed unresectable colorectal cancer. The benefits of these tablets in terms of a new therapeutic option have been demonstrated. However, the manufacturer has requested healthcare professionals to help develop safety measures for the appropriate and safe use of the tablets. In this study, we evaluated the efficacy and safety of the tablets in 16 patients who received the tablets at our hospital. Among the 4 evaluable patients, none achieved a complete or partial response. One patient (25.0%) had stable disease according to the Response Evaluation Criteria in Solid Tumors (RECIST) Guidelines outlined in the General Rules of the Study of Colorectal Cancer (The 8th Edition). Lonsurf® is considered to be a third-line (or later) treatment. Among the 16 cases studied, Lonsurf® was used as a third-, fourth-, and fifth-line treatment in 9, 6, and 1 cases, respectively. Therefore, Grade 3 or worse toxicities were a potential concern. Despite a high incidence of Grade 3 or worse neutropenia (7 of the 16 patients [43.8%]), none of the patients were hospitalized due to neutropenia or other treatment-related adverse events. Pharmacists have made 126 proposals to physicians regarding the use of Lonsurf®, 121 (96.0%) of which have been adopted. All of the adverse reactions experienced by our patients were resolved after supportive therapy.

  19. 盐酸帕罗西汀缓释片的研制%Preparation of Paroxetine Hydrochloride Sustained-Release Tablets

    Institute of Scientific and Technical Information of China (English)

    胡献跃; 郑一美

    2016-01-01

    目的:制备盐酸帕罗西汀缓释片。方法通过以不同黏度的羟丙基甲基纤维素( HPMC )为阻滞剂,比较试制缓释片与SEROXAT对照片的体外释放曲线,采用 f2相似因子法评价两者溶出曲线的相似度,并对释放行为进行机制拟合。结果确定以HPMC E50和K4M按1:1配比为阻滞剂,制备成的缓释片与上市样品的体外释放曲线基本一致,f2值为77.25,试制片与对照片的体外释放均符合Korsmeyer-reppas方程。结论该处方工艺简单,体外释放与上市对照药高度拟合。%Objective To prepare the Paroxetine Hydrochloride Sustained-Release Tablets. Methods The HPMC of different specifica-tions was used as the blocking agent, the release characteristics of the self-made and SEROXAT reference tablets were compared in vitro, f2 was used to evaluate the similarity of the two dissolution curves, and the mechanism of the release behavior was fitted. Results The sustained-release tablets were made using HPMC E50 and K4M ( 1:1 ) as blocker, and the in vitro release behaviors were basi-cally the same with the reference tablets, the f2 was 77. 25. Both the release curve fitted the Korsmeyer-reppas equation. Conclusion The preparation method of Paroxetine Hydrochloride Sustained-Release Tablets is simple, and its dissolution behavior is highly similar to the reference tablets in the market.

  20. 盐酸氯米帕明口腔崩解片的制备工艺%Preparation Technology of Clomipramine Hydrochloride Orally Disintegrating Tablets

    Institute of Scientific and Technical Information of China (English)

    吴杏梅; 谢燕萍

    2011-01-01

    Objective: To optimize the formulation of clomipramine hydrochloride orally disintegrating tablets by orthogonal experiment and to determine the dissolution. Method: The formulation of the tablets was optimized by orthogonal experiment based on four factors, those were the amount of microcrystalline cellulose, lactose, and sodium carboxymethl starch and the concentration of hydroxypropyl methyl cellulose, and 3 indices, those were disintegrating time (t1,), wetting time (t) and suspending stability (△A). The dissolution of the tablets was determined by HPLC. Result: The optimum preparation technical conditions for the tablets were as follows: the proportions of microcrystalline cellulose,lactose and the sodium carboxymethl starch and the concentration of hydroxypropyl cellulose was 30% ,30% >0. 75% and 1% respectively. The tablets disintegrated completely within 30s with mean td of 13. 2 s,t of 21.6 s,and △A of 0.001 2. Conclusion: The formula of the clomipramine hydrochloride orally disintegrating tablets is reasonable and valuable to be studied further.%目的:采用正交试验筛选盐酸氯米帕明口腔崩解片的处方,并测定其溶出度.方法:以微晶纤维素、乳糖、羧甲基淀粉钠的用量以及羟丙纤维素的浓度为考查因素,以口腔崩解片的崩解时间(td)、润湿时间(t)和混悬稳定性(ΔA)为评价指标进行正交试验,确定最佳处方;对优化处方所制样品测定其溶出度.结果:优选工艺为微晶纤维素30%、乳糖30%、羧甲基淀粉钠0.75%、羟丙纤维素的浓度是1%,所制样品平均td为13.2s,t为21.6s,ΔA为0.001 2;30 min内药物溶出超75%.结论:盐酸氯米帕明口腔崩解片处方设计合理,可进一步开发.

  1. 盐酸氨基葡萄糖分散片的制备及质量控制%Preparation and quality control of glucosamine hydrochloride dispersible tablets

    Institute of Scientific and Technical Information of China (English)

    陈亮; 刘祖雄

    2011-01-01

    Objective To analyze the preparation technology of glucosamine hydrochloride dispersible tablets and its quality control method. Methods Microcrystalline cellulose was selected as the diluent; sodium carboxymethyl starch, low-substituted hydroxypropylcellulose and crospovidone were selected as disintegrants; asipatan was selected as flavoring, peppermint oil was se lected as aromatic, magnesium stearate was selected as lubricant, aerosil was selected as glidant. The contents of glucosamine hydrochloride dispersible tablets were determined by UV spectrophotomery. Results The glucosamine hydrochloride dispersible tablets can be obtained with good taste, smooth-surface and convenient in use. The linear range of glucosamine hydrochloride was 12 ~ 32mg/L (r = O. 9998), the average rate of recovery was 99.65%, RSD was 0.35% ( n = 9). Conclusion The preparation technology is reliable, the methods are simple and accurate which can be used in hospital production and using.%目的 探讨盐酸氨基葡萄糖分散片的制备及质量控制方法.方法 选用微晶纤维素为填充剂,羧甲基淀粉钠、低取代羟丙纤维素、交联聚维酮为崩解剂,阿斯帕坦为矫味剂,薄荷油为芳香剂,硬脂酸镁为润滑剂,微粉硅胶为助流剂.采用紫外分光光度法测定其含量.结果 制得的盐酸氨基葡萄糖分散片口感好、表面光滑、服用方便.盐酸氨基葡萄糖分散片的含量测定的线性范围为12~32 mg/L(r=0.999 8),平均回收率为99.65%,RSD为0.35%(n=9).结论 本制剂处方工艺可靠,检测方法简便、准确、适用于医院配制和应用.

  2. Liver failure induced by overdose of paracetamol, pseudoephedrine hydrochloride and dextromethorphan hydrobromide tablets Ⅱ/paracetamol, pseudoephedrine hydrochloride,diphenhydramine hydrochloride and dextromethorphan hydrobromide tablets%氨酚伪麻美芬片Ⅱ/氨麻苯美片过量致肝衰竭

    Institute of Scientific and Technical Information of China (English)

    王开利; 徐长江; 金晶; 高登莲; 邢汉前; 颜丽; 赵军

    2011-01-01

    A 22-year-old man developed nausea and vomiting following suicide attempt taking 120 paracetamol, pseudoephedrine hydrochloride and dextromethorphan hydrobromide tablets Ⅱ /paracetamol, pseudoephedrine hydrochloride, diphenhydramine hydrochloride and dextromethorphan hydrobromide tablets (total dose of paracetamol 39 g). He was hospitalized about 13 hours after ingesting the drug. Laboratory tests revealed following levels and values; ALT 7385 U/L, Tbil 26.5 μmol/L, Dbil 15.4 μmol/L, PTA 23. 1% , and lactate 3.9 mmol/L. Drug-induced acute liver failure were diagnosed. He received treatment with liver-protective drugs, molecular adsorbent recirculating system (MARS) , and plasma exchange. On day 13 after admission, the patient nearly recovered to normal condition. Repeat liver function tests showed the following levels; ALT 146 U/L, Tbil 16.7 μmol/L, and Dbil 8. 3 μmol/L; and then he was discharged.%1例22岁男性,因企图自杀口服氨酚伪麻美芬片Ⅱ/氨麻苯美片120片(对乙酰氨基酚总剂量39 g),出现恶心呕吐,服药后13 h入院。实验室检查:丙氨酸转氨酶(ALT)7385 U/L,总胆红素(TBil)26.5μmol/L,直接胆红素(DBi1)15.4 μmol/L,凝血酶原活动度23.1%;血乳酸3.9 mmol/L。诊断为药物性肝衰竭。给予保肝药物,分子吸附再循环和血浆置换治疗。入院第13天患者基本恢复正常,肝功能复查:ALT 145U/L,TBil 16.7 μmol/L,DBil 8.3μmol/L,遂出院。

  3. Determination of related substance in Ritodrine hydrochloride tablets by HPLC%HPLC测定盐酸利托君片的有关物质

    Institute of Scientific and Technical Information of China (English)

    刘加元; 何胜利

    2013-01-01

    目的 应用HPLC测定盐酸利托君片的有关物质.方法 采用Apollo C8色谱柱(250 mm×4.6 mm,5μm),甲醇-磷酸氢二铵和庚烷磺酸钠混合溶液(30∶70)为流动相,流速1.0 mL· min-1,检测波长214 nm.结果 盐酸利托君与有关物质分离完全,最低检测限为3×10-5 μg,RSD=0.52%.结论 方法简便、准确、灵敏,可用于盐酸利托君片有关物质的测定.%OBJECTIVE To determine the related substances of Ritodrine hydrochloride tablets by HPLC.METHOD The separation was performed on Apollo C8 column(250 mm× 4.6 mm,5 μm).The mobile phase consisted of methanol-mixture of diammonium hydrogen phosphate and heptane mahogany acid sodium(30:70),and the flow rate was set at 1.0 mL·min-1 with detection wave at 214 nm.RESULTS Under the established chromatographic condition,the related substances and Ritodrine hydrochloride were separated completely,the limit of detection was 3 × 10-5 μg.The precision was good (RSD =0.52%).CONCLUSION The method is simple,accurate,specific and sensitive for the determination of Ritodrine hydrochloride tablets and its related substance.

  4. Investigation and Evaluation of an in Situ Interpolymer Complex of Carbopol with Polyvinylpyrrolidone as a Matrix for Gastroretentive Tablets of Ranitidine Hydrochloride.

    Science.gov (United States)

    Yusif, Rehab Mohammad; Abu Hashim, Irhan Ibrahim; Mohamed, Elham Abdelmonem; El Rakhawy, Mohamed Magdy

    2016-01-01

    Carbopol (CP) is a biocompatible bioadhesive polymer used as a matrix for gastroretentive (GR) tablets, however, its rapid hydration shortens its bioadhesion and floating when incorporated in effervescent formulae. The interpolymer complexation of CP with polyvinylpyrrolidone (PVP) significantly reduced the excessive hydration of CP, prolonging floating and maintaining the mucoadhesiveness. In early attempts, a lengthy process was followed to prepare such an interpolymer complex. In this study, an in situ interpolymer complexation between CP and two grades of PVP (K25 and K90) in 0.1 N HCl was investigated and characterized by Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Hence, directly compressed GR tablets of different combinations of PVP and CP with sodium bicarbonate (SB) as an effervescent agent were examined for prolonged gastroretention and sustained release of ranitidine hydrochloride (RHCl) as a model drug. Tablets were evaluated for in vitro buoyancy, bioadhesiveness, swelling, and drug release in 0.1 N HCl. All GR tablets containing PVP-CP combinations achieved more prolonged floating (>24 h) than CP tablets (5.2 h). Their bioadhesiveness, swelling, and drug release were dependent on the PVP molecular weight and its ratio to CP. Drug release profiles of all formulae followed non-Fickian diffusion. Formula containing the PVP K90-CP combination at a respective ratio of 1 : 3 (P90C13) was a promising system, exhibiting good floating and bioadhesive properties as well as sustained drug release. Abdominal X-ray imaging of P90C13 formula, loaded with barium sulfate, in six healthy volunteers showed a mean gastric retention period of 6.8±0.3 h.

  5. Implementation of QbD Approach to the Analytical Method Development and Validation for the Estimation of Propafenone Hydrochloride in Tablet Dosage Form

    Directory of Open Access Journals (Sweden)

    Monika L. Jadhav

    2013-01-01

    Full Text Available Chromatographic and spectrophotometric methods were developed according to Quality by Design (QbD approach as per ICH Q8(R2 guidelines for estimation of propafenone hydrochloride in tablet dosage form. QbD approach was carried out by varying various parameters and these variable parameters were designed into Ishikawa diagram. The critical parameters were determined by using principal component analysis as well as by observation. Estimated critical parameters in HPTLC method include solvent methanol, mode of detection absorbance, precoated aluminium backed TLC plate (10 cm 10 cm, wavelength: 250 nm, saturation time: 20 min, band length: 8 mm, solvent front: 70 mm, volume of mobile phase: 5 mL, type of chamber: 10 cm 10 cm, scanning time: 10 min, and mobile phase methanol : ethyl acetate : triethylamine (1.5 : 3.5 : 0.4 v/v/v. Estimated critical parameters in zero order spectrophotometric method were solvent methanol, sample preparation tablet, wavelength: 247.4 nm, slit width: 1.0, scan speed medium, and sampling interval: 0.2, and for first order derivative spectrophotometric method it was scaling factor: 5 and delta lambda 4. The above methods were validated according to ICH Q2(R1 guidelines. Proposed methods can be used for routine analysis of propafenone hydrochloride in tablet dosage form as they were found to be robust and specific.

  6. 熔融制粒法制备盐酸二甲双胍缓释片%Preparation of Metformin Hydrochloride Sustained-release Tablets By Melt Granulation

    Institute of Scientific and Technical Information of China (English)

    许谙; 孙丹青

    2013-01-01

    OBJECTIVE To prepare metformin hydrochloride sustained-release tablets and to study its release characterization in vitro and the factors affecting drug release.METHODS Metformin hydrochloride sustained-release tablets were prepared with glycery behenate as matrix material,microcrystalline cellulose as pore-forming agent by melt granulation.The impacts of releasing transmitter,contents of glycery behenate and microcrystalline cellulose,and preparation process factors on the drug release in vitro of the tablets were studied.RESULTS The contents of glycery behenate and microcrystalline cellulose were critical factors affecting drug release rate.The tablets had a remarkable sustained-release property,the drug release profile in vitro followed zero order or Higuchi kinetics.CONCLUSION Using glycery behenate as the wax matrix material,combining with other filers,a sustained release tablet of once daily administration is prepared by melt granulation.%目的 制备盐酸二甲双胍缓释片,并考察其释药行为及影响因素.方法 以山嵛酸甘油酯为骨架材料,微晶纤维素为致孔剂,采用熔融制粒技术制备盐酸二甲双胍缓释片,并考察不同释放介质,山嵛酸甘油酯、微晶纤维素的不同用量以及制备工艺参数等对该缓释片体外释放的影响.结果 山嵛酸甘油酯和微晶纤维素的用量为药物释放的主要影响因素,制备的缓释片具有明显的缓释特征,体外释药过程符合零级动力学模型.结论 采用山嵛酸甘油酯作为蜡质骨架材料,结合其他辅料,采用熔融制粒技术可制备日服1次的盐酸二甲双胍缓释片.

  7. Controlled-release effervescent floating matrix tablets of ciprofloxacin hydrochloride: development, optimization and in vitro-in vivo evaluation in healthy human volunteers.

    Science.gov (United States)

    Tadros, Mina Ibrahim

    2010-02-01

    Ciprofloxacin hydrochloride has a short elimination half-life, a narrow absorption window and is mainly absorbed in proximal areas of GIT. The purpose of this study was to develop a gastroretentive controlled-release drug delivery system with swelling, floating, and adhesive properties. Ten tablet formulations were designed using hydroxypropylmethylcellulose (HPMC K15M) and/or sodium alginate (Na alginate) as release-retarding polymer(s) and sodium bicarbonate (NaHCO(3)) or calcium carbonate (CaCO(3)) as a gas former. Swelling ability, floating behaviour, adhesion period and drug release studies were conducted in 0.1 N HCl (pH 1.2) at 37+/-0.5 degrees C. The tablets showed acceptable physicochemical properties. Drug release profiles of all formulae followed non-Fickian diffusion. Statistical analyses of data revealed that tablets containing HPMC K15M (21.42%, w/w), Na alginate (7.14%, w/w) and NaHCO(3) (20%, w/w) (formula F7) or CaCO(3) (20%, w/w) (formula F10) were promising systems exhibiting excellent floating properties, extended adhesion periods and sustained drug release characteristics. Both formulae were stored at 40 degrees C/75% RH for 3months according to ICH guidelines. Formula F10 showed better physical stability. Abdominal X-ray imaging of formula F10, loaded with barium sulfate, in six healthy volunteers revealed a mean gastric retention period of 5.50+/-0.77h.

  8. Comparative study of ion-exchange resin Indion 204 and Indion 214 for the taste masking of metoclopramide hydrochloride and formulation of rapid-disintegrating tablets

    Directory of Open Access Journals (Sweden)

    Dahima Rashmi

    2010-01-01

    Full Text Available The purpose of this research was to mask the intensely bitter taste of metoclopramide hydrochloride and to formulate a rapid-disintegrating tablet of the taste-masked drug. Taste masking was done by complexing the drug with ion exchange resin, Indion 204 and Indion 214, in different ratios. The complex loading process was optimized for the concentration of resin, swelling time, stirring time, pH, and temperature for maximum drug loading. Drug-resin complexes (DRC were tested for flow properties, drug content, in-vitro release in simulated salivary fluid, and in simulated gastric fluid (SGF, taste evaluation by the panel method. Taste evaluation of DRC revealed considerable taste masking with the degree of bitterness below threshold value (40 μg/ml in 0 to 5 min. Complex of both Indion 204 and Indion 214 masked the taste, but on the basis of the comparative study, resin 214 was selected for taste masking property. Disintegrant croscarmellose (5% wt/wt gave the minimum disintegration time in comparison to crosspovidone and sodium starch glycolate. The batch of tablet containing Pearlitol SD and Avicel (PH102 in the ratio 60:40 and 5% (wt/wt Croscarmellose showed faster disintegration i.e. 32 s, as compare to marketed tablet. It also revealed rapid drug release (t 80 , 6 min in SGF compared with marketed formulation (t 80 , 9 min.

  9. 盐酸利托君片在中国健康志愿者体内的生物等效性%Bioequivalence of ritodrine hydrochloride tablets in Chinese healthy volunteers

    Institute of Scientific and Technical Information of China (English)

    陶春蕾; 许钒; 宋欣; 周燕

    2011-01-01

    Objective: To investigate the bioequivalence of different ritodrine tablets produced by different manufacturers.Methods: According to the similarity of height and weight, a biperiodic two cross test was designed.Totally 18 healthy female subjects were orally administered with 2 pieces ( 10 mg per piece) of test or reference ritodrine hydrochloride tablets.Then, ritodrine HCl concentrations in plasma were determined by LC-MS/MS method with an internal standard.The pharmacokinetic parameters were calculated using the DAS 2.0.1 software,and the bioequivalence of the two preparations was evaluated.Results: The pharmacokinetic parameters of reference tablets were t1/2 = (2.623 ± 1.223) h, Cmax = ( 12.425 ± 6.891 ) ng· mL-1, Tmax = (0.769 ± 0.555 ) h,AUC0~t = (28.416 ±9.102) ng·h·mL-1, AUC0~∞ = (33.199 ± 12.338) ng·h·mL-1; those of test tablets were t1/2 = (2.539 ±0.670) h, Cmax = ( 14.475 ± 11.262) ng·mL-1, Tmax = (0.741 ±0.509) h, AUC0~t = (30.499 ±11.402) ng· h· mL - 1, AUC0~∞ = ( 34.258 ± 12.094 ) ng· h· mL - 1.The relative bioavailability of the test tablets was ( 109.6 ± 23.0) % ( AUC0~t) or ( 108.0 ± 26.2 ) % ( AUC0~∞ ).Conclusion: The test and reference ritodrine hydrochloride tablets are bioequivalent.%目的:研究不同生产厂家生产的利托君片的生物等效性.方法:根据身高体重相近原则,18例健康女性受试者采用双周期两交叉给药方案,分别一次性口服2片(10 mg·片-1)试验盐酸利托君片或参比盐酸利托君片,用LC-MS/MS内标法测定健康受试者血浆中盐酸利托君浓度,采用DAS 2.0.1软件计算药动学参数,并进行2种制剂的生物等效性评价.结果:经药动学参数计算其参比药t1/2=(2.623±1.223)h,Cmax=(12.425±6.891)ng·mL-1,Tmax=(0.769±0.555)h,AUC0-t=(28.416±9.102)ng·h·mL-1,AUC0-∞=(33.199±12.338)ng·h·mL-1;试验制荆t1/2=(2.539±0.670)h,Cmax=(14.475±11.262)ng·mL-1,Tmax=(0.741±0.509)h,AUC0~t=(30.499±11.402)ng·h·mL-1

  10. Determination of donepezil hydrochloride in Donepezil Hydrochloride Tablets by HPLC%高效液相色谱法测定盐酸多奈哌齐片中的盐酸多奈哌齐

    Institute of Scientific and Technical Information of China (English)

    陈泊颖; 王博; 孟策; 陈欣怡; 任晓文

    2016-01-01

    Objective To develop an HPLC method for the content determination of donepezil hydrochloride in Donepezil Hydrochloride Tablets.Methods The HPLC analysis was performed on a Thermo ODS C18 column (250 mm × 4.6 mm,5 μμm);0.02 mol/L sodium 1-heptanesulfonate-acetonitrile-chlorine acid (50∶50∶1) was used as mobile phase;The detection wavelength was set at 271 nm and column temperature was maintained at 30 ℃;the flow rate was 1.0 mL/min and injection volume was 20 μL.Results The method showed a good linear relationship within the concentration range of 50-350 μg/mL (r =0.999 9),and the average recovery was 99.34% with RSD of 0.72% (n =9).Conclusion This method is convenient,rapid,accurate,and with good specificity and reproducibility,which could be used for quantitative determination of donepezil raw material drug and Donepezil Hydrochloride Tablets.%目的 建立高效液相色谱法测定盐酸多奈哌齐片中盐酸多奈哌齐的方法.方法 采用高效液相色谱法,用Thermo ODS C18色谱柱(250 mm×4.6mm,5 μm);以0.02 mol/L庚烷磺酸钠-乙腈-高氯酸(50∶50∶1)为流动相;波长271 nm;柱温30℃;体积流量为1.0 mL/min;进样体积20μL.结果 盐酸多奈哌齐在50~350 μg/mL与峰面积呈良好的线性关系,r=0.999 9(n=7);平均加样回收率为99.34%,RSD值为0.72%(n=9).结论 本法操作简便、准确,专属性强,重复性好,可用于盐酸多奈哌齐原料及盐酸多奈哌齐片的定量测定.

  11. Formulation Development and Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate, Cetirizine Hydrochloride in Combined Pharmaceutical Dosage Form: A New Era in Novel Drug Delivery for Pediatrics and Geriatrics

    Science.gov (United States)

    Sharma, Deepak; Singh, Gurmeet; Kumar, Dinesh; Singh, Mankaran

    2015-01-01

    The objective of the present study was to prepare the fast disintegrating tablet of Salbutamol Sulphate, Cetirizine Hydrochloride in combined tablet dosage form for respiratory disorders such as bronchitis, asthma, and coughing for pediatrics and geriatrics. The tablets were prepared by direct compression technique. Superdisintegrant such as Sodium Starch Glycolate was optimized as 4% on the basis of least disintegration time. Different binders such as MCC and PVP K-30 were optimized along with optimized superdisintegrant concentration. 1% MCC was selected as optimum binder concentration on the basis of least disintegration time. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time, and drug content uniformity. Optimized formulation was further evaluated by in vitro dissolution test, drug-excipient compatibility, and accelerated stability study. Percent weight variation and content uniformity were within the acceptable limit. The friability was less than 1%. The wetting time and disintegration time were practically good for all formulations. FTIR studies and accelerated stability study showed that there was no interaction between the drug and excipients. It was concluded that, by employing commonly available pharmaceutical excipients such as superdisintegrants, hydrophilic and swellable excipients and proper filler, a fast disintegrating tablet of Salbutamol Sulphate, Cetirizine Hydrochloride in combined tablet dosage form, were formulated successfully with desired characteristics. PMID:25810924

  12. Formulation Development and Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate, Cetirizine Hydrochloride in Combined Pharmaceutical Dosage Form: A New Era in Novel Drug Delivery for Pediatrics and Geriatrics

    Directory of Open Access Journals (Sweden)

    Deepak Sharma

    2015-01-01

    Full Text Available The objective of the present study was to prepare the fast disintegrating tablet of Salbutamol Sulphate, Cetirizine Hydrochloride in combined tablet dosage form for respiratory disorders such as bronchitis, asthma, and coughing for pediatrics and geriatrics. The tablets were prepared by direct compression technique. Superdisintegrant such as Sodium Starch Glycolate was optimized as 4% on the basis of least disintegration time. Different binders such as MCC and PVP K-30 were optimized along with optimized superdisintegrant concentration. 1% MCC was selected as optimum binder concentration on the basis of least disintegration time. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time, and drug content uniformity. Optimized formulation was further evaluated by in vitro dissolution test, drug-excipient compatibility, and accelerated stability study. Percent weight variation and content uniformity were within the acceptable limit. The friability was less than 1%. The wetting time and disintegration time were practically good for all formulations. FTIR studies and accelerated stability study showed that there was no interaction between the drug and excipients. It was concluded that, by employing commonly available pharmaceutical excipients such as superdisintegrants, hydrophilic and swellable excipients and proper filler, a fast disintegrating tablet of Salbutamol Sulphate, Cetirizine Hydrochloride in combined tablet dosage form, were formulated successfully with desired characteristics.

  13. 盐酸羟考酮控释片治疗老年癌痛体会%Treatment for cancerous pain in the elderly with Oxy-Codone hydrochloride controlled-release tablets.

    Institute of Scientific and Technical Information of China (English)

    刘彦芳; 刘端祺; 李红英; 张侠

    2010-01-01

    Objective To evaluate effectiveness and side effects, as well as its safety, of Oxy-Codone hydrochloride controlled-release tablets (Oxycontin) for the elderly patients with moderate to severe cancerous pain. Methods From March 2005 to February 2009,106 elderly patients ( aged more than 60 years) suffered from moderate to severe cancerous pain were treated with Oxycontin,at initial dose of 10 mg/12 h. For the patients using making them pain-free or pain relieved mostly. Every patient was treated for 4 weeks at least. Severity of pain,sleeping status, appetite, fatigue, mental status, daily life, scores of understanding and cooperation, and side effects were .observed.Results The minimal effective dose of Oxycontin was 10 mg/d for the elderly patients with cancerous pain. Twenty-three patients (21.7%) were treated with it at dose of ≥200 mg/d,30 patients (28. 2% )at dose of 100 - 180 mg/d,and 53 patients (50. 0% ) at dose of 10 -90 mg/d. Pain was relieved in 97. 16% of the patients after treatment, with common side effects of constipation, nausea, vomiting;and drug treatment was needed for 24. 53% (26/106) of the patients with more common constipation. Conclusions Oxycontin is effective,tolerable,less side-effects for the elderly patients with moderate to severe cancerous pain, and can improve their quality of life.%目的 观察盐酸羟考酮控释片(商品名:奥施康定),治疗老年恶性肿瘤患者中、重度疼痛的临床效果及不良反应,明确该药在治疗老年癌痛中的有效性及安全性.方法 2005年3月至2009年2月中、重度疼痛老年恶性肿瘤患者(年龄≥60岁)106例,给予盐酸羟考酮控释片镇痛治疗,初始剂量10 mg/12 h,正在用吗啡类镇痛药者,按照口服吗啡1/2剂量换算,根据疼痛情况调整剂量,直至患者无痛或基本无痛,每位患者至少治疗4周以上.同时进行疼痛强度、睡眠、食欲、疲乏、精神状态、日常生活、理解配合程度评

  14. Relative Bioavailability of Sustained Release Tablets of Tramadol Hydrochloride%盐酸曲马多缓释片的相对生物利用度研究

    Institute of Scientific and Technical Information of China (English)

    葛庆华; 王浩; 张小红; 刘戈; 周臻

    2001-01-01

    18名男性健康受试者,随机交叉口服两种盐酸曲马多缓释片,采用反相高效液相色谱-荧光检测法测定血浆药物浓度。单剂量口服100 mg两种缓释片的Cmax为205.0±51.3和193.5±44.0 ng/ml;Tmax为5.6±2.1和5.8±2.6 h;t1/2为7.3±2.6和7.3±2.8 h。供试制剂的相对生物利用度为97.36±10.01%。多剂量口服两种缓释片达稳态后的峰谷比为1.42±0.17和1.44±0.22;波动度为36.09±12.78和34.37±14.22%。经统计处理均无显著性差异(P>0.05)。经双单侧t检验,两种缓释片具有生物等效性。%The pharmacokinetics and relative bioavailability of two brands of sustained release tramadol hydrochloride tablets administrated orally by 18 healthy male volunteers were investigated, according to a randomized crossover design. The plasma concentration of tramadol hydrochloride was determined by RP-HPLC method with fluorescence detection. The pharmacokinetic parameters for the single oral dose of 100 mg sustained release tramadol hydrochloride tablets were Cmax 205.0±51.3 and 193.5±44.0 ng/ml; Tmax 5.6±2.1 and 5.8±2.6 h;t1/2 7.3±2.6 and 7.3±2.8 h, for tested and reference tablets, respectively. The relative bioavailability for the tested tablets was 97.36±10.01%. For the multiple dosing, the concentration peak-trough ratio (PTR) were 1.42±0.17 and 1.44±0.22, the degree of fluctuation (DF) were 36.09±12.78 and 34.37±14.22%, respectively. The results of two-one-sided t test showed that the tablets of two brands were bioequivalent.

  15. Determination of glibenclamide, metformin hydrochloride and rosiglitazone maleate by reversed phase liquid chromatographic technique in tablet dosage form

    Directory of Open Access Journals (Sweden)

    Havele Shweta S.

    2014-01-01

    Full Text Available A simple, precise and accurate high performance liquid chromatography (HPLC method was developed for the simultaneous estimation of metformin hydrochloride, rosiglitazone maleate, glibenclamide present in multicomponent dosage forms. Chromatography was performed on a 25 cm × 4.6 mm i.d., 5-μm particle, C18 column with 78:22 (v/v methanol: 20 mM potassium dihydrogen phosphate buffer as mobile phase at a flow rate of 1.0 ml/min and UV detection at 238 nm for metformin hydrochloride, rosiglitazone maleate, and glibenclamide. The total elution time was shorter than 9 min. This method was found to be precise and reproducible. This proposed method was successfully applied for the analysis of metformin hydrochloride, rosiglitazone maleate, glibenclamide as a bulk drug and in pharmaceutical formulation without any interference from the excipients.

  16. Detection of Dextroisomer in Levamisole Hydrochloride Tablets%盐酸左旋咪唑片的右旋体监测

    Institute of Scientific and Technical Information of China (English)

    缪宁梅; 尹菁; 张梅; 李忠红; 纪宇

    2012-01-01

    The enantiomers of levamisole hydrochloride was detected and controlled by HPLC and polarimetry. In the HPLC method, a chiral AGP column was applied with the mobile phase consisting of 10mmol·L-1 ammonium formate solution (pH 6.2). Detection wavelength was at 214 nm. The resolution of enantiomers was more than 1.5. In the polarimetry method, extracting with dichloromethane before determination could avoid the disturbance of excipients. Both of the methods can be used for the control of dextroisomer in levamisole hydrochloride tablets.%分别采用手性高效液相色谱法和旋光法检查和控制盐酸左旋咪唑片中右旋异构体的含量.方法一:使用Chiral AGP手性柱,10 mmol·L-1甲酸铵溶液(pH值约6.2)为流动相,检测波长为214 nm,盐酸左旋咪唑与对映体的分离度大于1.5.方法二:使用二氯甲烷提取后测定旋光度,可有效消除辅料的干扰.两种方法均可用于盐酸左旋咪唑片中的右旋体杂质的控制.

  17. 盐酸乙哌立松片在健康人体内的药代动力学及生物等效性%Pharmacokinetics and bioequivalence of eperisone hydrochloride tablet in healthy subjects

    Institute of Scientific and Technical Information of China (English)

    魏欣; 丁黎; 高家敏; 李君; 张胜强; 沈建平; 张银娣

    2004-01-01

    Aim To develop a HPLC-ESI-MS assay for determination of eperisone hydrochloride in human plasma and investigate the pharmacokinetics and bioequivalence of two eperisone hydrochloride tablets in human. Methods Buflomedil hydrochloride was used as the internal standard. After alkalized with saturated sodium bicarbonate solution, plasma was extracted with diethylether-cyclohexane (1:1) and separated using HPLC on a reversed-phase C18 column with a mobile phase of 10mmol·L-1 ammonium acetate buffer solution (adjusted to pH 3.88 with acetic acid)-methanol (20:80). HPLC-ESI-MS was performed in the selected ion monitoring (SIM) mode using target ions at m/z 260 for eperisone and m/z 308 for the internal standard. A randomized crossover design was performed in 20 healthy volunteers. In the two study periods, a single 100mg dose of each tablet was administered to each volunteer. Results Calibration curve was linear over the range of 0.02-20μg·L-1. The limit of quantification for eperisone hydrochloride in plasma was 0.02μg·L-1. The main pharmacokinetics parameters T1/2, Tmax and Cmax were (2.7±0.4)h, (1.1±0.5)h and (2.8±2.8)μg·L-1 for the reference tablet; (2.8±0.5)h, (1.1±0.4)h and (3±4)μg·L-1 for the test tablet, respectively. The relative bioavalability of the test tablet was (101±13)%. Conclusion The assay was proved to be sensitive, accurate and convenient. The two formulations were bioequivalent.

  18. Study on the Improvement of the Standard of Prazosin Hydrochloride Tablets%盐酸哌唑嗪片质量标准改进研究

    Institute of Scientific and Technical Information of China (English)

    吴珺; 钱忠义; 袁华峰

    2015-01-01

    Objective:To improve the present quality standard of Prazosin Hydrochloride Tablets, and to increase the accuracy of the test results and the environmental friendliness of the operation.Methods:A reverse-phase HPLC method was established for the determination of the contents, content uniformity and related substances in Prazosin Hydrochloride Tablets. The Waters Sunifre C18 column(4.6 mm×250 mm, 5 μm)was adopted with the mobile phase of methanol-phosphate buffer solution(containing 0.1 mol·L-1 potassium dihydrogen phosphate and 0.4% triethylamine, adjusted to pH 4.5 with phosphoric acid) (40∶60). The flow rate was 1 mL·min-1, and the detection wavelength was 245 nm. The column temperature was 35℃, and the volume of injection was 10 μL.Results:The linear range of Prazosin Hydrochloride was 4.910-49.10 μg•mL-1(r=1.000, n=6). The average recovery rate was 99.50%, RSD=0.70%.Conclusion:Veriifed by methodology, the method could be applied to determine the content, content uniformity and related substances in Prazosin Hydrochloride Tablets.%目的:改进盐酸哌唑嗪片现行质量标准,使检测结果更准确,操作更环保。方法:建立反相高效液相色谱法测定盐酸哌唑嗪片的含量、含量均匀度和有关物质。采用Waters Sunfire C18柱(4.6 mm×250 mm,5μm),流动相为甲醇-磷酸盐缓冲液(磷酸二氢钾1.36 g,加水溶解并稀释制成1000 mL,加三乙胺4 mL,用磷酸调节pH值至4.5)(40∶60),流速:1 mL·min-1,检测波长:245 nm,柱温:35℃,进样体积:10μL。结果:盐酸哌唑嗪在4.910~49.10μg·mL-1范围内线性关系良好(r=1.000, n=6);平均回收率为99.50%,RSD=0.70%。结论:本方法经方法学验证,可用于盐酸哌唑嗪片含量、含量均匀度测定和有关物质检查。

  19. 盐酸美金刚片在中国健康人体的生物等效性%Study on the bioequivalence of memantine hydrochloride tablets in Chinese healthy volunteers

    Institute of Scientific and Technical Information of China (English)

    郑恒; 周华; 任丽; 钱振宇; 彭彦

    2012-01-01

    目的:评价国产与进口盐酸美金刚片在中国健康人体的生物等效性.方法:20名健康男性受试者随机交叉单剂量口服受试制剂或参比制剂盐酸美全刚片各10 mg.用高效液相色谱-串联质谱法测定血浆中美金刚浓度;用DAS3.0软件计算药动学参数,并对两种药物进行生物等效性评价.结果:受试制剂和参比制剂的主要药动学参数:Cmax分别为(18.1±3.8)和(20.3±4.2)ng·mL-1;tmax分别为(12.7±15.1)和(8.8±3.0)h;t1/2分别为(60.8±15.5)和(61.4±19.2)h;AUC0-t分别为(1748.6±338.9)和(1720.2±317.3)ng·h·mL-1.AUC0-t、AUC0-∞、Cmax的90%置信区间分别为89.8%~105.6%、89.7%~106.1%、84.8%~93.9%.受试制剂相对生物利用度F0-t为(95.5±2.9)%.结论:受试制剂与参比制剂具有生物等效性.%OBJECTIVE To evaluate the bioequivalence of two preparations of memantine hydrochloride in healthy volunteers. METHODS A single oral dose of 10 mg test preparation or reference preparation memantine hydrochloride tablets were given to 20 male healthy volunteers in a randomized crossover study. The concentrations of memantine were determined by HPLC-MS/MS method. The pharmacokinetic parameters and relative bioavailability were calculated by DAS 3. 0 software, and then the bioequivalence was judged. RESULTS The main pharmacokinetic parameters of test preparation and reference preparation were as follows: Cmax was (18. 1 ±3.8), (20. 3 ±4. 2) ng·mL-1; t max was (12. 7 ± 15. 1), (8.8 ± 3.0) h; t1:2 was (60.8 + 15.5), (61. 4 ± 19.2) h; AUC0-t was (1 748. 6 ± 338. 9). (1 720. 2 ± 317. 3) ng·h· mL-1 , respectively. The 90% CIs for the ratios of AUG0-T、AUG0-∞ ,C max were 89. 8% ~1()5. 6%,89. 7%~106. 1%,84. 8%~93. 9%, respectively. The relative bioavailability of test preparation was (95.5 ±2. 9)%. CONCLUSION The results demonstrated that the two preparations were bioequivalent.

  20. Bioequivalence Study of Paroxetine Hydrochloride Film-Coated Tablets%盐酸帕罗西汀薄膜衣片的生物等效性研究

    Institute of Scientific and Technical Information of China (English)

    施爱明; 王蒙; 周文佳; 张全英

    2012-01-01

    目的 以盐酸帕罗西汀片(赛乐特)为参比制剂,研究盐酸帕罗西汀薄膜衣片的人体相对生物利用度,以判断两种制剂是否具有生物等效性.方法 采用随机、开放、双周期交叉试验设计,24例男性健康受试者禁食过夜后空腹单剂量口服盐酸帕罗西汀制剂20 mg,液相色谱-串联质谱法(LC- MS/MS)测定血浆中帕罗西汀的浓度,应用DAS2.0软件计算有关药动学参数并评价两种制剂的生物等效性.结果 单剂量口服受试制剂和参比制剂的主要药动学参数pmax分别为(5.102±2.955)和(5.396±2.852)μg·L-1;tmax分别为(5.22±1.83)和(5.35±0.78)h;t1/2分别为(11.76±2.91)和(11.98±3.57)h;AUC0~96h分别为(118.1±90.2)和(118.9±86.0)μg·h·L-1,AUC0-∞分别为(120.2±91.0)和(121.5±87.6) μg·h·L-1.结论 受试制剂与参比制剂的人体相对生物利用度为( 100.6±22.0)%,两种制剂具有生物等效性.%OBJECTIVE To evaluate the relative bioavailibility and bioequivalence of paroxetine hydrochloride film-coated tablets. METHODS In a randomized crossover study, 24 healthy Chinese male subjects received a single oral dose (20 mg) of either test or reference paroxetine hydrochloride tablets after an overnight fast The plasma concentrations of paroxetine were determined by a validated LC-MS/MS method. The pharmacokinetic parameters, the relative bioavailability and bioequivalence of two formulations were evaluated by DAS 2. 0 software. RESULTS After a single oral dose of 20 mg test or reference paroxetine tablets, the pharmacokinetic parameters of paroxetine were as follows: ρmax ( 5. 102 ± 2. 955) and ( 5. 396 ± 2. 852 ) μg · L-1; tmax ( 5. 22 ± 1. 83 ) and (5. 35 ± 0.78) h ; t1/2(11.76±2.91) and (11.98 ±3.57) h; AUC0-96h (118. 1 ±90.2) and (118. 9 ± 86. 0) μg · h · L-1; AUC0-8 (120. 2 ±91.0) and ( 121. 5 ±87. 6) μg · h · L-1 , respectively. CONCLUSION The relative bioavailability of the test paroxetine hydrochloride film

  1. Continuous twin screw melt granulation of glyceryl behenate: Development of controlled release tramadol hydrochloride tablets for improved safety.

    Science.gov (United States)

    Keen, Justin M; Foley, Connor J; Hughey, Justin R; Bennett, Ryan C; Jannin, Vincent; Rosiaux, Yvonne; Marchaud, Delphine; McGinity, James W

    2015-06-20

    Interest in granulation processes using twin screw extrusion machines is rapidly growing. The primary objectives of this study were to develop a continuous granulation process for direct production of granules using this technique with glyceryl behenate as a binder, evaluate the properties of the resulting granules and develop controlled release tablets containing tramadol HCl. In addition, the granulation mechanism was probed and the polymorphic form of the lipid and drug release rate were evaluated on stability. Granules were prepared using a Leistritz NANO16 twin screw extruder operated without a constricting die. The solid state of the granules were characterized by differential scanning calorimetry and X-ray diffraction. Formulated tablets were studied in 0.1N HCl containing 0-40% ethanol to investigate propensity for alcohol induced dose dumping. The extrusion barrel temperature profile and feed rate were determined to be the primary factors influencing the particle size distribution. Granules were formed by a combination immersion/distribution mechanism, did not require subsequent milling, and were observed to contain desirable polymorphic forms of glyceryl behenate. Drug release from tablets was complete and controlled over 16 h and the tablets were determined to be resistant to alcohol induced dose dumping. The drug release rate from the tablets was found to be stable at 40°C and 75% relative humidity for the duration of a 3 month study.

  2. 反相高效液相色谱法测定妇炎消片中盐酸小檗碱含量%Determination of Berberine Hydrochloride Content in Fuyanxiao Tablets by RP-HPLC

    Institute of Scientific and Technical Information of China (English)

    赵为民; 仲崇林; 杨美林; 刘诗月

    2005-01-01

    An RP-HPLC method was used to determine the content of berberine hydrochloride in Fuyanxiao tablets on a Diamonsil C18 column. The mobile phase was a CH3CN/KH2PO4(volume ratio 30:70) mixture of pH=3, and the average rate of recovery of berberine hydrochloricde was 98.18%, with a RSD of 0.92% (n=5). The method is simple and accurate, and can be used for the quality control in the production of Fuyanxiao tablet.

  3. 光纤传感技术对盐酸普萘洛尔片快速分析方法学建立%Establishment of rapid fiber optic sensor analysis method about propranolol hydrochloride tablets

    Institute of Scientific and Technical Information of China (English)

    冯翠娟; 李莉; 张春玲; 靳露; 杨婷

    2012-01-01

    目的:建立光纤传感快速分析盐酸普萘洛尔片的方法,并进行定性、定量分析.方法:采用光纤传感分析技术对盐酸普萘洛尔片进行紫外吸收光谱鉴定和含量测定.探头直接浸入药品溶液,进行数据采集,通过计算机自动处理数据,测得药物含量.同时与中国药典(二部)2010年版收载的含量测定方法进行测定比较.结果:本法测定不需过滤辅料,样品处理方法简单,可瞬间获得片剂的特征图谱,提取相关参数;含量测定结果与药典方法比较无显著性差异(P>0.05).结论:光纤传感分析法可用于快速、准确对盐酸普萘洛尔片进行定性定量分析.%To develop a method that can analyze Propranolol Hydrochloride tablets by fiber optic sensor rapidly ,and determine the spectrum and content of Propranolol Hydrochloride tablets. Methods:using fiber - optical sensing technology to determine the ultraviolet absorption spectrum and content of Propranolol Hydrochloride, the detector end was dipped into the original solution of the Propranolol Hydrochloride tablets directly, when information related to the samples was imported into the computer.it can show the scanning map and provide drug content. And compared the consistency of this method with the method in ChP (2010) in regard to determination at the same time. Results:The method can be instantaneous access to the feature map of the Propranolol Hydrochloride tablets and obtain the related parameters. The determination results obtained by this method had no significant difference compared with the method in ChP (2010) (P >0. 05). Conclusion:The method of analysis by fiber optic sensor can be used for rapid analysis for Propranolol Hydrochloride tablets.

  4. Formulation and Evaluation of a Sustained-Release Tablets of Metformin Hydrochloride Using Hydrophilic Synthetic and Hydrophobic Natural Polymers

    OpenAIRE

    K J Wadher; Kakde, R. B.; M J Umekar

    2011-01-01

    Metformin hydrochloride has relatively short plasma half-life, low absolute bioavailability. The need for the administration two to three times a day when larger doses are required can decrease patient compliance. Sustained release formulation that would maintain plasma level for 8-12 h might be sufficient for daily dosing of metformin. Sustained release products are needed for metformin to prolong its duration of action and to improve patient compliances. The overall objective of this study ...

  5. Development and validation of a liquid chromatographic method for estimation of dicyclomine hydrochloride, mefenamic Acid and paracetamol in tablets.

    Science.gov (United States)

    Shah, D A; Rana, Jainika P; Chhalotiya, Usmangani K; Baldania, S L; Bhatt, K K

    2014-01-01

    Liquid chromatographic method was developed for simultaneous quantitative determination of dicyclomine hydrochloride, mefenamic acid and paracetamol in their combined dosage form. The separation was achieved using a C18 column (250×4.6 mm id, 5 μm) using acetonitrile:20 mM potassium dihydrogen phosphate 70:30 (v/v) adjusted to pH 4 using orthophosphoric acid as mobile phase at a flow rate of 1 ml/min and detection at 220 nm. Separation was completed within 12 min. The retention times of dicyclomine hydrochloride, mefenamic acid and paracetamol were 3.8, 9.3 and 2.5 minutes respectively. The proposed method was found to have linearity in concentration range of 10-100 μg/ml for dicyclomine hydrochloride, 0.05-10 μg/ml for mefenamic acid and 0.1-20 μg/ml for paracetamol. The developed method has been statistically validated and was found to be simple, precise, reproducible and accurate. The developed and validated method was successfully used for the quantitative analysis of commercially available dosage form.

  6. 布洛伪麻分散片的溶出度测定%Determination of Dissolution of Ibuprofen and Pseudoephedrine Hydrochloride Dispersible Tablets

    Institute of Scientific and Technical Information of China (English)

    邱颖姮; 王铁杰; 周寿林; 张弘; 李清

    2012-01-01

    The dissolubilities of ibuprofen and pseudoephedrine hydrochloride dispersible tablets in different dissolution mediums and different rotation speeds were discussed. The dissolution method was determined as follows: using the second dissolution method in Chinese Pharmacopoeia 2010 edition, at the rotation speed of 50 r/min and with the phosphate buffer solution (pH 5.5) of 900 ml. Ibuprofen and pseudoephedrine hydrochloride were detemined by HPLC. A C18 column was used with the mobile phase of acetonitrile-water (1 : 1) (containing sodium dodecyl sulfate 2.5 g and phosphoric acid 1 ml dissolved in 1 000 ml, adjusted to pH 3.2 with ammonia) at the detection wavelength of 215 nm. The calibration curves of ibuprofen and pseudoephedrine hydrochloride were linear in the concentration ranges of 10 -1 000 μg/ml and 1.5 -150 μg/ml. The recoveries were 98.1 % and 100.4%, with RSDs of 2.6% and 0.4%.%建立了布洛伪麻分散片的溶出度检查方法.考察在不同的溶出介质、转速下布洛伪麻分散片中布洛芬和盐酸伪麻黄碱的溶出情况,确定了溶出参数:照中国药典2010年版溶出度第二法装置,以pH 5.5的磷酸盐缓冲液900ml为溶出介质,转速50 r/min.采用HPLC法测定每片中布洛芬和盐酸伪麻黄碱的溶出量.使用C18色谱柱,流动相为乙腈-水(1∶1)(每1 000ml含十二烷基磺酸钠2.5 g,加磷酸1 ml,混匀后用氨水调至pH 3.2),检测波长215 nm.布洛芬和盐酸伪麻黄碱在10~1 000 μg/ml和1.5~150 μ.g/ml范围内线性关系良好,回收率为98.1%和100.4%,RSD为2.6%和0.4%.

  7. Controlled release of ropinirole hydrochloride from a multiple barrier layer tablet dosage form: effect of polymer type on pharmacokinetics and IVIVC.

    Science.gov (United States)

    Malewar, Nikhil; Avachat, Makarand; Pokharkar, Varsha; Kulkarni, Shirish

    2013-09-01

    The purpose of the present study was to control in vitro burst effect of the highly water-soluble drug, ropinirole hydrochloride to reduce in vivo dose dumping and to establish in vitro-in vivo correlation. The pharmacokinetics of two entirely different tablet formulation technologies is also explored in this study. For pharmacokinetics study, FDA recommends at least 10% difference in drug release for formulations to be studied but here a different approach was adopted. The formulations F8A and F9A having similar dissolution profiles among themselves and with Requip® XL™ (f 2 value 72, 77, 71 respectively) were evaluated. The C max of formulation F8A comprising hypromellose 100,000 cP was 1005.16 pg/ml as compared to 973.70 pg/ml of formulation F9A comprising hypromellose 4000 cP irrespective of T max of 5 and 5.75 h, respectively. The difference in release and extent of absorption in vivo was due to synergistic effect of complex RH release mechanism; however, AUC0-t and AUC0-∞ values were comparable. The level A correlation using the Wagner-Nelson method supported the findings where R (2) was 0.7597 and 0.9675 respectively for formulation F8A and F9A. Thus, in vivo studies are required for proving the therapeutic equivalency of different formulation technologies even though f 2 ≥ 50. The technology was demonstrated effectively at industrial manufacturing scale of 200,000 tablets.

  8. Development and Validation for the Simultaneous Quantification of Nebivolol Hydrochloride and Hydrochlorothiazide by UV Spectroscopy, RP-HPLC and HPTLC in Tablets

    Directory of Open Access Journals (Sweden)

    B. Dhandapani

    2010-01-01

    Full Text Available Simultaneous quantification of nebivolol hydrochloride (NEB-H and hydrochlorothiazide (HCT in tablets by UV spectroscopy, RP-HPLC and HPTLC methods were developed. In UV spectrophotometric determination NEB-H and HCT was quantified by simultaneous equation method and absorbance ratio method. In simultaneous equation method absorbance measurements at 282.5 nm (λmax NEB-H and 271.5 nm (λmax HCT, in absorbance ratio method absorbance measurements at 282.5 nm and 275 nm (iso absorptive point in methanol. In RP-HPLC method, the drugs were resolved using a mobile phase of 30 mM phosphate buffer (K2HPO4, acetonitrile and triethylamine (50:50:0.1 % v/v with pH 5.5 using orthophosphoric acid on a C18-ODS- Phenomenex (5 μm, 250 mm x 4.6 mm column in isocratic mode, Atorvastatin (ATR used as a internal standard. The retention time of HCT, NEB-H and ATR was 3.31, 4.30 and 6.93 min respectively. In the HPTLC method, the chromatograms were developed using a mobile phase of ethyl acetate: methanol: ammonia (8.5:1:0.5 v/v on precoated plate of silica gel 60 F254 and quantified by densitometric absorbance mode at 285 nm. The Rf of HCT and NEB-H were 0.21 and 0.41 respectively. Recovery studies of 98.88-102.41%, percentage relative std deviation of not more than 0.8 and correlation coefficient (linearity range of 0.9954-0.9999 shows that developed methods were accurate and precise. These methods can be employed for the routine analysis of tablets containing NEB-H and HCT.

  9. 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.

  10. XLGB Capsule Combined with Glucosamine Hydrochloride Tablets in the Treatment of Knee Osteoarthritis 60 Cases%仙灵骨葆胶囊联合盐酸氨基葡萄糖片治疗膝骨性关节炎

    Institute of Scientific and Technical Information of China (English)

    韩国栋; 蒋再轶; 谭洁; 彭芝配

    2011-01-01

    目的:观察仙灵骨葆胶囊联合盐酸氨基葡萄糖片治疗膝骨性关节炎的临床疗效.方法:将60例患者随机分为治疗组与对照组,治疗组仙灵骨葆胶囊+盐酸氨基葡萄糖片口服(仙灵骨葆胶囊,3粒/次,2次/d;盐酸氨基葡萄糖片,480 mg/次,3次/d),对照组盐酸氨基葡萄糖片口服(480 mg/次,3次/d),8周为1个疗程.结果:治疗组有效率89.3%,对照组为71.9%,两组差异显著(P<0.05);两组治疗后疼痛缓解时间比较,差异显著(P<0.05).结论:仙灵骨葆胶囊联合盐酸氨基葡萄糖片治疗膝骨性关节炎疗效明显,且能够缩短关节疼痛时间.%Objective: To observe the joint Xiangling Cubao ( XLCB ) capsules with glucosamine hydrochloride tablets in the treatment of knee osteoarthritis. Method; Sixty patients were randomly divided into treatment group and control group, treatment group received XLCB capsules + glucosamine hydrochloride tablet(XLCB capsules, 3 capsules, 2 twice daily + glucosamine hydrochloride tablets, 480 mg, 3 times daily) , the control group received glucosamine hydrochloride tablet (480 mg, 3 times daily) , 8 weeks for a course of treatment. Result: The treatment group' s effective rate was 89.3% , the control group rate was 71.9% , the difference was statistically significant ( P < 0. 05) , Comparing the pain relief time after treatment, the difference was statistically significant ( P < 0. 05 ) . Conclusion: XLCB capsule combined with glucosamine hydrochloride tablets in the treatment of knee osteoarthritis shows efficacy significantly, joint pain can be shortened.

  11. Development and validation of a novel RP-HPLC method for simultaneous determination of paracetamol, phenylephrine hydrochloride, caffeine, cetirizine and nimesulide in tablet formulation

    Directory of Open Access Journals (Sweden)

    A.P. Dewani

    2015-07-01

    Full Text Available The present work describes development and validation of a high-performance liquid chromatography–diode array detection (HPLC–DAD procedure for the analysis of phenylephrine hydrochloride (PHE, paracetamol (PAR, caffeine anhydrous (CAF, cetirizine Dihydrochloride (CET, nimesulide (NIM in pharmaceutical mixture. Effective chromatographic separation of PHE, PAR, CAF, CET and NIM was achieved using a Kinetex-C18 (4.6 mm, 150 mm, 5 mm column with gradient elution of the mobile phase composed of 10 mM phosphate buffer (pH 3.3 and acetonitrile. The elution was a three step gradient elution program step-1 started initially with 2% (by volume acetonitrile and 98% phosphate buffer (pH 3.3 for first 2 min. In step-2 acetonitrile concentration changed linearly to 20% up to 12 min the analysis was concluded by step-3 changing acetonitrile to 2% up to 20 min. The proposed HPLC method was statistically validated with respect to linearity, ranges, precision, accuracy, selectivity and robustness. Calibration curves were linear in the ranges of 5–100, 100–1000 and 10–200 mg/mL for PHE, PAR, CAF, CET and NIM respectively, with correlation coefficients >0.9996. The HPLC method was applied to tablet dosage form in which the analytes were successfully quantified with good recovery values with no interfering peaks from the excipients.

