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Sample records for epirubicin hydrochloride mitomycin

  1. Prospective Evaluation of Transcatheter Arterial Chemoembolization (TACE) with Multiple Anti-Cancer Drugs (Epirubicin, Cisplatin, Mitomycin C, 5-Fluorouracil) Compared with TACE with Epirubicin for Treatment of Hepatocellular Carcinoma

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    Sahara, Shinya; Kawai, Nobuyuki; Sato, Morio, E-mail: morisato@mail.wakayama-med.ac.jp; Tanaka, Takami; Ikoma, Akira; Nakata, Kouhei; Sanda, Hiroki; Minamiguchi, Hiroki; Nakai, Motoki; Shirai, Shintaro; Sonomura, Tetsuo [Wakayama Medical University, Department of Radiology (Japan)

    2012-12-15

    Purpose: To compare the efficacy of transcatheter arterial chemoembolization (TACE) using multiple anticancer drugs (epirubicin, cisplatin, mitomycin C, and 5-furuorouracil: Multi group) with TACE using epirubicin (EP group) for hepatocellular carcinoma (HCC). Materials and Methods: The study design was a single-center, prospective, randomized controlled trial. Patients with unrespectable HCC confined to the liver, unsuitable for radiofrequency ablation, were assigned to the Multi group or the EP group. We assessed radiographic response as the primary endpoint; secondary endpoints were progression-free survival (PFS), safety, and hepatic branch artery abnormality (Grade I, no damage or mild vessel wall irregularity; Grade II, overt stenosis; Grade III, occlusion; Grades II and III indicated significant hepatic artery damage). A total of 51 patients were enrolled: 24 in the Multi group vs. 27 in the EP group. Results: No significant difference in HCC patient background was found between the groups. Radiographic response, PFS, and 1- and 2-year overall survival of the Multi vs. EP group were 54% vs. 48%, 6.1 months vs. 8.7 months, and 95% and 65% vs. 85% and 76%, respectively, with no significant difference. Significantly greater Grade 3 transaminase elevation was found in the Multi group (p = 0.023). Hepatic artery abnormality was observed in 34% of the Multi group and in 17.1% of the EP group (p = 0.019). Conclusion: TACE with multiple anti-cancer drugs was tolerable but appeared not to contribute to an increase in radiographic response or PFS, and caused significantly more hepatic arterial abnormalities compared with TACE with epirubicin alone.

  2. Prevention of venous pain and phlebitis caused by epirubicin hydrochloride.

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    Sugimoto, Masakazu; Matsui, Masateru; Harada, Masanori; Yamauchi, Yumiko; Moriyama, Nao; Andou, Kanae; Yamamoto, Makoto; Yamaoka, Hisayo; Ono, Chiemi; Ishikawa, Mami; Kamo, Nobuyuki; Ikeda, Tadashi; Yamaoka, Keiko

    2009-06-01

    Many patients complain of venous pain or develop phlebitis following treatment with epirubicin hydrochloride(EPI). To ensure effective and safe treatment with this drug, it is essential to deal with the adverse events associated with it appropriately. At our hospital, EPI was previously administered by drip infusion(diluted with 50mL of physiological saline)over 15 minutes after pretreatment(EPI main route). With this method of treatment, venous pain and phlebitis developed in 14 of 15 cases. In 3 of these 14 cases, the regimen was modified. Following this experience, EPI administration was switched to drip infusion from the fully-opened side tube used for pretreatment(EPI sub-route). Switching to this route resulted in a sharp decrease in the incidence of venous pain and phlebitis, to only 1 of 15 cases. Stimulation of vascular tunica intima by EPI has been considered a factor principally responsible for the venous pain and phlebitis seen after EPI therapy. To prevent these adverse reactions, it is necessary to modify the method of administration so that strong or long-term exposure of blood vessels to EPI can be reduced. The results of this study suggest that the EPI sub-route we devised is useful in achieving this goal.

  3. An Attempt to Shorten Loading Time of Epirubicin into DC Beads® Using Vibration and a Sieve

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    Sonoda, Akinaga; Nitta, Norihisa; Yamamoto, Takefumi; Tomozawa, Yuki; Ohta, Shinichi; Watanabe, Shobu; Murata, Kiyoshi

    2017-01-01

    PurposeWe investigated the possibility of shortening the time required for loading epirubicin into calibrated polyvinyl alcohol-based hydrogel beads (DC Beads ® ) to be used for transarterial chemoembolization.MethodAfter separating the beads suspended in phosphate-buffered saline (PBS) solution by the use of a sieve (clearance 75 µm), epirubicin hydrochloride (EH) was loaded for 20, 30, or 60 s under vibration into DC beads. The EH loading rate into conventionally prepared (control) beads, i.e., beads loaded for 30 min without vibration, and vibration-loaded beads were calculated from the residual EH concentration in the bead-depleted EH solution. The amount of EH eluted from conventionally and vibration-loaded samples into a PBS solution (pH 7.0) was measured at 15 and 30 min and 1, 2, 6, 12, and 24 h. We also recorded the inhibitory effect of the PBS solution on the loading time. Using frozen sections, the EH load in the beads was evaluated visually under a fluorescence microscope.ResultsSpectrophotometry (495 nm) showed that the loading rate was 98.98 ± 0.34, 99.02 ± 0.32, and 99.50 ± 0.11 % with 20-, 30-, and 60-s vibration, respectively. The eluted rate was statistically similar between vibration- and statically loaded (control) beads. The PBS solution hampered EH loading into the beads. Visually, the distribution of EH in conventionally and vibration-loaded DC beads was similar.DiscussionThe use of vibration and the removal of PBS solution when epirubicin hydrochloride was loaded into DC beads dramatically shortened the loading time of epirubicin hydrochloride into DC beads.

  4. An Attempt to Shorten Loading Time of Epirubicin into DC Beads{sup ®} Using Vibration and a Sieve

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    Sonoda, Akinaga, E-mail: akinagasonoda@yahoo.co.jp; Nitta, Norihisa [Shiga University of Medical Science, Department of Radiology (Japan); Yamamoto, Takefumi [Shiga University of Medical Science, Central Research Laboratory (Japan); Tomozawa, Yuki; Ohta, Shinichi; Watanabe, Shobu; Murata, Kiyoshi [Shiga University of Medical Science, Department of Radiology (Japan)

    2017-04-15

    PurposeWe investigated the possibility of shortening the time required for loading epirubicin into calibrated polyvinyl alcohol-based hydrogel beads (DC Beads{sup ®}) to be used for transarterial chemoembolization.MethodAfter separating the beads suspended in phosphate-buffered saline (PBS) solution by the use of a sieve (clearance 75 µm), epirubicin hydrochloride (EH) was loaded for 20, 30, or 60 s under vibration into DC beads. The EH loading rate into conventionally prepared (control) beads, i.e., beads loaded for 30 min without vibration, and vibration-loaded beads were calculated from the residual EH concentration in the bead-depleted EH solution. The amount of EH eluted from conventionally and vibration-loaded samples into a PBS solution (pH 7.0) was measured at 15 and 30 min and 1, 2, 6, 12, and 24 h. We also recorded the inhibitory effect of the PBS solution on the loading time. Using frozen sections, the EH load in the beads was evaluated visually under a fluorescence microscope.ResultsSpectrophotometry (495 nm) showed that the loading rate was 98.98 ± 0.34, 99.02 ± 0.32, and 99.50 ± 0.11 % with 20-, 30-, and 60-s vibration, respectively. The eluted rate was statistically similar between vibration- and statically loaded (control) beads. The PBS solution hampered EH loading into the beads. Visually, the distribution of EH in conventionally and vibration-loaded DC beads was similar.DiscussionThe use of vibration and the removal of PBS solution when epirubicin hydrochloride was loaded into DC beads dramatically shortened the loading time of epirubicin hydrochloride into DC beads.

  5. [Promising new injection method to prevent angialgia/phlebitis from epirubicin hydrochloride therapy for breast cancer].

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    Ono, Chiemi; Yamagami, Mitsue; Kamatani, Rika; Yamamoto, Makoto; Mukouyama, Tomoya; Sugimoto, Masakazu; Suzuki, Taizan; Kamo, Nobuyuki; Seki, Nobuhiko; Eguchi, Kenji; Ikeda, Tadashi

    2012-05-01

    Epirubicin hydrochloride(EPI)is well known to cause phlebitis as a typical adverse drug reaction. By preventing the development of severe phlebitis, patients are expected to continue effective chemotherapy with EPI without a decrease in QOL. We have previously reported promising results of a new injection method to prevent phlebitis from occurring during EPI therapy thorough a prospective clinical trial in our hospital(Jpn J Cancer Chemother 36: 969-974, 2009). In the present study, we have compared the conventional injection method(EPI main -route method, n=15)with our new method, which has been consistently practiced at present(EPI sub -route method, n=77). We found that in the EPI main -route method, angialgia/phlebitis developed in 14 of 15 cases(Grade 3, 53. 3%), leading to alteration of the regimen in 3 cases. On the other hand, with the EPI sub -route method, incidence of angialgia/phlebitis was markedly decreased, and only 6 of 77 cases developed these adverse reactions(Grade 3, 0%). One possible explanation for these results is that the reduction of intimal stimulation by the EPI sub -route method might be caused by the dilution and washout of EPI with pre-medication, as well as the shortened infusion times of EPI. Therefore, on the basis of the above hypothesis, we conclude that the EPI sub-route method might be a more effective treatment for the expected prevention of angialgia/phlebitis.

  6. A Hydrogel-Based Epirubicin Delivery System for Intravesical Chemotherapy

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    Ching-Wen Liu

    2016-06-01

    Full Text Available This study aimed to examine the efficacy of epirubicin-loaded gelatin hydrogel (EPI-H in the treatment of superficial urothelium carcinoma. Hydrogel was prepared by Schiff base-crosslinking of gelatin with glutaraldehyde. EPI-H exhibited high entrapment efficiency (59.87% ± 0.51%. EPI-H also increased epirubicin accumulation in AY-27 cells when compared with the effect of aqueous solutions of epirubicin (EPI-AQ; respective epirubicin-positive cell counts were 69.0% ± 7.6% and 38.3% ± 5.8%. EPI-H also exhibited greater cytotoxicity against AY-27 cells than that of EPI-AQ; IC50 values were 13.1 ± 1.1 and 7.5 ± 0.3 μg/mL, respectively. Cystometrograms showed that EPI-H reduced peak micturition, threshold pressures, and micturition duration, and that it increased bladder compliance more so than EPI-AQ. EPI-H enhanced epirubicin penetration into basal cells of urothelium in vivo, whereas EPI-AQ did so only to the umbrella cells. EPI-H inhibited tumor growth upon intravesical instillation to tumor-bearing bladder of F344 rats, inducing higher levels of caspase-3 expression than that observed with EPI-AQ treatment; the number of caspase-3 positive cells in treated urothelium carcinoma was 13.9% ± 4.0% (EPI-AQ and 34.1% ± 1.0%, (EPI-H. EPI-H has value as an improved means to administer epirubicin in intravesical instillation treatments for bladder cancer.

  7. Compatibility of epirubicin-loaded DC bead™ with different non-ionic contrast media.

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    Sarakbi, Iman; Krämer, Irene

    2016-12-01

    The aim of this study was to determine the compatibility of epirubicin-loaded DC bead™ with different non-ionic contrast media over a period of seven days when stored light protected under refrigerated conditions. DC bead™ (2 ml) (Biocompatibles UK Ltd) of the bead size 70-150 µm ( = DC bead M1) or bead size 100-300 µm were loaded with 75 mg epirubicin powder formulation (Farmorubicin® dissolved in 3 ml water for injection to a concentration of 25 mg/ml) or 76 mg epirubicin injection solution (Epimedac® 2 mg/ml) within 2 h or 6 h, respectively. After removal of the excess solution, the epirubicin-loaded beads were mixed in polypropylene syringes with an equal volume (∼1.5 ml) of contrast media, i.e. Accupaque™ 300 (Nycomed Inc.), Imeron® 300 (Bracco S.p.A), Ultravist® 300 (Bayer Pharma AG), Visipaque™ 320 (GE Healthcare) and agitated in a controlled manner to get a homogenous suspension. Syringes with loaded beads in contrast media were stored protected from light under refrigeration (2-8℃). Compatibility was determined by measuring epirubicin concentrations in the suspensions in triplicate on day 0, 1, and 7. A reversed phase high-performance liquid chromatography assay with ultraviolet detection was utilized to analyze the concentration and purity of epirubicin. Mixing of epirubicin-loaded beads with different non-ionic contrast media released 0.1-0.5% of epirubicin over a period of 24 h, irrespectively, of the DC bead™ size or type of contrast media. No further elution or degradation was observed after seven days when the admixtures were stored protected from light under refrigeration. Compatibility of epirubicin-loaded DC bead™ with an equal volume of different contrast media in polypropylene syringes is given over a period of seven days. Due to a maximum elution of 0.1-0.5% of epirubicin from loaded DC bead™, admixtures with contrast media can be prepared in advance in centralized cytotoxic preparation units

  8. Risk factors for the leakage of chemotherapeutic agents into systemic circulation after transcatheter arterial chemoembolization of hepatocellular carcinoma

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    Ming-Yen Hsieh

    2011-10-01

    Full Text Available This prospective study was to investigate the possible risk factors for the leakage of chemotherapeutic agent into the systemic circulation after transcatheter arterial chemoembolization (TACE of hepatocellular carcinoma (HCC. Peripheral plasma concentrations of chemotherapeutic agents were determined at 1 hour and 72 hours after TACE by high-performance liquid chromatography in 53 patients. HCC were divided into three types namely single nodule (<5 cm, multiple nodules (all <5 cm, and main nodule measuring 5 cm or more. Forty-four patients (83% showed detectable chemotherapeutic concentrations within 72 hours after TACE. Patients with single nodular-type HCC had lower incidence of detectable plasma chemotherapeutic agents after TACE than the other two groups (all p<0.05. The injected doses of lipiodol, epirubicin, and mitomycin C were lower in patients without detection than in patients with detectable chemotherapeutic agents (all p<0.05. Multivariate logistic regression showed that tumor type and injected dose of lipiodol were two independent risk factors for the leakage of mitomycin C at 1 hour after TACE (all p<0.05, and the injected dose of mitomycin C was the risk factor for the leakage of epirubicin at 1 hour after TACE (p<0.05. In conclusion, multiple nodular type and large nodule measuring 5 cm or more have a risk of leakage of mitomycin C after TACE. Injected dose of lipiodol and mitomycin C as risk factor for the leakage of mitomycin C and epirubicin respectively may be because of competition of their injected volume within the limited space of target.

  9. [Improvement of epirubicin-induced phlebitis to switch from liquid preparation to lyophilized formulation].

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    Suga, Yukio; Kumazaki, Masafumi; Nishigami, Jun; Takeda, Kazuyoshi; Kawagishi, Atsufumi; Ishizaki, Junko; Inokuchi, Masafumi; Miyamoto, Ken-Ichi; Arai, Kunizo

    2009-01-01

    Adjuvant chemotherapy containing epirubicin is commonly used to treat patients with pre- or post-operative breast cancer. It is known that the epirubicin(FarmorubicinRTU)preparation often caused phlebitis, whereas dexamethasone has been used to prevent that reaction. We examined whether the lyophilized formulation of epirubicin(Farmorubicin)can reduces the incidence of phlebitis compared with the preparation. All infusions were administered through a peripheral vein. Adverse drug reaction including phlebitis was evaluated after each infusion and at the subsequent visit to four or six cycles. Sixty-two patients were given the preparation and 35 the lyophilized formulation. Epirubicininduced phlebitis was observed in 45.7% of patients given the preparation and in 48.4% of those given the lyophilized formulation. There was no statistically significant difference between the two groups(p=0.41). However, the incidence of severe phlebitis requiring treatment with steroid ointment was significantly increased among patients treated with the preparation(27.4% vs 9.7%, pphlebitis between the two groups. In this study, lyophilized formulations of epirubicin significantly reduced the incidence of severe phlebitis compared with that among patients receiving the preparation. Using lyophilized formulations of epirubicin should be considered to prevent a reduction in QOL with epirubicin-induced phlebitis in patients with breast cancer.

  10. Can the epirubicin cardiotoxicity in cancer patients be prevented by angiotensin converting enzyme inhibitors?

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    Radulescu, D; Buzdugan, E; Ciuleanu, T E; Todor, N; Stoicescu, L

    2013-01-01

    The aim of this study was to assess whether treatment with angiotensin converting enzyme inhibitors (ACEI) can prevent the alteration of left ventricular systolic and diastolic performance in cancer patients treated with different chemotherapy regimens containing epirubicin. In this prospective study , 68 patients with different malignant tumors treated with epirubicin and perindopril in different chemotherapy protocols (study group), and a gender- and age-matched group of 68 patients with different malignant tumors treated with epirubicin without perindopril in different chemotherapy protocols (control group), were assessed by Doppler echocardiography. Left ventricular systolic function was assessed by measuring left ventricular ejection fraction (EF). Left ventricular diastolic function was assessed by Doppler ultrasound by evaluating the transmitral flow. We also assessed the QTc on the 12 lead electrocardiograms. At the end of chemotherapy the left ventricular systolic function was less altered in the study group compared to the control group and was superior in the study group (epirubicin+ACEI) compared to the control group (epirubicin alone). We documented a significantly deteriorated left ventricular diastolic function in both groups at the completion of chemotherapy. QTc time in both arms was also significantly prolonged. In the present echo-Doppler study we documented a preserved left ventricular systolic performance in patients with various malignancies treated with epirubicin plus perindopril. Although co-treatment with ACEI prevented the alteration of systolic performance, it failed to prevent the deterioration of the left ventricular diastolic performance impairment due to poor left ventricular compliance.

  11. Long-term heart function after adjuvant epirubicin chemotherapy for breast cancer

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    Appel, Jon M; Zerahn, Bo; Møller, Susanne

    2012-01-01

    Newer studies raise concern that adjuvant anthracycline treatment for breast cancer (BC) causes long-term heart damage. We aimed to examine whether heart failure or impairment could be demonstrated several years after low-dose epirubicin-based adjuvant treatment.......Newer studies raise concern that adjuvant anthracycline treatment for breast cancer (BC) causes long-term heart damage. We aimed to examine whether heart failure or impairment could be demonstrated several years after low-dose epirubicin-based adjuvant treatment....

  12. Structural characterization of the mitomycin 7-O-methyltransferase

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    Singh, Shanteri; Chang, Aram; Goff, Randal D.; Bingman, Craig A.; Grüschow, Sabine; Sherman, David H.; Phillips, Jr., George N.; Thorson, Jon S. (Michigan); (UW)

    2014-10-02

    Mitomycins are quinone-containing antibiotics, widely used as antitumor drugs in chemotherapy. Mitomycin-7-O-methyltransferase (MmcR), a key tailoring enzyme involved in the biosynthesis of mitomycin in Streptomyces lavendulae, catalyzes the 7-O-methylation of both C9{beta}- and C9{alpha}-configured 7-hydroxymitomycins. We have determined the crystal structures of the MmcR-S-adenosylhomocysteine (SAH) binary complex and MmcR-SAH-mitomycin A (MMA) ternary complex at resolutions of 1.9 and 2.3 {angstrom}, respectively. The study revealed MmcR to adopt a common S-adenosyl-L-methionine-dependent O-methyltransferase fold and the presence of a structurally conserved active site general acid-base pair is consistent with a proton-assisted methyltransfer common to most methyltransferases. Given the importance of C7 alkylation to modulate mitomycin redox potential, this study may also present a template toward the future engineering of catalysts to generate uniquely bioactive mitomycins.

  13. Co-encapsulation of chrysophsin-1 and epirubicin in PEGylated liposomes circumvents multidrug resistance in HeLa cells.

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    Lo, Yu-Li; Tu, Wei-Chen

    2015-12-05

    Chrysophsin-1, an amphipathic alpha-helical antimicrobial peptide, is isolated from the gills of the red sea bream and possesses different structure and mechanism(s) in comparison with traditional multidrug resistance (MDR) modulators. For the purpose of reducing off-target normal cell toxicity, it is rational to incorporate chrysophsin-1 and epirubicin in a PEGylated liposomal formulation. In the present study, we report a multifunctional liposomes with epirubicin as an antineoplastic agent and an apoptosis inducer, as well as chrysophsin-1 as a MDR transporter inhibitor and an apoptosis modulator in human cervical cancer HeLa cells. Co-incubation of HeLa cells with PEGylated liposomal formulation of epirubicin and chrysophsin-1 resulted in a significant increase in the cytotoxicity of epirubicin. The liposomal formulations of epirubicin and/or chrysophsin-1 were shown to considerably improve the intracellular H2O2 and O2(-) levels of HeLa cells. Furthermore, these treatments were found to extensively reduce mRNA expression levels of MDR1, MRP1, and MRP2. The addition of chrysophsin-1 in liposomes was demonstrated to substantially enhance the intracellular accumulation of epirubicin in HeLa cells. Moreover, the PEGylated liposomes of epirubicin and chrysophsin-1 were also found to significantly increase the mRNA expressions of p53, Bax, and Bcl-2. The ratio of Bax to Bcl-2 was noticeably amplified in the presence of these formulations. Apoptosis induction was also validated by chromatin condensation, a reduction in mitochondrial membrane potential, the increased sub-G1 phase of cell cycle, and more populations of apoptosis using annexin V/PI assay. These formulations were verified to increase the activity and mRNA expression levels of caspase-9 and caspases-3. Collectively, our findings provide the first evidence that cotreatment with free or liposomal chrysophsin-1 and epirubicin leads to cell death in human cervical cancer cells through the ROS

  14. Influence of Alternative Tubulin Inhibitors on the Potency of a Epirubicin-Immunochemotherapeutic Synthesized with an Ultra Violet Light-Activated Intermediate: Influence of incorporating an internal/integral disulfide bond structure and Alternative Tubulin/Microtubule Inhibitors on the Cytotoxic Anti-Neoplastic Potency of Epirubicin-(C3-amide)-Anti-HER2/neu Synthesized Utilizing a UV-Photoactivated Anthracycline Intermediate.

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    Coyne, C P; Jones, Toni; Bear, Ryan

    2012-11-01

    Immunochemotherapeutics, epirubicin-(C 3 - amide )-SS-[anti-HER2/ neu ] with an internal disulfide bond, and epirubicin-(C 3 - amide )-[anti-HER2/ neu ] were synthesized utilizing succinimidyl 2-[(4,4'-azipentanamido) ethyl]-1,3'-dithioproprionate or succinimidyl 4,4-azipentanoate respectively. Western blot analysis was used to determine the presence of any immunoglobulin fragmentation or IgG-IgG polymerization. Retained HER2/ neu binding characteristics of epirubicin-(C 3 - amide )-[anti-HER2/ neu ] and epirubicin-(C 3 - amide )-SS-[anti-HER2/ neu ] were validated by cell-ELISA using a mammary adenocarcinoma (SKBr-3) population that highly over-expresses trophic HER2/ neu receptor complexes. Cytotoxic anti-neoplastic potency of epirubicin-(C 3 - amide )-[anti-HER2/ neu ] and epirubicin-(C 3 - amide )-SS-[anti-HER2/ neu ] between epirubicin-equivalent concentrations of 10 -10 M and 10 -6 M was determined by measuring the vitality/proliferation of chemotherapeutic-resistant mammary adenocarcinoma (SKBr-3 cell type). Cytotoxic anti-neoplastic potency of benzimidazoles (albendazole, flubendazole, membendazole) and griseofulvin were assessed between 0-to-2 μg/ml and 0-to-100 μg/ml respectively while mebendazole and griseofulvin were analyzed at fixed concentrations of 0.35 μg/ml and 35 g/ml respectively in dual combination with gradient concentrations of epirubicin-(C 3 - amide )-[anti-HER2/ neu ] and epirubicin-(C 3 - amide )-SS-[anti-HER2/ neu ]. Cytotoxic anti-neoplastic potency for epirubicin-(C 3 - amide )-[anti-HER2/ neu ] and epirubicin-(C 3 - amide )-SS-[anti-HER2/ neu ] against chemotherapeutic-resistant mammary adenocarcinoma (SKBr-3) was nearly identical at epirubicin-equivalent concentrations of 10 -10 M and 10 -6 M. The benzimadazoles also possessed cytotoxic anti-neoplastic activity with flubendazole and albendazole being the most and least potent respectively. Similarly, griseofulvin had cytotoxic anti-neoplastic activity and was more potent than

  15. Epirubicin, oxaliplatin, and capectabine is just as "MAGIC"al as epirubicin, cisplatin, and fluorouracil perioperative chemotherapy for resectable locally advanced gastro-oesophageal cancer

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    Bhawna Sirohi

    2014-01-01

    Full Text Available Background: The perioperative use of epirubicin, cisplatin, and fluorouracil (ECF significantly improves outcomes in patients with gastric and gastro-oesophageal (GO cancers but is cumbersome to administer. Given the equivalence of epirubicin, oxaliplatin, and capectabine (EOX with ECF in advanced setting, we analyzed the compliance, efficacy, and toxicity of perioperative EOX in resectable but locally advanced cancers. Methods: This is a retrospective analysis of prospectively maintained database of patients treated between January 2012 and September 2013 at Tata Memorial Centre. Patients were planned to receive 3# of neoadjuvant (NA and 3# of adjuvant EOX (intravenous epirubicin 50 mg/m 2 D1, oxaliplatin 130 mg/m 2 , on D1, capecitabiine 1250 mg/m 2 D1-21 every 21 days. On completion of NA therapy, patients were planned to undergo gastrectomy and D2 lymphadenectomy. Results: A total of 99 patients (76% males, median age 51 years were treated with perioperative EOX. Preoperatively, 93% patients completed EOX. Post-NA chemotherapy, 4 patients progressed, 1 patient died and 94 were taken up for surgery. Of these, 9 were inoperable and 85 patients underwent radical surgery. Of these, 71% (60/85 were able to complete three cycles of adjuvant EOX. The compliance to complete all 6 cycles of perioperative chemotherapy was 64%. Grade 3 and 4 toxicities were comparable to the MAGIC dataset apart from higher number of diarrhea in our patients. Conclusions: In patients with resectable GO adenocarcinoma, it is possible to deliver the MAGIC-type perioperative chemotherapy with EOX with better compliance, toxicity, and efficacy rates.

  16. Application of multifunctional targeting epirubicin liposomes in the treatment of non-small-cell lung cancer

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    Song X

    2017-10-01

    Full Text Available Xiao-li Song,1 Rui-jun Ju,2 Yao Xiao,1 Xin Wang,1 Shuang Liu,1 Min Fu,1 Jing-jing Liu,1 Li-yan Gu,1 Xue-tao Li,1 Lan Cheng1 1School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian, 2Department of Pharmaceutical Engineering, Beijing Institute of Petrochemical Technology, Beijing, China Abstract: Chemotherapy for aggressive non-small-cell lung cancer (NSCLC usually results in a poor prognosis due to tumor metastasis, vasculogenic mimicry (VM channels, limited killing of tumor cells, and severe systemic toxicity. Herein, we developed a kind of multifunctional targeting epirubicin liposomes to enhance antitumor efficacy for NSCLC. In the liposomes, octreotide was modified on liposomal surface for obtaining a receptor-mediated targeting effect, and honokiol was incorporated into the lipid bilayer for inhibiting tumor metastasis and eliminating VM channels. In vitro cellular assays showed that multifunctional targeting epirubicin liposomes not only exhibited the strongest cytotoxic effect on Lewis lung tumor cells but also showed the most efficient inhibition on VM channels. Action mechanism studies showed that multifunctional targeting epirubicin liposomes could downregulate PI3K, MMP-2, MMP-9, VE-Cadherin, and FAK and activate apoptotic enzyme caspase 3. In vivo results exhibited that multifunctional targeting epirubicin liposomes could accumulate selectively in tumor site and display an obvious antitumor efficacy. In addition, no significant toxicity of blood system and major organs was observed at a test dose. Therefore, multifunctional targeting epirubicin liposomes may provide a safe and efficient therapy strategy for NSCLC. Keywords: octreotide, honokiol, chemotherapy, vasculogenic mimicry, tumor metastasis, targeting drug delivery

  17. Epirubicin-adsorbed nanodiamonds kill chemoresistant hepatic cancer stem cells.

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    Wang, Xin; Low, Xinyi Casuarine; Hou, Weixin; Abdullah, Lissa Nurrul; Toh, Tan Boon; Mohd Abdul Rashid, Masturah; Ho, Dean; Chow, Edward Kai-Hua

    2014-12-23

    Chemoresistance is a primary cause of treatment failure in cancer and a common property of tumor-initiating cancer stem cells. Overcoming mechanisms of chemoresistance, particularly in cancer stem cells, can markedly enhance cancer therapy and prevent recurrence and metastasis. This study demonstrates that the delivery of Epirubicin by nanodiamonds is a highly effective nanomedicine-based approach to overcoming chemoresistance in hepatic cancer stem cells. The potent physical adsorption of Epirubicin to nanodiamonds creates a rapidly synthesized and stable nanodiamond-drug complex that promotes endocytic uptake and enhanced tumor cell retention. These attributes mediate the effective killing of both cancer stem cells and noncancer stem cells in vitro and in vivo. Enhanced treatment of both tumor cell populations results in an improved impairment of secondary tumor formation in vivo compared with treatment by unmodified chemotherapeutics. On the basis of these results, nanodiamond-mediated drug delivery may serve as a powerful method for overcoming chemoresistance in cancer stem cells and markedly improving overall treatment against hepatic cancers.

  18. A MONOCLONAL ANTIBODY-BETA-GLUCURONIDASE CONJUGATE AS ACTIVATOR OF THE PRODRUG EPIRUBICIN-GLUCURONIDE FOR SPECIFIC TREATMENT OF CANCER

    NARCIS (Netherlands)

    Haisma, Hidde; BOVEN, E; VANMUIJEN, M; DEJONG, J; VANDERVIJGH, WJF; PINEDO, HM

    The anti-pan carcinoma monoclonal antibody (MAb) 323/A3, linked to E. coli-derived beta-glucuronidase (GUS) was used to study the tumour-site-selective activation of the prodrug Epirubicin-glucuronide (Epi-glu). Epi-glu was isolated from the urine of patients treated with Epirubicin (Epi) by

  19. Dacryocystorhinostomy without intubation with intraoperative mitomycin-c

    International Nuclear Information System (INIS)

    Rahman, A.; Channa, S.; Memon, M.S.; Niazi, J.H.

    2006-01-01

    To evaluate the success rate and complications of intraoperative Mitomycin-C in dacryocystorhinostomy surgery. This study included total 90 eyes of 90 patients fulfilling the inclusion criteria.The surgical procedure of external DCR done with intraoperative Mitomycin-C with a neurosurgical cottonoid soaked with 0.2mg/ml. Mitomycin C was applied to the anastomosed flaps and osteotomy site for 10 minutes, without Silicon tube intubation. Surgery was done under local as well as general anesthesia. Patients were followed for 6 months. Out of 90 patients included in this study, only 2 patients complained of persistent epiphora after 6 months follow-up and were labeled as failed DCR. Remaining 88 had either no tearing or significant improvement of tearing after 6 months follow up and patent lacrimal system by syringing without pressure. Success rate in this procedure was 97.77% (p-value< 0.001). This study showed very high rate of success. Only complication noted was excessive nasal bleeding which was easily controlled. Intraoperative Mitomycin-C application in external DCR is safe, effective, cheap adjunct that helps to achieve good results of DCR surgery. (author)

  20. Teratogenic interactions between methylmercury and mitomycin-C in mice

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    Inouye, Minoru; Kajiwara, Yuji

    1988-01-01

    Pregnant mice were given p.o. various nonteratogenic doses (0, 2.5 and 10 mg/kg) of methylmercuric chloride on day 9 of pregnancy, and then injected i.p. with a teratogenic dose (4 mg/kg) of mitomycin-C on day 10. Major malformations produced by mitomycin-C alone were cervical rib and vertebral anomaly, polydactyly of the hindlimb and tail anomaly. Combined treatment significantly increased the incidence of these malformations, showing the dose-effect relationship of methylmercury, whereas methylmercury alone is known not to produce such malformations. When mitomycin-C treatment alone was performed on day 9.5 of pregnancy, only vertebral anomalies increased in incidence. Therefore, mitomycin-C teratogenicity in terms of the manifestation of cervical rib, polydactyly and tail anomaly, but not vertebral anomaly, was suggested to be enhanced by methylmercury. A considerable number of foetuses showed cleft palate involvement following combined treatments, but not by either chemical alone. Cleft palate is known to be a major malformation in mice that is caused by methylmercury, and mitomycin-C also induces cleft palate. Therefore, the two chemicals might have affected foetuses additively and thereby induced cleft palate. (orig.)