  12. Determination of pioglitazone hydrochloride tablets by HPLC%HPLC法测定盐酸吡格列酮片的含量

    Institute of Scientific and Technical Information of China (English)

    何厚洪; 陈建

    2001-01-01

    An HPLC method was established to assay the content of pioglitazone hydrochloride tablets. The solid phase was Hypersil C18. The mobile phase consisted of acetonitrile and 10mmol/L ammonium acetate buffer(pH 6.0)(60∶40). The detector was set at 229nm. The flow rate was 1.0ml/min. The calibration curve was linear from 10μg/ml to 200μg/ml. The average recovery was 99.73%(RSD=1.22%).%采用反相HPLC法,以C18为固定相,乙腈-10mmol/L醋酸铵缓冲液(pH 6.0)(60∶40)为流动相,检测波长为229nm,流速为1.0ml/min,测定了盐酸吡格列酮片的含量。线性范围为10~200μg/ml,平均回收率为99.73%(RSD=1.22%)。

  13. Simultaneous determination of pyridoxine hydrochloride and doxylamine succinate from tablets by ion pair reversed-phase high-performance liquid chromatography (RP-HPLC).

    Science.gov (United States)

    Argekar, A P; Sawant, J G

    1999-08-01

    A new, simple, precise, and rapid ion pair reversed-phase high-performance liquid chromatography (RP-HPLC) method has been developed for the simultaneous determination of pyridoxine hydrochloride (PYR) and doxylamine succinate (DOX) in tablets. The stationary phase was a Microbondapak C18 column (10 mu, 300 mm x 3.9 mm i.d.). The mobile phase was water:methanol (60:40) containing 10 mM heptanesulfonic acid and 0.25% triethylamine and adjusted to pH 2.2 with orthophosphoric acid. Detection was carried out at 263 nm using an ultraviolet (UV) detector. The flow rate was 1.0 ml/min, and retention times were 3.65 min and 7.32 min for PYR and DOX, respectively. The linearity was obtained in the concentration range 0.5-500 micrograms/ml for PYR and DOX. Mean percentage recoveries were 100.20% and 101.20% for PYR and DOX, respectively.

  14. Use of a Sonogel-Carbon electrode modified with bentonite for the determination of diazepam and chlordiazepoxide hydrochloride in tablets and their metabolite oxazepam in urine.

    Science.gov (United States)

    Naggar, Ahmed Hosny; Elkaoutit, Mohammed; Naranjo-Rodriguez, Ignacio; El-Sayed, Abd El-Aziz Yossef; de Cisneros, José Luis Hidalgo-Hidalgo

    2012-01-30

    Sonogel-Carbon electrode (SngCE) modified with bentonite (BENT) shows an interesting alternative electrode to be used in the determination of 1,4-benzodiazepines by square wave adsorptive cathodic stripping voltammetry (SWAdCSV). Diazepam (DZ) and chlordiazepoxide hydrochloride (CPZ), were determined using SngCE modified by 5% BENT. An electrochemical study of different parameters (such as pH, buffer type, ionic strength, accumulation potential, scan rate, and accumulation time) which affect the determination of DZ and CPZ is reported. Linear concentration ranges of 0.028-0.256 μg mL(-1) DZ (r=0.9997) and 0.034-0.302 μg mL(-1) CPZ (r=0.9997) are successfully obtained after an accumulation time of 60s. The quantification and detection limits were calculated to be 14.0 and 4.0 ng mL(-1) for DZ, and 16.0 and 5.0 ng mL(-1) for CPZ, respectively. The surface of the proposed electrode was characterized by scanning electron microscopy (SEM) and energy dispersive X-ray analysis (EDAX). The developed method was applied to the analysis of commercially available tablets and human urine real samples. Analysis was performed with better precision, very low detection limits, and faster than previously reported voltammetric techniques.

  15. 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

  16. Formulation and In Vitro Evaluation of Bilayer Tablets of Nebivolol Hydrochloride and Nateglinide for the Treatment of Diabetes and Hypertension

    Directory of Open Access Journals (Sweden)

    Harika Ryakala

    2015-01-01

    Full Text Available Diabetes mellitus (DM and hypertension are two common diseases that often coexist. The most common cause of death in the diabetic patient is heart disease. In the present investigation we combine Nebivolol and Nateglinide for better patient compliance. IR layer was formulated using various superdisintegrants like Crospovidone, Croscarmellose sodium, and sodium starch glycolate and SR layer was formulated using polymers and gums like HPMC E15, ethyl cellulose, Gaur gum, and Xanthan gum. The disintegration and dissolution study of both layers showed that inclusion of surfactant (sodium lauryl sulphate to the tablet formulation (IR and dissolution medium (SR enhanced the release of drugs from both layers. Kinetic studies of optimized IR layer (NBL8 and SR layer (N9 showed good linearity with regression coefficient of 0.9714 (Higuchi model and 0.9931 (zero order kinetics, respectively. The above results reveal that the optimized IR layer of Nebivolol (NBL8 and SR layer of Nateglinide (N9 might be suitable for the treatment of diabetes and hypertension by sequential release of the two drugs in a bilayer tablet. IR-immediate release, SR-sustain release, NBL8-Nebivolol 8, N9-Nateglinide 9.

  17. Clinical Evaluation of Oral Valaciclovir Hydrochloride Tablets Pidotimod Tablets in the Treatment of Recurrent Genital Herpes%评价口服盐酸伐昔洛韦片联合匹多莫德片治疗复发性生殖器疱疹的临床疗效

    Institute of Scientific and Technical Information of China (English)

    何志光; 姜乐

    2016-01-01

    目的:分析和评价口服盐酸伐昔洛韦片联合口服匹多莫德片治疗复发性生殖器疱疹的临床疗效。方法选取我院2014年4月~2015年10月收治的82例复发性生殖器疱疹患者,按照抽签法将患者平均分为观察组和对照组,观察组患者接受盐酸伐昔洛韦片联合匹多莫德片的治疗,对照组患者仅接受盐酸伐昔洛韦片的治疗,比较临床疗效。结果观察组患者治疗有效率更高(97.56%vs.80.49%,χ2=4.493,P<0.05)、复发率更低(43.90%vs.70.73%,P<0.05)。结论盐酸伐昔洛韦片联合匹多莫德片口服治疗复发性生殖器疱疹临床疗效显著,可提高患者治疗有效率、降低复发率。%Objective Clinical analysis and evaluation of oral and oral valaciclovir hydrochloride tablets pidotimod tablets in the treatment of recurrent genital herpes.MethodsIn our hospital from April 2014 to October 2015, 82 cases of recurrence of genital herpes patients, according to the draw method patients were divided into the observation group and the control group and observation group patients were treated with valaciclovir hydrochloride valacyclovir tablets combined with pidotimod tablets, patients in the control group only received the treatment of valaciclovir hydrochloride tablets, compared the clinical efifcacy.Results The effective rate of the observation group was higher (97.56%vs. 80.49%, χ2=4.493,P< 0.05), and the recurrence rate was lower (43.90%vs. 70.73%,P < 0.05). Conclusion Hydrochloride cutting valacyclovir tablets combined with pidotimod tablets oral in the treatment of recurrent genital herpes clinical curative effect significantly, improve treatment efficiency and reduce the recurrence rate.

  18. Process Modeling in Dissolution Method of Glucosamine Hydrochloride Tablets%盐酸氨基葡萄糖片的溶出度方法及模型建立

    Institute of Scientific and Technical Information of China (English)

    朱毅; 刘佳佳

    2015-01-01

    采用紫外分光光度法建立了盐酸氨基葡萄糖片溶出度的测定方法,测定了不同溶出介质(水、0.1 mol/L盐酸溶液和0.01 mol/L盐酸溶液)、不同转速(50 rpm、75 rpm、100 rpm)下盐酸氨基葡萄糖片的溶出曲线。经方法学验证,本文建立的测定条件简单易行,准确度高。采用Origin 软件对盐酸氨基葡萄糖片全溶曲线进行Weibull曲线拟合计算,拟合度好,且拟合图形和样品的全溶出曲线一致。%UV spectrophotometric determination was employed to detecting the dissolution curve of glucosamine hydrochloride tablets with the different medium ( water, 0. 1 mol/L hydrochloric acid and 0. 01 mol/L hydrochloric acid) and speed (50 r/min, 75 r/min and 100 r/min). The optimal determination of glucosamine hydrochloride tablets was established by dissolution test method validation which turned to be simple and accurate. Curve fitting by origin software showed the same dissolution of glucosamine hydrochloric tablets with the complex distribution of Weibull’s Type.

  19. Development and validation of a gas chromatographic method for the assay of memantine hydrochloride in pure and tablet dosage forms

    Directory of Open Access Journals (Sweden)

    Siddappa K.

    2011-01-01

    Full Text Available A gas chromatographic method has been developed and validated for the determination of memantine hydrochloride (MMT in pure and pharmaceutical preparations. The detection was carried out using flame ionization detector. Separation was achieved on a DB-624 fused silica packed capillary column (30 m x 0.320 mm x 1.8 μm. Nitrogen was used as a carrier gas at a flow rate of 40 mL/min. The column temperature was maintained at 300°C while the temperature of injection port and detector were maintained at 270° and 300°C, respectively. Gabapentin (GPN was used as an internal standard. The procedure gave a linear response over the concentration range of 0.5-3.5 mg/mL with sufficient reproducibility. The method has been applied successfully for the determination of MMT in pure and pharmaceutical formulations. The excipients present in the formulations did not interfere with the assay procedure. The recovery values were found to be in the range of 99.85-100.1% with RSD values less than 1%. The results obtained from this method were compared with the reference method (HPTLC reported in literature and no significant difference was found statistically.

  20. Determination of Pyridoxine Hydrochloride in Luojijiangya Tablets by HPLC%HPLC法检测罗己降压片中盐酸吡哆辛含量

    Institute of Scientific and Technical Information of China (English)

    刘信奎

    2015-01-01

    目的:建立HPLC法测定罗己降压片中盐酸吡哆辛含量。方法:使用十八烷基硅烷键合硅胶为填充剂,以0.04%戊烷磺酸钠溶液(用冰醋酸调节p H至3.0)-甲醇(85:15)为流动相,检测波长为291n m进行测定。流速1.0m L•m i n-1,柱温35℃。结果:平均加样回收率盐酸吡哆辛为99.04%,RSD=0.17%(n=9)。盐酸吡哆辛在0.4000~1.600μg范围内,进样量与峰面积值呈良好的线性关系(r=0.9999)。结论:方法简便、结果准确、重现性好,可为罗己降压片的质量控制提供依据。%ObjectiveHPLC method was established for the determination of Pyridoxine Hydrochloride in Luojijiangya Tablets. Methods ODS C18 column was used. The mobile phase was 0.04% sodium pentanesulfonate(adjusted to pH 3.0 with acetic acid)-methanol(85:15). The detection wavelength was 291nm. The flow rate was 1.0 mL•min-1 with the column temperature at 35℃. Results The average recoveries were 99.04%,RSD=0.17%(n=9). The linear range of Pyridoxine was within 0.4000~1.600µg (r=0.9999). Conclusion T he method is simple, accurate, stableand reliable. It can be used for quality control of Luojijiangya tablets.

  1. First derivative synchronous fluorescence spectroscopy for the simultaneous determination of sulpiride and mebeverine hydrochloride in their combined tablets and application to real human plasma.

    Science.gov (United States)

    Walash, M; Sharaf El-Din, M; El-Enany, Nahed; Eid, M; Shalan, Sh

    2010-11-01

    A rapid, simple and highly sensitive first derivative synchronous fluorometric method has been developed for the simultaneous analysis of binary mixture of sulpiride (SUL) and mebeverine hydrochloride (MEB). The method is based upon measurement of the synchronous fluorescence intensity of these drugs at ∆λ = 100 nm in water. The different experimental parameters affecting the fluorescence of the two drugs were carefully studied and optimized. The fluorescence-concentration plots were rectilinear over the range of 0.05-1 µg/mL and 0.2-3.2 µg/mL for SUL and MEB respectively with lower detection limits (LOD) of 0.006 and 0.01 µg/mL and quantification limits (LOQ) of 0.0.02 and 0.05 µg/mL for SUL and MEB, respectively. The proposed method was successfully applied for the determination of the two compounds in synthetic mixtures and in commercial tablets. The high sensitivity attained by the proposed method allowed the determination of both of SUL and MEB metabolite (veratic acid) in real human plasma samples applying second derivative synchronous fluorometric technique. The mean% recoveries (n = 3) for both MEB metabolite (veratic acid) and SUL were 99.82 ± 2.53 and 98.84 ± 6.20 for spiked human plasma respectively, while for real human plasma, the mean% recoveries (n = 3) were 91.49 ± 4.25 and 91.36 ± 8.46 respectively.

  2. 1 Cases of Extrapyramidal Symptoms Caused by Comound Paracetamol and Amantadine Hydrochloride Tablets%复方氨酚烷胺片致锥体外系症状1例

    Institute of Scientific and Technical Information of China (English)

    张良芬; 赵韵超

    2014-01-01

    复方氨酚烷胺片不良反应为白细胞或血小板减少、食欲缺乏、恶心、呕吐、皮疹等。本文介绍因感冒自行服用"复方氨酚烷胺片(新秀)2片"后外出活动时突发全身不自主抖动,实属罕见,给予停服复方氨酚烷胺片,加用银杏达莫注射液(杏丁)输注5d后症状逐渐减轻,直至消失。出现的锥体外系症状副反应可能与特异体质或体敏感性有关。一旦有该症状,应立即停用药物,避免锥体外系等不良反应的发生。%The adverse reactions Comound Paracetamol and Amantadine Hydrochloride Tablets white cellor platelet reduction, lack of appetite, nausea, vomiting, skin rash. In this paper because of cold to take"Comound Paracetamol and Amantadine Hydrochloride Tablets (Rookie) 2"after traveling burst body involuntary jit er, rare, give of Comound Paracetamol and Amantadine Hydrochloride Tablets, plus Ginkgo Leaf Extract and Dipyridamole Injection (Xing Ding) infusion of 5 days after the symptoms gradual y reduced, until it disappeared. Extrapyramidal side ef ects may be related to the special physique or body sensitivity. Once the symptoms, should immediately stop using the drug, avoid adverse reaction of extrapyramidal system etc.

  3. Clinical studies of severe cancer pain oxycodone hydrochloride sustained-release tablets in the treatment of%盐酸羟考酮缓释片治疗中重度癌痛的临床研究

    Institute of Scientific and Technical Information of China (English)

    李成彪; 王玉珮; 齐雪花; 罗艳琴

    2015-01-01

    ObjectiveTo observe the oral oxycodone hydrochloride sustained-release tablets were administered the back-ground of moderate to severe cancer pain titration, titration analysis of efficacy and safety in order to reasonably extended release formulation of oxycodone titration improve moderate to severe cancer pain pain, improve the quality of life of patients. Methods in April 2011 to June 2013 to 116 cases with moderate to severe cancer pain patients in this study, should be completed im-mediately BPI pain scale outbreak. Taking oxycodone hydrochloride sustained-release tablets 10mg one hour after pain assess-ment, such as pain can not be controlled, preclude the use of immediate-release morphine titrated until pain control. Record achieve pain control titration number of cycles needed, while also recording the life quality improvement and evaluation of drug safety before and after treatment. Selected results of 116 cases of cancer pain, moderate pain 104 cases, 12 patients with severe cancer pain, male 80 cases, female 36 cases, in the course of treatment, pain control to compare different sex ratio, chi-square value = 0.006, P=0.938, no significant difference difference; compare pain control rate of the different nature of pain, the chi-square value = 2.377, P=0.305 comparing the difference was not significant difference varying degrees of pain Comparison of pain control rate, chi-square value = 20.135, P=0.000, there was a significant difference comparing the difference; compare different ages pain control rate, the chi-square value = 0.041, P=0.839, comparing the difference was not significant differ-ence. Comparison of different intensity of pain titration period, t=-3.683, P=0.13, the degree of pain pain control cycle impact;the groups before and after comparison of complications, chi-square =33.294, P=0.000, patient into After the set of concurrent symptoms of nausea, vomiting accounted for 6.90%, accounting for 70.69 percent of constipation, urinary

  4. Clinical Analysis on the Treatment of Peptic Ulcer by Ranitidine Hydrochloride Tablets Combine Omeprazole Sodium for Injection%雷尼替丁联合奥美拉唑治疗消化性溃疡的临床研究

    Institute of Scientific and Technical Information of China (English)

    孙晓春

    2015-01-01

    目的:探究消化性溃疡患者采用雷尼替丁联合奥美拉唑综合治疗的效果。方法选取2013年2月~2014年3月收治的40例消化性溃疡患者进行治疗,随机分组,实验组23例患者采用雷尼替丁和奥美拉唑的综合治疗,对照组17例患者选择雷尼替丁的治疗,对比疗效。结果实验组患者治疗有效率为91.30%,复发率为8.7%,对照组治疗有效率为76.47%,复发率为29.4%。两组患者的治疗效果和复发率差异有统计学意义(P<0.05)。结论消化性溃疡患者采用雷尼替丁和奥美拉唑的综合治疗,能够缓解恶心等胃肠道反应,复发率低,效果显著。%Objective To explore the effect on the treatment of peptic ulcer by ranitidine hydrochloride tablets combine omeprazole sodium for injection. Methods We divided the 40 patients into control group(17 cases)and experimental group(23 cases). Al the cases were chosen from February 2013 to March 2014. The patients in the experimental group adopted the ranitidine hydrochloride tablets combine omeprazole sodium for injection treatment and the control group adopted the ranitidine hydrochloride tablets treatment. We compared the difference beteen the two groups. Results The effective rate in the experimental group was 91.30%,and the recurrence rate was 8.7%. The effective rate in the control group was 76.47%,and the recurrence rate was 29.4%. It was in a high treatment efficiency and obvious difference between the two groups and the statistical y significant(P<0.05). Conclusion The patients with peptic ulcer adopt the ranitidine hydrochloride tablets combine omeprazole sodium for injection treatment wil obviously al eviate gastrointestinal reactions such as nausea. The recurrence rate was lower than others.

  5. Determination of Acetaminophen in Compound Paracetamol and Amantadine Hydrochloride Capsules and Tablets by HPLC%HPLC法对二种复方氨酚烷胺制剂中对乙酰氨基酚含量测定

    Institute of Scientific and Technical Information of China (English)

    苏彦文; 张凤荣; 苏彦斌

    2012-01-01

    Purpose:The method of determining content of acetaminophen in compound paracetamol and amantadine hydrochloride capsules and tablets by HPLC is established.The determination of acetaminophen in compound paracetamol and amantadine hydrochloride capsules and tablets was carried on a column of agilent C18,150×4.6 mm,5 μm,by HLPC.The mobile phase was 7525 of methanol-0.4% glacial acetic acid,the flow rate maintained at 0.7 mlomin-1.The detection wavelength was 249 nm and the column temperature was 30 ℃.The results show that the sample size in determination by HPLC for acetaminophen in compound paracetamol and amantadine hydrochloride capsules and tablets was between 0.093 μg and 0.93 μg,for ideal linearity,r=0.999 9.The average recoveries was 98.83% with the RSD=0.69%,n=9.Conclusion:The method is accurate and reliable for quality control of acetaminophen in compound paracetamol and amantadine hydrochloride capsules and tablets.%目的:建立复方氨酚烷胺制剂中对乙酰氨基酚的HPLC含量测定方法.方法:色谱柱Agilent C18柱(150 min×4.6 mm,5μm),V(甲醇)V(0.4%冰醋酸溶液)为75 25为流动相,流速:0.7 mL.min-1,检测波长为249 nm,柱温:30℃.结果对乙酰氨基酚在0.093~0.93μg范围内线性关系良好(r=0.999 99).平均回收率为99.83%,RSD=0.69%(n=9).结论:方法准确可靠,可作为复方氨酚烷胺片剂和胶囊的质量控制方法.

  6. SIMULTANEOUS ESTIMATION OF MEFENAMIC ACID AND DICYCLOMINE HYDROCHLORIDE BY SPECTROSCOPIC METHODS

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    D.N. Prajapati et al

    2012-10-01

    Full Text Available A novel, simple, accurate, sensitive, reproducible, economical spectroscopic method was developed and validated for the determination of Mefenamic acid and Dicyclomine hydrochloride in combined dosage form. Three different analytical methods, Absorption correction method, Differential derivative method, Simultaneous equation method were developed for estimation of Dicyclomine hydrochloride(10mg and Mefenamic acid (250mg in tablet dosage form. wavelength for estimation was 223nm for Dicyclomine hydrochloride and 308.60nm for Mefenamic acid in absorption correction method. 211.60nm was Zero crossing point of Mefenamic acid and 308.80nm was Zero crossing point of Dicyclomine hydrochloride which can estimate in differential derivative method. Simultaneous equation method was developed in NaOH which was linear in the range of 1-6µg/ml for Dicyclomine hydrochloride and 25-150µg/ml for Mefenamic acid, the correlation coefficient obtained was nearer to one. The method was validated for linearity, accuracy and precision as per ICH guidelines. The developed and validated method was successfully used for the quantitative analysis of commercially available dosage form.

  7. Determination of Artesunate and Amodiaquine Hydrochloride Tablets by RP-HPLC%RP-HPLC法测定青蒿琥酯阿莫地喹片中主药的含量

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    胡志强; 蒋锋; 姚忠

    2014-01-01

    A method for the determination of artesunate and amodiaquine hydrochloride tablets by RP-HPLC was established.The agilent C18(4.6 mm×15 cm)column was used,and the detection wavelength of artesunate was 210 nm.The mobile phase of artesunate was acetonitrile and the buffer solution.The detection wavelength of amodiaquine hydrochloride was 224 nm.The mobile phase of amodiaquine hydrochloride was methanol:phosphate buffer.The linear ranges of artesu-nate (0.500 5-2.002 mg/mL)and amodiaquine hydrochloride (25.03-100.1μg/mL)were good (r=0.999)with the average recovery rates of 98.6%and 99.5%.The method is simple and accurate,and it can be used for the determination of artesunate and amodiaquine hydrochloride tablets.%建立RP-HPLC法测定青蒿琥酯阿莫地喹片中主药的含量。色谱柱为安捷伦的C18柱(4.6 mm×15 cm),测定青蒿琥酯的流动相为乙腈-磷酸盐缓冲液,检测波长为210 nm,测定阿莫地喹的流动相为甲醇-磷酸盐缓冲液,检测波长为224 nm。在考察青蒿琥酯(0.5005~2.002 mg/mL)和阿莫地喹(25.03~100.1μg/mL)的质量浓度范围内具有良好的线性关系,r均达到0.999,平均回收率分别为98.6%和99.5%。结果表明,两套分析方法测定主药的含量,结果准确、可靠。

  8. Preparation and quality evaluation of Mucoadhesive Buccal Tablets of Tiazanidine Hydrochloride%盐酸替扎尼定口腔黏附片的研制及质量评价

    Institute of Scientific and Technical Information of China (English)

    杨晓艳; 张友智; 耿立坚

    2014-01-01

    目的:制备盐酸替扎尼定口腔黏附片并评价其质量。方法采用不同配比的羟丙甲基纤维素(H PM C )、羧甲基纤维素钠(SCMC)、β-环糊精和羟丙基-β-环糊精等辅料,用直接压片法压片制备盐酸替扎尼定口腔黏附片,并对黏附片的理化性质、药物含量、药物体外释放度和黏附力进行评价。结果得到各项指标均较适宜的处方:盐酸替扎尼定4.56 mg ,羟丙甲纤维素20 mg ,羧甲基纤维素钠75mg,羟丙基-β-环糊精27.36mg,甘露醇4mg,阿斯巴甜1mg,微粉硅胶1mg。结论成功制备了盐酸替扎尼定口腔黏附片,可用于进一步的体内、体外研究。%Objective To prepare and evaluate a buccal adhesive tablet containing tiazanidine hydrochloride .Methods The tablets were prepared by using hydroxypropyl methyl cellulose (HPMC ) ,sodium carboxymethylcellulose (SCMC ) ,β-cyclodextrin , hydroxypropyl-β-cyclodextrin ,etc as the auxiliary materials .Direct compression process was used to prepare the buccal adhesive tablets ,and different parameters such as physicochemical property ,drug content ,in vitro drug release ,and mucoadhesive strength were evaluated .Results The prescription was as follows :tiazanidine hydrochloride 4 .56 mg ,hydroxypropyl methyl cellulose 20 mg ,sodium carboxymethylcellulose 75 mg ,hydroxypropyl-β-cyclodextrin 27 .36 mg ,mannitol 4 mg ,aspartame 1 mg and aerosil 1 mg .Conclusion The buccal adhesive tablets of tiazanidine hydrochloride were prepared successfully ,and which can be used for the further study both in vivo and in vitro .

  9. 盐酸阿莫地喹片溶出度测定的方法学研究%Studies on Methodological Validation of Solubility of Amodiaquine Hydro-chloride Tablets

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    岳莉

    2014-01-01

    OBJECTIVE To validated the methodology detection of solubility of Amodiaquine Hydrochloride Tablets.METHODS The detection was carried out following the procedure described in the second method in ap-pendix ⅩC,second part of 2010 edition of Chinese Pharmacopoeia.The solubility of Artesunate Tablets was detected with ultraviolet spectrophotometry at 342nm.According to the results ,we validated it methodology.RESULTS The determination of Amodiaquine Hydrochloride Tablets was carried out by using this method ,respectively in pH 1.2, 4.5 ,6.8 ,four water dissolution medium ,we performed a linear regression analysis by using the concentration and UV absorption as independent and dependent variables respectively.Within the concentration range of 4~25μg· mL-1 , excellent linear relevance was witnessed between concentration and absorption.In the above four kinds of dissolution medium average recovery and standard deviation were conform to the requirements.CONCLUSION The dissolubil-ity determination Amodiaquine Hydrochloride Tablets method can be used for the quality control of products .%目的:对盐酸阿莫地喹片的溶出度检查进行方法学验证。方法参照《中国药典》2010年版二部附录ⅩC第二法对其溶出度进行检查。采用紫外分光光度法,在342 nm的波长处测定吸光度,进行了方法学验证。结果采用该方法测定盐酸阿莫地喹片,分别在pH 1.2、4.5、6.8的缓冲溶出介质及水4种溶出介质中,以浓度对吸收度进行线性回归,盐酸阿莫地喹在4~25μg · mL -1范围内浓度与吸收度呈良好的线性关系。在以上4种溶出介质中的平均回收率和标准偏差均符合要求。结论本法测定盐酸阿莫地喹片溶出量方法可行,可用于该产品的质量控制。

  10. 盐酸美沙酮片维持治疗重度或难治性癌性疼痛效果分析%Effect of Methadone Hydrochloride Tablets in the Treatment of Severe or Refractory Cancer Pain

    Institute of Scientific and Technical Information of China (English)

    孙建明

    2015-01-01

    Objective To explore the analgesic effect and safety of methadone hydrochloride tablets in the treatment of severe or refractory cancer pain.Methods 68 cases of advanced cancer patients with severe or refractory cancer pain,were al used morphine tablets titration,when the pain intensity was less than or equal to 3 points used methadone hydrochloride tablets maintenance treatment.ResultsThere was a significant difference in the analgesic effect of 2,4,6 and 8 during the treatment of methadone hydrochloride tablets(P< 0.05). The adverse reaction rate in the patients of dizziness,nausea vomiting, constipation, cold sweat and lethargy was7.4%、2.9%、19.1%、1.5%、2.9%.Conclusion Analgesic effect of severe or refractory cancer pain treated by methadone maintenance treatment is good, safe and high.%目的:探究盐酸美沙酮片维持治疗重度或难治性癌性疼痛的效果。方法选取存在重度或难治性癌性疼痛的晚期癌症患者68例,均采用吗啡片滴定,待疼痛强度≤3分后转换为盐酸美沙酮片维持治疗。结果盐酸美沙酮片维持治疗期间患者第2、4、6和8周末镇痛效果比较,差异存在统计学意义(P<0.05);患者头晕、恶心呕吐、便秘、冷汗以及嗜睡等不良反应发生率分别为7.4%、2.9%、19.1%、1.5%、2.9%。结论重度或难治性癌性疼痛采用盐酸美沙酮维持治疗镇痛效果良好,安全性高。

  11. Principles for quality evaluation of marketed metformin hydrochloride tablets%市售盐酸二甲双胍片的质量评价

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    薛晶; 邹文博; 崔学文; 马文利; 薛立宁; 胡昌勤

    2011-01-01

    Objective: To compare the quality of generic drugs manufactured by domestic pharmaceuticals with the original product and list principles for quality evaluation of marketed drugs with metformin hydrochloride tablets as an example. Methods: Based on three basic elements of drugs ( safety, efficacy and quality control),comparison and evaluation of the quality were performed on related substances, dissolution and content, which closely related to clinical efficiency. Results: In related substances and content, domestically produced generic drugs and the original product were equivalent, but there were differences on dissolution. Conclusion: Compared with the original product, the safety and quality control of domestically produced generic drugs are satisfactory.However, whether the in vivo bioavailability, clinical efficiency and side effects of some domestic samples are entirely consistent with the original product or not will be further explored.%目的:以盐酸二甲双胍片为例,从药物分析角度对国产仿制药的质量与原研厂的产品质量进行对比研究,浅析上市药品质量评价的几点原则.方法:从药品的安全性、有效性和质量可控性3个基本要素出发,选择具有临床意义的有关物质、溶出度和含量等指标进行比较和评价.结果:国产仿制药与原研厂产品在有关物质和含量方面的质量相当,但溶出度存在差异.结论:与原研厂产品相比,国产仿制药的安全性和质量可控性令人满意,但部分厂家的样品与原研厂产品在体内生物利用度、临床疗效及副作用方面是否完全一致有待进一步的探讨.

  12. Clinic Observation of Methadone Hydrochloride Tablets as Therapy for 39 Patients with Refractory Cancer Pain%盐酸美沙酮片治疗难治性癌症疼痛39例临床观察

    Institute of Scientific and Technical Information of China (English)

    黄莎; 黄诚; 张晶; 陈奕贵

    2016-01-01

    Objective To evaluate the efficacy and safety of Methadone Hydrochloride Tablets as therapy for patients with refractory cancer pain. Methods Advanced cancer with cancer pain were consecutively enrolled in this study. Patients were applied oral morphia or oxycodone titration, when their pain intensity still NRS>3, then replace Methadone Hydrochloride Tablets to treatment. Use a medicine for full 2 weeks, is a qualified case. Results 39 patients with refractory cancer pain who accept Methadone Hydrochloride Tablets treatment, the treatment time is 2-9 weeks. After treatment of Methadone Hydrochloride Tablets two weeks, their pain intensity has decreased (P<0.05), pain treatment efficient is 84.61%. An average dose of Methadone Hydrochloride Tablets is (51.67±52.81)mg by the second weekend, 87.18% of patients within 2 times to take medicine in the 39 patients by the second weekend. The incidence of adverse events under 3% of dizziness, drowsiness, fatigue, nausea, vomiting, constipation rate is 25.64%.There are no case of serious adverse events correlative with Methadone Hydrochloride Tablets, laboratory examination found no effect on liver and kidney function and no electrocardiogram (ecg) change. Conclusions Methadone Hydrochloride Tablets has definite analgesic effect for refractory cancer pain, dosage is significantly lower than that of morphine or oxycodone. As the stable analgesic dose, 2 times daily medication only. The clinical manifestations of the adverse reactions and the incidence is similar to morphine and other opioids.%目的:观察盐酸美沙酮片用于难治性癌痛的镇痛效果及其安全性。方法对重度癌痛患者给予吗啡即释片或羟考酮滴定,滴定期间每日使用吗啡剂量≥120 mg 或羟考酮剂量≥60 mg 且疼痛强度评分仍然 NRS >3分,属于难治性癌痛,给予转换为盐酸美沙酮片止痛,用药满2周者为合格病例。结果筛选出39例难治性癌痛患者接受盐酸美沙

  13. Efficacy Comparison of Oxycodone Hydrochloride Controlled-release Tablets and Tramadol Hydrochloride Sustained-release Tablets in the Treatment of Moderate Cancer Pain%盐酸羟考酮缓释片与曲马多缓释片治疗中度癌痛的近期疗效比较

    Institute of Scientific and Technical Information of China (English)

    张锦丰; 杨权烈; 吴国武; 郭维新; 张英燕; 古银芳; 叶敏

    2014-01-01

    目的:比较盐酸羟考酮缓释片(奥施康定)与曲马多缓释片(奇曼丁)治疗中度癌痛的近期疗效。方法将100例伴有中度癌痛患者随机分为奥施康定组和奇曼丁组,每组50例,分别接受奥施康定和奇曼丁的治疗。结果奥施康定组治疗后第3、7、10天的NRS评分均较奇曼丁组低,且奥施康定组治疗后第3天NRS评分下降幅度较奇曼丁组明显( P﹤0.05);奥施康定组的CR率和有效率分别为34.0%和100.0%,明显高于奇曼丁组的10.0%和84.0%(P﹤0.05);2组毒副反应发生率比较差异均无统计学意义(P﹥0.05)。结论与奇曼丁相比,应用奥施康定治疗中度癌痛患者,能更快更有效缓解疼痛,而未增加毒副反应。%Objective To compare the efficacy and tolerability of oxycodone hydrochloride controlled-release tab-lets( oxycodone)and tramadol hydrochloride sustained-release tablets( tramadol)in the treatment of patients with moderate cancer pain. Methods A total of 100 patients with moderate cancer pain were randomly divided into two groups,50 patients of the oxycodone group was treated with oxycodone,and 50 patients of the tramadol group was treated with tramadol. Results The NRS scorce in the oxy-codone group had declined more significantly than the tramadol group,and the decrease was statistically significant in the first three days (P﹤0. 05). The CR rate and the response rate in the oxycodone group were significantly better than those of the tramadol group (34.0% vs10.0% and100.0% vs84.0%)(P﹤0.05).There was no statistic significant difference in the toxicity incidences be-tween the two groups(P﹥0. 05). Conclusion Compared with tramadol,oxycodone is faster and more effective to relieve pain,and don’t increase the toxicities.

  14. DEVELOPMENT AND VALIDATION OF STABILITY-INDICATING TLC-DENSITOMETRY METHOD FOR THE SIMULTANEOUS DETERMINATION OF EPERISONE HYDROCHLORIDE AND PARACETAMOL IN BULK AND TABLET DOSAGE FORM

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    Pritam S. Jain

    2013-08-01

    Full Text Available A rapid and reproducible stability indicating TLC-densitometric method was developed for the determination of eperisone hydrochloride and paracetamol in presence of their degraded products in bulk drugs and pharmaceutical formulations. Uniform degradation conditions were maintained by refluxing reaction mixtures for 8 h at 60°C including acidic, alkaline hydrolysis. Oxidation at room temperature, photochemical and dry heating degradation studies were also carried out. A sensitive and robust stability indicating TLC-densitometric method for simultaneous quantification of eperisone hydrochloride and paracetamol in bulk drugs and pharmaceutical formulations has been developed and validated. Separation was done on TLC aluminum sheets, pre-coated with silica gel 60F-254 using ethyl acetate: toluene: methanol (2:2:1 v/v/v. Spots at Rf 0.42 ± 0.04 and Rf 0.60 ± 0.02 were recognized as paracetamol and eperisone hydrochloride, respectively. Densitometric analysis of chromatoplates was carried out in absorbance mode at isobastic point 260 nm. The developed method was optimized and validated as per ICH guidelines. Method was found linear over the concentration range of 100-350 ng / spot for eperisone hydrochloride and 600-2100 ng / spot for paracetamol with the correlation coefficient (r2 of 0.999 and 0.999 for eperisone hydrochloride and paracetamol, respectively. The developed TLC method can be applied for routine analysis of eperisone hydrochloride and paracetamol in presence of their degraded products in their combined pharmaceutical formulations.

  15. Preparation of oral osmotic pump tablets of terazosin hydrochloride%正交试验优化盐酸特拉唑嗪渗透泵控释片生产工艺

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    马廷升; 李高; 宋思才; 刘志华; 朱兰寸

    2011-01-01

    目的 研究盐酸特拉唑嗪渗透泵控释片生产的最佳工艺.方法 采用正交实验设计L3(34),以药物25 h累积释药百分率为评价指标筛选工艺.结果 优选实验因素:促渗剂用量为(w/w)20%、促渗透聚合物CMC-Na用量(w/w)为6%、包衣液增重(w/w)为4%、释药孔径为600μm.渗透泵控释片25 h累积释药百分率平均值为82.6%,RSD为2.65%(n=5).结论 由正交试验筛选制备盐酸特拉唑嗪渗透泵控释片的工艺条件是可靠的,为该药的靶向制剂、缓控制剂的药剂学研究奠定基础.%Objective To determine the best preparation craft of oral osmotic pump tablets of terazosin hydrochloride.Methods Taking the 25 h cumulative drug delivering percentage as the index, the oral osmotic pump tablets of terazosin hydrochloride were prepared by ultrasonic dispersing method with orthogonal design L9 (34 ). Results Optimal experiment factors were as follows: the dosage of penetration enhancers agent was 20% (ω/ω), the dosage of penetration enhancers polymer CMC-Na was 6% (ω/ω), the weight increment of coating liquid was 4% (ω/ω), and the aperture of drug delivering was 600 μm. The average cumulative delivering percentage of drug was 82. 6%, and RSD was 2. 65% (n=5). Conclusion The preparation of oral osmotic pump tablets of terazosin hydrochloride by ultrasonic dispersing method and orthogonal design is suitable, which lays the foundation for the extended-release preparation study.

  16. Treatment of lantus and metformin hydrochloride and glibenclamide tablets on primary type 2 diabetesy%来得时联合拜唐平治疗初发Ⅱ型糖尿病疗效观察

    Institute of Scientific and Technical Information of China (English)

    曲建梅; 王晓梅

    2013-01-01

    目的 观察来得时联合拜唐平治疗初发Ⅱ型糖尿病的临床疗效,并作安全性评价.方法 将符合初发Ⅱ型糖尿病纳入标准病例90例,按入院顺序随机分为治疗组45例与对照组45例,对照组予以诺和灵30R治疗,治疗组给予来得时联合拜唐平治疗,比较两组的疗效,以及两组治疗前后各项实验室指标的变化情况.结果 治疗组总有效率明显优于对照组(P<0.05),且治疗组在降低空服血糖、餐后2小时血糖及糖化血红蛋白水平方面均明显优于对照组(P<0.05或P<0.01).治疗组低血糖发生率明显低于对照组,差异有统计学意义(P<0.05).结论 来得时联合拜唐平治疗初发Ⅱ型糖尿病疗效确切,安全有效,低血糖发生率低,值得临床推广应用.%Objective To observe the efficacy of lantus and metformin hydrochloride and glibenclamide tablets on primary type 2 diabetes.Methods 90 cases were randomly divided into treatment group (45 cases) and the control group (45 cases).The treatment group was treated with lantus and metformin hydrochloride and glibenclamide tablets and the control group with Novolin.The laboratory parameters before and after treatment were observed.Results The treatment group in the lower flight blood glucose 2-hour postprandial blood glucose and glycosylated hemoglobin levels significantly better than the control group (P<0.05 or P<0.01).The incidence of hypoglycemia in the Treatment group was significantly lower than that of the control group.The difference was statistically significant (P<0.05).Conclusion It is safe and effective to treat primary type 2 diabetes with lantus and metformin hydrochloride and glibenclamide tablets.

  17. 高效液相色谱法测定盐酸倍他司汀片的有关物质%Determination of Related Substances in Betahistine Hydrochloride Tablets by HPLC

    Institute of Scientific and Technical Information of China (English)

    王冬; 董煜; 钱小平; 秦彩明; 张瑜

    2013-01-01

    Objective To establish a HPLC method for the determination of the related substances in Betahistine Hydrochloride Tablet.Methods The chromatographic column was the C18 column(250 mm×4.6 mm,5 μm),the mobile phase consisted of mixed solution (taking NaH2PO4 2.76 g and sodium dodecyl sulfate 1.60 g for dissolution with 600 mL of water)-acetonitrile-hexylamine (600 ∶ 400∶1.6,adjusted to pH 3.5 with phosphoric acid) at the flow rate of 1.0 mL/min and the detection wavelength was set at 254 nm,the column temperature was 50 ℃ and the injection volumes was 100 μL.Results Betahistine hydrochloride and the impurity peaks were separated well.The lowest limit of quantitation for betahistine hydrochloride was 0.2 μg/mL.Conclusion This method is strongly specific and highly sensitive with accurate result,and can be used for the quality control of Betahistine Hydrochloride Tablets.%目的 建立测定盐酸倍他司汀片有关物质含量的高效液相色谱法.方法 采用C18色谱柱(250 mm×4.6 mm,5μm),以混合溶液(取磷酸二氢钠2.76g和十二烷基硫酸钠1.60g,用水600 mL溶解)-乙腈-己胺(600∶400∶1.6,用磷酸调pH至3.5)为流动相,检测波长254 nm,流速为1.0 mL/min,柱温50℃,进样量100μL.结果 盐酸倍他司汀与杂质峰之间分离良好,盐酸倍他司汀的最低定量限为0.2 μg/mL.结论 该方法专属性强、灵敏度高、结果准确,可用于盐酸倍他司汀片的质量控制.

  18. 盐酸二甲双胍肠溶片上市后人体生物等效性再评价%Post-Marketing Reevaluation of Bioequivalénce of Metformin Hydrochloride Enteric-Coated Tablets

    Institute of Scientific and Technical Information of China (English)

    张丹; 王振龙; 王涛; 刘会臣; 杨漫; 韩静; 王晓琳; 张丽娜; 张娅喃; 肖雪; 杜爱华; 刘曼

    2012-01-01

    OBJECTIVE To reevaluate the bioequivalence of marked metformin hydrochloride enteric-coated tablets. METHODS Using method 2 described in the appendix X D and apparatus 1 described in the appendix X C in Chinese Pharmacopoeia (edition 2010) , the in vitro release of metformin hydrochloride enteric-coated tablets from different pharmaceutical factories ( A,B,C,and D) was investigated. The contents were measured by utlraviolet ( UV) spectroscopy. Generic tablets from factory A and D were chosen to be test 1 and test 2 preparations, with the innovative metformin hydrochloride tablets (Glucophage) as the reference preparation. In a randomized, three-way crossover study,21 healthy male volunteers were given a single oral dose of test 1 ,test 2 and reference preparations containing 500 mg of metformin hydrochloride. Plasma concentrations of metformin were determined by LC-MS/MS. The pharmacokinetic parameters and relative bioavailability were calculated. The bioequivalence between test 1 and reference preparation,test 2 and reference preparation, and the bioequivalence between the two test preparations were evaluated. RESULTS The in vitro release of metformin hydrochloride enteric-coated tablets from factory B,C and D met the standard of Chinese Pharmacopoeia (the supplement edition of 2010) while that of the tablets from factory A did not. Metformin hydrochloride enteric-coated tablets from factory A and D were chosen to be test 1 and test 2 preparations,respectively. The FO-t and FO-∞ were (72. 8±9. 7) % and (73. 2±10. 0) % for test 1 preparation,and (45. 5 ±16. 2) % and (46. 2±16. 0) % for test 2 preparation,respectively. It was failed to conclude that test 1 and reference preparation were bioinequiva-lent. Test 2 and reference preparation were bioinequivalent, and the two test preparations were also bioinequivalent. CONCLUSION The bioinequivalence risk of metformin hydrochloride enteric-coated tablets is high. For metformin hydrochloride enteric-coated tablets

  19. Optimizing the preparation of doxycycline hydrochloride sustained release tablet using response surface methodology%响应面法优化盐酸多西环素缓释片处方工艺

    Institute of Scientific and Technical Information of China (English)

    喻佰启; 王永禄; 殷海翔; 王栋; 吕贝贝; 李学明

    2014-01-01

    目的:利用响应面分析法优化盐酸多西环素缓释片处方。方法通过单因素考察确定对释放度影响最大的3个因素:羟丙基甲基纤维素(hydroxypropyl methyl cellulose,HPMC)的用量、粘合剂聚乙烯吡咯烷酮-K30(polyvinylpyrrolidone-K30,PVP-K30)的浓度、乳糖与微晶纤维素(microcrystalline cellulose,MCC)的比例,以2 h、4 h、8 h 的释放度综合评分作为响应值,利用 Box-Benhnken中心组合实验设计原理,采用三因素三水平的响应面分析法,确定各处方的用量。结果筛选得到优化的处方为:HPMC K15质量分数为片重的30%、粘合剂PVP-K30浓度为10%、乳糖与MCC比例为13,其体外释药行为较理想。结论筛选所得的盐酸多西环素缓释片处方工艺稳定可行。%Objective In this article Response Surface Analysis(RSA)was applied to optimize the formulation of doxycycline hydrochloride sustained release tablet.Methods Single factor exploration was used to determine the three factors which have the greatest impact on the release rate.The three factors were the dosage of the HPMC in the total weight of the tablet,the concentration of PVP-K30,and the ratio of lactose to microcrystalline cellulose,respectively.The composite score of the release behaviour was taken as the response value.The dosage of the ingredients were determined by Box-Benhnke design principles and 3 factors and 3 levels.Results The optimized formulation and process are as follows:the dosage of the HPMC in the total weight of the tablet was 30%;the concentration of PVP-K30 was 10%,and the ratio of lactose to microcrystalline cellulose was 13.The release behavior in vitro is ideal.Conclusion The optimized preparation process of doxycycline hydrochloride sustained release tablet is stable,highly efficient and suitable for industrial production.

  20. Determination of the content of berberine hydrochloride tablets by potassium dichromate colormetric method%重铬酸钾比色法测定盐酸小檗碱片的含量

    Institute of Scientific and Technical Information of China (English)

    侯建敏; 刘群; 冯爱平

    2001-01-01

    目的 研究盐酸小檗碱片中盐酸小檗碱的含量测定方法,并与中国药典方法的测定结果比较,评价两种方法的相关性。方法 用重铬酸钾比色法测定含量,以421 nm为测定波长,0.2 mg*mL-1的基准重铬酸钾溶液作对照液。结果 盐酸小檗碱在4.0~28.0 μg*mL-1之间呈良好的线性关系,相关系数r=0.9999,平均回收率为100.05%(n=5),RSD为0.43%。比较本法和中国药典方法的测定结果,相关性显著。结论 本法简便、准确、重现性好,可用于盐酸小檗碱的含量测定。尤适于生产过程中的快速分析。%OBJECTIVE To develop an assay for the determination of berberine hydrochloride in berberine hydrochloride tablets,and to compare the results measured by colormetric method with the assay described in Chinese Pharmacopoeia 1995 for assessing the correlation of the two methods.METHODS Potassium dichromate colormetric method was selected to determine the content, and the 0.2 mg*mL-1Potassium dichromate was used as the reference solution. The absorbency was measured at 421 nm.RESULTS The calibration curve for berberine hydrochloride was linear within the concentration range of 4.0~28.0 μg*mL-1(r=0.9999).The average recovery was 100.05%(n=5),and the RSD was 0.43%.The analytical results for berberine hydrochloride between the two methods was found to be correlated.CONCLUSION The method was proved to be simple, precise and reproduciable. It can be used for the quantitative determination of berberine hydrochloride. It is especially practicable for rapid analysis in production.

  1. Determination of artesunate in artesunate and amodiaquine hydrochloride tablets by HPLC%HPLC法测定青蒿琥酯阿莫地喹片中青蒿琥酯的含量

    Institute of Scientific and Technical Information of China (English)

    蒋红艳; 曾雪; 陈义娟

    2015-01-01

    Objective To establish an HPLC method for the determination of artesunate in artesunate and amodiaquine hydrochloride tablets. Methods WondaSil C18-WR column was used with mobile phase consisted of acetonitrile:phosphoric acid aqueous solution(adjust pH to 3,gradient elution);wavelength was 210 nm; flow rate was 1 mL/min and the column temperature was 30℃.Results The standard curve was linear in the range of 0.2~3.2 mg/mL(r=0.9997), average recoveries were 99.0%(RSD=1.35%, n=6).Conclusion The method is accurate and sensitive, and it can be used to control the quality of artesunate and amodiaquine hydrochloride tablets.%目的:建立梯度洗脱HPLC法测定青蒿琥酯阿莫地喹片中青蒿琥酯含量。方法色谱柱为Wondasil C18-WR,流动相采用乙腈-磷酸水溶液(pH=3)的二元梯度洗脱,检测波长为210 nm;流速为1 mL/min;柱温为30℃。结果青蒿琥酯在0.2~3.2 mg/mL范围内线性关系良好(r=0.9997),平均加样回收率为99.0%(RSD=1.35%,n=6)。结论该方法准确、灵敏,重现性好,可作为该制剂的质量控制方法。

  2. Comparative of Therapeutic Efficacy of Oxycodone Hydrochloride Sustained-release Tablets vs. Morphine Sulfate Sustained-release Tablets for Severe Cancer Pain Control with Rectal Administration%盐酸羟考酮缓释片与硫酸吗啡缓释片直肠给药控制重度癌性疼痛的疗效比较

    Institute of Scientific and Technical Information of China (English)

    滕箭; 杨梅英; 沈季元; 王建华; 毛睿

    2012-01-01

    目的:比较盐酸羟考酮缓释片与硫酸吗啡缓释片经直肠给药治疗重度癌性疼痛的疗效和不良反应.方法:将102例伴有中、重度疼痛的癌症患者随机分为A组(50例)与B组(52例),分别经直肠给予盐酸羟考酮缓释片和硫酸吗啡缓释片,比较2组药物起效时间、癌痛类型和药品不良反应的差异.结果:A组患者治疗1、3h时的疼痛与B组同期比较,差异有统计学意义(P<0.05),2组内脏痛和躯体痛比较差异分别有统计学意义(P<0.05),2组的不良反应如恶心、呕吐、便秘比较分别有显著性差异(P<0.05),A组均优于B组.结论:盐酸羟考酮缓释片经直肠给药控制重度癌性疼痛,安全、有效、简便.%OBJECTIVE: To compare the efficacy and adverse drug reactions of oxycodone hydrochloride sustained-release tablets (Oxycontin, Oxycodone hydrochloride prolonged-release tablets) and Morphine sulfate sustained-release tablets (MS Contin, Morphine sulfate) with rectal administration in the treatment of severe cancer pain. METHODS: Clinical information of 102 cases of moderate to severe cancer pain were analyzed, and they were divided into 2 groups. 50 cases were given oxycodone hydrochloride sustained-release tablets with rectal administration group A and 52 cases were given morphine sulfate sustained-release tablets group B. The differences of onset time, the type of cancer pain and side effects were compared between 2 groups. RESULTS: There was statistical significance in the difference of cancer pain between 2 groups, after 1 h and 3 h treatment (P<0.05), there were statistical significance in the differences of visceral pain and somatic pain between 2 groups (P<0.05) ; there were significant differences in adverse drug reactions between 2 groups, such as nausea, vomiting, constipation (P<0.05), and group A was better than group B. CONCLUSION: As for non-hospitalized patients, dying patients and not oral due to various reasons, transrectal

  3. Hydrochloride oxycodone sustained-release tablet for titration in cancer pain management%盐酸羟考酮缓释片用于癌痛治疗的滴定

    Institute of Scientific and Technical Information of China (English)

    杨平(综述); 王昆(审校)

    2015-01-01

    Oxycodone sustained-release tablet is a new formulation of potent opioids, which are characterized by their exact anal-gesic effect, high safety for oral administration, and slight adverse drug reaction. Oxycodone improves the quality of life of patients with cancer pains and is among the selected drugs used for controlling moderate and severe cancer pains. Relief from prolonged pain is achieved by adjusting the dose of Oxycontin (oxycodone hydrochloride) sustained-release tablet according to its pharmacological char-acteristics. The details are reviewed in this article.%盐酸羟考酮缓释片作为一种新型的强阿片类镇痛药,镇痛效果确切、口服安全性高、不良反应轻微,持续应用可提高癌痛患者的生存质量,是临床治疗中重度癌痛的首选药物之一。针对盐酸羟考酮缓释片治疗癌痛的药理特点,近年国内外将其用于癌痛治疗过程中的剂量调整,取得了很好的效果,本文对此进行综述。

  4. Preparation of Sinomenine Hydrochloride Sustained Release Tablet and determination of the release rate%盐酸青藤碱缓释片的制备及其释放度测定

    Institute of Scientific and Technical Information of China (English)

    洪怡; 刘亚杰; 胡建峰

    2012-01-01

    Objective To prepare the Sinomenine Hydrochloride Sustained Release Tablet. Methods The prescription was selected by orthogonal design and the investigation index was the effect of EC, MCC and lactose to the release rate. The release rate and the release behavior were studied. Results The release rate of sustained release tablet fitted the first release eqution and the release rate for 12 h was more than 75%. Conclusion The prescription is reasonable, the technology is simple and the release effect is good.%目的 制备盐酸青藤碱缓释片.方法 采用正交设计法,考察乙基纤维素、微晶纤维素、乳糖对缓释片溶出度的影响,进行处方筛选,对最佳处方进行溶出度测定及释放行为的拟合.结果 缓释片的释放行为符合一级释放方程,12 h释放度大于75%.结论 该缓释片处方合理,工艺简单,缓释效果好.

  5. HPLC法测定复方黄连素片中盐酸小檗碱的溶出度%Dissolution Determination of Berberine Hydrochloride in Compound Berberine Tablets by HPLC

    Institute of Scientific and Technical Information of China (English)

    王红霞; 蒋立英

    2011-01-01

    目的:建立测定复方黄连素片中盐酸小檗碱溶出度的方法.方法:采用高效液相色谱法测定.色谱柱为Lichrospher ODS柱,流动相为0.033mol·L~(-1)乙腈-磷酸二氢钾溶液(40:60),检测波长为265nm,进样量为10μL.采用人工胃液(0.1mol·L~(-1)盐酸溶液)1000 ML为溶出介质,转速为120r·min~(-1),取样时间为45min,温度为37℃.结果:盐酸小檗碱进样童在0.0215-0.1720μg(r=0.9999)范围内与峰面积积分值呈良好线性关系,回收率为98.7%,结论:本法操作简便、准确、可靠,可用于复方黄连素片的质量控制.%OBJECTIVE: To develop the method for the dissolution determination of berberine hydrochloride in Compound berberine tablets.METHODS: HPLC method was used.The determination was performed on Lichrospher ODS column with mobile phase consisted of 0.033 mol· L-1 acetonitrile-monobasic potassium phosphate solution (40:60) at detection wavelength of 265 nm.The injection volume was 10 μL.1 000 mL of 0.1 mol· L-1 artificial gastric juice was used as solvent.The rotation speed was 120 r· min-1, the sampling time was 45 min and the temperature was 37 ℃.RESULTS: The linear range of berberine hydrochloride was 0.021 5~0.172 0 ug (r=0.999 9) with an average recovery rate of 98.7%.CONCLUSION: The method is simple, accurate and reliable for dissolution determination of berberine hydrochloride in Compound berberine tablets.