  1. Effect of transarterial chemoembolization with miriplatin plus epirubicin on local control of hepatocellular carcinoma: a retrospective comparison with miriplatin monotherapy

    Directory of Open Access Journals (Sweden)

    Hashimoto N

    2013-08-01

    Full Text Available Naoko Hashimoto,1 Jin Iwazawa,1 Shoichi Ohue,2 Takashi Mitani11Department of Radiology, Nissay Hospital, Nishiku, Osaka, Japan; 2Department of Radiology, Komatsu Hospital, Neyagawa, JapanObjective: We aimed to evaluate local tumor control after transarterial chemoembolization (TACE for hepatocellular carcinoma using miriplatin and low-dose epirubicin combination therapy.Methods: We retrospectively analyzed the records of patients who underwent TACE using miriplatin plus low-dose epirubicin (30 patients, 61 nodules, August 2011–March 2012 and control patients who underwent TACE using miriplatin alone (36 patients, 70 nodules, June 2010–July 2011. The local control rate was compared between the two groups using the Kaplan–Meier estimator and the log-rank test. Factors affecting local tumor recurrence were analyzed using multivariate logistic regression analysis. Treatment-related toxicity was evaluated using the Common Terminology Criteria for Adverse Events.Results: The local control rates at 6 months and 1 year were 87% and 65% for the miriplatin plus low-dose epirubicin group, and 61% and 43% for the miriplatin group, respectively. Local tumor control rates were significantly better in the miriplatin plus low-dose epirubicin group than in the miriplatin group (P = 0.038. Multivariate analysis showed that the addition of epirubicin was an independent factor associated with better local tumor control (hazard ratio 0.2, P = 0.001. Overall incidence rates for adverse events were not significantly different between the two groups.Conclusion: Additional usage of low-dose epirubicin for TACE using miriplatin improved local tumor control of hepatocellular carcinoma with adverse effects comparable to those observed with TACE using miriplatin alone.Keywords: combination therapy, local recurrence, liver, embolization, comparative study

  2. Repair system and mitomycin mutagenesis in Escherichia coli

    Energy Technology Data Exchange (ETDEWEB)

    Otsuji, N; Murayama, I [Kyushu Univ., Fukuoka (Japan). Faculty of Pharmaceutical Sciences

    1974-03-01

    Ultraviolet light sensitive mutants of E. coli defective at the uvrA, uvrB or uvrC locus showed increased sensitivity to the lethal effects of monofunctional mitomycin, 7-methoxymitosene (7-MMT) or decarbamoyl mitomycin C (DCMTC), as well as mitomycin C (MTC). (1) Treatment of wild type bacteria with these monofunctional mitomycins resulted in the production of single-strand breaks in DNA, which were repaired upon incubation in a growth medium. Such breaks in DNA were not produced in the UvrA and the UvrB mutants. In the UvrC mutant, single-strand breaks were produced by 7-MMT or by DCMTC, but these breaks were not repaired upon incubation. (2) Exposure of E. coli to MTC caused cross-linkage between DNA strands, which converted to a normally denaturable form during further incubation after treatment. This was not occurred in the UvrB strain. In the UvrC mutant, a portion of the cross-links was removed upon incubation. (3) 7-MMT and DCMTC induced mutation in UV sensitive UvrB and UvrC mutants with much higher frequency than in wild type bacteria, while MTC did not induce mutation in these Uvr-strains.

  3. Repair system and mitomycin mutagenesis in Escherichia coli

    International Nuclear Information System (INIS)

    Otsuji, Nozomu; Murayama, Ichiko

    1974-01-01

    Ultraviolet light sensitive mutants of E. coli defective at the uvrA, uvrB or uvrC locus showed increased sensitivity to the lethal effects of monofunctional mitomycin, 7-methoxymitosene (7-MMT) or decarbamoyl mitomycin C (DCMTC), as well as mitomycin C (MTC). (1) Treatment of wild type bacteria with these monofunctional mitomycins resulted in the production of single-strand breaks in DNA, which were repaired upon incubation in a growth medium. Such breaks in DNA were not produced in the UvrA and the UvrB mutants. In the UvrC mutant, single-strand breaks were produced by 7-MMT or by DCMTC, but these breaks were not repaired upon incubation. (2) Exposure of E. coli to MTC caused cross-linkage between DNA strands, which converted to a normally denaturable form during further incubation after treatment. This was not occurred in the UvrB strain. In the UvrC mutant, a portion of the cross-links was removed upon incubation. (3) 7-MMT and DCMTC induced mutation in UV sensitive UvrB and UvrC mutants with much higher frequency than in wild type bacteria, while MTC did not induce mutation in these Uvr-strains. (author)

  4. Incidence of chemotherapy-induced amenorrhea associated with epirubicin, docetaxel and navelbine in younger breast cancer patients

    Science.gov (United States)

    2010-01-01

    Background The rates of chemotherapy-induced amenorrhea (CIA) associated with docetaxel-based regimens reported by previous studies are discordant. For navelbine-based chemotherapies, rates of CIA have seldom been reported. Methods Of 170 premenopausal patients recruited between January 2003 and September 2008, 78 were treated with fluorouracil plus epirubicin and cyclophosphamide (FEC), 66 were treated with docetaxel plus epirubicin (TE), and 26 were treated with navelbine plus epirubicin (NE). Patient follow-up was carried up every 3-4 months during the first year, then every 9-12 months during subsequent years. Results In univariate analysis, the rates of CIA were 44.87% for the FEC regimen, 30.30% for the TE regimen and 23.08% for the NE regimen (P = 0.068). Significant differences in the rates of CIA were not found between the FEC and TE treatment groups (P > 0.05), but were found between the FEC and NE treatment groups (P 0.05). Tamoxifen use was a significant predictor for CIA (P = 0.001), and age was also a significant predictor (P < 0.001). In multivariate analysis, age (P < 0.001), the type of chemotherapy regimens (P = 0.009) and tamoxifen use (P = 0.003) were all significant predictors. Conclusions Age and administration of tamoxifen were found to be significant predictive factors of CIA, whereas docetaxel and navelbine based regimens were not associated with higher rates of CIA than epirubicin-based regimen. PMID:20540745

  5. Effect of Intraoperative mitomycin-c application in outcome of external dacryocystorhinostomy

    International Nuclear Information System (INIS)

    Jawad, M.; Ali, Z.; Aftab, H.

    2015-01-01

    Background: Patients develop postoperative fibrosis at the site of operation after dacryocystorhinostomy (DCR) which results in impairment of the osteum patency. This quasi-experimental study was undertaken to determine the role of intraoperative Mitomycin C (MMC) application in maintaining postoperative patency of the osteum. Methodology: The present study was conducted at the Eye department of Ayub Medical College, Abbottabad on patients in whom routine DCR was indicated. Subjects were divided into mitomycin C (Test) and non mitomycin C (Control) groups. In test group, Mitomycin C was applied to the anastomosed flaps and osteotomy site for 30 minutes. Postoperative patients were followed for up to 6 months and outcome of patency was documented. Results: A.total of 73 patients were included, divided into test (30) and control (43) groups. An overall success rate of 86.3 percentage was obtained for patent ostia; this was based on 96.67 percentage success in test group compared to 79.1 percentage in the control group (p=0.031). Conclusion: Intraoperative application of Mitomycin-C significantly improves the success rate in external dacryocystorhinostomy. (author)

  6. Epirubicin plus paclitaxel regimen as second-line treatment of patients with small-cell lung cancer.

    Science.gov (United States)

    Pasello, Giulia; Carli, Paolo; Canova, Fabio; Bonanno, Laura; Polo, Valentina; Zago, Giulia; Urso, Loredana; Conte, Pierfranco; Favaretto, Adolfo

    2015-04-01

    Most patients with small cell lung cancer (SCLC) experience relapse within one year after first-line treatment. The aim of this study was to describe activity and safety of second-line with epirubicin at 70 mg/m(2) followed by paclitaxel at 135 mg/m(2) on day 1 every three weeks for a maximum of six cycles. This is a retrospective review of all patients with SCLC evaluated for second-line treatment between 2003 and 2013 at our Institution. Sixty-eight patients received the study regimen of epirubicin with paclitaxel. We observed partial response in 19 (30%), stable disease in 22 (34%) and total early failure rate in 23 (36%) patients. Median progression free and overall survival were 21.8 and 26.5 weeks, respectively. Haematological toxicities were as follows: grade 3-4 leukopenia and neutropenia in 18 (31%) and 30 (22%) of patients, respectively; grade 3 anaemia and grade 4 thrombocytopenia were reported in 2 (3%) and 5 (9%) of patients, respectively. Epirubicin with paclitaxel is an active and tolerable second-line regimen in patients with SCLC. Copyright© 2015 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved.

  7. Phase I study of short-time oxaliplatin, capecitabine and epirubicin (EXE) as first line therapy in patients with non-resectable gastric cancer

    DEFF Research Database (Denmark)

    Dupont, Jeanette; Jensen, Helle A; Jensen, Benny V

    2007-01-01

    A phase I trial of short-time oxaliplatin (E), capecitabine (X) and epirubicin (E) for patients with metastatic gastric cancer was initiated to establish the recommended dose for further therapy with short-time EXE. Patients received out-patient therapy with a fixed dose of epirubicin 50 mg/m2 day......-8), median survival was 9.2 months and median TTP was 7.5 months. A combination of epirubicin 50 mg/m2 day 1, capecitabine 1,000 mg/m2 continuously and oxaliplatin 130 mg/m2 day 1 each 3 weeks is an easily administered and well tolerated out-patient regimen for patients with non-resectable gastric cancer....

  8. The Use of a Liposomal Formulation Incorporating an Antimicrobial Peptide from Tilapia as a New Adjuvant to Epirubicin in Human Squamous Cell Carcinoma and Pluripotent Testicular Embryonic Carcinoma Cells

    Science.gov (United States)

    Lo, Yu-Li; Lee, Hsin-Pin; Tu, Wei-Chen

    2015-01-01

    This study aims to explore the effects and mechanisms of hepcidin, a potential antimicrobial peptide from Tilapia, and epirubicin (Epi), an antineoplastic agent, on the generation of reactive oxygen species (ROS) and link the ROS levels to the reversal mechanisms of multidrug resistance (MDR) by epirubicin and hepcidin in human squamous cell carcinoma SCC15 and human embryonal carcinoma NT2D1 cells. The cells, pretreated with hepcidin, epirubicin, or a combination of these compounds in PEGylated liposomes, were used to validate the molecular mechanisms involved in inhibiting efflux transporters and inducing apoptosis as evaluated by cytotoxicity, intracellular accumulation, mRNA levels, cell cycle distribution, and caspase activity of this combination. We found that hepcidin significantly enhanced the cytotoxicity of epirubicin in liposomes. The co-incubation of epirubicin with hepcidin in liposomes intensified the ROS production, including hydrogen peroxide and superoxide free radicals. Hepcidin significantly increased epirubicin intracellular uptake into NT2D1 and SCC15 cells, as supported by the diminished mRNA expressions of MDR1, MDR-associated protein (MRP) 1, and MRP2. Hepcidin and/or epirubicin in liposomes triggered apoptosis, as verified by the reduced mitochondrial membrane potential, increased sub-G1 phase of cell cycle, incremental populations of apoptosis using annexin V/PI assay, and chromatin condensation. As far as we know, this is the first example showing that PEGylated liposomal TH1-5 and epirubicin gives rise to cell death in human squamous carcinoma and testicular embryonic carcinoma cells through the reduced epirubicin efflux via ROS-mediated suppression of P-gp and MRPs and concomitant initiation of mitochondrial apoptosis pathway. Hence, hepcidin in PEGylated liposomes may function as an adjuvant to anticancer drugs, thus demonstrating a novel strategy for reversing MDR. PMID:26393585

  9. Methotrexate and epirubicin conjugates as potential antitumor drugs

    Directory of Open Access Journals (Sweden)

    Szymon Wojciech Kmiecik

    2017-07-01

    Full Text Available Introduction: The use of hybrid molecules has become one of the most significant approaches in new cytotoxic drug design. This study describes synthesis and characterization of conjugates consisting of two well-known and characterized chemotherapeutic agents: methotrexate (MTX and epirubicin (EPR. The synthesized conjugates combine two significant anticancer strategies: combinatory therapy and targeted therapy. These two drugs were chosen because they have different mechanisms of action, which can increase the anticancer effect of the obtained conjugates. MTX, which is a folic acid analog, has high cytotoxic properties and can serve as a targeting moiety that can reach folate receptors (FRs overexpresing tumor cells. Combination of nonselective drugs such as EPR with MTX can increase the selectivity of the obtained conjugates, while maintaining the high cytotoxic properties.Materials and methods: Conjugates were purified by RP-HPLC and the structure was investigated by MS and MS/MS methods. The effect of the conjugates on proliferation of LoVo, LoVo/Dx, MCF-7 and MV-4-11 human cancer cell lines was determined by SRB or MTT assay.Results: The conjugation reaction results in the formation of monosubstituted (α, γ and disubstituted MTX derivatives. In vitro proliferation data demonstrate that the conjugates synthesized in our study show lower cytotoxic properties than both chemotherapeutics used alone.Discussion: Epirubicin cytotoxicity was not observed in obtained conjugates. Effective drugs release after internalization needs further investigation.

  10. Cationic PEGylated liposomes incorporating an antimicrobial peptide tilapia hepcidin 2-3: an adjuvant of epirubicin to overcome multidrug resistance in cervical cancer cells.

    Science.gov (United States)

    Juang, Vivian; Lee, Hsin-Pin; Lin, Anya Maan-Yuh; Lo, Yu-Li

    Antimicrobial peptides (AMPs) have been recently evaluated as a new generation of adjuvants in cancer chemotherapy. In this study, we designed PEGylated liposomes encapsulating epirubicin as an antineoplastic agent and tilapia hepcidin 2-3, an AMP, as a multidrug resistance (MDR) transporter suppressor and an apoptosis/autophagy modulator in human cervical cancer HeLa cells. Cotreatment of HeLa cells with PEGylated liposomal formulation of epirubicin and hepcidin 2-3 significantly increased the cytotoxicity of epirubicin. The liposomal formulations of epirubicin and/or hepcidin 2-3 were found to noticeably escalate the intracellular H 2 O 2 and O 2 - levels of cancer cells. Furthermore, these treatments considerably reduced the mRNA expressions of MDR protein 1, MDR-associated protein (MRP) 1, and MRP2. The addition of hepcidin 2-3 in liposomes was shown to markedly enhance the intracellular epirubicin uptake and mainly localized into the nucleus. Moreover, this formulation was also found to trigger apoptosis and autophagy in HeLa cells, as validated by significant increases in the expressions of cleaved poly ADP ribose polymerase, caspase-3, caspase-9, and light chain 3 (LC3)-II, as well as a decrease in mitochondrial membrane potential. The apoptosis induction was also confirmed by the rise in sub-G1 phase of cell cycle assay and apoptosis percentage of annexin V/propidium iodide assay. We found that liposomal epirubicin and hepcidin 2-3 augmented the accumulation of GFP-LC3 puncta as amplified by chloroquine, implying the involvement of autophagy. Interestingly, the partial inhibition of necroptosis and the epithelial-mesenchymal transition by this combination was also verified. Altogether, our results provide evidence that coincubation with PEGylated liposomes of hepcidin 2-3 and epirubicin caused programmed cell death in cervical cancer cells through modulation of multiple signaling pathways, including MDR transporters, apoptosis, autophagy, and/or necroptosis

  11. Uses and complications of mitomycin C in ophthalmology.

    Science.gov (United States)

    Mearza, Ali A; Aslanides, Ioannis M

    2007-01-01

    Mitomycin C is a chemotherapeutic agent that acts by inhibiting DNA synthesis. Its use and application in ophthalmology has been increasing in recent years because of its modulatory effects on wound healing. Current applications include pterygium surgery, glaucoma surgery, corneal refractive surgery, cicatricial eye disease, conjunctival neoplasia and allergic eye disease. Although it has been used successfully in these conditions, it has also been associated with significant complications. This article reviews the current trends and uses of mitomycin C in the eye and its reported complications.

  12. Mitomycin C dissolved in a reversible thermosetting gel: target tissue concentrations in the rabbit eye.

    Science.gov (United States)

    Ichien, K; Yamamoto, T; Kitazawa, Y; Oguri, A; Ando, H; Kondo, Y

    1997-01-01

    To determine whether a new, reversible thermosetting gel enhances mitomycin C transfer to target ocular tissues in the rabbit eye. A 0.1 ml solution of mitomycin C containing 0.22 microgram, 2.9 micrograms, or 28 micrograms of the agent dissolved in a reversible thermosetting gel consisting of methylcellulose, citric acid, and polyethylene glycol was injected subconjunctivally in 30 New Zealand albino rabbits. Scleral and conjunctival tissues were excised at 0.5, 1, 2, 4, or 24 hours after the injection and mitomycin C concentrations in these tissues were determined by high performance liquid chromatography. The concentration over time was approximated to a single exponential curve, and initial mitomycin C concentrations, time constants, and half life values were determined. Finally, the areas under the curves (AUCs) between 0.5 and 24 hours were calculated. The mitomycin C concentrations in the target tissues were dose dependent and decreased rapidly over 24 hours. Both the initial mitomycin C concentrations as well as AUCs in these eyes treated with mitomycin C, dissolved in a reversible thermosetting gel, were higher than those in eyes treated similarly in a previous study in which the gel was not used. Applied subconjunctivally in the rabbit eye, mitomycin C dissolved in the reversible thermosetting gel enhanced transfer of the agent to the sclera and the conjunctiva.

  13. Predictive and prognostic impact of TP53 mutations and MDM2 promoter genotype in primary breast cancer patients treated with epirubicin or paclitaxel.

    Directory of Open Access Journals (Sweden)

    Ranjan Chrisanthar

    Full Text Available BACKGROUND: TP53 mutations have been associated with resistance to anthracyclines but not to taxanes in breast cancer patients. The MDM2 promoter single nucleotide polymorphism (SNP T309G increases MDM2 activity and may reduce wild-type p53 protein activity. Here, we explored the predictive and prognostic value of TP53 and CHEK2 mutation status together with MDM2 SNP309 genotype in stage III breast cancer patients receiving paclitaxel or epirubicin monotherapy. EXPERIMENTAL DESIGN: Each patient was randomly assigned to treatment with epirubicin 90 mg/m(2 (n = 109 or paclitaxel 200 mg/m(2 (n = 114 every 3rd week as monotherapy for 4-6 cycles. Patients obtaining a suboptimal response on first-line treatment requiring further chemotherapy received the opposite regimen. Time from last patient inclusion to follow-up censoring was 69 months. Each patient had snap-frozen tumor tissue specimens collected prior to commencing chemotherapy. PRINCIPAL FINDINGS: While TP53 and CHEK2 mutations predicted resistance to epirubicin, MDM2 status did not. Neither TP53/CHEK2 mutations nor MDM2 status was associated with paclitaxel response. Remarkably, TP53 mutations (p = 0.007 but also MDM2 309TG/GG genotype status (p = 0.012 were associated with a poor disease-specific survival among patients having paclitaxel but not patients having epirubicin first-line. The effect of MDM2 status was observed among individuals harbouring wild-type TP53 (p = 0.039 but not among individuals with TP53 mutated tumors (p>0.5. CONCLUSION: TP53 and CHEK2 mutations were associated with lack of response to epirubicin monotherapy. In contrast, TP53 mutations and MDM2 309G allele status conferred poor disease-specific survival among patients treated with primary paclitaxel but not epirubicin monotherapy.

  14. Cationic PEGylated liposomes incorporating an antimicrobial peptide tilapia hepcidin 2–3: an adjuvant of epirubicin to overcome multidrug resistance in cervical cancer cells

    Directory of Open Access Journals (Sweden)

    Juang V

    2016-11-01

    Full Text Available Vivian Juang,1 Hsin-Pin Lee,2 Anya Maan-Yuh Lin,1,3 Yu-Li Lo1 1Department and Institute of Pharmacology, National Yang-Ming University, 2Department of Biological Sciences and Technology, National University of Tainan, 3Department of Medical Research, Taipei Veterans General Hospital, Taipei, Taiwan, Republic of China Abstract: Antimicrobial peptides (AMPs have been recently evaluated as a new generation of adjuvants in cancer chemotherapy. In this study, we designed PEGylated liposomes encapsulating epirubicin as an antineoplastic agent and tilapia hepcidin 2–3, an AMP, as a multidrug resistance (MDR transporter suppressor and an apoptosis/autophagy modulator in human cervical cancer HeLa cells. Cotreatment of HeLa cells with PEGylated liposomal formulation of epirubicin and hepcidin 2–3 significantly increased the cytotoxicity of epirubicin. The liposomal formulations of epirubicin and/or hepcidin 2–3 were found to noticeably escalate the intracellular H2O2 and O2- levels of cancer cells. Furthermore, these treatments considerably reduced the mRNA expressions of MDR protein 1, MDR-associated protein (MRP 1, and MRP2. The addition of hepcidin 2–3 in liposomes was shown to markedly enhance the intracellular epirubicin uptake and mainly localized into the nucleus. Moreover, this formulation was also found to trigger apoptosis and autophagy in HeLa cells, as validated by significant increases in the expressions of cleaved poly ADP ribose polymerase, caspase-3, caspase-9, and light chain 3 (LC3-II, as well as a decrease in mitochondrial membrane potential. The apoptosis induction was also confirmed by the rise in sub-G1 phase of cell cycle assay and apoptosis percentage of annexin V/propidium iodide assay. We found that liposomal epirubicin and hepcidin 2–3 augmented the accumulation of GFP-LC3 puncta as amplified by chloroquine, implying the involvement of autophagy. Interestingly, the partial inhibition of necroptosis and the epithelial

  15. Determination of epirubicin and its metabolite epirubicinol in saliva and plasma by HPLC

    NARCIS (Netherlands)

    Dodde, WIW; Maring, JG; Hendriks, G; Wachters, FM; Groen, HJM; de Vries, EGE; Uges, DRA

    We present a high-performance liquid chromatography (HPLC) method suitable for the analysis of epirubicin and its metabolite epirubicinol in saliva and plasma. Preparation of saliva and plasma samples was performed by extraction of analytes with a chloroform: 2-propanol mixture (6:1, vol/vol) and

  16. Effect of Intraoperative Mitomycin C on the Re-currence rate of ...

    African Journals Online (AJOL)

    ... effectif dans les cas recurrents. L'utilisation intra-operative du mitomycin C est fortement recommend après excision du pterygium du type primaire chez les Nigerian pour reduire le taux de recurrence. Mot clés: Pterygium, recurrence, mitomycin. West African Jnl of Pharmacology and Drug Research Vol.18 2002: 17-20 ...

  17. 21 CFR 522.2470 - Tiletamine hydrochloride and zolazepam hydrochloride for injection.

    Science.gov (United States)

    2010-04-01

    ... hydrochloride for injection. 522.2470 Section 522.2470 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT... injection. (a) Specifications. Tiletamine hydrochloride and zolazepam hydrochloride for injection when... pound of body weight. The maximum total safe dose is 13.6 milligrams per pound of body weight. (ii) In...

  18. Prospective randomized comparison of mitomycin C application in endoscopic and external dacryocystorhinostomy.

    Science.gov (United States)

    Mudhol, Rekha R; Zingade, N D; Mudhol, R S; Harugop, Anil S; Das, Amal T

    2013-08-01

    The aim of the study is to compare the subjective (relief of symptoms) and objective (endoscopic visualization of ostium patency at the time of syringing) outcomes at the end of two procedures-Endonasal DCR versus External DCR with Mitomycin C and to assess the role of Mitomycin C in maintaining patency of nasolacrimal drainage system. Prospective randomized comparative study was performed. Thirty-five patients were enrolled in each endoscopic and external dacryocystorhinostomy groups with Mitomycin C (MMC) application. The 37 eyes underwent endonasal DCR (28 unilateral primary eyes + 1 bilateral primary eyes + 5 unilateral revision eyes + 1 bilateral revision eye) while 35 eyes underwent external DCR (34 unilateral primary eyes + 1 unilateral revision eye). Mitomycin C 0.2 mg/ml was applied intra-operatively for 5 min to the ostium site at the end of endonasal or external DCR procedure. Objective assessment by syringing at the end of 1 year in the endonasal group showed 35 eyes (94%) were patent, 1 (3%) was partially blocked and 1(3%) was completely blocked; while in external group all 35 eyes (100%) were patent. Endoscopic visualization of the ostium at the time of syringing showed only one eye (3%) in the endonasal group was blocked while all the other eyes in both groups were patent. Both groups had a mean follow-up of 6-36 months. No complications were associated with use of Mitomycin C. In conclusion, intra-operative use of Mitomycin C in both endoscopic DCR and external DCR is safe and effective in increasing the success rate.

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

    Directory of Open Access Journals (Sweden)

    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.

  20. Comparison of mean corneal endothelial cell loss after trabeculectomy with and without mitomycin C

    International Nuclear Information System (INIS)

    Shaheer, M.; Amjad, A.; Ahmed, N.

    2018-01-01

    Objective:To compare mean endothelial cell loss in patients of primary open angle glaucoma undergoing trabeculectomy with and without mitomycin C. Study Design:Randomised control study. Place and Duration of Study:Institute of Ophthalmology, Mayo Hospital, Lahore, from May 2016 to April 2017. Methodology:Patients with primary open angle glaucoma, not controlled with medication, were selected from the outpatient department. Patients with secondary glaucomas and concomitant ocular disease were excluded. Selected patients were divided into two groups of 30 each. Group A patients underwent trabeculectomy with adjunctive mitomycin C while group B patients underwent trabeculectomy alone. Pre- and post-trabeculectomy endothelial cell counts were recorded with the help of specular microsope and entered on proforma. Results:Median cell loss was 283 (66.50) when trabeculectomy was done with the use of adjunctive mitomycin C in group A while median endothelial cell loss was 72.50 (19.25) when the trabeculectomy was done without the use of adjunctive mitomycin C in group B. Conclusion:Use of mitomycin C causes more endothelial cell loss during trabeculectomy as compared to when done without it. (author)

  1. 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. © Journal of the Association of Physicians of India 2011.

  2. Efficacy of External Dacryocystorhinostomy (DCR) with and without Mitomycin-C in Chronic Dacryocystitis

    International Nuclear Information System (INIS)

    Mukhtar, S. A.; Jamil, A. Z.; Ali, Z.

    2014-01-01

    Objective: To compare the efficacy of external dacryocystorhinostomy (DCR) with and without intraoperative application of mitomycin-C in patients with chronic dacryocystitis. Study Design: An experimental study. Place and Duration of Study: Department of Ophthalmology, Bahawal Victoria Hospital (BVH), Bahawalpur, from September 2009 to December 2010. Methodology: One hundred and sixty patients with chronic dacryocystitis undergoing external DCR were divided into two groups comprising of 80 patients each. Group A included patients, who underwent external DCR with intraoperative use of mitomycin-C. Group B included those patients who were not administered intraoperative mitomycin-C. Sociodemographic information and the data regarding the patency of the lacrimal drainage system by irrigation with normal saline were collected at the end of the third month after the surgery. Chi-square test was used, at 95% confidence level, as the test of significance to compare the success of surgery between the two groups. Results: Surgical success rate (efficacy) in group 'A' was found to be 97.5% and 86.25% in group 'B'. The difference in success rate was statistically significant (p=0.017). Conclusion: External dacryocystorhinostomy with intraoperative mitomycin-C is more efficacious in achieving lacrimal system patency than external dacryocystorhinostomy without mitomycin-C. (author)

  3. Zytoprotektion mit Amifostin (Ethyol®) in der Chemotherapie: Meta-Analyse zum pharmakokinetischen Interaktionspotential mit Zytostatika.

    Science.gov (United States)

    Czejka, Martin; Schüller, Johannes; Kletzl, Heidemarie

    2017-08-25

    The cytoprotective agent amifostine (AMI) is capable to protect healthy cells (contrary to tumor cells) due to higher activity of alkaline phosphatase at the membrane site of normal cells. In seven clinical trials the influence of AMI on the pharmacokinetics of different cytostatics was investigated. Preadministration of AMI increased Cmax of doxorubicin (+ 44 %, p < 0.06), epirubicin (+ 31 %, P < 0.08), mitomycin C (+ 41 %, p < 0.01) and docetaxel (+ 31 % and + 17 %, not significant). In contrary, the peak concentration of pirarubicin , the tetrahydropyranyl-prodrug of doxorubicin was decreased (- 50 %, P < 0.03), leading to an equal higher concentrationof doxorubicin in the blood . In accordance to the peak concentrations, the AUC'ast was increased by chemoprotection: doxorubicin + 53 % (p < 0.01) and epirubicin + 23 % (not significant), docetaxel + 25 % and + 31 % (not significant). AUC'ast of mitomycin C and paclitaxel seemed to be unaffected by preadministered AMI. A particular inhibition of the protein binding by AMI has been identified as one reason for higher serum concentrations of anthracycline drugs. After cytoprotection, a possible increase of the cytostatic's Serum concentrations should be taken into account for optimal dosage schedules.

  4. Conjunctival dysfunction and mitomycin C-induced hypotony.

    Science.gov (United States)

    Sihota, R; Dada, T; Gupta, S D; Sharma, S; Arora, R; Agarwal, H C

    2000-10-01

    To determine the role of a physically intact conjunctiva in the development of chronic hypotony after mitomycin C-enhanced trabeculectomy. Three patients with mitomycin C-related hypotonic maculopathy, but without a leak on Siedel test, had a thorough evaluation of the bleb area and an anterior segment fluorescein angiography. The bleb was excised and a pedicle flap, rotated from the temporal conjunctiva, was sutured to cover the defect superiorly. The scleral flap and its sutures were not disturbed. The excised bleb was subjected to light and electron microscopy. The Seidel test result was negative in all patients, but late phases of the anterior segment angiography showed a generalized seepage of aqueous from the bleb. After revision of the bleb, there was a gradual increase in the intraocular pressure, a reversal of the hypotonic maculopathy, and consequent improvement in visual acuity in all three patients, stable up to a minimum follow-up of 18 months. On histopathologic examination, the basement membrane was thickest under thin areas of the epithelium and thinnest below thicker epithelial layers. A dysfunctional conjunctival barrier, as evidenced by the "sweating" of the bleb and histopathologic alterations in the epithelial barrier, could be responsible for the hypotonic maculopathy in these patients. Excision of the conjunctiva alone and replacement by a pedicle conjunctival graft offers a safe and effective method of treating chronic hypotony after mitomycin C-augmented trabeculectomy in such patients.

  5. Self-association of analgesics in aqueous solution: micellar properties of dextropropoxyphene hydrochloride and methadone hydrochloride.

    Science.gov (United States)

    Attwood, D; Tolley, J A

    1980-08-01

    The solution properties of several analgesics including dextropropoxyphene hydrochloride, methadone hydrochloride, dextromoramide acid tartrate and dipipanone hydrochloride have been examined using light scattering, conductivity, vapour pressure osmometry and surface tension techniques. A micellar pattern of association was established for dextropropoxyphene hydrochloride and methadone hydrochloride and critical micelle concentrations and aggregation numbers are reported. The hydrophobic contribution to the free energy of micellization of dextropropoxyphene was determined from measurement of the critical micelle concentration in the presence of added electrolyte.