  6. Determination of Related Substances and Content of Buprenorphine Hydrochloride Sublingual Tablet by HPLC%HPLC法测定盐酸丁丙诺啡舌下片的含量和有关物质

    Institute of Scientific and Technical Information of China (English)

    刘胜春; 赵学刚; 冯雅慧; 康海霞; 滑千里; 王乃浩

    2013-01-01

    OBJECTIVE:To establish a method for the determination of content and related substances in Buprenorphine hydrochloride sublingual tablets.METHODS:HPLC method was adopted.The determination was performed on Agilent Eclipse XDB C18 column with mobile phase consisted of 1% ammonium acetate (containing 0.1% acetic acid)-methanol (15∶85) at the flow rate of 1.0 ml/min.The column temperature was 40 ℃,and detection wavelength was 288 nm.RESULTS:Buprenorphine hydrochloride was separated with its impurities thoroughly,and its linear range were 0.004 04-0.040 4 mg/ml (r=0.999 9) with average recovery of 100.1% (RSD=0.33 %,n=9).The detection limit was 0.5 ng.CONCLUSIONS:The method is simple,sensitive and accurate.It could be applied for the determination of content and related substance in Buprenorphine hydrochloride sublingual tablets.%目的:建立同时测定盐酸丁丙诺啡舌下片含量和有关物质的方法.方法:采用高效液相色谱法.色谱柱为Agilent Eclipse XDB C18,流动相为1%醋酸铵溶液(含0.1%冰醋酸)-甲醇(15∶85),流速为1.0 ml/min,柱温为40℃,检测波长为288nm.结果:有关物质与主成分有较好的分离,盐酸丁丙诺啡检测质量浓度线性范围为0.004 04~0.040 4 mg/ml(r=0.999 9),检测限为0.5 ng,平均回收率为100.1%,RSD为0.33%(n=9).结论:本方法简便、灵敏度高、结果准确,可用于盐酸丁丙诺啡舌下片含量和有关物质测定.

  7. Improvement of Determination Method for Paracetamol,Pseudoephedrine Hydrochloride and Chlorphenamine Maleate Tablets(Ⅱ)%氨酚伪麻那敏片(Ⅱ)含量测定方法的改进

    Institute of Scientific and Technical Information of China (English)

    刘东风; 王和协

    2012-01-01

    目的:建立改进的同时测定氨酚伪麻那敏片(Ⅱ)中对乙酰氨基酚、盐酸伪麻黄碱、马来酸氯苯那敏含量的HPLC法.方法:采用Inertsil C18柱(150 mm×4.6 mm,5 μm),流动相:0.3%十二烷基硫酸钠溶液(含0.2%磷酸溶液)- 乙腈(45:55)(用浓氨溶液调节pH至3.9),流速为1.0 ml·min-1,检测波长215 nm.结果:对乙酰氨基酚、盐酸伪麻黄碱、马来酸氯苯那敏分别在62~682,6.23~68.56,0.384~4.226 μg·ml-1浓度范围内与各自峰面积积分值呈良好的线性关系;平均回收率分别为99.47%(RSD=0.24%),99.33%(RSD=0.34%),99.18%(RSD=0.20%)(n=6).结论:该方法准确、简便,可用于氨酚伪麻那敏片(Ⅱ)中3个组分的含量测定.%Objective: To establish an improved HPLC method for the determination of paracetamol, pseudoephedrine hydrochloride and chlorphenamine maleate tablets( Ⅱ ). Method: An Inertsil C18( 150 mm×4. 6 mm,5μm ) column was used. The mobile phase was 0. 3% sodium dodecyl sulfate solution ( including 0. 2% phosphoric acid solution )- acetonitrile ( 45: 55 )( adjusting pH to 3. 9 with concentrated ammonium liquid). The flow rate was 1.0 ml · min-1 and the detection wavelength was at 215 nm. Result: The linear range was 62-682 μg · ml-1 for paracetamol, 6. 23-68. 56μg · ml-1 for pseudoephedrine hydrochloride and 0. 384-4. 226μg · ml-1 for chlorphenamine maleate. The average recovery was 99. 47% ( RSD = 0. 24% , n = 6 ), 99. 33% ( RSD = 0. 34% , n = 6 ) and 99. 18% ( RSD = 0. 20% , n = 6 ), respectively. Conclusion: The method is accurate and convenient, and can be used in the determination of paracetamol, pseudoephedrine hydrochloride and chlorphenamine maleate tablets.

  8. 国产盐酸米多君片在健康人体的生物等效性研究%Bioequivalence of domestic midodrine hydrochloride tablets in healthy volunteers

    Institute of Scientific and Technical Information of China (English)

    孙军; 李珍; 计一平; 刘罡一; 余琛; 胡晋红

    2012-01-01

    目的:比较国产与进口盐酸米多君片在健康人体的生物等效性.方法:20名健康男性受试者随机交叉单剂量口服国产(受试制剂)或进口盐酸米多君片(参比制剂)5 mg,用液相色谱-串联质谱法测定血浆中盐酸米多君的活性代谢产物脱甘氨酸米多君的浓度,以DAS 2.0软件计算药动学参数,进行生物等效性评价.结果:受试制剂和参比制剂的药动学参数分别为:t1/ 2 (3.19±0.33)和(3.02±0.31)h,tmax(0.6±0.3)和(0.7±0.5)h,Cmax(21.72±6.06)和(21.83±6.24) μg/L,AUC0~t (65.27±8.43)和(65.64±7.08) μg·h·L-1,AUC0~∞(70.08±9.05)和(69.85±7.83) μg·h·L-1.按AUC0~∞计算,国产盐酸米多君片的相对生物利用度为( 100.3±6.8)%.结论:国产与进口盐酸米多君片在健康人体内具有生物等效性.%Objective:To evaluate the bioequivalence of domestic and imported midodrine hydrochloride tablets in healthy volunteers. Methods; A randomized cross-over trial was performed in 20 healthy male volunteers. Each volunteer was randomized to receive a single dose of 5 mg domestic and imported midodrine hydrochloride tablets. Plasma concentrations of desglymidodrine were measured with HPLC-MS/MS method. The pharmacokinetic parameters were calculated with DAS 2.0 software, then bioequivalence of the two preparations was evaluated. Results: The main pharmacokinetic parameters of the domestic and imported preparations were as follows:f1/2(3. 19 + 0. 33) vs (3.02 + 0.31) h,tmax(0. 6 + 0. 3) vs (0.7 + 0.5) h, cmax(21. 72±6. 06) vs (21.83±6.24) μg/L, AUC0-, (65.27±8. 43) vs (65. 64±7.08) μg o h o L-1 ,AUC. (70.08±9.05) vs (69.85±7.83) μg o h o L-1 , respectively. Relative bioavailability of the domestic midodrine hydrochloride tablets was (100.3± 6. 8) % , when calculated according to AUC0. Conclusion:The two preparations of midodrine hydrochloride are bioequivalent in healthy volunteers.

  9. 78 FR 34108 - Determination That SUBOXONE (Buprenorphine Hydrochloride and Naloxone Hydrochloride) Sublingual...

    Science.gov (United States)

    2013-06-06

    ... HUMAN SERVICES Food and Drug Administration Determination That SUBOXONE (Buprenorphine Hydrochloride and... (buprenorphine hydrochloride (HCl) and naloxone HCl) sublingual tablets, 2 milligrams (mg)/0.5 mg and 8 mg/2 mg... to approve abbreviated new drug applications (ANDAs) for buprenorphine HCl and naloxone...

  10. 复方盐酸吡格列酮/盐酸二甲双胍控释片的制备及体外释放考察%Preparation and in Vitro Evaluation of Compound Pioglitazone Hydrochloride and Metformin Hydrochloride Controlled Release Tablets

    Institute of Scientific and Technical Information of China (English)

    张尧; 李永吉; 刘平; 武占楠; 尹莉芳

    2013-01-01

    Objective:Pioglitazone hydrochloride (PG) and metformin hydrochloride (MH) can be used together to treat type2 diabetes and control the blood sugar of patients by complementation of the two drugs.The compound controlled release PG/MH tablets were developed to achieve combined medication and controlled release.The in vitro release was evaluated.Methods:PVPK30,lactose and MH were used to compress the tablet by wet granulation,and then coated with coating solution including cellulose acetate (CA),PEG400 and benzoate.Delivery orifices were drilled by laser drill on both sides of the tablet.The compound controlled release PG/MH tablets were obtained by coating the tablet with coating solution containing PG.Formulations of tablet core and coating solution of controlled release layer,membrane thickness and diameter of delivery orifice were optimized by orthogonal design and single factor evaluation.Results:We can get a 24-hour zero order release MH layer and a rapid release PG layer.PEG400,benzoate and membrane thickness have significant influence on drug release.Conclusion:The optimized controlled release PG/MH tablets can achieve combined medication.%目的:盐酸吡格列酮(PG)和盐酸二甲双胍(MH)可联用治疗2型糖尿病,两者通过机理上的互补可增强对患者血糖的调控.本文通过将两者制成复方控释片达到联合用药,延长并控制药物释放的目的,并考察其体外释放特性.方法:以聚乙烯吡咯烷酮(PVPK30)、乳糖、MH作为片芯,通过湿法制粒压片,使用含醋酸纤维素、聚乙二醇(PEG400)、苯甲酸甲酯的包衣液进行包衣形成半透膜,并在片两面通过激光打孔机各打一小孔,进一步在控释片表面包PG的速释层,形成复方控释片.对片芯处方和控释层包衣液处方进行筛选,控制包衣膜厚度和释药孔径.结果:MH可达到24 h零级释放,PG快速释放.PEG400和苯甲酸甲酯用量,包衣膜厚度对MH释放有显著影响.结论:通过正交设计和

  11. Glucosamine hydrochloride

    Science.gov (United States)

    ... combination of glucosamine hydrochloride, chondroitin sulfate, and manganese ascorbate. Some evidence suggests that this combination can improve ... combination of glucosamine hydrochloride, chondroitin sulfate, and calcium ascorbate twice daily reduces joint swelling and pain, as ...

  12. Bioequivalence of Donepezil Hydrochloride Orally Disintegrating Tablets in Healthy Volunteers%盐酸多奈哌齐口腔崩解片人体生物等效性研究

    Institute of Scientific and Technical Information of China (English)

    宋薇; 杨静; 冯智军; 丁莉坤; 李雪晴; 周伦; 杨林; 文爱东

    2012-01-01

    目的:研究盐酸多奈哌齐口腔崩解片与盐酸多奈哌齐片人体的生物等效性.方法:20名男性健康志愿者随机交叉单剂量口服盐酸多奈哌齐口腔崩解片(受试制剂)与盐酸多奈哌齐片(参比制剂)5 mg,用液质联用法测定人血浆中多奈哌齐的浓度,用DAS 2.1软件计算药动学参数,并评价两制剂的生物等效性.结果:口服受试制剂和参比制剂药动学参数分别为Cmax(8.56±2.10)和(8.08±1.78) ng·ml-1,tmax(2.65±0.74)和(3.05±0.83)h,t1/2 (70.31±19.54)和(71.15±18.47)h,AUC0~216(373.76±94.15)和(353.04±81.42) ng·h·m1-1,AUC0~∞(420.30±110.99)和(399.80±108.56) ng·h·ml-1.受试制剂AUG~216的90%置信区间在参比制剂的等效范围内.结论:两种盐酸多奈哌齐制剂生物等效.%Objective; To study the bioequivalenee of donepezil hydrochloride orally disintegrating tablets and donepezil hydrochlo-ride tablets. Method: 20 healthy male volunteers were enrolled in a randomized crossover study in which the subjects were randomly assigned to receive single dose of 5 mg orally disintegrating tablets (test preparation) or donepezil hydrochloride tablets ( reference preparation). Plasma concentrations of donepezil were determined by liquid chromatography tandem mass spectrometry method. The pharma-cokinetic parameters were calculated by DAS 2. 1 software. Result; The main pharmacokinetic parameters of test and reference preparations after oral administration were as follows;^ of (8.56 ±2. 10) and (8.08 ± 1.78) ng ml"' ,tmax of (2.65 ±0.74) and(3.05 ± 0.83) h,tI/2 of (70.31 ±19.54) and (71.15 ± 18.47) h,AUC0_m of (373.76 ±94.15) and (353.04 ± 81.42) ng -h -ml-', AUC0_, of (420. 30 ±110.99) and (399. 80 ± 108.56) ng -h ml"1. The 90% confidential intervals (CI) of AUC0_2]6 of the test preparation was in the bioequivalent range of the reference preparation. Conclusion; The two kinds of donepezil formulations are bio-equivalent.

  13. Gastroretentive Ranitidine Hydrochloride Tablets with Combined Floating and Bioadhesive Properties: Factorial Design Analysis, In Vitro Evaluation and In Vivo Abdominal X-Ray Imaging.

    Science.gov (United States)

    Abduljabbar, Hana N; Badr-Eldin, Shaimaa M; Aldawsari, Hibah M

    2015-01-01

    Ranitidine HCl is an H2-antagonist that suffers from low oral bioavailability of 50%. The site-specific absorption from the upper part of the small intestine and the colonic metabolism of the drug could partially contribute to its reduced bioavailability. To surmount these drawbacks, this work aimed at the formulation of Ranitidine HCl gastroretentive floating-biaodhesive tablets. A 3(2) factorial design was applied to assess the effects of matrix former (HPMC K100M): drug ratio, and the release retardant (Carbopol 971) amount on the characteristics of the tablets prepared using direct compression technique. The prepared tablets were thoroughly evaluated for physical properties, floating, swelling, bioadhesive and in vitro release behaviors. Statistical analysis of the results revealed significant effects for both formulation variables on the swelling index, maximum detachment force and cumulative percent drug released after 6 hours. In addition, the matrix- former: drug ratio showed a statistically significant effect on the floating lag time. Kinetic analysis of the release data indicated Higuchi diffusion kinetics and anomalous transport mechanism for all formulations. Scanning electron micrographs of the selected tablet formulation; F8, revealed intact surface without any perforations or channels in the dry state, while polymer expansion (relaxation) with some perforated areas were observed on the surface of the tablets after 12 hours dissolution in 0.1 N HCl. Furthermore, in vivo abdominal x-ray imaging showed good floating behavior of the selected formulation; F8, for up to 6 hours with appropriate bioadhesive property. In conclusion, the selected ranitidine HCl floating-bioadhesive tablets could be regarded as a promising gastroretentive drug delivery system that could deliver the drug at a controlled rate.

  14. The influence of drug-excipient and drug-polymer interactions on butt adhesive strength of ranitidine hydrochloride film-coated tablets.

    Science.gov (United States)

    Sarisuta, Narong; Lawanprasert, Pojawon; Puttipipatkhachorn, Satit; Srikummoon, Krisana

    2006-04-01

    The influence of fillers and polymeric films on adhesive strength of hydroxypropyl methylcellulose (HPMC) and Eudragit E100 films coated on ranitidine HCl tablets containing either spray-dried rice starch (SDRS) or lactose monohydrate as fillers after storage at 45 degrees C/75% RH for four weeks was investigated by the use of butt adhesion technique. The adhesive strength of film-coated tablets of fillers without drug was found to slightly decrease after storage. In contrast, the adhesive strength of drug-containing film-coated tablets significantly reduced, the degree of which was higher for Eudragit E100 than HPMC. Physicochemical characterization by employing differential scanning calorimetry (DSC) and diffuse reflectance infrared Fourier transform spectroscopy (DRIFTS) revealed that the drug was obviously incompatible with lactose and possibly mild interaction with Eudragit E100 was suggested. The results indicated that the adhesive strength of film-coated tablets would be affected not only by the drug-excipient interaction, but also by the drug-polymeric film interaction.

  15. 氨酚曲马多片在中国健康志愿者体内的药动学研究%Pharmacokinetics of tramadol hydrochloride-paracetamol tablets in Chinese healthy volunteers

    Institute of Scientific and Technical Information of China (English)

    孙莉; 周芬; 范华莹; 梁军成; 刘丽京; 邓艳萍

    2011-01-01

    目的:研究氨酚曲马多片在中国健康志愿者体内的药动学.方法:12名健康志愿者,男女各半,采用3×3拉丁方设计,分别顿服氨酚曲马多片(盐酸曲马多37.5 mg+对乙酰氨基酚325 mg)1,2,3片.反相HPLC-UV法检测对乙酞酰基酚、曲马多及其代谢物Ml的含量,并采用3 P97药动学软件估算药动学参数,C_max和T_max采用实测值计算,AUC_o-tn采用梯形法计算.结果:口服不同剂量氨酚曲马多片后,对乙酰氨基酚、曲马多及其代谢物Ml药-时曲线拟合结果均符合一室模型,各剂量组的C_max和AUC_o-24随剂量增加而增大.结论:在给药剂量范围内氨酚曲马多单次给药后的C_max和AUC_o-24与剂量的线性关系尚不能得出明确结论.%Objective: To investigate the pharmacokinetics of tramadol hydrochloride-paracetamol tablets in Chinese healthy volunteers. Methods: 12 volunteers (6 men and 6 women) were divided into six groups by 3 ×3 design, and administered with single dose of 1, 2 and 3 tables in 3 cross periods. The concentrations of paracetamol, tramadol and its metabalite O-desmethyltramadol (M1) were determined by high performance liquid chromatography (HPLC). The pharmacokinetic parameters were calculated using 3P97 software. Results: The concentration-time curves of paracetamol, tramadol and M1 were described by one-compartment open model. The pharmacokinetics parameters such as Cmax and AUC0-24 were proportionally increased with doses. Conclusion: There is no clear conclusions that the process of tramadol hydrochloride-paracetamol tablets in the dose range 1 ~ 3 tables in human body fits linear dynamic feature.

  16. Bioequivalence Study of Two Orodispersible Rizatriptan Formulations of 10 mg in Healthy Volunteers

    Science.gov (United States)

    Cánovas, Mercè; Polonio, Francisco; Cabré, Francesc

    2016-01-01

    The aim of the study was to assess the bioequivalence and tolerability of two different oral formulations of rizatriptan. A bioequivalence study was carried out in 40 healthy volunteers according to an open label, randomized, two-period, two-sequence, crossover, single dose, and fasting conditions design. The test and reference formulations were administered in two treatment days, separated by a washout period of seven days. Plasma concentrations of rizatriptan were obtained by the LC/MS/MS (Liquid chromatography tandem-mass spectrometry) method. Log-transformed AUC0-t (area under the plasma concentration-time curve from zero to the last measurable concentration) and Cmax (maximum plasma concentration) values were tested for bioequivalence based on the ratios of the geometric means (test/reference). The tmax (time to reach maximum plasma concentration) was analysed nonparametrically. The 90% confidence intervals of the geometric mean values for the test/reference ratios for AUC0-t and Cmax were within the bioequivalence acceptance range of 80%–125%. According to the European Guideline, it may therefore be concluded that the test formulation of rizatriptan 10 mg orodispersible tablet is bioequivalent to the reference formulation (Maxalt® Max 10 mg oral lyophilisate). The safety profile of both formulations was consistent with the summary of the product characteristics.

  17. Bioequivalence Study of Two Orodispersible Rizatriptan Formulations of 10 mg in Healthy Volunteers.

    Science.gov (United States)

    Cánovas, Mercè; Polonio, Francisco; Cabré, Francesc

    2016-06-13

    The aim of the study was to assess the bioequivalence and tolerability of two different oral formulations of rizatriptan. A bioequivalence study was carried out in 40 healthy volunteers according to an open label, randomized, two-period, two-sequence, crossover, single dose, and fasting conditions design. The test and reference formulations were administered in two treatment days, separated by a washout period of seven days. Plasma concentrations of rizatriptan were obtained by the LC/MS/MS (Liquid chromatography tandem-mass spectrometry) method. Log-transformed AUC0-t (area under the plasma concentration-time curve from zero to the last measurable concentration) and Cmax (maximum plasma concentration) values were tested for bioequivalence based on the ratios of the geometric means (test/reference). The tmax (time to reach maximum plasma concentration) was analysed nonparametrically. The 90% confidence intervals of the geometric mean values for the test/reference ratios for AUC0-t and Cmax were within the bioequivalence acceptance range of 80%-125%. According to the European Guideline, it may therefore be concluded that the test formulation of rizatriptan 10 mg orodispersible tablet is bioequivalent to the reference formulation (Maxalt(®) Max 10 mg oral lyophilisate). The safety profile of both formulations was consistent with the summary of the product characteristics.

  18. HPLC法测定吡格列酮二甲双胍片中盐酸吡格列酮的有关物质%HPLC method for determinnation of the related substances of Pioglitazone hydrochloride of Pioglitazone Metformin Tablets

    Institute of Scientific and Technical Information of China (English)

    雍春; 赵琛

    2012-01-01

    摘要:目的:建立吡格列酮二甲双胍片中盐酸吡格列酮有关物质的高效液相色谱方法。方法:采用为依利特c18色谱柱(250×4.6mm,5um);以水-乙腈-乙酸=550:450:1.2(用氨试液调节pH值至5.8)作为流动相;检测波长为225nm。结果:三批样品(BE1101、BE1102、BE1103)盐酸吡格列酮单个杂质(%)分别为0.15、0.14、0.14;有关物质(%)分别为0.22、0.21、0.21。结论:采用HPLC法测定盐酸吡格列酮有关物质方法简便,结果准确可靠,二甲双胍无干扰。%Purpose: To establish an RP- HPLC method for determinnation of the related substances of Pioglitazone hydrochloride of Pioglitazone Metformin Tablets . Methods: The separation was performed on an Elite C18 column (250 × 4.6 mm, 5 um); and the mobile phase consisted of water - acetonitrile - acetic acid = 550:450:1.2 (ammonia solution adjusted to pH 5.8).The detection was set at 225nm. Results: The three batches of samples (BE1101,BE1102,BE1103) hydrochloride pioglitazone single impurity (%) were 0.15,0.14,0.14; related substances (%) were 0.22,0.21,0.21. Conclusion: the method for determination of pi- oglitazone hydrochloride related substances method is simple, accurate and reliable, metformin no interference.

  19. 高效液相色谱法拆分盐酸舍曲林片的光学异构体%Separation of Four Optical Isomers Determination of Sertraline Hydrochloride Tablets by HPLC

    Institute of Scientific and Technical Information of China (English)

    陈积暖; 冯晓梅

    2012-01-01

    目的 建立测定盐酸舍曲林片光学异构体的高效液相色谱法.方法 采用反相高效液相色谱法,以外标法测定.色谱柱为依利特Hypersil ODS2柱(150mm×4.6mm,5μm),流动相为磷酸二氢钠缓冲液(取磷酸二氢钠12.5g,β-环糊精12.8g,HP-β-环糊精17.3g,加水至1 000 mL)-乙腈-三乙胺[800:200:10,用磷酸调节pH为(2.5±0.5)]为流动相,流速为1.0 mL/min,检测波长为214 nm.结果 所建立的流动相能拆分盐酸舍曲林4个光学异构体,光学异构体之间的分离度均良好.结论 该方法专属性好,准确、灵敏,盐酸舍曲林异构体与主峰分离良好,可作为控制盐酸舍曲林片有关物质检查的方法.%Objective To establish a HPLC method for determining four optical isomers in Sertraline Hydrochloride Tablets. Methods RP - HPLC was adopted with the external standard method for detection. The separation was carried out on the Hypersil ODS2 column (150 mm×4. 6 mm,5 μm) with the mobile phase of sodium dihydrogen phosphate buffer (taking sodium dihydrogen phosphate 12.5 g, beta - cyclodextrin 12.8 g, hydroxypropyl - beta - cyclodextrin 17. 3 g and adding water to 1 000 mL) - acetonitrile - triethylamine (800 : 200 : 10,adjusting to pH 2.5 ±0.5 with phosphoric acid). The flow rate was 1.0 mL/min and the detection wavelength was 214 nm. Results Four optical isomers of sertraline hydrochloride were effectively separated by the established the mobile phase. The degree of separation among isomers was good. Conclusion This method is specific, accurate and sensitive with better separation of isomers from main peak,and can be used as the detection method for controlling the related substances of Sertraline Hydrochloride Tabletso

  20. DEVELOPMENT AND VALIDATION OF FIRST ORDER DERIVATIVE SPECTROPHOTOMETRIC METHOD FOR SIMULTANEOUS ESTIMATION OF PARACETAMOL AND TAPENTADOL HYDROCHLORIDE IN TABLET DOSAGE FORM

    Directory of Open Access Journals (Sweden)

    SAMIL D. DESAI*, BHAVNA A. PATEL, SHRADDHA J. PARMAR, NAITIK N. CHAMPANERI

    2013-09-01

    Full Text Available A simple, precise, accurate and reproducible spectrophotometric method has been developed forSimultaneous estimation of Paracetamol and Tapentadol Hydrochloride by employing first order derivativezero crossing method in 0.1 N Sodium Hydroxide. The first order derivative absorption at 257.1 nm (zerocross point of Paracetamol was used for quantification of Tapentadol HCl and 289.0 nm (zero cross point ofTapentadol HCl for quantification of Paracetamol. The linearity was established over the concentrationrange of 15-35

  1. A multicenter, randomized, double-blind, placebo-controlled, 6-month trial of bupropion hydrochloride sustained-release tablets as an aid to smoking cessation in hospital employees

    DEFF Research Database (Denmark)

    Dalsgareth, Oli Jacob; Hansen, Niels-Christian Gerner; Søes-Petersen, Ulrik

    2004-01-01

    Despite changes in smoking behavior, one-third of the Danish population continues to smoke. Many of these smokers are hospital employees. This 6-month, multicenter, parallel group, randomized, double-blind, placebo-controlled study evaluated treatment with bupropion hydrochloride sustained release...... (Zyban) compared with placebo as an aid to smoking cessation in health care workers. A total of 336 hospital employees who smoked at least 10 cigarettes daily were randomized (2:1) to 7 weeks of treatment with bupropion (n=222) or placebo (n=114). All participants were motivated to quit smoking......% in the bupropion group and 18% in the placebo group, pinsomnia, and pruritus appeared...

  2. 微乳液相色谱法同时测定氨酚曲麻片中5种成分的含量%Simultaneous determination of the contents of five ingredients in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets by microemulsion liquid chromatography

    Institute of Scientific and Technical Information of China (English)

    江洁; 杨若因; 任晶波; 周岳森; 李宁

    2012-01-01

    Objective To establish a novel microemulsion system and develop this method for the rapid simultaneous determination of contents of acetaminophen, caffeine, salicylamide, pseudoephedrine hydrochloride and triprolidine hydrochloride in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets by microemulsion liquid chromatography (MELC). Methods The effect on the chromatography of various operating parameters was studied,the parameters including the surfactant concentration,the type and concentration of oil phase,the pH of eluent,/3-cyclodextrin concentration. MELC was performed on a Venu-sil ASB C18 analytical column( 150 mm ×4. 6 mm,5 μm) at 30 t. The optimized MELC system with microemulsion consisted of 3. 0% ( w) SDS-6. 0% ( w) butanol-0. 6% ( w) octane-0. 3% (φ) triethylamine-10 mmoloL-1 β-cyclodextrin-90% (w) water, the pH of which was adjusted to 5.0 with phosphoric acid; The flow rate was set at 0. 7 mLomin-1 and the samples were measured at multiple wavelengths:0-8.0 min 280 nm,8.1-15.0 min 257 nm,15.1 min 233 nm. Results Rapid separations of five ingredients in paracetamol triprolidine hydrochloride and pseudophedrine hydrochloride tablets were achieved in 25 min,The linearity established was 20%- 180% of theoretical concentrations of each product in dosage form with r ≥ 0. 999 0;The mean recoveries were 98.4% to 101. 5%. Conclusions The proposed MELC procedure for the separation of five ingredients in the tablets is less expensive compared with the conventional RP-HPLC method, and it is proved to be a simple and rapid way. The optimized and validated method can be applied to qualitative analysis of five ingredients in the tablets.%目的 建立一种新的微乳液相色谱法,同时测定氨酚曲麻片中对乙酰氨基酚、咖啡因、水杨酰胺、盐酸伪麻黄碱、盐酸曲普利啶5种成分的含量.方法 通过考察微乳流动相体系中表面活性剂SDS的浓度、油相的种类和浓度、流动相的pH

  3. Stability-Indicating HPLC Method for the Simultaneous Determination of HIV Tablet Containing Emtricitabine, Tenofovir Disoproxil Fumarate, and Rilpivirine Hydrochloride in Pharmaceutical Dosage Forms.

    Science.gov (United States)

    Venkatesan, S; Kannappan, N; Mannemala, Sai Sandeep

    2014-01-01

    A simple, accurate, rapid, and stability-indicating RP-HPLC method for a combination of tenofovir disoproxil fumarate, emtricitabine, and rilpivirine has been developed and subsequently validated in commercial tablets. The proposed HPLC method utilizes Phenomenex Gemini C18 column (150 mm × 4.6 mm i.d., 5 µm) and mobile phase consisting of MeCN, potassium dihydrogen phosphate buffer (20 mM, pH 3.3), and triethylamine 58.72 : 41.23 : 0.05 (v/v) at a flow rate of 1.7 mL/min. Quantitation was achieved with UV detection at 270 nm. The method was validated in terms of accuracy, precision, linearity, limits of detection, limits of quantitation, and robustness. This optimized method has been successively applied to pharmaceutical formulation and no interference from the tablet excipients was found. TDF, EMT, and RPV and their combination drug product were subjected to acid, base, neutral hydrolysis, oxidation, dry heat, and photolytic stress conditions and the stressed samples were analyzed by the proposed method. As the proposed LC method could effectively separate the drugs from its degradation products, it can be employed as stability-indicating method for the determination of instability of these drugs in bulk and commercial tablets.

  4. pH/溶剂双梯度反相高效液相色谱法同时测定氨酚曲麻片中的5种有效成分%Simultaneous determination of five cold medicine ingredients paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets by pH/organic solvent double-gradient high performance liquid chromatography

    Institute of Scientific and Technical Information of China (English)

    禤学怡; 黄丽娜; 潘晓玲; 李宁

    2013-01-01

    A pH/organic solvent double-gradient mode in reversed-phase high performance liquid chromatography (HPLC) has been established as a new approach to the simultaneous determination of acetaminophen, caffeine, salicylamide, pseudoephedrine hydrochloride and triprolidine hydrochloride in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets. Through the optimization of the organic solvent gradient mode and pH/organic solvent double-gradient mode, the optimum double-gradient HPLC system of the five cold medicine ingredients has been built. The determination was carried out on a Diamonsiol Cl8 column (250 mm ×4.6 mm, 5 μm). The mobile phase consisted of methanol, 0. 05 mol/L ammonium acetate solution and 0.08 mol/L acetic acid solution. The column temperature was set at 30 ℃. The flow rate was 1.0 mL/min. The sample was measured at multiple wavelengths; 0-6 min, 280 ran; 6 -7 min, 257 nm; 7 - 14 min, 280 run; 14 min, 233 run. The separation of the five cold medicine ingredients in the tablets was achieved in 25. 5 min. The linear ranges of acetaminophen, pseudoephedrine hydrochloride, caffeine, salicylamide and triprolidine hydrochloride were 0.055 - 0. 998 g/L, 0.053-0.946 g/L, 0.007 -0.129 g/L, 0.035 -0.622 g/L and 0.002-0.039 g/L, respectively,with their correlation coefficients greater than 0.999 0. The detection limits (S/N = 3) were 0.09, 6, 0.02, 0.128 and 0.02 mg/L, respectively. Their mean recoveries were 97. 9% - 102. 8%. The advantage of the method is the simultaneous determination of acidic, neutral and basic compounds. It also can improve the column efficiency of the analyte, compress the half-peak width and reduce the trailing. The optimized and validated method can be used for the simultaneous determination of the five cold medicine ingredients in the tablets.%建立了一种pH/溶剂双梯度反相高效液相色谱(HPLC)同时测定氨酚曲麻片中对乙酰氨基酚、咖啡因、水杨酰胺、盐酸伪

  5. 布洛芬盐酸苯海拉明分散片的制备及质量评价%Preparation of Ibuprofen and Diphenhydramine Hydrochloride Dispersible Tablets and Their Quality Evaluation

    Institute of Scientific and Technical Information of China (English)

    张玉洁; 罗永煌; 戈振凯; 田翠翠; 张贺; 尼玛仓木拉

    2012-01-01

    Objective To prepare and evaluate ibuprofen and diphenhydramine hydrochloride dispersible tablets in order to provide data for state category Ⅲ new drug application. Methods The formulations were optimized with disintegration time, dispersion homogeneity, rigidity and taste as reference parameters by single-factor and orthog onal tests. HPLC was performed to determine the content and dissolution of the tablets. Results Disintegrating a gent-6% PVPP (with an internal and external ratio of 2: 1) filling agent -24% MCC adhesive agent -2% PVPk30 solution and correctant with an aspartame/steviosin ratio of 1 ~ 9. The dispersible tablets thus prepared were good in taste, with a disintegration time of 64.6±5.73 s. The cumulative dissolution per- centage was more than 80 % within 5 min. Drug content and dispersion homogeneity were within the speci fied scope. Conclusion The prescription of the dispersible tablet is reasonable; the preparation process is simple the quality indexes conform to the requirement of dispersible tablets.%目的:筛选布洛芬盐酸苯海拉明分散片的最优处方并对其质量进行评价,为申报三类新药提供核心数据.方法:以崩解时限、分散均匀性、硬度和口感为指标,单因素试验筛选崩解剂和矫味剂,正交试验优化处方,湿法制粒制备分散片,HPLC测定其片剂的含量和溶出度.结果:崩解剂为6%PVPP(内外加比例2:1),填充剂为24%MCC,粘合剂为2%的PVPk30溶液适量,矫味剂占2%且阿司帕坦/甜菊素为1:9,所制备的分散片口感良好,崩解时限为64.63±3.58S,5min分散片中布洛芬和盐酸苯海拉明的溶出度均达到了80%以上,含量和分散均匀性均在规定范围内.结论:该分散片处方合理,工艺简单,质量指标符合分散片要求.

  6. A multicenter, randomized, double-blind, placebo-controlled, 6-month trial of bupropion hydrochloride sustained-release tablets as an aid to smoking cessation in hospital employees

    DEFF Research Database (Denmark)

    Dalsgareth, Oli Jacob; Hansen, Niels-Christian Gerner; Søes-Petersen, Ulrik;

    2004-01-01

    (Zyban) compared with placebo as an aid to smoking cessation in health care workers. A total of 336 hospital employees who smoked at least 10 cigarettes daily were randomized (2:1) to 7 weeks of treatment with bupropion (n=222) or placebo (n=114). All participants were motivated to quit smoking......Despite changes in smoking behavior, one-third of the Danish population continues to smoke. Many of these smokers are hospital employees. This 6-month, multicenter, parallel group, randomized, double-blind, placebo-controlled study evaluated treatment with bupropion hydrochloride sustained release...... more frequently in the bupropion group than in the placebo group. Bupropion was effective as an aid to smoking cessation in a broad group of hospital employees in Denmark....

  7. Bioequivalence of metformin hydrochloride tablets in Chinese healthy volunteers%盐酸二甲双胍片在中国健康人体的生物等效性

    Institute of Scientific and Technical Information of China (English)

    邱相君; 孙永健; 刘涛; 刘心霞; 袁世英; 陈汇

    2012-01-01

    Objective To evaluate the bioequivalence of two domestic metformin hydrochloride tablets in healthy volunteers. Methods A single oral dose (1. 0 g of test and reference formulation) was given to 20 healthy volunteers in a randomized crossover study. The concentrations of metformin hydrochloride in plasma were determined by HPLC. The bio-availability and bioequivalence of two formulations were evaluated by DAS 2. 0 software, then the bioequivalence was judged. Results After a single dose, the pharmacokinetic parameters for tested and reference metformin hydrochloride were as follows: Cmax were (2. 83 ± 0. 53 ), (2.57±0.57) mg , L-1; Twere (1.55 ±0. 39) , (t. 63 ±0. 36) h; t1/2 were ( 3. 70 + 1. 76), (3. 36 ± 0. 72) h; AUC0_24 were (10. 20 ± 1. 95), (9. 71 ± 2. 56) mg · h · L-1, respectively. The 90% confidential interval of AUC0-24, AUC0-∞ and Cmax of test formulation were 99. 1% -114.6% , 99. 1% -113. 8% and 100.6% -110.4% , respectively. The relative bioavailability of test to reference formulation was (108. 3 ± 20. 5 ) % . Conclusion The test and reference metformra hydrochloride were bioequivalence.%目的 评价2种国产盐酸二甲双胍片(口服降糖药)在中国健康人体的生物等效性.方法 20名健康男性受试者随机交叉单剂量口服盐酸二甲双胍片试验药物和对照药物,各1.0 g.用高效液相色谱法测定血浆中盐酸二甲双胍的浓度,用DAS 2.0软件计算药代动力学参数,并对2种药物进行生物等效性评价.结果 试验药物和对照药物的主要药代动力学参数如下:Cmax为(2.83±0.53),(2.57±0.57) mg· L-1;Tmax为(1.55±0.39),(1.63±0.36)h;t1/2为(3.70±1.76),(3.36±D.72) h;AUC0-24为(10.20±1.95),(9.71±2.56) mg·h·L-1.AUC0-24、AUC0-∞、Cmax的90%可信区间分别为99.1% ~114.6%、99.1% ~ 113.8%和100.6%~110.4%.试验药物相对于对照药物的生物利用度F为(108.3±20.5)%.结论 试验药物和对照药物生物等效.

  8. Comparative Study on Efficacy and Safety of Compound Glucosamine Hydrochloride Capsules and Tablets in Treatment of Osteoarthritis%复方盐酸氨基葡萄糖胶囊与片剂治疗骨关节炎疗效及安全性的对比研究

    Institute of Scientific and Technical Information of China (English)

    孙永红; 罗东方; 詹志军

    2016-01-01

    目的:探讨不同剂型的复方盐酸氨基葡萄糖治疗骨关节炎的疗效及安全性。方法:选取2012年7月—2016年6月湖北省谷城县人民医院收治的骨关节炎患者306例作为研究对象,采用区组随机化分组方法分为胶囊组、片剂组及安慰剂组3组,每组各102例。胶囊组患者给予复方盐酸氨基葡萄糖胶囊3粒,片剂组患者给予复方盐酸氨基葡萄糖片剂3片,安慰剂组患者给予复方盐酸氨基葡萄糖胶囊1粒、片剂1粒、安慰剂1粒,1日3次。观察不同用药方案的安全性与临床疗效。结果:胶囊组、片剂组患者的关节功能与视觉模拟评分法评分均明显低于安慰剂组,差异均有统计学意义( P<0.05);胶囊组与片剂组的总有效率均显著高于安慰剂组,差异均有统计学意义( P<0.05);3组患者不良反应发生率的差异无统计学意义( P>0.05)。结论:采用复方盐酸氨基葡萄糖胶囊剂或片剂治疗骨关节炎,均疗效显著,且安全可靠。%OBJECTIVE:To probe into the efficacy and safety of different formulations of compound Glucosamine hydrochloride capsules and tablets in treatment of osteoarthritis .METHODS:306 patients with osteoarthritis admitted into Hubei Province Gucheng County People's Hospital from Jul .2012 to Jun.2016 were selected to be divided into capsule group , tablet group and placebo group via the random number table , with 102 cases in each .The capsule group were given three compound Glucosamine hydrochloride capsules , the tablet group were treated with three Glucosamine hydrochloride tablets , and the placebo group received one Glucosamine hydrochloride capsule , one Glucosamine hydrochloride tablet , three times a day .The clinical efficacy and safety of different therapeutic regimen were observed .RESULTS: The joint function recovery and visual analogue scale score of capsule group and tablet group were significantly lower than that

  9. Improvement of assay method of metformin hydrochloride in Metformin and Glipizide Tablets%二甲双胍格列吡嗪片中盐酸二甲双胍含量测定方法改进

    Institute of Scientific and Technical Information of China (English)

    王长丹; 臧恒昌; 左艳红

    2015-01-01

    目的:建立高效液相法测定二甲双胍格列吡嗪片中盐酸二甲双胍含量测定方法。方法采用 C18(4.6 mm ×150 mm,5μm)色谱柱;以0.05%庚烷磺酸钠溶液(用10%磷酸溶液调节 pH 值至4.0)-乙腈(84:16)为流动相,流速:1.0 mL·min -1,检测波长:233 nm,柱温:30℃。结果盐酸二甲双胍在10.02~30.06μg·mL -1浓度范围内与峰面积呈良好的线性关系(r =0.9999),回收率为101.0%,RSD =0.66%(n =9)。结论所建立的方法较原国家注册标准专属性更强、更准确。%Objective To establish an HPLC method for the determination of metformin hydrochloride in Metformin and Glipizide Tablets. Methods The separation was performed on C18 column(4. 6 mm × 150 mm,5 μm),and the mobile phase was composed of 0. 05% sodium heptane - 1 - sulphonate solution(with 10% phosphoric acid solution to adjust pH value to 4. 0)- acetonitrile(84:16)with the flow rate of 1. 0 mL·min - 1 . The detection wavelength was 233 nm. The col-umn temperature was 30 ℃ . Results The linear range of metformin hydrochloride was 10. 02 ~ 30. 06 μg·mL - 1(r =0. 999 9). The average recovery rate was 101. 0% with RSD of 0. 66%(n = 9). Conclusion The established method was better and more accurate than the original national registered standard specificity.

  10. 氨酚咖黄烷胺片在人体的生物等效性研究%Bioequivalence of Paracetamol, Caffeine, Artificial Cow-bezoarand and Amantadine Hydrochloride Tablets in Healthy Volunteers

    Institute of Scientific and Technical Information of China (English)

    王晓波; 袭荣刚; 姜爽; 李野; 刘美林; 姜培航; 周慧梅; 谢小青; 魏晓明

    2011-01-01

    Objective: To study the pharmacokinetics and bioequivalence of two domestic Paracetamol, Caffeine, Artificial cowbezoarand and Amantadine Hydrochloride Tablets in healthy volunteers.Method: Single oral doses of the two kinds of Paracetamol,Caffeine, Artificial cow-bezoarand and Amantadine Hydrochloride Tablets were given to 24 healthy volunteers in an open randomized crossover design.The concentrations of Paracetamol and Caffeine in plasma were determined by HPLC,and the concentration of Amantadine was determined by HPLC-MS/MS.Result: The main pharmacokinetic parameters of Paracetamol in test and reference tablets were as follows:t1/2 of (3.93 ± 1.66) and (3.56 ± 1.38) h,Cmax of (6.301 2 ±0.840 8) and (6.695 6 ± 1.260 0) μg·ml-1 ,tmax of (0.79 ±0.42) and (0.77 ±0.59) h,AUC0-1 of (26.2 ±5.4) and (27.0 ±5.6) μg·h·ml -1 ,respectively.The relative bioavailability of Paracetamol was (98.1% ± 15.1 ) %.The main pharmacokinetic parameters of Caffeine in test and reference tablets were as follows:t1/2 of (6.50 ±2.53) and (6.70±2.37) h,Cmax of (795.1 ±182.5) and (811.8±194.1) ng·ml-1,tmax of (0.89 ±0.61)and (0.98 ±0.69) h,AUC0-1 of (7 008 ±2 615) and (7 330 ±2 669) ng·h·ml-1 ,respectively.The relative bioavailability of Caffeine was (96.7 % ± 18.7) %.The main pharmacokinetic parameters of Amantadine in test and reference tablets were as follows: t1/2 of (13.29±4.04) and (11.76±3.63) h,Cmax of (295.3 ±80.5) and (303.0±72.4) ng· ml-1,tmax of (2.10±1.13) and (2.13±1.17) h,AUC0-1 of (4 158 ± 1 653) and (4 097 ± 1 366) ng·h·ml-1 respectively.The relative bioavailability of Amantadine was ( 104.5 ±32.7) %.Conclusion: The results demonstrated that the two preparations were bioequivalent.%目的:研究氨酚咖黄烷胺的药物动力学和生物等效性.方法:接双周期随机交叉试验设计,24名健康男性受试者分别单次口服受试试剂和参比试剂后,HPLC法测定血浆中对乙酰氨基酚、咖啡因的浓

  11. 反相高效液相色潽法测定罗己降压片中维生素B6含量%Determination of Pyridoxine Hydrochloride in Luojijiangya Tablets by RP-HPLC

    Institute of Scientific and Technical Information of China (English)

    尹艳华

    2015-01-01

    Objective: HPLC method was established for the determination of Pyridoxine Hydrochloride in Luojijiangya Tablets. Methods:ODS C18 column w as used. The mobile phase was 0.04%sodium pentanesulfonate(adjusted to pH 3.0 with acetic acid)-methanol(85:15). The detection wavelength was 291nm. The flow rate was 1.0 mL·min-1 with the column temperature at 35℃. Results:The average recoveries were 99.04%,RSD=0.17%(n=9). The linear range of Pyridoxine was within 0.4000~1.600μg (r=0.9999). Con-clusion:The method is simple, accurate, stableand reliable. It can be used for quality control of Luojijiangy a Tablets.%目的:建立RP-HPLC法测定罗己降压片中维生素B6含量。方法:使用十八烷基硅烷键合硅胶为填充剂,以0.04%戊烷磺酸钠溶液(用冰醋酸调节pH至3.0)-甲醇(85:15)为流动相,检测波长为291nm进行测定。流速1.0mL·min-1,柱温35℃。结果:平均加样回收率维生素B6为99.04%,RSD=0.17%(n=9)。维生素B6在0.4000~1.600µg范围内,进样量与峰面积值呈良好的线性关系(r=0.9999)。结论:方法简便、结果准确、重现性好,可为罗己降压片的质量控制提供依据。

  12. Evaluation of Metformin Hydrochloride Tablets by Dissolution Curves in Different Media%多条溶出曲线评价盐酸二甲双胍片的溶出行为

    Institute of Scientific and Technical Information of China (English)

    王诗红; 黄斌; 张煌辉; 刘宏伟; 杨择瑜

    2016-01-01

    目的:比较7个厂家盐酸二甲双胍片在4种溶出介质中的溶出曲线,评价进口制剂与仿制制剂的溶出行为。方法:采用篮法,转速为100 r·min-1,分别以pH 1.0盐酸溶液、pH 4.5醋酸盐缓冲液、pH 6.8磷酸盐缓冲液、水为溶出介质,以紫外分光光度法测定溶出曲线,采用f2因子对溶出曲线的相似度进行评价。结果:在4种不同溶出介质中,仅有1个厂家盐酸二甲双胍片的4条溶出曲线与进口制剂相似,还有4家制剂的4条溶出曲线与进口制剂均不相似。结论:多数仿制制剂的溶出曲线与参比制剂不相似,建议改进制剂处方与工艺。%Objective: To compare the dissolution profiles of metform hydrochloride tables from seven pharmaceutical manufactures in four different dissolution media and evaluate the quality difference between the imported and the generic drugs. Methods: On the basis of the rotating basket method with the rotate speed at 100 r·min-1, the dissolution testing of tablets in various media at different pH values were per-formed by using UV spectrometry. The similarities of dissolution curves were analyzed by the f2 similarity factor. Results: Generic tablets from one manufacturer had similar dissolution profiles to the imported drugs in different dissolution media, while there were significant differences in the four dissolution curves between the generic tables from each of other manufacturers and the imported drugs. Conclusion: Most home man-ufactures cannot produce high-quality generic drugs with similar dissolution profiles to the original drugs. The results suggest that home manufactures should improve the production of generic drugs by changing the formulation and preparation process.

  13. Crossover comparison of efficacy and preference for rizatriptan 10 mg versus ergotamine/caffeine in migraine.

    Science.gov (United States)

    Christie, Suzanne; Göbel, Hartmut; Mateos, Valentin; Allen, Christopher; Vrijens, France; Shivaprakash, Malathi

    2003-01-01

    Rizatriptan is a selective 5-HT(1B/1D) receptor agonist with rapid oral absorption and early onset of action in the acute treatment of migraine. This randomized double- blind crossover outpatient study assessed the preference for 1 rizatriptan 10 mg tablet to 2 ergotamine 1 mg/caffeine 100 mg tablets in 439 patients treating a single migraine attack with each therapy. Of patients expressing a preference (89.1%), more than twice as many preferred rizatriptan to ergotamine/caffeine (69.9 vs. 30.1%, p rizatriptan and 54.2% of patients who preferred ergotamine/caffeine. The co-primary endpoint of being pain free at 2 h was also in favor of rizatriptan. Forty-nine percent of patients were pain free 2 h after rizatriptan, compared with 24.3% treated with ergotamine/caffeine (p rizatriptan being superior within 1 h of treatment. Headache relief at 2 h was 75.9% for rizatriptan and 47.3% for ergotamine/caffeine (p rizatriptan being superior to ergotamine/caffeine within 30 min of dosing. Almost 36% of patients taking rizatriptan were pain free at 2 h and had no recurrence or need for additional medication within 24 h, compared to 20% of patients on ergotamine/caffeine (p Rizatriptan was also superior to ergotamine/caffeine in the proportions of patients with no nausea, vomiting, phonophobia or photophobia and for patients with normal function 2 h after drug intake (p rizatriptan (69.8%) than at 2 h after treatment with ergotamine/caffeine (38.6%, p rizatriptan and 15.3% with ergotamine/caffeine. Both active treatments were well tolerated. The most common adverse events (incidence > or = 5% in one group) after rizatriptan and ergotamine/caffeine, respectively, were dizziness (6.7 and 5.3%), nausea (4.2 and 8.5%) and somnolence (5.5 and 2.3%).

  14. 盐酸特拉唑嗪分散片的人体生物利用度%Bioavailability of terazosin hydrochloride dispersible tablets in Chinese healthy volunteers

    Institute of Scientific and Technical Information of China (English)

    张志涛; 李见春; 蒋志文

    2009-01-01

    OBJECTIVE To study the relative bioequivalence of terazosin HCI dispersible tablets and its domestic convention-al tablets in Chinese healthy volunteers. METHODS A single oral dose of 2 mg terazosin HC1 was randomly given to 20 healthy volunteers in two-way cross-over design. Plasma concentration of terazosin HCI was determined by HPLC-fluoremetry method. Pharmacokinetics parameters were calculated. The bioequivalence of the two preparations was calculated by analysis of variance and two one side t-test. RESULTS After oral administration, the main pharmacokinetics parameters of test and reference CONCLUSION The two preparations were bioequivalent.%目的:研究盐酸特拉唑嗪分散片和国产普通片的人体生物等效性.方法:20名健康男性受试者自身交叉单剂量口服盐酸特拉唑嗪分散片和国产普通片,采用高效液相色谱-荧光法测定血浆药物浓度,计算药动学参数,以方差分析与双向单侧t检验进行统计学分析.结果:盐酸特拉唑嗪分散片和国产普通片的Gmax分别为(29.8±9.3)μg·L-1和(31.0±9.8)μg·L-1,tmax分别为(0.8±0.1)h和(1.5±0.9)h,AUC0→t分别为(325.9±75.5)μg·h·L-1和(362.3±105.6)μg·h·L-1.盐酸特拉唑嗪分散片的相对生物利用度为(91.5±26.6)%.结论:2种制剂具有生物等效性.

  15. 偏头痛应用尼美舒利分散片联合盐酸氟桂利嗪治疗的临床效果探究%The Clinical Effect of Migraine Treated by Beauty Nimesulide Dispersible Tablets combined Flunarizine Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    祝孔辉

    2015-01-01

    目的:研究尼美舒利分散片与盐酸氟桂利嗪治疗偏头痛的临床疗效。方法随机选取我院2012年3月至2014年3月共收治的66例偏头痛患者,将其分为治疗组与参照组。两组均给予盐酸氟桂利嗪治疗,治疗组加用尼美舒利分散片治疗,对比两组的临床效果。结果治疗组的总有效率显著高于参照组,两组比较存在显著性差异(P<0.05)。结论对于偏头痛患者,给予盐酸氟桂利嗪与尼美舒利分散片的治疗方案,效果显著。%ObjectiveTo study the "beauty nimesulide dispersible tablet and lfunarizine hydrochloride clinical curative effect for the treatment of migraine. MethodsRandomly selected from March 2012 to March 2012 a total of 66 patients with migraine treated, it can be divided into the treatment group and control group. In the two groups were given lfunarizine hydrochloride treatment, the treatment group treated with beauty, nimesulide dispersible tablet, compared the clinical effect of the two groups.ResultsThe total effective rate of treatment group is signiifcantly higher than control group, two groups compare exist signiifcant difference (P<0.05).ConclusionFor patients with migraine, lfunarizine hydrochloride and beauty nimesulide tablets treatment, the effect is remarkable.

  16. Novel buccal adhesive tablets using Aloe vera L and Sinapis alba--a promising option for improved bioavailability of diltiazem hydrochloride.

    Science.gov (United States)

    Sudhakar, Yajaman; Bandyopadhyay, A K

    2008-01-01

    In the current investigation, white mustard mucilage from whole seeds of Sinapis alba was evaluated for its physical properties and compared with the other mucoadhesive polymers such as hydroxy propyl methylcellulose 5Cps and Carbopol 934P. Further, methanol precipitable solids from whole leaves of Aloe Vera L were used as permeation enhancer. To achieve improved bioavailability of diltiazem, novel buccal adhesive tablets (NBATs) in cup and core fashion designed to achieve unidirectional release towards mucosa were prepared in a three-stage process using specially fabricated punches. The adhesive cups were studied for its shear, tensile, and peel strengths by specially designed apparatus using excised ruminant and porcine buccal mucosa as model substrates. Ex vivo permeation studies in a Franz diffusion cell were conducted through porcine buccal mucosa. Fourier transform infrared spectroscopy studies and differential scanning calorimetry thermographs showed no remarkable interactions. Histopathological studies showed no remarkable damage of buccal mucosa by the NBATs. In vivo studies were conducted on anaesthetized male New Zealand albino rabbits, estimated by reversed-phase high-performance liquid chromatography, and the pharmacokinetics were compared with the oral and intravenous bolus injection. NBATs exhibited a Cmax 74.6 ng/mL, Tmax 3.5 h, t(1/2) 4.36 h. The NBATs prevented salivary scavenging effect and exhibited 82.1% bioavailability.