  6. The effect of topical mitomycin C on full-thickness burns.

    Science.gov (United States)

    Tennyson, Heath; Helling, Eric R; Wiseman, Joseph; Dick, Edward; Lyons, Robert C

    2007-09-15

    Burns result in substantial morbidity because of fibroblast proliferation and contracture. Mitomycin C is a chemotherapeutic agent known to suppress fibroblast proliferation. It is used in ophthalmologic disorders and reduces scarring in upper aerodigestive surgery. No study of the effect of mitomycin C on cutaneous burns has been performed. This study examined burn healing in the presence of topical mitomycin C by evaluation of wound appearance, contraction, and histology in a pig model. Standardized full-thickness burns were produced on the flanks of three pigs. One animal received no further therapy and was an external control. Two animals underwent placement of topical mitomycin C, 0.4 mg/ml, on selected burn sites for 5 minutes. This was repeated 2 and 4 weeks after injury. Evaluation was performed at 2 and 6 months using a clinical assessment scale and a visual analogue scale. Scar length and histologic analysis were also evaluated. Clinical assessment scale and visual analogue scale scores showed improved appearance in the untreated external control wounds versus the untreated internal control and treated wounds (p Wound contraction was not significantly different between groups. Histologic characteristics between groups were similar except for epidermal hyperplasia, which was decreased in the untreated external control (p wounds at 0.4 mg/cc for three courses does not improve, and may worsen, clinical appearance and scarring during early healing. There is no difference in histology during the long-term healing process. Scar contraction was unchanged.

  7. Variability of Streptomyces narbonesis producing ν-1,3/1,4 glucanglucan hydrolasi induced by UV and mitomycin C

    International Nuclear Information System (INIS)

    Elinov, N.P.; Pronina, M.I.; Zaikina, N.A.; Azizov, P.I.

    1982-01-01

    Effect of mitomycin c and ultraviolet rays on spores and spore sprouts of 2 hour old of Streptomyces narbonensis of 2a producer of ν-1.3/1.4 glucanglucanhydrolase (ν-gluconase) has been studied. It is shown that the lethal effect of mitomycin c on spore sprouts is considerably higher than on producer spores. Mutageneous activity of mitomycin C is closely related to the process of spore germination. Under the effect of mitomycin C on spore sprouts noted is higher mutability as compared with the effect on spores. Frequency of morphological mutations is lower under the effect of ultraviolet rays as compared with the effect of mitomycin C. Under ultraviolet rays produced were mutants synthesizing during fermentation on medium without inductor of exotype ν-gluconase

  8. Knockdown of UbcH10 Enhances the Chemosensitivity of Dual Drug Resistant Breast Cancer Cells to Epirubicin and Docetaxel

    Directory of Open Access Journals (Sweden)

    Cheng Wang

    2015-03-01

    Full Text Available Breast cancer is one of the most common and lethal cancers in women. As a hub gene involved in a diversity of tumors, the ubiquitin-conjugating enzyme H10 (UbcH10, may also play some roles in the genesis and development of breast cancer. In the current study, we found that the expression of UbcH10 was up-regulated in some breast cancer tissues and five cell lines. We established a dual drug resistant cell line MCF-7/EPB (epirubicin/TXT (docetaxel and a lentiviral system expressing UbcH10 shRNA to investigate the effects of UbcH10 knockdown on the chemosensitivity of MCF-7/EPB/TXT cells to epirubicin and docetaxel. The knockdown of UbcH10 inhibited the proliferation of both MCF-7 and MCF-7/EPB/TXT cells, due to the G1 phase arrest in cell cycle. Furthermore, UbcH10 knockdown increased the sensitivity of MCF-7/EPB/TXT cells to epirubicin and docetaxel and promoted the apoptosis induced by these two drugs. Protein detection showed that, in addition to inhibiting the expression of Ki67 and cyclin D1, UbcH10 RNAi also impaired the increased BCL-2 and MDR-1 expression levels in MCF-7/EPB/TXT cells, which may contribute to abating the drug resistance in the breast cancer cells. Our research in the current study demonstrated that up-regulation of UbcH10 was involved in breast cancer and its knockdown can inhibit the growth of cancer cells and increase the chemosensitivity of the dual drug resistant breast cancer cells to epirubicin and docetaxel, suggesting that UbcH10 may be a promising target for the therapy of breast cancer.

  9. The Risk of Amenorrhea Is Related to Chemotherapy-Induced Leucopenia in Breast Cancer Patients Receiving Epirubicin and Taxane Based Chemotherapy

    Science.gov (United States)

    Liang, Xiuqing; He, Zhongyuan; Zha, Xiaoming; Liu, Xiaoan; Wang, Shui

    2012-01-01

    Background Chemotherapy-induced amenorrhea (CIA) is common in young breast cancer patients. The incidence of CIA associated with regimens involving epirubicin and taxane was not well known. Furthermore, previous studies suggested leucopenia and amenorrhea may reflect inter-individual variations in pharmacokinetics. The purpose of this study was to investigate the association between leucopenia after first cycle of chemotherapy and CIA in young breast cancer patients receiving epirubicin and taxane based chemotherapy. Furthermore, the incidence of CIA was also assessed. Methodology and Principal Findings Between October 2008 and March 2010, 186 consecutive premenopausal patients, treated with epirubicin and taxane based chemotherapy, were recruited. Information about CIA was collected by telephone and out-patient clinic. Of these 186 patients, data from 165 patients were included and analyzed. Of all 165 patients, CIA occurred in 72 patients (43.64%). In multivariate analysis, age older than 40 y (OR: 16.10, 95% CI: 6.34–40.88, P0.05). The rate of CIA in leucopenia group (52.56%) was significantly higher than that in normal leukocyte group (34.62%) (P = 0.024). In patients treated with a FEC regimen (cyclophosphamide, epirubicin and 5-fluorouracil), the rate of CIA in leucopenia group (59.57%) was significantly higher than that in normal leukocyte group (36.84%) (P = 0.037). Conclusions Age at diagnosis and previous childbearing were both found to significantly increase the risk of CIA, whereas additional taxane was not associated with increased rate of CIA. Importantly, leucopenia after first cycle of chemotherapy was associated with increased risk of CIA, which suggested that leucopenia may be an early predictor of chemotherapy-induced infertility. PMID:22615953

  10. The risk of amenorrhea is related to chemotherapy-induced leucopenia in breast cancer patients receiving epirubicin and taxane based chemotherapy.

    Directory of Open Access Journals (Sweden)

    Wenbin Zhou

    Full Text Available BACKGROUND: Chemotherapy-induced amenorrhea (CIA is common in young breast cancer patients. The incidence of CIA associated with regimens involving epirubicin and taxane was not well known. Furthermore, previous studies suggested leucopenia and amenorrhea may reflect inter-individual variations in pharmacokinetics. The purpose of this study was to investigate the association between leucopenia after first cycle of chemotherapy and CIA in young breast cancer patients receiving epirubicin and taxane based chemotherapy. Furthermore, the incidence of CIA was also assessed. METHODOLOGY AND PRINCIPAL FINDINGS: Between October 2008 and March 2010, 186 consecutive premenopausal patients, treated with epirubicin and taxane based chemotherapy, were recruited. Information about CIA was collected by telephone and out-patient clinic. Of these 186 patients, data from 165 patients were included and analyzed. Of all 165 patients, CIA occurred in 72 patients (43.64%. In multivariate analysis, age older than 40 y (OR: 16.10, 95% CI: 6.34-40.88, P0.05. The rate of CIA in leucopenia group (52.56% was significantly higher than that in normal leukocyte group (34.62% (P = 0.024. In patients treated with a FEC regimen (cyclophosphamide, epirubicin and 5-fluorouracil, the rate of CIA in leucopenia group (59.57% was significantly higher than that in normal leukocyte group (36.84% (P = 0.037. CONCLUSIONS: Age at diagnosis and previous childbearing were both found to significantly increase the risk of CIA, whereas additional taxane was not associated with increased rate of CIA. Importantly, leucopenia after first cycle of chemotherapy was associated with increased risk of CIA, which suggested that leucopenia may be an early predictor of chemotherapy-induced infertility.

  11. [Effect of mitomycin C dissolved in a reversible thermosetting gel on outcome of filtering surgery in the rabbit].

    Science.gov (United States)

    Ichien, K; Sawada, A; Yamamoto, T; Kitazawa, Y; Shiraki, R; Yoh, M

    1999-04-01

    Based on our previous report that showed enhanced transfer of mitomycin C to the sclera and the conjunctiva by dissolving the antiproliferative in a reversible thermo-setting gel, we conducted a study to investigate the efficacy of the mitomycin C-gel in the rabbit. We subconjunctivally injected 0.1 ml of the mitomycin C-gel solution containing several amounts of the drug. Trephination was performed in the injected region 24 hours later. Intraocular pressure measurement, and photography and ultrasound biomicroscopic examination of the filtering bleb were done 1, 2, and 4 weeks postoperatively. The gel containing 3.0 micrograms or more mitomycin C significantly enhanced bleb formation in addition to reducing the intraocular pressure. The reversible thermo-setting gel seems to facilitate filtration following glaucoma filtering surgery in the rabbit and deserves further investigation as a new method of mitomycin C application.

  12. 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...

  13. Delayed healing at transurethral resection of bladder tumour sites after immediate postoperative mitomycin C instillation

    DEFF Research Database (Denmark)

    Aagaard, Mark F; Mogensen, Karin; Hermann, Gregers G

    2014-01-01

    The most common reactions to mitomycin C are dysuria and drug-related palmar and genital desquamation. This report describes two cases of delayed healing of the mucosa at resection sites after transurethral resection of bladder tumours, most likely due to immediate postoperative mitomycin C...

  14. Mitomycin C application in resistant caustic esophageal stricture

    African Journals Online (AJOL)

    procedures and in laryngotracheal stenosis [4]. Topical application of .... replacement [1], stents with its high incidence of failure and morbidity [5], and .... 8 Fröhlich T, Greess H, Köhler H. Topical mitomycin C treatment of a benign oesophageal ...

  15. β3 integrin promotes chemoresistance to epirubicin in MDA-MB-231 through repression of the pro-apoptotic protein, BAD

    Energy Technology Data Exchange (ETDEWEB)

    Nair, Madhumathy G.; Desai, Krisha; Prabhu, Jyothi S.; Hari, P.S.; Remacle, Jose; Sridhar, T.S., E-mail: tssridhar@sjri.res.in

    2016-08-01

    Resistance to anthracycline based chemotherapy is a major limitation in the treatment of breast cancer, particularly of the triple negative sub-type that lacks targeted therapies. Resistance that arises from tumor-stromal interaction facilitated by integrins provides the possibility of targeted disruption. In the present study, we demonstrate that integrin β3 signaling inhibits apoptosis induced by a DNA-damaging chemotherapeutic agent, epirubicin, in MDA-MB-231 breast cancer cells. Drug efflux based mechanisms do not contribute to this effect. We show that integrin β3 employs the PI3K-Akt and the MAPK pathway for enabling cell survival and proliferation. Further, our results indicate that integrin β3 helps inhibit epirubicin induced cytotoxicity by repression of the pro-apoptotic protein BAD, thus promoting an anti-apoptotic response. Myristoylated RGT peptide and a monoclonal antibody against integrin β3 brought about a reversal of this effect and chemosensitized the cells. These results identify β3 integrin signaling via repression of BAD as an important survival pathway used by breast cancer cells to evade chemotherapy induced stress. - Highlights: • Integrin β3 signaling promotes chemoresistance to epirubicin in breast cancer cells. • Integrin β3 promotes cell survival and proliferation in drug treated cells through the PI3K and MAPK pathways. • Integrin signaling helps evade drug induced cytotoxicity by repression of pro-apoptotic molecule; BAD.

  16. Galectin-3 silencing inhibits epirubicin-induced ATP binding cassette transporters and activates the mitochondrial apoptosis pathway via β-catenin/GSK-3β modulation in colorectal carcinoma.

    Directory of Open Access Journals (Sweden)

    Yung-Kuo Lee

    Full Text Available Multidrug resistance (MDR, an unfavorable factor compromising the treatment efficacy of anticancer drugs, involves the upregulation of ATP binding cassette (ABC transporters and induction of galectin-3 signaling. Galectin-3 plays an anti-apoptotic role in many cancer cells and regulates various pathways to activate MDR. Thus, the inhibition of galectin-3 has the potential to enhance the efficacy of the anticancer drug epirubicin. In this study, we examined the effects and mechanisms of silencing galectin-3 via RNA interference (RNAi on the β-catenin/GSK-3β pathway in human colon adenocarcinoma Caco-2 cells. Galectin-3 knockdown increased the intracellular accumulation of epirubicin in Caco-2 cells; suppressed the mRNA expression of galectin-3, β-catenin, cyclin D1, c-myc, P-glycoprotein (P-gp, MDR-associated protein (MRP 1, and MRP2; and downregulated the protein expression of P-gp, cyclin D1, galectin-3, β-catenin, c-Myc, and Bcl-2. Moreover, galectin-3 RNAi treatment significantly increased the mRNA level of GSK-3β, Bax, caspase-3, and caspase-9; remarkably increased the Bax-to-Bcl-2 ratio; and upregulated the GSK-3β and Bax protein expressions. Apoptosis was induced by galectin-3 RNAi and/or epirubicin as demonstrated by chromatin condensation, a higher sub-G1 phase proportion, and increased caspase-3 and caspase-9 activity, indicating an intrinsic/mitochondrial apoptosis pathway. Epirubicin-mediated resistance was effectively inhibited via galectin-3 RNAi treatment. However, these phenomena could be rescued after galectin-3 overexpression. We show for the first time that the silencing of galectin-3 sensitizes MDR cells to epirubicin by inhibiting ABC transporters and activating the mitochondrial pathway of apoptosis through modulation of the β-catenin/GSK-3β pathway in human colon cancer cells.

  17. Interaction of the antiemetics ondansetron and granisetron with the cytotoxicity induced by irradiation, epirubicin, bleomycin, estramustine, and cisplatin in vitro

    Energy Technology Data Exchange (ETDEWEB)

    Behnam Motlagh, P. [Dept. of Oncology, Umeaa Univ. Hospital (Sweden); Henriksson, R. [Dept. of Oncology, Umeaa Univ. Hospital (Sweden); Grankvist, K. [Dept. of Clinical Chemistry, Umeaa Univ. Hospital (Sweden)

    1995-12-31

    At cancer treatment, the use of antiemetics are often needed due to induction of nausea and vomiting. Some antiemetics have been shown to interact with the direct cytotoxic effects. The newly developed antiemetics have, so far as we know, not been studied in this respect. In the present study, the effects of the 5-HT{sub 3} receptor antagonists ondansetron and granisetron were evaluated on the cytotoxicity, induced by irradiation, bleomycin, epirubicin, estramustine, and cisplatin using fibroblasts (V79) and lung cancer cells (P31) in vitro. Ondansetron or granisetron (10{sup -5} mol/l) had no effect on the survival of irradiated cells. Granisetron (10{sup -5} mol/l) significantly potentiated cytoxocity of 2.5 mg/l epirubicin on fibroblasts whereas the effect of granisetron (10{sup -7} mol/l) on the cytotoxic effect of 25 mg/l bleomycin, and estramustine (80 mg/l) seemed additive to lung cancer cells. Ondansetron was non-interactive with the cytotoxicity induced by any of the anti-cancer drugs. Although the encountered observation with an enhancing effect of granisetron on the epirubicin-induced cytotoxicity is seen in a specific experimental situation in vitro, the fact that 5-HT{sub 3} receptor antagonists are routinely used during cancer treatment indicate that attention should be given to a possible interaction with the antineoplastic action of cancer treatment. (orig.).

  18. Interaction of the antiemetics ondansetron and granisetron with the cytotoxicity induced by irradiation, epirubicin, bleomycin, estramustine, and cisplatin in vitro

    International Nuclear Information System (INIS)

    Behnam Motlagh, P.; Henriksson, R.; Grankvist, K.

    1995-01-01

    At cancer treatment, the use of antiemetics are often needed due to induction of nausea and vomiting. Some antiemetics have been shown to interact with the direct cytotoxic effects. The newly developed antiemetics have, so far as we know, not been studied in this respect. In the present study, the effects of the 5-HT 3 receptor antagonists ondansetron and granisetron were evaluated on the cytotoxicity, induced by irradiation, bleomycin, epirubicin, estramustine, and cisplatin using fibroblasts (V79) and lung cancer cells (P31) in vitro. Ondansetron or granisetron (10 -5 mol/l) had no effect on the survival of irradiated cells. Granisetron (10 -5 mol/l) significantly potentiated cytoxocity of 2.5 mg/l epirubicin on fibroblasts whereas the effect of granisetron (10 -7 mol/l) on the cytotoxic effect of 25 mg/l bleomycin, and estramustine (80 mg/l) seemed additive to lung cancer cells. Ondansetron was non-interactive with the cytotoxicity induced by any of the anti-cancer drugs. Although the encountered observation with an enhancing effect of granisetron on the epirubicin-induced cytotoxicity is seen in a specific experimental situation in vitro, the fact that 5-HT 3 receptor antagonists are routinely used during cancer treatment indicate that attention should be given to a possible interaction with the antineoplastic action of cancer treatment. (orig.)

  19. First-line treatment of advanced ovarian cancer with paclitaxel/carboplatin with or without epirubicin (TEC versus TC)-a gynecologic cancer intergroup study of the NSGO, EORTC GCG and NCIC CTG

    DEFF Research Database (Denmark)

    Lindemann, K.; Christensen, R. D.; Vergote, I.

    2012-01-01

    Background: The addition of anthracyclines to platinum-based chemotherapy may provide benefit in survival in ovarian cancer patients. We evaluated the effect on survival of adding epirubicin to standard carboplatin and paclitaxel. Patients and methods: We carried out a prospectively randomized...... of epirubicin to standard carboplatin and paclitaxel treatment did not improve survival in patients with advanced ovarian, tubal or peritoneal cancer....

  20. Respiration shutoff in Escherichia coli K12 strains is induced by far ultraviolet radiations and by mitomycin C

    International Nuclear Information System (INIS)

    Swenson, P.A.; Norton, I.L.

    1984-01-01

    Near ultraviolet radiations (UV) cause respiration to shutoff in Escherichia coli B/r. It has been reported that E. coli K12 strains do not shut off respiration after UV. It is also reported that mitomycin C did not cause this 'SOS' response. In this paper it is reported that higher UV fluences than were previously used will cause respiration shutoff in K12 strain W3110 and that cyclic AMP increases the sensitivity of respiration shutoff of irradiated cell suspensions. Also mitomycin C shuts off respiration in this strain. Neither UV nor mitomycin C causes respiration shutoff in the recA56 derivative of W3110. Thus respiration shutoff is a recA dependent response to UV and mitomycin C in E. coli K12 strains. (Auth.)

  1. Exploration of two methods for quantitative Mitomycin C measurement in tumor tissue in vitro and in vivo

    DEFF Research Database (Denmark)

    Fischer, Lee MacKenzie; Vásquez, Juan Luis; Gehl, Julie

    2013-01-01

    Two methods of quantifying Mitomycin C in tumor tissue are explored. A method of ultraviolet-visible absorption microscopy is developed and applied to measure the concentration of Mitomycin C in preserved mouse tumor tissue, as well as in gelatin samples. Concentrations as low as 60 μM can...... be resolved using this technique in samples that do not strongly scatter light. A novel method for monitoring the Mitomycin C concentrations inside a tumor is developed, based on microdialysis and ultraviolet-visible spectroscopy. A pump is used to perfuse a microdialysis probe with Ringer’s solution, which...

  2. Transconjunctival penetration of mitomycin C

    Directory of Open Access Journals (Sweden)

    Velpandian T

    2008-01-01

    Full Text Available Aims: The study was performed to estimate transconjunctival penetration of mitomycin C (MMC to Tenon′s tissue following application over the intact conjunctiva before routine trabeculectomy. Settings and Design: Institution-based case series. Materials and Methods: In 41 eyes of 41 patients, MMC (0.4 mg/ml for 3 min was applied over the intact conjunctiva before beginning trabeculectomy. Tenon′s capsule directly beneath the site of application was excised during trabeculectomy and was homogenized, centrifuged and MMC concentrations were analyzed using high-performance liquid chromatography (HPLC. Statistical Analysis Used: Statistical analysis was performed using stata0 8.0 version software (STATA Corporation, Houston, TX, USA. In this study, P -values less than 0.05 were considered as statistically significant. Results: The average weight of the sample of Tenon′s tissue excised was 5.51 ± 4.42 mg (range: 0.9-17.1 and the average estimated MMC concentration found to be present in Tenon′s tissue using HPLC was 18.67 ± 32.36 x 10−6 moles/kg of the tissue (range: 0.38-197.05 x 10−6 . In 36 of the 41 patients (87.80%, the MMC concentration reached above 2 x 10−6 moles/kg of the tissue concentration required to inhibit human conjunctival fibroblasts. Conclusions: Mitomycin C does permeate into the subconjunctival tissue after supraconjunctival application for 3 min. Application of MMC over the conjunctiva may be a useful alternative to subconjunctival or subscleral application during routine trabeculectomy and as an adjunct for failing blebs.

  3. 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 ...

  4. Anthracycline-induced cardiotoxicity. Changes in left ventricular function evaluated by radionuclide cardiography during and after epirubicin therapy and predictive value of the method for heart failure; Antracyclin-induceret kardiotoxicitet. Aendringer i venstre ventrikels funktion vurderet ved isotopkardiografi under og efter behandling med epirubicin, og metodens evne til at praediktere klinisk hjerteinsufficiens

    Energy Technology Data Exchange (ETDEWEB)

    Schaadt, Bente Krogsgaard

    1998-12-31

    Eighty-nine patients with breast cancer participated in this study of the left ventricular function determined by radionuclide cardiography before, during and after epirubicin treatment. Radiocardiography (MUGA = MUlti Gated Acquisition) was performed on patients in horizontal position after an intravenous injection of {sup 99m}Tc-labelled human serum albumin. Of these patients 67 were treated with at least 850 mg/m{sup 2} of the drug. Eight of the patients developed clinical signs of heart failure, whereas 59 did not. A fall in left ventricular ejection fraction (LVEF) was recorded during the first of the treatment period in both groups. The age was significantly higher and LVEF lower before epirubicin treatment in the group that developed heart failure, but the change in LVEF during treatment was of the same magnitude in the two groups. Whereas internationally recommended criteria for interruption of chemotherapy had low predictive values in these patients, a combination of 3 criteria: age {>=} 50 years, pre-treatment LVEF {<=} 0.60 and a fall in LVEF below 0.50 during epirubicin treatment yielded a high diagnostic value with regard to development of heart failure. The sensitivity and specificity of these criteria were 88% and 95%, respectively, and the predictive value of a positive and a negative test 70% and 98%. (au)

  5. Butriptyline Hydrochloride and Imipramine Hydrochloride in the ...

    African Journals Online (AJOL)

    used tricyclic antidepressants, imipramine hydrochloride, was undertaken in 28 patients suffering from non-psychotic depression in a doubleblind trial. Three criteria-side-effects, depression and anxiety-were observed at each visit. The scoring ...

  6. Lithium chloride attenuates mitomycin C induced necrotic cell death in MDA-MB-231 breast cancer cells via HMGB1 and Bax signaling.

    Science.gov (United States)

    Razmi, Mahdieh; Rabbani-Chadegani, Azra; Hashemi-Niasari, Fatemeh; Ghadam, Parinaz

    2018-07-01

    The clinical use of potent anticancer drug mitomycin C (MMC) has limited due to side effects and resistance of cancer cells. The aim of this study was to investigate whether lithium chloride (LiCl), as a mood stabilizer, can affect the sensitivity of MDA-MB-231 breast cancer cells to mitomycin C. The cells were exposed to various concentrations of mitomycin C alone and combined with LiCl and the viability determined by trypan blue and MTT assays. Proteins were analyzed by western blot and mRNA expression of HMGB1 MMP9 and Bcl-2 were analyzed by RT-PCR. Flow cytometry was used to determine the cell cycle arrest and percent of apoptotic and necrotic cells. Concentration of Bax assessed by ELISA. Exposure of the cells to mitomycin C revealed IC 50 value of 20 μM, whereas pretreatment of the cells with LiCl induced synergistic cytotoxicity and IC 50 value declined to 5 μM. LiCl combined with mitomycin C significantly down-regulated HMGB1, MMP9 and Bcl-2 gene expression but significantly increased the level of Bax protein. In addition, the content of HMGB1 in the nuclei decreased and pretreatment with LiCl reduced the content of HMGB1 release induced by MMC. LiCl increased mitomycin C-induced cell shrinkage and PARP fragmentation suggesting induction of apoptosis in these cells. LiCl prevented mitomycin C-induced necrosis and changed the cell death arrest at G2/M-phase. Taking all together, it is suggested that LiCl efficiently enhances mitomycin C-induced apoptosis and HMGB1, Bax and Bcl-2 expression may play a major role in this process, the findings that provide a new therapeutic strategy for LiCl in combination with mitomycin C. Copyright © 2018 Elsevier GmbH. All rights reserved.

  7. Intervention of raltitrexed combined with epirubicin in hepatic arterial infusion and embolization in treatment of primary liver cancer

    Directory of Open Access Journals (Sweden)

    WANG Baoxin

    2015-05-01

    Full Text Available ObjectiveTo evaluate the therapeutic effect of intervention of raltitrexed combined with epirubicin in hepatic arterial infusion and embolization in the treatment of advanced primary liver cancer. MethodsA total of 80 patients with advanced primary liver cancer who were admitted to the Central Hospital of China National Petroleum Corporation from January 2011 to May 2013 and not suitable for surgical treatment were selected and randomly divided into study group (n=40 and control group (n=40. The study group was treated with intervention of raltitrexed combined with epirubicin in hepatic arterial infusion and embolization, while the control group was treated with intervention of fluorouracil (5-FU combined with epirubicin in hepatic arterial infusion and embolization. The treatment was given once every four weeks for a total of three to six circles. The response rate (RR, disease control rate (DCR, median time to progression, survival rate, and the decreases in alpha fetoprotein (AFP, carcinoembryonic antigen (CEA, transaminase, and bilirubin of the two groups were observed. Comparison of categorical data between the two groups was made by chi-square test, and comparison of continuous data was made by t test. ResultsThe RRs of the study group and control group were 52.5% and 22.5%, respectively, and the difference was significant (χ2=7.680, P=0.006; the DCRs of the study group and control group were 87.5% and 60.0%, respectively, and the difference was significant (χ2=7.813, P=0.005; the median time to progression of the study group and control group was 12.2 and 8.0 months, respectively, and the difference was significant (t=5.118, P=0.00; the 1- and 2-year survival rates of the study group were 85.0% and 60.0%, respectively, with the control group being 65.0% and 37.5%, and the difference was significant (χ2=4.267, P=0.039; χ2=4.053, P=0.044. One month after chemoembolization, the number of patients whose AFP, transaminase, and bilirubin

  8. Validation and use of microdialysis for determination of pharmacokinetic properties of the chemotherapeutic agent mitomycin C - an experimental study

    International Nuclear Information System (INIS)

    Sørensen, Olaf; Andersen, Anders; Olsen, Harald; Alexandr, Kristian; Ekstrøm, Per Olaf; Giercksky, Karl-Erik; Flatmark, Kjersti

    2010-01-01

    Mitomycin C is a chemotherapeutic agent used in the treatment of peritoneal surface malignancies, administered as hyperthermic intraperitoneal chemotherapy after cytoreductive surgery. Pharmacokinetic studies have been based on analyses of blood, urine and abdominal perfusate, but actual tissue concentrations of the drug have never been determined. Microdialysis is an established method for continuous monitoring of low-molecular substances in tissues, and in the present study microdialysis of mitomycin C was studied in vitro and in vivo. Using in vitro microdialysis, relative recovery was determined when varying drug concentration, temperature and perfusion flow rate. In vivo microdialysis was performed in rats to verify long-term stability of relative recovery in four compartments (vein, peritoneum, extraperitoneal space and hind leg muscle). Subsequently, intravenous and intraperitoneal bolus infusion experiments were performed and pharmacokinetic parameters were calculated. In vitro, compatibility of mitomycin C and microdialysis equipment was demonstrated, and relative recovery was stable over an adequate concentration range, moderately increased by raising medium temperature and increased when flow rate was reduced, all according to theory. In vivo, stable relative recovery was observed over seven hours. Mitomycin C exhibited fast and even distribution in rat tissues, and equal bioavailability was achieved by intravenous and intraperitoneal infusion. The half-life of mitomycin C calculated after intravenous infusion was 40 minutes. Mitomycin C concentration can be reliable monitored in vivo using microdialysis, suggesting that this technique can be used in pharmacokinetic studies of this drug during hyperthermic intraperitoneal chemotherapy

  9. 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.

  10. 21 CFR 522.1642 - Oxymorphone hydrochloride injection.

    Science.gov (United States)

    2010-04-01

    ... § 522.1642 Oxymorphone hydrochloride injection. (a) Specifications. The drug contains 1 or 1.5 milligrams of oxymorphone hydrochloride per milliliter of aqueous solution containing 0.8 percent sodium... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxymorphone hydrochloride injection. 522.1642...

  11. 21 CFR 522.536 - Detomidine hydrochloride injection.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Detomidine hydrochloride injection. 522.536... § 522.536 Detomidine hydrochloride injection. (a) Specification. Each milliliter of sterile aqueous solution contains 10 milligrams of detomidine hydrochloride. (b) Sponsor. See 052483 in § 510.600(c) of...

  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. (b...

  13. Cartap hydrochloride poisoning: A clinical experience

    OpenAIRE

    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 to...

  14. Treatment of multiple-level tracheobronchial stenosis secondary to endobronchial tuberculosis using bronchoscopic balloon dilatation with topical mitomycin-C.

    Science.gov (United States)

    Faisal, Mohamed; Harun, Hafaruzi; Hassan, Tidi M; Ban, Andrea Y L; Chotirmall, Sanjay H; Abdul Rahaman, Jamalul Azizi

    2016-04-14

    Tracheobronchial stenosis is a known complication of endobronchial tuberculosis. Despite antituberculous and steroid therapy, the development of bronchial stenosis is usually irreversible and requires airway patency to be restored by either bronchoscopic or surgical interventions. We report the use of balloon dilatation and topical mitomycin-C to successful restore airway patency. We present a 24-year old lady with previous pulmonary tuberculosis and laryngeal tuberculosis in 2007 and 2013 respectively who presented with worsening dyspnoea and stridor. She had total left lung collapse with stenosis of both the upper trachea and left main bronchus. She underwent successful bronchoscopic balloon and manual rigid tube dilatation with topical mitomycin-C application over the stenotic tracheal segment. A second bronchoscopic intervention was performed after 20 weeks for the left main bronchus stenosis with serial balloon dilatation and topical mitomycin-C application. These interventions led to significant clinical and radiographic improvements. This case highlights that balloon dilatation and topical mitomycin-C application should be considered in selected patients with tracheobronchial stenosis following endobronchial tuberculosis, avoiding airway stenting and invasive surgical intervention.

  15. 21 CFR 520.1660b - Oxytetracycline hydrochloride capsules.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride capsules. 520.1660b... Oxytetracycline hydrochloride capsules. (a) Specifications. The drug is in capsule form with each capsule containing 125 or 250 milligrams of oxytetracycline hydrochloride. Oxytetracycline is the antibiotic...

  16. 21 CFR 522.1662a - Oxytetracycline hydrochloride injection.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride injection. 522.1662a... § 522.1662a Oxytetracycline hydrochloride injection. (a)(1) Specifications. The drug contains 50 milligrams of oxytetracycline hydrochloride in each milliliter of sterile solution. (2) Sponsor. See No...

  17. Immobilisation of impala (Aepyceros melampus with a ketamine hydrochloride / medetomidine hydrochloride combination, and reversal with atipamezole hydrochloride

    Directory of Open Access Journals (Sweden)

    M. Bush

    2004-06-01

    Full Text Available A combination of medetomidine hydrochloride (medetomidine and ketamine hydrochloride (ketamine was evaluated in 16 boma-confined and 19 free-ranging impalas (Aepyceros melampus to develop a non-opiate immobilisation protocol. In free-ranging impala a dose of 220 + 34 mg/kg medetomidine and 4.4 + 0.7 mg/kg ketamine combined with 7500 IU of hyaluronidase induced recumbency within 4.5+1.5 min, with good muscle relaxation, a stable heart rate and blood pH. PaCO2 was maintained within acceptable ranges. The animals were hypoxic with reduced oxygen saturation and low PaO2 in the presence of an elevated respiration rate, therefore methods for respiratory support are indicated. The depth of sedation was adequate for minor manipulations but additional anaesthesia is indicated for painful manipulations. Immobilisation was reversed by 467 + 108 mg/kg atipamezole hydrochloride (atipamezole intramuscularly, but re-sedation was observed several hours later, possibly due to a low atipamezole:medetomidine ratio of 2:1. Therefore, this immobilisation and reversal protocol would subject impalas to possible predation or conspecific aggression following reversal if they were released into the wild. If the protocol is used on free-ranging impala, an atipamezole:medetomidine ratio of 5:1 should probably be used to prevent re-sedation.

  18. Induced chromosomal aberrations in somatic cells of Nigella sativa L. by mitomycin C.

    Science.gov (United States)

    Kumar, P; Nizam, J

    1978-01-01

    A cytological study was carried out on root tips of Nigella sativa L. by treatment with Mitomycin C at 0.001% for six time intervals (10, 15, 20, 30, 40, and 50 min). The chromosomal abnormalities were increasingly proportionate to the increase in time of treatment. The seedlings treated with a 0.001% concentration of Mitomycin C for 10 min. did not show any significant effect. At other time intervals, the effect was observed to be quite significant. Beyond 40 min. treatment almost all the cells would become sticky. Thirty minutes' treatment showed significant effect, inducing various types of chromosomal aberrations in the anaphase, such as bridges and fragments of 34.13% and 48.07%, respectively.

  19. Preparation of venlafaxine hydrochloride sustained-release tablets

    Directory of Open Access Journals (Sweden)

    GUO Lingling

    2013-08-01

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

  20. Commentary on "Optimal schedule of bacillus Calmette-Guérin for non-muscle-invasive bladder cancer: A meta-analysis of comparative studies." Zhu S, Tang Y, Li K, Shang Z, Jiang N, Nian X, Sun L, Niu Y, Department of Urology Tianjin Institute of Urology, 2nd Hospital of Tianjin Medical University, People's Republic of China.: BMC Cancer 2013; 13:332. doi:10.1186/1471-2407-13-332.

    Science.gov (United States)

    See, William A

    2014-11-01

    To explore the necessity of maintenance, efficacy of low-dose and superiority of various combination therapies of Bacillus Calmette-Guérin (BCG) in treatment of superficial bladder cancer (BCa). Comprehensive searches of electronic databases (PubMed, Embase, and the Cochrane Library), were performed, then a systematic review and cumulative meta-analysis of 21 randomized, controlled trials (RCTs) and 9 retrospective comparative studies were carried out according to, predefined inclusion criteria. Significantly better recurrence-free survivals (RFS) were observed respectively in patients who received BCG maintenance, standard-dose and BCG plus epirubicin therapy comparing to those received induction, low-dose and BCG alone. BCG maintenance therapy was also associated with significantly better progression-free survival (PFS), but there were more incidences of adverse events. Pooled results showed no remarkable advantage of BCG combined with Mitomycin C or with interferon α-2b in improving oncologic outcomes. Sensitivity-analyses stratified by study-design and tumor stage led to very similar overall results and often to a decrease of the between-study heterogeneity. Our data confirmed that non-RCT only affected strength rather than direction of the overall results. All patients with superficial BCa should be encouraged to accept BCG maintenance therapy with standard-dose if well tolerated. Patients can benefit from BCG combined with epirubicin but not from BCG combined with Mitomycin C or interferon α-2b. Copyright © 2014 Elsevier Inc. All rights reserved.

  1. Controlled release of mitomycin C from PHEMAH-Cu(II) cryogel membranes.

    Science.gov (United States)

    Bakhshpour, Monireh; Yavuz, Handan; Denizli, Adil

    2018-02-19

    Molecular imprinting technique was used for the preparation of antibiotic and anti-neoplastic chemotherapy drug (mitomycin C) imprinted cryogel membranes (MMC-ICM). The membranes were synthezied by using metal ion coordination interactions with N-methacryloyl-(l)-histidine methyl ester (MAH) functional monomer and template molecules (i.e. MMC). The 2-hydroxyethyl methacrylate (HEMA) monomer and methylene bisacrylamide (MBAAm) crosslinker were used for the preparation of mitomycin C imprinted cryogel membranes by radical suspension polymerization technique. The imprinted cryogel membranes were characterized by scanning electron microscopy (SEM), Brunauer-Emmett-Teller (BET), Fourier transform infrared spectroscopy-attenuated total reflectance (FTIR-ATR) and swelling degree measurements. Cytotoxicity of MMC-ICMs was investigated using mouse fibroblast cell line L929. Time-dependent release of MMC was demonstrated within 150 h from cryogel membranes. Cryogels demonstrated very high MMC loading efficiency (70-80%) and sustained MMC release over hours.

  2. Phase II study of short-time oxaliplatin, capecitabine and epirubicin (EXE) as first-line therapy in patients with non-resectable gastric cancer

    DEFF Research Database (Denmark)

    Schonnemann, K.R.; Jensen, H.A.; Yilmaz, M.

    2008-01-01

    Epirubicin, cisplatin and continuous infusion of 5-FU is a widely used palliative regimen in patients with gastric cancer. If cisplatin is substituted by oxaliplatin and 5-FU by capecitabine this regimen can be administered in the outpatient setting. Dose-limiting toxicity of oxaliplatin...... is peripheral sensory neuropathy and it is recommended to give oxaliplatin as a 120 min infusion. However, in patients with colorectal cancer a 30 min infusion of oxaliplatin can safely be administered without increasing neurotoxicity, standard infusion time is 30 min at our departments. In our phase I study...... the recommended doses of EXE was established (Dupont et al, 2006). Patients with non-resectable gastric adenocarcinoma were eligible. Patients received EXE (epirubicin 50 mg m(-2) day 1; capecitabine 1000 mg m(-2) day(-1) continuously and oxaliplatin 130 mg m(-2) day 1) as outpatient therapy every third week...

  3. 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.

  4. 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.

  5. Improved outcome from substituting methotrexate with epirubicin: results from a randomised comparison of CMF versus CEF in patients with primary breast cancer

    DEFF Research Database (Denmark)

    Ejlertsen, Bent Laursen; Mouridsen, Henning T; Jensen, Maj-Britt

    2007-01-01

    We compared the efficacy of CEF (cyclophosphamide, epirubicin, and fluorouracil) against CMF (cyclophosphamide, methotrexate, and fluorouracil) in moderate or high risk breast cancer patients. We randomly assigned 1224 patients with completely resected unilateral breast cancer to receive nine...... breast cancer without subsequent increase in late toxicities...

  6. One-electron reduction of mitomycin c by rat liver : role of cytochrome P-450 and NADPH-cytochrome P-450 reductase

    NARCIS (Netherlands)

    Vromans, R M; Van de Straat, R; Groeneveld, M.; Vermeulen, N P

    1. The role of cytochrome P-450 in the one-electron reduction of mitomycin c was studied in rat hepatic microsomal systems and in reconstituted systems of purified cytochrome P-450. Formation of H2O2 from redox cycling of the reduced mitomycin c in the presence of O2 and the alkylation of

  7. Ifosfamide, mesna and epirubicin as second-line chemotherapy in advanced breast cancer.

    Science.gov (United States)

    Kiraz, S; Baltali, E; Güler, N; Barista, I; Benekli, M; Celik, I; Güllü, I H; Kars, A; Tekuzman, G; Firat, D

    1996-08-01

    The ifosfamide, mesna and epirubicin (IMEpi) combination is administered to 16 patients having advanced metastatic breast carcinoma as second-line chemotherapy. We observed complete response in 6%, partial response in 44% (total overall response rate of 50%), stable disease in 12% and progressive disease in the remaining 38% of the patients. The median remission duration in responders was calculated to be 9.6 months. IMEpi regimen had a tolerable toxicity profile including alopecia, nausea and vomiting, microscopic hematuria, leukopenia and neurotoxicity in which serious complications necessitating discontinuation of the chemotherapy were not encountered. It might be concluded that IMEpi chemotherapy combination is an effective alternative among schedules in the management of patients with stage IV breast carcinoma without serious side effects.

  8. Spectrophotometric determination of procainamide hydrochloride using sodium periodate

    Directory of Open Access Journals (Sweden)

    S. Al-Tamrah

    2015-09-01

    Full Text Available A simple spectrophotometric method has been described for the determination of procainamide hydrochloride. The method is based on the oxidation of procainamide hydrochloride by sodium periodate in the presence of sulfuric acid and measurement of the absorbance of the violet color formed at 531 nm. Parameters affecting the reaction were studied and conditions were optimized. Linear calibration graph was obtained from 50 to 700 μg ml−1 of procainamide hydrochloride and the limit of detection was 25 μg ml−1. The method was successfully applied for the determination of procainamide hydrochloride in pharmaceutical preparation.

  9. 21 CFR 520.1660c - Oxytetracycline hydrochloride tablets/boluses.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride tablets/boluses. 520....1660c Oxytetracycline hydrochloride tablets/boluses. (a) Specifications. Each tablet or bolus contains 250, 500, or 1,000 milligrams of oxytetracycline hydrochloride. (b) Sponsors. For sponsors in § 510...

  10. Comparative Efficacy Of 1% Terbinafine Hydrochloride And 1% Butenafine Hydrochloride Cream In The Treatment Of Tinea Cruris

    Directory of Open Access Journals (Sweden)

    Rathi Sanjay K

    2001-01-01

    Full Text Available The aim of the study was to evaluate the comparative efficacy of 1% terbinafine hydrochloride and 1% butenafine hydrochloride cream in the treatment of Tinea cruris, was done taking with ten patients in each study group. They were found to be equipotent in one and two weeks treatment respectively.

  11. A randomized study of accelerated fractionation radiotherapy with and without mitomycin C in the treatment of locally advanced head and neck cancer

    DEFF Research Database (Denmark)

    Ezzat, M.; Shouman, T.; Zaza, K.

    2005-01-01

    Objectives: This single-institution study evaluates the feasibility of accelerated fractionation radiotherapy (AF) with and without mitomycin C (MMC) in the treatment of locally advanced head and neck cancer. Patients and Methods: Between May 1998 and October 2001, sixty patients with locally...... advanced stage III and IV of head and neck cancer were randomized into three treatment arms: (1) conventional fractionation radiotherapy (CF) (5 fractions per week); (2) accelerated fractionation radiotherapy (AF) (6 fractions per week); and (3) AF plus Mitomycin C (MMC). Results: The 2-year overall....... Key Words: Head and Neck cancer , Radiotherapy , Altered fractionation , Mitomycin C....

  12. Thermodynamic studies of drug–α-cyclodextrin interactions in water at 298.15 K: Procaine hydrochloride/lidocaine hydrochloride/tetracaine hydrochloride/ranitidine hydrochloride + α-cyclodextrin + H2O systems

    International Nuclear Information System (INIS)

    Shaikh, Vasim R.; Terdale, Santosh S.; Hundiwale, Dilip G.; Patil, Kesharsingh J.

    2014-01-01

    Graphical abstract: The encapsulation of guest tetracaine hydrochloride TC·HCl (C 15 H 24 N 2 O 2 ·HCl), in α-cyclodextrin cavities in aqueous solutions at 298.15 K. -- Highlights: • The osmotic coefficient measurements are reported for PC·HCl/LC·HCl/TC·HCl/RT·HCl + 0.1 m α-CD + water at 298.15 K. • The concentration variation of mean activity coefficients of drug molecules in water–α-CD solutions has been studied. • The transfer Gibbs free energies have been calculated using the activity data. • Pair and triplet interaction parameters and equilibrium constant (log K) values are also estimated. • The results are discussed with emphasis on host–guest interaction concepts. -- Abstract: The osmotic coefficient measurements have been carried out for ternary aqueous solutions containing a fixed concentration of α-cyclodextrin (α-CD) of ∼0.1 mol · kg −1 and varying the concentrations (∼0.012 to ∼0.21 mol · kg −1 ) of drugs Procaine hydrochloride (PC·HCl), Lidocaine hydrochloride (LC·HCl), Tetracaine hydrochloride (TC·HCl) and Ranitidine hydrochloride (RT·HCl) at 298.15 K using vapour pressure osmometry. The water activities for each ternary system were measured and used to obtain the activity coefficients of α-cyclodextrin (α-CD) and drugs following the methodology developed by Robinson and Stokes for isopiestic measurements. The transfer Gibbs free energies of electrolyte (or drug) from water to an aqueous nonelectrolyte (α-CD) solutions (ΔG tr E ) and that of nonelectrolyte (α-CD) from water to an aqueous electrolyte (or drug) solutions (ΔG tr N ) have been calculated using the activity data. These were further used for the estimation of pair and triplet interaction parameters. By applying the method based on the application of the McMillan–Mayer theory of virial coefficients to transfer free energy data, the salting constant (k s ) values have been estimated at 298.15 K. The equilibrium constant (log K) values for the

  13. Preparation and evaluation of doxycycline hydrochloride and bromhexine hydrochloride dosage forms for pigeons / Marga le Roux

    OpenAIRE

    Le Roux, Marga

    2004-01-01

    Objective: To prepare and evaluate three different dosage forms, containing doxycycline hydrochloride (HCI) and bromhexine hydrochloride (HCI) respectively and in combination, for the treatment of respiratory diseases in pigeons. Background: Birds have held a place in man's affection since the ancient Egyptians and Romans kept birds. Europeans have successfully bred birds, especially smaller birds and pigeons, for centuries. Only in recent years, however, have science and me...

  14. Two simple amine hydrochlorides from the soft coral Lobophytum strictum

    Digital Repository Service at National Institute of Oceanography (India)

    Parameswaran, P.S.; Naik; Das, B.; Kamat, S.Y.

    Two simple amine hydrochlorides, viz., 1-amino-1, 1-dimethyl-3-oxo-butane hydrochloride (1) (Diacetonamine) and 2, 2, 6, 6-tetramethylpiperidone hydrochloride (2) have been isolated from the fraction of the methanolic extract of the soft coral...

  15. Degree of corneal anaesthesia after topical application of 0.4% oxybuprocaine hydrochloride and 0.5% proparacaine hydrochloride ophthalmic solution in clinically normal cattle.

    Science.gov (United States)

    Little, W B; Jean, G St; Sithole, F; Little, E; Jean, K Yvorchuk-St

    2016-06-01

    The use of corneal anaesthesia is necessary for a range of clinical purposes. Therefore, we assessed and compared the efficacy of corneal anaesthesia after application of 0.4% oxybuprocaine hydrochloride and 0.5% proparacaine hydrochloride ophthalmic solution in clinically normal cattle. The 24 clinically normal cows were allocated into two groups. Cows in group 1 (n = 12) received 0.2 mL of 0.4% oxybuprocaine hydrochloride with fluorescein ophthalmic solution in one eye and 0.2 mL of sterile saline (0.9% NaCl) with fluorescein in the contralateral eye (control). Group 2 (n = 12) received 0.2 mL of 0.4% oxybuprocaine hydrochloride with fluorescein ophthalmic solution in one eye and 0.2 mL of 0.5% proparacaine hydrochloride with fluorescein in the contralateral eye (control). In each group, corneal touch threshold was determined by Cochet-Bonnet aesthesiometer for both eyes immediately prior to topical administration of solutions, at 1 min and 5 min after administration of topical solutions and every 5 min thereafter for a total of 75 min. Significant corneal anaesthesia was noted immediately following topical application of both oxybuprocaine and proparacaine as compared with controls, with maximal corneal anaesthesia noted 1 min after administration. Both oxybuprocaine and proparacaine produced significant corneal anaesthesia for the duration of the 75-min study. Neither oxybuprocaine hydrochloride nor proparacaine hydrochloride treatment resulted in visible adverse effects. There are limited data available demonstrating the efficacy and duration of corneal anaesthetic agents in cattle. Both oxybuprocaine hydrochloride and proparacaine hydrochloride should be considered practical options for providing corneal anaesthesia in cattle in a clinical setting. © 2016 Australian Veterinary Association.

  16. 21 CFR 524.1662a - Oxytetracycline hydrochloride and hydrocortisone spray.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride and hydrocortisone... NEW ANIMAL DRUGS § 524.1662a Oxytetracycline hydrochloride and hydrocortisone spray. (a) Specifications. Each 3-ounce unit of oxytetracycline hydrochloride and hydrocortisone spray contains 300...

  17. [Response of HeLa cells to mitomycine C. III. The analysis of nucleoli of mother and daughter cells].

    Science.gov (United States)

    Petrov, Iu P; Neguliaev, Iu A; Tsupkina, N V

    2014-01-01

    The comparative analysis of the number of nucleoli in cells of the established HeLa-M line was carried out before and after exposure to mitomycin C in a concentration of 10 μg/ml for 2 h. Using time-lapse microscopy, nucleoli in mother and their respective daughter cells were computed. It has been shown that the average number of nucleoli per cell is generally higher in daughter cells than in mother cells, and a standard deviation, on the contrary, decreases. An average number of nucleoli in daughter cells, whose mother cells had been treated with mitomycin C, was higher than in corresponding cells of control group. The separate analysis has been performed for the cells having from 1 to 4 nucleoli. Nonrandom complete coincidence of the number of nucleoli in mather and daughter cells has been typicaly shown for about 1/7 of the total cell population. Mitomycin C reduces this value of about 1.5 times.

  18. Sensitivity of pathogenic and free-living Leptospira spp. to UV radiation and mitomycin C

    International Nuclear Information System (INIS)

    Stamm, L.V.; Charon, N.W.

    1988-01-01

    The habitats for the two major Leptospira spp. differ. The main habitat of L. biflexa is soil and water, whereas L. interrogans primarily resides in the renal tubules of animals. We investigated whether these two species, along with L. illini (species incertae sedis), differ with respect to their sensitivity to UV radiation. The doses of UV resulting in 37, 10 and 1% survival were determined for representive serovars from each species. L. interrogans serovar pomona was 3.0 to 4.8 times more sensitive to UV than the other Leptospira species under the 37, 10, and 1% survival parameters. In comparison to other bacteria, L. interrogans serovar pomona is among the most sensitive to UV. In a qualitative UV sensitivity assay., L. interrogans serovars were found to be in general more sensitive than L. biflexa serovars. All three species were found to have a photoreactivation DNA repair mechanism. Since organisms that are resistant to UV are often resistant to the DNA cross-linking agent mitomycin C, we tested the relative sensitivity of several Leptospira serovars to this compound. With few exceptions, L. biflexa and L. illini serovars were considerably more resistant to mitomycin C than the L. interrogans serovars. The mitomycin C sensitivity assay could be a useful addition to current characterization tests used to differentiate the Leptospira species

  19. Sensitivity of pathogenic and free-living Leptospira spp. to UV radiation and mitomycin C

    Energy Technology Data Exchange (ETDEWEB)

    Stamm, L.V.; Charon, N.W.

    1988-03-01

    The habitats for the two major Leptospira spp. differ. The main habitat of L. biflexa is soil and water, whereas L. interrogans primarily resides in the renal tubules of animals. We investigated whether these two species, along with L. illini (species incertae sedis), differ with respect to their sensitivity to UV radiation. The doses of UV resulting in 37, 10 and 1% survival were determined for representive serovars from each species. L. interrogans serovar pomona was 3.0 to 4.8 times more sensitive to UV than the other Leptospira species under the 37, 10, and 1% survival parameters. In comparison to other bacteria, L. interrogans serovar pomona is among the most sensitive to UV. In a qualitative UV sensitivity assay., L. interrogans serovars were found to be in general more sensitive than L. biflexa serovars. All three species were found to have a photoreactivation DNA repair mechanism. Since organisms that are resistant to UV are often resistant to the DNA cross-linking agent mitomycin C, we tested the relative sensitivity of several Leptospira serovars to this compound. With few exceptions, L. biflexa and L. illini serovars were considerably more resistant to mitomycin C than the L. interrogans serovars. The mitomycin C sensitivity assay could be a useful addition to current characterization tests used to differentiate the Leptospira species.

  20. Accelerometric comparison of the locomotor pattern of horses sedated with xylazine hydrochloride, detomidine hydrochloride, or romifidine hydrochloride.

    Science.gov (United States)

    López-Sanromán, F Javier; Holmbak-Petersen, Ronald; Varela, Marta; del Alamo, Ana M; Santiago, Isabel

    2013-06-01

    To evaluate the duration of effects on movement patterns of horses after sedation with equipotent doses of xylazine hydrochloride, detomidine hydrochloride, or romifidine hydrochloride and determine whether accelerometry can be used to quantify differences among drug treatments. 6 healthy horses. Each horse was injected IV with saline (0.9% NaCl) solution (10 mL), xylazine diluted in saline solution (0.5 mg/kg), detomidine diluted in saline solution (0.01 mg/kg), or romifidine diluted in saline solution (0.04 mg/kg) in random order. A triaxial accelerometric device was used for gait assessment 15 minutes before and 5, 15, 30, 45, 60, 75, 90, 105, and 120 minutes after each treatment. Eight variables were calculated, including speed, stride frequency, stride length, regularity, dorsoventral power, propulsive power, mediolateral power, and total power; the force of acceleration and 3 components of power were then calculated. Significant differences were evident in stride frequency and regularity between treatments with saline solution and each α2-adrenoceptor agonist drug; in speed, dorsoventral power, propulsive power, total power, and force values between treatments with saline solution and detomidine or romifidine; and in mediolateral power between treatments with saline solution and detomidine. Stride length did not differ among treatments. Accelerometric evaluation of horses administered α2-adrenoceptor agonist drugs revealed more prolonged sedative effects of romifidine, compared with effects of xylazine or detomidine. Accelerometry could be useful in assessing the effects of other sedatives and analgesics. Accelerometric data may be helpful in drug selection for situations in which a horse's balance and coordination are important.

  1. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent lidocaine...

  2. Spectrophotometric determination of procainamide hydrochloride using sodium periodate

    OpenAIRE

    Al-Tamrah, S.; Al-Abbad, S.

    2015-01-01

    A simple spectrophotometric method has been described for the determination of procainamide hydrochloride. The method is based on the oxidation of procainamide hydrochloride by sodium periodate in the presence of sulfuric acid and measurement of the absorbance of the violet color formed at 531 nm. Parameters affecting the reaction were studied and conditions were optimized. Linear calibration graph was obtained from 50 to 700 μg ml−1 of procainamide hydrochloride and the limit of detection wa...

  3. Development of method of tritium labeling of pharmacological preparate of drotaverine hydrochloride (NOSPA)

    International Nuclear Information System (INIS)

    Kim, A.A.; Djuraeva, G.T.; Shukurov, B.V.

    2004-01-01

    Full text: The method for tritium labeling of pharmacological preparate of drotaverine hydrochloride (no spa) was developed. Drotaverine hydrochloride was labeled by thermally activated tritium in apparatus for tritium labeling. The optimum regime of labeling was selected. The system of purification of tritium labeled drotaverine hydrochloride by thin layer chromatography (TLC) has been developed. The TLC system of purification of tritium labeled drotaverine hydrochloride was developed. Tritium labeled preparation of drotaverine hydrochloride was purified by TLC on silicagel in system isopropanol: ammonia: water (8:1:1). We found appearance of additional fractions in tritium labeled preparation of drotaverine hydrochloride that testifies to partial transformation of drotaverine hydrochloride during procedure of labeling. Application of TLC for purification of tritium labeled preparation allows to purify completely drotaverine hydrochloride of by-products. The output of purified tritium labeled preparation of drotaverine hydrochloride was about 25 %. The received preparation had specific radioactivity - 3,2 MBq/mg, radiochemical purity of a preparation was 95 %. TLC purification seems inexpensive, fast and suitable for purification of tritium-labeled drotaverine hydrochloride. Thus developed method allows obtain tritium labeled preparation of drotaverine hydrochloride (no - spa), suitable for medical and biologic researches

  4. Use of a simian virus 40-based shuttle vector to analyze enhanced mutagenesis in mitomycin C-treated monkey cells

    International Nuclear Information System (INIS)

    Roilides, E.; Munson, P.J.; Levine, A.S.; Dixon, K.

    1988-01-01

    When monkey cells were treated with mitomycin C 24 h before transfection with UV-irradiated pZ189 (a simian virus 40-based shuttle vector), there was a twofold increase in the frequency of mutations in the supF gene of the vector. These results suggest the existence of an enhancible mutagenesis pathway in mammalian cells. However, DNA sequence analysis of the SupF- mutants suggested no dramatic changes in the mechanisms of mutagenesis due to mitomycin C treatment of the cells

  5. Corneal melanosis successfully treated using topical mitomycin-C and alcohol corneal epitheliectomy: a 3-year follow-up case report

    Directory of Open Access Journals (Sweden)

    Mehmet Balcı

    2015-08-01

    Full Text Available ABSTRACTWe report a case of primary acquired corneal melanosis without atypia associated with corneal haze in a patient with a history of limbal malignant melanoma and the effect of mitomycin-C. A 75-year-old woman with a history of limbal malignant melanoma presented with loss of vision in right eye. Corneal examination showed a patchy melanotic pigmentation with a central haze. Topical mitomycin-C improved visual acuity and corneal haze. However, the pigmented lesions persisted, and they were removed with alcohol corneal epitheliectomy. Histopathological examination demonstrated primary acquired melanosis without atypia. The lesions were successfully removed, and there were no recurrences during the follow-up period of 36 months. The association of conjunctival and corneal melanosis without atypia is a rare condition. In addition, co-existence of central corneal haze and melanosis may decrease visual acuity. Topical mitomycin-C and alcohol corneal epitheliectomy can be useful treatments in this condition.

  6. Comparison of the effectiveness and toxicity of neoadjuvant chemotherapy regimens, capecitabine/epirubicin/cyclophosphamide vs 5-fluorouracil/epirubicin/cyclophosphamide, followed by adjuvant, capecitabine/docetaxel vs docetaxel, in patients with operable breast cancer

    Directory of Open Access Journals (Sweden)

    Zhang MM

    2016-06-01

    Full Text Available Minmin Zhang,* Wei Wei,* Jianlun Liu, Huawei Yang, Yi Jiang, Wei Tang, Qiuyun Li, Xiaoming Liao Department of Breast Surgery, Affiliated Tumor Hospital of Guangxi Medical University, Nanning, Guangxi, People’s Republic of China *These authors contributed equally to this work Abstract: The aim of this study was to compare the effectiveness and toxicity of neoadjuvant chemotherapy regimens, xeloda/epirubicin/cyclophosphamide (XEC vs 5-fluorouracil/epirubicin/cyclophosphamide (FEC, followed by adjuvant chemotherapy regimens, capecitabine/taxotere (XT vs taxotere (T, in axillary lymph node (LN-positive early-stage breast cancer. In this randomized, Phase III trial, 137 patients with operable primary breast cancer (T2-0, N0-1 who were tested axillary LN positive through aspiration biopsy of axillary LNs were randomized (1:1 to four 3-weekly cycles of XEC or FEC. Patients underwent surgery within 4–6 weeks after the fourth cycle, followed by four adjuvant cycles of 3-weekly XT or T. The primary end point was tumor pathological complete response. Toxicity profiles were secondary objectives. In total, 131 patients had clinical and radiological evaluation of response and underwent surgery. Treatment with XEC led to an increased rate of pathological complete response in primary tumor (18% vs 6%, respectively, P=0.027 and objective remission rate (87% vs 73%, P=0.048 compared to FEC. Clinical complete response occurred in 20% and 7% for XEC and FEC, respectively. Compared to FEC, XEC was associated with more hand-foot syndrome (57% vs 11%, P<0.001 and 3/4 grade nausea/vomiting/diarrhea (30% vs 14%, P=0.034 but less phlebitis (3% vs 14%, P=0.035. XT and T adjuvant chemotherapy regimens were well tolerated: treatment-related 3/4 grade adverse events occurred in 28% and 17% of patients receiving XT and T, respectively. Keywords: breast cancer, capecitabine, docetaxel, neoadjuvant chemotherapy, curative effect, toxic side effects

  7. 21 CFR 524.1982 - Proparacaine hydrochloride ophthalmic solution.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Proparacaine hydrochloride ophthalmic solution... SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524.1982 Proparacaine hydrochloride ophthalmic solution. (a) Specifications. The drug is...

  8. Phase II study of docetaxel in combination with epirubicin and protracted venous infusion 5-fluorouracil (ETF) in patients with recurrent or metastatic breast cancer. A Yorkshire breast cancer research group study.

    Science.gov (United States)

    Humphreys, A C; Dent, J; Rodwell, S; Crawford, S M; Joffe, J K; Bradley, C; Dodwell, D; Perren, T J

    2004-06-01

    This study was originally designed as a phase I/II study, with a dose escalation of docetaxel in combination with epirubicin 50 mg m(-2) and 5-fluorouracil (5-FU) 200 mg m(-2) day(-1). However, as dose escalation was not possible, the study is reported as a phase II study of the combination to assess response and toxicity. A total of 51 patients with locally advanced or metastatic breast cancer were treated on this phase II study, with doses of docetaxel 50 mg m(-2), epirubicin 50 mg m(-2) and infusional 5-FU 200 mg m(-2) day(-1) for 21 days. The main toxicity of this combination was neutropenia with 89% of patients having grade 3 and 4 neutropenia, and 39% of patients experiencing febrile neutropenia. Nonhaematological toxicity was mild. The overall response rate in the assessable patients was 64%, with median progression-free survival of 38 weeks, and median survival of 70 weeks. The ETF regimen was found to be toxic, and it was not possible to escalate the dose of docetaxel above the first dose level. This regimen has therefore not been taken any further, but as a development of this a new study is ongoing, combining 3-weekly epirubicin, weekly docetaxel and capecitabine, days 1-14.

  9. Enhanced healing of mitomycin C-treated healing-impaired wounds in rats with PRP-containing fragmin/protamine microparticles (PRP&F/P MPs).

    Science.gov (United States)

    Takikawa, Megumi; Ishihara, Masayuki; Takabayashi, Yuki; Sumi, Yuki; Takikawa, Makoto; Yoshida, Ryuichi; Nakamura, Shingo; Hattori, Hidemi; Yanagibayashi, Satoshi; Yamamoto, Naoto; Kiyosawa, Tomoharu

    2015-04-13

    The purpose of this study was to evaluate the accelerating effects of platelet-rich plasma-containing (PRP&) fragmin/protamine microparticles (F/P MPs) for repairing mitomycin C-treated healing-impaired wounds. Staining with terminal deoxynucleotidyl transferase-mediated dUTP nick-end labelling (TUNEL-staining) showed that apoptosis of dermal fibroblast cells (DFCs) and epidermal keratinocyte cells (EKCs) were significantly induced in the skin of the mitomycin C-treated rats. Full-thickness skin defects were made on the back of rats and mitomycin C was applied on the wounds to prepare a healing-impaired wound. After washing out the mitomycin C, saline (control), F/P MPs alone, PRP alone, and PRP&F/P MPs were injected around the wounds. The rats were later euthanised and histological sections of the wounds were then prepared at indicated time periods after the treatment. These results indicated the numbers of large, medium, and small capillary lumens 7 days after injection of PRP&F/P MPs were significantly higher than those after injection of PRP or F/P MPs alone. Furthermore, epithelium and granulation tissue formations were significantly stimulated in the healing-impaired wounds treated with PRP&F/P MPs 3, 7 and 14 days after injection of PRP&F/P MPs.