  17. Effect of levamisole hydrochloride tablets in treating skin myiasis in children%盐酸左旋咪唑片治疗儿童皮肤蝇蛆病的效果分析

    Institute of Scientific and Technical Information of China (English)

    张晓庆

    2016-01-01

    Objective To explore the effect of levamisole hydrochloride tablets in treating skin myiasis in children.Methods Clinical data of 38 children with skin maggot from September 2010 to September 2014 who received levamisole hydrochloride tablets and adrenal cortex hormone were retrospectively analyzed.The white blood cell count,percentage of eosinophils,high-sensitivity C-reactive protein (hs-CRP) levels and liver function (aspartate aminotransferase,alanine aminotransferase) were detected before and after treatment;the safety was also evaluated.Results All 38 cases had close contact with animals.The typical clinical symptoms included muscle pain,fever,skin lesions after polypide climbing out of the skin,multiple subcutaneous nodules,migratory pricking,and multiple skin damage.The maggots drilled from the skin in 24 cases,were taken out using forceps in 10 cases,were taken out by incision.Twenty-eight cases were cured,maggots still discharged in 10 cases and completely drained 1 week later.After treatment,the white blood cell count,hs-CRP,IL-6,TNF-α were significantly reduced compared with pretreatment [(9.4 ± 1.6) × 109/L vs (13.6 ± 2.6) × 109/L,(4.2 ± 0.7) % vs (6.1 ± 2.0) %,(0.39 ± 0.21) mg/L vs (2.34 ± 0.81) mg/L] (P <0.05).After treatment,the aspartate aminotransferase and alanine aminotransferase were not significantly changed (P > 0.05).No serious adverse events were observed;mild vomiting occurred in 1 case,dizziness occurred in 2 cases.Conclusion The effect of levamisole hydrochloride tablets in treating children's skin myiasis is well with high safety.%目的 探讨盐酸左旋咪唑片对儿童皮肤蝇蛆病的治疗效果.方法 收集2010年9月至2014年9月于四川省阿坝州人民医院治疗的38例皮肤蝇蛆病患儿的临床资料进行回顾性分析.所有患儿均口服盐酸左旋咪唑片和肾上腺皮质激素,观察该病的发病机制、临床表现及诊治效果,比较治疗前后患儿白细胞计数、嗜酸细

  18. The Effects of Terbinafme Hydrochloride Vaginal Effervescent Tablets Combined with Live Lactobacillus Capsule on Recurrent Vulvovaginal Candidasis%盐酸特比萘芬阴道泡藤片联合乳杆菌活菌治疗复发性外阴阴道假丝酵母菌病57例临床观察

    Institute of Scientific and Technical Information of China (English)

    戈静; 叶珂帆

    2012-01-01

    Objective To observe effects of terbinafine hydrochloride vaginal effervescent tablets combined with living preparation of lactobacillus on recurrent vulvovaginal candidasis (RVVC). Methods One hundred and sixty-four patients of RVVC were randomly divided into treatment group treated with terbinafine hydrochloride vaginal effervescent tablets plus live lactobacillus capsule, control group 1 treated with terbinafine hydrochloride vaginal effervescent tablets alone and control group 2 treated with miconazole nitrate vaginal capsules, observing the recurrence rate after treatment one year. Results After one year, the effective rate was 89. 47% ,80.00% ,73.68% and recurrence rate waslO. 00% ,25.64% ,26. 19% in treatment group, control 1 and 2 group respectively. There was a significant difference between treatment group and the two control groups (p<0. 05). Conclusion The combination of terbinafine hydrochloride vaginal effervescent tablets with living preparation of lactobacillus capsule showed satisfactory efficacy and low recurrence rate in treatment recurrent vulvovaginal candidasis.%目的 观察盐酸特比萘芬阴道泡藤片联合乳杆菌活菌治疗复发性外阴阴道假丝酵母菌病(RVVC)的临床疗效.方法 将164例RVVC患者随机分为3组,治疗组(57例)予盐酸特比萘芬阴道泡藤片联合乳杆菌活菌胶囊治疗,对照1组(50例)仅予盐酸特比萘芬阴道泡藤片治疗,对照2组(57例)仅予硝酸咪康唑阴道胶囊治疗.3组患者均随访1年.结果 1年后,治疗组、对照1组和对照2组有效率分别为89.47%,80.00%,73.68%,复发率分别为10.00%,25.64%和26.19%,3组的有效率和复发率比较,差异均有统计学意义(P均<0.05).结论盐酸特比萘芬阴道泡藤片联合乳杆菌活菌治疗RVVC的疗效好,复发率低.

  19. GC Determination of Pargyline Hydrochloride in Compound Pargyline Tablets%GC法测定复方帕吉林片中盐酸帕吉林的含量

    Institute of Scientific and Technical Information of China (English)

    费嘉

    2012-01-01

    Objective To establish a method for determination of pargyline in compound pargyline tablets. Methods The chromatographic column was DB-624(30 m ×0. 32 mm, 1.4 μm). The column temperature programming was 110 t maintained for 12 min before rising to 250 °C (at rate of 40 t/min) that was maintained for 10 min. For FID detection,the temperature was 300 °C. The split ratio was 20:1. Results The linear range of pargyline was within 0.21-1.05 mg/ml(Y =0.6949X -0.0112, r =0.9995). Conclusion This method to determinate pargyline is reliable and accurate.%目的 测定复方帕吉林片中盐酸帕吉林的含量.方法 改性聚乙二醇毛细管柱(30 m ×0.32 mm,1.4 μm),柱温110℃保持12 min,再以40℃/min的速度升温至250℃保持10 min;进样口温度为270℃;氢火焰检测器,检测器温度为300℃;分流比为20:1.结果 盐酸帕吉林的回归方程为:Y =0.6949X -0.0112,r=0.9995,表明盐酸帕吉林在0.21~1.05mg/ml的浓度范围内具有良好的线性关系.结论 本法测定复方帕吉林片中的盐酸帕吉林的含量准确可靠.

  20. 新型盐酸二甲双胍控释片的研制及在Beagle犬体内的药代动力学研究%Preparation of novel metformin hydrochloride osmotic pump controlled release tablets and study on pharmacokinetics in Beagle dogs

    Institute of Scientific and Technical Information of China (English)

    殷健; 冯岩; 卢骏; 刘志东; 师健鑫

    2012-01-01

    Objective;To prepare novel large-dose metformin hydrochloride osmotic pump controlled release tablets, and to investigate the pharmacokinetics of the marketed metformin hydrochloride tablets and the self-made ones in Beagle dogs and the in vitro-in vivo correlation. Methods; Polyethylene oxide (PEO) was used as suspension agent and SDS was applied as surfactant. The similarity factor f2 was used to evaluate the release behavior between the self-made formulation and marketed tablets. In the cross-over study of single-dose and multiple-dose , the in vivo pharmacokinetics of the self-made formulation and the marketed tablets were studied in Beagle dogs. Results; Compared to marketed metformin hydrochloride tablets, the f2 value was 75.0. The relative bioavailabilities of the self-made formulation after single-dose and multiple-dose administration were (101.31 ± 15.81 )% and (99. 46 ± 12.55)% , respectively. Conclusion; Compared with the marketed tablets, self-made metformin hydrochloride osmotic pump controlled release tablets have similar pharmacokinetic profile and bioavailability.%目的:制备新型大剂量盐酸二甲双胍渗透泵控释片,以市售控释片为对照,对服用渗透泵片的Beagle犬进行体内药代动力学研究,并对体外释放和体内吸收的相关性做出评价.方法:选用聚环氧乙烷(PEO)和十二烷基硫酸钠(SDS)等为主要辅料,制备盐酸二甲双胍单层渗透泵片;用f2相似因子法考察剂型的体外释放行为,并与市售控释片释放度进行比较;采用单剂量和多剂量交叉试验进行Beagle犬体内药代动力学研究.结果:与市售控释片进行比较,相似因子f2 =75.0.单剂量和多剂量犬体内试验相对生物利用度分别为(101.31±15.81)%和(99.46±12.55)%.结论:自制盐酸二甲双胍渗透泵片具有与市售片相似的缓释效果,主要药代动力学参数无显著差异,两个制剂的生物利用度接近.

  1. Study on Bioequivalence of Ambroxol Hydrochloride Oral Disintegrating Tablets in Healthy Volunteers%盐酸氨溴索口腔崩解片的人体生物等效性研究

    Institute of Scientific and Technical Information of China (English)

    陈白莹; 夏铮铮; 常宏

    2013-01-01

    目的:对生产工艺重大改变前、后盐酸氨溴索口腔崩解片在健康人体的生物等效性进行对比研究.方法:20名健康男性受试者按交叉试验设计方案分别口服受试制剂和参比制剂各30 mg,采集服药后48 h内的动态血标本,以普拉克索为内标,采用液-质联用(LC-MS)法测定血浆中盐酸氨溴索的质量浓度,并用DAS 2.0软件统计分析药动学参数.结果:参比制剂和受试制剂药动学参数分别为:cmax (84.96±32.46)、(90.86±44.81)ng/ml,tmax(1.7±0.7)、(1.4±0.3)h,AUC0-48 h(678.85±235.17)、(663.87±214.37)ng·h/ml,t1/2(9.8±1.9)、(9.7±2.0)h,主要药动学参数无显著性差异.结论:生产工艺重大改变前、后生产的两种制剂生物等效.%OBJECTIVE:To study the bioequivalence of Ambroxol hydrochloride oral disintegrating tablets in healthy volunteers after significant change of manufacturing technology.METHODS:Test preparation and reference preparation each 30 mg were given to 20 male healthy volunteers in randomized two-way crossover design.Blood samples were collected within 48 h after medication using pramipexole as internal standard.Plasma concentrations of ambroxol hydrochloride were determined by LC-MS,and pharmacokinetic parameters were analyzed using DAS 2.0 software.RESULTS:The pharmacokinetics parameters of test preparation and reference preparation were as follows:cmax(84.96 ± 32.46)ng/ml and (90.86 ± 44.81) ng/ml;tmax(1.7 ± 0.7) h and (1.4 ± 0.3) h; AUC0-48 h(678.85 ± 235.17) ng·h/ml and (663.87 ± 214.37)ng·h/ml;t1/2(9.8 ± 1.9) h and (9.7 ± 2.0)h,respectively.There was no significant difference in main pharmacokinetic parameters of them.CONCLUSIONS:Two preparations are bioequivalent after significant change of manufacturing technology.

  2. 盐酸哌甲酯控释片治疗儿童注意缺陷多动障碍疗效%Efficacy of Methylphenidate Hydrochloride controlled-release tablets on Attention-Deficit Hyperactivity Disorder in Children

    Institute of Scientific and Technical Information of China (English)

    陈敏; 华丽; 刘琳; 徐璐; 郝燕; 侯凌

    2015-01-01

    Objective To observe the therapeutic effect of methylphenidate hydrochloride controlled-release tablets (OROS-MPH) on attention-deficit hyperactivity disorder (ADHD). Methods Seventy-two cases of children with ADHD were randomly divided into treatment group (40) and control group (32). Cases of treatment group were given 0.8-1.0 mg��kg-1 of OROS-MPH for three months. Cases of control group were given 1.2-1.4 mg��kg-1 of atomoxetine hydrochloride for three months. After 12 weeks treatment, children were evaluated by Wechsler intelligence test, Integrated visual and auditory continuous performance test (IVA-CPT), the SNAP-Ⅳ effect assessment scale and TESS scale. Results The treatment efficiency was similar in both groups. Attention deficit and hyperactivity in both groups were improved obviously. Wechsler intelligence score was significantly elevated ( P<0. 05), SNAP-Ⅳ score was significantly decreased ( P<0. 05), and IVA-CPT score was increased significantly after treatment ( P<0.05) . The changes of scores on hyperactivity, auditory attention and visual attention were more in OROS-MPH group than those in atomoxetine group(P<0.05). There was loss of appetite in 10 children of OROS-MPH group and in 14 children of atomoxetine group. There was drowsiness in 1 child of OROS-MPH group and in 5 children of atomoxetine group, as well as difficulty to fall asleep in 6 children of OROS-MPH group and 1 child of atomoxetine group (P<0.05). One child developed a transient spasm after 4-month treatment. Conclusion Both of OROS-MPH and atomoxetine hydrochloride can improve learning ability and the symptom of attention deficit and hyperactivity, and they are similarly effective and safe in children with ADHD, but OROS-MPH can work faster.%目的:研究盐酸哌甲酯控释片治疗儿童注意缺陷多动障碍( ADHD)的疗效。方法将72例ADHD患儿随机分成治疗组40例和对照组32例。治疗组给予盐酸哌甲酯控释片,初始剂量为每天0

  3. Erlotinib hydrochloride.

    Science.gov (United States)

    Minna, John D; Dowell, Jonathan

    2005-05-01

    Erlotinib hydrochloride (Tarceva; OSI Pharmaceuticals/Genentech/Roche), a member of a class of targeted anticancer drugs that inhibit the activity of the epidermal growth factor receptor, was approved by the US FDA in November 2004 for the treatment of advanced non-small-cell lung cancer after failure of at least one prior chemotherapy regimen. It is the first such drug to demonstrate an increase in survival in Phase III trials in patients with advanced non-small-cell lung cancer.

  4. 21 CFR 520.446 - Clindamycin capsules and tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Clindamycin capsules and tablets. 520.446 Section... capsules and tablets. (a) Specifications—(1) Each capsule contains the equivalent of 25, 75, 150, or 300... 150 mg clindamycin as the hydrochloride salt. (3) Each capsule contains the equivalent of 25, 75, or...

  5. SUSTAINED RELEASE ITOPRIDE HYDROCHLORIDE MATRIX TABLET

    Directory of Open Access Journals (Sweden)

    BHUPENDRA, PRAJAPATI, NIKLESH PATEL, HITESH

    2013-09-01

    Full Text Available Oral route gets the highest priority for thedelivery of the drug as well as better patient compliance incase of self delivery dosage formulation. The aim ofpresent investigation was undertaken with the objective offormulating sustain release formulation of Itopridehydrochloride for oral drug delivery. Itopride hydrochlorideis highly water soluble prokinetic drug.Hydroxypropylmethylcellulose K4M (lower viscositygrade and K100M (higher viscosity grade were used as amatrix forming agents to control the release of drug. HPMCK4M and HPMC K100M were used individually as well asin combination with different proportion in the preparationof the Sustained release formulation. 32 factorial designswere applied to the polymer concentration that affects thedrug release profile. Reduced equation for drug release at2hr,6hr,and10hrwere22 1 2 1 Q 37.644 5.41X 3.25X 2.017X ,26 1 2 1 Q 72.367 8.05X 4.4X 3.75X ,and10 1 1 2 90.844 5.8 2.633 2.8 2 Q X X X Xrespectively. Optimized batch F019 shows good tabletproperties like hardness(7-9kg/cm2, thickness(4.48mm,friability(0.024%,assay(99.3% and nearly similar drugrelease profile to the targeted reference drug release profileand it was indicated by similarity factor (f2=86.04.

  6. Times to pain relief and pain freedom with rizatriptan 10 mg and other oral triptans

    OpenAIRE

    Ng-Mak, D S; Hu, X. H.; Chen, Y.; Ma, L.; Solomon, G

    2007-01-01

    Background: In the clinical trial setting, oral rizatriptan 10 mg has greater efficacy than other oral triptans in freedom from migraine headache pain 2 h after dosing. Objective: The study objective is to compare the effectiveness of rizatriptan 10 mg and other oral triptans for acute migraine attack in a naturalistic setting. Methods: A total of 673 patients took rizatriptan 10 mg or their usual-care oral triptans for two migraine attacks in a sequential, cross-over manner and recorded outc...

  7. Study on in vitro release and bioequivalence in Beagle dogs of ambroxol hydrochloride push-pull osmotic pump controlled-release tablets%盐酸氨溴索双层渗透泵控释片体外释放及Beagle犬生物等效性

    Institute of Scientific and Technical Information of China (English)

    马银玲; 赵锋; 金晓利; 王静; 曹德英

    2011-01-01

    目的:研究自制片的体外释药行为及体内生物等效性.方法:采用相似因子(f2)为评价指标,考察自制片的体外释放行为;采用单剂量交叉试验考察Beagle犬口服自制片与参比制剂的生物等效性及体内外相关性.结果:自制片体外释放零级特征明显(r=0.992 1)且释药完全(90%).犬体内两制剂生物等效,相对生物利用度(100.0±12.6)%,自制片体内外相关性良好(r=0.98).结论:盐酸氨溴索双层渗透泵控释片具有很好的开发前景.%OBJECTIVE In vitro release and bioequivalence of self-made tablets were evaluated. METHODS Using similar factor (f2) as evaluate index, in vitro release of self-made tablets were evaluated. In vivo study, ultilizing Beagle dogs orally single-dose crossing administrated, the bioequivalence between the self-made controlled-release tablets and marketed sustained capsules and the correlation coefficient between the fraction of absorption in vivo and the release rate in vitro were investigated. RESULTS Self-made tablets possessed character of zero-order release (r = 0.992 1) and drug release completely(90%) in vitro release. The relative bioavailability was (100. 0 ± 12. 6) %. The correlation coefficient between the fraction of absorption in vivo and the release rate in vitro was 0. 98. CONCLUSION Ambroxol hydrochloride push-pull osmotic pump controlled-releasetablets have much developing potential.

  8. Effect of Gulong capsule combined with glucosamine hydrochloride tablet in treating knee osteoarthritis%骨龙胶囊联合盐酸氨基葡萄糖片治疗膝关节骨性关节炎的临床效果分析

    Institute of Scientific and Technical Information of China (English)

    王志忠; 胡叶暖; 刘献旺

    2015-01-01

    Objective To explore the effect of Gulong capsule combined with glucosamine hydrochloride tablet in treating knee osteoarthritis (KOA).Methords Totally 68 KOA patients from March 2012 to March 2015 were randomly divided into observation group (30 cases) orally given Gulong capsule (2.5 g, 3 times/d)combined with glucosamine hydrochloride tablet (240 mg, 3 tines/d), and control group (34 cases) orally given glucosamine hydrochloride tablet (240 mg, 3 times/d oral).Before and 60 days after treatment, the degree of arthralgia, arthroncus, range of motion and walking ability were assessed and graded;the effective rate and incidence of adverse reactions were compared between groups.Results In observation group, 3 cases were clinically cured, 16 cases were markedly effective, 11 cases were effective, 4 cases were ineffective;in control group, none was cured, 9 cases were markedly effective, 13 cases were effective, 12 cases were ineffective;the total effective rate in observation group was significantly higher than that in control group [88.2% (30/34) vs 64.7%(22/34)] (P < 0.05).The adverse reaction degree was relatively mild in both groups;the incidence of adverse reactions was not significantly different between groups (P > 0.05).Conclusion Gulong capsule combined with glucosamine hydrochloride tablets is safe and effective in treating KOA, it can relieve joint pain and improve the life quality.%目的 探讨骨龙胶囊联合盐酸氨基葡萄糖片治疗膝关节骨性关节炎(KOA)的临床效果.方法 选取2013年3月至2015年5月于北京军区总医院第三门诊部和骨科门诊就诊的膝关节骨性关节炎患者68例,完全随机分为观察组和对照组,各34例.观察组给予骨龙胶囊2.5g,3次/d口服,盐酸氨基葡萄糖片240 mg,3次/d口服;对照组给予盐酸氨基葡萄糖片240 mg,3次/d口服.分别观察治疗前及治疗后60d2组患者的关节疼痛程度、关节肿胀、关节活动度、步行

  9. 盐酸左氧氟沙星片在健康受试者体内的相对生物利用度与生物等效性研究%Relative Bioavailability and Bioequivalence of Levofloxacin Hydrochloride Tablets in Healthy Chinese Subjects

    Institute of Scientific and Technical Information of China (English)

    李忠芳; 陈华庭; 曾繁典; 师少军

    2011-01-01

    Objective:To evaluate the relative bioavailability and bioequivalence of domestic levofloxacin hydrochloride tablets in healthy male volunteers. Method: A single oral dose of 200 mg levofloxacin hydrochloride test and reference tablets were given to 20 male healthy volunteers in a randomized crossover design. Serum levofloxacin concentrations were determined by reversed-phase high performance liquid chromatography ( HPLC) method. The pharmacokinetic parameters and relative bioavailability were calculated with DAS program to evaluate the bioequivalence of the two preparations. Result: The main pharmacokinetic parameters of levofloxacin hydrochloride test and reference tablets were as the follows:t1/2 of (7. 37 ±0. 88) and (7. 39 ±0. 96) h,tmax of ( 1. 13 ±0. 30) and (1.06 ±0.24) h.Cmax of (2. 08 ±0.42) and (2. 03 ±0.35) mg·L-1 ,and AUC0-24 of (13. 17 ±2.32) and (13. 73 ±2.89) mg·h· L-1,respectively. The relative bioavailability of the test tablets was (97. 7 ± 16. 7)%. Conclusion:The two preparations of levofloxacin hydrochloride are bioequivalent.%目的:研究国产盐酸左氧氟沙星片的人体相对生物利用度与生物等效性.方法:20名男性健康志愿者随机交叉单剂量口服国产盐酸左氧氟沙星受试和参比制剂(彼妥)200 mg,采用反相高效液相色谱法测定其血药浓度,计算其药动学参数和相对生物利用度,评价2种制剂的生物等效性.结果:国产盐酸左氧氟沙星受试和参比制剂的主要药动学参数:t1/2分别为(7.37±0.88),(7.39±0.96)h;tmax分别为(1.13±0.30),(1.06±0.24)h;Cmax分别为(2.08±0.42),(2.03±0.35) mg·L-1;AUC0~24分别为(13.17±2.32),(13.73±2.89) mg·h·L-1.国产盐酸左氧氟沙星受试制剂的相对生物利用度为(97.7±16.7)%.结论:2制剂具有生物等效性.

  10. [Tablet splitting].

    Science.gov (United States)

    Quinzler, R; Haefeli, W E

    2006-06-01

    The splitting of scored tablets provides many advantages. One benefit is to achieve dose flexibility to account for the huge interindividual differences in dose requirements for instance in paediatric and geriatric patients, which are often not covered by the available strengths in the market. Moreover, large-sized tablets can easier be swallowed if broken before swallowing and medication costs can often be reduced by splitting brands with higher strength. But not all tablets, mostly unscored tablets, are suitable for splitting. Splitting of extended release formulations can result in an overdose by uncontrolled release of the active component and degradation of the compound can occur if an enteric coating is destroyed by the splitting process. Whether tablets are suitable for splitting depends on the properties of the active component (e.g. light sensitivity), the galenics, the shape of the tablet, and the shape of the scoreline. Moreover, not all patients are informed, able, or willing to split tablets and the majority of the elderly population is not capable to break tablets. When split tablets are prescribed it is therefore important to view the shape of the tablet, to assess the patients ability and willingness to break tablets, to properly inform the patient about the appropriate way of splitting, and if necessary to suggest (and instruct) the use of a tablet splitting device.

  11. Simultaneous Determination of Amiloride and Hydrochlorothiazide in a Compound Tablet by Diffuse Reflectance Spectroscopy and Chemometrics

    Science.gov (United States)

    Tang, J.; Li, X.; Feng, Y.; Liang, B.

    2016-09-01

    This paper studies the simultaneous determination of amiloride hydrochloride (AMH) and hydrochlorothiazide (HCTZ) in amiloride hydrochloride tablets by ultraviolet-visible-shortwave near-infrared diffuse reflectance spectroscopy (UV-Vis-swNIR DRS) and chemometrics. Quantitative models for the two components were established by partial least squares (PLS) and support vector regression (SVR), respectively. For the PLS models of AMH and HCTZ, the determination coefficient R2 of the calibration set was 0.9503 and 0.9538, and the coefficient R2 of the prediction set was 0.8983 and 0.9260, respectively. The root mean square error of the calibration set (RMSEC) was 0.8 mg and 8.1 mg, while the root mean square error of the prediction set (RMSEP) was 1.0 mg and 8.7 mg, respectively. For the SVR models of AMH and HCTZ, the R2 of the calibration set was 0.9668 and 0.9609; the R2 of the prediction set was 0.9145 and 0.9446, respectively. The RMSEC was 0.7 and 7.5 mg, and the RMSEP was 0.9 and 8.9 mg, respectively. The results show that SVR modeling has a satisfactory prediction effect. The proposed method based on UV-vis-swNIR and chemometrics is efficient, nondestructive, and expected to be used for online quality monitoring in the production of drugs.

  12. Simultaneous determination of pseudoephedrine hydrochloride and cetrizine hydrochloride by reverse phase high performance liquid chromatography

    Directory of Open Access Journals (Sweden)

    Nalini C

    2006-01-01

    Full Text Available A reversed phase high performance liquid chromatographic method has been developed using Shimadzu HPLC-VP series, LC-10 ATV pump, SPD10 AVP and C8 column, for simultaneous determination of pseudoephedrine hydrochloride and cetrizine hydrochloride in three marketed tablet formulations (extended release. The mobile phase consists of phosphate buffer of pH 7.0 and acetonitrile HPLC grade in the ratio of 1:1. The flow rate was maintained at 1 ml/min and the ultraviolet detection was done at 242 nm, which is the isosbestic point. Linearity coefficients, assay values, recovery studies and repeatability studies showed that the method is accurate and precise.

  13. 盐酸二甲双胍缓释片释放度及体内体外相关性研究%Study on Correlation Between in Vitro Release and in Vivo Absorption of Metformin Hydrochloride Sustained-Release Tablets

    Institute of Scientific and Technical Information of China (English)

    杨婧; 齐宪荣

    2011-01-01

    OBJECTIVE To study the correlation between the in vitro release and in vivo absorption of metformin hydrochloride sustained-release tablets. METHODS The rotatory-basket method was used to determine the release rate, and UV spectrophotometer at 233 run was used to assay the concentration. Similarity factor was calculated to compare the release rates of the test product and the original product A single dose of metformin hydrochloride sustained-release tablets was given to 20 healthy volunteers, and the metformin hydrochloride concentrations in plasma at different time were determined. RESULTS The test product and the original product showed similar in vitro release characteristics, and the test product demonstrated good in vitro-in vivo correlation. CONCLUSION The in vitro release characteristic of the test product is qualified, and similar to that of the original product The in vitro release curve of the test product can be used to evaluate its in vivo absorption.%目的 测定受试制剂盐酸二甲双胍缓释片的体外释放度,并进行体内体外相关性研究.方法 采用转篮法测定释放度,紫外分光光度法测定含量,测定波长233 nrn,计算受试制剂与原研产品释放曲线的相似因子f2,进行释放度的比较;单剂量口服受试制剂后测定血药浓度,将体外释放度数据与用Wagner-Nelson方法计算的药物体内吸收百分数进行线性回归后,进行体内体外相关性研究.结果 受试制剂与原研产品体外释药曲线相似,受试制剂的体内体外相关性良好.结论 受试制剂体外释放度合格,与原研产品有相似的体外释放特性,且可以通过体外释放曲线预测体内情况.

  14. Content Determination and Release Rate in Metformin Hydrochloride Sustained-release Tablets by HPLC%高效液相色谱法测定盐酸二甲双胍缓释片中盐酸二甲双胍的含量和释放度

    Institute of Scientific and Technical Information of China (English)

    宋新康; 曾玉梅

    2016-01-01

    目的:建立测定盐酸二甲双胍缓释片中盐酸二甲双胍含量和释放度的方法。方法:采用C18色谱柱(150 mm ×4.6 mm,5μm);流动相:0.05%庚烷磺酸钠溶液(用10%磷酸溶液调节pH至4.0)-乙腈( V∶V=84∶16),流速:0.8 ml/min;检测波长:233 nm;柱温:35℃。结果:盐酸二甲双胍在2.45~98.00μg/ml(r=1,n=6)呈良好的线性关系,回收率99.2%,RSD为0.84%。结论:该方法适用于盐酸二甲双胍缓释片的质量控制。%OBJECTIVE: To establish a method of content determination and release rate in Metformin hydrochloride sustained-release tablets by HPLC .METHODS: C18 chromatographic column ( 150 mm ×4.6 mm, 5 μm) was adopted , the mobile phase was 0.05% heptane sodium sulfonate solution ( with 10% phosphoric acid solution to adjust pH value to 4.0 ) -acetonitrile ( V∶V =84∶16 ) , with flow rate of 0.8 ml/min.The detection wavelength was 233 nm and the column temperature was 35 ℃.RESULTS:Metformin hydrochloride had good linear relationship in 2.45-98.00 μg/ml ( r=1 , n=6 ) , The recovery rate was 99.2% and RSD was 0.84%. CONCLUSIONS:The method is suitable for Metformin hydrochloride sustained-release tablets quality control .

  15. Pharmaceutical development of an amorphous solid dispersion formulation of elacridar hydrochloride for proof-of-concept clinical studies.

    Science.gov (United States)

    Sawicki, E; Schellens, J H M; Beijnen, J H; Nuijen, B

    2017-04-01

    A novel tablet formulation containing an amorphous solid dispersion (ASD) of elacridar hydrochloride was developed with the purpose to resolve the drug's low solubility in water and to conduct proof-of-concept clinical studies. Elacridar is highly demanded for proof-of-concept clinical trials that study the drug's suitability to boost brain penetration and bioavailability of numerous anticancer agents. Previously, clinical trials with elacridar were performed with a tablet containing elacridar hydrochloride. However, this tablet formulation resulted in poor and unpredictable absorption which was caused by the low aqueous solubility of elacridar hydrochloride. Twenty four different ASDs were produced and dissolution was compared to crystalline elacridar hydrochloride and a crystalline physical mixture. The formulation with highest dissolution was characterized for amorphicity. Subsequently, a tablet was developed and monitored for chemical/physical stability for 12 months at +15-25 °C, +2-8 °C and -20 °C. The ASD powder was composed of freeze dried elacridar hydrochloride-povidone K30-sodium dodecyl sulfate (1:6:1, w/w/w), appeared fully amorphous and resulted in complete dissolution whereas crystalline elacridar hydrochloride resulted in only 1% dissolution. The ASD tablets contained 25 mg elacridar hydrochloride and were stable for at least 12 months at -20 °C. The ASD tablet was considered feasible for proof-of-concept clinical studies and is now used as such.

  16. 盐酸伐昔洛韦与复方甘草酸苷片联合治疗初发性生殖器疱疹临床观察%Clinical Treatment Observation of Valaciclovir Hydrochloride Combined With Compound Glycyrrhizin Tablets in Primary Genital Herpes

    Institute of Scientific and Technical Information of China (English)

    王艳

    2016-01-01

    Objective Hydrochloride on cutting famciclovir combined with compound glycyrrhizic acid glucoside tablets in the treatment of early send sexual genital bleb clinical effect.Methods 86 cases of primary genital herpes patients were divided into study group (HCl valaciclovir+ compound licorice tablets) and control group (valaciclovir).ResultsThe total effective rate of the study group was higher than that of the control group (P0.05).Conclusion Hydrochloric acid cutting famciclovir combined with compound glycyrrhizic acid glucoside tablets in the treatment of early send sexual genital bleb has a good clinical effect.%目的:探讨盐酸伐昔洛韦联合复方甘草酸苷片治疗初发性生殖器疱疹的临床效果。方法将86例初发性生殖器疱疹患者分为研究组(盐酸伐昔洛韦+复方甘草酸苷片)和对照组(盐酸伐昔洛韦)。结果研究组总有效率高于对照组(P<0.05);复发率低于对照组(P<0.05);两组不良反应发生率无统计学差异(P>0.05)。结论盐酸伐昔洛韦联合复方甘草酸苷片治疗初发性生殖器疱疹有较好临床效果。

  17. Simultaneous determination of gatifloxacin and ambroxol hydrochloride from tablet dosage form using reversed-phase high performance liquid chromatography%反相高效液相色谱法同时测定片剂中的加替沙星与盐酸氨溴索

    Institute of Scientific and Technical Information of China (English)

    SHAHED Mirza; NANDA Rabindra; DEHGHAN Muhammad Hassan; NASREEN Huda; FEROZ Shaikh

    2008-01-01

    A reversed-phase high performance liquid chromatography (HPLC) method was developed, validated, and used for the quantitative determination of gatifloxacin (GA) and ambroxol hydrochloride (AM), from its tablet dosage form. Chromatographic separation was performed on a HiQ Sil C18 column (250 mm×4.6 mm, 5 μm), with a mobile phase comprising of a mixture of 0.01 mol/L potassium dihydrogen orthophosphate buffer and acetonitrile(70:30,v/v),and pH adjusted to 3 with orthophosphoric acid, at a flow rate of 1 mL/min, with detection at 247 nm. Separation was completed in less than 10 min. As per International Conference on Harmonisation (ICH) guidelines the method was validated for linearity, accuracy, precision, limit of quantitation, limit of detection, and robustness. Linearity of GA was found to be in the range of 10-60 μg/mL and that for AM was found to be 5-30 μg/mL. The correlation coefficients were 0.999 6 and 0.999 3 for GA and AM respectively. The results of the tablet analysis (n=5) were found to be 99.94% with ±0.25% standard deviation (SD) and 99.98% with±0.36% SD for GA and AM respectively. Percent recovery of GA was found to be 99.92% -100.02% and that of AM was 99.86% -100.16% . The assay experiment shows that the method is free from interference of excipients. This demonstrates that the developed HPLC method is simple, linear, precise, and accurate, and can be conveniently adopted for the routine quality control analysis of the tablet.

  18. 丙戊酸镁缓释片联合盐酸多奈哌齐胶囊改善老年性痴呆患者认知行为的疗效观察%Magnesium Valproate Tablet Combined with Donepezil Hydrochloride Donepezil Capsules Improve Senile Dementia Cognitive Behavioral Effect Observed

    Institute of Scientific and Technical Information of China (English)

    范丽伟

    2013-01-01

    目的:评价丙戊酸镁缓释片联合盐酸多奈哌齐胶囊改善老年性痴呆(AD)患者认知行为的有效性及安全性.方法:对32例老年性痴呆患者采用丙戊酸镁缓释片联合盐酸多奈哌齐胶囊治疗16 w,治疗前后用简易智能精神状态检查量表(MMSE)、AD评定量表(ADAS)及Blessed-Roth痴呆量表评价患者认知功能及痴呆严重程度、精神行为异常(ADAS non-cog)及日常生活自理能力(ADL),并进行安全性评价.结果:丙戊酸镁缓释片联合盐酸多奈哌齐胶囊治疗后,老年性痴呆患者MMSE评价较治疗前提高(P<0.01),ADAS认知部分、ADAS non-cog及Blessed-Roth日常生活自理能力部分均有改善(P<0.01,P<0.05);1例出现轻度副作用.结论:丙戊酸镁缓释片联合盐酸多奈哌齐胶囊治疗老年性痴呆患者有较好的疗效并安全性好,副作用小.%Objective:To evaluate magnesium valproate sustained-release tablets joint donepezil hydrochloride capsules improve the efficacy and safety of Alzheimer's disease (AD) patients with cognitive behavioral.Methods:32 cases of senile dementia patients with magnesium valproate sustained-release tablets joint donepezil hydrochloride capsules 16 weeks of treatment,before and after treatment with a simple mental state examination Scale (MMSE),AD Assessment Scale (ADAS) and Blessed-Roth The dementia scale evaluation of patients with cognitive function and dementia severity,behavioral and psychological abnormalities (ADAS non-cog)and activities of daily living ability (ADL),and the safety evaluation.Results:magnesium valpronte sustained-release tablets joint donepezil hydrochloride capsules treatment MMSE evaluation of patients with senile dementia than before treatment (P < 0.01),ADAS cognitive portion of the ADAS non-cog and the Blessed-Roth daily livingThe ability of parts were improved (P < 0.01,P <0.05) ; cases of mild side effects.Conclusion:The sustained-release tablets of magnesium valproate joint

  19. Fabrication of Spherical AlSi10Mg Powders by Radio Frequency Plasma Spheroidization

    Science.gov (United States)

    Wang, Linzhi; Liu, Ying; Chang, Sen

    2016-05-01

    Spherical AlSi10Mg powders were prepared by radio frequency plasma spheroidization from commercial AlSi10Mg powders. The fabrication process parameters and powder characteristics were investigated. Field emission scanning electron microscope, X-ray diffraction, laser particle size analyzer, powder rheometer, and UV/visible/infrared spectrophotometer were used for analyses and measurements of micrographs, phases, granulometric parameters, flowability, and laser absorption properties of the powders, respectively. The results show that the obtained spherical powders exhibit good sphericity, smooth surfaces, favorable dispersity, and excellent fluidity under appropriate feeding rate and flow rate of carrier gas. Further, acicular microstructures of the spherical AlSi10Mg powders are composed of α-Al, Si, and a small amount of Mg2Si phase. In addition, laser absorption values of the spherical AlSi10Mg powders increase obviously compared with raw material, and different spectra have obvious absorption peaks at a wavelength of about 826 nm.

  20. Release Characteristics of Diltiazem Hydrochloride Wax-Matrix ...

    African Journals Online (AJOL)

    Michael Horsfall

    diltiazem hydrochloride-wax matrix granules with sintering. ... The drug release was by Higuchi controlled diffusion mechanism and it followed ... of plastic matrix tablets. Polymer films with different permeability have been .... More so, with increase in temperature and ..... characterization of ibuprofen-cetyl alcohol beads by.

  1. Clinical observation of methadone hydrochloride tablet in the treatment of moderate and severe cancer pain%盐酸美沙酮片治疗中重度癌性疼痛的临床观察

    Institute of Scientific and Technical Information of China (English)

    陈碧茵; 林丹; 李一璟

    2015-01-01

    目的:观察盐酸美沙酮片(美沙酮)治疗中重度癌性疼痛的临床效果、不良反应及生活质量改善情况。方法42例中重度癌性疼痛患者给予美沙酮镇痛治疗,初始剂量5 mg/12 h,根据疼痛情况调整剂量,直至患者无痛或基本无痛,每位患者至少治疗15 d以上。观察患者的疼痛缓解情况、生活质量评分及不良反应。结果42例患者经过个体化给药后确定最终剂量为5~70 mg,每12小时1次,绝大部分患者疼痛达到明显缓解以上,疼痛的总缓解率为90.5%,其中完全缓解11例(26.2%),明显缓解27例(64.3%),对中度疼痛的缓解率为93.8%,重度疼痛的缓解率为88.5%。治疗前中位KPS评分为50分,治疗后中位KPS评分为75分,患者的生活质量明显改善(P<0.05)。全组KPS评分9例(21.4%)明显改善,13例(31.0%)有改善,20例(47.6%)达到稳定,无评分下降病例;不良反应少且轻微。结论美沙酮治疗中重度癌性疼痛安全有效,不良反应发生率较低,能够明显提高患者的生活质量。%Objective To observe the clinical effect,adverse reaction,and improvement of patient’s living quality of methadone hydrochloride tablet (methadone) treating moderate and severe cancer pain. Methods Forty-two patients suf-fering from moderate or severe cancer pain were treated by methadone at an initial dosage of 5 mg/12 h.According to severity of pain,the dosage of methadone was adjusted until these patients didn’t feel pain or basically had no sensation of pain.The course of treatment for each participant lasted at least 15 days.At the same time,pain relief and quality of life were scored,and adverse reaction were observed. Results After 42 patients were given the individualized drug ad-ministration,the final dosage was set from 5 to 70 mg,at an interval of 12 h.After taking methadone,the vast majority of patients with pain was more than significantly alleviate,and the total alleviation

  2. Cartap Hydrochloride Poisoning.

    Science.gov (United States)

    Kalyaniwala, Kimmin; Abhilash, Kpp; Victor, Peter John

    2016-08-01

    Cartap hydrochloride is a moderately hazardous nereistoxin insecticide that is increasingly used for deliberate self-harm in India. It can cause neuromuscular weakness resulting in respiratory failure. We report a patient with 4% Cartap hydrochloride poisoning who required mechanical ventilation for 36-hours. He recovered without any neurological deficits. We also review literature on Cartap hydrochloride poisoning.

  3. Dexmethylphenidate--Novartis/Celgene. Focalin, D-MPH, D-methylphenidate hydrochloride, D-methylphenidate, dexmethylphenidate, dexmethylphenidate hydrochloride.

    Science.gov (United States)

    2002-01-01

    Celgene has developed a chirally pure form of methylphenidate (Ritalin), called dexmethylphenidate [d-methylphenidate, d-methylphenidate hydrochloride, d-MPH; Focalin]. The drug has been launched in the USA and is undergoing registration in Canada for the treatment of children with attention-deficit hyperactivity disorder (ADHD). Dexmethylphenidate is the single isomer version of racemic methylphenidate (Ritalin), which contains the active d isomer of Ritalin. Dexmethylphenidate acts via the inhibition of reuptake of norepinephrine and dopamine. Research is ongoing to further clarify the mode of therapeutic action in ADHD. Dexmethylphenidate was developed with the aim of reducing drug load, adverse events and drug interactions. Dexmethylphenidate provides effective management of attention-deficit hyperactivity disorder at half the dose of Ritalin. In April 2000, worldwide rights (excluding Canada) to dexmethylphenidate were granted to Novartis. Celgene has also granted Novartis rights to all related intellectual properties and patents. Novartis will fund all remaining development and marketing expenses required for regulatory approval and commercialisation of dexmethylphenidate. Crystaal Corporation, the marketing division of Biovail Corporation International, has exclusive Canadian marketing rights for all formulations of dexmethylphenidate. Novartis launched dexmethylphenidate (Focalin) in the USA during Q1 2002. It is available as a D-shaped tablet (2.5, 5 and 10 mg doses). Novartis had planned to use the tradename Ritadex, however the FDA recommended an alternative name due to potential prescribing errors with Ritalin. The finalized tradename to be used is Focalin. In July 2001, a new drug submission was filed with Canada's Therapeutic Products Programme for dexmethylphenidate in the treatment of attention-deficit disorder and attention-deficit hyperactivity disorder. Novartis is also developing an extended-release version of chirally pure dexmethylphenidate

  4. Compound Glycyrrhizin Tablets Combined with Levocetirizine Hydrochloride in Treating Neurodermatitis in 43 Cases%复方甘草酸苷片联合盐酸左西替利嗪治疗神经性皮炎43例临床疗效观察

    Institute of Scientific and Technical Information of China (English)

    黄河

    2016-01-01

    Objective To explore the clinical efficacy of Compound Glycyrrhizin Tablets combined with levocetirizine hydrochloride in the treatment of neurodermatitis. Methods 86 cases of neurodermatitis patients were randomly divided into the treatment group and the control group, both of which were given treatment of mizolastine and clobetasol propionate cream. The treatment group was additionally given Compound Glycyrrhizin Tablets and levocetirizine hydrochloride orally. After treatment of 4 weeks, the symptom score, skin lesion score and clinical efficacy of the two groups were compared. Results After treatment of 4 weeks, the control group clinical effective rate was 83. 72%, which was obviously lower than 95. 35% of the treatment group ( P < 0. 05 ) . The symptoms score of the treatment group was ( 0. 24 ± 0. 12 ) points, which was obviously lower than ( 0. 89 ± 0. 29 ) points of the control group ( P < 0. 05 ) . The skin lesion score of the treatment group was ( 0. 42 ± 0. 14 ) points, which was obviously lower than ( 1. 03 ± 0. 20 ) points of the control group ( P < 0. 05 ) . Conclusion Compound Glycyrrhizin Tablets combined with levocetirizine hydrochloride has better clinical efficacy in treating nerve dermatitis.%目的:探讨复方甘草酸苷片联合盐酸左西替利嗪治疗神经性皮炎的临床疗效。方法选择86例神经性皮炎患者,随机均分为治疗组及对照组,均给予咪唑斯汀、丙酸氯倍他索乳膏治疗,治疗组患者加用复方甘草酸苷片及盐酸左西替利嗪口服溶液。治疗4周后比较两组症状积分、皮损积分及临床疗效。结果治疗4周后,对照组患者临床有效率为83.72%,明显低于治疗组的95.35%,差异有统计学意义( P<0.05);治疗组症状积分为(0.24±0.12)分,明显低于对照组的(0.89±0.29)分,差异有统计学意义( P<0.05);治疗组皮损积分为(0.42±0.14)分,明显低于对照组的(1.03±0.20)分

  5. Effects of Oxycodone Hydrochloride Controlled-release Tablets on Cancer-relate Pain following Different Routes of Administration%盐酸羟考酮缓释片不同给药途径治疗癌痛的临床观察

    Institute of Scientific and Technical Information of China (English)

    尹卫华; 范惠珍; 夏红梅; 陈凤舞; 李丽华; 樊松; 何健; 庄小捷; 陈金平

    2013-01-01

    目的 观察盐酸羟考酮缓释片口服给药与直肠给药2种途径治疗癌痛的疗效和不良反应.方法 选择宜春市人民医院肿瘤科2012年2月至2013年2月收治的癌症晚期患者60例,按随机数字表法将60例患者分为口服给药组和直肠给药组,每组30例,比较2种给药途径的缓解疼痛的疗效、改善患者生活质量以及不良反应发生情况.结果 口服给药组疼痛缓解有效率为93.3%,直肠给药组有效率为90.0%,疗效和生活质量的改善相当,2组比较差异无统计学意义(P>0.05);直肠给药组消化道不良反应低于口服给药组,2组比较差异有统计学意义(P<0.05).结论 直肠给药与口服给药止痛效果相当;直肠给药不良反应少,对于胃肠道梗阻、意识障碍的患者,不失为一种简单方便、安全有效的方法.%Objective To compare the curative efficacy and side effect of orally and rectally administered oxycodone hydrochloride controlled-release tablets in cancer-relate pain.Methods Sixty advanced cancer patients treated in Yichun People's Hospital between February 2012 and February 2013 were randomly administered oxycodone hydrochloride controlled-release tablets via oral route (oral administration group,n=30) or rectal route (rectal administration group,n=30).Pain relief,quality of life and side effect were compared between the two groups.Results The effectiveness of pain relief was 93.3% in oral administration group and 90.0% in rectal administration group.There were no significant differences in the improvement in the efficacy and quality of life between the two groups (P>0.05)).However,the incidence of gastrointestinal adverse reactions in rectal administration group was significantly lower than that in oral administration group (P<0.05).Conclusion There was no obvious difference in the effectiveness of pain relief between orally and rectally administered oxycodone hydrochloride controlled-release tablets

  6. 盐酸哌甲酯控释剂治疗儿童注意缺陷与多动障碍的疗效探析%The Clinical Observation of Methylphenidate Hydrochloride Controlled Re-lease Tablets in the Treatment of Attention Deficit and Hyperactivity Disor-der in Children

    Institute of Scientific and Technical Information of China (English)

    贾小红

    2015-01-01

    目的:探析盐酸哌甲酯控释剂治疗儿童注意缺陷与多动障碍效果。方法整群选择2012年6月—2014年8月该院儿科多动症门诊就诊的132例注意缺陷与多动障碍患儿。并随机分为控释组(72例)与速释组(60例),控释组患儿给予盐酸哌甲酯控释片治疗,速释组患儿给予速释哌甲酯片治疗。观察给药2周、6个月后两组患儿用药依从性、用药不良反应、行为及注意力改善情况。结果两组患儿用药后不良反应均较轻。给药2周、6个月后控释组临床有效率分别为98.6%、94.4%,均优于速释组的91.7%、53.3%(P<0.05),比较给药1个月后两组患儿用药依从性不太明显,给药3个月、6个月及12个月后,控释组患儿依从性则明显优于速释组(P<0.05)。结论对于儿童注意缺陷多动障碍,应用哌甲酯控释剂治疗不仅能显著提高患儿注意力与认知功能,而且药物不良反应少,患儿依从性高。%Objective To study the effect of methylphenidate hydrochloride controlled release tablets in the treatment of at-tention deficit and hyperactivity disorder in children. Methods 132 cases of children with attention deficit and hyperactivity disorder treated in our hospital from June 2012 to August 2014 were selected and randomly divided into control group (72 cases) and rapid release group (60 cases), patients in the control group were given methylphenidate hydrochloride controlled release tablets treatment and patients in the rapid release group were given rapid release of methyl ester hydrochloride tablets treatment. After 2 weeks and 6 months from giving medicine, Medication compliance, adverse drug reactions and the improvement of behavior and attention of the two groups were observed. Results The adverse reactions of the two groups after taking medicine were mild. After 2 weeks and 6 months from giving medicine, the clinical effective rate of the control group was 98.6% and 94

  7. 盐酸羟考酮缓释片治疗胃癌患者中重度癌痛的临床疗效观察%Efficacy of Oxycodone Hydrochloride Controlled Release Tablet in the Treatment of Gastric Cancer Patients with Moderate to Severe Cancer Pain

    Institute of Scientific and Technical Information of China (English)

    赵松峰; 张亚玲; 张晓; 师秀琴; 张祥; 张晓坚

    2016-01-01

    Objective To observe efficacy and toxicities of oxycodone hydrochloride controlled release tablet in the treatment of gastric cancer patients with moderate to severe cancer pain. Methods The 135 cases of gastric cancer patients with moderate to severe cancer pain were was administrated with oxycodone hydrochloride controlled release tablet. The starting dose was 10 to 20 mg every 12 h,the dose was adjusted according to pain degree. Every patients were treated for two weeks. The pain relief,quality of life and toxicities were evaluated after treatment. Re-sults For the 135 patients,the NRS score after treatment(1. 68 ± 0. 98)was lower than that before treatment (7. 22 ± 2. 13)(P ﹤ 0. 05). The cancer pain relief rate was 92. 6% . The improvement rate of quality of life was 74. 1% . The main toxicities were light degree nausea and vomiting,constipation drowsiness. Conclusion Oxyc-odone hydrochloride controlled release tablet can control cancer pain and improve quality of life in the treatment of gastric cancer patients with moderate to severe cancer pain,and has good safety.%目的:探讨盐酸羟考酮缓释片用于胃癌患者中重度癌痛的临床疗效和毒副反应。方法135例胃癌中重度癌痛患者均接受口服盐酸羟考酮缓释片控制癌痛,初始剂量10~20 mg/次,q12 h,用药过程中根据疼痛评估情况进行剂量调整,直至癌痛控制良好。2周后采取 NRS 评分法进行疼痛评分,并观察疼痛缓解情况、生活质量、药物毒副反应等。结果所有135例患者治疗后 NRS 评分为(1.68±0.98)分,明显低于治疗前的(7.22±2.13)分,差异有统计学意义(P ﹥0.05)。治疗后总疼痛缓解率为92.6%。生活质量改善率为74.1%。主要毒副反应为恶心呕吐、便秘、嗜睡等,均为轻度,未影响治疗的顺利进行。结论盐酸羟考酮缓释片用于胃癌患者能够良好控制中重度癌痛,明显改善患者的生活质量,且用药较为安全。

  8. Effectiveness and safety of a 10mg warfarin initiation nomogram in Asian population.

    Science.gov (United States)

    Chandriah, Haarathi; Kumolosasi, Endang; Islahudin, Farida; Makmor-Bakry, Mohd

    2015-05-01

    Anticoagulant responses to warfarin vary among patients, based on genetic factors, diet, concomitant medications, and disease state. We evaluated the effectiveness and safety of a 10mg warfarin initiation nomogram in an Asian population. Retrospective cross-sectional audit studies were conducted from March 2009 to March 2010. The use of a 10mg-loading dose to initiate warfarin treatment resulted in 33(84.6%) patients attaining a therapeutic INR within four days (mean time, 2.6 days). There was no significant correlation between age, gender, race, and serum albumin for the time to reach a therapeutic INR. A significant correlation was noted for patient's baseline INR and time to reach a therapeutic INR (Pwarfarin nomogram was effective in rapidly achieving a therapeutic INR. However, the nomogram's safety is debatable owing to the high over-anticoagulation rate warfarin-administered patients. Caution is recommended in the initiation of warfarin treatment using the 10mg nomogram.

  9. Mifepristone 5 mg versus 10 mg for emergency contraception: double-blind randomized clinical trial

    Directory of Open Access Journals (Sweden)

    Carbonell JL

    2015-01-01

    Full Text Available Josep Lluis Carbonell,1 Ramon Garcia,2 Adriana Gonzalez,2 Andres Breto,2 Carlos Sanchez2 1Mediterranea Medica Clinic, Valencia, Spain; 2Eusebio Hernandez Gynecology and Obstetrics Teaching Hospital, Havana, Cuba Purpose: To estimate the efficacy and safety of 5 mg and 10 mg mifepristone for emergency contraception up to 144 hours after unprotected coitus. Methods: This double-blind randomized clinical trial was carried out at Eusebio Hernandez Hospital (Havana, Cuba. A total of 2,418 women who requested emergency contraception after unprotected coitus received either 5 mg or 10 mg mifepristone. The variables for assessing efficacy were the pregnancies that occurred and the fraction of pregnancies that were prevented. Other variables assessed were the side effects of mifepristone, vaginal bleeding, and changes in the date of the following menstruation. Results: There were 15/1,206 (1.2% and 9/1,212 (0.7% pregnancies in the 5 mg and 10 mg group, respectively (P=0.107. There were 88% and 93% prevented pregnancies in the 5 mg and 10 mg group, respectively. The side effect profiles were similar in both groups. Delayed menstruation ≥7 days was experienced by 4.9% and 11.0% of subjects in the 5 mg and 10 mg group, respectively (P=0.001. There was a significant high failure rate for women weighing >75 kg in the 5 mg group. Conclusion: It would be advisable to use the 10 mg dose of mifepristone for emergency contraception as there was a trend suggesting that the failure rate of the larger dose was lower. Keywords: mifepristone, emergency contraception

  10. Development of mini-tablets with 1mm and 2mm diameter.

    Science.gov (United States)

    Tissen, Corinna; Woertz, Katharina; Breitkreutz, Joerg; Kleinebudde, Peter

    2011-09-15

    The feasibility of formulating mini-tablets with 1mm diameter on a rotary-die press in comparison to mini-tablets of 2mm was investigated. To gain insight into the production of 1mm mini-tablets, three model drugs of different compression characteristics were chosen, namely quinine hydrochloride, ibuprofen and spray-dried gentian extract. A high drug load in combination with robust and reproducible mechanical properties was requested. Depending on the individual drug substance, mini-tablets were produced by direct compression or after roll-compaction/dry granulation. The tensile strength, mass, and their variation coefficients were determined to assess the mechanical properties of the tablets. The content uniformity and the dissolution behavior of selected batches were analyzed. For the first time 1mm mini-tablets could be successfully produced by direct compression (90% quinine hydrochloride; 90% dried gentian extract) and after roll compaction (70% ibuprofen). Depending on the applied compression pressure, 1mm mini-tablets with quinine hydrochloride exhibited robust mechanical properties (e.g. median tensile strength of 2.02N/mm(2)) with equal or lower variance of distribution compared to the 2mm compacts. With respect to content uniformity of dosage forms, 1mm mini-tablets containing 80% quinine hydrochloride met the requirements of the European Pharmacopeia (AV=6.8).

  11. Tablet Weaving

    Science.gov (United States)

    Kren, Margo

    1976-01-01

    Article described a weaving technique called tablet weaving, an ancient textile process that provides opportunity for making a variety of items, such as guitar straps, belts, and decorative bands. (Author/RK)

  12. Biowaiver monographs for immediate release solid oral dosage forms based on biopharmaceutics classification system (BCS) literature data: verapamil hydrochloride, propranolol hydrochloride, and atenolol.

    Science.gov (United States)

    Vogelpoel, H; Welink, J; Amidon, G L; Junginger, H E; Midha, K K; Möller, H; Olling, M; Shah, V P; Barends, D M

    2004-08-01

    Literature data related to the Biopharmaceutics Classification System (BCS) are presented on verapamil hydrochloride, propranolol hydrochloride, and atenolol in the form of BCS-monographs. Data on the qualitative composition of immediate release (IR) tablets containing these active substances with a Marketing Authorization (MA) in the Netherlands (NL) are also provided; in view of these MA's the assumption was made that these tablets were bioequivalent to the innovator product. The development of a database with BCS-related data is announced by the International Pharmaceutical Federation (FIP).