  10. Systematic analysis of trimazolin hydrochloride as adrenergic vasoconstrictor

    Directory of Open Access Journals (Sweden)

    Nikolić Goran

    2008-01-01

    Full Text Available Trimazolin-hydrochloride, which is used as a pharmaceutically active component (adrenergic vasoconstrictor for the production of decongestive preparations, was investigated in this paper by performing systematic analysis. In domestic and foreign pharmacopoeias, as well as in scientific and patent literature, there are no data on trimazolin and the methods of its investigation. Systematic analysis involves two investigation phases. A complete physicochemical characterization of the synthesized substance was done by previous investigation. In the second phase, a chemical structure of the synthesized pharmacologically active substance was confirmed to a certain degree of certainty by using the absorption spectroscopic methods (FTIR, UV-VIS, 1H-NMR. The spectroscopic methods used proved to be successful at identifying and investigating the purity of trimazolin hydrochloride. Liquid (RP-HPLC chromatography was used for the analysis of trimazolin hydrochloride in the nasal preparation (Adrianol. The method of titrimetric analysis was developed with the aim of quantitative determination of trimazolin hydrochloride in decongestive preparations.

  11. 21 CFR 520.2345g - Tetracycline hydrochloride and sodium novobiocin tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tetracycline hydrochloride and sodium novobiocin... § 520.2345g Tetracycline hydrochloride and sodium novobiocin tablets. (a) Specifications. Each tablet contains the equivalent of 60 milligrams of tetracycline hydrochloride and 60 milligrams of novobiocin, or...

  12. RP-HPLC Estimation of Imipramine Hydrochloride and Diazepam in Tablets.

    Science.gov (United States)

    Srikantha, D; Raju, R R

    2015-01-01

    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 (hydrochloride and diazepam in tablets.

  13. Radical radiation therapy with 5-fluorouracil infusion and mitomycin C for oesophageal squamous carcinoma

    International Nuclear Information System (INIS)

    Keane, T.J.; Harwood, A.R.; Elhakim, T.; Rider, W.D.; Cummings, B.J.; Ginsberg, R.J.; Cooper, J.C.

    1985-01-01

    Thirty-five patients with clinically staged non-metastatic squamous carcinoma of the oesophagus were treated with radiation combined with mitomycin C, and 5-fluorouracil (5-FUra) infusion. Twenty patients were planned for a split course regimen 2250-2500 cGy in 10 fractions and chemotherapy. This dose of radiation to be repeated with another course of chemotherapy after 4 weeks rest. Fifteen patients were planned for a single course 4500-5000 cGy in 20 fractions and a single course of chemotherapy. Patients were matched for age, sex, TNM stage, and total radiation dose. There was a significant difference in survival p = 0.004 and local relapse-free rate p = 0.05 for patients receiving radiation and chemotherapy. We conclude that radiation combined with mitomycin C, and 5-FUra infusion appears to have a significant benefit compared to radiation as a single modality in the management of oesophageal squamous carcinoma. (orig.)

  14. Minocycline hydrochloride nanoliposomes inhibit the production of TNF-α in LPS-stimulated macrophages

    Directory of Open Access Journals (Sweden)

    Liu D

    2012-08-01

    Full Text Available D Liu, P S YangShandong Provincial Key Laboratory of Oral Biomedicine, College of Stomatology, Shandong University, Shandong Province, People's Republic of ChinaBackground: As an adjunctive treatment of chronic periodontitis, it seems that the application of periocline or the other antimicrobials is effective against periodontopathogens. In this study, nanoliposomes were investigated as carriers of minocycline hydrochloride and the inhibition effects of minocycline hydrochloride nanoliposomes on the proliferation and lipopolysaccharide (LPS-stimulated production of tumor necrosis factor-α (TNF-α of macrophages were elucidated.Methods: After stimulation with 10 µg/mL LPS, murine macrophages (ANA-1 were treated with 10, 20, 40, 50 and 70 µg/mL 2% minocycline hydrochloride nanoliposomes, minocycline hydrochloride solution, and periocline for 6, 12, 24, 48 and 60 hours, respectively. A tetrazolium (MTT assay was used to evaluate macrophages cell proliferation rate and the levels of TNF-α mRNA were measured by SYBR Green Real Time PCR.Results: Ten to 70 µg/mL 2% minocycline hydrochloride nanoliposomes, minocycline hydrochloride solution, and periocline showed dose- and time-dependent inhibition of ANA-1 proliferation. Minocycline hydrochloride nanoliposomes showed dose- and ratio-dependent inhibition of LPS-stimulated TNF-α secretion of ANA-1. The inhibition effect of 10 µg/mL minocycline hydrochloride nanoliposomes was significantly better than that of two positive control groups, and equated to that of 60 or 70 µg/mL periocline. The expression of TNF-α mRNA in experimental group continued to reduce linearly with time.Conclusion: All three preparations of minocycline hydrochloride showed dose- and time-dependent inhibition of proliferation of ANA-1. Minocycline hydrochloride nanoliposomes have stronger and longer inhibition effect on LPS-stimulated TNF-α secretion of macrophages cell than minocycline hydrochloride solution and periocline

  15. Developmental rates of immatures of three Chrysomya species (Diptera: Calliphoridae) under the effect of methylphenidate hydrochloride, phenobarbital, and methylphenidate hydrochloride associated with phenobarbital.

    Science.gov (United States)

    Rezende, Fábio; Alonso, Marcela A; Souza, Carina M; Thyssen, Patrícia J; Linhares, Arício X

    2014-05-01

    Entomotoxicology is focused on obtaining data on necrophagous entomofauna, for criminal investigations purposes. This study aimed to evaluate the effect of different concentrations of methylphenidate hydrochloride, phenobarbital, and their association on the developmental rate, larval and pupal survivorship, and the interval of emergence of adults of Chrysomya albiceps (Wiedemann), Chrysomya megacephala (Fabricius), and Chrysomya putoria (Wiedemann) (Diptera: Calliphoridae). Considering the therapeutic dose (TD) of methylphenidate hydrochloride (0.29 mg/Kg), the concentrations tested were 10× TD, 50× TD, and 100× TD. For phenobarbital, the concentrations used were 1× TD (=150 mg/Kg), 3.3× TD, and 6.7× TD. For the association of the drugs, the combinations used were 10× TD-methylphenidate hydrochloride plus 1× TD-phenobarbital, 50× TD-methylphenidate hydrochloride plus 3.3× TD-phenobarbital, and 100× TD-methylphenidate hydrochloride plus 6.7× TD-phenobarbital. The control group, without addition of drug, was maintained under the same conditions of temperature (25 ± 1 °C), humidity (70 ± 10%), and photoperiod (12 h). Specimens of each group were weighed every 12 h until pupariation. The developmental rate of the three Chrysomya species immatures was monitored. For C. albiceps the developmental time was delayed in 24 h for methylphenidate hydrochloride group and in 12 h for the phenobarbital and the drugs association groups. The effect was observed only at specific ages for C. megacephala, without altering the developmental time. For C. putoria, the developmental time was delayed in 12 h for methylphenidate hydrochloride group and in 24 h for the phenobarbital and the drugs association groups. The emergence interval was similar among all experimental groups, but larval and pupal viabilities were affected in different ways.

  16. Tetrathiomolybdate sensitizes ovarian cancer cells to anticancer drugs doxorubicin, fenretinide, 5-fluorouracil and mitomycin C

    International Nuclear Information System (INIS)

    Kim, Kyu Kwang; Lange, Thilo S; Singh, Rakesh K; Brard, Laurent; Moore, Richard G

    2012-01-01

    Our recent study showed that tetrathiomolybdate (TM), a drug to treat copper overload disorders, can sensitize drug-resistant endometrial cancer cells to reactive oxygen species (ROS)-generating anticancer drug doxorubicin. To expand these findings in the present study we explore TM efficacy in combination with a spectrum of ROS-generating anticancer drugs including mitomycin C, fenretinide, 5-fluorouracil and doxorubicin in ovarian cancer cells as a model system. The effects of TM alone or in combination with doxorubicin, mitomycin C, fenretinide, or 5-fluorouracil were evaluated using a sulforhodamine B assay. Flow cytometry was used to detect the induction of apoptosis and ROS generation. Immunoblot analysis was carried out to investigate changes in signaling pathways. TM potentiated doxorubicin-induced cytotoxicity and modulated key regulators of apoptosis (PARP, caspases, JNK and p38 MAPK) in SKOV-3 and A2780 ovarian cancer cell lines. These effects were linked to the increased production of ROS, as shown in SKOV-3 cells. ROS scavenging by ascorbic acid blocked the sensitization of cells by TM. TM also sensitized SKOV-3 to mitomycin C, fenretinide, and 5-fluorouracil. The increased cytotoxicity of these drugs in combination with TM was correlated with the activity of ROS, loss of a pro-survival factor (e.g. XIAP) and the appearance of a pro-apoptotic marker (e.g. PARP cleavage). Our data show that TM increases the efficacy of various anticancer drugs in ovarian cancer cells in a ROS-dependent manner

  17. Effect of donepezil hydrochloride on normal-tension glaucoma

    International Nuclear Information System (INIS)

    Yoshida, Yukiko; Sugiyama, Tetsuya; Ikeda, Tsunehiko; Utsunomiya, Keita; Ogura, Yasuharu; Narabayashi, Isamu

    2007-01-01

    Peroral donepezil hydrochloride is claimed to be effective for Alzheimer disease, by elevating concentration of acetylcholine in the brain resulting in improved recognition and intracerebral circulation. It has been reported that some cases of normal-tension glaucoma (NTG) show cerebral circulation similar to patients of Alzheimer disease. The purpose of this study was to evaluate the effect of donepezil hydrochloride on NTG. This study was made on 10 eyes of 5 NTG patients who showed cerebral circulation similar to Alzheimer disease by 123 I-iofetamine (IMP) single photon emission computed tomography (SPECT). The series comprised 3 males and 2 females. Their age ranged from 64 to 79 years, average 69 years. They were given donepezil hydrochloride at the daily dosis of 5 mg for 6 months. Circulation in the optic nervehead was measured by laser speckle flowmetry. Circulation in the brain and optic nervehead significantly increased after 6 months of treatment. MD value by Humphrey tonometer improved in 5 eyes (50%). There was no change in intraocular pressure. Peroral donepezil hydrochloride may improve optic neuropathy in NTG through its neuroprotective action. (author)

  18. 21 CFR 524.1662b - Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride, polymyxin B sulfate... DOSAGE FORM NEW ANIMAL DRUGS § 524.1662b Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment. (a) Specifications. Each gram of the ointment contains oxytetracycline hydrochloride equivalent...

  19. FORMULATION AND EVALUATION OF ISONIAZID AND ETHAMBUTOL HYDROCHLORIDE COMBINATION TABLETS

    OpenAIRE

    Margret Chandira R; Jayakar B; Palanisamy P.

    2012-01-01

    Ethambutol hydrochloride and Isoniazid Drugs are used as Antituberculosis agents. It is mainly used in the initial Treatment of pulmonary tuberculosis. Here in present study compressed tablet of Ethambutol hydrochloride and Isoniazid prepared by using HPMC, HPC, and PVPK -30 as binders. Compressed tablets of Ethambutol hydrochloride and Isoniazid were prepared by wet granulation method. Among different trials of F1 to F9 with wet granulation, the trial F1 showed satisfactory in-vitro drug re...

  20. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms. ...

  1. Human serum paraoxonase-1 (hPON1): in vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium.

    Science.gov (United States)

    Türkeş, Cüneyt; Söyüt, Hakan; Beydemir, Şükrü

    2015-01-01

    In this study, we investigated the effects of antibacterial drugs (moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium) on human serum paraoxonase-1 (hPON1) enzyme activity from human serum in vitro conditions. For this purpose, hPON1 enzyme was purified from human serum using simple chromatographic methods. The antibacterial drugs exhibited inhibitory effects on hPON1 at low concentrations. Ki constants were calculated to be 2.641 ± 0.040 mM, 5.525 ± 0.817 mM, 35.092 ± 1.093 mM, 252.762 ± 5.749 mM and 499.244 ± 10.149 mM, respectively. The inhibition mechanism of moxifloxacin hydrochloride was competitive, whereas levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium were noncompetitive inhibitors.

  2. NEEDLE REVISION WITH MITOMYCIN-C IN ENCAPSULATED BLEBS

    Directory of Open Access Journals (Sweden)

    R Zarei

    2008-08-01

    Full Text Available "nThe most common cause of failure during the first trimester after trabeculectomy is encapsulated bleb and needling bleb revision is a less invasive method in the management of refractory cases. The purpose of this study is to determine the efficacy and safety of mitomycin-C (MMC augmented bleb revision of failed filtration surgery. This study is a before-after (paired observation. 33 patients with failed trabeculectomy because of bleb encapsulation, whose intraocular pressure (IOP was not reduced under 21 mmHg despite of medications and digital massage , underwent needling bleb revision and subconjunctival injection of 0.1 ml MMC (0.4 mg/ml.The mean follow-up time was 9.24 ± 5.27 months (1-20 months. Statistical analysis of the data included the paired two-tailed Student's t test for preoperative and postoperative IOP and number of medications. 36 needling procedures (mean, 1.09 ± 0.21 revisions per eye were performed on 33 eyes. Patients were between 10-80 years old (mean, 45.67 ± 22.41 years and mean follow-up was 9.24 ± 5.27 months. IOP decreased from 29.06 ± 5.03 mmHg to 18.21 ± 6.76 mmHg at last follow-up (P= 0.000. Antiglaucoma medications decreased from 2.18 ± 0.58 to 1.36 ± 0.29 at last follow-up (P= 0.000.Overall, 6 (18.2% of 33 cases achieved a complete success and 20 (60.6% of cases achieved a qualified success. The complications of this procedure were subconjunctival hemorrhage (17 cases, hyphema (5 cases and conjunctival button hole (2 cases. Needling bleb revision with mitomycin-C appears to be an effective and relatively safe way to revive failed filtration surgery.

  3. Fundamentals of ionic conductivity relaxation gained from study of procaine hydrochloride and procainamide hydrochloride at ambient and elevated pressure.

    Science.gov (United States)

    Wojnarowska, Z; Swiety-Pospiech, A; Grzybowska, K; Hawelek, L; Paluch, M; Ngai, K L

    2012-04-28

    The pharmaceuticals, procaine hydrochloride and procainamide hydrochloride, are glass-forming as well as ionically conducting materials. We have made dielectric measurements at ambient and elevated pressures to characterize the dynamics of the ion conductivity relaxation in these pharmaceuticals, and calorimetric measurements for the structural relaxation. Perhaps due to their special chemical and physical structures, novel features are found in the ionic conductivity relaxation of these pharmaceuticals. Data of conductivity relaxation in most ionic conductors when represented by the electric loss modulus usually show a single resolved peak in the electric modulus loss M(")(f) spectra. However, in procaine hydrochloride and procainamide hydrochloride we find in addition another resolved loss peak at higher frequencies over a temperature range spanning across T(g). The situation is analogous to many non-ionic glass-formers showing the presence of the structural α-relaxation together with the Johari-Goldstein (JG) β-relaxation. Naturally the analogy leads us to name the slower and faster processes resolved in procaine hydrochloride and procainamide hydrochloride as the primary α-conductivity relaxation and the secondary β-conductivity relaxation, respectively. The analogy of the β-conductivity relaxation in procaine HCl and procainamide HCl with JG β-relaxation in non-ionic glass-formers goes further by the finding that the β-conductivity is strongly related to the α-conductivity relaxation at temperatures above and below T(g). At elevated pressure but compensated by raising temperature to maintain α-conductivity relaxation time constant, the data show invariance of the ratio between the β- and the α-conductivity relaxation times to changes of thermodynamic condition. This property indicates that the β-conductivity relaxation has fundamental importance and is indispensable as the precursor of the α-conductivity relaxation, analogous to the relation found

  4. Formulation and evaluation of tramadol hydrochloride rectal suppositories

    OpenAIRE

    Saleem M; Taher M; Sanaullah S; Najmuddin M; Ali Javed; Humaira S; Roshan S

    2008-01-01

    Rectal suppositories of tramadol hydrochloride were prepared using different bases and polymers like PEG, cocoa butter, agar and the effect of different additives on in vitro release of tramadol hydrochloride was studied. The agar-based suppositories were non-disintegrating/non-dissolving, whereas PEGs were disintegrating/dissolving and cocoa butter were melting suppositories. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content a...

  5. VEGF111b, a new member of VEGFxxxb isoforms and induced by mitomycin C, inhibits angiogenesis

    Energy Technology Data Exchange (ETDEWEB)

    Gu, Fang; Li, Xiuli [Department of Obstetrics and Gynecology, Chinese PLA General Hospital, Beijing (China); Kong, Jian [Department of Hepatobiliary Surgery, Beijing Chaoyang Hospital, Capital Medical University, Beijing (China); Pan, Bing [The Institute of Cardiovascular Sciences, Peking University Health Science Center, Key Laboratory of Molecular Cardiovascular Sciences of Education Ministry, Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides of Health Ministry, Beijing (China); Institute of Systems Biomedicine, School of Basic Medical Sciences, Peking University Health Science Center, Key Laboratory of Molecular Cardiovascular Sciences of Education Ministry, Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides of Health Ministry, Beijing (China); Sun, Min [Department of Obstetrics and Gynecology, Tangdu Hospital, Fourth Military Medical University, Xian (China); Zheng, Lemin, E-mail: zhengl@bjmu.edu.cn [The Institute of Cardiovascular Sciences, Peking University Health Science Center, Key Laboratory of Molecular Cardiovascular Sciences of Education Ministry, Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides of Health Ministry, Beijing (China); Institute of Systems Biomedicine, School of Basic Medical Sciences, Peking University Health Science Center, Key Laboratory of Molecular Cardiovascular Sciences of Education Ministry, Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides of Health Ministry, Beijing (China); Yao, Yuanqing, E-mail: yqyao@126.com [Department of Obstetrics and Gynecology, Chinese PLA General Hospital, Beijing (China)

    2013-11-08

    Highlights: •We discovered a new member of VEGFxxxb family-VEGF111b. •We found VEGF111b mRNA and protein can be induced by mitomycin C. •We confirmed VEGF111b over-expression inhibits angiogenesis. •VEGF111b inhibits angiogenesis through inhibiting VEGF-R2/PI3K/Akt and VEGF-R2/ERK1/2 phosphorylation. -- Abstract: Vascular endothelial growth factor (VEGF-A) stimulating angiogenesis is required for tumor growth and progression. The conventional VEGF-A isoforms have been considered as pro-angiogenic factors. Another family of VEGF-A isoforms generated by alternative splicing, termed VEGFxxxb isoforms, has anti-angiogenic property, exemplified by VEGF165b. Here, we identify a new number of VEGFxxx family-VEGF111b induced by mitomycin C, although not detected in mitomycin C-unexposed ovarian cancer cells. SKOV3 cells were transfected with pcDNA{sub 3.1} empty vector, pcDNA{sub 3.1}-VEGF111b or pcDNA{sub 3.1}-VEGF165b to collect conditioned mediums respectively. VEGF111b overexpression inhibits proliferation, migration and tube formation of endothelial cell by inhibiting VEGF-R2 phosphorylation and its downstream signaling, similar to VEGF165b but slightly lower than VEGF165b. The anti-angiogenic property depends on the six amino acids of exon 8b of the VEGFxxxb isoforms. Our results show that VEGF111b is a novel potent anti-angiogenic agent that can target the VEGF-R2 and its signaling pathway to inhibit ovarian tumor growth.

  6. VEGF111b, a new member of VEGFxxxb isoforms and induced by mitomycin C, inhibits angiogenesis

    International Nuclear Information System (INIS)

    Gu, Fang; Li, Xiuli; Kong, Jian; Pan, Bing; Sun, Min; Zheng, Lemin; Yao, Yuanqing

    2013-01-01

    Highlights: •We discovered a new member of VEGFxxxb family-VEGF111b. •We found VEGF111b mRNA and protein can be induced by mitomycin C. •We confirmed VEGF111b over-expression inhibits angiogenesis. •VEGF111b inhibits angiogenesis through inhibiting VEGF-R2/PI3K/Akt and VEGF-R2/ERK1/2 phosphorylation. -- Abstract: Vascular endothelial growth factor (VEGF-A) stimulating angiogenesis is required for tumor growth and progression. The conventional VEGF-A isoforms have been considered as pro-angiogenic factors. Another family of VEGF-A isoforms generated by alternative splicing, termed VEGFxxxb isoforms, has anti-angiogenic property, exemplified by VEGF165b. Here, we identify a new number of VEGFxxx family-VEGF111b induced by mitomycin C, although not detected in mitomycin C-unexposed ovarian cancer cells. SKOV3 cells were transfected with pcDNA 3.1 empty vector, pcDNA 3.1 -VEGF111b or pcDNA 3.1 -VEGF165b to collect conditioned mediums respectively. VEGF111b overexpression inhibits proliferation, migration and tube formation of endothelial cell by inhibiting VEGF-R2 phosphorylation and its downstream signaling, similar to VEGF165b but slightly lower than VEGF165b. The anti-angiogenic property depends on the six amino acids of exon 8b of the VEGFxxxb isoforms. Our results show that VEGF111b is a novel potent anti-angiogenic agent that can target the VEGF-R2 and its signaling pathway to inhibit ovarian tumor growth

  7. Floating Microparticulate Oral Diltiazem Hydrochloride Delivery ...

    African Journals Online (AJOL)

    Delivery System for Improved Delivery to Heart ... Conclusion: Microparticulate floating (gastroretentive) oral drug delivery system of diltiazem prepared ..... treatment of cardiac disease. ... hydrochloride-loaded mucoadhesive microspheres.

  8. Microencapsulation of tramadol hydrochloride and physicochemical evaluation of formulations

    International Nuclear Information System (INIS)

    Murtaza, G.; Ahmad, M.

    2009-01-01

    The present project involves the microencapsulation of tramadol hydrochloride with ethocel using a non-solvent addition coacervation technique. The concentration of ethocel was varied to get a prolonged release profile. Then microparticles were compressed into tablets to study the variation of drug release between the microparticles and tablets. The microparticles were off white, aggregated and irregular in morphology having good percentage entrapment efficiency and percentage production yield. Dissolution study was made using USP XXIV apparatus I and II respectively, in 900 ml double distilled water at 50 rpm maintained at 37 degree C. An Initial burst effect was noted in the drug release behavior. Polyisobutylene concentration affected inversely the rate of drug release from microparticles. Dissolution media and stirring speed affected insignificantly (p>.05) the release pattern. Tramadol hydrochloride tablets showed good stability and reproducibility. UV and FTIR spectroscopy and X-Ray diffractometry proved that tramadol hydrochloride was completely and uniformly distributed in ethocel with out any strong interaction. The mechanism of drug release was anomalous diffusion that was best fit to Higuchi's equation. It can be concluded that multi-unit, slow-release tramadol hydrochloride microparticles can be formulated efficiently with non-solvent addition coacervation technique using ethocel. (author)

  9. Radiotherapy, combined with simultaneous chemotherapy with mitomycin C and bleomycin for inoperable head and neck cancer--preliminary report

    International Nuclear Information System (INIS)

    Smid, Lojze; Lesnicar, Hotimir; Zakotnik, Brane; Soba, Erika; Budihna, Marjan; Furlan, Ladica; Zargi, Miha; Rudolf, Zvone

    1995-01-01

    Purpose: Prospectively designed randomized clinical study was undertaken to assess the efficacy of simultaneous application of irradiation, Mitomycin C, and Bleomycin in treatment of patients with inoperable head and neck carcinoma. Methods and Materials: Between March 1991 and October 1993, 49 patients with inoperable head and neck carcinoma were randomly assigned to receive either radiation therapy alone (group A) or radiotherapy combined with simultaneous application of Mitomycin C and Bleomycin (group B). Patients in both groups were irradiated five times weekly with 2 Gy to the total dose of 66-70 Gy. Chemotherapy regimen included intramuscular application of Bleomycin 5 units twice a week, with the planned dose being 70 units and Mitomycin C 15 mg/m 2 applied intravenously after delivery of 9-10 Gy of irradiation. The application of Mitomycin C was planned to be repeated on last day of radiotherapy in the dose of 10 mg/m 2 . In attempt to enhance the effect of chemotherapeutic drugs, patients in group B received also Nicotinamide, Chlorpromazine, and Dicoumarol. Results: The difference in complete response rate between both treatment groups (24% in group A and 63% in group B) was statistically significant (p = 0.015). The difference in response rate was much more pronounced in patients with oropharyngeal carcinoma only (18% in group A compared to 81% in group B; p = 0.0003), while for all other subgroups added together, there was observed no benefit of multidrug therapy. Median follow-up was 18 months. Disease-free survival of patients in group A (9%) was significantly lower then in group B (48%) (p 0.001). The difference between both treatment groups was even greater in patients with oropharyngeal carcinoma only: disease-free survival of these patients in group B was 66%, while in group A, all recurred (p = 0.00001). Conclusion: From results of our prospective randomized study it seems that the group of patients that received multidrug treatment with

  10. High Performace Liquid Chromtographic Determination of Nicardipine Hydrochloride in Human Plasma

    Directory of Open Access Journals (Sweden)

    Y. S. R. Krishnaiah

    2004-01-01

    Full Text Available A sensitive high-performance liquid chromatographic method was developed for the estimation of nicardipine hydrochloride in human plasma. Varying amount of nicardipine hydrochloride (2.5 to 150 ng/0.5 mL and fixed quantity (100 ng/0.5 mL of nifedipine (internal standard was added to blank human plasma, and a single step extraction was carried out with ethyl acetate. The mixture was centrifuged, ethyl acetate layer separated, dried and reconstituted with 100 μL of acetonitrile. Twenty microliters of this solution was injected into a reverse phase C-18 column using a mobile phase consisting of acetonitrile: 0.02 M potassium dihydrogen phosphate (pH 4.0 in the ratio of 60:40 v/v and the eluents were monitored at 239 nm. The method was validated for its linearity, precision and accuracy. The calibration curve was linear in the range of 5-150 ng/0.5 mL of plasma and the lower detection limit was 2.5 ng/0.5 mL of plasma. The intra- and inter-day variation was found to be less than 2.5% indicating that the method is highly precise. The mean recovery of nicardipine hydrochloride from plasma samples was 89.6±2.60%. The proposed HPLC method was applied for the estimation of nicardipine hydrochloride in human plasma after oral administration of an immediate release nicardipine hydrochloride capsule (dose 30 mg to 6 adult male volunteers. There was no interference of either the drug metabolites or other plasma components with the proposed HPLC method for the estimation of nicardipine hydrochloride in human plasma. Due to its simplicity, sensitivity, high precision and accuracy, the proposed HPLC method may be used for biopharmaceutical and pharmacokinetic evaluation of nicardipine hydrochloride and its formulations in humans

  11. Systems of pyridine, piperidine, piperazine, morpholine hydrochlorides-terbium (dysprosium) chloride-water

    International Nuclear Information System (INIS)

    Gajfutdinova, R.K.; Sharafutdinova, A.A.; Murinov, Yu.I.

    1988-01-01

    The isothermal cross section method at 25 and 50 deg C is applied to study pyridine hydrochloride-terbium chloride-water (1) piperidine hydrochloride-dysprosium chloride-water (2), piperazine dihydrochloride-dysprosium chloride-water (3) and morpholine hydrochloride-terbium chloride (4) systems. Solubility isotherma prove the formation of incongruently soluble compound of the TbCl 3 x6C 5 H 5 NxHCl composition systems (1). The individuality of the new solid phase is proved by the chemical and DTA methods. Systems (2-4) are of a simple eutonic type

  12. Colestipol hydrochloride prophylaxis of diarrhea during pelvic radiotherapy

    International Nuclear Information System (INIS)

    Stryker, J.A.; Chung, C.K.; Layser, J.D.

    1983-01-01

    Thirty-three patients were randomized prior to pelvic radiotherapy to receive the bile acid-sequestering resin colestipol hydrochloride, 5 grams qid, during the entire time of their therapy or diphenoxylate hydrochloride and atropine sulfate 2.5-20 mg per day (control) if they experienced diarrhea. The colestipol patients also took diphenoxylate if they had diarrhea. The patients in the colestipol group often experienced nausea, vomiting, and abdominal cramps and 8 were forced to discontinue the drug. There was no difference in the weekly stool frequency between the colestipol and the control patients but the colestipol patients who took at least 50% of the prescribed dose required fewer diphenoxylate tablets than the controls. The data suggest that colestipol hydrochloride is not of value in preventing radiation-induced diarrhea because of the side effects associated with the drug, but the theory on which the use of bile acid-sequestering agents is based may be correct

  13. A review of the efficacy of mitomycin C in glaucoma filtration surgery

    Directory of Open Access Journals (Sweden)

    Al Habash A

    2015-10-01

    Full Text Available Ahmed Al Habash,1,2 Leyla Ali Aljasim,1 Ohoud Owaidhah,1 Deepak P Edward1,3 1King Khaled Eye Specialist Hospital, Riyadh, Kingdom of Saudi Arabia; 2Department of Ophthalmology, University of Dammam, Dammam, Saudi Arabia; 3Wilmer Eye Institute, Johns Hopkins University School of Medicine, Baltimore, MD, USA Abstract: The success of trabeculectomy, which is considered the gold standard in the surgical treatment of glaucoma, depends on the wound healing response. The introduction of antiproliferative agents such as mitomycin C (MMC has increased the success rates of trabeculectomy. However, complications due to these agents can be challenging to manage. Hence, it is important to determine the most efficacious dose and duration of exposure. Multiple studies suggest that many factors, including but not limited to MMC preparation, different concentrations, different exposure times, and method of application may affect success rate, and these factors were reviewed in this article. We concluded that lower concentrations of MMC that are prepared and applied in a standardized fashion, such as that using the Mitosol® kit (for 2–3 minutes during trabeculectomy, could potentially provide trabeculectomy success rates similar to that reported with off-label preparations, and that such a treatment regime could result in in lower complication rates than higher doses of MMC. Keywords: mitomycin C, Mitosol, filtering surgery, trabeculectomy, outcomes

  14. An enantioselective synthesis of S-γ-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3-14C] hydrochloride, an important metabolite of fluoxetine hydrochloride

    International Nuclear Information System (INIS)

    Wheeler, W.J.

    1992-01-01

    The S-enantiomer of γ-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3- 14 C] hydrochloride has been prepared in eight steps from acetophenone-[carbonyl- 14 C]. The key step in the synthesis involved the enantioselective reduction of R-2-chloroacetophenone-[1- 14 C]with (-)-diisopinocampheyl-chloroborane in an 86.5% yield. The chlorohydrin was converted to R-phenyloxirane-[1- 14 C], which was subsequently converted to the corresponding R-cyanohydrin by reaction with TMS-CN/CaO. Borane reduction and arylation, followed by salt formation yielded S-γ-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3- 14 C] hydrochloride. (author)

  15. In-silico analysis of amotosalen hydrochloride binding to CD-61 of platelets

    International Nuclear Information System (INIS)

    Chaudhary, H.T.

    2016-01-01

    To determine the docking of Amotosalen hydrochloride (AH) at CD-61 of platelets, and to suggest the cause of bleeding in AH treated platelets transfusion. Study Design: Descriptive study. Place and Duration of Study: Medical College, Taif University, Taif, Saudi Arabia, from October 2014 to May 2015. Methodology: The study was carried out in-silico. PDB (protein data bank) code of Tirofiban bound to CD-61 was 2vdm. CD-61 was docked with Tirofiban using online docking tools, i.e. Patchdock and Firedock. Then, Amotosalen hydrochloride and CD-61 were also docked. Best docking poses to active sites of 2vdm were found. Ligplot of interactions of ligands and CD-61 were obtained. Then comparison of hydrogen bonds, hydrogen bond lengths, and hydrophobic bonds of 2vdm molecule and best poses of docking results were done. Patchdock and Firedock results of best poses were also analysed using SPSS version 16. Results: More amino acids were involved in hydrogen and hydrophobic bonds in Patchdock and Firedock docking of Amotosalen hydrochloride with CD-61 than Patchdock and Firedock docking of CD-61 with Tirofiban. The binding energy was more in latter than former. Conclusion: Amotosalen hydrochloride binds to the active site of CD-61 with weaker binding force. Haemorrhage seen in Amotosalen hydrochloride-treated platelets might be due to binding of Amotosalen hydrochloride to CD-61. (author)

  16. HPLC method validation for modernization of the tetracycline hydrochloride capsule USP monograph

    Directory of Open Access Journals (Sweden)

    Emad M. Hussien

    2014-12-01

    Full Text Available This paper is a continuation to our previous work aiming at development and validation of a reversed-phase HPLC for modernization of tetracycline-related USP monographs and the USP general chapter . Previous results showed that the method is accurate and precise for the assay of tetracycline hydrochloride and the limit of 4-epianhydrotetracycline impurity in the drug substance and oral suspension monographs. The aim of the current paper is to examine the feasibility of the method for modernization of USP tetracycline hydrochloride capsule monograph. Specificity, linearity, accuracy and precision were examined for tetracycline hydrochloride assay and 4-epianhydrotetracycline limit. The method was linear in the concentration range from 80% to 160% (r>0.9998 of the assay concentration (0.1 mg/mL for tetracycline hydrochloride and from 50% to 150% (r>0.997 of the acceptance criteria specified in tetracycline hydrochloride capsule monograph for 4-epianhydrotetracycline (NMT 3.0%. The recovery at three concentration levels for tetracycline hydrochloride assay was between 99% and 101% and the RSD from six preparations at the concentration 0.1 mg/mL is less than 0.6%. The recovery for 4-epianhydrotetracycline limit procedure over the concentration range from 50% to 150% is between 96% and 102% with RSD less than 5%. The results met the specified acceptance criteria.

  17. Effect of Gamma irradiation on the antimicrobial activity of selenomorphiline hydrochloride

    International Nuclear Information System (INIS)

    Bashand, A.S.

    2002-01-01

    The effect of selenomorphiline hydrochloride on dell growth of two steains of bacteria bacillus subtilis as a gram positive and esherichia coli as a gram negative strain and asperagillus flavus as a fungal strain were investigated in batch broth culture supplemented with different concentrations (50, 100, 150, 200, 300 and 400 mg/ml) of irradiated se (1,2,4 KGY) and its control (non irradiated). The data showed that the antibacterial activity of selenomorphiline hydrochloride is concentration and time depenent. The doses 2 doses 2 and 3 KGY of Gamma-radiation were actually the most effective doses activating selenomorphiline hydrochloride as antibiotic

  18. Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Proguanil Hydrochloride.

    Science.gov (United States)

    Plöger, Gerlinde F; Abrahamsson, Bertil; Cristofoletti, Rodrigo; Groot, Dirk W; Langguth, Peter; Mehta, Mehul U; Parr, Alan; Polli, James E; Shah, Vinod P; Tajiri, Tomokazu; Dressman, Jennifer B

    2018-07-01

    Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To elucidate the Biopharmaceutics Classification System (BCS) classification, experimental solubility and dissolution studies were also carried out. The antimalarial proguanil hydrochloride, effective via the parent compound proguanil and the metabolite cycloguanil, is not considered to be a narrow therapeutic index drug. Proguanil hydrochloride salt was shown to be highly soluble according to the U.S. Food and Drug Administration, World Health Organization, and European Medicines Agency guidelines, but data for permeability are inconclusive. Therefore, proguanil hydrochloride is conservatively classified as a BCS class 3 substance. In view of this information and the assessment of risks associated with a false positive decision, a BCS-based biowaiver approval procedure can be recommended for orally administered solid immediate release products containing proguanil hydrochloride, provided well-known excipients are used in usual amounts and provided the in vitro dissolution of the test and reference products is very rapid (85% or more are dissolved in 15 min at pH 1.2, 4.5, and 6.8) and is performed according to the current requirements for BCS-based biowaivers. Copyright © 2018 American Pharmacists Association®. All rights reserved.

  19. Analgesic Effect of Intraperitoneal Bupivacaine Hydrochloride After Laparoscopic Sleeve Gastrectomy: a Randomized Clinical Trial.

    Science.gov (United States)

    Alamdari, Nasser Malekpour; Bakhtiyari, Mahmood; Gholizadeh, Barmak; Shariati, Catrine

    2018-03-01

    The indications for sleeve gastrectomy as a primary procedure for the surgical treatment of morbid obesity have increased worldwide. Pain is the most common complaint for patients on the first day after laparoscopic sleeve gastrectomy. There are various methods for decreasing pain after laparoscopic sleeve gastrectomy such as the use of intraperitoneal bupivacaine hydrochloride. This clinical trial was an attempt to discover the effects of intraperitoneal bupivacaine hydrochloride on alleviating postoperative pain after laparoscopic sleeve gastrectomy. In general, 120 patients meeting the inclusion criteria were enrolled. Patients were randomly allocated into two interventions and control groups using a balanced block randomization technique. One group received intraperitoneal bupivacaine hydrochloride (30 cm 3 ), and the other group served as the control one and did not receive bupivacaine hydrochloride. Diclofenac suppository and paracetamol injection were administered to both groups for postoperative pain management. The mean subjective postoperative pain score was significantly decreased in patients who received intraperitoneal bupivacaine hydrochloride within the first 24 h after the surgery; thus, the instillation of bupivacaine hydrochloride was beneficial in managing postoperative pain. The intraoperative peritoneal irrigation of bupivacaine hydrochloride (30 cm 3 , 0.25%) in sleeve gastrectomy patients was safe and effective in reducing postoperative pain, nausea, and vomiting (IRCT2016120329181N4).

  20. Pulse radiolysis study of the reduction mechanism of an antitumor antibiotic, mitomycin C

    International Nuclear Information System (INIS)

    Machtalere, G.; Houee-Levin, C.; Gardes-Albert, M.; Ferradini, C.; Hickel, B.

    1988-01-01

    Mitomycin C is a quinonic antitumor metabolized in vivo by one-electron reduction. We have studied the mechanism of the one-electron reduction of this drug by pulse radiolysis using C00 .- free radicals as reductants. Semiquinonic and hydroquinonic intermediates are formed. The hydroquinonic form undergoes a methanol elimination leading to a transient which can disappear in one of two ways: by either internal redox reaction or hydrolysis of the aziridine. 17 refs [fr

  1. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride implantation or injectable dosage forms. 522.1662 Section 522.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or injectable...

  2. In vitro and in vivo antimutagenic effects of DIG, a herbal preparation of Berberis vulgaris, Taraxacum officinale and Arctium lappa, against mitomycin C.

    Science.gov (United States)

    Di Giorgio, C; Boyer, L; De Meo, M; Laurant, C; Elias, R; Ollivier, E

    2015-07-01

    DIG, a liquid herbal preparation made from a mixture of diluted mother tinctures of Berberis vulgaris, Taraxacum officinale and Arctium lappa, was assessed for its antimutagenic properties against mitomycin C. The micronucleus assay on Chinese hamster ovary (CHO)-K1 cells was used to evaluate the in vitro anticlastogenic activity of DIG compared to those of separately diluted mother tinctures. The micronucleus assay was performed on mouse erythrocytes and the comet assay was performed on mouse liver, kidney, lung, brain and testicles to assess the protective effects of DIG (0.2 and 2 % at libitum) against an intraperitoneal injection of mitomycin C (1 mg Kg(-1)) in mice. DIG exerted a powerful anticlastogenic activity, under both pretreatment and simultaneous treatment conditions as assessed by the micronucleus assay in CHO-K1 cells. Its protective activity was greater than that observed for each mother tincture. DIG reduced micronuclei levels in mouse erythrocytes and suppressed >80 % of DNA strand breaks in the liver, kidney, lung, brain and testicles of mice exposed to mitomycin C.

  3. Immobilization of swift foxes with ketamine hydrochloride-xylazine hydrochloride

    Science.gov (United States)

    Telesco, R.L.; Sovada, Marsha A.

    2002-01-01

    There is an increasing need to develop field immobilization techniques that allow researchers to handle safely swift foxes (Vulpes velox) with minimal risk of stress or injury. We immobilized captive swift foxes to determine the safety and effectiveness of ketamine hydrochloride and xylazine hydrochloride at different dosages. We attempted to determine appropriate dosages to immobilize swift foxes for an adequate field-handling period based on three anesthesia intervals (induction period, immobilization period, and recovery period) and physiologic responses (rectal temperature, respiration rate, and heart rate). Between October 1998–July 1999, we conducted four trials, evaluating three different dosage ratios of ketamine and xylazine (2.27:1.2, 5.68:1.2, and 11.4:1.2 mg/kg ketamine:mg/kg xylazine, respectively), followed by a fourth trial with a higher dosage at the median ratio (11.4 mg/kg ketamine:2.4 mg/kg xylazine). We found little difference in induction and recovery periods among trials 1–3, but immobilization time increased with increasing dosage (Pimmobilization period and recovery period increased in trial 4 compared with trials 1–3 (P≤0.03). There was a high variation in responses of individual foxes across trials, making it difficult to identify an appropriate dosage for field handling. Heart rate and respiration rates were depressed but all physiologic measures remained within normal parameters established for domestic canids. We recommend a dosage ratio of 10 mg/kg ketamine to 1 mg/kg xylazine to immobilize swift foxes for field handling.

  4. UV Spectrophotometric Method for theEstimation of Itopride Hydrochloride in Pharmaceutical Formulation

    OpenAIRE

    K. R. Gupta; R. R. Joshi; R. B. Chawla; S. G. Wadodkar

    2010-01-01

    Three simple, precise and economical UV methods have been developed for the estimation of itopride hydrochloride in pharmaceutical formulations. Itopride hydrochloride in distilled water shows the maximum absorbance at 258.0 nm (Method A) and in first order derivative spectra of the same shows sharp peak at 247.0 nm, when n = 1 (Method B). Method C utilises area under curve (AUC) in the wavelength range from 262.0-254.0 nm for analysis of itopride hydrochloride. The drug was found to obey Bee...

  5. Anti-Inflammatory Effects of Berberine Hydrochloride in an LPS-Induced Murine Model of Mastitis

    Directory of Open Access Journals (Sweden)

    Xichun Wang

    2018-01-01

    Full Text Available Berberine hydrochloride is an isoquinoline type alkaloid extracted from Berberidaceae, Rutaceae, and other plants. Previous reports have shown that berberine hydrochloride has anti-inflammatory properties. However, the underlying molecular mechanisms remain unclear. In this study, a lipopolysaccharide- (LPS- induced murine model of mastitis was established to explore the anti-inflammatory action of berberine hydrochloride. Sixty mice that had been lactating for 5–7 days were randomly divided into six groups, including control, LPS, three berberine hydrochloride treatment groups (5, 10, and 20 mg/kg, and a dexamethasone (DEX (5 mg/kg group. Berberine hydrochloride was administered intraperitoneally 1 h before and 12 h after LPS-induced mastitis, and all mice were sacrificed 24 h after LPS induction. The pathological and histopathological changes of the mammary glands were observed. The concentrations and mRNA expressions of TNF-α, IL-1β, and IL-6 were measured by ELISA and qRT-PCR. The activation of TLR4 and NF-κB signaling pathways was analyzed by Western blot. Results indicated that berberine hydrochloride significantly attenuated neutrophil infiltration and dose-dependently decreased the secretion and mRNA expressions of TNF-α, IL-1β, and IL-6 within a certain range. Furthermore, berberine hydrochloride suppressed LPS-induced TLR4 and NF-κB p65 activation and the phosphorylation of I-κB. Berberine hydrochloride can provide mice robust protection from LPS-induced mastitis, potentially via the TLR4 and NF-κB pathway.

  6. Anti-Inflammatory Effects of Berberine Hydrochloride in an LPS-Induced Murine Model of Mastitis

    Science.gov (United States)

    Feng, Shibin; Ding, Nana; He, Yanting; Li, Cheng; Li, Manman; Ding, Xuedong; Ding, Hongyan; Li, Jinchun

    2018-01-01

    Berberine hydrochloride is an isoquinoline type alkaloid extracted from Berberidaceae, Rutaceae, and other plants. Previous reports have shown that berberine hydrochloride has anti-inflammatory properties. However, the underlying molecular mechanisms remain unclear. In this study, a lipopolysaccharide- (LPS-) induced murine model of mastitis was established to explore the anti-inflammatory action of berberine hydrochloride. Sixty mice that had been lactating for 5–7 days were randomly divided into six groups, including control, LPS, three berberine hydrochloride treatment groups (5, 10, and 20 mg/kg), and a dexamethasone (DEX) (5 mg/kg) group. Berberine hydrochloride was administered intraperitoneally 1 h before and 12 h after LPS-induced mastitis, and all mice were sacrificed 24 h after LPS induction. The pathological and histopathological changes of the mammary glands were observed. The concentrations and mRNA expressions of TNF-α, IL-1β, and IL-6 were measured by ELISA and qRT-PCR. The activation of TLR4 and NF-κB signaling pathways was analyzed by Western blot. Results indicated that berberine hydrochloride significantly attenuated neutrophil infiltration and dose-dependently decreased the secretion and mRNA expressions of TNF-α, IL-1β, and IL-6 within a certain range. Furthermore, berberine hydrochloride suppressed LPS-induced TLR4 and NF-κB p65 activation and the phosphorylation of I-κB. Berberine hydrochloride can provide mice robust protection from LPS-induced mastitis, potentially via the TLR4 and NF-κB pathway.

  7. 21 CFR 524.1662 - Oxytetracycline hydrochloride ophthalmic and topical dosage forms.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride ophthalmic and topical dosage forms. 524.1662 Section 524.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... DOSAGE FORM NEW ANIMAL DRUGS § 524.1662 Oxytetracycline hydrochloride ophthalmic and topical dosage forms. ...

  8. HER2 and TOP2A in high-risk early breast cancer patients treated with adjuvant epirubicin-based dose-dense sequential chemotherapy

    Directory of Open Access Journals (Sweden)

    Fountzilas George

    2012-01-01

    Full Text Available Abstract Background HER2 and TOP2A parameters (gene status, mRNA and protein expression have individually been associated with the outcome of patients treated with anthracyclines. The aim of this study was to comprehensively evaluate the prognostic/predictive significance of the above parameters in early, high-risk breast cancer patients treated with epirubicin-based, dose-dense sequential adjuvant chemotherapy. Methods In a series of 352 breast carcinoma tissues from patients that had been post-operatively treated with epirubicin-CMF with or without paclitaxel, we assessed HER2 and TOP2A gene status (chromogenic in situ hybridization, mRNA expression (quantitative reverse transcription PCR, as well as HER2 and TopoIIa protein expression (immunohistochemistry. Results HER2 and TOP2A amplification did not share the same effects on their downstream molecules, with consistent patterns observed in HER2 mRNA and protein expression according to HER2 amplification (all parameters strongly inter-related, p values Conclusions This study confirms the favorable prognostic value of HER2/TOP2A co-amplification and the adverse prognostic value of high TOP2A mRNA expression extending it to the adjuvant treatment setting in early high-risk breast cancer. The strong adverse prognostic impact of high HER2/TOP2A mRNA co-expression needs further validation in studies designed to evaluate markers predictive for anthracyclines. Trial registration Australian New Zealand Clinical Trials Registry ACTRN12611000506998.

  9. Interaction between lidocaine hydrochloride (with and without adrenaline) and various irrigants: A nuclear magnetic resonance analysis.

    Science.gov (United States)

    Vidhya, Nirmal; Karthikeyan, Balasubramanian Saravana; Velmurugan, Natanasabapathy; Abarajithan, Mohan; Nithyanandan, Sivasankaran

    2014-05-01

    Interaction between local anesthetic solution, lidocaine hydrochloride (with and without adrenaline), and root canal irrigants such as sodium hypochlorite (NaOCl), ethylene diamine tetra-acetic acid (EDTA), and chlorhexidine (CHX) has not been studied earlier. Hence, the purpose of this in vitro study was to evaluate the chemical interaction between 2% lidocaine hydrochloride (with and without adrenaline) and commonly used root canal irrigants, NaOCl, EDTA, and CHX. SAMPLES WERE DIVIDED INTO EIGHT EXPERIMENTAL GROUPS: Group I-Lidocaine hydrochloride (with adrenaline)/3% NaOCl, Group II-Lidocaine hydrochloride (with adrenaline)/17% EDTA, Group III- Lidocaine hydrochloride (with adrenaline)/2% CHX, Group IV-Lidocaine hydrochloride (without adrenaline)/3% NaOCl, Group V-Lidocaine hydrochloride (without adrenaline)/17% EDTA, Group VI-Lidocaine hydrochloride (without adrenaline)/2% CHX, and two control groups: Group VII-Lidocaine hydrochloride (with adrenaline)/deionized water and Group VIII-Lidocaine hydrochloride (without adrenaline)/deionized water. The respective solutions of various groups were mixed in equal proportions (1 ml each) and observed for precipitate formation. Chemical composition of the formed precipitate was then analysed by nuclear magnetic resonance spectroscopy (NMR) and confirmed with diazotation test. In groups I and IV, a white precipitate was observed in all the samples on mixing the respective solutions, which showed a color change to reddish brown after 15 minutes. This precipitate was then analysed by NMR spectroscopy and was observed to be 2,6-xylidine, a reported toxic compound. The experimental groups II, III, V, and VI and control groups VII and VIII showed no precipitate formation in any of the respective samples, until 2 hours. Interaction between lidocaine hydrochloride (with and without adrenaline) and NaOCl showed precipitate formation containing 2,6-xylidine, a toxic compound.

  10. Measurement and correlation of solubility of cefmenoxime hydrochloride in pure solvents and binary solvent mixtures

    International Nuclear Information System (INIS)

    Wang, Jinxiu; Xie, Chuang; Yin, Qiuxiang; Tao, Linggang; Lv, Jun; Wang, Yongli; He, Fang; Hao, Hongxun

    2016-01-01

    Highlights: • Solubility of cefmenoxime hydrochloride in pure and binary solvents was determined. • The experimental solubility data were correlated by thermodynamic models. • A model was employed to calculate the melting temperature of cefmenoxime hydrochloride. • Mixing thermodynamic properties of cefmenoxime hydrochloride were calculated. - Abstract: The solubility of cefmenoxime hydrochloride in pure solvents and binary solvent mixtures was measured at temperatures from (283.15 to 313.15) K by using the UV spectroscopic method. The results reveal that the solubility of cefmenoxime hydrochloride increases with increasing temperature in all solvent selected. The solubility of cefmenoxime hydrochloride reaches its maximum value when the mole fraction of isopropanol is 0.2 in the binary solvent mixtures of (isopropanol + water). The modified Apelblat equation and the NRTL model were successfully used to correlate the experimental solubility in pure solvents while the modified Apelblat equation, the CNIBS/R–K model and the Jouyban–Acree model were applied to correlate the solubility in binary solvent mixtures. In addition, the mixing thermodynamic properties of cefmenoxime hydrochloride in different solvents were also calculated based on the NRTL model and experimental solubility data.

  11. Spectrophotometric determination of eflornithine hydrochloride ...

    African Journals Online (AJOL)

    Purpose: To develop and validate a spectrophotometric method for the quantitative determination of eflornithine hydrochloride as a pure compound and in pharmaceutical formulations. Methods: The method involved the reaction of the target compound with vanillin reagent at specific pH 5.6 to produce a green reddish color ...

  12. Spectrophotometric Determination of Eflornithine Hydrochloride ...

    African Journals Online (AJOL)

    Purpose: To develop and validate a spectrophotometric method for the quantitative determination of eflornithine hydrochloride as a pure compound and in pharmaceutical formulations. Methods: The method involved the reaction of the target compound with vanillin reagent at specific pH. 5.6 to produce a green reddish color ...

  13. Spectrophotometric method of the determination of gold (III) by using imipramine hydrochloride and promethazine hydrochloride

    International Nuclear Information System (INIS)

    Dembinski, B.; Kurzawa, M.; Szydlowska-Czerniak, A.

    2003-01-01

    Imipramine hydrochloride (IPM.HCl) and promethazine hydrochloride (PMT-HCl) were used for the spectrophotometric determination of gold (III) in the aqueous solution. The halides complexes of gold (III) created a coloured coupling with the studied drugs which were extractable in chloroform. These new compounds were characterized by IR,UV-VIS spectra and thermal and elemental analysis. Rapid and sensitive spectrophotometric method for the determination of gold (III) in the aqueous solution is described. The absorbance was found to be linear function of the gold (III) concentration in the range from 0.2 to 20 x10/sup -1/ mg. The ratio of complex (AuX/sub 4/) to the organic cation from drug in the obtained compounds was determined as 1:1. The method was satisfactorily applied to the analysis of gold (III). A great advantage of the proposed method is that the trace amounts of gold (III) can also be examined. (author)

  14. Atovaquone and proguanil hydrochloride for treatment of malaria.

    Science.gov (United States)

    Kremsner, P G; Looareesuwan, S; Chulay, J D

    1999-05-01

    Safe and effective new drugs are needed for treatment of malaria. Atovaquone and proguanil hydrochloride is a new antimalarial combination that has recently become available in many countries. Data from clinical trials evaluating atovaquone/proguanil for treatment of malaria were reviewed. In 10 open-label clinical trials, treatment of uncomplicated falciparum malaria with 1000 mg atovaquone and 400 mg proguanil hydrochloride (or the equivalent based on body weight in patients proguanil has been used to provide radical cure of asymptomatic Plasmodium falciparum infections prior to initiation of placebo-controlled trials of malaria prophylaxis. Recurrent parasitemia occurred within 28 days in 0 of 99 subjects who subsequently received prophylaxis with atovaquone/proguanil and 1 of 81 subjects who subsequently received placebo. Atovaquone/proguanil is also effective for treatment of malaria caused by the other three Plasmodium species that cause malaria in humans. For treatment of vivax malaria, therapy with primaquine in addition to atovaquone/proguanil is needed to prevent relapse from latent hepatic hypnozoites. Atovaquone and proguanil hydrochloride is a safe and effective combination for treatment of malaria.

  15. Quantization of buspirone hydrochloride in pure and pharmaceutical formulation by spectrophotometric method

    International Nuclear Information System (INIS)

    Kazi, A.A.; Mumtaz, A.; Sabri, M.U.

    2008-01-01

    A simple and sensitive method is described for the determination of bus pirone hydrochloride in bulk drug and in formulations employing spectrophotometric technique. The method is based on the interaction orbuspirone hydrochloride with ammonium molybdate in acidic media and the absorbance is measured at 700 nm. Beer's Law is obeyed in the range of 5 macro g to 350 micro g/ml and RSD is 0.96% for buspirone hydrochloride. Analytical data for the determination of pure compound is presented along with the application of the proposed method for the analysis of pharmaceutical formulation. (author)

  16. [Preparation and characterization of Forms A and B of benazepril hydrochloride].

    Science.gov (United States)

    Fang, Hong; Hu, Xiu-rong; Gu, Jian-ming; Chen, Guan-xi; Feng, Jian-yue; Tang, Gu-ping

    2012-11-01

    To prepare Form A and Form B of benazepril hydrochloride and to compare the differences in spectrums, thermodynamics and crystal structure between two polymorphic forms. Form A and Form B of benazepril hydrochloride were characterized by Fourier transform infrared spectroscopy (IR), thermal gravimetric analysis (TG), differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD) and single crystal x-ray diffraction (SCXRD). Preparation method, crystal structure and polymorphic stability of Form A and Form B of benazepril hydrochloride were obtained. Based on the analysis of crystal structure of both polymorphs, Form A belonged to monoclone space group P2(1) with a=7.8655(4)Å, b= 11.7700(6)Å, c= 13.5560(7)Å, β= 102.9470(10)°, V=1223.07 (11)Å(3) and Z=2, while Form B belonged to orthorhombic space group P212121, with a=7.9353(8)Å, b=11.6654(11)Å, c=26.6453(16)Å, V=2466.5(4)Å(3) and Z=4. From the DSC and XRD results, Form B of benazepril hydrochloride could be transformed into Form A after heating treatment. Form A and Form B of benazepril hydrochloride are both anhydrous and displayed different polymorphs due to different molecular configuration. Furthermore, Form A exhibits more stable than Form B at high temperatures.

  17. Influence of intraperitoneal therapy with mitomycin C adsorbed on activated carbon on anastomotic and wound healing in rats

    NARCIS (Netherlands)

    Jansen, M; Jansen, PL; Fass, J; Langejurgen, E; Forsch, S; Tietze, L; Schumpelick, [No Value

    In an effort to prevent intraperitoneal dissemination of gastric carcinoma, local chemotherapy with mitomycin C adsorbed to activated carbon (MMC-CH) has been implemented. Results of clinical studies showed improved survival and a reduced systemic toxicity after the use of prophylactic treatment

  18. Rescue of Mitomycin C- or Psoralen-Inactivated Micrococcus Radiodurans by Additional Exposure to Radiation or Alkylating Agents

    DEFF Research Database (Denmark)

    Hansen, M. Trier

    1982-01-01

    The processing of damaged DNA was altered in a mitomycin C-sensitive mutant (mtcA) of Micrococcus radiodurans. Even though the mutant retained resistance to 254-nm UV radiation, it did not, in contrast to the wild-type strain, show any excessive DNA degradation or cell death when incubated...

  19. Switching the Loaded Agent from Epirubicin to Cisplatin: Salvage Transcatheter Arterial Chemoembolization with Drug-eluting Microspheres for Unresectable Hepatocellular Carcinoma

    International Nuclear Information System (INIS)

    Seki, Akihiko; Hori, Shinich

    2012-01-01

    Purpose: There is no consensus on switching anticancer agents loaded onto drug carriers in transcatheter arterial chemoembolization (TACE) for hepatocellular carcinoma (HCC). This study aimed to evaluate the safety and clinical outcomes of TACE with cisplatin-loaded microspheres (CLM-TACE) in HCC patients refractory to TACE with epirubicin-loaded microspheres (ELM-TACE). Methods: Between February 2008 and June 2010, 85 patients with unresectable HCC refractory to ELM-TACE were enrolled to undergo CLM-TACE. The number of ELM-TACE sessions until judgment of resistance ranged from 1 to 4 (median, 2.1). CLM-TACE was performed using 50–100-μm superabsorbent polymer microspheres loaded with 1 mg cisplatin/1 mg microspheres together with hepatic arterial infusion of 25 mg cisplatin and 500 mg 5-fluorouracil per patient. Tumor responses were evaluated by computed tomography according to the European Association for the Study of the Liver criteria. Results: The median number of CLM-TACE treatment sessions was 1.8 (range, 1–5), and the mean total dose of cisplatin per session was 42.8 mg (range, 30.0–59.0). After 6 months, 3 (3.5%) patients achieved complete response, 31 (36.5%) had partial response, 15 (17.6%) had stable disease, and 36 (42.4%) had progressive disease. The median overall survival and time to treatment failure after initial CLM-TACE were 13.3 and 7.2 months, respectively. Overall, 9.4% of patients experienced grade 3/4 adverse events. Conclusions: witching the loaded agent from epirubicin to cisplatin is a safe, well-tolerated, and efficacious treatment strategy for salvage TACE with drug-eluting microspheres in HCC patients refractory to ELM-TACE.

  20. Effect of mitomycin c and 5-flurouracil adjuvant therapy on the outcomes of Ahmed glaucoma valve implantation.

    Science.gov (United States)

    Cui, Qi N; Hsia, Yen C; Lin, Shan C; Stamper, Robert L; Rose-Nussbaumer, Jennifer; Mehta, Nitisha; Porco, Travis C; Naseri, Ayman; Han, Ying

    2017-03-01

    To examine the effect of mitomycin c and 5-flurouracil on treatment outcomes following Ahmed glaucoma valve implantation. Retrospective consecutive case series. Fifty patients who received Ahmed glaucoma valve implantation from 1999 to 2013 in the San Francisco Veterans Administration Hospital. The +INJECTION group received intraoperative mitomycin c followed by postoperative mitomycin c and/or 5-flurouracil, whereas the -INJECTION group did not. Primary outcome was treatment success at 1 year post-implantation. Intraocular pressure, hypertensive phase, and the number of glaucoma medications were also examined. Twenty-six patients/eyes in the +INJECTION group and 24 patients/eyes in the -INJECTION group were included. Treatment success was higher in the +INJECTION compared with the -INJECTION group (86 vs. 58%; P = 0.04). Intraocular pressure was lower in the +INJECTION compared with the -INJECTION group at 1, 3, 6 and 12 months (P ≪ 0.00001, P = 0.00003, 0.0008 and 0.024). Hypertensive phase occurred less often in the +INJECTION compared with the -INJECTION group (3.8 vs. 54%; P = 0.021). The +INJECTION group required fewer medications compared with the -INJECTION group (P = 0.02, 0.002, 0.003 and 0.008 at 1, 3, 6 and 12 months). Complication rates were comparable between groups (46.2 and 54.2%; P = 0.63). Adjuvant treatment with antifibrotics following Ahmed glaucoma valve implantation decreased the hypertensive phase and improved surgical outcomes without impacting complication rates at 1 year. This study postulates a role for antifibrotics in the postoperative management of Ahmed glaucoma valves. © 2016 Royal Australian and New Zealand College of Ophthalmologists.

  1. 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 Levamisole hydrochloride tablet or oblet (bolus). (a) Chemical name. (-)-2,3,5,6-Tetrahydro... using in severely debilitated animals. (2) It is used in a tablet for sheep as follows: (i) Amount. 0...

  2. An enantioselective synthesis of S-[gamma]-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3-[sup 14]C] hydrochloride, an important metabolite of fluoxetine hydrochloride

    Energy Technology Data Exchange (ETDEWEB)

    Wheeler, W.J. (Lilly (Eli) and Co., Indianapolis, IN (United States). Lilly Research Labs.)

    1992-06-01

    The S-enantiomer of [gamma]-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3-[sup 14]C] hydrochloride has been prepared in eight steps from acetophenone-[carbonyl-[sup 14]C]. The key step in the synthesis involved the enantioselective reduction of R-2-chloroacetophenone-[1-[sup 14]C]with (-)-diisopinocampheyl-chloroborane in an 86.5% yield. The chlorohydrin was converted to R-phenyloxirane-[1-[sup 14]C], which was subsequently converted to the corresponding R-cyanohydrin by reaction with TMS-CN/CaO. Borane reduction and arylation, followed by salt formation yielded S-[gamma]-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3-[sup 14]C] hydrochloride. (author).

  3. Stability of methadone hydrochloride in 0.9% sodium chloride injection in single-dose plastic containers.

    Science.gov (United States)

    Denson, D D; Crews, J C; Grummich, K W; Stirm, E J; Sue, C A

    1991-03-01

    The stability of methadone hydrochloride in 0.9% sodium chloride injection in flexible polyvinyl chloride containers was studied. Commercially available methadone hydrochloride 20 mg/mL and 25-mL single-dose bags of 0.9% sodium chloride injection were used. Six samples each were prepared at methadone hydrochloride concentrations of 1, 2, and 5 mg/mL. The solutions were stored at room temperature and were not protected from light. Immediately after preparation and after two, three, and four weeks of storage, each of the 18 samples was divided into three aliquots, each of which was analyzed in duplicate for methadone hydrochloride concentration by gas chromatography. There was less than 10% change in methadone hydrochloride concentration in any sample throughout the four-week study period. Methadone hydrochloride at concentrations of 1, 2, and 5 mg/mL prepared in commercially available flexible polyvinyl chloride containers of 0.9% sodium chloride injection and stored at room temperature without deliberate protection from light is stable for at least four weeks.

  4. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Science.gov (United States)

    2010-07-01

    ... Insulation Resins by Hydroxylamine Hydrochloride B Appendix B to Subpart NNN of Part 63 Protection of...—Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride 1. Scope This method was... hydrochloric acid that is liberated when hydroxylamine hydrochloride reacts with formaldehyde to form...

  5. 21 CFR 520.2345h - Tetracycline hydrochloride, sodium novobiocin, and prednisolone tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tetracycline hydrochloride, sodium novobiocin, and... ANIMAL DRUGS § 520.2345h Tetracycline hydrochloride, sodium novobiocin, and prednisolone tablets. (a... the first stage of parturition when administered during the last trimester of pregnancy and may...