  13. 芬太尼透皮贴剂与盐酸羟考酮缓释片治疗中重度癌痛疗效和安全性的Meta分析%Meta-analysis of Curative Effect and Safety of Transdermal Fentanyl and Oxycodone Hydrochloride Sustained-release Tablets in the Treatment of Moderate and Severe Cancer Pain

    Institute of Scientific and Technical Information of China (English)

    刘思; 余正; 胡霞

    2015-01-01

    Objective: To evaluate the curative effect and safety of transdermal fentanyl and oxycodone hy-drochloride sustained-release tablets in the treatment of moderate and severe cancer pain . Methods: Based on the literature review from CNKI and Wanfang database and med . Wanfang data , literature and information were ex-tracted according to certain inclusion and exclusion criteria. Data was analyzed using RevMan 5.3 software. Results:A total of 4 research papers involved 635 cases were included . The results of meta-analysis showed that the inci-dence of pain remission was not significantly different between the two groups using transdermal fentanyl and oxy-codone hydrochloride sustained-release tablets [ RR=0 . 99 , 95%CI ( 0 . 94 , 1 . 04 ) , P=0 . 72 ] . No significant difference was found between the two groups in the incidence of constipation [ RR=0 . 83 , 95%CI ( 0 . 53 , 1 . 28 ) , P=0 . 39 ] , dizzi-ness [ RR=0 . 85 , 95%CI ( 0 . 46 , 1 . 57 ) , P=0 . 61 ] , somnolence [ RR=0 . 49 , 95%CI ( 0 . 22 , 1 . 06 ) , P=0 . 07 ] , urinary reten-tion [ RR=0 . 53 , 95%CI ( 0 . 15 , 1 . 89 ) , P=0 . 33 ] and mental disorder [ RR=0 . 72 , 95%CI ( 0 . 29 , 1 . 78 ) , P=0 . 47 ] , except the incidence of nausea and vomitting [ RR=0 . 45 , 95%CI ( 0 . 26 , 0 . 76 ) , P=0 . 003 ] , with incidence of 6 . 03%( 17/282 ) and 11 . 33%( 40/353 ) respectively . Conclusion: Transdermal fentanyl and oxycodone hydrochloride sustained-release tablets had similar efficacy in the treatment of moderate and severe cancer pain . The incidence of nausea and vomit-ing caused by transdermal fentanyl was lower than oxycodone hydrochloride sustained-release tablets but the safety of the two drugs are similar .%目的:评价芬太尼透皮贴剂和盐酸羟考酮缓释片治疗中重度癌痛的临床疗效和安全性。方法:检索CNKI、万方数据库和万方医学网获得相关文献,按照一定的纳入和排除标准筛选文献并提取信息,采用RevMan 5.3软件进

  14. 盐酸羟考酮控释片联合普瑞巴林治疗癌性神经病理性疼痛的临床研究%Clinical study of oxycodone hydrochloride controlled-release tablets combined with pregabalin in the treatment of malignant neuropathic pain

    Institute of Scientific and Technical Information of China (English)

    陈强; 李焕丽; 何斐; 郭素香

    2014-01-01

    目的:观察盐酸羟考酮控释片联合普瑞巴林治疗癌性神经病理性疼痛的临床疗效及不良反应。方法选择疼痛门诊治疗的癌性疼痛患者87例,口服盐酸羟考酮控释片1周,并进行随访调查。接受治疗患者第8天11点数字分级法评定( NRS)﹤4入A组,继续给予羟考酮治疗2周;NRS≥4随机入B1、B2组,B1组继续服用羟考酮2周, B2组联合普瑞巴林治疗2周。观察三组患者的疼痛评分及不良反应情况。结果84例(96.55%)完成第一阶段治疗。在第二阶段A组、B1组、B2组分别有28、27、26例患者。三组疼痛评分第15天均降低,第22天无改善,B2组比B1组第22天疼痛评分降低,但差异无统计学意义(P﹥0.05)。B2组羟考酮用量比B1组明显减少(P﹤0.05)。三组不良反应观察中便秘发生率最高,分别为17.9%、29.6%、34.6%。结论盐酸羟考酮控释片联合普瑞巴林治疗癌性神经病理性疼痛疗效明确,能够减少盐酸羟考酮控释片用量,是治疗癌性疼痛性价比较高的方案。%Objective To observe the clinical effect and adverse reactions of oxycodone hydro-chloride controlled-release tablets combined with pregabalin in the treatment of malignant neuropathic pain. Methods Eighty-seven patients with cancer pain admitted in pain clinic were chose,oxycodone hydro-chloride controlled-release tablets were orally given for 1 week,and the patients were followed-up. On the eighth day,patients with numeric rating scale( NRS)﹤4 were enrolled in group A,and were given oxyc-odone treatment for another 2 weeks. Patients with NRS≥4 were randomly divided into group B1 and group B2,the patients in group B1 were given oxycodone for another 2 weeks,and patients in group B2 were given combined treatment of oxycodone and pregabal for 2 weeks. The pain scores and adverse reactions were ob-served among the three groups. Results Eighty-four patients( 96. 55%)completed the

  15. 胰岛素联合西格列汀二甲双胍片治疗2型糖尿病肥胖心功能不全患者的疗效观察%Treatment effect observation of insulin combined with Sitagliptin Phosphate/metformin Hydrochloride Tablets in treating type 2 diabetic obesity heart failure

    Institute of Scientific and Technical Information of China (English)

    由晓丹

    2015-01-01

    目的:研究胰岛素联合西格列汀二甲双胍片治疗2型糖尿病肥胖心功能不全患者的疗效。方法将2012年8月—2014年8月期间该院收治的76例2型糖尿病肥胖伴心功能不全患者纳入研究,随机分为两组,对照组患者仅给予胰岛素治疗,观察组患者给予胰岛素联合西格列汀二甲双胍片治疗,比较两组患者的血糖情况、胰岛素用量、心功能情况。结果(1)血糖情况:观察组患者的空腹血糖、餐后血糖、糖化血红蛋白含量低于对照组;(2)胰岛素抵抗:观察组患者的 HOMA-IR、单日胰岛素用量低于对照组;(3)心功能情况:观察组患者的E峰值、LVEDD、LVEF高于对照组。结论胰岛素联合西格列汀二甲双胍片治疗有助于控制血糖水平、改善胰岛素抵抗和心功能,是治疗2型糖尿病肥胖患者伴心功能不全的理想方法。%Objective To study effect of insulin combined with Sitagliptin Phosphate/metformin Hydrochloride Tablets in treating type 2 diabetic obesity heart failure. Methods 76 cases of type 2 diabetic obesity heart failure patients in our hospital from 2012 March to 2014 April were enrolled and randomly divided into two groups. Control group received insulin therapy, observation group received insulin combined with Sitagliptin Phosphate/metformin Hydrochloride Tablets. Then blood glucose, insulin dosage, heart function were compared. Results (1): blood glucose condition:fasting blood glucose, postprandial blood glucose and glycosy-lated hemoglobin content of observation group were lower than those of the control group;(2)insulin resistance: HOMA-IR, daily insulin dosage of observation group were lower than those of control group;(3)heart function:E peak, LVEDD, LVEF of observation group were higher than those of control group. Conclusion insulin combined with Sitagliptin Phosphate/metformin Hydrochloride treatment is helpful to control blood sugar levels, improve

  16. 盐酸尼卡地平单层渗透泵片的制备及其体外释放行为的考察%Preparation of Nicardipine Hydrochloride Monolithic Osmotic Pump Tablets and Its in Vitro Release Behavior

    Institute of Scientific and Technical Information of China (English)

    马锐; 王洪亮; 刘玉玲; 夏学军; 董武军

    2011-01-01

    目的:制备盐酸尼卡地平(Nic)单层渗透泵片,提高难溶性药物溶解度,实现平稳释药.方法:以吸水速率、渗透压及Nic 溶解度为指标,从柠檬酸、氯化钠、乳糖和甘露醇中筛选适当的渗透压促进剂,制备Nic单层渗透泵片,并考察其体外释放行为,拟合释药模型.结果:4种渗透压促进剂中,以柠檬酸所制片剂吸水速率较高(71.83mg·h-1),渗透压值最高,可使Nic溶解度(7.90mg·mL-1)提高约10倍(80.33mg·mL-1);以柠檬酸为渗透压促进剂制备的渗透泵片,其24h药物累积释放度在95%以上,且符合零级释药模型.结论:柠檬酸能显著提高Nic溶解度;以柠檬酸为渗透压促进剂制备的Nic单层渗透泵片可平稳释药,且24 h内基本释放完全.%OBJECTIVE: To prepare the monolithic osmotic pump tablets of nicardipine hydrochloride (Nic) which can enhance the dissolution and make a good performance on its' releasing profile. METHODS: Using absorbing rate, osmotic pressure and the solubility of Nic as index, the optimal osmotic pressure accelerator was selected among critic acid, sodium chloride, lactose and mannitol to prepare Nic monolithic osmotic pump tablets. The drug release behavior of Nic monolithic osmotic pump tablets was investigated and drug release mode was fitted. RESULTS: Among 4 kinds of osmotic pressure accelerator, citric acid had high absorbing rate (71.83 mg·h-1) and osmotic pressure, the dissolubility of Nic in citric acid (80.33 mg·mL-1) was ten times than it in water (7.90 mg·mL-1). Accumulative release rate of Nic monolithic osmotic pump tablets which was prepared using citric acid as osmotic pressure accelerator was more than 95% within 24 h and accorded with zero order kinetics equation. CONCLUSION: Citric acid can improve the solubility of Nic significantly. Nic monolithic osmotic pump tablets which were prepared using citric acid as osmotic pressure accelerator can release in full during 24 h.

  17. Flunarizine in migraine prophylaxis: efficacy and tolerability of 5 mg and 10 mg dose levels.

    Science.gov (United States)

    Centonze, V; Magrone, D; Vino, M; Caporaletti, P; Attolini, E; Campanale, G; Albano, O

    1990-02-01

    The use of flunarizine, a drug which has proven its efficacy in migraine, is often associated with important side effects. The aim of this paper has been to check their incidence at different dose levels (5 mg vs 10 mg). Our data confirm the occurrence of important side effects (in particular weight gain); on the other hand, they emphasize the dose-dependency of the side effects.

  18. [Neuropharmacological studies on tolperisone hydrochloride (author's transl)].

    Science.gov (United States)

    Fujii, Y; Ishii, Y; Suzuki, T; Murayama, S

    1979-10-01

    Neuropharmacological properties of tolperisone hydrochloride (2,4'-dimethyl-3-piperidinopropiophenone hydrochloride) were investigated in mice, rats and cats. Tolperisone inhibited the spontaneous movement and methamphetamine-induced hyperactivity in mice and the ED50 was approx. 50 mg/kg, s.c. At this dose, tolperisone did not prolong the pentobarbital-induced sleeping time. Tolperisone inhibited convulsions induced by pentylenetetrazol, nicotine and maximum electric shock, but did not affect convulsions induced by strychnine and picrotoxin. Tolperisone induced muscle relaxation in mice and rats in several pharmacological tests, but did not affect neuro-muscular transmission. Tolperisone did not affect conditioned avoidance response in rats and methamphetamine-induced rotational behaviour in nigro-lesioned rats. Tolperisone reduced decerebrated rigidity in cats with i.v. administration of 5 approximately 10 mg/kg and intraduodenal administration of 50 approximately 100 mg/kg. Tolperisone elicited a slight drowsy pattern in the spontaneous EEG of cats at 5 approximately 10 mg/kg, i.v., and inhibited the EEG arousal response and pressor response to stimulation of mesencephalic reticular formation or posterior hypothalamic area. These results suggest that inhibition of the activity in the gamma pathway descending from the mesencephalic reticular formation may be involved in the mechanism of muscle relaxant action of tolperisone.

  19. Formulation of Sustained-Release Matrix Tablets Using Cross ...

    African Journals Online (AJOL)

    Erah

    JSS College of Pharmacy, JSS University, Mysore, Karnataka-570015, India. Abstract. Purpose: To develop sustained release matrix tablets of diltiazem hydrochloride (DTZ) using ... channel blocker that is widely prescribed for ..... appearance of new peaks which were absent ... penetration of dissolution media into the.

  20. 小儿智力糖浆联合盐酸哌甲酯片治疗儿童注意缺陷多动障碍的疗效观察%Clinical observation of Xiaoer Zhili Syrup combined with Methylphenidate Hydrochloride Tablets in treatment of attention deficit hyperactivity disorder

    Institute of Scientific and Technical Information of China (English)

    朱小冰

    2015-01-01

    目的:探讨小儿智力糖浆联合盐酸哌甲酯片治疗儿童注意缺陷多动障碍的临床疗效。方法选择2012年1月—2014年12月重庆市开县人民医院儿科收治儿童注意缺陷多动障碍患者90例,随机分为对照组和治疗组,每组45例。对照组患者口服盐酸哌甲酯片,2片/次,1次/d。治疗组患者在对照组的治疗基础上口服小儿智力糖浆,10 mL/次,2次/d。3周为1个疗程,全部患者均治疗3个疗程。观察两组的临床疗效,同时比较两组治疗前后Conner行为评定量表各因子评分及不良反应情况。结果治疗后,对照组和治疗组总有效率分别为77.78%、88.89%,两组比较差异具有统计学意义(P<0.05)。治疗后,两组患者冲动多动、多动指数、学习问题、品行问题、焦虑、身心问题评分均较较治疗前显著降低,同组治疗前后差异有统计学意义(P<0.05);且治疗组治疗后各评分均显著低于对照组,两组比较差异有统计学意义(P<0.05)。两组不良反应发生率比较差异无统计学意义。结论小儿智力糖浆联合盐酸哌甲酯片治疗儿童注意缺陷多动障碍,能够显著提高临床疗效,且无严重不良反应,具有一定的临床推广价值。%Objective To investigate the clinical effect of Xiaoer Zhili Syrup combined with Methylphenidate Hydrochloride Tablets in treatment of attention deficit hyperactivity disorder.Methods Patients (90 cases) with attention deficit hyperactivity disorder in the derpartment of paediatrics of People’s Hospital of Kaixian County in Chongqing from January 2012 to December 2014 were randomly divided into control and treatment groups. Each group had 45 cases. Patients in control group werepo administered with Methylphenidate Hydrochloride Tablets, 2 tablets/time, once daily. Patients in treatment group werepo administered with Xiaoer Zhili Syrup on the basis of the control group, 10 m

  1. Establishment of Drug Release Determination Method for Methylphenidate Hydrochloride Bipolar Con-trolled Release Osmotic Pump Tablets%盐酸哌甲酯双相控释渗透泵片释放度测定方法的建立

    Institute of Scientific and Technical Information of China (English)

    夏琼琼; 刘辉; 何佩芳

    2016-01-01

    Objective:To establish the drug release determination conditions and method for methylphenidate hydrochloride bipolar controlled release osmotic pump tablets. Methods: The drug release of the tablets was determined by HPLC using a Diamonsil C18 (250 mm × 4. 6 mm, 5 μm) column with acetonitrile-KH2 PO4 (0. 02 mol·L-1 ,and pH was adjusted to 3. 0 by 1% H3 PO4 solution) (30∶ 70) as the mobile phase at a flow rate of 1 ml·min-1 , the column temperature was 35 ℃ and the injection volume was 20 μl. The effects of release medium, release apparatus and rotation speed on the release of methylphenidate hydrochloride bipolar controlled release osmotic pump tablets were studied as well. Results:The established drug release determination method had a good linear rela-tionship within the range of 1. 0-24. 0 μg·ml-1(r=0. 999 5), and the average recovery was 100. 5%(RSD=1. 58%, n = 6). Un-der the conditions of 900 ml pH 3. 0 phosphate buffer solution as the release medium and the rotation speed of 50 r·min-1 , the drug was quickly released in 0-2h, and then the release behavior was complied with a zero-level model in vitro in 2-10h with the release e-quation of Q=5. 505t+44. 221(r=0. 994 5). Conclusion:The method is simple, accurate and reliable, and suitable for the quality control of methylphenidate hydrochloride bipolar controlled release osmotic pump tablets.%目的::建立盐酸哌甲酯双相控释渗透泵片释放度的测定条件和释放度的测定方法。方法:采用HPLC法测定盐酸哌甲酯双相控释渗透泵片的释放度,色谱条件:Diamonsil C18(250 mm ×4.6 mm,5μm)为色谱柱,流动相为0.02 mol·L-1磷酸二氢钾溶液(用1%磷酸溶液调节pH为3.0)∶乙腈=70∶30,检测波长为220 nm,流速为1.0 ml·min-1,柱温为35℃,进样量为20μl;考察释放介质、不同释放装置和转速对盐酸哌甲酯双相控释渗透泵片释放度的影响。结果:建立的释放量测定方法在1.0~24.0μg·ml-1

  2. Comparison of initial loading doses of 5 mg and 10 mg for warfarin therapy

    Directory of Open Access Journals (Sweden)

    Sidnei Lastória

    2014-03-01

    Full Text Available CONTEXT: The question of what is the best loading dosage of warfarin when starting anticoagulant treatment has been under discussion for ten years. We were unable to find any comparative studies of these characteristics conducted here in Brazil. OBJECTIVE: To compare the safety and efficacy of two initial warfarin dosage regimens for anticoagulant treatment. METHODS: One-hundred and ten consecutive patients of both sexes, with indications for anticoagulation because of venous or arterial thromboembolism, were analyzed prospectively. During the first 3 days of treatment, these patients were given adequate heparin to keep aPTT (activated partial thromboplastin time between 1.5 and 2.5, plus 5 mg of warfarin. From the fourth day onwards, their warfarin doses were adjusted using International Normalized Ratios (INR; target range: 2 to 3. This prospective cohort was compared with a historical series of 110 patients had been given 10 mg of warfarin on the first 2 days and 5 mg on the third day with adjustments based on INR thereafter. Outcomes analyzed were as follows: recurrence of thromboembolism, bleeding events and time taken to enter the therapeutic range. RESULTS: Efficacy, safety and length of hospital stay were similar in both samples. The sample that were given 10 mg entered the therapeutic range earlier (means: 4.5 days vs. 5.8 days, were on lower doses at discharge and had better therapeutic indicators at the first return appointment. CONCLUSIONS: The 10 mg dosage regimen took less time to attain the therapeutic range and was associated with lower warfarin doses at discharge and better INR at first out-patients follow-up visit.

  3. Zolpidem 10 mg given at daytime is not antagonized by 300 mg caffeine in man.

    Science.gov (United States)

    Mattila, M J; Nurminen, M L; Vainio, P; Vanakoski, J

    1998-07-01

    Caffeine counteracts various effects of traditional benzodiazepines (BZDs). As zolpidem, a short-acting hypnotic, is an atypical GABAA-BZD agonist, we investigated when caffeine would counteract the effects of zolpidem as well. In daytime study I, zolpidem 10 mg (capsule) and caffeine 150 or 300 mg (in decaffeinated coffee) were given, alone and in combinations, to parallel groups (n = 15-17) of healthy students in double-blind and placebo-controlled manner. Objective and subjective tests were done before and 45 min and 90 min after intake. Ranked delta values (changes from baseline) were analysed by one-way contrast ANOVA and Scheffe's tests. In daytime study II, four healthy subjects took zolpidem 10 mg alone, and together with blinded caffeine 250 mg or (at -45 min) erythromycin 750 mg. Objective and subjective effects were measured and plasma zolpidem concentrations assayed at baseline and 45 min and 90 min after zolpidem intake. In study I, practice effects after placebo (ad + 30%) were seen for letter cancellation and digit symbol substitution but not for flicker fusion tests. Zolpidem alone significantly impaired (P effects of zolpidem and either dose of caffeine matched those measured after zolpidem alone. Zolpidem + caffeine 300 mg was not stronger than zolpidem + caffeine 150 mg in impairing immediate memory and causing subjective sedation. In study II, zolpidem caused objective and subjective sedation; neither caffeine nor erythromycin modulated the effects of zolpidem or plasma zolpidem concentrations. The sedative effects of 10 mg of zolpidem are not antagonized by 150-300 mg of caffeine in pharmacodynamic or pharmacokinetic terms.

  4. Anisotropic Mechanical Behavior of AlSi10Mg Parts Produced by Selective Laser Melting

    Science.gov (United States)

    Tang, Ming; Pistorius, Petrus Christiaan

    2017-03-01

    AlSi10Mg cylinders produced by laser powder-bed fusion have somewhat different yield behavior for cylinders with XY orientation and Z orientation. Earlier yielding for Z-oriented samples is likely related to micro-residual stress, resulting from the difference in thermal expansion of the aluminum matrix and cellular silicon. Smaller tensile reduction in area of Z-oriented samples is related to tearing along the softer region at the boundaries of melt pools, where the silicon cell spacing is larger. Indentation measurements confirmed the lower hardness at the edges of melt pools.

  5. Determination of paracetamol, caffeine, chlorphenamine maleate in Compound paracetamol and amantadine hydrochloride tablets by HPLC%HPLC测定复方氨酚烷胺片中的对乙酰氨基酚、咖啡因和马来酸氯苯那敏

    Institute of Scientific and Technical Information of China (English)

    谢华; 傅萍; 张悦杨; 张蕾

    2012-01-01

    OBJECTIVE To develop a method for determination of paracetamol, caffeine, chlorphenamine maleate in Compound paracetamol and amantadine hydronhloride tablets. METHODS The chromatography was performed on C18 column with 1 % acetic acid solution (pH was regulated to 3.7 with Hiethylamine) - methanol(62 : 38 )as the mobile phase. Paracetamol was detected at 246 nm while caffeine and chlorphenamine maleate were detected at 262 nm. RESULTS The linear ranges of paracetamol, caffeine and chlorphenamine maleate were 0. 1055 - 2. 11 μg( r = 0. 9999) ,0. 245 - 7. 35μg( r = 0. 9997) and 0. 04216 - 0. 8432 μg( r = 0.9999), respectively. Their average recoveries(n =9) were 98. 7% ,98. 6% and 101.1% .respectively. CONCLUSION This method is simple,accurate and reproducible, and can be used for controlling the quality of Compound paracetamol and amantadine hydro-chloride tablets.%目的 采用HPLC同时测定复方氨酚烷氨片中对乙酰氨基酚、咖啡因、马来酸氯苯那敏的含量,增加小剂量成分咖啡因、马来酸氯苯那敏含量均匀度检查的方法.方法采 用C18柱,流动相为1%醋酸(二乙胺凋pH3.7)-甲醇(62∶38),检测波长对乙酰氨基酚用246 nm,咖啡因、马来酸氯苯那敏用262 nm.结果 对乙酰氨基酚、咖啡因、马来酸氯苯那敏分别在0.1055 ~2.11μg(r=0.9999) 、0.245~7.35μg(r=0.9997) 、0.04216~0.8432 μg(r=0.9999)与峰面积有良好的线性关系;平均回收率分别为98.7% 、98.6%、101.1%(n =9).结论 所用方法操作简便、准确、重复性好,可用于复方氨酚烷氨片的质量控制.

  6. 盐酸氨溴索推挽式渗透泵控释片的制备及犬体内药动学%Preparation of Ambroxol Hydrochloride Push-pull Osmotic Pump Controlled-release Tablets and Its Pharmacokinetics in Dogs

    Institute of Scientific and Technical Information of China (English)

    赵锋; 马银玲; 金晓利; 王静; 曹德英

    2011-01-01

    以不同分子量的聚氧化乙烯为助悬剂和膨胀剂,制备盐酸氨溴索推挽式渗透泵控释片.采用相似因子(f_2)为评价指标,考察含药层中助悬剂种类和助推层中膨胀剂种类的影响.通过正交试验优化处方,考察自制片的体外释放行为和释药机理,并考察其在Beagle犬体内的药动学行为.结果表明,自制片零级释药特征明显(r=0.9921)、释药完全(90%).释药机理符合渗透泵原理且体外释放行为不受片芯直径、硬度、转速及释放介质pH的影响;体内外相关性良好(r=0.984 9).%The push-pull osmotic pump-based controlled-release tablets loaded with ambroxol hydrochloride were prepared, with polyethylene oxide of different molecular weight as suspending agent and extender.Using similar factor (f2) as evaluation index, different suspending agent in drug layer and different extender in push layer were investigated by in vitro release.Following orthogonal design, in vitro release and release mechanism of the preparation were investigated.The pharmacokinetics of the preparation in Beagle dogs was also studied.The results showed that the preparation possessed character of zero-order release (r=0.992 1) and drug release completely (90 %).The pH of media and rotation speed had no significant effect on the in vitro release, while hardness and size of tablets hardly influenced.The correlation coefficient between the fraction of absorption in vivo and the release rate in vitro was 0.984 9.

  7. Compatibility of cholecalciferol, haloperidol, imipramine hydrochloride, levodopa/carbidopa, lorazepam, minocycline hydrochloride, tacrolimus monohydrate, terbinafine, tramadol hydrochloride and valsartan in SyrSpend SF PH4 oral suspensions.

    Science.gov (United States)

    Polonini, H C; Silva, S L; Cunha, C N; Brandão, M A F; Ferreira, A O

    2016-04-01

    A challenge with compounding oral liquid formulations is the limited availability of data to support the physical, chemical and microbiological stability of the formulation. This poses a patient safety concern and a risk for medication errors. The objective of this study was to evaluate the compatibility of the following active pharmaceutical ingredients (APIs) in 10 oral suspensions, using SyrSpend SF PH4 (liquid) as the suspending vehicle: cholecalciferol 50,000 IU/mL, haloperidol 0.5 mg/mL, imipramine hydrochloride 5.0 mg/mL, levodopa/carbidopa 5.0/1.25 mg/mL, lorazepam 1.0 mg/mL, minocycline hydrochloride 10.0 mg/mL, tacrolimus monohydrate 1.0 mg/mL, terbinafine 25.0 mg/mL, tramadol hydrochloride 10.0 mg/mL and valsartan 4.0 mg/mL. The suspensions were stored both refrigerated (2 - 8 degrees C) and at controlled room temperature (20 - 25 degrees C). This is the first stability study for these APIs in SyrSpend SF PH4 (liquid). Further, the stability of haloperidol,ilmipramine hydrochloride, minocycline, and valsartan in oral suspension has not been previously reported in the literature. Compatibility was assessed by measuring percent recovery at varying time points throughout a 90 days period. Quantification of the APIs was performed by high performance liquid chromatography (HPLC-UV). Given the percentage of recovery of the APIs within the suspensions, the beyond-use date of the final preparations was found to be at least 90 days for most suspensions both refrigerated and at room temperature. Exceptions were: Minocycline hydrochloride at both storage temperatures (60 days), levodopa/carbidopa at room temperature (30 days), and lorazepam at room temperature (60 days). This suggests that compounded suspensions of APIs from different pharmacological classes in SyrSpend SF PH4 (liquid) are stable.

  8. 盐酸氟桂利嗪预防性治疗偏头痛性眩晕临床疗效分析%Effect of preventive treatment of Flunarizine hydrochloride for migrainous vertigo

    Institute of Scientific and Technical Information of China (English)

    米彦芳; 闫保星; 单子丽

    2012-01-01

    Objective To observe the effect of Flunarizine hydrochloride in treating migrainous vertigo ( MV). Methods Totally 46 patients with MV were divied into treatment group and control group. Flunarizine hydrochloride capsules (10mg, QN) + Betahistine mesilate tablets (6mg, TID) were used in treatment group, and Betahistine mesilate tablets (6mg, TID) in control group. The number of episodes and severity of attack about MV were observed within 3 months of treatment. Results The number of episodes and severity of attack about MV in treatment group was lighter than that of the control group with statistically significant difference ( P > 0. 05). Conclusions The effect of preventive treatment of Flunarizine hydrochloride for MV is clear.%目的 观察探讨盐酸氟桂利嗪预防性治疗偏头痛性眩晕的疗效.方法 选取临床确诊的偏头痛性眩晕患者46例,将其分为观察组及对照组.观察组给予盐酸氟桂利嗪胶囊( 10mg,QN)+甲磺酸培他司汀片(6mg,TID)联合口服;对照组给予甲磺酸培他司汀片(6mg,tid)单独口服.观察开始治疗3个月内头痛和眩晕发作的严重程度和发作的次数.结果 治疗后3个月内,观察组较对照组在头痛发和眩晕发作的程度和次数上均有有明显减轻,差异具有统计学意义(P>0.05).结论 盐酸氟桂利嗪预防性治疗偏头痛性眩晕具有明确疗效.

  9. Iontophoretic transdermal delivery of buspirone hydrochloride in hairless mouse skin.

    Science.gov (United States)

    Al-Khalili, Mohammad; Meidan, Victor M; Michniak, Bozena B

    2003-01-01

    The transdermal delivery of buspirone hydrochloride across hairless mouse skin and the combined effect of iontophoresis and terpene enhancers were evaluated in vitro using Franz diffusion cells. Iontophoretic delivery was optimized by evaluating the effect of drug concentration, current density, and pH of the vehicle solution. Increasing the current density from 0.05 to 0.1 mA/cm2 resulted in doubling of the iontophoretic flux of buspirone hydrochloride, while increasing drug concentration from 1% to 2% had no effect on flux. Using phosphate buffer to adjust the pH of the drug solution decreased the buspirone hydrochloride iontophoretic flux relative to water solutions. Incorporating buspirone hydrochloride into ethanol:water (50:50 vol/vol) based gel formulations using carboxymethylcellulose and hydroxypropylmethylcellulose had no effect on iontophoretic delivery. Incorporation of three terpene enhancers (menthol, cineole, and terpineol) into the gel resulted in a synergistic effect when combined with iontophoresis. Menthol was the most active enhancer, and when combined with iontophoresis it was possible to deliver 10 mg/cm2/day of buspirone hydrochloride.

  10. Trifluridine and Tipiracil Hydrochloride

    Science.gov (United States)

    This page contains brief information about trifluridine and tipiracil hydrochloride and a collection of links to more information about the use of this combination drug, research results, and ongoing clinical trials.

  11. Doxylamine succinate–pyridoxine hydrochloride (Diclegis) for the management of nausea and vomiting in pregnancy: an overview

    OpenAIRE

    Nuangchamnong N; Niebyl J

    2014-01-01

    Nina Nuangchamnong, Jennifer Niebyl Department of Obstetrics and Gynecology, University of Iowa Hospitals and Clinics, Iowa, IA, USA Abstract: Nausea and vomiting in pregnancy (NVP) is common and often undertreated, in part due to fears of adverse effects of medications on the fetus during early pregnancy. In April 2013, the US Food and Drug Administration (FDA) approved doxylamine succinate 10 mg and pyridoxine hydrochloride (a vitamin B6 analog) 10 mg as a delayed-release combination pill ...

  12. Development and evaluation of natural gum-based extended release matrix tablets of two model drugs of different water solubilities by direct compression

    OpenAIRE

    Ofori-Kwakye, Kwabena; Mfoafo, Kwadwo Amanor; Kipo, Samuel Lugrie; Kuntworbe, Noble; Boakye-Gyasi, Mariam EL

    2015-01-01

    The study was aimed at developing extended release matrix tablets of poorly water-soluble diclofenac sodium and highly water-soluble metformin hydrochloride by direct compression using cashew gum, xanthan gum and hydroxypropylmethylcellulose (HPMC) as release retardants. The suitability of light grade cashew gum as a direct compression excipient was studied using the SeDeM Diagram Expert System. Thirteen tablet formulations of diclofenac sodium (∼100 mg) and metformin hydrochloride (∼200 mg) ...

  13. 75 FR 69088 - Determination That Amphetamine Sulfate, 5 and 10 Milligram Tablets, Was Not Withdrawn From Sale...

    Science.gov (United States)

    2010-11-10

    ... HUMAN SERVICES Food and Drug Administration Determination That Amphetamine Sulfate, 5 and 10 Milligram... Amphetamine sulfate, 5 and 10 milligram (mg) tablets, was not withdrawn from sale for reasons of safety or... Amphetamine sulfate, 5 mg and 10 mg tablets, if all other legal and regulatory requirements are met....

  14. Integral Data Test of HENDL1.0/MG and VisualBUS with Neutronics Shielding Experiments (Ⅰ)

    Institute of Scientific and Technical Information of China (English)

    高纯静; 许德政; 李静惊; 吴宜灿; 邓铁如

    2004-01-01

    HENDL1.0/MG, a multi-group working library of the Hybrid Evaluated Nuclear Data Library, was home-developed by the FDS Team of ASIPP (Institute of Plasma Physics, Chinese Academy of Sciences) on the basis of several national data libraries. To validate and qualify the process of producing HENDL1.0/MG, simulating calculations of a series of existent spherical shell benchmark experiments (Al, Mo, Co, Ti, Mn, W, Be and V) have been performed with HENDL1.0/MG and the multifunctional neutronics code system named VisualBUS home-developed also by FDS Team.

  15. Aqueous Polymer Dispersion Coating Used for Osmotic Pump Tablets: Membrane Property Investigation and IVIVC Evaluation.

    Science.gov (United States)

    Cheng, Lizhen; Gai, Xiumei; Wen, Haoyang; Liu, Dandan; Tang, Xin; Wang, Yanyan; Wang, Tuanjie; Pan, Weisan; Yang, Xinggang

    2017-07-10

    The objective of this study was to investigate the fundamental properties of propranolol hydrochloride osmotic pump tablets coated by aqueous polymer dispersion, simultaneously exploring the in vitro and in vivo correlation of the tablet. The physicochemical properties and parameters of aqueous polymer dispersion membranes (SEM, water uptake, and water vapor transmission coefficient) were investigated. In addition, the release behavior and the in vitro release and in vivo absorption profiles of the tablets coated by aqueous polymer dispersion were investigated by comparing with propranolol hydrochloride osmotic pump tablets coated by an organic solvent. Results showed that the similarity factor (f 2) between cellulose acetate-coated tablet and Eudragit-coated tablet was 78.1, and f 2 between cellulose acetate-coated tablet and Kollicoat-coated tablet was 77.6. The linear IVIVC of Eudragit-coated and Kollicoat-coated osmotic pump tablets was determined, which confirmed excellent correlation between the absorption in vivo and the drug release in vitro. Consequently, the membrane coated by aqueous polymer dispersion or organic solvent has similar in vitro release rates of controlled release. Also, compared with organic solvent coating, aqueous polymer dispersion has numerous advantages, such as reduced toxicity and no environmental damage. Therefore, the aqueous polymer dispersion technology has enormous potential as a replacement of organic solvent coating.

  16. Rapid Solidification: Selective Laser Melting of AlSi10Mg

    Science.gov (United States)

    Tang, Ming; Pistorius, P. Chris; Narra, Sneha; Beuth, Jack L.

    2016-03-01

    Rapid movement of the melt pool (at a speed around 1 m/s) in selective laser melting of metal powder directly implies rapid solidification. In this work, the length scale of the as-built microstructure of parts built with the alloy AlSi10Mg was measured and compared with the well-known relationship between cell size and cooling rate. Cooling rates during solidification were estimated using the Rosenthal equation. It was found that the solidification structure is the expected cellular combination of silicon with α-aluminum. The dependence of measured cell spacing on calculated cooling rate follows the well-established relationship for aluminum alloys. The implication is that cell spacing can be manipulated by changing the heat input. Microscopy of polished sections through particles of the metal powder used to build the parts showed that the particles have a dendritic-eutectic structure; the dendrite arm spacings in metal powder particles of different diameters were measured and also agree with literature correlations, showing the expected increase in secondary dendrite arm spacing with increasing particle diameter.

  17. Effect of heat treatment on structural changes in metastable AlSi10mg alloy

    Directory of Open Access Journals (Sweden)

    Jordović B.

    2014-01-01

    Full Text Available This paper presents a study on structural changes occurring in a rapidly quenched metastable AlSi10Mg alloy during heating cycles within the temperature range from room temperature to 800 K. Measurement of electrical resistivity of a ribbon showed that structural stabilization takes place at temperatures ranging from 450 K to 650 K. The isotherms of the electrical resistivity measured at temperatures 473 K, 483 K and 498 K revealed two stages of structural stabilization i.e. a kinetic process and diffusion process. Measurement of the thermoelectromotive force of the thermocouple made from the investigated alloy and a copper conductor by a mechanical joining was used to determine relative changes in the electron density of states of the quenched sample after successive heat treatments. The same alloy sample was subjected to successive heat treatments at temperatures up to 503 K, 643 K, 683 K and 763 K. The change in the thermopower suggested that each heating was followed by an increase in free electron density in the alloy. Therefore, the abrupt decline in electrical resistivity was induced by an increase in both the mean free electron path and free electron density during the thermal stabilization of the structure. [Projekat Ministarstva nauke Republike Srbije, br. OI 172057: Controlled synthesis, structure and properties of multifunctional materials

  18. 高效液相色谱法测定氨麻美敏片3个组分含量方法的改进%Improvement of HPLC Method for Determination of Three Components in Pseudoephedrine Hydrochloride,Dextromethorphan Hydrobromide and Chlorphenamine Maleate Tablets

    Institute of Scientific and Technical Information of China (English)

    赵爱桔

    2012-01-01

    目的 建立测定氨麻美敏片中盐酸伪麻黄碱、氢溴酸右美沙芬、马来酸氯苯那敏含量的高效液相色谱法.方法 采用Waters Xterra RP18柱(250mm×4.6 mm,5μm),流动相为乙腈-水-三乙胺(17:81.5:1.5),流速为1.0mL/min,检测波长210nm,柱温35℃.结果 盐酸伪麻黄碱、氢溴酸右美沙芬、马来酸氯苯那敏质量浓度分别在150~360μg/mL(r=0.9999),80~190 μg/mL(r=1.0000),1O~24μg/mL(r=1.0000)范围内与峰面积呈良好的线性关系,平均回收率分别为99.89%,99.92%,99.91%,RSD分别为0.73%,0.34%,0.35%(n=9),检测限分别为0.69,0.75,1.48 μg/mL.结论 该方法准确、简便,可用于氨麻美敏片中3个组分的的含量测定.%Objective To establish an HPLC method to determine the content of pseudoephedrine hydrochloride, dextromethorphan hydro-bromide, chlorphenamine maleate in tablet. Methods A Waters Xterra HPn column (250 mm x4. 6 mm,5 (im) is used, mobile phase is acetonitrile - water - triethylamine (17:81.5 : 1.5),flow rate is 1. 0 mL/min, detection wavelength is 210nm and column temperature is 35℃ . Results A good linearity was observed between each component and corresponding peak area for pseudoephedrine hydrochloride, dextromethorphan hydrobromide and chlorphenamine maleate in the range of 150 -360 μg/mL ( r = 0. 999 9),0 - 190 μ.g/mL( r = 1. 000 0), 10-24 μg/mL(r= 1. 000 0) respectively, the average recovery rate was 99. 89% ,99. 92% and 99. 91%,the USD was 0. 73% ,0. 34% and 0.35%( n = 9 )and the LOD was 0. 69, 0. 75 , 1. 48 μg/mL. Conclusion This analytical method is accurate and facilitative and is

  19. 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…

  20. 哌甲酯控释剂对自发性高血压大鼠纹状体胶质细胞源性神经营养因子mRNA表达的作用%Effects of methylphenidate hydrochloride controlled-release tablets on the expression of GDNF mRNA in striate body of the spontaneously hypertensine

    Institute of Scientific and Technical Information of China (English)

    胡颖; 林忠东; 郑飞霞

    2011-01-01

    目的:哌甲酯控释剂对自发性高血压大鼠纹状体胶质细胞源性神经营养因子((GDNF)mRNA基因表达的影响.方法:将SHR随机分为模型对照组(MC组)和哌甲酯控释剂组(MPH组).各组按设计剂量给药14d后.取纹状体组织和血清,采用高效液相法检测多巴胺(DA)的含量、原位杂交法检测纹状体GDNF mRNA的基因表达.结果:哌甲酯控释剂组的纹状体神经元的细胞膜及细胞浆GDNF mRNA基因表达明显增强,模型对照组未见明显表达;哌甲酯控释刺组与模型对照组比较,血清和纹状体中多巴胺的含量显著升高.结论:哌甲酯控释剂有促进纹状体GDNF mRNA的基因表达和增加纹状体和血清中多巴胺的含量的作用,这可能是其治疗ADHD的作用机制之一.%Objective To investigate the effects of methylphenidate hydrochloride controlled-release tablets on the expression of GDNF mRNA in striate body of the Spontaneously hypertensine rats. Methods SHR rats were randomized into MC group and MPH group, and received gastric gavage of corresponding drugs according to the experimental design for 14 days. HPLC was used to detecte the content of DA in striate body and sera, and GDNF mRNA in striate body was detected by in situ hybridization after treatment. Results GDNF mRNA was positively expressed in striate body of rats in MPH group, and was not expressed in those in MC group. The content of DA in striate body and sera of rats in MPH group was significantly higher than that in MC group. Conclusion MPH can increase the expression of GDNF mRNA and the content of DA in striate body and sera in SHR rats, which may be involved in the mechanisms of its treating effect on ADHD.

  1. Lubrication in tablet formulations.

    Science.gov (United States)

    Wang, Jennifer; Wen, Hong; Desai, Divyakant

    2010-05-01

    Theoretical aspects and practical considerations of lubrication in tablet compression are reviewed in this paper. Properties of the materials that are often used as lubricants, such as magnesium stearate, in tablet dosage form are summarized. The manufacturing process factors that may affect tablet lubrication are discussed. As important as the lubricants in tablet formulations are, their presence can cause some changes to the tablet physical and chemical properties. Furthermore, a detailed review is provided on the methodologies used to characterize lubrication process during tablet compression with relevant process analytical technologies. Finally, the Quality-by-Design considerations for tablet formulation and process development in terms of lubrication are discussed.

  2. NOOK tablet for dummies

    CERN Document Server

    Sandler, Corey

    2012-01-01

    The fun is just a tap away with the nifty NOOK Tablet! It's an e-reader, it's a tablet, and it's hot! The NOOK Tablet offers all the advantages of an Android-based tablet, and this small-trim book is packed with information about how to use it. Learn to set up your NOOK Tablet, navigate the touchscreen, download and read e-books, access the Internet, use all the cool Android apps that are included, and much more. Find out how to create your own e-books, share books with others, listen to music or watch streaming video on your NOOK Tablet, personalize your tablet, add accessories, and

  3. Effect of diluents on tablet integrity and controlled drug release.

    Science.gov (United States)

    Zhang, Y E; Schwartz, J B

    2000-07-01

    The objective of this study was to evaluate the effect of diluents and wax level on tablet integrity during heat treatment and dissolution for sustained-release formulations and the resultant effect on drug release. Dibasic calcium phosphate dihydrate (DCPD), microcrystalline cellulose (MCC), and lactose were evaluated for their effect on tablet integrity during drug dissolution and heat treatment in wax matrix formulations. A newly developed direct compression diluent, dibasic calcium phosphate anhydrous (DCPA), was also evaluated. Compritol 888 ATO was used as the wax matrix material, with phenylpropanolamine hydrochloride (PPA) as a model drug. Tablets were made by direct compression and then subjected to heat treatment at 80 degrees C for 30 min. The results showed that MCC, lactose, and DCPA could maintain tablets intact during heat treatment above the melting point of wax (70 degrees C-75 degrees C). However, DCPD tablets showed wax egress during the treatment. MCC tablets swelled and cracked during drug dissolution and resulted in quick release. DCPD and lactose tablets remained intact during dissolution and gave slower release than MCC tablets. DCPA tablets without heat treatment disintegrated very quickly and showed immediate release. In contrast, heat-treated DCPA tablets remained intact through the 24-hr dissolution test and only released about 80% PPA at 6 hr. In the investigation of wax level, DCPD was used as the diluent. The drug release rate decreased as the wax content increased from 15% to 81.25%. The dissolution data were best described by the Higuchi square-root-of-time model. Diluents showed various effects during heat treatment and drug dissolution. The integrity of the tablets was related to the drug release rate. Heat treatment retarded drug release if there was no wax egress.

  4. Inclusions, Porosity, and Fatigue of AlSi10Mg Parts Produced by Selective Laser Melting

    Science.gov (United States)

    Tang, Ming

    Additive manufacturing (AM) has experienced remarkable growth in the past decade with applications in both rapid prototyping and rapid manufacturing for functional end-usable parts. As one of the most promising AM processes, selective laser melting (SLM) can be used to fabricate metal products line by line and layer upon layer within a powder bed system. Such process allows the building of parts with customized shapes, which brings higher design flexibility than traditional casting and wrought manufacturing. In this work, AlSi10Mg powder is chosen as the raw material for producing parts by SLM, since aluminum alloys are widely used in automotive and aerospace industries thanks to an excellent combination of low density and competitive mechanical properties. However, there remain multiple drawbacks which limit further applications of aluminum parts produced by SLM: lack of prediction of solidification microstructure, few studies on fatigue properties, and cost and time caused by the limited production rate. All these issues were studied in this work and summarized as follows: Rapid movement of the melt pool (at a speed around 1 m/s) in SLM of metal powder directly implies rapid solidification. In this research, the length scale of the as-built microstructure of parts built with the alloy AlSi10Mg was measured and compared with the well-known relationship between cell size and cooling rate. Cooling rates during solidification were estimated using the Rosenthal equation. It was found that the solidification structure is the expected cellular combination of silicon with alpha-aluminum. The dependence of the measured cell spacing on the calculated cooling rate follows the well-established relationship for aluminum alloys. The implication is that cell spacing can be manipulated by changing the heat input. Microscopy of polished sections through particles of the metal powder used to build the parts showed that the particles have a dendritic-eutectic structure; the

  5. "Sustained release formulation of Metoclopramide Hydrochloride "

    Directory of Open Access Journals (Sweden)

    Dabbagh MA

    2000-08-01

    Full Text Available In this research, several formulations containing, an anti emetic agent (Metoclopramide hydrochloride, a hydrophilic polymer (hydroxypropylmethylcellulose and a hydrophobic polymer (ethylcellulose 10 cP were prepared by direct compression. Different factors such as: the effect of different ratios of the polymers, particle size, pressure force and differences of release in acidic and distilled water as media were investigated. After developing the ideal formulation, the effect of changing the ratio of drug in core: coating on the formulation was investigated. Coating of tablets with ethylcellulose, changed the release mechanism of drug and shifted it to near zero order release. The results showed that except when matrices were coated with ethylcellulose, drug release was proportioned to the square root of time, which might be due to the change of release pattern from matrix to reservoir system.

  6. 羟考酮控释片用于滴定中度癌痛的疗效观察%Effect of the Titration of Oxycodone Controlled-release Tablets on Moderate Pain

    Institute of Scientific and Technical Information of China (English)

    张颖一; 韩廷; 汪颖; 刘璐; 王宁; 王雅杰

    2011-01-01

    目的 评价盐酸羟考酮控释片对中度癌性疼痛滴定期的疗效优势.方法 本研究选取67例无阿片类药物使用史的中度癌痛患者,随机分为两组,A组(35例)使用盐酸羟考酮控释片5mg作为初始剂量对其进行滴定,B组(32例)使用硫酸吗啡控释片10mg滴定,达到疼痛明显缓解或完全缓解后进入维持期.观察期4天,以服药后1h的NRS评分(numerical rating scale,数字模拟评分法)为主要观察指标,将两组疗效进行对比.结果 给药1h后盐酸羟考酮控释片组中有1例患者疼痛获得完全缓解,12例症状明显缓解,11例达到中度缓解,总有效率高达68.6% ;硫酸吗啡控释片组有4例获得明显缓解,10例疼痛中度缓解,总有效率43.8%.服药第4天两组患者疼痛总缓解率均在90%左右.结论 在迅速缓解疼痛方面,盐酸羟考酮控释片组具有优势;而在维持期控制疼痛方面,两组疗效相当.%Objective To evaluate the efficacy advantage of oxycodone hydrochloride controlled - release tablets for moderate cancer pain. Methods This study selected 67 patients suffering from moderate pain without a history of opioid. They were randomly divided into 2 groups. A group (35 cases) used the oxycodone hydrochloride controlled - release tablets 5mg as the initial dose for titration, and B group ( 32 cases) used the morphine sulfate controlled - release tablets 10mg. All of them entered the maimenance phase after been titrated to achieve obvious relief or complete relief of pain. Within 4 - day observation period, we got the NRS score ( Numerical Rating Scale,digital analog scale) [2] the first hour after taking the pills as the main observation index to compare the two groupa. Results In the group of oxycodone hydrochloride controlled - release tablets, 1 patient achieved complete relief after 1 hour administration, 12 were obviously relieved, and 11 were moderate relieved The total efficiency was up to 68.6% . At the same time, in the

  7. VALIDATION METHOD OF ULTRAVIOLET SPECTROPHOTOMETRY DETERMINATION OF CONTENT IN AMBROXOL HCl TABLET

    OpenAIRE

    Tedy Kurniawan Bakri; Fathur Rahman Harun; Misrahanum .; Sadli .

    2015-01-01

    Ambroxol Hydrochloride (Ambroxol HCI) is one of mucolytic drugs that is commonly used to dilute thesecretion within the respiratory tract. This process is completed by lowering the viscosity of mucopolysaccharides, in which its characteristic which is mucolytic within the respiratory tract. This research aims to conduct a validation of the UV spectrophotometry method in determining the level of ambroxol HCI in tablets. This methos is also used to obtain the level of amboxol HCI in tablets tha...

  8. Analytical method development and validation of Drotaverine Hydrochloride and Aceclofenac in bulk and pharmaceutical dosage forms by UV-Spectrophotometer

    OpenAIRE

    Ram Babu Durgam; Sireesha. D; V. V. L. N Prasad; Diwan, Prakash V.

    2013-01-01

    New simple, precise, rapid and reproducible UV-spectrophotometric method has been developed for the estimation of Drotaverine Hydrochloride and Aceclofenac in both bulk and tablet formulation. Drotaverine and Aceclofenac in combined tablet formulation were estimated by using the multicomponent mode at 307 nm for Drotaverine and 276 nm for Aceclofenac in their solution in ethanol: distilled water in the ratio of 50:50 (v/v %), With correlation coefficient of 0.999 for the both the drugs. The B...

  9. Design and Evaluation of Chronomodulated Drug Delivery of Tramadol Hydrochloride.

    Science.gov (United States)

    Alekya, Thota; Narendar, Dudhipala; Mahipal, Donthi; Arjun, Narala; Nagaraj, Banala

    2017-09-26

    Rheumatoid arthritis is an auto immune disease which requires chronotherapy as it occurs during early morning. Tramadol hydrochloride (TH) is an analgesic drug, used to treat rheumatoid arthritis. The aim of the present investigation was to develop chronomodulated drug delivery system of tramadol hydrochloride such that it releases the drug early in the morning, during which the symptoms of rheumatoid arthritis worsen. To develop chronomodulated drug delivery system of TH, initially core tablets of TH were prepared using three different supradisintegrants followed by coating with pH dependent polymer of Eudragit S100. The prepared core tablets are evaluated for physical parameters and an optimal system was identified. Further, coating composition of Eudragit S100 was optimized and coating tablets of TH was prepared. The prepared coated tablets were evaluated for weight variation, hardness, drug content and in vitro release studies in 0.1N HCl, pH 6.8 phosphate buffer and pH 7.4 phosphate buffer. Formulation with 7.5% of coating solution (ES2) had shown a significant drug release after a lag time of 3 h (in pH 6.8 medium), 6 h (in pH 6.8 medium) and 8 h (in pH 7.4 medium), respectively. DSC studies revealed that no interaction between core and coated materials with drug was observed. Thus, chronomodulated drug delivery system of TH was formulated and assuming that if a tablet is administered around 9 pm to 10 pm, the drug release starts after a lag time of 6 h i. e., around 3am to 4 am. © Georg Thieme Verlag KG Stuttgart · New York.

  10. An open-label,randomized,cross-over bioequivalence study of lafutidine 10 mg under fasting condition

    Institute of Scientific and Technical Information of China (English)

    Bhupesh; Dewan; Raghuram; Chimata

    2010-01-01

    AIM:To assess the relative bioavailability and pharmacokinetic properties of two formulations(test and reference) of Lafutidine 10 mg.METHODS:The study was performed as an open label,randomized,two-way,two-period,two-treatment,single dose cross-over bioequivalence study,under non-fed condition to compare the pharmacokinetic prof iles of the lafutidine formulation manufactured by Emcure Pharmaceuticals Ltd.,India using an indigenously developed active pharmaceutical ingredient(API) and the commercially available Stogra formulation,of UCB Japan Co.,Ltd.,Japan.The two treatments were separated by a washout period of 5 d.After an overnight fasting period of 10 h,the subjects were administered either the test or the reference medication as per the randomization schedule.Blood samples were collected at intervals up to 24 h,as per the approved protocol.Concentrations of lafutidine in plasma were analyzed by a validated liquid chromatography/tandem mass spectrometry(LC/MS/MS) method,and a non-compartmental model was used for pharmacokinetic analysis.The pharmacokinetic parameters were subjected to a 4-way ANOVA accounting for sequence,subjects,period and treatment.Statistical significance was evaluated at 95% conf idence level(P ≥ 0.05).RESULTS:The mean(±SD) values of the pharmacokinetic parameters(test vs reference) were Cmax(265.15±49.84 ng/mL vs 246.79±29.30 ng/mL,P<0.05),Area under the curve(AUC)(0-t)(1033.13±298.74 ng.h/mL vs 952.93±244.07 ng.h/mL,P < 0.05),AUC(0-∞)(1047.61±301.22 ng.h/mL vs 964.21±246.45 ng.h/mL,P<0.05),and tv2(1.92±0.94 h vs 2.05±1.01 h,P<0.05).The 90% conf idence intervals(CI) for the test/reference ratio of mean Cmax,AUC(0-t),and AUC(0-∞) were within the acceptable range of 80.00 to 125.00.The mean times(± SD) to attain maximal plasma concentration(tmax) of lafutidine were 0.95±0.24 h vs 1.01±0.29 h(P<0.05) for the test and the reference formulations respectively.Both the formulations were well tolerated.

  11. 21 CFR 520.2098 - Selegiline hydrochloride tablets.

    Science.gov (United States)

    2010-04-01

    ... use—Dogs—(1) Dosage. 1 milligram per kilogram (0.45 milligram per pound) of body weight. (i... kilogram once daily. Federal law restricts this drug to use by or on the order of a licensed veterinarian. (2) Dosage. 0.5 to 1.0 milligram per kilogram of body weight once daily. (i) Indications for use....

  12. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Science.gov (United States)

    2010-04-01

    ...) Conditions of use. (1) The drug is used in dogs and cats to relieve anxiety and to help control psychomotor... preanesthetic.1 (2) The drug is administered orally to dogs and cats at a dosage level of 1 to 2 milligrams...

  13. High performance thin layer chromatographic method for simultaneous estimation of ibuprofen and pseudoephedrine hydrochloride

    Directory of Open Access Journals (Sweden)

    Chitlange S

    2008-01-01

    Full Text Available High performance thin layer chromatographic method is developed for simultaneous estimation of ibuprofen and pseudoephedrine hydrochloride in tablets. Silica gel 60F 254 plates were used as stationary phase and t.butanol: ethyl acetate: glacial acetic acid: water (7:4:2:2 v/v as mobile phase. Wavelength selected for analysis was 254 nm. Percent estimation of ibuprofen and pseudoephedrine hydrochloride was found to be 99.56% and 98.77%, respectively. Percent recovery for both the drugs was found in the range of 98.27% to 100.91%, respectively.

  14. RP-HPLC Determination of vitamins B1, B3, B6, folic acid and B12 in multivitamin tablets

    OpenAIRE

    2005-01-01

    Abstract:Asimple and sensitive reversed-phase, ion-pair HPLC method was developed and validated for the simultaneous determination of B-group vitamins, thiamine chloride hydrochloride (B1), nicotinamide (B3), pyridoxine hydrochloride (B6) and folic acid in Pentovit® coated tablets. The cyanocobalamine (B12) was determined separately, because of its low concentration in the investigated multivitamin preparation. RP-HPLC analysis was performed with a LKB 2150 HPLC system, equipped with a UV/VI...