  6. IMPACT OF STRESS FACTORS ON OPTICAL ISOMERISM OF BENAZEPRIL HYDROCHLORIDE.

    Science.gov (United States)

    Kublin, Elżbieta; Czerwińska, Krystyna; Wyszomirska, Elżbieta; Zajaczkowską, Anna; Malanowicz, Ewa; Kaczmarska-Graczyk, Barbara; Mazurek, Aleksander P

    2015-01-01

    Benazepril hydrochloride contains two stereogenic centers, but is currently available as single enantiomer (S,S configuration) for the treatment of hypertension. Its enantiomer (R,R configuration) and the diastereoisomeric pair (R,S and S,R) can be regarded as impurities. Stereochemical stability of S,S isomer of benazepril hydrochloride and its potential susceptibility to conversion in the.active substance and in Lisonid tablets were examinated. The separation with the use of the TLC method with the following system: chromatographic plates Chiralplate and a mobile phase: methanol - acetonitrile - 1 mM copper(II) acetate (4 : 2 : 4, v/v/v) with saturation of glacial acetic acid for 1 h and the HPLC method system: Chiral AGP column (150 x 4.0 man x 5 µm) and a mobile phase: phosphate buffer pH = 6.0 - methanol (80 : 20, v/v) were obtained. Active substance - benazepril hydrochloride and Lisonid tablets 20 mg were subjected to the impact of different stress factors. Samples were examined after 1 and 6 weeks. It was found that none of the applied stress factors caused the transformation of the S,S enantiomer of benazepril hydrochloride in the substance and tablets to other identified stereoisomers - only the compound decomposition has occurred.

  7. Chemical stability of diphenhydramine hydrochloride from an elixir and lidocaine hydrochloride from a viscous solution when mixed together.

    Science.gov (United States)

    Gupta, Vishnu D

    2006-01-01

    The stability of diphenhydramine hydrochloride (from an elixir) and lidocaine hydrochloride (from a viscous solution) in a mixture (1:1) was studied using a stability-indicating high-peformance liquid chromatographic assay method. The concentrations of the drugs were related directly to peak heights and the percent relative standard deviations based on five injections were 1.4 for diphenhydramine and 1.3 for lidocaine. The products of hydrolysis from the both the drugs and a number of excipients present in the dosage forms did not interfere with the developed assay procedure. The mixture was stable for at least 21 days when stored in amber-colored bottles at room temperature. The pH value of the mixture remained constant, and the physical appearance did not change during the study period.

  8. Simultaneous estimation of Montelukast sodium and Bambuterol hydrochloride in tablets by spectrophotometry.

    Science.gov (United States)

    Nanda, R K; Pangarkar, V B; Thomas, A B; Kothapalli, L P; Pawar, A A

    Two simple, rapid, accurate and precise methods have been developed for simultaneous estimation of Montelukast sodium and Bambuterol hydrochloride from tablet dosage form. In the first method, the first derivative spectrum was determined. Montelukast sodium showed zero crossing point at 209.5 nm and Bambuterol hydrochloride showed zero crossing point at 238.5 nm. The dA/dlambda was measured at 209.5 nm for Bambuterol hydrochloride and 238.5 nm for Montelukast sodium and calibration curves were plotted as dA/dlambda versus concentration respectively. Quantitative determination of Montelukast sodium and Bambuterol hydrochloride in tablets was carried out using calibration curve by interpolation method. In the second method, Multicomponent mode of analysis was used and the measurement of absorbances at two wavelengths, 283.6 nm (lambda-max of MKST) and 211.8 nm (working wavelength selected for BHC) in 95% methanol, was carried out. These methods were validated statistically as per ICH guidelines. The recovery studies confirm the accuracy of the proposed method.

  9. Modified Synthesis of Erlotinib Hydrochloride

    Directory of Open Access Journals (Sweden)

    Leila Barghi

    2012-06-01

    Full Text Available Purpose: An improved and economical method has been described for the synthesis of erlotinib hydrochloride, as a useful drug in treatment of non-small-cell lung cancer. Methods: Erlotinib hydrochloride was synthesized in seven steps starting from 3, 4-dihydroxy benzoic acid. In this study, we were able to modify one of the key steps which involved the reduction of the 6-nitrobenzoic acid derivative to 6-aminobenzoic acid derivative. An inexpensive reagent such as ammonium formate was used as an in situ hydrogen donor in the presence of palladium/charcoal (Pd/C instead of hydrogen gas at high pressure. Results: This proposed method proceeded with 92% yield at room temperature. Synthesis of erlotinib was completed in 7 steps with overall yield of 44%.Conclusion: From the results obtained it can be concluded that the modified method eliminated the potential danger associated with the use of hydrogen gas in the presence of flammable catalysts. It should be mentioned that the catalyst was recovered after the reaction and could be used again.

  10. Fast and Convenient NIR Spectroscopy Procedure for Determination of Metformin Hydrochloride in Tablets

    Science.gov (United States)

    Pyzowski, J.; Lenartowicz, M.; Sobańska, A. W.; Brzezińska, E.

    2017-09-01

    A rapid and convenient near-infrared (NIR) reflectance spectroscopic procedure for the determination of metformin hydrochloride in tablets is presented. Determination was based on calibration curves that were obtained using a range of standards containing different concentrations of metformin hydrochloride blended with polyvinylpyrrolidone. The raw spectra of the standards, neat PVP, metformin hydrochloride, and powdered tablets were processed using a Multiplicative Scatter Correction filter as well as by the derivative spectroscopy method to give a basis for the calibration curve construction. The results were validated by thin-layer chromatography followed by UV-densitometry.

  11. Use of xylazine hydrochloride-ketamine hydrochloride for immobilization of wild leopards (Panthera pardus fusca) in emergency situations.

    Science.gov (United States)

    Belsare, Aniruddha V; Athreya, Vidya R

    2010-06-01

    In India, leopards (Panthera pardus fusca) inhabit human-dominated landscapes, resulting in encounters that require interventions to prevent harm to people, as well as the leopards. Immobilization is a prerequisite for any such intervention. Such emergency field immobilizations have to be carried out with limited tools, often amidst large uncontrollable crowds. An effective and practicable approach is discussed, based on 55 wild leopard immobilizations undertaken between January 2003 and April 2008. A xylazine hydrochloride (1.4 +/- 0.3 mg/kg)--ketamine hydrochloride (5 +/- 2 mg/kg) mixture was used for immobilization of leopards, based on estimated body weight. When weight could not be estimated, a standard initial dose of 50 mg of xylazine--150 mg of ketamine was used. Supplemental doses (50-75 mg) of only ketamine were used as required. No life-threatening adverse effects of immobilization were documented for at least 1 mo postimmobilization.

  12. Successful endoscopic management with Mitomycin C application for sinusitis with orbital cellulitis

    Directory of Open Access Journals (Sweden)

    Anil S Harugop

    2013-01-01

    Full Text Available Background: Sinusitis with orbital complication is a potentially fatal disease that has been known since the days of Hippocrates. Primary sinus infection is the most common cause of orbital cellulitis. It is an emergency that threatens not only vision but also life from complications such as meningitis, cavernous sinus thrombosis, and brain abscess. Surgical intervention is mandatory whenever antibiotic treatment fails. There are two surgical options for the drainage, an external approach via a Lynch incision and an intranasal endoscopic procedure. Materials and Methods: Five patients with orbital cellulitis secondary to acute on chronic rhinosinusitis were included in the study from the period of 2010 - 2011. All five patients did not respond to medical management and hence underwent endoscopic sinus surgery with treatment of orbital pathology. At the end of the surgical procedure Mitomycin C in a concentration of 0.4mg/ml was applied with a cottonoid for a period of 4 minutes to prevent chance of adhesion formation. Results: In this series 3 females and 2 male patient with orbital cellulitis secondary to acute on chronic rhinosinusitis underwent endoscopic sinus surgery with treatment of orbital pathology. All 5 patients showed subjective and objective improvement within one week of endoscopic management. Conclusion: Though antibiotics have altered the course of sinusitis, its grave complications still persist in our environment. The excellent results and the absence of any major complications of endoscopic sinus surgery and drainage of abscess with application of Mitomycin C can be recommended as the preferred surgical technique.

  13. The effect of mitomycin C trabeculectomy on the progression of visual field defect in normal-tension glaucoma.

    Science.gov (United States)

    Hagiwara, Y; Yamamoto, T; Kitazawa, Y

    2000-03-01

    We investigated in a prospective fashion the visual prognosis and complications in normal-tension glaucoma following unilateral trabeculectomy with adjunctive mitomycin C. Trabeculectomy with adjunctive mitomycin C was carried out unilaterally in 21 cases of normal-tension glaucoma. Intraocular pressure (IOP), visual prognosis, and complications were compared between the operated eyes and the non-operated fellow eyes. The follow-up period ranged from 2 to 7 years. The IOP dropped significantly from 14.8+/-1.8 mmHg (mean +/- SD) to 9.6+/-3.9 mmHg in the operated eyes (P=0.0002, Wilcoxon signed-rank test), but did not drop in the non-operated eyes. The mean deviation (MD) was -12.69+/-6.41 dB preoperatively and -14.70+/-5.49 dB at the last clinic visit in the operated eyes, whereas in non-operated eyes it was -7.85+/-5.65 dB and -11.15+/-5.62 dB, respectively. The MD deteriorated significantly in both operated and non-operated eyes (operated eyes P=0.0239, non-operated eyes: P=0.0002; Wilcoxon signed-rank test). The MD slope was -0.37+/-0.60 dB/year and -0.71+/-0.89 dB/year for the operated and non-operated eyes, respectively (P=0.5243, Mann-Whitney U-test). Visual field deterioration was more frequently observed in the non-operated eyes by a pointwise definition of the progression (Ptest). Visual acuity deteriorated in 6 of the operated eyes and in 5 of the non-operated eyes. Cataract developed in 6 (29%) of the 21 operated eyes, while among the non-operated eyes 4 (19%) developed cataract. Mitomycin C trabeculectomy is effective in delaying progression of visual field defect in normal-tension glaucoma, but complications may arise and cause some visual disturbance.

  14. Niosomal encapsulation of ethambutol hydrochloride for increasing its efficacy and safety.

    Science.gov (United States)

    El-Ridy, Mohammed Shafik; Yehia, Soad Aly; Kassem, Mahfouz Abd-El-Megeid; Mostafa, Dina Mahmoud; Nasr, Essam Amin; Asfour, Marwa Hasanin

    2015-01-01

    Tuberculosis (TB) is a worldwide health concern. In 2011, about 8.7 million new cases developed TB and 1.4 million people died from it. Enhancement of ethambutol hydrochloride activity and safety in treatment of TB through niosomal encapsulation. Niosomes were prepared by the thin-film hydration method. They were characterized, investigated for in vitro release, lung disposition and in vivo biological evaluation. Entrapment efficiency of ethambutol hydrochloride ranged from 12.20% to 25.81%. Zeta potential values inferred stability of neutral and negatively charged formulations. In vitro release was biphasic. Lung targeting was increased by niosomal encapsulation. Biological evaluation revealed superiority of niosomal ethambutol hydrochloride over the free drug. Neutral and negatively charged niosomal vesicles are dispersed homogenously unlike positively charged vesicles. Niosomal encapsulation results in controlled drug release. Niosomal formulations targeted more drugs to mice lungs for a prolonged period of time resulting in: decreased root-specific lung weight, bacterial counts in lung homogenates and optimizing pathological effect on guinea pigs lungs, livers and spleens. Encapsulation of ethambutol hydrochloride in niosomal formulations for the treatment of TB provides higher efficacy and safety compared with the free drug.

  15. LASIK flap buttonhole treated immediately by PRK with mitomycin C.

    Science.gov (United States)

    Kymionis, George D; Portaliou, Dimitra M; Karavitaki, Alexandra E; Krasia, Maria S; Kontadakis, Georgios A; Stratos, Aimilianos; Yoo, Sonia H

    2010-03-01

    To describe the visual outcomes of three patients who had LASIK flap buttonhole and were treated immediately with photorefractive keratectomy (PRK) and topical mitomycin C (MMC) 0.02%. Three patients underwent bilateral LASIK with the SCHWIND Carriazo-Pendula 90 microm head microkeratome. In all three cases, a buttonhole flap occurred in the left eye. The flap was repositioned and phototherapeutic keratectomy for 50 microm was used for epithelial removal while immediate PRK with MMC was performed to treat the buttonhole flap. Three months after the procedure, uncorrected distance visual acuity and corrected distance visual acuity were 20/20 with regular topographic findings. Using PRK with MCC immediately after the occurrence of the LASIK flap buttonhole may be an effective treatment.

  16. Trabeculectomy with mitomycin-c

    International Nuclear Information System (INIS)

    Baig, M.S.A.; Ali, M.A.

    2008-01-01

    To study the efficacy and safety of trabeculectomy augmented with intra-operative application of Mitomycin- C (MMC) in various types of refractory glaucomas. Forty patients with a number of refractory glaucomas who underwent trabeculectomies with MMC. MMC 0.02% (0.2mg/ml) was applied to 52 eyes of 40 patients being operated for trabeculectomies under the partial thickness scleral flap with an exposure time of three minutes. Visual outcome, control of intraocular pressure (IOP) and complications were evaluated. There were 25 males and 15 females in the study with an average age of 41.3 (range 1-65) years and an average follow up of 26.4 months (range 12-60 months). The average preoperative IOP was 32.5mm Hg (range 24- 52 mmHg) on an average of 1.34 medications, and the mean postoperative IOP after one year in successful cases was 14.42mmHg (range 12-18 mm Hg) without any medication (qualified success) in 45(86.5%) cases; five patients required one medication. Early postoperative complications included hypotony of more than one month duration in 11(21.2%) cases, hyphema of more than one week duration in 7(13.5%) and epithelial defect in 3(5.76%) cases. Late complication included cataract in 21(40.4%) cases, uncontrolled intraocular pressure despite medical therapy in two (3.84%) cases who further underwent Ahmed glaucoma valve implantation. One case (1.92%) of hypotonous maculopathy was noted. Trabeculectomy with MMC is a promising, safe and effective modality in the management of refractory glaucomas. As the complications related to bleb thinning increases with time, hence further study is required to determine the long term complications. (author)

  17. A novel and rapid microbiological assay for ciprofloxacin hydrochloride

    Directory of Open Access Journals (Sweden)

    Edith Cristina Laignier Cazedey

    2013-10-01

    Full Text Available The present work reports a simple, fast and sensitive microbiological assay applying the turbidimetric method for the determination of ciprofloxacin hydrochloride (CIPRO HCl in ophthalmic solutions. The validation method yielded good results and included excellent linearity, precision, accuracy and specificity. The bioassay is based on the inhibitory effect of CIPRO HCl upon the strain of Staphylococcus epidermidis ATCC 12228 used as the test microorganism. The results were treated statistically by analysis of variance (ANOVA and were found to be linear (r=0.9994, in the range of 14.0–56.0 µg/mL, precise (intraday RSD%=2.06; interday RSD%=2.30 and accurate (recovery=99.71%. The turbidimetric assay was compared to the UV spectrophotometric and HPLC methods for the same drug. The turbidimetric bioassay described on this paper for determination of ciprofloxacin hydrochloride in ophthalmic solution is an alternative to the physicochemical methods disclosed in the literature and can be used in quality control routine. Keywords: Antibiotics, Fluoroquinolones, Ciprofloxacin hydrochloride, Quality control, Microbiological assay, Turbidimetric method

  18. Repairability during G 1 phase of inducting lesions of sister chromatid exchange produced by mitomycin C in salivary gland cells of mice In Vivo

    International Nuclear Information System (INIS)

    Cruz Vallejo, V.L.

    1991-01-01

    The repairability of the injuries that lead to the formation of sister chromatid exchange (SCE) produced by mitomycin C (MMC) with a dose of 2.1 mg/g in vivo, during the G 1 phase in the first cycle of cellular division (before the incorporation of BrdU [5-bromo-2 deoxyurine] to the DNA), as well as during the G 1 phase of the second cycle of cellular division (after the incorporation of BrdU) were analyzed. A 35.1% decrease in the frequency of SCE produced by Mitomycin C was observed, in the early G 1 phase of the first division, with respect to the frequency of SCE induced in the later G 1 phase. When Mitomycin C is given to cells whose DNA is substituted with BrdU in only one of the chain's filaments such decrease is not observed. The results suggest that the injuries caused by MMC, which give place to the SCE, in cells of the salivary glands of the mouse in vivo, are partially repaired only when induced in DNA which has not been substituted with BrdU. (Author)

  19. Conservative treatment for late-onset bleb leaks after trabeculectomy with mitomycin C in patients with ocular surface disease

    Directory of Open Access Journals (Sweden)

    Sagara H

    2012-08-01

    Full Text Available Hideto Sagara,1,2 Tomohiro Iida,2,3 Kimimori Saito,4 Hiroki Noji,2 Masashi Ogasawara,2 Hiroshi Oyamada21The Marui Eye Clinic, Fukushima, 2Department of Ophthalmology, Fukushima Medical University School of Medicine, Fukushima, 3Tokyo Women's Medical University, Tokyo, 4Matuki Eye Clinic, Fukushima, JapanBackground: Sodium hyaluronate and autologous serum eye drops are used to treat ocular surface disease (OSD and are reported to prevent and treat late-onset bleb leaks following trabeculectomy with mitomycin C. In this study, we evaluated the efficacy of a combination of sodium hyaluronate and autologous serum eye drops and treatment for obstructive meibomian gland dysfunction as a therapy for late-onset bleb leaks after trabeculectomy with mitomycin C.Methods: This was a retrospective, interventional, nonsimultaneous study of 12 subjects (12 eyes of mean age of 64.3 ± 18.3 years with OSD and apparent late-onset bleb leaks following trabeculectomy with mitomycin C between 1998 and 2008. We compared patients diagnosed with leakages before July 2005, who had been treated with separate eye drop solutions containing 0.1% sodium hyaluronate, 50% autologous serum, and 0.3% ofloxacin (sodium hyaluronate and autologous serum group, n = 7, with patients diagnosed from August 2005 to December 2008, who were treated with a combination of eye drops (0.1% sodium hyaluronate, 50% autologous serum, and 0.08% levofloxacin hydrate and eyelid massage and warm compresses for obstructive meibomian gland dysfunction (combination eye drop group, n = 5.Results: Leakage was resolved in one patient (14.3% in the separately treated sodium hyaluronate and autologous serum eye drop group and in five patients (100% in the combination eye drop group (P = 0.015. The period after resolution of leakage with conservative treatment was 23 months in the one eye in the sodium hyaluronate and autologous serum group and 36–61 (mean 52.4 ± 10.1 months in the five eyes in the

  20. Photoacoustic imaging to detect rat brain activation after cocaine hydrochloride injection

    Science.gov (United States)

    Jo, Janggun; Yang, Xinmai

    2011-03-01

    Photoacoustic imaging (PAI) was employed to detect small animal brain activation after the administration of cocaine hydrochloride. Sprague Dawley rats were injected with different concentrations (2.5, 3.0, and 5.0 mg per kg body) of cocaine hydrochloride in saline solution through tail veins. The brain functional response to the injection was monitored by photoacoustic tomography (PAT) system with horizontal scanning of cerebral cortex of rat brain. Photoacoustic microscopy (PAM) was also used for coronal view images. The modified PAT system used multiple ultrasonic detectors to reduce the scanning time and maintain a good signal-to-noise ratio (SNR). The measured photoacoustic signal changes confirmed that cocaine hydrochloride injection excited high blood volume in brain. This result shows PAI can be used to monitor drug abuse-induced brain activation.

  1. Compatibility of ondansetron hydrochloride and methylprednisolone sodium succinate in multilayer polyolefin containers.

    Science.gov (United States)

    Bougouin, Christelle; Thelcide, Chloë; Crespin-Maillard, Fabienne; Maillard, Christian; Kinowski, Jean Marie; Favier, Mireille

    2005-10-01

    The compatibility of ondansetron hydrochloride and methylprednisolone sodium succinate in 5% dextrose injection and 0.9% sodium chloride injection was studied. Test solutions of ondansetron hydrochloride 0.16 mg/mL and methylprednisolone sodium succinate 2.4 mg/mL were prepared in triplicate and tested in duplicate. Total volumes of 4 and 2 mL of ondansetron hydrochloride solution and methylprednisolone sodium succinate solution, respectively, were added to 50-mL multilayer polyolefin bags containing 5% dextrose injection or 0.9% sodium chloride injection. Bags were stored for 24 hours at 20-25 degrees C and for 48 hours at 4-8 degrees C. Chemical compatibility was measured with high-performance liquid chromatography, and physical compatibility was determined visually. Ondansetron hydrochloride was stable for up to 24 hours at 20-25 degrees C and up to 48 hours at 4-8 degrees C. Methylprednisolone sodium succinate was stable for up to 48 hours at 4-8 degrees C. When stored at 20-25 degrees C, methylprednisolone sodium succinate was stable for up to 7 hours in 5% dextrose injection and up to 24 hours in 0.9% sodium chloride injection. Compatibility data for solutions containing ondansetron hydrochloride plus methylprednisolone sodium succinate revealed that each drug was stable for up to 24 hours at 20-25 degrees C and up to 48 hours at 4-8 degrees C. Ondansetron 0.16 mg/mL (as the hydrochloride) and methylprednisolone 2.4 mg/mL (as the sodium succinate) mixed in 50-mL multilayer polyolefin bags were stable in both 5% dextrose injection and 0.9% sodium chloride injection for up to 24 hours at 20-25 degrees C and up to 48 hours at 4-8 degrees C.

  2. Molecular interactions between selected sodium salts of bile acids and morphine hydrochloride.

    Science.gov (United States)

    Poša, Mihalj; Csanádi, János; Kövér, Katalin E; Guzsvány, Valéria; Batta, Gyula

    2012-06-01

    The objective of this study was to understand the prolonged analgesic action of morphine hydrochloride observed in the presence of sodium 12-oxochenodeoxycholanate. Based on literature, this phenomenon may be due to the formation of aggregates in the cell between the molecules of bile acids and morphine. In addition to the sodium 12-oxochenodeoxycholanate, the present investigation also included salts of cholic and 7-oxodeoxycholic acids. Saturation transfer difference NMR experiments showed that morphine binds to the bile acid molecule close to the aromatic protons H1 and H2 provided that the concentration of the bile acid salt approaches the critical micellar concentration (CMC). The spin-lattice relaxation times (T(1)) of the affected protons decrease significantly in the presence of micellar solutions of the bile acid salts, and the most pronounced change in T(1) was observed for sodium 7-oxodeoxycholate. Diffusion-ordered NMR experiments suggested that morphine hydrochloride can interact only with sodium 7-oxochenodeoxycholate. It can be supposed that the molecular ratio of sodium 7-oxodeoxycholate and morphine hydrochloride in the mixed micelle is 2:1. The CMC values of mixed micelles do not differ from the CMC values of the micelle constituents, which suggests that the binding of morphine hydrochloride does not perturb the hydrophobic domain of the bile acid molecule. In the presence of bile acids, the transfer rate constant (k(12)) of morphine hydrochloride from the buffered aqueous solution to chloroform (model of the cell membrane) shows a decrease. A significant decrease of the k(12) was also observed in the presence of micellar solutions. Kinetic measurements indicated that, in addition to micellar interaction between morphine hydrochloride and sodium salts of bile acids, a complex may also be formed in chloroform via hydrogen bonds formed between the drug and bile acid molecules. Copyright © 2012 Elsevier B.V. All rights reserved.

  3. Influence of family history, irradiation and anti-cancer drug (mitomycin C) on the occurrence of multiple primary neoplasms in breast carcinoma patients

    International Nuclear Information System (INIS)

    Yoshimoto, Masataka; Sakamoto, Goi; Sugano, Haruo; Kasumi, Fujio; Fukami, Atsuo; Kuno, Keijiro.

    1984-01-01

    The influence of family history, irradiation and anti-cancer drug (Mitomycin C) on the occurrence of multiple primary neoplasms was analysed using the person-year method in 1359 Japanese breast carcinoma patients. There were 111 multiple primary neoplasms, including bilaterl breast cancer, in 109 patients; the incidence rate was 0.0072 per person-year. The incidence rate in patients with a family history of cancer was 1.29 times higher than in those without. In the bilateral breast cancer group there was about a 3 times higher frequency of family history of breast cancer. Irradiation therapy raised the occurrence of multiple primary neoplasms 1.28 fold, and Mitomycin C (40 mg) had no effect on the occurrence of neoplasms during a 10-year observation period. (author)

  4. Neuroprotection against vascular dementia after acupuncture combined with donepezil hydrochloride: P300 event related potential

    Directory of Open Access Journals (Sweden)

    Qiang Liu

    2016-01-01

    Full Text Available Acupuncture can be used to treat various nervous system diseases. Here, 168 vascular dementia patients were orally administered donepezil hydrochloride alone (5 mg/day, once a day for 56 days, or combined with acupuncture at Shenting (DU24, Tianzhu (BL10, Sishencong (Extra, Yintang (Extra, Renzhong (DU26, Neiguan (PC6, Shenmen (HT7, Fengchi (GB20, Wangu (GB12 and Baihui (DU20 (once a day for 56 days. Compared with donepezil hydrochloride alone, P300 event related potential latency was shorter with an increased amplitude in patients treated with donepezil hydrochloride and acupuncture. Mini-Mental State Examination score was also higher. Moreover, these differences in P300 latency were identified within different infarcted regions in patients treated with donepezil hydrochloride and acupuncture. These findings indicate that acupuncture combined with donepezil hydrochloride noticeably improves cognitive function in patients with vascular dementia, and exerts neuroprotective effects against vascular dementia.

  5. Geometry optimization of antimuscarinic, anticholinergic and antispasmodic aprophen hydrochloride

    International Nuclear Information System (INIS)

    Bano, F.; Akhter, N.

    2013-01-01

    Aprophen hydrochloride extensively used as anticholinergic, antimuscarinnin and antispasmodic agent. Structure based drug designed is based on the firm understanding of molecular recognition between active site group and interacting molecules ,it is strategy that become as integral part of modem drug discovery. The aim of present study is find out the minimum potential energy for aprophen hydrochloride. The potential energy of the molecule in molecular mechanics calculated by using force field concept. Potential energy effect the inter action of drug molecule with receptor these properties could be use to synthesize new drug candidates with improve pharmacological and therapeutic activity. (author)

  6. Simultaneous determination of nortriptyline hydrochloride and fluphenazine hydrochloride in microgram quantities from low dosage forms by liquid chromatography–UV detection

    Directory of Open Access Journals (Sweden)

    Safwan Ashour

    2012-12-01

    Full Text Available A novel method for the simultaneous high-performance liquid chromatographic determination of nortriptyline hydrochloride and fluphenazine hydrochloride was developed and validated. Fluvastatin sodium was used as internal standard. The determination was performed on a Hypersil Gold C8 column (250 mm × 4.6 mm i.d., 5 μm particle size at 25 °C; the mobile phase, consisting of a mixture of formic acid (0.1 M, pH 2.16-methanol (33:67, v/v, was delivered at a flow rate of 1.1 mL/min and detector wavelength at 251 nm. The retention time of nortriptyline, fluphenazine and fluvastatin was found to be 5.11, 8.05 and 11.38 min, respectively. Linearity ranges were 5.0–1350.0 and 10.0–1350.0 μg/mL with limit of detection values of 0.72 and 0.31 μg/mL, for nortriptyline and fluphenazine, respectively. Results of assay and recovery studies were statistically evaluated for its accuracy and precision. Correlation coefficients (r2 of the regression equations were greater than 0.999 in all cases. According to the validation results, the proposed method was found to be specific, accurate, precise and could be applied to the simultaneous quantitative analysis of nortriptyline and fluphenazine. Keywords: Nortriptyline hydrochloride, Fluphenazine hydrochloride, Liquid chromatography, Pharmaceutical dosage form

  7. Cinacalcet hydrochloride for the treatment of hyperparathyroidism

    NARCIS (Netherlands)

    Verheyen, N.; Pilz, S.; Eller, K.; Kienreich, K.; Fahrleitner-Pammer, A.; Pieske, B.; Ritz, E.; Tomaschitz, A.

    2013-01-01

    Introduction: Effective therapeutic strategies are warranted to reduce the burden of parathyroid hormone excess related morbidity and mortality. The calcimimetic agent cinacalcet hydrochloride is a promising treatment strategy in hyperparathyroidism. Areas covered: This review provides an overview

  8. 141 137 Effect of Guanidium Hydrochloride o

    African Journals Online (AJOL)

    2008-12-02

    Dec 2, 2008 ... Effect of Guanidium Hydrochloride on the Stability of Horse Skeletal. Muscle Myoglobin ... Proteins carry out the most important tasks in living organisms. To do so, most proteins fold spontaneously into a well defined three –.

  9. UV Spectrophotometric Method for theEstimation of Itopride Hydrochloride in Pharmaceutical Formulation

    Directory of Open Access Journals (Sweden)

    K. R. Gupta

    2010-01-01

    Full Text Available Three simple, precise and economical UV methods have been developed for the estimation of itopride hydrochloride in pharmaceutical formulations. Itopride hydrochloride in distilled water shows the maximum absorbance at 258.0 nm (Method A and in first order derivative spectra of the same shows sharp peak at 247.0 nm, when n = 1 (Method B. Method C utilises area under curve (AUC in the wavelength range from 262.0-254.0 nm for analysis of itopride hydrochloride. The drug was found to obey Beer-Lambert’s law in the concentration range of 5-50 μg/mL for all three proposed methods. Results of the analysis were validated statistically and recovery studies were found to be satisfactory.

  10. Salt Solubility Products of Diprenorphine Hydrochloride, Codeine and Lidocaine Hydrochlorides and Phosphates – Novel Method of Data Analysis Not Dependent on Explicit Solubility Equations

    Directory of Open Access Journals (Sweden)

    Gergely Völgyi

    2013-12-01

    Full Text Available A novel general approach was described to address many of the challenges of salt solubility determination of drug substances, with data processing and refinement of equilibrium constants encoded in the computer program pDISOL-XTM. The new approach was illustrated by the determinations of the solubility products of diprenorphine hydrochloride, codeine hydrochloride and phosphate, lidocaine hydrochloride and phosphate at 25 oC, using a recently-optimized saturation shake-flask protocol.  The effects of different buffers (Britton-Robinson universal and Sörensen phosphate were compared. Lidocaine precipitates were characterized by X-ray powder diffraction (XRPD and polarization light microscopy. The ionic strength in the studied systems ranged from 0.25 to 4.3 M. Codeine (and possibly diprenorphine chloride were less soluble than the phosphates for pH > 2. The reverse trend was evident with lidocaine.  Diprenorphine saturated solutions showed departure from the predictions of the Henderson-Hasselbalch equation in alkaline (pH > 9 solutions, consistent with the formation of a mixed-charge anionic dimer.

  11. Effect of paclitaxel, epirubicin and tamoxifen on labelling index in cultured ehrlich ascites tumor cells

    International Nuclear Information System (INIS)

    Arican, G. Oe.; Oezalpan, A.

    2001-01-01

    The effect of Paclitaxel (PAC), Epirubicin (EPR) and Tamoxifen (TAM) on ''3H-thymidine labelling index (''3H-TdR LI) of Ehrlich ascites tumor cells (EAT) was investigated in cultured. In the present study, an estrogen receptor positive ER(+) hyper diploid cell lines were studied. We used optimum doses of PAC, EPR and TAM (12 mg/ml, 12 mg/ml and 2 mg/ml, respectively). Cells were treated with these doses for 0, 4, 8, 16 and 32 hours. At the end of these periods, both control and treated cells were labelled for 5 mCi/ml 3H-thymidine for 30 minutes. The results showed that inhibition of DNA synthesis in cultured EAT cells were increased in the combined treatment of two drugs when compared to the treatment of a single drug (p<0.01). In the treatment of three drugs, however, this effect reached a maximum (p<0.001). As a result, PAC+EPR+TAM treatment's had a maximum synergistic effect at 4 hours treatment

  12. Spectrophotometric determination of dopamine hydrochloride in pharmaceutical, banana, urine and serum samples by potassium ferricyanide-Fe(III).