  15. Relative bioavailability and bioequivalence study of terbinafine hydrochloride tablets in healthy volunteers%盐酸特比萘芬片在健康人体中的相对生物利用度及生物等效性试验

    Institute of Scientific and Technical Information of China (English)

    陈红; 孙艳伏; 蔡丽伟; 张欣; 丁艳华

    2012-01-01

    目的:评价盐酸特比萘芬片在健康人体的相对生物利用度和生物等效性.方法:20名健康受试者随机交叉单剂量口服盐酸特比萘芬片受试制剂(T)和参比制剂(R),采用液质联用分析方法( LC-MS/MS)测定血浆中特比萘芬浓度.结果:20名健康受试者口服受试制剂和参比制剂后的主要药代动力学参数为:Tmax分别为(1.7±0.6)和(2.2±0.7)h;Cmax分别为(1590±489)和(1266.6±432.8) ng·mL-1;t1/2分别为:(21.6±3.6)和(21.0±10.1) h;AUC0~t分别为(8272.2±2280.6)和(8138.9±2424.0) ng·h·mL-1.受试制剂的AUC0~1或Cmax的90%置信区间对应于参比制剂相应参数的93.44%~111.87%或112.83% ~141.91%范围内;受试制剂相对于参比制剂的相对生物利用度为(105.5±26.3)%.结论:受试制剂与参比制剂的生物利用度相当,但受试制剂峰浓度增加,达峰时间提前,没有增加不良反应,疗效也未见降低.%Objective; To evaluate the relative bioavailability and bioequivalence of lerbinafine hydrochloride tablets in healthy volunteers. Methods; The plasma concentrations of terbinafine in 20 healthy subjects, who received a single crossover dose of test formulation (T) and reference formulation ( R) , were measured by LC-MS/ MS. Results; The pharmacokinetic parameters of the test and reference terbinafine were as follows; Tmax (1.7 ± 0.6) and (2.2±0.7) h; Cmax, (1590±489) and (1 266.6 ±432. 8) ng·mL1; t1/2, (21.6 ±3.6) and (21.0 ± 10.1) h; AUC0-1, (8 272. 2 ±2 280. 6) and (8 138.9 ±2 424.0) ng·h·mL1 .respectively. The 90% CIs of the AUC0-t and Cm of the test formulation were respectively within 93.44% -111.87% andll2.83% -141.91% of the reference preparation. The relative bioavailability of the test formulation to the reference formulation was (105.5 ±26.3)%. Conclusion; The test and reference formulations are basicly bioequivalent. The test formulation has higher Cmax and shorter Tmax compared to the reference formulation

  16. Serotonin syndrome induced by a combination of venlafaxine hydrochloride sustained-release tablets and Ahuganjieyu capsules(舒肝解郁胶囊)%盐酸文拉法辛缓释片联用舒肝解郁胶囊致5-羟色胺综合征

    Institute of Scientific and Technical Information of China (English)

    张云琛; 钱小容; 段丽芳; 费燕

    2016-01-01

    1例73岁女性患者因抑郁症、高血压病口服盐酸文拉法辛缓释片(75 mg、1次/d)、舒肝解郁胶囊(2粒、1次/12 h)、坎地沙坦酯(8 mg、1次/d)、苯磺酸氨氯地平(5 mg、1次/d)、琥珀酸美托洛尔(47.5 mg、1次/d)、胞磷胆碱钠(0.2 g、1次/8 h)和艾司唑仑(1 mg、每晚)。第8天出现头晕、发热,第9天出现尿失禁、胡言乱语,停用所有药物。第10天出现谵妄、肌张力增高。第11天出现双侧瞳孔散大、皮肤潮湿、肌肉痉挛。考虑为5-羟色胺综合征,给予赛庚啶6mg口服、1次/6h。2d后,患者精神状态、自主神经功能、神经肌肉功能明显改善,赛庚啶减量为4mg、1次/8h;4d后,患者生命体征平稳,停用赛庚啶。%A 73-year-old female took venlafaxine hydrochloride sustained-release tablets 75 mg once daily,Ahuganjieyu capsule 2 capsules once every 12 hours, candesartan cilexetil 8 mg once daily, amlodipine besylate 5 mg once daily,metoprolol succinate 47. 5 mg once daily,citicoline sodium 0. 2 g once every 8 hours and estazolam 1 mg per night for treating depression and hypertension. On day 8,the patient developed dizziness and fever. On day 9, she had urinary incontinence and rave, the drugs were discontinued. On day 10,the patient presented delirium and increased muscle tone. On day 11,she had bilateral mydriasis, wet skin and muscle cramps. Drug-induced serotonin syndrome was considered. Cyproheptadine 6 mg once every 6 hours was administered orally. The patient's mental state,functions of the autonomic nervous system and neuromuscular improved significantly after 2 days, then the dose of cyproheptadine was reduced to 4 mg once every 8 hours. After 4 days of treatment,the patient's vital signs were stable and cyproheptadine was stopped.

  17. FORMULATION AND EVALUATION OF TIZANIDINE SUSTAINED RELEASE MATRIX TABLETS USING HYDROXY PROPYL METHY CELLULOSE

    Directory of Open Access Journals (Sweden)

    Ankita Srivastava et al

    2012-09-01

    Full Text Available Tizanidine is a muscle relaxant agent, with the half life of 2.5 hours and requires daily doses to maintain adequate plasma concentrations. The present study was undertaken to with an aim to formulation development and evaluation of Tizanidine hydrochloride sustained release tablets using hydrophilic polymer to sustain the action of Tizanidine. Different batches of Tizanidine hydrochloride were prepared based on preformulation studies using HPMC K100M HPMC K4M and HPMC K100 having different viscosities to calculate the sustained release properties. Tizanidine hydrochloride was analysed by using HPLC using wavelength 240 nm. Results of in-vitro study indicate that the trial formulation 5 having considerable sustaining property. From the discussion it is concluded that the trial formulation 5 had considerable in-vitro drug release. Trial formulation 5 can be taken as an ideal or optimized formulation of sustained release tablets for 12 hours release and it fulfils all the requirements for sustained.

  18. Accuracy of tablet splitting.

    Science.gov (United States)

    McDevitt, J T; Gurst, A H; Chen, Y

    1998-01-01

    We attempted to determine the accuracy of manually splitting hydrochlorothiazide tablets. Ninety-four healthy volunteers each split ten 25-mg hydrochlorothiazide tablets, which were then weighed using an analytical balance. Demographics, grip and pinch strength, digit circumference, and tablet-splitting experience were documented. Subjects were also surveyed regarding their willingness to pay a premium for commercially available, lower-dose tablets. Of 1752 manually split tablet portions, 41.3% deviated from ideal weight by more than 10% and 12.4% deviated by more than 20%. Gender, age, education, and tablet-splitting experience were not predictive of variability. Most subjects (96.8%) stated a preference for commercially produced, lower-dose tablets, and 77.2% were willing to pay more for them. For drugs with steep dose-response curves or narrow therapeutic windows, the differences we recorded could be clinically relevant.

  19. Development of a floating dosage form of ranitidine hydrochloride by statistical optimization technique.

    Science.gov (United States)

    Jain, S; Srinath, Ms; Narendra, C; Reddy, Sn; Sindhu, A

    2010-10-01

    The objective of this study was to evaluate the effect of formulation variables on the release properties, floating lag time, and hardness, when developing floating tablets of Ranitidine hydrochloride, by the statistical optimization technique. The formulations were prepared based on 3(2) factorial design, with polymer ratio (HPMC 100 KM: Xanthan gum) and the amount of aerosil, as two independent formulation variables. The four dependent (response) variables considered were: percentage of drug release at the first hour, T(50%) (time taken to release 50% of the drug), floating lag time, and hardness of the tablet. The release profile data was subjected to a curve fitting analysis, to describe the release mechanism of the drug from the floating tablet. An increase in drug release was observed with an increase in the polymer ratio, and as the amount of aerosil increased, the hardness of the tablet also increased, without causing any change in the floating lag time. The desirability function was used to optimize the response variables, each having a different target, and the observed responses were in accordance with the experimental values. The results demonstrate the feasibility of the model in the development of floating tablets containing Ranitidine hydrochloride.

  20. Ipilimumab 10 mg/kg versus ipilimumab 3 mg/kg in patients with unresectable or metastatic melanoma

    DEFF Research Database (Denmark)

    Ascierto, Paolo A; Del Vecchio, Michele; Robert, Caroline

    2017-01-01

    BACKGROUND: A phase 2 trial suggested increased overall survival and increased incidence of treatment-related grade 3-4 adverse events with ipilimumab 10 mg/kg compared with ipilimumab 3 mg/kg in patients with advanced melanoma. We report a phase 3 trial comparing the benefit-risk profile...... of ipilimumab 10 mg/kg versus 3 mg/kg. METHODS: This randomised, double-blind, multicentre, phase 3 trial was done in 87 centres in 21 countries worldwide. Patients with untreated or previously treated unresectable stage III or IV melanoma, without previous treatment with BRAF inhibitors or immune checkpoint...... for metastatic melanoma, and Eastern Cooperative Oncology Group performance status. The patients, investigators, and site staff were masked to treatment assignment. The primary endpoint was overall survival in the intention-to-treat population and safety was assessed in all patients who received at least one...

  1. The Influence of Selective Laser Melting Parameters on Density and Mechanical Properties of AlSi10Mg

    Directory of Open Access Journals (Sweden)

    Raus A. A.

    2016-01-01

    Full Text Available Selective Laser Melting (SLM is one of the most effective powder bed technique in the additive Manufacturing (AM which able to fabricate functional metal parts directly from 3D Computer Aided Design (CAD file data. In this paper, the influence of SLM parameters, such as laser power, scanning speed and hatching distance on the density of AlSi10Mg samples are investigated using one factor at a time (OFAT. Furthermore, the optimum results are used to fabricate samples for hardness, tensile strength, and impact toughness test. It is revealed that AlSi10Mg parts fabricated by SLM achieving the best density of 99.13% at the value of 350 watts laser power, 1650 mm/s scanning speed and hatching distance 0.13mm, whereby resulted comparable and even better mechanical properties to those of conventionally HDPC A360F and HDPC A360T6 alloys although without any comprehensive post processing methods.

  2. Evaluation of Rapidly Disintegrating Vaginal Tablets of Tenofovir, Emtricitabine and Their Combination for HIV-1 Prevention

    Directory of Open Access Journals (Sweden)

    Meredith R. Clark

    2014-12-01

    Full Text Available Vaginal tablets are being developed as an alternative to gels as an inexpensive, discreet dosage form for the administration of microbicides. This work describes the pharmacokinetic (PK evaluation of rapidly disintegrating vaginal tablets containing tenofovir (TFV, 10 mg, emtricitabine (FTC, 10 mg, and the combination of TFV and FTC (10 mg each under in vitro and in vivo conditions, and in direct comparison to the clinical TFV 1% gel, a microbicide product in Phase III clinical testing. The PK of TFV and FTC from tablets were also evaluated in female rabbits following intravaginal administration. Direct comparison of a single dose of TFV tablets (intact or predissolved at 10 mg/mL and TFV 1% gel showed no differences in the vaginal PK of TFV between groups; however systemic bioavailability of TFV was significantly higher from the gel. When rabbits were dosed either once or daily for seven days with intact tablets of TFV, FTC, or the combination of TFV/FTC, vaginal and systemic concentrations of TFV and FTC were unaffected by co-formulation. Moreover, plasma PK parameters were similar following a single dose or seven once-daily doses. Tissue concentrations of TFV and FTC in the cranial vagina 4 h after administration ranged between 104 and 105 ng/g. Concentrations of TFV-diphospate (TFV-DP, the active metabolite were also high (over 103 ng/g or about 3000 to 6000 fmol/mg in the cranial vagina 4 h after administration and similar to those measured following administration of TFV 1% gel. These data demonstrate that rapidly disintegrating vaginal tablets may be a suitable topical microbicide dosage form providing similar vaginal TFV PK to that of TFV 1% gel. The data also support co-administration of FTC with TFV in a single vaginal tablet to create a combination microbicide in a simple and inexpensive dosage form.

  3. Tensile Properties Characterization of AlSi10Mg Parts Produced by Direct Metal Laser Sintering via Nested Effects Modeling

    OpenAIRE

    Biagio Palumbo; Francesco Del Re; Massimo Martorelli; Antonio Lanzotti; Pasquale Corrado

    2017-01-01

    A statistical approach for the characterization of Additive Manufacturing (AM) processes is presented in this paper. Design of Experiments (DOE) and ANalysis of VAriance (ANOVA), both based on Nested Effects Modeling (NEM) technique, are adopted to assess the effect of different laser exposure strategies on physical and mechanical properties of AlSi10Mg parts produced by Direct Metal Laser Sintering (DMLS). Due to the wide industrial interest in AM technologies in many different fields, it is...

  4. Design of Controlled Release Non-erodible Polymeric Matrix Tablet Using Microwave Oven-assisted Sintering Technique.

    Science.gov (United States)

    Patel, Dm; Patel, Bk; Patel, Ha; Patel, Cn

    2011-07-01

    The objective of the present study was to evaluate the effect of sintering condition on matrix formation and subsequent drug release from polymer matrix tablet for controlled release. The present study highlights the use of a microwave oven for the sintering process in order to achieve more uniform heat distribution with reduction in time required for sintering. We could achieve effective sintering within 8 min which is very less compared to conventional hot air oven sintering. The tablets containing the drug (propranolol hydrochloride) and sintering polymer (eudragit S-100) were prepared and kept in a microwave oven at 540 watt, 720 watt and 900 watt power for different time periods for sintering. The sintered tablets were evaluated for various tablet characteristics including dissolution study. Tablets sintered at 900 watt power for 8 min gave better dissolution profile compared to others. We conclude that microwave oven sintering is better than conventional hot air oven sintering process in preparation of controlled release tablets.

  5. Biowaiver monographs for immediate release solid oral dosage forms: amitriptyline hydrochloride.

    Science.gov (United States)

    Manzo, R H; Olivera, M E; Amidon, G L; Shah, V P; Dressman, J B; Barends, D M

    2006-05-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing amitriptyline hydrochloride are reviewed. Its therapeutic uses, its pharmacokinetic properties, the possibility of excipient interactions and reported BE/bioavailability (BA) problems are also taken into consideration. Literature data indicates that amitriptyline hydrochloride is a highly permeable active pharmaceutical ingredient (API). Data on the solubility according to the current Biopharmaceutics Classification System (BCS) were not fully available and consequently amitriptyline hydrochloride could not be definitively assigned to either BCS Class I or BCS Class II. But all evidence taken together, a biowaiver can currently be recommended provided that IR tablets are formulated with excipients used in existing approved products and that the dissolution meets the criteria defined in the Guidances.

  6. Multi-walled carbon nanotubes based catalyst plasmon resonance light scattering analysis of tetracycline hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    It was found that multi-walled carbon nanotubes (MWNTs) could catalyze the redox reaction between chlorauric acid (HAuCl4) and reductive drugs such as tetracycline hydrochloride (TC), producing gold nanoparticles (Au NPs). By measuring the plasmon resonance light scattering (PRLS) signals of the resulting Au NPs, tetracycline hydrochloride can be detected simply and rapidly with a linear range of 4―26 μmol/L, a correlated coefficient (r ) of 0.9955, and a limit of detection (3σ) of 6.0 nmol/L. This method has been successfully applied to the detection of tetracycline hydrochloride tablets in clinic with the recovery of 101.9% and that of fresh urine samples with the recovery of 98.3%―102.0%.

  7. Clinical effect of venlafaxine combined with methylphenidate hydrochloride on narcolepsy

    Directory of Open Access Journals (Sweden)

    YAN Bin

    2013-11-01

    Full Text Available This study aims to explore the clinical effect of venlafaxine sustained-release capsules combined with methylphenidate hydrochloride tablets on narcolepsy. Thirty-eight cases of narcoleptic patients were randomly divided into venlafaxine combined with methylphenidate hydrochloride treatment group (observation group, N = 19 and methylphenidate hydrochloride and clomipramine treatment group (control group, N = 19. After a total of 12-week treatment, clinical curative effect and adverse drug reactions were observed in 2 groups of patients. The results showed that effective rate of the treatment for excessive daytime sleepiness (EDS in observation group was higher than that of the control group (15/19 vs 8/19, P = 0.044, and effective rate of the treatment for cataplexy in observation group was higher than that of the control group (13/19 vs 6/19, P = 0.048. The rate of adverse drug reactions in observation group was lower than that in the control group (χ2 = 8.889, P = 0.003. It was indicated that venlafaxine combined with methylphenidate had good curative effect on narcolepsy with EDS and cataplexy symptoms.

  8. Tablet Technologies and Education

    OpenAIRE

    Heidi L. Schnackenberg

    2013-01-01

    Recently, tablet technologies have grown tremendously in popularity. They lend themselves to a myriad of learning modalities and therefore may be well suited to use in schools and universities. While teachers work to find useful applications for tablets, students have already begun using them at home and, in secondary and higher education, in classes. Unfortunately, sometimes when students use tablets for courses they play with “apps,” rather than using the technology as a useful and powerful...

  9. 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).

  10. Preparation and evaluation of combination tablet containing incompatible active ingredients.

    Science.gov (United States)

    Wang, Xiaoyan; Cui, Fude; Yonezawa, Yorinobu; Sunada, Hisakazu

    2003-07-01

    Combination preparation plays an important role in clinical treatment because of its better and wider curative synergism and weaker side effects. However, the existence of incompatibility between active ingredients or between active ingredients and excipients presents a serious obstacle in the preparation of such combination solid dosage forms. In this study, aspirin and ranitidine hydrochloride, between which there existed a chemical interaction, were selected as model drugs. Aspirin powders without any additives were granulated with hydroxypropyl methyl cellulose (HPMC) water solution as a binder using a Wurster coating apparatus and the operation conditions were optimized by Artificial Neural Network (ANN) analysis. Under these conditions, the aspirin granules prepared showed good flowability and compressibility. On the other hand, ranitidine hydrochloride was coated with Aquacoat (ethyl cellulose aqueous dispersion) after preliminary granulation with the Wurster coating apparatus. The aspirin granules and coated ranitidine hydrochloride particles were compressed into tablets with suitable excipients. The combination tablets showed good dissolution, content uniformity and improved stability of active ingredients.

  11. Safety and tolerability of ramipril 10 mg in patients at high risk of cardiovascular events: an observational study.

    Science.gov (United States)

    Hathial, Manish

    2008-07-01

    To assess the safety and tolerability of ramipril 10 mg in patients at high risk of cardiovascular (CV) events by observing the levels of blood pressure (BP) and by recording the incidence of cough in these patients, a study was conducted in a total of 1048 patients who participated in the registry. Eligible patients in this prospective, observational, longitudinal, multicentre registry included all normotensives--including treated hypertensives--with BP risk reduction and had been prescribed by the treating physician. The primary outcome was the effect on BP at 8 weeks, and the secondary outcome was the incidence of cough at 8 weeks. Ramipril was initiated at 2.5 mg once daily (OD) for a week, followed by 5 mg OD for 3 weeks and was then increased to 10 mg OD. Data was analysed using ANOVA and Chi-square test. A total of 1,048 patients participated in this registry; 868 (82.82%) continued with the treatment till the end of the registry (ie, 8 weeks). At baseline, systolic BP was 130.10 +/- 5.38 mm Hg, while diastolic BP was 81.07 +/- 4.36 mm Hg. At 8 weeks, these values changed non-significantly to 123.41 +/- 6.33 mm Hg and 79.03 +/- 4.84 mm Hg, respectively. At week 1, 41 patients had cough, which increased non-significantly to 58 by week 8. Only 6 patients complained of severe cough at week 8, which did not lead to treatment discontinuation. Tolerability of the treatment was assessed to be 'excellent' or 'good' by 63.3% patients and 67% physicians. Treatment with ramipril 10 mg daily in patients with high risk of CV events and normal/ controlled BP produced neither a significant fall in BP nor significant adverse events in real-world clinical practice and was well tolerated.

  12. 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

  13. On the Selective Laser Melting (SLM of the AlSi10Mg Alloy: Process, Microstructure, and Mechanical Properties

    Directory of Open Access Journals (Sweden)

    Francesco Trevisan

    2017-01-01

    Full Text Available The aim of this review is to analyze and to summarize the state of the art of the processing of aluminum alloys, and in particular of the AlSi10Mg alloy, obtained by means of the Additive Manufacturing (AM technique known as Selective Laser Melting (SLM. This process is gaining interest worldwide, thanks to the possibility of obtaining a freeform fabrication coupled with high mechanical properties related to a very fine microstructure. However, SLM is very complex, from a physical point of view, due to the interaction between a concentrated laser source and metallic powders, and to the extremely rapid melting and the subsequent fast solidification. The effects of the main process variables on the properties of the final parts are analyzed in this review: from the starting powder properties, such as shape and powder size distribution, to the main process parameters, such as laser power and speed, layer thickness, and scanning strategy. Furthermore, a detailed overview on the microstructure of the AlSi10Mg material, with the related tensile and fatigue properties of the final SLM parts, in some cases after different heat treatments, is presented.

  14. Taste masked orodispersible formulation of fexofenadine hydrochloride using ion exchange resins

    Directory of Open Access Journals (Sweden)

    Divya Suares

    2015-01-01

    Full Text Available The objective of this research work was to mask the intense bitter taste of fexofenadine hydrochloride using weak cation exchange resins and to formulate orodispersible tablet of taste masked drug-resin complex. Five resins indion 204, indion 234, indion 414, kyron T-114 and kyron T-314 were used. Depending on maximum drug loading capacity of resins indion 234 and kyron T-314 were finalized for further study. Drug-resin complex was optimized by considering parameters such as drug to resin ratio, soaking time of resins, stirring time, temperature and pH on maximum drug loading. The drug-resin complex was characterized by Fourier transform infrared spectroscopy. The drug-resin complex was also subjected to various evaluation studies such as taste mask evaluation by panel method, drug content and in vitro drug release at salivary and gastric pH. The orodispersible tablets of taste masked drug-resin complex for indion 234 and kyron T-314 were prepared by direct compression method. Formulated orodispersible tablets were subjected to various evaluation parameters such as diameter and thickness measurement, hardness test, weight variation test, in vitro United States Pharmacopoeia disintegration test, wetting time, test for content uniformity, assay, friability test and in vitro dissolution studies. The results indicate that orodispersible tablets of fexofenadine hydrochloride containing indion 234 and kyron T-314 are palatable and provide quick disintegration and fast drug release without addition of superdisintegrants.

  15. Taste Masked Orodispersible Formulation of Fexofenadine Hydrochloride Using Ion Exchange Resins.

    Science.gov (United States)

    Suares, Divya; Hiray, Arti

    2015-01-01

    The objective of this research work was to mask the intense bitter taste of fexofenadine hydrochloride using weak cation exchange resins and to formulate orodispersible tablet of taste masked drug-resin complex. Five resins indion 204, indion 234, indion 414, kyron T-114 and kyron T-314 were used. Depending on maximum drug loading capacity of resins indion 234 and kyron T-314 were finalized for further study. Drug-resin complex was optimized by considering parameters such as drug to resin ratio, soaking time of resins, stirring time, temperature and pH on maximum drug loading. The drug-resin complex was characterized by Fourier transform infrared spectroscopy. The drug-resin complex was also subjected to various evaluation studies such as taste mask evaluation by panel method, drug content and in vitro drug release at salivary and gastric pH. The orodispersible tablets of taste masked drug-resin complex for indion 234 and kyron T-314 were prepared by direct compression method. Formulated orodispersible tablets were subjected to various evaluation parameters such as diameter and thickness measurement, hardness test, weight variation test, in vitro United States Pharmacopoeia disintegration test, wetting time, test for content uniformity, assay, friability test and in vitro dissolution studies. The results indicate that orodispersible tablets of fexofenadine hydrochloride containing indion 234 and kyron T-314 are palatable and provide quick disintegration and fast drug release without addition of superdisintegrants.

  16. Pharmacokinetics study of extended release formulations of buspirone hydrochloride in Beagle dogs

    Institute of Scientific and Technical Information of China (English)

    CUI Meng-cun; LI Jing-lai; CHEN Yan; WANG Xiao-ying; QIAO Jian-zhong; ZHANG Zhen-qing; RUAN Jin-xiu

    2008-01-01

    Objective To evaluate the pharmacokinetics (PK) properties of extended release formulations of buspirone hydrochloride in Beagle dogs. Methods A randomized, two period, two treatment, two sequence crossover bioequivalenee study was designed; six healthy Beagle dogs were randomly divided into two groups, each group was orally given buspirone tablets or buspirone extended capsule containing 15 mg buspirone hydrochloride. Blood samples (about 1 mL) were collected in heparinized tubes before dosing and at 0.33, 0.67, 1,2, 3, 4, 6, 8, 10, 12, 18, 24 h after administration, and were then immediately centrifuged at 3000 rpm for 15 min. The pharmacokinetics (PK) properties of the drugs were evaluated using the liquid chromatographic-tandem mass spectrometric (LC-MS/MS) method. Results The mean tmax was 4.7, 0.8 h and Cmax values was 1.8, 6.9 μg·L-1, respectively for the sustained-release test (capsule) and reference formulation (tablet). When compared to the tablets, the residence time of the sustained capsules was dramatically prolonged and Cmax Was reduced (P<0.01). The initial release speed was slow and stable. The bioavailability was similar to the common tablets. Conclusions The sustained capsule had showed good pharmacokinetics property of sustained-release in the Beagle dogs.

  17. A novel rapid quantitative analysis of drug migration on tablets using laser induced breakdown spectroscopy.

    Science.gov (United States)

    Yokoyama, Makoto; Tourigny, Martine; Moroshima, Kenji; Suzuki, Junsuke; Sakai, Miyako; Iwamoto, Kiyoshi; Takeuchi, Hirofumi

    2010-11-01

    There have been few reports wherein drug migration from the interior to the surface of a tablet has been analyzed quantitatively until now. In this paper, we propose a novel, rapid, quantitative analysis of drug migration in tablets using laser induced breakdown spectroscopy (LIBS). To evaluate drug migration, model tablets containing nicardipine hydrochloride as active pharmaceutical ingredient (API) were prepared by a conventional wet granulation method. Since the color of this API is pale yellow and all excipients are white, we can observe the degree of drug migration by visual inspection in these model tablets. In order to prepare tablets with different degrees of drug migration, the temperature of the drying process after tableting was varied between 50 to 80 °C. Using these manifold tablets, visual inspection, Fourier transform (FT)-IR mapping and LIBS analysis were carried out to evaluate the drug migration in the tablets. While drug migration could be observed using all methods, only LIBS analysis could provide quantitative analysis wherein the average LIBS intensity was correlated with the degree of drug migration obtained from the drying temperature. Moreover, in this work, we compared the sample preparation, data analysis process and measurement time for visual inspection, FT-IR mapping and LIBS analysis. The results of the comparison between these methods demonstrated that LIBS analysis is the simplest and the fastest method for migration monitoring. From the results obtained, we conclude that LIBS analysis is one of most useful process analytical technology (PAT) tools to solve the universal migration problem.

  18. Bioadhesive ranitidine hydrochloride for gastroretention with controlled microenvironmental pH.

    Science.gov (United States)

    Adhikary, Anuradha; Vavia, Pradeep R

    2008-08-01

    Ranitidine hydrochloride is a H(2) receptor blocker used in the treatment of gastric ulcers. Pharmacological factors, in addition to the dosage regimen, favor development of a sustained-release system for ranitidine especially in the therapeutic condition of erosive esophagitis. This investigation delves into the development of bioadhesive type of gastroretentive formulation (tablets) of ranitidine. The effect of mucoadhesive polymers such as Carbopol, hydroxypropyl methyl cellulose, and dextrose were studied. Mucoadhesion, in vitro drug release profile, water uptake, and swelling of the tablet were evaluated. Alkalizing agents were incorporated in an attempt to maintain an alkaline microenvironment within the tablet and improve the stability of the drug in acidic medium. The stability was evaluated using dye test and degradation studies. The drug release profiles were fit into various kinetic models.

  19. Development of novel prasugrel base microsphere-loaded tablet with enhanced stability: Physicochemical characterization and in vivo evaluation in beagle dogs.

    Science.gov (United States)

    Kim, Kyeong Soo; Kim, Jin Cheul; Jin, Sung Giu; Kim, Dong Wuk; Kim, Dong Shik; Yong, Chul Soon; Kim, Jong Oh; Youn, Yu Seok; Oh, Kyung Taek; Woo, Jong Soo; Choi, Han-Gon

    2016-10-01

    The objective of this study was to develop a novel prasugrel base microsphere-loaded tablet (PBMST) with enhanced stability as a bioequivalent to the commercial prasugrel hydrochloride-loaded tablet. Numerous prasugrel base-loaded microspheres were prepared with hydroxypropylmethyl cellulose (HPMC), colloidal silica and various acidifying agents using a spray-drying process, and the physicochemical properties, solubility and stability were investigated. The PBMSTs were prepared and their dissolution, pharmacokinetics in beagle dogs and stability were evaluated compared to commercial prasugrel hydrochloride-loaded tablets. Among the acidifying agents tested, phosphoric acid provided the greatest increase in drug solubility, by as much as 110-fold. The prasugrel base-loaded microspheres composed of prasugrel base, HPMC, colloidal silica and phosphoric acid at a weight ratio of 10/10/5/2.5 provided an amorphous drug and reduced particle size of about 11.3μm. Moreover, it exhibited excellent solubility and improved stability compared to prasugrel base and hydrochloride. Moreover, PBMST drug dissolution was improved in comparison to the prasugrel base-loaded tablet (PBT), with similar dissolution to the commercial prasugrel hydrochloride-loaded tablet at pH 1.2 and 4.0. PBMST provided significantly higher plasma concentrations of AUC and Cmax in beagle dogs compared to PBT. In particular, the AUC of PBMST was approximately four times greater than PBT, leading to improved oral bioavailability. There were no significant differences observed for all pharmacokinetic parameters between PBMST and the commercial prasugrel hydrochloride-loaded tablet, suggesting their bioequivalence in beagle dogs. Furthermore, the prepared PBMSTs were stable for at least six months. Therefore, this novel prasugrel base microsphere-loaded tablet could be a potential alternative for enhancing the stability and bioavailability of prasugrel.

  20. Corrosion Behavior of AlSi10Mg Alloy Produced by Additive Manufacturing (AM vs. Its Counterpart Gravity Cast Alloy

    Directory of Open Access Journals (Sweden)

    Avi Leon

    2016-06-01

    Full Text Available The attractiveness of additive manufacturing (AM relates to the ability of this technology to rapidly produce very complex components at affordable costs. However, the properties and corrosion behavior, in particular, of products produced by AM technology should at least match the properties obtained by conventional technologies. The present study aims at evaluating the corrosion behavior and corrosion fatigue endurance of AlSi10Mg alloy produced by selective laser melting (SLM in comparison with its conventional counterpart, gravity cast alloy. The results obtained indicate that the corrosion resistance of the printed and cast alloys was relatively similar, with a minor advantage to the printed alloy. The corrosion fatigue endurance of the printed alloy was relatively improved compared to the cast alloy. This was mainly attributed to the significant differences between the microstructure and defect characteristics of those two alloys.

  1. Efficacy and tolerability of rizatriptan 10 mg compared with sumatriptan 100 mg: an evidence-based analysis.

    Science.gov (United States)

    Göbel, Hartmut

    2010-04-01

    Acute migraine attacks have a strong impact on quality of life and require immediate therapeutic intervention to achieve rapid pain relief. The introduction of triptans into the market in 1993 has increased the therapeutic options in migraine patients considerably. The seven currently available triptans show many similar characteristics but there are also some clinically relevant pharmacological differences. Rizatriptan 10 mg has demonstrated, in a head-to-head study, higher response rates and a more rapid onset of action than sumatriptan 100 mg, together with a favorable tolerability profile. Meta-analyses of double-blind placebo-controlled studies confirmed the superior efficacy of rizatriptan. Owing to the limited efficacy of sumatriptan, a more effective triptan treatment is needed in the majority of patients with acute migraine attacks.

  2. Tensile Properties Characterization of AlSi10Mg Parts Produced by Direct Metal Laser Sintering via Nested Effects Modeling

    Directory of Open Access Journals (Sweden)

    Biagio Palumbo

    2017-02-01

    Full Text Available A statistical approach for the characterization of Additive Manufacturing (AM processes is presented in this paper. Design of Experiments (DOE and ANalysis of VAriance (ANOVA, both based on Nested Effects Modeling (NEM technique, are adopted to assess the effect of different laser exposure strategies on physical and mechanical properties of AlSi10Mg parts produced by Direct Metal Laser Sintering (DMLS. Due to the wide industrial interest in AM technologies in many different fields, it is extremely important to ensure high parts performances and productivity. For this aim, the present paper focuses on the evaluation of tensile properties of specimens built with different laser exposure strategies. Two optimal laser parameters settings, in terms of both process quality (part performances and productivity (part build rate, are identified.

  3. Dimensional Accuracy and Surface Roughness Analysis for AlSi10Mg Produced by Selective Laser Melting (SLM

    Directory of Open Access Journals (Sweden)

    Kamarudin K.

    2016-01-01

    Full Text Available Selective Laser Melting (SLM is an Additive Manufacturing (AM technique that built 3D part in a layer-by-layer method by melting the top surface layer of a powder bed with a high intensity laser according to sliced 3D CAD data. AlSi10Mg alloy is a traditional cast alloy that is broadly used for die-casting process and used in automotive industry due its good mechanical properties. This paper seeks to investigate the requirement SLM in rapid tooling application. The feasibility study is done by examining the surface roughness and dimensional accuracy as compared to the benchmark part produced through the SLM process with constant parameters. The benchmark produced by SLM shows the potential of SLM in a manufacturing application particularly in moulds.

  4. Calcification prevention tablets

    Science.gov (United States)

    Lindsay, Geoffrey A.; Hasting, Michael A.; Gustavson, Michael A.

    1991-01-01

    Citric acid tablets, which slowly release citric acid when flushed with water, are under development by the Navy for calcification prevention. The citric acid dissolves calcium carbonate deposits and chelates the calcium. For use in urinals, a dispenser is not required because the tablets are non-toxic and safe to handle. The tablets are placed in the bottom of the urinal, and are consumed in several hundred flushes (the release rate can be tailored by adjusting the formulation). All of the ingredients are environmentally biodegradable. Mass production of the tablets on commercial tableting machines was demonstrated. The tablets are inexpensive (about 75 cents apiece). Incidences of clogged pipes and urinals were greatly decreased in long term shipboard tests. The corrosion rate of sewage collection pipe (90/10 Cu/Ni) in citric acid solution in the laboratory is several mils per year at conditions typically found in traps under the urinals. The only shipboard corrosion seen to date is of the yellow brass urinal tail pieces. While this is acceptable, the search for a nontoxic corrosion inhibitor is underway. The shelf life of the tablets is at least one year if stored at 50 percent relative humidity, and longer if stored in sealed plastic buckets.

  5. 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...

  6. 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.

  7. 21 CFR 582.5676 - Pyridoxine hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Pyridoxine hydrochloride. 582.5676 Section 582.5676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Dietary Supplements 1 § 582.5676 Pyridoxine hydrochloride. (a) Product. Pyridoxine hydrochloride....

  8. Guar gum, xanthan gum, and HPMC can define release mechanisms and sustain release of propranolol hydrochloride.

    Science.gov (United States)

    Mughal, Muhammad Akhlaq; Iqbal, Zafar; Neau, Steven Henry

    2011-03-01

    The objectives were to characterize propranolol hydrochloride-loaded matrix tablets using guar gum, xanthan gum, and hydroxypropylmethylcellulose (HPMC) as rate-retarding polymers. Tablets were prepared by wet granulation using these polymers alone and in combination, and physical properties of the granules and tablets were studied. Drug release was evaluated in simulated gastric and intestinal media. Rugged tablets with appropriate physical properties were obtained. Empirical and semi-empirical models were fit to release data to elucidate release mechanisms. Guar gum alone was unable to control drug release until a 1:3 drug/gum ratio, where the release pattern matched a Higuchi profile. Matrix tablets incorporating HPMC provided near zero-order release over 12 h and erosion was a contributing mechanism. Combinations of HPMC with guar or xanthan gum resulted in a Higuchi release profile, revealing the dominance of the high viscosity gel formed by HPMC. As the single rate-retarding polymer, xanthan gum retarded release over 24 h and the Higuchi model best fit the data. When mixed with guar gum, at 10% or 20% xanthan levels, xanthan gum was unable to control release. However, tablets containing 30% guar gum and 30% xanthan gum behaved as if xanthan gum was the sole rate-retarding gum and drug was released by Fickian diffusion. Release profiles from certain tablets match 12-h literature profiles and the 24-h profile of Inderal(®) LA. The results confirm that guar gum, xanthan gum, and HPMC can be used for the successful preparation of sustained release oral propranolol hydrochoride tablets.

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

    Directory of Open Access Journals (Sweden)

    Traudi Klein

    2012-01-01

    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.

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

    Directory of Open Access Journals (Sweden)

    Traudi Klein

    2013-02-01

    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.

  11. 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.

  12. Olaparib tablet formulation

    DEFF Research Database (Denmark)

    Plummer, Ruth; Swaisland, Helen; Leunen, Karin

    2015-01-01

    BACKGROUND: The oral PARP inhibitor olaparib has shown efficacy in patients with BRCA-mutated cancer. This Phase I, open-label, three-part study (Parts A-C) in patients with advanced solid tumours evaluated the effect of food on the pharmacokinetics (PK) of olaparib when administered in tablet...... formulation. METHODS: PK data were obtained in Part A using a two-treatment period crossover design; single-dose olaparib 300 mg (two 150 mg tablets) was administered in two prandial states: fasted and fed. In Part B, patients received olaparib tablets (300 mg bid) for 5 days under fasting conditions; in Part...... exposure to olaparib 300 mg tablets, although in the absence of an effect on the extent of olaparib absorption....

  13. Intestinal Anisakiasis Treated Successfully with Prednisolone and Olopatadine Hydrochloride

    Directory of Open Access Journals (Sweden)

    Hideki Toyoda

    2016-02-01

    Full Text Available The clinical characteristic of gastrointestinal anisakiasis is severe abdominal pain after eating raw fish. Intestinal anisakiasis is more uncommon than gastric anisakiasis. Most patients with intestinal anisakiasis need hospitalization because anisakiasis can cause intestinal obstruction, ileus, peritonitis or intestinal perforation. We report a case of intestinal anisakiasis. A 43-year-old woman presented with symptoms of intermittent abdominal pain 2 days after eating raw fish. Her brother had eaten the same food and had been suffering from gastric anisakiasis. Abdominal ultrasonography in this patient showed localized jejunal wall thickening with dilated lumen of proximal jejunum and ascites. According to the clinical course and examinations, she was diagnosed with intestinal anisakiasis. Administration of prednisolone 5 mg/day and olopatadine hydrochloride 10 mg/day improved her symptoms quickly without hospitalization. Prednisolone was administered for 10 days, and olopatadine hydrochloride was administered for a total of 6 weeks according to ultrasonographic findings. Six months after the treatment, the abdominal ultrasonography demonstrated normal findings. This case demonstrates that ultrasonography was quite useful for the diagnosis and surveillance of intestinal anisakiasis. Furthermore, treatment with corticosteroid and an antiallergic agent could be an option for patients with intestinal anisakiasis.

  14. Quality by design I: Application of failure mode effect analysis (FMEA) and Plackett-Burman design of experiments in the identification of "main factors" in the formulation and process design space for roller-compacted ciprofloxacin hydrochloride immediate-release tablets.

    Science.gov (United States)

    Fahmy, Raafat; Kona, Ravikanth; Dandu, Ramesh; Xie, Walter; Claycamp, Gregg; Hoag, Stephen W

    2012-12-01

    As outlined in the ICH Q8(R2) guidance, identifying the critical quality attributes (CQA) is a crucial part of dosage form development; however, the number of possible formulation and processing factors that could influence the manufacturing of a pharmaceutical dosage form is enormous obviating formal study of all possible parameters and their interactions. Thus, the objective of this study is to examine how quality risk management can be used to prioritize the number of experiments needed to identify the CQA, while still maintaining an acceptable product risk profile. To conduct the study, immediate-release ciprofloxacin tablets manufactured via roller compaction were used as a prototype system. Granules were manufactured using an Alexanderwerk WP120 roller compactor and tablets were compressed on a Stokes B2 tablet press. In the early stages of development, prior knowledge was systematically incorporated into the risk assessment using failure mode and effect analysis (FMEA). The factors identified using FMEA were then followed by a quantitative assessed using a Plackett-Burman screening design. Results show that by using prior experience, literature data, and preformulation data the number of experiments could be reduced to an acceptable level, and the use of FMEA and screening designs such as the Plackett Burman can rationally guide the process of reducing the number experiments to a manageable level.

  15. 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.

  16. 3D printing of tablets using inkjet with UV photoinitiation.

    Science.gov (United States)

    Clark, Elizabeth A; Alexander, Morgan R; Irvine, Derek J; Roberts, Clive J; Wallace, Martin J; Sharpe, Sonja; Yoo, Jae; Hague, Richard J M; Tuck, Chris J; Wildman, Ricky D

    2017-08-30

    Additive manufacturing (AM) offers significant potential benefits in the field of drug delivery and pharmaceutical/medical device manufacture. Of AM processes, 3D inkjet printing enables precise deposition of a formulation, whilst offering the potential for significant scale up or scale out as a manufacturing platform. This work hypothesizes that suitable solvent based ink formulations can be developed that allow the production of solid dosage forms that meet the standards required for pharmaceutical tablets, whilst offering a platform for flexible and personalized manufacture. We demonstrate this using piezo-activated inkjetting to 3D print ropinirole hydrochloride. The tablets produced consist of a cross-linked poly(ethylene glycol diacrylate) (PEGDA) hydrogel matrix containing the drug, photoinitiated in a low oxygen environment using an aqueous solution of Irgacure 2959. At a Ropinirole HCl loading of 0.41mg, drug release from the tablet is shown to be Fickian. Raman and IR spectroscopy indicate a high degree of cross-linking and formation of an amorphous solid dispersion. This is the first publication of a UV inkjet 3D printed tablet. Consequently, this work opens the possibility for the translation of scalable, high precision and bespoke ink-jet based additive manufacturing to the pharmaceutical sector. Copyright © 2017. Published by Elsevier B.V.

  17. Microporous bilayer osmotic tablet for colon-specific delivery.

    Science.gov (United States)

    Chaudhary, Anil; Tiwari, Neha; Jain, Vikas; Singh, Ranjit

    2011-05-01

    Microporous bilayer osmotic tablet bearing dicyclomine hydrochloride and diclofenac potassium was developed using a new oral drug delivery system for colon targeting. The tablets were coated with microporous semipermeable membrane and enteric polymer using conventional pan-coating process. The developed microporous bilayer osmotic pump tablet (OPT) did not require laser drilling to form the drug delivery orifice. The colon-specific biodegradation of pectin could form in situ delivery pores for drug release. The effect of formulation variables like inclusion of osmogen, amount of HPMC and NaCMC in core, amount of pore former in semipermeable membrane was studied. Scanning electron microscopic photographs showed formation of in situ delivery pores after predetermined time of coming in contact with dissolution medium. The number of pores was dependent on the amount of the pore former in the semipermeable membrane. In vitro dissolution results indicated that system showed acid-resistant, timed release and was able to deliver drug at an approximate zero order up to 24h. The developed tablets could be effectively used for colon-specific drug delivery to treat IBS. Copyright © 2011 Elsevier B.V. All rights reserved.

  18. Additive Manufacturing of AlSi10Mg Alloy Using Direct Energy Deposition: Microstructure and Hardness Characterization

    Science.gov (United States)

    Javidani, M.; Arreguin-Zavala, J.; Danovitch, J.; Tian, Y.; Brochu, M.

    2017-04-01

    This paper aims to study the manufacturing of the AlSi10Mg alloy with direct energy deposition (DED) process. Following fabrication, the macro- and microstructural evolution of the as-processed specimens was initially investigated using optical microscopy and scanning electron microscopy. Columnar dendritic structure was the dominant solidification feature of the deposit; nevertheless, detailed microstructural analysis revealed cellular morphology near the substrate and equiaxed dendrites at the top end of the deposit. Moreover, the microstructural morphology in the melt pool boundary of the deposit differed from the one in the core of the layers. The remaining porosity of the deposit was evaluated by Archimedes' principle and by image analysis of the polished surface. Crystallographic texture in the deposit was also assessed using electron backscatter diffraction and x-ray diffraction analysis. The dendrites were unidirectionally oriented at an angle of 80° to the substrate. EPMA line scans were performed to evaluate the compositional variation and elemental segregation in different locations. Eventually, microhardness (HV) tests were conducted in order to study the hardness gradient in the as-DED-processed specimen along the deposition direction. The presented results, which exhibited a deposit with an almost defect free structure, indicate that the DED process can suitable for the deposition of Al-Si-based alloys with a highly consolidated structure.

  19. Additive Manufacturing of AlSi10Mg Alloy Using Direct Energy Deposition: Microstructure and Hardness Characterization

    Science.gov (United States)

    Javidani, M.; Arreguin-Zavala, J.; Danovitch, J.; Tian, Y.; Brochu, M.

    2016-12-01

    This paper aims to study the manufacturing of the AlSi10Mg alloy with direct energy deposition (DED) process. Following fabrication, the macro- and microstructural evolution of the as-processed specimens was initially investigated using optical microscopy and scanning electron microscopy. Columnar dendritic structure was the dominant solidification feature of the deposit; nevertheless, detailed microstructural analysis revealed cellular morphology near the substrate and equiaxed dendrites at the top end of the deposit. Moreover, the microstructural morphology in the melt pool boundary of the deposit differed from the one in the core of the layers. The remaining porosity of the deposit was evaluated by Archimedes' principle and by image analysis of the polished surface. Crystallographic texture in the deposit was also assessed using electron backscatter diffraction and x-ray diffraction analysis. The dendrites were unidirectionally oriented at an angle of 80° to the substrate. EPMA line scans were performed to evaluate the compositional variation and elemental segregation in different locations. Eventually, microhardness (HV) tests were conducted in order to study the hardness gradient in the as-DED-processed specimen along the deposition direction. The presented results, which exhibited a deposit with an almost defect free structure, indicate that the DED process can suitable for the deposition of Al-Si-based alloys with a highly consolidated structure.

  20. Efficacy and safety of drotaverine hydrochloride in irritable bowel syndrome: A randomized double-blind placebo-controlled study

    OpenAIRE

    Ramesh R Rai; Manisha Dwivedi; Nirmal Kumar

    2014-01-01

    Backgrounds/Aims: To study the efficacy and safety of drotaverine hydrochloride (HCl) 80 mg tablet given thrice a day in the symptomatic relief of patients with irritable bowel syndrome (IBS). Patients and Methods: The study was a multicentric, randomized, double-blind, placebo-controlled parallel group study performed at three centers. The patients who fulfilled Rome II Criteria of IBS were included in the study. A total of 180 patients with IBS were randomized to drotaverine and placebo tre...

  1. The efficacy of a generic doxycycline tablet in the treatment of canine monocytic ehrlichiosis

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    Josephus J. Fourie

    2015-03-01

    Full Text Available The objective of the present study was to evaluate the therapeutic efficacy of a generic doxycycline tablet (DoxyVet® against Ehrlichia canis infection in dogs. Canine monocytic ehrlichiosis is caused by the bacterium E. canis and transmitted by the brown kennel tick (Rhipicephalus sanguineus. Six disease-free and tick-free dogs were infested with E. canis infected ticks. Once diagnosed (with polymerase chain reaction [PCR] analysis and platelet counts as positive for infection, doxycycline tablets were administered orally once a day for 20 consecutive days, at a target dose level of 10 mg/kg. The actual dose administered was calculated as ranging between 10 mg/kg and 11.7 mg/kg. The PCR analysis, 28 days after the first administration of the tablets, failed to detect E. canis in any of the dogs. On Day 56 of the study, four of the dogs were diagnosed with E. canis for the second time and a fifth dog was diagnosed on Day 70. The platelet counts of the sixth dog remained within normal levels and it was discharged from the study on Day 84. Doxycycline tablets were then administered to the remaining five infected dogs for 28 consecutive days. Four of these dogs had no positive PCR results during the following 3 months. The fifth dog was diagnosed with E. canis for the third time 58 days after the last tablets of the second treatment had been administered, after which it was rescue treated (doxycycline for a further 28 days. The results indicate that doxycycline administered in tablet form (DoxyVet® at 10 mg/kg – 11.7 mg/kg body mass once daily for 28 consecutive days clears most dogs of infection. The importance of a concomitant tick-control programme is therefore stressed.

  2. Comparison of novel granulated pellet-containing tablets and traditional pellet-containing tablets by artificial neural networks.

    Science.gov (United States)

    Huang, Ying; Yao, Qinghe; Zhu, Chune; Zhang, Xuan; Qin, Lingzhen; Wang, Qinruo; Pan, Xin; Wu, Chuanbin

    2015-01-01

    Novel granulated pellets technique was adopted to prepare granulated pellet-containing tablets (GPCT). GPCT and traditional pellet-containing tablets (PCT) were prepared according to 29 formulations devised by the Design Expert 7.0, with doxycycline hydrochloride as model drug, blends of Eudragit FS 30D and Eudragit L 30D-55 as coating materials, for the comparison study to confirm the superiority of GPCT during compaction. Eudragit FS 30D content, coating weight gain, tablet hardness and pellet size were chosen as influential factors to investigate the properties and drug release behavior of tablets. The correlation coefficients between the experimental values and the predicted values by artificial neural networks (ANNs) for PCT and GPCT were 0.9474 and 0.9843, respectively, indicating the excellent prediction of ANNs. The similarity factors (f2) for release profiles of GPCT and the corresponding original pellets were higher than those of PCT, suggesting that the excipient layer of granulated pellets absorbed the compressing force and protected the integrity of coating films during compaction.

  3. Design and evaluation of an extended-release matrix tablet formulation; the combination of hypromellose acetate succinate and hydroxypropylcellulose

    Directory of Open Access Journals (Sweden)

    Sachiko Fukui

    2017-03-01

    Full Text Available The purpose of this study was to develop an extended-release (ER matrix tablet that shows robust dissolution properties able to account for the variability of pH and mechanical stress in the GI tract using a combination of enteric polymer and hydrophilic polymer. Hypromellose acetate succinate (HPMCAS and hydroxypropylcellulose (HPC were selected as ER polymers for the ER matrix tablet (HPMCAS/HPC ER matrix tablet. Oxycodone hydrochloride was employed as a model drug. Dissolution properties of the HPMCAS/HPC ER matrix tablets were evaluated and were not affected by the pH of the test medium or paddle rotating speed. In a USP apparatus 3 (bio-relevant dissolution method, dissolution profiles of the HPMCAS/HPC ER matrix tablets containing oxycodone hydrochloride were similar to that of the reference product (OxyContin. Moreover, in vivo performance after oral administration of the HPMCAS/HPC ER matrix tablets to humans was simulated by GastroPlus based on dissolution profiles from the USP apparatus 3. The plasma concentration-time profile simulated was similar to that of the reference product. These results suggest that the combination of HPMCAS and HPC shows a robust dissolution profile against pH and paddle rotating speed and indicates the appropriate extended-release profile in humans.

  4. Drug release characteristics from chitosan-alginate matrix tablets based on the theory of self-assembled film.

    Science.gov (United States)

    Li, Liang; Wang, Linlin; Shao, Yang; Ni, Rui; Zhang, Tingting; Mao, Shirui

    2013-06-25

    The aim of this study was to better understand the underlying drug release characteristics from chitosan-alginate matrix tablets containing different types of drugs. Theophylline, paracetamol, metformin hydrochloride and trimetazidine hydrochloride were used as model drugs exhibiting significantly different solubilities (12, 16, 346 and >1000 mg/ml at 37 °C in water). A novel concept raised was that drugs were released from chitosan-alginate matrix tablets based on the theory of a self-assembled film-controlled release system. The film was only formed on the surface of tablets in gastrointestinal environment and originated from chitosan-alginate polyelectrolyte complex, confirmed by differential scanning calorimetry characterization. The formed film could decrease the rate of polymer swelling to a degree, also greatly limit the erosion of tablets. Drugs were all released through diffusion in the hydrated matrix and polymer relaxation, irrespective of the drug solubility. The effects of polymer level and initial drug loading on release depended on drug properties. Drug release was influenced by the change of pH. In contrast, the impact of ionic strength of the release medium within the physiological range was negligible. Importantly, hydrodynamic conditions showed a key factor determining the superiority of the self-assembled film in controlling drug release compared with conventional matrix tablets. The new insight into chitosan-alginate matrix tablets can help to broaden the application of this type of dosage forms.

  5. Spectrophotometric Method for Estimation of Tamsulosin Hydrochloride in Pharmaceutical Dosage Form Using Bromate-Bromide and Methyl Orange Reagent

    Directory of Open Access Journals (Sweden)

    Bharatkumar Ganeshbhai Chaudhari

    2012-09-01

    Full Text Available A simple, rapid, accurate and precise assay procedure based on Spectrophotometric method has been developed for the estimation of Tamsulosin hydrochloride in Pharmaceutical formulation. The method was based on the bromination of Tamsulosin hydrochloride with a known excess amount of Bromate-bromide mixture in acidic medium followed by the determination of surplus bromine by reacting with dye methyl orange and measuring the absorbance at 513 nm. Validation was carried out in compliance with International Conference on Harmonization guidelines. Linear regression analysis of method showed good linearity with the correlation co-efficient (r of 0.9978 with respect to absorbance in the concentration range of 2-12 μg/mL and the mean recovery for Tamsulosin hydrochloride was 99.65% ± 0.47 . The proposed method can be successfully applied for the analysis of tablet formulations.

  6. [Examination of effectiveness of olopatadine hydrochloride in atopic dermatitis].

    Science.gov (United States)

    Shimizu, Tadamichi; Mashiko, Maki; Shimizu, Hiroshi

    2005-02-01

    Subjective/objective symptoms (itching, papula, erythema, lichenification, desquamation, scratching, erosion) and the levels of IgE, LDH, interleukin (IL) -6, thymus and activation-regulated chemokine (TARC) were compared before and after administering olopatadine hydrochloride (ALLELOCK tablets) to 17 atopic dermatitis (AD) patients. Subject/objective symptoms improved significantly after administering the agent, and the total dosage of the combined topical steroids was also significantly decreased after administration (p<0.05), although IgE, IL-6 and LDH levels did not change, TARC was significantly decreased (p<0.05). The correlation between the levels of IgE, IL-6, LDH and TARC before and after the administration was examined. There was a positive correlation between IgE and TARC (r=0.62, p<0.01) and between IL-6 and TARC (r=0.78, p<0.01). Olopatadine hydrochloride is therefore useful in improving the symptoms in AD, and TARC may be used as an indicator of the symptom improvement.

  7. Tribological Behavior of Aluminum Alloy AlSi10Mg-TiB2 Composites Produced by Direct Metal Laser Sintering (DMLS)

    Science.gov (United States)

    Lorusso, Massimo; Aversa, Alberta; Manfredi, Diego; Calignano, Flaviana; Ambrosio, Elisa Paola; Ugues, Daniele; Pavese, Matteo

    2016-08-01

    Direct metal laser sintering (DMLS) is an additive manufacturing technique for the production of parts with complex geometry and it is especially appropriate for structural applications in aircraft and automotive industries. Aluminum-based metal matrix composites (MMCs) are promising materials for these applications because they are lightweight, ductile, and have a good strength-to-weight ratio This paper presents an investigation of microstructure, hardness, and tribological properties of AlSi10Mg alloy and AlSi10Mg alloy/TiB2 composites prepared by DMLS. MMCs were realized with two different compositions: 10% wt. of microsize TiB2, 1% wt. of nanosize TiB2. Wear tests were performed using a pin-on-disk apparatus on the prepared samples. Performances of AlSi10Mg samples manufactured by DMLS were also compared with the results obtained on AlSi10Mg alloy samples made by casting. It was found that the composites displayed a lower coefficient of friction (COF), but in the case of microsize TiB2 reinforcement the wear rate was higher than with nanosize reinforcements and aluminum alloy without reinforcement. AlSi10Mg obtained by DMLS showed a higher COF than AlSi10Mg obtained by casting, but the wear rate was higher in the latter case.

  8. 穴位埋线联合盐酸二甲双胍片治疗肾虚痰湿型多囊卵巢综合征胰岛素抵抗50例临床观察%Observation of acupoint catgut implantation combined with metformin hydrochloride tablets on renal defi-ciency and phlegm-damp type polycystic ovarian syndrome with insulin resistance

    Institute of Scientific and Technical Information of China (English)

    蒋雪霞; 孟君

    2014-01-01

    Objective To observe the effect of acupoint catgut implantation combined with metformin hydro -chloride tablets on renal deficiency and phlegm -damp type polycystic ovarian syndrome ( PCOS) with insulin resist-ance ( IR) .Methods 100 PCOS patients were randomly divided into two groups .50 patients in control group were treated by metformin hydrochloride tablets .50 cases in treatment group were treated by acupoint catgut implantation in the non-menstrual period on the basis of control group treatment .The changes of BMI, FPG, 2 hPG, fasting insulin, postprandial 2h insulin, Homeostasis model of insulin resistance index (HOMA-IR), HOMA-β, T, TG, HDLC, LDL-C, ApoA, APOB,LH, FSH, E2 , T and LH/FSH levels were observed and compared in two groups .Results The levels of BMI after treatment were decreased signif-icantly in two groups (P <0.05), there was difference between groups (P<0.05).The levels of FPG, fasting insulin, 2 hPG, postprandial 2 h insulin, HOMA-IR and HOMA-βafter treatment were obviously decreased in treatment group (P<0.05), but the levels of FPG, fasting insulin, HOMA-IR and HOMA-βafter treatment were decreased in control group (P<0.05).And there were significant differences between two groups on the levels of FPG, fasting insulin and HOMA-IR after treatment (P<0.05).The levels of TG, LDL-C and Apo-A after treat-ment were decreased and the level of HDL -C was increased in treatment group (P<0.05).But in control group the levels of TG and LDL -C were reduced and the level of HDL -C was increased after treatment ( P<0.05 ) .And there were significant differences between two groups on the changes of levels of TG , LDL-C, HDL-C and Apo-A after treatment (P<0.05).The levels of LH, LH/FSH and T after treatment were significantly decreased in treat-ment group (P<0.05).But in control group the levels of LH and T were significantly reduced after treatment (P<0.05).And there was significant difference between two groups on the levels of LH and LH /FSH after

  9. Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation

    Institute of Scientific and Technical Information of China (English)

    Bayoumy I Eassa; Mohamed A El-Shazly

    2013-01-01

    Premature ejaculation (PE) is the most common sexual disorder.It affects 20%-30% of adult men; the aetiology of this condition has not yet been elucidated.The aim of this study is to evaluate the efficacy,safety,tolerability,undesirable effects and improved satisfaction with sexual intercourse with tramadol hydrochloride at different dosages for the treatment of PE.A total of 300 patients who presented with lifelong (primary) PE were included in this study.The study was performed for 28 weeks,in which placebo (starch tablet) was given for 4 weeks,and active ingredient (tramadol hydrochloride) was administered at different therapeutic dosages for 24 weeks.Patients were divided into three equal groups,each consisting of 100 patients.The first group (A) was given tramadol hydrochloride capsule 25 mg.The second group (B) was given tramadol hydrochloride capsule 50 mg.The third group (C) was given tramadol hydrochloride capsule 100 mg.All of the 300 participants included completed the study voluntarily.The age of the patients varied from 25 to 50 years.After the treatment period,the recorded data were collected for each group and analysed.The results showed a highly significant increase in the mean intravaginal ejaculatory latency time (IELT) in all groups compared to baseline data (P<0.0001).We concluded that using tramadol hydrochloride at different doses on demand for the treatment of PE is effective,safe and tolerable,with minimal undesirable effects,and approval for this indication should be sought.

  10. Rabeprazole 10 mg versus 20 mg in preventing relapse of gastroesophageal reflux disease: a meta-analysis

    Institute of Scientific and Technical Information of China (English)

    ZHU Hai-di; WANG Heng; XIA Xian-ming; XU Shu-man; LAN Yao

    2013-01-01

    Background Several randomized controlled trials (RCTs) have compared endoscopic and symptomatic relapses in patients with erosive gastroesophageal reflux disease (GERD).We have summarized current evidence for rabeprazole 10 or 20 mg once daily for GERD maintenance treatment over 1 or 5 years.Methods MEDLINE,EMBASE,and the Cochrane Central Register of Controlled Trials were searched,through August 2012,for eligible RCTs of adults with erosive GERD.The efficacies of rabeprazole 10 and 20 mg/d were compared.Results The search identified 288 citations,and five RCTs containing 1480 patients were considered eligible.Heartburn relapse rates did not differ significantly between patients treated with rabeprazole 10 and 20 mg/d for 1 year (relative risk (RR)=1.29; 95% confidence interval (CI):0.97-1.72),but differed in patients treated for 5 years (RR=1.274; 95% CI:1.005-1.615).Endoscopic relapse rates differed significantly between rabeprazole 10 and 20 mg/d for 1 year (RR=1.92;95% CI:1.21-3.06),for 5 years (RR=1.667; 95% CI:1.073-2.589),and in combined 1-and 5-year maintenance trials (RR=1.785; 95% CI:1.298-2.456).Conclusion Rabeprazole 20 mg/d was superior to rabeprazole 10 mg/d in preventing endoscopic relapse of erosive GERD,but that the two dosages were equivalent in symptomatic relief over 1 year.

  11. SPECTROPHOTOMETRIC ESTIMATION OF BUSPIRONE HYDROCHLORIDE IN BULK AND ITS PHARMACEUTICAL FORMULATION

    Directory of Open Access Journals (Sweden)

    B.DHANDAPANI,

    2010-05-01

    Full Text Available Three simple, accurate, rapid and sensitive methods developed for the determination of buspirone hydrochloride in bulk drug and in its tablets by UV Spectroscopy (Method – A – Water as a Solvent, UV Spectroscopy (Method – B – Methanol as a Solvent, and Colorimetry (Method - C. In Method A buspirone hydrochloride estimated at 236 nm using distilled water as a solvent. The linearity was observed in the concentration range of 5 – 25 μg/ml with correlation co efficient of 0.9866. In Method B methanol used as a solvent. The linearity wasobserved in the concentration range of 10 – 50 μg/ml with correlation co efficient of 0.9905. In Method C buspirone hydrochloride is a colorless compound undergoes oxidation with 0.005M Potassium ermanganate Solution in the presence of 0.5M Sodium Hydroxide gives Pink color. The intensity of color directly proportional to theconcentration of buspirone hydrochloride and its found that intensity of color stable for 20mins and the absorbance was measured at 610 nm with different time intervals with the linearity range and correlation co -efficient of 10 – 50 μg/ml and 0.9924. The result of analysis for all the methods was validated statistically and by ecovery studies.

  12. DESIGN OF GASTRO RETENTIVE DRUG DELIVERY SYSTEM OF DILTIAZEM HYDROCHLORIDE

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    L. K. Omray

    2014-02-01

    Full Text Available Gastro retentive drug delivery system of diltiazem hydrochloride was designed and evaluated for its effectiveness for the management of mild to moderate hypertension. Gastro retentive drug delivery system were prepared using polyvinyl alcohol and sodium carboxy methyl cellulose as the polymers and sodium bicarbonate as a gas generating agent for the reduction of floating lag time. Gastro retentive drug delivery system tablets were prepared by wet granulation method by compression in tablet compression machine. Formulations DL1, DL2, DL3, DL4 and DL5 were developed which differed in the ratio of polyvinyl alcohol and sodium carboxy methyl cellulose polymers. All the formulations were evaluated for hardness, weight variation, friability, drug content, swelling index, buoyancy studies and in vitro drug release study. In vitro drug release study was performed using United State Pharmacopoeia 23 type 2 dissolution test apparatus employing paddle stirrer at 50 r/pm. Dissolution medium was 900 ml of 0.1N hydrochloric acid at 37ºC ± 3ºC. Formulations DL3 was found to be better as compared to other formulation.

  13. Determination of ranitidine hydrochloride in pharmaceutical preparations by titrimetry and visible spectrophotometry using bromate and acid dyes.

    Science.gov (United States)

    Basavaiah, K; Nagegowda, P

    2004-02-01

    Four new methods using titrimetry and spectrophotometry are described for the determination of ranitidine hydrochloride (RNH) with potassium bromate as the oxidimetric reagent and acid dyes, methyl orange, indigo carmine and metanil yellow. In direct titrimetry (method A), the drug is titrated directly with bromate in acid medium and in the presence of excess of bromide using methyl orange indicator. In back titrimetry (method B), the drug is treated with a measured excess of bromate in the presence of bromide and acid, and the unreacted bromine is determined iodometrically. Both spectrophotometric methods are based on the oxidation of RNH by a known excess of bromate in acid medium and in the presence of excess of bromide followed by estimation of surplus oxidant by reacting with either indigo carmine (method C) or metanil yellow (method D), and measuring the absorbance at 610 or 530 nm. In methods B, C and D, reacted oxidant corresponds to the drug content. The experimental conditions are optimized. Titrimetric procedures are applicable over the ranges 1-10 mg (A) and 1-17 mg (B), and the reaction stoichiometry is found to be 1:1 (BrO(-)(3): RNH). In spectrophotometric methods, the absorbance is found to increase linearly with increasing concentration of RNH, which is corroborated by the calculated correlation coefficient (r) of 0.9984 (C) and 0.9976 (D). The systems obey Beer's law for 2-12 and 1-7 microg ml(-1), for methods C and D, respectively. Method D with a molar absorptivity of 9.82 x 10(4) l mol(-l) cm(-1) is found to be more sensitive than method C ( epsilon = 2.06 x l0(4) l mol(-1) cm(-1)). The limits of detection and quantification are reported for both the spectrophotometric methods. The proposed methods were applied successfully to the determination of RNH in tablets and injections. The reliability of the assay was established by parallel determination by the official method and by recovery studies.

  14. Development of LC Method for the Simultaneous Determination of Antidepressant Drug Combination Melitracen Hydrochloride and Flupentixol Dihydrochloride in their Combined Dosage Form

    Directory of Open Access Journals (Sweden)

    Usmangani K. Chhalotiya

    2011-01-01

    Full Text Available A simple, specific and stability-indicating reversed-phase high-performance liquid chromatographic method was developed for the simultaneous determination of melitracen hydrochloride and flupentixol dihydrochloride in tablet dosage form. A Brownlee C-18, 5 μm column having 250×4.6 mm i.d. in isocratic mode, with mobile phase containing 0.025 M potassium dihydrogen phosphate: methanol (10 : 90, v/v; pH 7.3 was used. The flow rate was 1.0 mL/min, and effluents were monitored at 230 nm. The retention times of melitracen hydrochloride and flupentixol dihydrochloride were 7.75 min and 5.50 min, respectively. The linearity for melitracen hydrochloride and flupentixol dihydrochloride were in the range of 0.5–60 μg/mL. The recoveries obtained for melitracen hydrochloride and flupenthixol dihydrochloride was 99.81–100.77% and 99.42–100.12%, respectively. Both the drugs were subjected to acid and alkali hydrolysis, chemical oxidation, and dry heat degradation and photodegradation. The proposed method was validated and successfully applied to the estimation of melitracen hydrochloride and flupentixol dihydrochloride in combined tablet dosage form.

  15. 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

  16. 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

  17. Cartap hydrochloride poisoning: A clinical experience

    OpenAIRE

    Hari K Boorugu; Anugrah Chrispal

    2012-01-01

    Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular to...

  18. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride with promazine... RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222b Ketamine.... Ketamine hydrochloride, (±),-2-(o-chlorophenyl)-2-(methylamino) cyclohexanone hydrochloride, with promazine...

  19. Thermoanalytical Investigation of Terazosin Hydrochloride

    OpenAIRE

    Mona Mohamed Abdel-Moety; Ali Kamal Attia

    2013-01-01

    Purpose: Thermal analysis (TGA, DTG and DTA) and differential scanning calorimetry (DSC) have been used to study the thermal behavior of terazosin hydrochloride (TER). Methods: Thermogravimetric analysis (TGA/DTG), differential thermal analysis (DTA) and differential scanning calorimetry (DSC) were used to determine the thermal behavior and purity of the used drug. Thermodynamic parameters such as activation energy (E*), enthalpy (∆H*), entropy (∆S*) and Gibbs free energy change of the decomp...

  20. The Nebusarsekim Tablet

    NARCIS (Netherlands)

    Stadhouders, H.A.I.

    2008-01-01

    During the summer of 2007 an internet hype was unleashed by the breaking news that an Old Testament name of some importance, figuring in the Book of Jeremiah Ch. 39, had been positively identified on a cuneiform clay tablet, viz. a bill of receipt from the time of this prophet's floruit. Many a scho

  1. Effects of vacuum annealing treatment on microstructures and residual stress of AlSi10Mg parts produced by selective laser melting process

    Science.gov (United States)

    Chen, Tian; Wang, Linzhi; Tan, Sheng

    2016-07-01

    Selective laser melting (SLM)-fabricated AlSi10Mg parts were heat-treated under vacuum to eliminate the residual stress. Microstructure evolutions and tensile properties of the SLM-fabricated parts before and after vacuum annealing treatment were studied. The results show that the crystalline structure of SLM-fabricated AlSi10Mg part was not modified after the vacuum annealing treatment. Additionally, the grain refinement had occurred after the vacuum annealing treatment. Moreover, with increasing of the vacuum annealing time, the second phase increased and transformed to spheroidization and coarsening. The SLM-produced parts after vacuum annealing at 300∘C for 2 h had the maximum ultimate tensile strength (UTS), yield strength (YS) and elongation, while the elastic modulus decreased significantly. In addition, the tensile residual stress was found in the as-fabricated AlSi10Mg samples by the microindentation method.

  2. New co-polymer zwitterionic matrices for sustained release of verapamil hydrochloride.

    Science.gov (United States)

    Kostova, Bistra; Rachev, Dimitar

    2007-12-01

    Stable co-polymer [vinyl acetate-co-3-dimethyl(methacryloyloxyethyl) ammonium propane sulfonate, p(VA-co-DMAPS)] latex of different compositions has been synthesized for the first time by emulsifier-free emulsion copolymerization. The unusual >overshooting< behavior of the co-polymer tablets has been explained by the formation of specific clusters from the opposite oriented dipoles-zwitterionic species. The change of their concentration with the DMAPS unit fraction (mDMAPS), pH and ionic strength has been considered responsible for the differences observed in the swelling kinetics. The results obtained prove that mDMAPS and ionic strength could be used to control the swelling degree of the p(VA-co-DMAPS) matrices and their sustained drug delivery. In this way, p(VA-co-DMAPS) matrices could be effectively used to control the sustained release of drugs with basic properties like verapamil hydrochloride from model tablets.

  3. Raman spectroscopy as a complementary tool to assess the content uniformity of dosage units in break-scored warfarin tablets.

    Science.gov (United States)

    Arruabarrena, J; Coello, J; Maspoch, S

    2014-04-25

    Due to the side effects of overdosing, the therapeutic dose of warfarin preparations must be very strictly controlled. In order to make it easier for the patient to take the required dose, two different strategies can be followed: The medicine can be commercialized in different dosages and/or tablets can be scored in order to make them easy to split. The splitting of the tablets introduces the question of how to control that the fractions contain the desirable amount of warfarin. The regulations regarding the content uniformity of dosage unit for scored tablets have changed considerably in the last 10 years, and they are still evolving. Warfarin is commercialized under the trademark of Aldocumar in four different preparations, containing 1, 3, 5 and 10 mg sodium warfarin per tablet. All these tablets are also scored, thus suggesting the possibility of splitting. A quantitative Raman method has been developed for the determination of warfarin in tablets and in the potential fragments, taking into account the score lines on the tablet surface. This method is suggested as an auxiliary procedure to verify the uniformity of API distribution in dividable tablets. A combination of a second derivative and standard normal variate (SNV) was used as spectral pre-treatments, and partial least squares (PLS) as the regression algorithm. The relative standard deviation in API content among portions was found to be less than 5%. An HPLC procedure has been used as a reference analytical method.

  4. Development and evaluation of natural gum-based extended release matrix tablets of two model drugs of different water solubilities by direct compression.

    Science.gov (United States)

    Ofori-Kwakye, Kwabena; Mfoafo, Kwadwo Amanor; Kipo, Samuel Lugrie; Kuntworbe, Noble; Boakye-Gyasi, Mariam El

    2016-01-01

    The study was aimed at developing extended release matrix tablets of poorly water-soluble diclofenac sodium and highly water-soluble metformin hydrochloride by direct compression using cashew gum, xanthan gum and hydroxypropylmethylcellulose (HPMC) as release retardants. The suitability of light grade cashew gum as a direct compression excipient was studied using the SeDeM Diagram Expert System. Thirteen tablet formulations of diclofenac sodium (∼100 mg) and metformin hydrochloride (∼200 mg) were prepared with varying amounts of cashew gum, xanthan gum and HPMC by direct compression. The flow properties of blended powders and the uniformity of weight, crushing strength, friability, swelling index and drug content of compressed tablets were determined. In vitro drug release studies of the matrix tablets were conducted in phosphate buffer (diclofenac: pH 7.4; metformin: pH 6.8) and the kinetics of drug release was determined by fitting the release data to five kinetic models. Cashew gum was found to be suitable for direct compression, having a good compressibility index (ICG) value of 5.173. The diclofenac and metformin matrix tablets produced generally possessed fairly good physical properties. Tablet swelling and drug release in aqueous medium were dependent on the type and amount of release retarding polymer and the solubility of drug used. Extended release of diclofenac (∼24 h) and metformin (∼8-12 h) from the matrix tablets in aqueous medium was achieved using various blends of the polymers. Drug release from diclofenac tablets fitted zero order, first order or Higuchi model while release from metformin tablets followed Higuchi or Hixson-Crowell model. The mechanism of release of the two drugs was mostly through Fickian diffusion and anomalous non-Fickian diffusion. The study has demonstrated the potential of blended hydrophilic polymers in the design and optimization of extended release matrix tablets for soluble and poorly soluble drugs by direct

  5. FORMULATION AND EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF VENLAFAXINE HCl

    Directory of Open Access Journals (Sweden)

    P S Rajasekhar

    2012-12-01

    Full Text Available The purpose of the present investigation is to formulate gastroretentive floating tablets of Venlafaxine hydrochloride thus increasing its gastric residence time as well as bioavailability and therapeutic efficacy. Venlafaxine HCl having a short biological half-life of 4h is eliminated quickly from the body leading to low therapeutic efficacy. Therefore a sustained release medication was advantageous so as to achieve the prolonged therapeutic effect and to reduce peak and valley effect in plasma concentration. This can be circumvented by formulating modified gastro retentive sustained release dosage forms which resides in the stomach for sufficient time to release the drug in vicinity of the absorption zone. Nine formulations of Venlafaxine HCl tablets were formulated by hot melt extrusion technique (HME using three polymers like HPMC K15M, Xanthan gum and Guar gum in a various concentrations. Bees wax was used as a melting aid and sodium bicarbonate was used as a gas generating agent. The prepared tablets were evaluated for pre and post compression parameters, buoyancy time, floating lag time and in vitro dissolution study. In vitro dissolution study was carried out in pH 1.2 buffer. It had been found that increase in polymer concentration diminishes drug release profile. The in vitro cumulative % drug release of nine formulations ranged from 88.58 – 99.19 with more than 12h buoyancy. The in vitro drug release of optimised formulation followed Higuchi kinetics and the drug release mechanism was found to be non- fickian type.

  6. A method for combined Sr-Nd-Hf isotopic analysis of <10 mg dust samples: implication for ice core science

    Science.gov (United States)

    Ujvari, Gabor; Wegner, Wencke; Klötzli, Urs

    2017-04-01

    Aeolian mineral dust particles below the size of 10-20 μm often experience longer distance transport in the atmosphere, and thus Aeolian dust is considered an important tracer of large-scale atmospheric circulation. Since ice core dust is purely Aeolian in origin, discrimination of its potential source region(s) can contribute to a better understanding of past dust activity and climatic/environmental causes. Furthermore, ice core dust source information provides critical experimental constraints for model simulations of past atmospheric circulation patterns [1,2]. However, to identify dust sources in past dust archives such as ice cores, the mineralogy and geochemistry of the wind-blown dust material must be characterized. While the amount of dust in marine cores or common terrestrial archives is sufficient for different types of analyses and even for multiple repeat measurements, dust content in ice cores is usually extremely low even for the peak dusty periods such as the Last Glacial Maximum (LGM) (5-8 mg dust/kg ice; [3]). Since the most powerful dust fingerprinting methods, such as REE composition and Sr-Nd-Pb isotopic analyses are destructive there is a clear need to establish sequential separation techniques of Sr, Nd, Pb and other REEs to get the most information out of small (5-10 mg) dust samples recovered from ice cores. Although Hf isotopes have recently been added as a robust tool of aerosol/dust source discrimination (e.g. [4,5,6,7]), precise Hf isotopic measurements of small (Central Europe (NUS), China (BEI) and the US (JUD) were processed (all acetic acid treated for carbonate removal, i.e. aluminosilicate fractions were analysed). Sr isotopic compositions varied between the aliquots within a range of ˜0.00007 for the three samples. Comparison of these values with previously obtained 87Sr/86Sr isotopic ratios from the same samples (different acid/sample amounts) reveals that these values are very sensitive to the acetic acid treatment (acid

  7. Rapacuronium 2.0 or 2.5 mg kg(-1) for rapid-sequence induction : comparison with succinylcholine 1.0 mg kg(-1)

    NARCIS (Netherlands)

    Blobner, M; Mirakhur, RK; Wierda, JMKH; Wright, PMC; Olkkola, KT; Debaene, B; Pendeville, P; Engbaek, J; Rietbergen, H; Sparr, HJ

    2000-01-01

    The purpose of this nine-centre study in 602 patients was to show that the frequency of acceptable intubating conditions after rapacuronium 2.0 or 2.5 mg kg(-1) is not more than 10% lower than the frequency after succinylcholine 1.0 mg kg(-1) during rapid-sequence induction of anaesthesia with fenta

  8. Study on Amlodipine Besylate and Benazepril Hydrochloride Tablets Mixture in Reducing Hypertension Atrial Fibrillation in Patients With Left Ventricular Hypertrophy%氨氯地平贝那普利片合剂减少高血压伴左室肥厚患者新发房颤的研究

    Institute of Scientific and Technical Information of China (English)

    宋宏雁; 景江新; 方志敏; 钟小兰; 刘顺民; 陆云

    2015-01-01

    Objective To compare amlodipine benazepril tablet and single agent to reduce the morbidity of atrial ifbrillation of hypertension patients with left ventricular hypertrophy. Methods 256 patients with hypertension with left ventricular hypertrophy were randomly divided into three groups, amlodipine group (n=85), the benazepril tablet group (n=87), amlodipine benazepril mixture group (n=84), Course of treatment is 18 months. Before and after treatment, blood pressure and echocardiography, dynamic electrocardiogram inspection and new atrial fibrillation and adverse reactions occur were been recorded. Results After treatment, the numerical value of amlodipine benazepril mixture group of patients including diastolic blood pressure, systolic pressure, diastolic left ventricular wall thickness, left atrial diameter value lower than single drug group was obviously, (P<0.05). New af rate is lower than single drug group, incidence of adverse reactions obviously lower than single drug group. Conclusion Amlodipine benazepril tablet is an effective drug to treat hypertension with left ventricular hypertrophy, can obviously control the patient's blood pressure and reverse left ventricular hypertrophy and left atrial enlargement, more signiifcant effect and higher security, lower incidence of atrial ifbrillation.%目的:比较氨氯地平贝那普利片和单剂减少高血压伴左室肥厚患者新发房颤的效果。方法高血压伴左室肥厚患者256例随机分为三组,氨氯地平组(n=85),贝那普利片组(n=87),氨氯地平贝那普利合剂组(n=84),疗程均为18个月。治疗前后进行血压和超声心动图、动态心电图检查和记录新发房颤和不良反应发生情况。结果治疗后,氨氯地平贝那普利合剂组患者舒张压、收缩压、舒张末期左室后壁厚度、左房内径数值较单药组降低明显(P均<0.05);新发房颤率低于单药组,不良反应发生率低于单药组。结论氨

  9. Tableting and tablet properties of alginates: characterisation and potential for Soft Tableting.

    Science.gov (United States)

    Schmid, Wolfgang; Picker-Freyer, Katharina M

    2009-05-01

    The aim of the study was to evaluate the suitability of alginates for Soft Tableting. For this purpose the compaction properties of alginates, varying in molecular weight, guluronic acid/mannuronic acid ratio and salt, were investigated and compared to MCC. Based on the mechanical properties, the suitability of the tested excipients for Soft Tableting was predicted. In order to test the prediction the tested materials were used to tablet enteric coated pellets, which served as a pressure sensitive material. The tableting behaviour was analysed by the 3-D modeling technique. The tablet properties were analysed by determining the elastic recovery and the compactibility. Alginates in general deformed elastically. The compression behaviour depended on the chemical composition of the alginates with sodium alginates being more elastic than potassium alginates. Tablets containing alginates with low guluronic acid content exhibited higher elasticity than tablets with alginates having a low mannuronic acid content. The plasticity of potassium alginates was higher than for sodium alginates. However, the plasticity of all tested alginates was lower than the plasticity of MCC. The compactibility of the tested alginates was sufficient. The proposed prediction, which states that tableting excipients with higher elasticity are more suitable for tableting sensitive materials than plastic excipients, was valid for the tested materials. The elastic alginates inflicted less damage on the pellets than the plastic MCC. Thus, all alginates were more appropriate for tableting pressure sensitive materials than MCC.

  10. Formulation, development and evaluation of patient friendly dosage forms of metformin, Part-I: Orally disintegrating tablets

    OpenAIRE

    Mohapatra Ashutosh; Parikh Rajesh; Gohel Mukesh

    2008-01-01

    Metformin hydrochloride is an orally administered antihyperglycemic agent, used in the management of non-insulin-dependant (type-2) diabetes mellitus. Difficulty in swallowing (dysphagia) is common among all age groups, especially in elderly and pediatrics. Unfortunately, a high percentage of patients suffering from type-2 diabetes are elderly people showing dysphagia. In this study, orally disintegrating tablets were prepared using direct compression and wet granulation method. First, the ta...

  11. An innovative matrix controlling drug delivery produced by thermal treatment of DC tablets containing polycarbophil and ethylcellulose.

    Science.gov (United States)

    Caviglioli, Gabriele; Baldassari, Sara; Cirrincione, Paola; Russo, Eleonora; Parodi, Brunella; Gatti, Paolo; Drava, Giuliana

    2013-12-15

    An innovative matrix, produced by thermal treatment on direct compression (DC) tablets containing polycarbophil (POL) and ethylcellulose (EC), identified as matrix forming polymers, and able to control the release of diltiazem hydrochloride, was developed. At pH 7.2, 72 ± 1.2% (w/w) of drug loaded was released in 25 h, mostly at constant rate. This swellable and unerodible matrix controls drug release by an anomalous transport mechanism. The modifications induced by the thermal treatment are irreversible and can be used to control and characterize the matrix. A 3-component constrained mixture design allowed the investigation of the experimental domain in which the matrix forms and the computation of a mathematical model that can be used to optimize the formulation properties. The release rate can be modulated (0.032-0.064% drug released/min) through the choice of suitable treatment conditions and tablet composition. The maximum amount of diltiazem hydrochloride released by zero-order kinetics, at the lowest release rate, occurs for POL:EC ratio in the range of 1:1-2:3 with 20-30% of diluent. The tablets are able to load up to 50% (w/w) of diltiazem hydrochloride without losing their properties. A stability study performed on a selected formulation containing DTZ showed stability for at least 2.7 years at RT conditions.

  12. 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.

  13. The efficacy and safety of 10 mg vortioxetine in the treatment of major depressive disorder: a meta-analysis of randomized controlled trials

    Directory of Open Access Journals (Sweden)

    Li G

    2016-02-01

    Full Text Available Guangjian Li, Xu Wang, Dihui Ma Department of Neurology and Neuroscience Center, First Hospital of Jilin University, Changchun, People’s Republic of China Background: Vortioxetine is an investigational multimodal antidepressant. We conducted this meta-analysis to assess the efficacy and safety of 10 mg vortioxetine in the treatment of major depressive disorder (MDD. Methods: Randomized controlled trials (RCTs published in PubMed, Web of Science, Embase, and ClinicalTrials.gov were systematically reviewed to assess the treatment effects and safety profiles of patients with MDD who were treated with 10 mg vortioxetine. The outcome measures included response rate, remission rate, changes from baseline in Montgomery–Asberg Depression Rating Scale (MADRS, Hamilton Rating Scale for Depression (24-items (HAM-D24, Clinical Global Impression-Severity (CGI-S, and Clinical Global Impression-Improvement (CGI-I scores. Results were expressed with risk ratio or weighted mean difference with 95% confidence intervals. Pooled results were calculated using a fixed-effects model or a random-effects model according to the heterogeneity among included trials. Results: Six RCTs with a total of 1,801 patients met the inclusion criteria and were included in this meta-analysis. The 10 mg vortioxetine dose significantly increased the response rate and remission rate in the treatment of MDD compared with placebo. Moreover, there was a statistically significant reduction from baseline in the MADRS, HAM-D24, CGI-S, and CGI-I scores with 10 mg vortioxetine vs placebo. The incidence of treatment-emergent adverse events such as nausea, vomiting, constipation, and hyperhidrosis was higher in the 10 mg vortioxetine group than in the placebo group. Conclusion: Vortioxetine 10 mg can significantly increase the response rate and remission rate, and reduce the MADRS, HAM-D24, CGI-S, and CGI-I scores in patients with MDD with an acceptable risk of treatment-emergent adverse

  14. Thermoanalytical Investigation of Terazosin Hydrochloride

    Directory of Open Access Journals (Sweden)

    Mona Mohamed Abdel-Moety

    2013-02-01

    Full Text Available Purpose: Thermal analysis (TGA, DTG and DTA and differential scanning calorimetry (DSC have been used to study the thermal behavior of terazosin hydrochloride (TER. Methods: Thermogravimetric analysis (TGA/DTG, differential thermal analysis (DTA and differential scanning calorimetry (DSC were used to determine the thermal behavior and purity of the used drug. Thermodynamic parameters such as activation energy (E*, enthalpy (H*, entropy (S* and Gibbs free energy change of the decomposition (G* were calculated using different kinetic models. Results: The purity of the used drug was determined by differential scanning calorimetry (99.97% and specialized official method (99.85% indicating to satisfactory values of the degree of purity. Thermal analysis technique gave satisfactory results to obtain quality control parameters such as melting point (273 ºC, water content (7.49% and ash content (zero in comparison to what were obtained using official method: (272 ºC, (8.0% and (0.02% for melting point, water content and ash content, respectively. Conclusion: Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs. DSC data indicated that the degree of purity of terazosin hydrochloride is similar to that found by official method.

  15. 高压氧联合盐酸多奈哌齐治疗卒中后认知功能障碍%Hyperbaric Oxygen Combined with Donepezil Hydrochloride in the Treatment of Post-Stroke Cognitive Impair-ment

    Institute of Scientific and Technical Information of China (English)

    许颖; 杨坚; 高宁沁; 陈小平

    2015-01-01

    目的:分析高压氧联合盐酸多奈哌齐对卒中后认知功能障碍的疗效。方法:将90例住院治疗的卒中后认知功能障碍患者分为高压氧联合盐酸多奈哌齐10 mg组、盐酸多奈哌齐10 mg组、盐酸多奈哌齐5 mg组,每组各30例。采用简易精神状态量表(MMSE)及日常生活能力量表(ADL)评价3组患者治疗前后的认知功能。结果:高压氧联合盐酸多奈哌齐10 mg组患者治疗后MMSE和ADL评分较单用盐酸多奈哌齐组明显增加,差异有统计学意义(P<0.01)。结论:高压氧联合盐酸多奈哌齐(10 mg )对卒中后伴认知功能障碍患者的疗效较好。%Objective:To analyze the efficacy of hyperbaric oxygen combined with donepezil hydrochloride on post‐stroke cogni‐tive impairment .Methods:Ninety hospitalized patients with post‐stroke cognitive impairment were selected .They were divided into hyperbaric oxygen combined with donepezil hydrochloride 10 mg group ,donepezil hydrochloride 10 mg group and donepezil hydrochloride 5 mg group ,with 30 cases in each group .Cognitive functions in 3 groups before and after the treatment were e‐valuated with the mini mental state examination (MMSE) and the ability of daily living scale (ADL) .Results:The scores of MMSE and ADL of patients in hyperbaric oxygen combined with donepezil hydrochloride 10 mg group increased more than those in donepezil hydrochloride groups after treatment ,and the differences were statistically significant (P<0 .01) .Conclu‐sions:Hyperbaric oxygen combined with donepezil hydrochloride 10 mg shows superior efficacy on post‐stroke patients accom‐panied by cognitive impairment .

  16. Acute Psychotic Symptoms due to Benzydamine Hydrochloride Abuse with Alcohol

    Directory of Open Access Journals (Sweden)

    Yahya Ayhan Acar

    2014-01-01

    Full Text Available Benzydamine hydrochloride is a locally acting nonsteroidal anti-inflammatory drug. Benzydamine hydrochloride overdose can cause stimulation of central nervous system, hallucinations, and psychosis. We presented a young man with psychotic symptoms due to benzydamine hydrochloride abuse. He received a total dose of 1000 mg benzydamine hydrochloride with alcohol for its hallucinative effects. Misuse of benzydamine hydrochloride must be considered in differential diagnosis of first-episode psychosis and physicians should consider possibility of abuse in prescribing.

  17. Development of ligustrazine hydrochloride carboxymethyl chitosan and collagen microspheres: Formulation optimization, characterization, and vitro release.

    Science.gov (United States)

    Lin, Qiang; Huo, Qing; Qin, Yingzhe; Zhao, Zhuo; Tao, Fengyun

    2017-01-02

    This study investigates the preparation of ligustrazine hydrochloride carboxymethyl chitosan and collagen microspheres. This experiment investigates effects of the ratio of carboxymethyl chitosan and collagen blend, water to oil ratio, stirring speed, and other factors on the microsphere properties. The experiment had the following conditions: a 1:2 proportion of carboxymethyl chitosan and collagen, a 1:2 proportion of drugs and materials, a 5:1 proportion of oil phase and water phase, 0.5% of span80, a 600r/min stirring speed, 3 ml of a cross-linking agent, 3 h of cross-linking curing, 1.25 ± 0.05 mm diameter LTH microcapsules, a 54.08% envelop rate, and a 14.16% carrier rate. The microspheres release rate reached 66% within 1 h, then steadily released within 5 h in vitro. The experimental results showed that the ligustrazine hydrochloride microsphere production process was stable and exhibited a good release effect compared with other ligustrazine hydrochloride tablets and pills.

  18. Voltammetric behaviour of drotaverine hydrochloride in surfactant media and its enhancement determination in Tween-20.

    Science.gov (United States)

    Jain, Rajeev; Vikas; Rather, Jahangir Ahmad

    2011-02-01

    Simple, sensitive and rapid adsorptive voltammetric behaviour of drotaverine hydrochloride onto the HMDE has been explored and validated in surfactant media by using cyclic, differential pulse and square-wave voltammetry. Addition of Tween-20 to the drotaverine hydrochloride containing electrolyte enhances the reduction current signal. The voltammograms of the drug with Tween-20 in phosphate buffers of pH 2.5-11.0 exhibit a single well defined reduction peak which may be due to the reduction of -CC- group. The cyclic voltammetric studies indicated the reduction of drotaverine hydrochloride at the electrode surface through two electron irreversible step and diffusion-controlled. The peak current showed a linear dependence with the drug concentration over the range 0.8-7.2μgmL(-1). The calculated LOD and LOQ are 1.8 and 6.0ngmL(-1) by SWCAdSV and 8.1 and 27.2ngmL(-1) by DPCAdSV, respectively. The procedure was applied to the assay of the drug in tablet form with mean percentage recoveries of 100.2% with SWCAdSV and 99.7% with DPCAdSV. The validity of the proposed methods was further assessed by applying a standard addition technique.

  19. Evaluation of Plantago major L. seed mucilage as a rate controlling matrix for sustained release of propranolol hydrochloride.

    Science.gov (United States)

    Saeedi, Majid; Morteza-Semnani, Katayoun; Sagheb-Doust, Mehdi

    2013-03-01

    Polysaccharide mucilage derived from the seeds of Plantago major L. (family Plantaginaceae) was investigated for use in matrix formulations containing propranolol hydrochloride. HPMC K4M and tragacanth were used as standards for comparison. The hardness, tensile strength, and friability of tablets increased as the concentration of mucilage increased, indicating good compactibility of mucilage powders. The rate of release of propranolol hydrochloride from P. major mucilage matrices was mainly controlled by the drug/mucilage ratio. Formulations containing P. major mucilage were found to exhibit a release rate comparable to HPMC containing matrices at a lower drug/polymer ratio (drug/HPMC 2:1). These results demonstrated that P. major mucilage is a better release retardant compared to tragacanth at an equivalent content. The results of kinetic analysis showed that in F3 (containing 1:2 drug/mucilage) the highest correlation coefficient was achieved with the zero order model. The swelling and erosion studies revealed that as the proportion of mucilage in tablets was increased, there was a corresponding increase in percent swelling and a decrease in percent erosion of tablets. The DSC and FT-IR studies showed that no formation of complex between the drug and mucilage or changes in crystallinity of the drug had occurred.

  20. Floating matrix dosage form for propranolol hydrochloride based on gas formation technique: development and in vitro evaluation.

    Science.gov (United States)

    Chaturvedi, Kiran; Umadevi, S; Vaghani, Subhash

    2010-01-01

    Gastroretentive tablets of propranolol hydrochloride were developed by direct compression method using citric acid and sodium bicarbonate as the effervescent base. Hydroxypropyl methylcellulose; HPMC K15M was used to prepare the floating tablets to retard the drug release for 12h in stomach. Na-carboxymethyl cellulose (NaCMC) or carbopol 934P was added to alter the drug release profile or the dimensional stability of the formulation. Dicalcium phosphate (DCP) was used as filler. Formulations were evaluated for floating lag time, duration of floating, dimensional stability, drug content and in vitro drug release profile. The formulations were found to have floating lag time less than 1min. It was found that the dimensional stability of the formulations increase with increasing concentration of the swelling agent. The release mechanism of propranolol hydrochloride from floating tablets was evaluated on the basis of Peppas and Higuchi model. The ânâ value of the formulations ranged from 0.5201 to 0.7367 (0.5DCP, 3.75% citric acid and 18.75% sodium bicarbonate seemed most desirable. FTIR, DSC and XRPD studies indicated the absence of any significant chemical interaction within dug and excipients. Stability study of optimized formulation revealed no significant change and found to be stable.

  1. Spectrophotometric determination of diphenhydramine hydrochloride using dipicrylamine.

    Science.gov (United States)

    Shamsa, F A; Maghssoudi, R H

    1976-05-01

    A spectrophotometric procedure for the determination of diphenhydramine hydrochloride based on the reaction with dipicrylamine was developed. A yellow complex forms and is easily extractable by chloroform at pH 5. The mole ratio of diphenydramine hydrochloride to dipicrylamine in the complex is 1:3. The absorbance of the complex obeys Beer's law over the concentration range of 3-10 mug of diphenhydramine hydrochloride per ml of chloroform. This procedure can be carried out in the presence of other compounds without interference.

  2. Assessing Student Writing on Tablets

    Science.gov (United States)

    Davis, Laurie Laughlin; Orr, Aline; Kong, Xiaojing; Lin, Chow-Hong

    2015-01-01

    There is increasing expectation that schools should be able to use tablets for a range of instructional and assessment purposes. This article considers the comparability of student writing on tablets and laptops to ensure that writing assessment is conducted in a way that is fair to all students. Data were collected from a sample of 826 students…

  3. Tablet PCs: The Write Approach

    Science.gov (United States)

    Milner, Jacob

    2006-01-01

    This article discusses the transforming effects of tablet PCs in the classroom. As 1-to-1 computing becomes the goal on K-12 campuses, school districts are turning to this newer, pen-based technology. Saint Mary's School's new Lenovo ThinkPad X41 tablet PCs had transformed the way Saint Mary's teachers did their jobs. Teachers created outlines for…

  4. Perbandingan Penilaian Visual Analog Scale dari Injeksi Subkutan Morfin 10 mg dan Bupivakain 0,5% pada Pasien Pascabedah Sesar dengan Anestesi Spinal

    Directory of Open Access Journals (Sweden)

    Wulan Fadinie

    2016-08-01

    Full Text Available ocal anesthetic agent and opioid can subcutaneously be injected into the wound to reduce postoperative pain. This study was conducted to evaluate pain intensity using visual analog scale (VAS, which can be a very effective method of postoperative pain assessment, and to compare VAS when resting and coughing between local infiltration of 10 mg morphine and 2 mg/kgBW 0.5% bupivacaine after caesarian section. This study was a double blinded randomized clinical trial on 100 subjects. The inclusion criteria were pregnant women, aged 20–40 years, with physical ASA I–II status who underwent elective and emergency caesarean section in Haji Adam Malik Hospital, dr. Pirngadi Hospital, Putri HijauHospital, Haji Hospital, and Sundari Hospital during the period of July 2014. Subjects were divided into group A with 10 mg morphine infiltration and group B with 2 mg/kgBW 0.5% bupivacaine local infiltration. The resulting VAS scores were analyzed statistically using Mann-Whitney. ItLower VAS scores were found in group A 4.72 (SB=1.54 when compared to group B 2.14 (SB=1.21. In conclusion, local infiltration of 10 mg morphine is better compared to 2 mg/kgBW 0.5% bupivacaine.

  5. Bioequivalency of ranitidine tablets.

    Science.gov (United States)

    Alkaysi, H N; Salem, M A; Gharaibeh, A M; el-Sayed, Y M; Ali-Gharaibeh, K I; Badwan, A A

    1989-04-01

    The bioavailability of two brands of ranitidine tablets was studied in 10 healthy volunteers. Formulation factors were compared by performing disintegration, dissolution and content uniformity tests. Plasma concentrations of ranitidine were measured using a sensitive and precise high pressure liquid chromatographic (HPLC) procedure. Pharmacokinetic parameters were determined for both formulations and included: Cmax, AUCt, AUC infinity, tmax, t1/2 and the terminal rate of elimination (k). Statistical analysis revealed that differences between the brands were not significant. The two formulations can be considered to be bioequivalent.

  6. Tablets i skolen

    DEFF Research Database (Denmark)

    Lorentzen, Rasmus Fink

    2012-01-01

    Denne rapport afslutter CELMS undersøgelse af Odder Kommunes projekt med indførelse af iPads på alle kommunens skoler. Undersøgelsen har til formål at belyse om der er pædagogiske og læringsmæssige fordele forbundet med brugen af tablets i undervisningen i grundskolen og i givet fald hvilke...... designer og tablet’ens egenskaber i et generelt perspektiv. Rapporten afsluttes med en række anbefalinger til henholdsvis lærere og skoleledere med henblik på videre udvikling af indsatsen....

  7. Windows for tablets for dummies

    CERN Document Server

    Rathbone, Andy

    2013-01-01

    Just for you--Windows 8 from the tablet user's perspective If you're an experienced Windows user, you don't need a guide to everything that Windows 8 can do, just to those tools and functions that work on your tablet. And so here it is. This new book zeros in on what you need to know to work best on your tablet with Windows 8. Topics include navigating the new Windows 8 interface and how it works on a touchscreen, how to safely connect to the Internet, how to work with apps or share your tablet in a group, and much more. If you're a new tablet user, you'll particularly appre

  8. SIMULTANEOUS ESTIMATION AND VALIDATION OF VARDENAFIL AND DAPOXETINE HYDROCHLORIDE IN PHARMACEUTICAL FORMULATION BY THIN LAYER CHROMATOGRAPHIC DENSITOMETRIC METHOD

    Directory of Open Access Journals (Sweden)

    Bhavin Chapla

    2012-05-01

    Full Text Available The present manuscript describes new, simple, accurate, and precise high performance thin layer chromatography method for the simultaneous determination of Vardenafil and Dapoxetine in combined tablet dosage form. Chromatographic separation of the drugs was performed on aluminium plates pre coated with silica gel 60 F254 as the stationary phase and the solvent system consisted of Chloroform: Methanol: Acetonitrile: Formic acid (4: 0.8: 4: 1 v/v/v/v. Densitometric evaluation of the separated zones was performed at 232 nm. The two drugs were satisfactorily resolved with Rf values 0.47 and 0.79 for Vardenafil and Dapoxetine Hydrochloride, respectively. The linear regression data for the calibration plots showed good relationship with r2 = 0.9995 from 150-750 ng/spot for Vardenafil and r2 = 0.9980 from 450-2250 ng/spot for Dapoxetine Hydrochloride. The methods were validated for precision, accuracy, and recovery. The percentage recovery for Vardenafil was found to be 99.58 – 100.72 % and 99.97 – 100.21% for Dapoxetine Hydrochloride. The limits of detection and quantification were 21.86 and 66.25 ng/spot per spot for Vardenafil and 128.58. and 389.64 ng/spot per spot for Dapoxetine Hydrochloride, respectively.

  9. EFFECTIVENESS AND SAFETY OF MIFEPRISTONE IN DIFFERENT DOSE (10 MG AND 25 MG FOR THE TREATMENT OF UTERINE FIBROIDS AND TO EVALUATE QUALITY OF LIFE

    Directory of Open Access Journals (Sweden)

    Pratibha Rai

    2016-07-01

    Full Text Available BACKGROUND Mifepristone is Selective Progesterone Receptor Modulators (SPRMS and is emerging as a best medical treatment increasing the quality of life as well as saving the patient from surgery. This drug has shown great effectiveness, e.g.: 2.5 mg, 5 mg and 10 mg, but with less reduction in uterine volume as well as reduction in fibroids size. Ref. 1 Yang Y et al. AIM The aim of this study was to evaluate the safety and improvement of life pattern using 10 mg and 25 mg daily doses of Mifepristone for six months with a nine month follow-up period for the regress of fibroids as well as uterine volume to improve quality of life without any surgery in premenopausal women with complaint of menorrhagia, dysmenorrhoea, abdominal discomfort, dyspareunia, rectal pain, urinary problem and weakness due to anaemia. DESIGN The research was a randomized double blind clinical study undertaken at Patliputra Medical College Hospital, Dhanbad (Jharkhand. SEARCH METHOD I had searched a number of international journals, reference lists, databases and ongoing trails and the internet. Also searched the specialised register of Cochrane menstrual disorders and subfertility (Cochrane menstrual disorder and subfertility. The Cochrane central register of control trails (Central. The Cochrane library 2011, Issue 4. METHODOLOGY The trial was done on 100 patients. Patients were divided into two equal groups (All were with symptomatic uterine fibroids to evaluate safety as well as quality of life. Dose decided was 10 mg (A and 25 mg (B of Mifepristone. Subjects were taken from Gynaecological outdoor of Patliputra Medical College Hospital, Dhanbad, (Jharkhand, after taking their consent. All women were between the age group of 35 to 48 years with symptomatic multiple fibroids of various sizes and site. At enrolment patients of both groups underwent clinical assessment, Per Abdomen (P/A and Per Vaginal (P/V examination, USG for uterine volume and size of fibroid. Endometrial

  10. A Novel Synthesis of Difloxacin Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Difloxacin hydrochloride, one of aryl-fluoro quinolone antibiotic, has been synthesized in seven steps from 2, 4-dichloro-5-fluoroacetophenone via oxalylation, ethoxymethylenation,amination, cyclization, hydrolysis, decarbonylation and N-methylpiperazination. Additional four new intermediates are produced.

  11. A novel asymmetric synthesis of cinacalcet hydrochloride

    OpenAIRE

    Arava, Veera R; Laxminarasimhulu Gorentla; Pramod K. Dubey

    2012-01-01

    A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R)-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described.

  12. A novel asymmetric synthesis of cinacalcet hydrochloride

    Directory of Open Access Journals (Sweden)

    Veera R. Arava

    2012-08-01

    Full Text Available A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described.

  13. A novel asymmetric synthesis of cinacalcet hydrochloride

    Science.gov (United States)

    Gorentla, Laxminarasimhulu; Dubey, Pramod K

    2012-01-01

    Summary A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R)-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described. PMID:23019473

  14. Formulation, development and evaluation of patient friendly dosage forms of metformin, Part-I: Orally disintegrating tablets

    Directory of Open Access Journals (Sweden)

    Mohapatra Ashutosh

    2008-01-01

    Full Text Available Metformin hydrochloride is an orally administered antihyperglycemic agent, used in the management of non-insulin-dependant (type-2 diabetes mellitus. Difficulty in swallowing (dysphagia is common among all age groups, especially in elderly and pediatrics. Unfortunately, a high percentage of patients suffering from type-2 diabetes are elderly people showing dysphagia. In this study, orally disintegrating tablets were prepared using direct compression and wet granulation method. First, the tablets of metformin were prepared using starch RX1500 and microcrystalline cellulose by direct compression. The tablets showed erosion behavior rather than disintegration. Then lactose was incorporated which created pores to cause burst release of drug. But these tablets did not give good mouth feel. Thus, Pearlitol SD 200 (spray dried mannitol was used to prepare tablets by wet granulation (10% polyvinylpyrrolidone in Isopropyl alcohol as binder. The optimized batches of tablets (LMCT3 and MP13 not only exhibited desired mouth feel but also disintegration time, in vitro dispersion time, water absorption ratio, and in vitro drug release. All the batches contained 15% starch 1500 and 4% of croscarmellose sodium. The optimized batches prepared by direct compression and wet granulation showed 85% drug release at 4 min and 8 min, respectively. The strong saline and slight bitter taste of the drug was masked using nonnutritive sweetener and flavor.

  15. Feasibility of amlodipine besylate, chloroquine phosphate, dapsone, phenytoin, pyridoxine hydrochloride, sulfadiazine, sulfasalazine, tetracycline hydrochloride, trimethoprim and zonisamide in SyrSpend(®) SF PH4 oral suspensions.

    Science.gov (United States)

    Ferreira, Anderson O; Polonini, Hudson C; Silva, Sharlene L; Patrício, Fernando B; Brandão, Marcos Antônio F; Raposo, Nádia R B

    2016-01-25

    The objective of this study was to evaluate the feasibility of 10 commonly used active pharmaceutical ingredients (APIs) compounded in oral suspensions using an internationally used suspending vehicle (SyrSpend(®) SF PH4 liquid): (i) amlodipine, (as besylate) 1.0mg/mL; (ii) chloroquine phosphate,15.0 mg/mL; (iii) dapsone, 2.0 mg/mL; (iv) phenytoin, 15.0 mg/mL; (v) pyridoxine hydrochloride, 50.0 mg/mL; (vi) sulfadiazine, 100.0 mg/mL; (vii) sulfasalazine, 100.0 mg/mL; (viii) tetracycline hydrochloride, 25.0 mg/mL; (ix) trimethoprim, 10.0 mg/mL; and (x) zonisamide, 10.0 mg/mL. All suspensions were stored both at controlled refrigeration (2-8 °C) and controlled room temperature (20-25 °C). Feasibility was assessed by measuring the percent recovery at varying time points throughout a 90-day period. API quantification was performed by high-performance liquid chromatography (HPLC-UV), via a stability-indicating method. Given the percentage of recovery of the APIs within the suspensions, the expiration date of the final products (API+vehicle) was at least 90 days for all suspensions with regard to both the controlled temperatures. This suggests that the vehicle is stable for compounding APIs from different pharmacological classes.

  16. MOUTH DISSOLVING TABLET: AN OVERVIEW

    Directory of Open Access Journals (Sweden)

    Kulkarni S. D.

    2011-04-01

    Full Text Available Mouth dissolving Tablets disintegrate and/or dissolve rapidly in the saliva without the need for water. Some tablets are designed to dissolve in saliva extremely fast, within a few seconds, and are true fast-dissolving tablets. Others contain agents to enhance the rate of tablet disintegration in the oral cavity, and are more appropriately termed fast-disintegrating tablets, as they may take up to a minute to completely disintegrate. Mouth or Fast dissolving tablets have been formulated for pediatric, geriatric and bedridden patients and in the many elderly persons will have difficulties in taking conventional oral dosage forms because of hand tremors and dysphagia. The technologies used for manufacturing fast-dissolving tablets are freeze-drying, spray-drying, molding, sublimation, sugar-based excipients, compression, and disintegration addition. As a result of increased life expectancy, the elderly constitute a large portion of the worldwide population today. These people eventually will experience deterioration of their physiological and physical abilities.

  17. Quantitative analysis of polymorphic mixtures of ranitidine hydrochloride by Raman spectroscopy and principal components analysis.

    Science.gov (United States)

    Pratiwi, Destari; Fawcett, J Paul; Gordon, Keith C; Rades, Thomas

    2002-11-01

    Ranitidine hydrochloride exists as two polymorphs, forms I and II, both of which are used to manufacture commercial tablets. Raman spectroscopy can be used to differentiate the two forms but univariate methods of quantitative analysis of one polymorph as an impurity in the other lack sensitivity. We have applied principal components analysis (PCA) of Raman spectra to binary mixtures of the two polymorphs and to binary mixtures prepared by adding one polymorph to powdered tablets of the other. Based on absorption measurements of seven spectral regions, it was found that >97% of the spectral variation was accounted for by three principal components. Quantitative calibration models generated by multiple linear regression predicted a detection limit and quantitation limit for either forms I or II in mixtures of the two of 0.6 and 1.8%, respectively. This study demonstrates that PCA of Raman spectroscopic data provides a sensitive method for the quantitative analysis of polymorphic impurities of drugs in commercial tablets with a quantitation limit of less than 2%.

  18. Impact of release characteristics of sinomenine hydrochloride dosage forms on its pharmacokinetics in beagle dogs

    Institute of Scientific and Technical Information of China (English)

    Jin Sun; Jie-Ming Shi; Tian-Hong Zhang; Kun Gao; Jing-Jing Mao; Bing Li; Ying-Hua Sun; Zhong-Gui He

    2005-01-01

    AIM: To investigate the effect of release behavior of sustained-release dosage forms of sinomenine hydrochloride dosage forms, including commercial 12-h sustained-release tablets and 24-h sustained-release pellets prepared in our laboratory, was examined. The two dosage forms were orally administrated to beagle dogs, and then the in vivo formulation was achieved by mixing slow- and rapid-of the sustained-release pellets were scarcely influenced by the pH of the dissolution medium. Release from the 12-h sustained-release tablets was markedly quicker than that from the 24-h sustained-release pellets, the cumulative release up to 12-h was 99.9% vs68.7%. From release pellets had longer tmax and lower Cmax compared to the 12-h sustained-release tablets, the tmax being 2.67±0.52 h vs9.83±0.98 h and the Cmax being 1 334.45±368.76 ng/mL vs 893.12±292.55 ng/mL, respectively. However, the AUC0-tn preparations were statistically bioequivalent. Furthermore,percentage absorption in vivo and the cumulative percentage release in vitro.CONCLUSION: The in vitro release properties of the dosage forms strongly affect their pharmacokinetic behavior in vivo. Therefore, managing the in vitro release behavior of dosage forms is a promising strategy for obtaining the optimal in vivo pharmacokinetic characteristics and safe therapeutic drug concentration-time curves.

  19. COMPARISON OF SAFETY AND EFFICACY OF ROSUVASTATIN (10 MG AND ATORVASTATIN (20 MG IN CASES OF DYSLIPIDAEMIA OVER SIX WEEKS OF TREATMENT

    Directory of Open Access Journals (Sweden)

    Anubhav

    2016-05-01

    Full Text Available AIMS AND OBJECTIVES To Compare the Safety and Efficacy of Rosuvastatin (10 Mg and Atorvastatin (20 Mg in Cases of Dyslipidaemia Over Six Weeks of Treatment. MATERIALS AND METHODS Inclusion Criteria: Both male and female (Excluding Pregnancy above 18 years of age with hypercholesterolaemia, having LDL-C concentration of >159 and, 259 mg/dL and triglyceride concentration of <400 mg/dL, who had failed to have achieved LDL-C goals laid down by the NECP ATP-III guidelines after therapeutic lifestyle change (TLC: HDL-C level: <40 mg/dL for men and, <50 mg/dL for women. 60 cases of dyslipidaemia were selected and 30 were treated with rosuvastatin 10 mg (Study group ‘A’ and 30 of them were treated with atorvastatin 20 mg (study group ‘B’. Exclusion Criteria 1. Use of lipid lowering agents within the past 6 months. 2. Any history of known familial hypercholesterolaemia. 3. Any history of serious or hypersensitivity reactions to other statins. 4. Uncontrolled hypothyroidism; uncontrolled hypertension. 5. Acute liver diseases or hepatic dysfunction. After estimation of total cholesterol, triglycerides, HDL- cholesterol and LDL-c in a basal state, 30 patients were put on rosuvastatin 10 mg and 30 patients were put on atorvastatin 20 mg daily after night meals. After taking drugs, lipid fractions were re-estimated at the end of 4 weeks and 6 weeks. Clinical examination and questions about occurrence of side effects were carried out at interval of 2 weeks. Present study was conducted in the Department of Medicine and Pathology, of Katihar Medical College, Katihar, B. N. Mandal University, Madhepura; Bihar. Approval of the Institutional Ethical Committee was taken. Study conducted by “Keith C et al (2006” showed 37.1±1.3%, improvement in patients treated with RSV (10 and 38.5±1%, with (ATV 20, (ARIES TRIAL, “Cheng J. W. et al (2004” found 43% improvement in levels of LDL-C, with RSV (10 and “Herregod et al (2008” found that RSV (10

  20. [Pharmaceutical technology of Cordaflex tablets].

    Science.gov (United States)

    Erdös, S

    1996-01-01

    First the possibilities of solubilization and the photosensibility of nifedipine (the active ingredient of Cordaflex tablets) were investigated. The technology of retard tablet involves the preparation of a coprecipitate through spraying a solution containing nifedipine, a hydrotropic and a reardizing substance on carrier. After drying the produced granulated material was blended with common auxiliary ingredients, compressed into tablet and coated. The ratio of the two types of coprecipitating substances has a direct effect on the dissolution, so it proved predictable. The reproducibility of technology was good.

  1. Process induced transformations during tablet manufacturing: phase transition analysis of caffeine using DSC and low frequency micro-Raman spectroscopy.

    Science.gov (United States)

    Hubert, Sébastien; Briancon, Stéphanie; Hedoux, Alain; Guinet, Yannick; Paccou, Laurent; Fessi, Hatem; Puel, François

    2011-11-25

    The phase transition of a model API, caffeine Form I, was studied during tableting process monitored with an instrumented press. The formulation used had a plastic flow behavior according to the Heckel model in the compression pressure range of 70-170 MPa. The quantitative methods of analysis used were Differential Scanning Calorimetry (DSC) and low frequency Micro Raman Spectroscopy (MRS) which was used for the first time for the mapping of polymorphs in tablets. They brought complementary contributions since MRS is a microscopic spectral analysis with a spatial resolution of 5 μm(3) and DSC takes into account a macroscopic fraction (10mg) of the tablet. Phase transitions were present at the surfaces, borders and center of the tablets. Whatever the pressure applied during the compression process, the transition degree of caffeine Form I toward Form II was almost constant. MRS provided higher transition degrees (50-60%) than DSC (20-35%). MRS revealed that caffeine Form I particles were partially transformed in all parts of the tablets at a microscopic scale. Moreover, tablet surfaces showed local higher transition degree compared to the other parts.

  2. Bioequivalence studies of film-coated tablet and chewable tablet generic formulations of montelukast in healthy volunteers.

    Science.gov (United States)

    Cánovas, Mercedes; Arcabell, Marta; Martínez, Gemma; Canals, Mirela; Cabré, Francesc

    2011-01-01

    Two studies were conducted in order to assess the bioequivalence of montelukast (CAS 151767-02-1) 10 mg film-coated tablet (FCT) and 5 mg chewable tablet (CT) test formulations in comparison with the original brands. Under fasting conditions, healthy male and female volunteers received one 10 mg FCT or 5 mg CT orally as a single dose of a test or reference formulation. Both studies were designed as open-label, randomized, two-period, two-sequence, crossover studies with a 7-day washout interval. Plasma samples were collected up to 24 h after drug administration and montelukast levels were determined by a validated LC/ MS/MS method. Pharmacokinetic parameters were calculated using non-compartmental analysis and were statistically compared by analysis of variance for test and reference formulation. Bioequivalence between products was determined by calculating 90% confidence interval of the ratio test/reference of least-square means of logarithmically transformed Cmax and AUC0-t parameters. AUC0-infinity was also analysed to obtain additional information. The calculated 90% confidence intervals for the ratios of Cmax and AUC0-t parameters were 89.33-110.52 and 92.06-109.46, respectively, in the FCT study, and 91.58-101.86 and 92.15-98.83, respectively, in the CT study, which are all within the bioequivalence acceptance range of 80-125%. Based on the results, it can be concluded that the evaluated test FCT and CT formulations are bioequivalent to their respective reference formulation in terms of rate and extent of absorption.

  3. PEDIATRIC FORMULATION OF RANITIDINE USING FROM COMMERCIALLY AVAILABLE TABLETS IN ALBANIA

    Directory of Open Access Journals (Sweden)

    Briseida Dosti

    2016-03-01

    Full Text Available Background: Ranitidine Hydrochloride is H2 – receptor antagonist indicated for duodenal ulcer. It is used for the treatment of gastric/duodenal ulcer and GERD for both neonates and children, in respective dosage 1.5- 2mg/kg/24h, q12h and 1-5mg/kg/24h, q6-8h. For use in children is needed cutting into smaller parts to obtain appropriate units, since are missing more appropriate pharmaceuticals forms, such as liquid formulations. Objectives: The purpose of this study was to evaluate the accuracy of splitting ranitidine hydrochloride 150 mg tablets, in dosage for children. Prepare extemporaneous Ranitidine syrup from commercially available tablets and determine it stability. Methods: This study was conducted with three different types of ranitidine tablets, chosen based on the presence or not of the score line. For the preparation of Ranitidine syrup were pulverized tablets of Ranitidine 150 mg and suspended in base solution distilled water and simple syrup. This mixture was diluted to a total volume of 120 ml; resulting in a final ranitidine concentration of 15 mg/ml. A UV-VIS spectrophotometer (Cary 100, Varian was used to determine ranitidine concentration at wavelength 315 nm. Results: Cutting Ranitidine TBL into halves and quarters lead to large deviations. These deviations were related to the presence or not of the score line. It was shown that prepared formulations retain minimum 98% of initial Ranitidine concentration after 7 days of storage at 25°C and 4°C.

  4. Studies on applicability of press-coated tablets using hydroxypropylcellulose (HPC) in the outer shell for timed-release preparations.

    Science.gov (United States)

    Fukui, E; Uemura, K; Kobayashi, M

    2000-08-10

    Press-coated tablets, containing diltiazem hydrochloride (DIL) in the core tablet and coated with hydroxypropylcellulose (HPC) as the outer shell, were examined for applicability as timed-release tablets with a predetermined lag time and subsequent rapid drug release phase. Various types of press-coated tablets were prepared using a rotary tabletting machine and their DIL dissolution behavior was evaluated by the JP paddle method. The results indicated that tablets with the timed-release function could be prepared, and that the lag times were prolonged as the viscosity of HPC and the amount of the outer shell were increased. The lag times could be controlled widely by the above method, however, the compression load had little effect. Two different kinds of timed-release press-coated tablets that showed lag times of 3 and 6 h in the in vitro test (denoted PCT(L3) and PCT(L6), respectively) were administered to beagle dogs. DIL was first detected in the plasma more than 3 h after administration, and both tablets showed timed-release. The lag times showed a good agreement between the in vivo and in vitro tests in PCT(L3). However, the in vivo lag times were about 4 h in PCT(L6) and were much shorter than the in vitro lag time. The dissolution test was performed at different paddle rotation speeds, and good agreement was obtained between the in vivo and in vitro lag times at 150 rpm. This suggested that the effects of gastrointestinal peristalsis and contraction should also be taken into consideration for the further development of drug delivery systems.

  5. Octenidine hydrochloride in hydatid disease.

    Science.gov (United States)

    Altindis, Mustafa; Arikan, Yuksel; Cetinkaya, Zafer; Polat, Coskun; Yilmaz, Sezgin; Akbulut, Gökhan; Dilek, Osman Nuri; Gokce, Ozcan

    2004-01-01

    Hydatid disease is still endemic in many devoloping countries and continues to be an important cause of morbidity. The objective of this study was to determine the in vitro scolicidal effects of octenidine hydrochloride in different concentrations using different exposure times. After hydatid cyst liquid was left to precipitate for 1 h to obtain cystic sand, various concentrations of octenidine (undiluted, 1% and 0.1% diluted) were added to concentrated hydatid cyst sediments for 5, 10, 15, 20, 25, 30, 45, and 60 min, and scolicidal effects of octenidine were compared with 20% saline and control group for the same times. It was found that undiluted octenidine had a strong scolicidal effect at 15 min compared to saline at 20%. One percent octenidine had a scolicidal effect at 30 min. However, 0.1% octenidine did not have enough scolicidal effect in 1 h. It was concluded that undiluted and 1% diluted octenidine might be used for scolicidal purpose in the treatment of hydatid disease.

  6. Formulation and Evaluation Of Metformin HCl Mouth Dissolving Tablet Using Sublimating Agent

    Directory of Open Access Journals (Sweden)

    Sofiya Moris

    2015-07-01

    Full Text Available The present study was focused on the development of orodispersible tablets of Metformin HCl for improving patient compliance, especially pediatric and geriatric categories by sublimation technique and comparing the super disintegrating property of benzoic acid and camphor .The other ingredients used in the formulations are crosspovidone, xylitol, magnesium stearate, talc and directly compressible mannitol to enhance the mouth feel. The total seven batches were prepared (F1–F6 and F7 (without superdisintegrant. Tablets were evaluated for weight variation, friability, hardness, drug content uniformity, in-vitro disintegration and dissolution studies. Among all the formulated tablets F3 which is based on Metformin Hcl with 40 mg benzoic acid was found to be the highest dissolution (92.56% in 10 mins. From the dissolution result it is clear that the benzoic acid at different concentration showed better dissolution rate as a disintegrant as compare to camphor. Hence, benzoic acid was a good alternative as a disintegrant for the preparation of directly compressible mouth dissolving tablets of Metformin Hydrochloride.

  7. Tableting technology from the individual and new galenic alkaloid consisting preparations of the Phellodendron lavallei bark.

    Science.gov (United States)

    Meskheli, M; Vachnadze, V; Kurdiani; Tsagareishvili, N; Bakuridze, A

    2011-06-01

    The aim of the research was to work out the technology and tablet composition from new galenic preparations consisting of alkaloids of the bark of Phellodendron lavallei and hydrochloride of berberin on the base of complex research. The bark of the Phellodendron lavallei introduced in Georgia contains alkaloids, from which 2% is berberine used for curing chronicle hepatitis, hepatic cholecystitis and bilestone disease. The structural-mechanical and technological character of tablets and their masses were defined by the known methodic. Friability was studied by defining the fluctuation and bending corner. Volume density was established by using vibration cylinder. Volume density of powders was studied by pyknometers. Porosity was calculated by the bearing of volume density of the masses. The size of pressing was established by defining the firmness of tablets. The granule composition was defined by analysis. On the basis of studying technological and physical-chemical character features of the substances of new galenic preparations and individual substances consisting of alkaloids got from the bark of Phellodendron lavallei, it is scientifically proved and practically offered optimal technological parameters of tablets forming process and recipes.

  8. Influence of Polymer Type on the Physical Properties and Release Profile of Papaverine Hydrochloride From Hard Gelatin Capsules.

    Science.gov (United States)

    Polski, Andrzej; Iwaniak, Karol; Kasperek, Regina; Modrzewska, Joanna; Sobótka-Polska, Karolina; Sławińska, Karolina; Poleszak, Ewa

    2015-01-01

    The capsule is one of the most important solid dosage forms in the pharmaceutical industry. It is easier and faster to produce than a tablet, because it requires fewer excipients. Generally, capsules are easy to swallow and mask any unpleasant taste of the substances used while their release profiles can be easily modified. Papaverine hydrochloride was used as a model substance to show different release profiles using different excipients. The main aim of the study was to analyze the impact of using different polymers on the release profile of papaverine hydrochloride from hard gelatin capsules. Six series of hard gelatin capsules containing papaverine hydrochloride as a model drug and different excipients were made. Then, the angle of repose, flow rate, mass flow rate and volume flow rate of the powders used for capsule production were analyzed. The uniform weight and disintegration time of the capsules were studied. The dissolution study was performed in a basket apparatus, while the amount of papaverine hydrochloride released was determined spectrophotometrically at 251 nm. Only one formula of powder had satisfactory flow properties, while all formulas had good Hausner ratios. The best properties were from powder containing polyvinylpyrrolidone 10k. The disintegration time of capsules varied from 1:30 min to 2:00 min. As required by Polish Pharmacopoeia X, 80% of the active substance in all cases was released within 15 minutes. The capsules with polyvinylpyrrolidone 10k were characterized by the longest release. On the other hand, capsules containing microcrystalline cellulose had the fastest release profile. Using 10% of different polymers, without changing the other excipients, had a significant impact on the physical properties of the powders and papaverine hydrochloride release profile. The two most preferred capsule formulations contained either polyvinylpyrrolidone 10k or microcrystalline cellulose.

  9. Compound list: fluoxetine hydrochloride [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available fluoxetine hydrochloride FLX 00158 ftp://ftp.biosciencedbc.jp/archive/open-tggates/...LATEST/Human/in_vitro/fluoxetine_hydrochloride.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/o...pen-tggates/LATEST/Rat/in_vivo/Liver/Single/fluoxetine_hydrochloride.Rat.in_vivo.Liver.Single.zip ftp://ftp....biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liver/Repeat/fluoxetine_hydrochloride.Rat.in_vivo.Liver.Repeat.zip ...

  10. Formulation and Evaluation of sustained release matrix tablets of Glipizide

    Directory of Open Access Journals (Sweden)

    Shallu Sandhan*

    2013-12-01

    Full Text Available The aim of present investigation was to enhance the solubility of glipizide (BCS Class II. Glipizide is an oral antidiabetic agent with relatively short elimination half life. Inclusion complex of Glipizide with β-cyclodextrin was prepared by kneading method and evaluated for its in-vitro release. Phase solubility studies were performed according to method reported by Higuchi and Connors which was classified as AL type characterized by apparent 1:1 stability constant. The Glipizide & Beta Cyclodextrin found to be compatible which was observed from FTIR spectra of Glipizide β- CD Complex. The dissolution study of Glipizide β- CD complex shows significant increase in the drug release than pure drug. Matrix Glipizide β- CD complex tablet complex equivalent to 10 mg Glipizide were prepared by using Hydroxy propyl methyl cellulose (HPMC, Carboxy methyl cellulose sodium (NaCMC and Microcrytalline cellulose (MCC. The tablets were evaluated for various tests like hardness, friability, disintegration and in-vitro dissolution studies.

  11. Maintenance of remission with low-dose olopatadine hydrochloride for itch in well-controlled chronic urticaria

    Directory of Open Access Journals (Sweden)

    Makino T

    2012-09-01

    Full Text Available Teruhiko Makino,1 Yoshiaki Takegami,1 Mati Ur Rehman,1 Yoko Yoshihisa,1 Waka Ishida,2 Takashi Toyomoto,3 Tadamichi Shimizu11Department of Dermatology, University of Toyama, Toyama, Japan; 2Department of Dermatology, Niigata Central Hospital, Joetsu, Japan; 3Department of Dermatology, Saiseikai Takaoka Hospital, Takaoka, JapanBackground: The long-term follow-up of chronic urticaria (CU is important to ensure the adequate treatment of patients. Olopatadine hydrochloride is one of the second-generation nonsedating antihistamines.Methods: This study was designed to assess the optimal dose of olopatadine to suppress symptoms of chronic urticarial itch in well-controlled patients. After CU patients were treated with 10 mg olopatadine, patients having a visual analogue scale (VAS itch score of less than 20 were randomly allocated into one of three groups: 10 mg/day (n = 35, 5 mg/day (n = 30, or no medication (n = 32.Results: The suppressive effects of both the 5 mg and 10 mg olopatadine treatments on the VAS itch score were more significant and longer lasting over a period of 4 weeks than the no-medication treatment. Both the 5-mg group and the 10-mg group showed improved urticarial symptoms and maintained their VAS itch score within normal limits compared to the no-medication group. The differences between the 5-mg and 10-mg groups were not significant.Conclusion: These results demonstrate that treatment with olopatadine at a dose of 5 mg once daily is effective and safe for the management and prevention of CU symptoms for itch in well-controlled patients.Keywords: chronic urticaria, olopatadine, dose, antihistamine, itch, histamine

  12. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Glutamic acid hydrochloride. 182.1047 Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride....

  13. HPTLC method for the simultaneous estimation of Tizanidine and Rofecoxib in tablets

    Directory of Open Access Journals (Sweden)

    Ravi T

    2006-01-01

    Full Text Available A new simple, accurate and precise HPTLC method has been developed for the simultaneous estimation of tizanidine and rofecoxib in tablet formulation. In this method, standard and sample solutions of tizanidine and rofecoxib were applied on precoated silica gel G 60 F254 TLC plate, and developed using n- butyl acetate: formic acid: chloroform (6:4:2 v/v/v, as mobile phase. The drugs on plate were scanned at 315 nm. The dynamic linearity range was 2-10 mg/spot for tizanidine and 16-80 mg/spot for rofecoxib. The method was validated for precision, accuracy, and reproducibility.

  14. Efficacy of Long-Term Daily Dosage of Alfuzosin 10 mg upon Sexual Function of Benign Prostatic Hypertrophy Patients: Two-Year Prospective Observational Study.

    Science.gov (United States)

    Yoon, Sol; Choi, Jae Hwi; Lee, Seung Hyun; Choi, See Min; Jeh, Seong Uk; Kam, Sung Chul; Hwa, Jeong Seok; Chung, Ky Hyun; Hyun, Jae Seog

    2014-12-01

    To identify sexual function improvement associated with alfuzosin (10 mg daily for 2 years). We enrolled 30 men with lower urinary tract symptom (LUTS) who visited Gyeongsang National University Hospital between 2010 and 2012. At first visit, urinalysis, prostate specific antigen, transrectal ultrasound, and uroflowmetry were performed. The nternational Prostate Symptom Score (IPSS), quality of life (QoL), International Index of Erectile Function (IIEF), and Male Sexual Health Questionnaire Ejaculation Function Domain (MSHQ-EjFD) questionnaires were administered, and the subjects answered the same questionnaires at 1 month, 6 months, 1 year, and 2 years of follow-up. Twelve men completed of the entire study. After administration of alfuzosin, the median IPSS at first visit, 1 month, 6 months, 1 year, and 2 years was 18.00 (interquatile range [IQR]: 14.00~29.75), 20.00 (IQR: 11.50~30.00), 15.50 (IQR: 8.50~25.25), 14.50 (IQR: 9.25~19.50), and 11.50 (IQR: 5.00~17.75), respectively, which showed an improvement. The median QoL at the same times was 4.50 (IQR: 4.00~5.00), 4.50 (IQR: 4.00~5.00), 3.00 (IQR: 2.00~4.00), 3.50 (IQR: 2.25~4.00), and 3.00 (IQR: 1.00~3.00), respectively, and also showed improvement. Likewise, the median IIEF was 36.50 (IQR: 24.50~46.75), 37.50 (IQR: 26.75~47.25), 45.50 (IQR: 35.00~59.75), 48.50 (IQR: 34.75~62.75), and 47.50 (IQR: 43.25~61.00), while the median MSHQ-EjFD was 19.00 (IQR: 12.0~24.75), 19.50 (IQR: 13.50~27.75), 23.00 (IQR: 19.25~32.25), 26.50 (IQR: 18.25~34.50), 27.00 (IQR: 21.50~32.50), respectively, with both showing improvement. After administration of alfuzosin (10 mg daily for 2 years), the IPSS, QoL, IIEF, and MSHQ-EjFD all improved significantly. This means long-term administration of 10 mg of alfuzosin daily would be effective not only for LUTS but also erectile function and ejaculation.

  15. Fetal Exposure to Sertraline Hydrochloride Impairs Pancreatic β-Cell Development.

    Science.gov (United States)

    De Long, Nicole E; Gutgesell, Marie K; Petrik, James J; Holloway, Alison C

    2015-06-01

    Ten percent to 15% of women take selective serotonin reuptake inhibitor (SSRI) antidepressants during pregnancy. Offspring exposed to SSRIs are more likely to have low birth weight; this is associated with an increased risk of development of diabetes in adulthood in part due to altered pancreatic development. The effects of perinatal exposure to SSRIs on pancreatic development are unknown. Therefore, the objective of this study was to determine the effect of fetal exposure to sertraline hydrochloride on pregnancy outcomes and pancreatic development. Wistar rats were given vehicle (n = 5) or sertraline hydrochloride (10 mg/kg/d; n = 8) via daily subcutaneous injection from the confirmation of mating until parturition. Results from this animal model demonstrated that offspring born to sertraline-exposed dams have no changes in birth weight but had a reduction in pancreatic β-cell area. The altered pancreatic islet development was a result of altered gene expression regulating islet development and survival. Therefore, fetal exposure to sertraline reduces β-cell capacity at birth, raising concerns regarding the long-term metabolic sequelae of such exposures.

  16. Effect of the addition of Al-Ti-C master alloy on the microstructure and microhardness of a cast Al-10Mg alloy

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    The microstructure and microhardness of a cast Al-10wt%Mg (henceforth Al-l0Mg) alloy with 0.2wt% addition of Al-5Ti-0.25C master alloy were compared with those of a refiner-free alloy of similar chemical composition.It was found that this level of the master alloy addition not only caused an effective grain refinement, but also caused a significant increase in the microhardness of the Al-10Mg alloy.Microchemical analysis revealed that TiC particles existed in the grain center.The relationship between the holding time and grain size was also studied.It shows that the grain refining efficiency is faded observably with the holding time.This is explained in terms of the instability of TiC particles.

  17. Fabrication of extended-release patient-tailored prednisolone tablets via fused deposition modelling (FDM) 3D printing.

    Science.gov (United States)

    Skowyra, Justyna; Pietrzak, Katarzyna; Alhnan, Mohamed A

    2015-02-20

    Rapid and reliable tailoring of the dose of controlled release tablets to suit an individual patient is a major challenge for personalized medicine. The aim of this work was to investigate the feasibility of using a fused deposition modelling (FDM) based 3D printer to fabricate extended release tablet using prednisolone loaded poly(vinyl alcohol) (PVA) filaments and to control its dose. Prednisolone was loaded into a PVA-based (1.75 mm) filament at approximately 1.9% w/w via incubation in a saturated methanolic solution of prednisolone. The physical form of the drug was assessed using differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD). Dose accuracy and in vitro drug release patterns were assessed using HPLC and pH change flow-through dissolution test. Prednisolone loaded PVA filament demonstrated an ability to be fabricated into regular ellipse-shaped solid tablets using the FDM-based 3D printer. It was possible to control the mass of printed tablet through manipulating the volume of the design (R(2) = 0.9983). On printing tablets with target drug contents of 2, 3, 4, 5, 7.5 and 10mg, a good correlation between target and achieved dose was obtained (R(2) = 0.9904) with a dose accuracy range of 88.7-107%. Thermal analysis and XRPD indicated that the majority of prednisolone existed in amorphous form within the tablets. In vitro drug release from 3D printed tablets was extended up to 24h. FDM based 3D printing is a promising method to produce and control the dose of extended release tablets, providing a highly adjustable, affordable, minimally sized, digitally controlled platform for producing patient-tailored medicines. Copyright © 2015. Published by Elsevier B.V.

  18. Lipid- regulatory Efficacy and Safety of Rosuvastatin (10 mg·d~(-1)) for Chinese Population: A Metaanalysis%瑞舒伐他汀10 mg·d~(-1)对国人调脂作用有效性和安全性的Meta分析

    Institute of Scientific and Technical Information of China (English)

    郑雅婷; 周立岩; 刘松岭

    2009-01-01

    OBJECTIVE: To evaluate the lipid - regulatory efficacy and safety of rosuvastatin (10 mg·d ~(-1)) for Chinese population. METHODS: The pertinent literature comparing the serum blood lipid level before and after treatment with rosuvastatin (10 mg·d~(-1)) between 2001 and 2008 were collected by retrieving Wanfang database, CNKI, Weipu electronic periodicals; and the data were given a meta - analysis using RevMan 4.2 software, meanwhile the safety of rosuvastatin was e-valuated. RESULTS: A total of 346 patients were enrolled in 5 trials. After treatment with rosuvastatin (10 mg·d ~(-1)), the low density lipoproteincholesterol(LDL-C) was lowered by 1.71 mmol·L ~(-1) on average; the total cholesterol (TC) was lowered by 1.98 mmol·L ~(-1) on average; high density lipoprotein cholesterol(HDL-C) was increased by 0.17 mmol·L ~(-1) on average; and the level of triglyeride was lowered by 0.79 mmol·L~(-1) on average. A total of 54 adverse events were reported, and the adverse drug reactions manifested chiefly as upper respiratory infection, mild notalgia, debilitation and gastrointestinal upset. No severe side effects were reported. CONCLUSION: It has been confirmed by domestic clinical trials that rosuvastatin (10 mg · d ~(-1)) is safe and effective for Chinese population.%目的:评价瑞舒伐他汀10 mg·d~(-1)对国人调脂作用的有效性和安全性.方法:从万方数据库、中国期刊网全文数据库、维普全文电子期刊中检索2001~2008年的相关文献,比较应用瑞舒伐他汀10 mg·d~(-1)前、后血脂的变化,并利用RevMan4.2对数据进行Meta分析,同时对其安全性作出评价.结果:5项研究共346例患者入选,经瑞舒伐他汀10 mg·d~(-1)治疗后低密度脂蛋白胆固醇(LDL-C)平均降低1.71 mmol·L~(-1),总胆固醇(TC)平均降低1.98 mmol·L~(-1),高密度脂蛋白胆固醇(HDL-C)平均升高0.17 mmol·L~(-1),甘油三酯(TG)平均降低0.79 mmol·L~(-1).共报道了54例不良事件,主要为轻微的上呼

  19. 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.

  20. 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

    2017-09-11

    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.

  1. Capillary electrophoresis for the assay of fixed-dose combination tablets of artesunate and amodiaquine

    Directory of Open Access Journals (Sweden)

    Amin N’Cho

    2012-05-01

    Full Text Available Abstract Background Quality control of drugs in formulations is still a major challenge in developing countries. For the quality control of artesunate and amodiaquine tablets in fixed-dose combination, only liquid chromatographic methods have been proposed in the literature. There are no capillary electrophoretic methods reported for the determination of these active substances, although this technique presents several advantages over liquid chromatography (long lifetime, low price of the capillary, low volumes of electrolyte consumption in addition to simplicity. In this paper, a reliable capillary electrophoresis method has been developed and validated for the quality control of these drugs in commercial fixed-dose combination tablets. Methods Artesunate and amodiaquine hydrochloride in bilayer tablets were determined by micellar electrokinetic capillary chromatography (MEKC. Analytes were extracted from tablets by sonication with a solvent mixture phosphate buffer pH 7.0-acetonitrile containing benzoic acid as internal standard. Separation was carried out on Beckman capillary electrophoresis system equipped with fused silica capillary, 30 cm long (20 cm to detector × 50 μm internal diameter, using a 25 mM borate buffer pH 9.2 containing 30 mM sodium dodecyl sulfate as background electrolyte, a 500 V cm−1 electric field and a detection wavelength of 214 nm. Results Artesunate, amodiaquine and benzoic acid were separated in 6 min. The method was found to be reliable with respect to specificity,linearity of the calibration line (r2 > 0.995, recovery from synthetic tablets (in the range 98–102%, repeatability (RSD 2–3%, n = 7 analytical procedures. Application to four batches of commercial formulations with different dosages gave content in good agreement with the declared content. Conclusion The MEKC method proposed is reliable for the determination of artesunate and amodiaquine hydrochloride in fixed

  2. Simultaneous Estimation of Hydrochlorothiazide, Hydralazine Hydrochloride, and Reserpine Using PCA, NAS, and NAS-PCA.

    Science.gov (United States)

    Sharma, Chetan; Badyal, Pragya Nand; Rawal, Ravindra K

    2015-01-01

    In this study, new and feasible UV-visible spectrophotometric and multivariate spectrophotometric methods were described for the simultaneous determination of hydrochlorothiazide (HCTZ), hydralazine hydrochloride (H.HCl), and reserpine (RES) in combined pharmaceutical tablets. Methanol was used as a solvent for analysis and the whole UV region was scanned from 200-400 nm. The resolution was obtained by using multivariate methods such as the net analyte signal method (NAS), principal component analysis (PCA), and net analyte signal-principal component analysis (NAS-PCA) applied to the UV spectra of the mixture. The results obtained from all of the three methods were compared. NAS-PCA showed a lot of resolved data as compared to NAS and PCA. Thus, the NAS-PCA technique is a combination of NAS and PCA methods which is advantageous to obtain the information from overlapping results.

  3. Simultaneous determination of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate in pharmaceutical preparations using multivariate calibration 1

    Science.gov (United States)

    Samadi-Maybodi, Abdolraouf; Hassani Nejad-Darzi, Seyed Karim

    2010-04-01

    Resolution of binary mixtures of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate with minimum sample pre-treatment and without analyte separation has been successfully achieved by methods of partial least squares algorithm with one dependent variable, principal component regression and hybrid linear analysis. Data of analysis were obtained from UV-vis spectra of the above compounds. The method of central composite design was used in the ranges of 1-15 mg L -1 for both calibration and validation sets. The models refinement procedure and their validation were performed by cross-validation. Figures of merit such as selectivity, sensitivity, analytical sensitivity and limit of detection were determined for all three compounds. The procedure was successfully applied to simultaneous determination of the above compounds in pharmaceutical tablets.

  4. Characterization of omega-3 tablets.

    Science.gov (United States)

    Vestland, Tina Lien; Jacobsen, Øyvind; Sande, Sverre Arne; Myrset, Astrid Hilde; Klaveness, Jo

    2016-04-15

    Omega-3 nutraceuticals are extensively used as health supplements worldwide. Various administration forms for delivery of omega-3 are available. However, the niche omega-3 tablets have so far remained unexplored. In this work tablets containing 25-40% (w/w) omega-3 oil as triglycerides or ethyl esters were prepared utilizing a direct compaction grade powder with β-cyclodextrin as encapsulating agent. It was found that powders with up to 35% (w/w) triglyceride oil and 30% (w/w) ethyl ester oil, respectively, can be directly compressed into tablets of excellent quality. Physical properties of omega-3 containing powders and tablets are described. The powder X-ray diffractograms of the powders and crushed tablets show evidence of the formation of new crystalline phases not present in β-cyclodextrin. In addition, (1)H NMR data suggest that the ethyl esters form inclusion complexes with β-cyclodextrin. Compaction of other, commercially available, omega-3 powders was performed as a comparison and deemed unsuccessful.

  5. Dissolution and permeation characteristics of artemether tablets ...

    African Journals Online (AJOL)

    and permeation characteristics of the formulations were studied using USP methods. Results: Tablets .... Table 2: Physical properties of the artemether tablets. Batch. Code. CS (kgf) ..... metformin using prosopis gum with antidiabetic potential.

  6. Anestesia espinhal com 10 mg de bupivacaína hiperbárica associada a 5 µg de sufentanil para cesariana: estudo de diferentes volumes Anestesia espinal con 10 mg de bupivacaína hiperbárica asociada a 5 µg de sufentanil para cesárea: estudio de diferentes volúmenes Spinal Block with 10 mg of hyperbaric bupivacaine associated with 5 µg of sufentanil for cesarean section: study of different volumes

    Directory of Open Access Journals (Sweden)

    Angélica de Fátima de Assunção Braga

    2010-04-01

    Full Text Available JUSTIFICATIVA E OBJETIVOS: Diversos fatores influenciam na dispersão cefálica da solução anestésica no espaço subaracnóideo, entre os quais destacam-se as alterações fisiológicas inerentes à gravidez, baricidade, dose e volume do anestésico local. O objetivo deste estudo foi avaliar em cesarianas a efetividade e os efeitos colaterais de diferentes volumes da associação de bupivacaína hiperbárica e sufentanil por via subaracnóidea. MÉTODO: Quarenta pacientes, ASA I e II, submetidas à cesariana eletiva sob raquianestesia distribuídas em dois grupos, de acordo com o volume da solução anestésica empregada: Grupo I (4 mL e Grupo II (3 mL. Nos dois grupos o anestésico local empregado foi a bupivacaína hiperbárica (10 mg-2 mL associada ao sufentanil (5 µg-1 mL. No Grupo I, para obtenção do volume de 4 mL, foi adicionado 1 mL de solução fisiológica a 0,9%. Foram avaliados: latência do bloqueio; nível máximo do bloqueio sensitivo; grau do bloqueio motor; tempo para regressão do bloqueio motor; duração total da analgesia; efeitos adversos maternos e repercussões neonatais. RESULTADOS: A latência, o nível máximo do bloqueio sensitivo, o grau e o tempo para regressão do bloqueio motor foram semelhantes nos dois grupos; a duração da analgesia foi maior no Grupo I, com diferença significativa em relação ao Grupo II. Os efeitos adversos ocorreram com frequência semelhante em ambos os grupos. Ausência de alterações cardiocirculatórias maternas e repercussões neonatais. CONCLUSÕES: A bupivacaína hiperbárica na dose de 10 mg associada ao sufentanil na dose de 5 µg, com volume de 4 mL, foi mais eficaz que a mesma associação em menor volume (3 mL, proporcionando melhor analgesia intra e pós-operatória, sem repercussões materno-fetais.JUSTIFICATIVA Y OBJETIVOS: Diversos factores influyen en la dispersión cefálica de la solución anestésica en el espacio subaracnoideo, entre los cuales se destacan las

  7. Evaluation of quick disintegrating calcium carbonate tablets

    OpenAIRE

    Fausett, Hector; Gayser, Charles; Dash, Alekha K.

    2000-01-01

    The purpose of this investigation was to develop a rapidly disintegrating calcium carbonate (CC) tablet by direct compression and compare it with commercially available calcium tablets. CC tablets were formulated on a Carver press using 3 different forms of CC direct compressed granules (Cal-Carb 4450®, Cal-Carb 4457®, and Cal-Carb 4462®). The breaking strength was measured using a Stokes-Monsanto hardness tester. The disintegration and dissolution properties of the tablets were studied using...

  8. ORALLY DISINTEGRATING TABLETS: A REVIEW

    Directory of Open Access Journals (Sweden)

    Mudgal Vinod Kumar

    2011-04-01

    Full Text Available Orally disintegrating tablets (ODTs are gaining prominence as new drug delivery systems and emerged as one of the popular and widely accepted dosage forms, especially for the pediatric and geriatric patients. To obviate the problem of dysphagia and to improve patient compliance, ODTs have gained considerable attention as preferred alternatives to conventional tablet and capsule formulations. Various scientific techniques including freeze drying, moulding, spray drying, sublimation, direct compression, cotton candy process, mass extrusion, melt granulation etc. have been employed for the development of ODTs. These techniques render the disintegration of tablet rapidly and dissolve in mouth without chewing or additional water intake. The current article is focused on ideal characteristics, significant features, patented technologies, formulation aspects including the use of superdisintegrants. Various marketed preparations along with numerous scientific advancements made so far in this avenue have also been discussed.

  9. Automated visual inspection of imprinted pharmaceutical tablets

    Science.gov (United States)

    Bukovec, Marko; Špiclin, Žiga; Pernuš, Franjo; Likar, Boštjan

    2007-09-01

    This paper is on automated visual inspection of tablets that may, in contrast to manual tablet sorting, provide objective and reproducible tablet quality assurance. Visual inspection of the ever-increasing numbers of produced imprinted tablets, regulatory enforced for unambiguous identification of active ingredients and dosage strength of each tablet, is especially demanding. The problem becomes more tractable by incorporating some a priori knowledge of the imprint shape and/or appearance. For this purpose, we consider two alternative automated tablet defect detection methods. The geometrical method, incorporating geometrical a priori knowledge of the imprint shape, enables specific inspection of the imprinted and non-imprinted tablet surface, while the statistical method exploits statistical a priori knowledge of tablet surface appearance, derived from a training image database. The two methods were evaluated on a large tablet image database, consisting of 3445 images of four types of imprinted tablets, with and without typical production defects. A 'gold standard' for testing the performances of the two inspection methods was established by manually classifying the tablets into good and five defective classes. The results, obtained by ROC (receiver operating characteristics) analysis, indicate that the statistical method yields better defect detection sensitivity and specificity than the geometrical method. Both presented image analysis methods are quite general and promising tools for automated visual inspection of imprinted pharmaceutical tablets.

  10. 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…

  11. 21 CFR 520.1310 - Marbofloxacin tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Marbofloxacin tablets. 520.1310 Section 520.1310... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1310 Marbofloxacin tablets. (a) Specifications. Each tablet contains 25, 50, 100, or 200 milligrams (mg) marbofloxacin....

  12. A Study on the Control of Pseudoephedrine Hydrochloride Release from Hydroxypropylmethylcellulose Matrices

    Energy Technology Data Exchange (ETDEWEB)

    Cho, H.; Chung, Y.S. [Department of Chemistry, Chungbuk National University, Cheongju (Korea); Bang, M.S. [Department of Industrial Chemistry, Chonan National Technical College, Chonnam (Korea)

    1999-04-01

    Hydroxypropylmethylcelluloses (HPMC) are cellulose ethers which may be used as the basis for hydrophilic matrices for controlled release oral delivery and offer the advantages of being non-toxic and relatively inexpensive. In this work, we designed new drug release system using HPMC as matrix, manufactured by direct compression technology and have investigated the effects of the controlling factors on drug release from a swellable hydrophillic delivery system. It was found that the release rate of the drug decreased with increasing the polymer molecular weight and the polymer content in tablets, and was independent of compaction pressure and pH of dissolution fluids. Especially, the ability of the anionic surfactant, sodium laurylsulfate, to retard the release of pseudoephedrine hydrochloride from HPMC was characterised. With increasing the concentration of the sodium laurylsulfate within the matrix, drug release rate decreased. It is believed that, provided the pseudoephedrine hydrochloride and the sodium laurylsulfate are oppositely charged, they will bind together in situ within the HPMC matrix, leading to reduced drug release rates. 23 refs., 7 figs.

  13. Simultaneous derivative spectrophotometric analysis of doxylamine succinate, pyridoxine hydrochloride and folic Acid in combined dosage forms.

    Science.gov (United States)

    Pathak, A; Rajput, S J

    2008-01-01

    Two UV spectrophotometric methods have been developed, based on first derivative spectrophotometry for simultaneous estimation of doxylamine succinate, pyridoxine hydrochloride, and folic acid in tablet formulations. In method I, the concentrations of these drugs were determined by using linear regression equation. Method II is also based on first derivative spectrophotometry however simultaneous equations (Vierdot's method) were derived on derivative spectra. The first derivative amplitudes at 270.0, 332.8 and 309.2 nm were utilized for simultaneous estimation of these drugs respectively by both methods. In both the methods, linearity was obtained in the concentration range 2.5-50 mug/ml, 1-40 mug/ml and 1-30 mug/ml for doxylamine succinate, pyridoxine hydrochloride, and folic acid respectively. The developed methods show best results in terms of linearity, accuracy, precision, LOD, LOQ and ruggedness for standard laboratory mixtures of pure drugs and marketed formulations. The common excipients and additives did not interfere in their determinations.

  14. Simultaneous derivative spectrophotometric analysis of doxylamine succinate, pyridoxine hydrochloride and folic acid in combined dosage forms

    Directory of Open Access Journals (Sweden)

    Pathak A

    2008-01-01

    Full Text Available Two UV spectrophotometric methods have been developed, based on first derivative spectrophotometry for simultaneous estimation of doxylamine succinate, pyridoxine hydrochloride, and folic acid in tablet formulations. In method I, the concentrations of these drugs were determined by using linear regression equation. Method II is also based on first derivative spectrophotometry however simultaneous equations (Vierdot′s method were derived on derivative spectra. The first derivative amplitudes at 270.0, 332.8 and 309.2 nm were utilized for simultaneous estimation of these drugs respectively by both methods. In both the methods, linearity was obtained in the concentration range 2.5-50 µg/ml, 1-40 µg/ml and 1-30 µg/ml for doxylamine succinate, pyridoxine hydrochloride, and folic acid respectively. The developed methods show best results in terms of linearity, accuracy, precision, LOD, LOQ and ruggedness for standard laboratory mixtures of pure drugs and marketed formulations. The common excipients and additives did not interfere in their determinations.

  15. Stability of piperacillin sodium-tazobactam sodium and ranitidine hydrochloride in 0.9% sodium chloride injection during simulated Y-site administration.

    Science.gov (United States)

    Choi, J S; Burm, J P; Jhee, S S; Chin, A; Ulrich, R W; Gill, M A

    1994-09-15

    The stability of piperacillin sodium plus tazobactam sodium and ranitidine hydrochloride in 0.9% sodium chloride injection during simulated Y-site administration was studied. Triplicate test solutions of piperacillin 40 mg/mL plus tazobactam 5 mg/mL (as the sodium salts) or piperacillin 80 mg/mL plus tazobactam 10 mg/mL (as the sodium salts) were mixed 1:1 with ranitidine 0.5 and 2.0 mg/mL (as the hydrochloride salt). The solutions were stored at 23 degrees C, and samples were removed at zero, one, two, and four hours for measurement of drug concentration by stability-indicating high-performance liquid chromatography. At the time of sampling and before any dilution, each sample was visually inspected for color and precipitation, and pH was determined. At all sampling times, the concentrations of piperacillin, tazobactam, and ranitidine were > 90% of initial concentrations. There were no substantial changes in pH or color. Tazobactam 5 mg/mL (as the sodium salt) and ranitidine 0.5 and 2 mg/mL (as the hydrochloride salt) in 0.9% sodium chloride injection were stable for up to four hours during simulated Y-site administration. Piperacillin 80 mg/mL plus tazobactam 10 mg/mL (as the sodium salts) and ranitidine 0.5 and 2 mg/mL (as the hydrochloride salt) were stable for up to four hours during simulated Y-site administration.

  16. Cartap hydrochloride poisoning: A clinical experience

    Directory of Open Access Journals (Sweden)

    Hari K Boorugu

    2012-01-01

    Full Text Available Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular toxicity resulting in respiratory failure. It is hypothesized that the primary effect of Cartap hydrochloride is through inhibition of the [ 3 H]-ryanodine binding to the Ca 2+ release channel in the sarcoplasmic reticulum in a dose-dependent manner and promotion of extracellular Ca 2+ influx and induction of internal Ca 2+ release. This results in tonic diaphragmatic contraction rather than paralysis. This is the basis of the clinical presentation of acute Cartap poisoning as well as the treatment with chelators namely British Anti Lewisite and sodium dimercaptopropane sulfonate.

  17. 21 CFR 556.350 - Levamisole hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride. 556.350 Section 556.350 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs...

  18. Cartap hydrochloride poisoning: A clinical experience.

    Science.gov (United States)

    Boorugu, Hari K; Chrispal, Anugrah

    2012-01-01

    Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular toxicity resulting in respiratory failure. It is hypothesized that the primary effect of Cartap hydrochloride is through inhibition of the [(3)H]-ryanodine binding to the Ca(2+) release channel in the sarcoplasmic reticulum in a dose-dependent manner and promotion of extracellular Ca(2+) influx and induction of internal Ca(2+) release. This results in tonic diaphragmatic contraction rather than paralysis. This is the basis of the clinical presentation of acute Cartap poisoning as well as the treatment with chelators namely British Anti Lewisite and sodium dimercaptopropane sulfonate.

  19. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food... chapter; meat products as defined in § 170.3(n)(29) of this chapter; milk products as defined in § 170.3(n)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this chapter; and...

  20. SOME CUNEIFORM TABLETS IN JERUSALEM

    Institute of Scientific and Technical Information of China (English)

    Wu; Yuhong

    2014-01-01

    <正>During the four and half months of my staying at the Albright Institute of Archaeological Research in Jerusalem and in the Hebrew University(01.12.2013–13.04.2014),I had the chance to read and study some unpublished cuneiform tablets.Here,I would like to make a small contribution to the work of publishing the precious information hidden in the cuneiform tablets from ancient Mesopotamia,and hope that some colleagues can give some improved reading to

  1. VALIDATION METHOD OF ULTRAVIOLET SPECTROPHOTOMETRY DETERMINATION OF CONTENT IN AMBROXOL HCl TABLET

    Directory of Open Access Journals (Sweden)

    Tedy Kurniawan Bakri

    2015-09-01

    Full Text Available Ambroxol Hydrochloride (Ambroxol HCI is one of mucolytic drugs that is commonly used to dilute thesecretion within the respiratory tract. This process is completed by lowering the viscosity of mucopolysaccharides, in which its characteristic which is mucolytic within the respiratory tract. This research aims to conduct a validation of the UV spectrophotometry method in determining the level of ambroxol HCI in tablets. This methos is also used to obtain the level of amboxol HCI in tablets that are available in the market. The parameters of the validation are accuracy, precision, limit of detection (LOD, and limit of qualification (LOQ. The samples of ambroxol HCI was consisted of one (1generic tablet and five (5 from branded tablets from the market. The results of the validation tested gave an accuracy of 99.58% in recovery percentage and Relative Standard Deviation (RSD of 1.14%. These results showed that this method gave good precision and exactness, with the limit of detection (LOD 0,1505 µg/ml andlimit of quantification (LOQ 0,5018 µg/ml. These numbers are obtained from tablets with brands namely Lapimuc® (PT. Lapi with its level of ambroxol HCI of 99,71 ± 0,64%; Epexol® (PT. Sanbe with levels of ambroxol HCI of 99,78 ± 0,52%; Mucera® (PT. Otto with levels of ambroxol HCI of 99,76 ± 0,5239%; Mucos® (PT. Meprofarm with levels of ambroxol HCI of 99,8 ± 0,75%; Mucopect® (PT. Boehringer Ingelheim with levels of ambroxol HCI of99,5 ± 0,70%; and finally a generic tablet with the of ambroxolHCl( PT. Phapros of 99,6 ± 0,59%. All tablets used within this research have conform to the general levels of amboxol HCI in a tablet which is not less than 90.0% and not more that 110% from the number written in the regulation.

  2. Maternal urinary iodine concentration up to 1.0 mg/L is positively associated with birth weight, length, and head circumference of male offspring.

    Science.gov (United States)

    Rydbeck, Filip; Rahman, Anisur; Grandér, Margaretha; Ekström, Eva-Charlotte; Vahter, Marie; Kippler, Maria

    2014-09-01

    Adequate iodine status in early life is crucial for neurodevelopment. However, little is known about the effects of maternal iodine status during pregnancy on fetal growth. The present study investigated the potential impact of maternal iodine status during pregnancy on offspring birth size. This large prospective cohort study was nested in a Bangladeshi population-based randomized supplementation trial in pregnant women [MINIMat (Maternal and Infant Nutrition Interventions in Matlab)]. Urine samples obtained at 8 wk of gestation from 1617 women were analyzed for iodine and other elements, such as arsenic and cadmium, using inductively coupled plasma mass spectrometry. Anthropometric measurements at birth included weight, length, and head and chest circumference. Maternal urinary iodine concentrations (UICs) ranged from 0.020 to 10 mg/L, with a median of 0.30 mg/L. Below ∼1.0 mg/L, UIC was significantly positively associated with birth weight and length. Birth weight and length increased by 9.3 g (95% CI: 2.9, 16) and 0.042 cm (95% CI: 0.0066, 0.076), respectively, for each 0.1-mg/L increase in maternal UIC. No associations were observed between UIC and head or chest circumference. When we stratified the analyses by newborn sex, the positive associations between maternal UIC (<1 mg/L) and measurements of size at birth were restricted to boys, with no evidence in girls. Among boys, the mean weight, length, and head circumference increased by 70 g (P = 0.019), 0.41 cm (P = 0.013), and 0.28 cm (P = 0.031) for every 0.5-mg/L increase in maternal UIC. Maternal iodine status was positively associated with weight, length, and head circumference in boys up to ∼1 mg/L, which is well above the recommended maximum concentration of 0.5 mg/L. The associations leveled off at UIC ≥ 1 mg/L. Our findings support previous conclusions that the advantages of correcting potential iodine deficiency outweigh the risks of excess exposure.

  3. 78 FR 40484 - Determination That METADATE ER (Methylphenidate Hydrochloride) Extended-Release Tablet, 10...

    Science.gov (United States)

    2013-07-05

    ... INFORMATION CONTACT: Reena Raman, Center for Drug Evaluation and Research, Food and Drug Administration, 10903... drug product to the ``Discontinued Drug Product List'' section of the Orange Book. Tedor Pharma...

  4. 21 CFR 520.1660c - Oxytetracycline hydrochloride tablets/boluses.

    Science.gov (United States)

    2010-04-01

    ... (shipping fever complex, pasteurellosis) caused by Pasteurella multocida. (2)(i) Amount. 500 milligrams per... Pasteurella multocida. (3) Limitations. Dosage should continue until the animal returns to normal and for 24... beef and dairy cattle—(1)(i) Amount. 250 milligrams per 100 pounds of body weight every 12 hours...

  5. [Splitting of tablets: small pieces a risk].

    Science.gov (United States)

    Picksak, Gesine; Stichtenoth, Dirk O

    2007-09-01

    For economic reasons physicians prescribe more and more multiunit tablets. Splitting of multiunit tablets depends on the physical-chemical properties of the agents, the galenic of the dosage form, the size and contour of the tablet and the shape of the score. Tablets with one or more scores are prepared to be divided for a single/multiple dose. How easily and exact a tablet can be divided depends heavily on the physical shape, its size and the outfit of the score. The fragments have to fulfil the requirements according to the European Pharmacopoeia: Uniformity of multiunit tablets. Since exact dosing is guaranteed only if tablets are divided properly, information and guidance of the patients by the physician and pharmacist is of critical importance.

  6. 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.

  7. Strong cation exchange resin for improving physicochemical properties and sustaining release of ranitidine hydrochloride

    Directory of Open Access Journals (Sweden)

    Khan S

    2007-01-01

    Full Text Available In the present study strong cation exchange resin (Amberlite IRP69 was used to improve the physicochemical properties of ranitidine hydrochloride such as taste and bulk properties and to sustain dissolution rate. Drug-resin complexes were prepared using batch method. Drug loading was done under different processing conditions such as temperature, pH, drug-resin ratio, and drug concentration to get the optimum condition for resinate preparation. Resinate prepared under optimized condition was tested for taste, bulk properties and release rate. Degree of bitterness of ranitidine was found to reduce to zero after complexation with resin. Improvement in flow properties was also observed. Angle of repose for resinate was found to be 33.21 o as compared to 42.27 o for ranitidine HCl. Effect of dissolution medium and particle size on in vitro release of drug from resinate was also investigated. Resinate with drug to resin ratio of 2:3 and particle size> 90 µm showed about 90% of drug release within 12 h. The orodispersible tablet formulated from the resinate containing 10% croscarmellose sodium disintegrated within 35 sec in oral cavity and showed similar dissolution profile as the resinate. Tablets were found stable after stability studies with no change in dissolution profile.

  8. Design and evaluation of osmotic pump-based controlled release system of Ambroxol Hydrochloride.

    Science.gov (United States)

    Cheng, Xiongkai; Sun, Min; Gao, Yan; Cao, Fengliang; Zhai, Guangxi

    2011-08-01

    The purpose of the present study was to design and evaluate an osmotic pump-based drug delivery system for controlling the release of Ambroxol Hydrochloride (Amb). Citric acid, lactose and polyethylene glycol 6000 (PEG 6000) were employed as osmotic agents. Surelease EC containing polyethylene glycol 400 (PEG 400) controlling the membrane porosity was used as semi-permeable membrane. The formulation of tablet core was optimized by orthogonal design and evaluated by weighted mark method. The influences of the amount of PEG 400 and membrane thickness on Amb release were investigated. The optimal osmotic pump tablet (OPT) was evaluated in different release media and at different stirring rates. The major release power confirmed was osmotic pressure. The release of Amb from OPT was verified at a rate of approximately zero-order, and cumulative release percentage at 12?h was 92.6%. The relative bioavailability of Amb OPT in rabbits relative to the commercial sustained capsule was 109.6%. Our results showed that Amb OPT could be a practical preparation with a good prospect.

  9. Lanthanum carbonate versus sevelamer hydrochloride: improvement of metabolic acidosis and hyperkalemia in hemodialysis patients.

    Science.gov (United States)

    Filiopoulos, Vassilis; Koutis, Ioannis; Trompouki, Sofia; Hadjiyannakos, Dimitrios; Lazarou, Dimitrios; Vlassopoulos, Dimosthenis

    2011-02-01

    Sevelamer hydrochloride (SH) has been reported to aggravate metabolic acidosis and hyperkalemia. This study was performed to evaluate acid-base status and serum potassium changes after replacing SH with lanthanum carbonate (LC) in hemodialysis patients. SH was prescribed for 24 weeks in 14 stable hemodialysis patients and replaced by LC in a similar treatment schedule. Laboratory tests, including indices of acid-base status, nutrition, bone/mineral metabolism, and dialysis adequacy, were performed monthly during the study. Dialysate bicarbonate, potassium and calcium concentrations remained constant. Serum bicarbonate and pH rose, and serum potassium dropped significantly under LC. Alkaline phosphatase also decreased significantly under LC. No significant differences were observed in the other studied parameters between the two treatment periods. Control of serum phosphate was similar under both phosphate-binders and no differences were observed in calcium, Ca × P product, CRP, or lipid levels. Dialysis adequacy was constantly kept within K/DOQI target-range. Although full compliance to treatment was reported, three patients on LC complained of gastrointestinal upset and/or a metallic taste, and four had difficulty chewing the LC tablet. LC improves metabolic acidosis and hyperkalemia in hemodialysis patients previously under SH. Although both medications are well-tolerated, the gastrointestinal side-effects appear to occur more frequently with LC; a fact that, together with difficulties in chewing the tablet, may result in decreased compliance.

  10. Optimization of a metformin effervescent floating tablet containing hydroxypropylmethylcellulose and stearic acid.

    Science.gov (United States)

    Rajab, M; Jouma, M; Neubert, R H; Dittgen, M

    2010-02-01

    This study optimizes the composition of an effervescent floating tablet (EFT) containing m