    Science.gov (United States)

    Guo, Li; Zhang, Yan; Li, Quanmin

    2009-12-01

    In the present work, we developed a simple, sensitive and inexpensive method to determine dopamine hydrochloride using potassium ferricyanide-Fe(III) by spectrophotometry. The results show that Fe(III) is deoxidized to Fe(II) by dopamine hydrochloride at pH 4.0, and then Fe(II) reacts with potassium ferricyanide to form a soluble prussian blue (KFe(III)[Fe(II)(CN)6]). The absorbance of this product was monitored over time using a spectrophotometer at an absorption maximum of 735 nm, and the amount of dopamine hydrochloride could be calculated based on the absorbance. A good linear relationship of the concentration of dopamine hydrochloride versus absorbance was observed, and a linear regression equation of A = 0.022 + 0.16921C (microg mL(-1)) was obtained. Moreover, the apparent molar absorption coefficient for the indirect determination of dopamine hydrochloride was 3.2 x 10(4) L mol(-1) cm(-1). This described method has been used to determine dopamine hydrochloride in pharmaceutical, banana, urine and serum samples with satisfactory results.

  13. Preparation and evaluation of mebeverine hydrochloride as ...

    African Journals Online (AJOL)

    Purpose: To formulate and evaluate an antispasmodic drug, mebeverine hydrochloride (Mbv-HCl), as a local anesthetic mucoadhesive buccal tablet. Methods: Mbv-HCl loaded tablets were formulated, using a direct compression technique, with varying polymer concentrations including carbopol 934P alone, carbopol ...

  14. Formulation of Extended-Release Metformin Hydrochloride Matrix ...

    African Journals Online (AJOL)

    Methods: Various metformin hydrochloride formulations containing a hydrophobic carrier (stearic acid) and a hydrophilic polymer (polyethylene oxide) were prepared using a 32 factorial design. ... The release data were subjected to various release kinetic models and also compared with those of a commercial brand.

  15. Application of physiologically based pharmacokinetic modeling in predicting drug–drug interactions for sarpogrelate hydrochloride in humans

    Directory of Open Access Journals (Sweden)

    Min JS

    2016-09-01

    Full Text Available Jee Sun Min,1 Doyun Kim,1 Jung Bae Park,1 Hyunjin Heo,1 Soo Hyeon Bae,2 Jae Hong Seo,1 Euichaul Oh,1 Soo Kyung Bae1 1Integrated Research Institute of Pharmaceutical Sciences, College of Pharmacy, The Catholic University of Korea, Bucheon, 2Department of Pharmacology, College of Medicine, The Catholic University of Korea, Seocho-gu, Seoul, South Korea Background: Evaluating the potential risk of metabolic drug–drug interactions (DDIs is clinically important. Objective: To develop a physiologically based pharmacokinetic (PBPK model for sarpogrelate hydrochloride and its active metabolite, (R,S-1-{2-[2-(3-methoxyphenylethyl]-phenoxy}-3-(dimethylamino-2-propanol (M-1, in order to predict DDIs between sarpogrelate and the clinically relevant cytochrome P450 (CYP 2D6 substrates, metoprolol, desipramine, dextromethorphan, imipramine, and tolterodine. Methods: The PBPK model was developed, incorporating the physicochemical and pharmacokinetic properties of sarpogrelate hydrochloride, and M-1 based on the findings from in vitro and in vivo studies. Subsequently, the model was verified by comparing the predicted concentration-time profiles and pharmacokinetic parameters of sarpogrelate and M-1 to the observed clinical data. Finally, the verified model was used to simulate clinical DDIs between sarpogrelate hydrochloride and sensitive CYP2D6 substrates. The predictive performance of the model was assessed by comparing predicted results to observed data after coadministering sarpogrelate hydrochloride and metoprolol. Results: The developed PBPK model accurately predicted sarpogrelate and M-1 plasma concentration profiles after single or multiple doses of sarpogrelate hydrochloride. The simulated ratios of area under the curve and maximum plasma concentration of metoprolol in the presence of sarpogrelate hydrochloride to baseline were in good agreement with the observed ratios. The predicted fold-increases in the area under the curve ratios of metoprolol

  16. Atovaquone and proguanil hydrochloride for prophylaxis of malaria.

    Science.gov (United States)

    Shanks, G D; Kremsner, P G; Sukwa, T Y; van der Berg, J D; Shapiro, T A; Scott, T R; Chulay, J D

    1999-05-01

    The spread of drug-resistant malaria and appreciation of side effects associated with existing antimalarial drugs emphasize the need for new drugs to prevent malaria. The combination of atovaquone and proguanil hydrochloride was previously shown to be safe and highly effective for treatment of malaria, including multi-drug-resistant Plasmodium falciparum. We reviewed results of clinical trials that evaluated either a fixed-dose combination of atovaquone and proguanil hydrochloride for malaria prophylaxis or atovaquone alone for causal prophylactic activity against P. falciparum. In three placebo-controlled trials, 331 subjects received 250 mg atovaquone and 100 mg proguanil hydrochloride (or an equivalent dose based on body weight in children) once daily for 10 to 12 weeks. The overall efficacy for preventing parasitemia was 98%. Among 175 nonimmune volunteers taking the same dose of atovaquone/proguanil once daily for 10 weeks while temporarily residing in a malaria-endemic area, malaria developed in one patient who was noncompliant with therapy. Results of volunteer challenge studies indicate that both atovaquone and proguanil have causal prophylactic activity directed against the liver stages of P. falciparum. Adverse events occurred with similar or lower frequencies in subjects treated with atovaquone/proguanil compared to placebo. Less than 1% of patients discontinued from these studies due to a treatment-related adverse event. A fixed-dose combination of atovaquone and proguanil hydrocloride is a promising new alternative for malaria prophylaxis.

  17. Simultaneous HPTLC Determination of Rabeprazole and Itopride Hydrochloride From Their Combined Dosage Form.

    Science.gov (United States)

    Suganthi, A; John, Sofiya; Ravi, T K

    2008-01-01

    A simple, precise, sensitive, rapid and reproducible HPTLC method for the simultaneous estimation of the rabeprazole and itopride hydrochloride in tablets was developed and validated. This method involves separation of the components by TLC on precoated silica gel G60F254 plate with solvent system of n-butanol, toluene and ammonia (8.5:0.5:1 v/v/v) and detection was carried out densitometrically using a UV detector at 288 nm in absorbance mode. This system was found to give compact spots for rabeprazole (Rf value of 0.23 0.02) and for itopride hydrochloride (Rf value of 0.75+/-0.02). Linearity was found to be in the range of 40-200 ng/spot and 300-1500 ng/spot for rabeprazole and itopride hydrochloride. The limit of detection and limit of quantification for rabeprazole were 10 and 20 ng/spot and for itopride hydrochloride were 50 and 100 ng/spot, respectively. The method was found to be beneficial for the routine analysis of combined dosage form.

  18. 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.

  19. 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.

  20. Therapeutic effect of an injectable sustained-release sinomenine hydrochloride and sodium hyaluronate compound in a rabbit model of osteoarthritis.

    Science.gov (United States)

    Liu, Wen-Guang; Ling, Pei-Xue; Lin, Xiu-Kun; Chen, Jian-Ying; Wang, Shao-Jin; Li, Peng; Wu, Xiao-Juan; Zhao, Dong-Mei; Liu, Sheng-Hou

    2012-07-01

    While intra-articular injection of sinomenine hydrochloride has a therapeutic effect on osteoarthritis, it has a short half-life, and is thermolabile and photolabile. The aim of this research was to evaluate the sustained-release of sinomenine hydrochloride from an injectable sinomenine hydrochloride and sodium hyaluronate compound (CSSSI) and its therapeutic effect in a rabbit model of osteoarthritis following intra-articular injection. An injectable compound consisting of 1% sodium hyaluronate and 2.5% sinomenine hydrochloride was prepared and kept as the experiment group, and 2.5% sinomenine hydrochloride was prepared and kept as the control group. The cumulative mass release was measured at different time points in each group in vitro. Sixty-five male Zelanian rabbits were randomly divided into five groups: 15 (30 knees) each for the control, sodium hyaluronate, sinomenine hydrochloride, and CSSSI groups respectively, and five (10 knees) for the modeling group. Papain was injected into both knees of each rabbit for model establishment. Subsequently, 0.2 ml of the corresponding drugs was injected into the articular cavities of the remaining experiment groups, while the control group was treated with 0.2 ml normal saline. All groups were treated once a week for 4 weeks. Seven days after the last treatment, knees were anatomized to perform pathological observations and Mankin's evaluation of the synovium. Four groups were compared using the SPSS 13.0 software package. In the in vitro sustained-release experiments, 90% of the drug was released in the experiment group 360 minutes following the injection. Comparison of the Mankin's evaluations of the four groups illustrated statistical discrepancies (P sodium hyaluronate/sinomenine hydrochloride groups, statistical significance was uniformly obtained. Moreover, sodium hyaluronate and sinomenine hydrochloride treatments showed significant improvement over the modeling control (P sodium hyaluronate vs. sinomenine

  1. O6-methylguanine DNA-methyltransferase (MGMT) overexpression in melanoma cells induces resistance to nitrosoureas and temozolomide but sensitizes to mitomycin C

    International Nuclear Information System (INIS)

    Passagne, Isabelle; Evrard, Alexandre; Depeille, Philippe; Cuq, Pierre; Cupissol, Didier; Vian, Laurence

    2006-01-01

    Alkylating agents play an important role in the chemotherapy of malignant melanomas. The activity of alkylating agents depends on their capacity to form alkyl adducts with DNA, in some cases causing cross-linking of DNA strands. However, the use of these agents is limited by cellular resistance induced by the DNA repair enzyme O 6 -methylguanine DNA-methyltransferase (MGMT) which removes alkyl groups from alkylated DNA strands. To determine to what extent the expression of MGMT in melanoma cells induces resistance to alkylating agents, the human cell line CAL77 Mer- (i.e., MGMT deficient) were transfected with pcMGMT vector containing human MGMT cDNA. Several clones expressing MGMT at a high level were selected to determine their sensitivity to chemotherapeutic drugs. Melanoma-transfected cells were found to be significantly less sensitive to nitrosoureas (carmustine, fotemustine, streptozotocin) and temozolomide with an increase of IC 5 values between 3 and 14 when compared to parent cells. No difference in cell survival rates between MGMT-proficient and -deficient cells was observed for melphalan, chlorambucil, busulphan, thiotepa and cisplatin which preferentially induce N 7 guanine lesions. Surprisingly, MGMT overexpression increased the sensitivity of CAL77 cells to mitomycin C by approximately 10-fold. Treatment of clonal cell lines with buthionine-[S,R]-sulfoximine (BSO), an inhibitor of γ-glutamylcysteine synthetase which depletes cellular glutathione, completely reversed this unexpected increase in sensitivity to mitomycin C. This observation suggests that glutathione is involved in the sensitivity of MGMT-transfected cells to mitomycin C and may act synergistically with MGMT via an unknown mechanism

  2. O(6)-methylguanine DNA-methyltransferase (MGMT) overexpression in melanoma cells induces resistance to nitrosoureas and temozolomide but sensitizes to mitomycin C.

    Science.gov (United States)

    Passagne, Isabelle; Evrard, Alexandre; Depeille, Philippe; Cuq, Pierre; Cupissol, Didier; Vian, Laurence

    2006-03-01

    Alkylating agents play an important role in the chemotherapy of malignant melanomas. The activity of alkylating agents depends on their capacity to form alkyl adducts with DNA, in some cases causing cross-linking of DNA strands. However, the use of these agents is limited by cellular resistance induced by the DNA repair enzyme O(6)-methylguanine DNA-methyltransferase (MGMT) which removes alkyl groups from alkylated DNA strands. To determine to what extent the expression of MGMT in melanoma cells induces resistance to alkylating agents, the human cell line CAL77 Mer- (i.e., MGMT deficient) were transfected with pcMGMT vector containing human MGMT cDNA. Several clones expressing MGMT at a high level were selected to determine their sensitivity to chemotherapeutic drugs. Melanoma-transfected cells were found to be significantly less sensitive to nitrosoureas (carmustine, fotemustine, streptozotocin) and temozolomide with an increase of IC(50) values between 3 and 14 when compared to parent cells. No difference in cell survival rates between MGMT-proficient and -deficient cells was observed for melphalan, chlorambucil, busulphan, thiotepa and cisplatin which preferentially induce N(7) guanine lesions. Surprisingly, MGMT overexpression increased the sensitivity of CAL77 cells to mitomycin C by approximately 10-fold. Treatment of clonal cell lines with buthionine-[S,R]-sulfoximine (BSO), an inhibitor of gamma-glutamylcysteine synthetase which depletes cellular glutathione, completely reversed this unexpected increase in sensitivity to mitomycin C. This observation suggests that glutathione is involved in the sensitivity of MGMT-transfected cells to mitomycin C and may act synergistically with MGMT via an unknown mechanism.

  3. Quantitative Determination of Metformin Hydrochloride in Tablet ...

    African Journals Online (AJOL)

    Purpose: To develop and validate a suitable method for the assay of metformin hydrochloride (HCl) in tablets containing croscarmellose sodium as an additive. Methods: Methanol and ethanol (99%) were assessed as solvents for sample preparation for the assay of metformin HCl in tablets containing croscarmellose ...

  4. Intraoperative Injection vs Sponge-applied Mitomycin C during Trabeculectomy: One-year Study.

    Science.gov (United States)

    S Khouri, Albert; Huang, Grace; Y Huang, Linda

    2017-01-01

    To determine the safety and efficacy of intraoperative injection of mitomycin C (MMC) against conventional sponge-applied MMC during trabeculectomy. This study was a retrospective, comparative case series. Thirty eyes with primary open-angle glaucoma underwent consecutive trabeculectomies with MMC injection (injection group), and thirty eyes with sponge-applied MMC were as controls (sponge group). Data were collected preoperatively and postoperatively at 1 day, 1 week, 1 month, 3 months, 6 months, and 1 year after surgery. Demographic data, applanation intraocular pressure (IOP), best-corrected visual acuity (VA), number of glaucoma medications, postoperative interventions, postoperative complications, and number of visits within 3 months were recorded. In order to stratify data, proportion of eyes achieving >30% IOP reduction from baseline with or without glaucoma medications was calculated and defined as surgical success. Mean IOP reduction at 1 year was significant in both the injection and sponge groups from baseline (46.8 and 37.8% respectively). The injection group had overall lower postoperative IOP and comparable complete treatment success, defined as achieving >30% IOP reduction without glaucoma medications (p = 0.941). The number of postoperative visits within 3 months and the proportion of eyes needing 5-fluorouracil (5-FU) intervention were significantly lower in the injection group (p = 0.03, p = 0.04 respectively). Injection of MMC was as safe and effective as sponge application with comparable estimated complete treatment success, less need for visits within 3 months, and 5-FU intervention. Surgeons may consider intraopera-tive injection of MMC in appropriate patient cohorts given comparable safety and efficacy and several advantages over traditional sponge application. Further study in a prospective, larger, long-term manner is necessary to assess this modality. How to cite this article: Khouri AS, Huang G, Huang LY. Intraoperative Injection vs

  5. A pilot study of acotiamide hydrochloride hydrate in patients with detrusor underactivity

    Directory of Open Access Journals (Sweden)

    Sugimoto K

    2015-05-01

    Full Text Available Koichi Sugimoto,1 Takahiro Akiyama,2 Nobutaka Shimizu,3 Naoki Matsumura,1 Taiji Hayashi,1 Tsukasa Nishioka,1 Hirotsugu Uemura3 1Department of Urology, Sakai Hospital, Kinki University Faculty of Medicine, Sakai, Osaka, Japan; 2Department of Urology, Sakai-Onshinkai Hospital, Sakai, Osaka, Japan; 3Department of Urology, Kinki University Faculty of Medicine, Osaka-Sayama, Osaka, Japan Aim: To investigate the clinical efficacy of acotiamide hydrochloride hydrate in patients with detrusor underactivity. Methods: We measured the post-void residual urinary volume in 19 patients with underactive bladders. All these patients had been under treatment with distigmine bromide and were prescribed acotiamide hydrochloride hydrate at a dose of 100 mg three times daily for 2 weeks. Results: Compared with the post-void residual urinary volume value at baseline (161.4±90.0 mL a statistically significant reduction was observed at the end of treatment (116.3±63.1 mL (P=0.006. The drug was generally well tolerated by the majority of patients. Conclusion: Maybe, acotiamide hydrochloride hydrate showed clinical efficacy in patients with underactive bladders and may, therefore, be used alternatively in patients who do not respond sufficiently to distigmine bromide. Keywords: acotiamide hydrochloride hydrate, distigmine bromide, underactive bladder, detrusor underactive

  6. Fe (III) complex of mefloquine hydrochloride: Synthesis ...

    African Journals Online (AJOL)

    As part of the ongoing research for more effective antimalarial drug, Fe (III) complex of mefloquine hydrochloride (antimalarial drug) was synthesized using template method. Mefloquine was tentatively found to have coordinated through the hydroxyl and the two nitrogen atoms in the quinoline and piperidine in the structure, ...

  7. Electrochemical monitoring of the interaction between mitomycin C and DNA at chitosan--carbon nanotube composite modified electrodes

    OpenAIRE

    CANAVAR, Pembe Ece; EKŞİN, Ece; ERDEM, Arzum

    2015-01-01

    Single-walled carbon nanotube (CNT) and chitosan composite (chitosan*CNT) based sensors were developed as DNA biosensors, and then they were applied for electrochemical investigation of the interaction between the anticancer drug mitomycin C (MC) and DNA. The oxidation signals of MC and guanine were monitored before and after the interaction process by differential pulse voltammetry (DPV). The DPV results were in good agreement with those of electrochemical impedance spectroscopy (EIS)....

  8. Locoregional mitomycin C injection for esophageal stricture after endoscopic submucosal dissection.

    Science.gov (United States)

    Machida, H; Tominaga, K; Minamino, H; Sugimori, S; Okazaki, H; Yamagami, H; Tanigawa, T; Watanabe, K; Watanabe, T; Fujiwara, Y; Arakawa, T

    2012-06-01

    This prospective study aimed to evaluate the feasibility and safety of locoregional mitomycin C (MMC) injection to treat refractory esophageal strictures after endoscopic submucosal dissection (ESD) for superficial esophageal carcinoma. Patients with dysphagia and strictures that were refractory to repeated endoscopic balloon dilation (EBD) were eligible. After EBD, MMC was injected into the dilated site. Between June 2009 and August 2010, five patients were recruited. The treatment was performed once in two patients and twice in three patients with recurrent dysphagia or restenosis. In all patients, passing a standard endoscope through the site was easy and the dysphagia grade improved (grade 3→1 in 3 patients, grade 4→2 in 2 patients). No serious complications were noted. During the observation period of 4.8 months, neither recurrent dysphagia nor re-stricture appeared in any of the patients. The combination of locoregional MMC injections and EBD is feasible and safe for the treatment of esophageal strictures after ESD.Recently, endoscopic submucosal dissection (ESD) has been developed and accepted as a new endoscopic treatment for gastrointestinal tumors. ESD is a promising treatment for superficial esophageal carcinoma (SEC), and it has a reliable en bloc resection rate. However, the application of ESD for widespread lesions is challenging because of the high risk of the development of severe strictures, which lead to a low quality of life after ESD. Although endoscopic balloon dilation (EBD) is effective for benign strictures, it needs to be performed frequently until the dysphagia disappears 1. Mitomycin C (MMC), which is a chemotherapeutic agent derived from some Streptomyces species 2, reduces scar formation when topically applied to a surgical lesion. MMC has been applied to treat strictures in a variety of anatomical locations, including a variety of organs 3. The aim of this study was to prospectively evaluate both the feasibility and the safety of

  9. The Impact of Hydrochloride Heroin on Mental Flexibility, Abstract Reasoning, Impulsivity, and Attention

    Directory of Open Access Journals (Sweden)

    Zahra Alam Mehrjerdi

    2011-04-01

    Full Text Available Introduction: Drug addiction could lead to severe impairments in executive and neurocognitive functions but study on the impact of hydrochloride heroin on executive functions has remained in infancy in Iran. The aim of this study was to examine the relationship between addiction to hydrochloride heroin and executive functioning in several cognitive domains including mental flexibility, abstract reasoning, impulsivity, and attention. Methods: A total of 60 cases of young male addicts aged 18 to 21 were recruited from outpatient addiction clinics in Karaj city and were matched with 60 non-drug using controls. A test battery including the Wisconsin Card Sorting Test (WCST, Porteus Maze Test (PMQS, Serial Seven Subtraction Test (SSST, and Color Trails Test (CTT were administered respectively. Results: The patient group showed more problems in impulse control compared with the control group, while mental flexibility, abstract reasoning and attention were not affected. Discussion: The findings indicated that addiction to hydrochloride heroin had a negative effect on impulse control. This issue could reflect the role of impaired inhibitory control on drug-seeking behaviors and relapse. Special treatment programs must be tailored to control impulsivity among addicts to hydrochloride heroin during treatment.

  10. Facilitatory effect of AC-iontophoresis of lidocaine hydrochloride on the permeability of human enamel and dentine in extracted teeth.

    Science.gov (United States)

    Ikeda, Hideharu; Suda, Hideaki

    2013-04-01

    The objectives of the present study were to quantitatively evaluate chemical permeability through human enamel/dentine using conductometry and to clarify if alternating current (AC) iontophoresis facilitates such permeability. Electrical impedance of different concentrations of lidocaine hydrochloride was measured using a bipolar platinum impedance probe. A quadratic curve closely fitted to the response functions between conductance and lidocaine hydrochloride. For analysis of the passage of lidocaine hydrochloride through human enamel/dentine, eight premolars that were extracted for orthodontic treatment were sectioned at the cemento-enamel junction. The tooth crowns were held between two chambers with a double O-ring. The enamel-side chamber was filled with lidocaine hydrochloride, and the pulp-side chamber was filled with extrapure water. Two platinum plate electrodes were set at the end of each chamber to pass alternating current. A simulated interstitial pulp pressure was applied to the pulp-side chamber. The change in the concentration of lidocaine hydrochloride in the pulp-side chamber was measured every 2min using a platinum recording probe positioned at the centre of the pulp-side chamber. Passive entry without iontophoresis was used as a control. The level of lidocaine hydrochloride that passed through enamel/dentine against the dentinal fluid flow increased with time. Electrical conductance (G, mho) correlated closely to the concentration (x, mmol/L) of lidocaine hydrochloride (G=2.16x(2)+0.0289x+0.000376, r(2)=0.999). Lidocaine hydrochloride can pass through enamel/dentine. Conductometry showed that the level of lidocaine hydrochloride that passed through enamel/dentine was increased by AC iontophoresis. Copyright © 2012 Elsevier Ltd. All rights reserved.

  11. Naratriptan hydrochloride in extemporaneosly compounded oral suspensions.

    Science.gov (United States)

    Zhang, Y P; Trissel, L A; Fox, J L

    2000-01-01

    The purpose of this study was to determine the pharmaceutical acceptability and chemical stability of naratriptan hydrochloride in three extemporaneously compounded suspension formulations. The naratriptan-hydrochloride oral suspensions were prepared from 2.5-mg commercial tablets yielding a nominal naratriptan concentration of 0.5 mg/mL. The suspension vehicles selected for testing were Syrpalta, an equal-parts mixture of Ora-Plus and Ora-Sweet, and an equal-parts mixture of Ora-Plus and Ora-Sweet SF. The tablets were crushed and thoroughly triturated to a fine powder using a porcelain mortar and pestle. The powder was incorporated into a portion of the Syrpalta or Ora-Plus suspension vehicle and mixed until homogeneous. The mixtures were then brought to volume with Syrpalta, Ora-Sweet or Ora-Sweet SF, as appropriate. The suspensions were packaged in amber, plastic, screw-cap prescription bottles and stored at 23 deg C for seven days and 4 deg C for 90 days. An adequate suspension was never achieved in Syrpalta. The crushed-tablet powder did not produce a uniformly dispersed mixture and exhibited clumping and a high rate of sedimentation. A distinct layer of the solid tablet material settled immediately after shaking. Over the next four hours, a densely packed, yellow, caked layer formed at the bottom of the containers, making resuspension difficult. During storage, the caking became worse. Chemical analysis was not performed. The Ora-Plus and Ora-Sweet or Ora-Sweet SF suspensions had a slight greenish cast and were resuspended without difficulty by shaking for approximately ten seconds, yielding easily poured and homogeneous mixtures throughout the study. Visible settling and layering did not begin for four hours with the Ora-Sweet suspension and 24 hours for the Ora-Sweet SF suspension. High pressure liquid chromatographic analysis found that the naratriptan concentration in both suspension-vehicle combinations exhibited little or no loss for seven days at 23

  12. The effect of azelastine hydrochloride on radiation dermatitis and pharyngo-laryngeal mucositis in radiotherapy for laryngeal cancer

    International Nuclear Information System (INIS)

    Sako, Tsukasa; Ishiguro, Ruichiro; Morimoto, Noriko; Sakamoto, Yutaka; Fukuda, Hiroyuki

    1998-01-01

    It has recently been suggested that reactive oxides produced by inflammation may result in cell injury, leading to mucositis and dermatitis. Azelastine hydrochloride suppresses the production of cytokines and reactive oxygen species, and some reports have documented its effectiveness in treating radiation mucositis and dermatitis. Therefore, we investigated the effectiveness of azelastine hydrochloride in preventing these diseases during radiation therapy for laryngeal cancer. Subjects were patients with laryngeal carcinomas who received curative radiation therapy. A close of 1 mg of azelastine hydrochloride was administered orally twice a day, from the start of the radiation therapy until one-four weeks after the completion of therapy. Chronological changes in the pharyngo-laryngeal cavity and the neck skin of the patients who received azelastine hydrochloride were compared with those of patients who did not. In the patients who received the azelastine hydrochloride, the onset of pharyngo-laryngeal mucositis and dermatitis was suppressed; symptoms were relieved earlier and were not exacerbated. No severe side effects were observed, and the effectiveness of the radiation therapy was not affected. The administration of azelastine hydrochloride concurrently with radiation therapy for laryngeal cancer suppressed the onset of pharyngo-laryngeal mucositis and dermatitis and alleviated the severity of these diseases. (K.H.)

  13. Reconstruction of delayed scleral flap melting with bovine pericardium after trabeculectomy with mitomycin C

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    Coutinho, Inês

    2017-06-01

    Full Text Available Aim: To present a challenging case of hypotony after trabeculectomy and its treatment. Case description: A 22-year-old woman with juvenile glaucoma underwent a conventional trabeculectomy with mitomycin C on the right eye (OD. In the immediate postoperative period, we observed a hyperfiltration bleb with hypotony refractory to conservative measures leading to hypotony maculopathy.A surgical revision with scleral flap resuture and conjunctival graft was performed with a satisfactory result and resolution of hypotony maculopathy. After two years, the patient complained of low visual acuity (VA of the OD. During examination, we observed a fine and avascular bleb with Seidel and visualization of the underlying uveal tissue, an intraocular pressure (IOP of 5 mmHg, and chorioretinal folds. A new revision of the trabeculectomy was performed. During the procedure, it was not possible to identify the scleral flap, so the fistula was closed with a patch of collagenous membrane derived from bovine pericardium (Tutopatch graft. A good clinical evolution occurred. After 2 months, IOP was 15 mmHg without Seidel or changes in the fundus and VA was 20/20. After of follow-up, the IOP remains stable without further complaints. Conclusion: This case illustrates the difficulties faced in the management of a common complication of trabeculectomy and highlights some of the options available for its treatment. There are few reports of scleral melting after trabeculectomy. However, trauma and scleral necrosis associated with mitomycin are listed as the main causes.The use of a scleral patch derived from bovine pericardium allows effective suturing and closure of the aqueous leak.

  14. Determination of Montelukast Sodium and Bambuterol Hydrochloride in Tablets using RP HPLC.

    Science.gov (United States)

    Patil, Smita; Pore, Y V; Kuchekar, B S; Mane, Aruna; Khire, V G

    2009-01-01

    An accurate, specific and precise assay level gradient reverse-phase high-performance liquid chromatographic method was developed for simultaneous determination of montelukast sodium and bambuterol hydrochloride in tablet dosage form. An inertsil ODS C-18, 5 mum column having 250x4.6 mm I.D. in gradient mode, with mobile phase A, containing 0.025 M sodium phosphate buffer: methanol (85:15) and mobile phase B, containing acetonitrile:methanol (85:15) was used at different time intervals. The flow rate was 1.5 ml/min and effluent was monitored at 218 nm. The retention times of montelukast sodium and bambuterol hydrochloride were 21.2 min and 5.8 min respectively. The linearity for both the drugs was in the range of 0.25-0.75 mg/ml with correlation coefficients of 0.9999 and 0.9996 for montelukast sodium and bambuterol hydrochloride, respectively.

  15. Stability studies of lincomycin hydrochloride in aqueous solution and intravenous infusion fluids.

    Science.gov (United States)

    Czarniak, Petra; Boddy, Michael; Sunderland, Bruce; Hughes, Jeff D

    2016-01-01

    The purpose of this study was to evaluate the chemical stability of Lincocin(®) (lincomycin hydrochloride) in commonly used intravenous fluids at room temperature (25°C), at accelerated-degradation temperatures and in selected buffer solutions. The stability of Lincocin(®) injection (containing lincomycin 600 mg/2 mL as the hydrochloride) stored at 25°C±0.1°C in sodium lactate (Hartmann's), 0.9% sodium chloride, 5% glucose, and 10% glucose solutions was investigated over 31 days. Forced degradation of Lincocin(®) in hydrochloric acid, sodium hydroxide, and hydrogen peroxide was performed at 60°C. The effect of pH on the degradation rate of lincomycin hydrochloride stored at 80°C was determined. Lincomycin hydrochloride w as found to maintain its shelf life at 25°C in sodium lactate (Hartmann's) solution, 0.9% sodium chloride solution, 5% glucose solution, and 10% glucose solution, with less than 5% lincomycin degradation occurring in all intravenous solutions over a 31-day period. Lincomycin hydrochloride showed less rapid degradation at 60°C in acid than in basic solution, but degraded rapidly in hydrogen peroxide. At all pH values tested, lincomycin followed first-order kinetics. It had the greatest stability near pH 4 when stored at 80°C (calculated shelf life of 4.59 days), and was least stable at pH 2 (calculated shelf life of 0.38 days). Lincocin(®) injection was chemically found to have a shelf life of at least 31 days at 25°C when added to sodium lactate (Hartmann's) solution, 0.9% sodium chloride solution, 5% glucose solution, and 10% glucose solution. Solutions prepared at approximately pH 4 are likely to have optimum stability.

  16. High-performance liquid chromatographic analysis of methadone hydrochloride oral solution.

    Science.gov (United States)

    Beasley, T H; Ziegler, H W

    1977-12-01

    A direct and rapid high-performance liquid chromatographic assay for methadone hydrochloride in a flavored oral solution dosage form is described. A syrup sample, one part diluted with three parts of water, is introduced onto a column packed with octadecylsilane bonded on 10 micrometer porous silica gel (reversed phase). A formic acid-ammonium formate-buffered mobile phase is linear programmed with acetonitrile. The absorbance is monitored continuously at 280 or 254 nm, using a flow-through, UV, double-beam photometer. An aqueous methadone hydrochloride solution is used for external standardization. The relative standard deviation was not more than 1.0%. Drug recovery from a syrup base was better than 99.8%.

  17. Simultaneous Determination of Ciprofloxacin Hydrochloride and Dexamethasone Sodium Phosphate in Eye Drops by HPLC

    Directory of Open Access Journals (Sweden)

    Prakash Katakam

    2012-01-01

    Full Text Available A liquid chromatographic method was developed and validated for the simultaneous determination of ciprofloxacin hydrochloride and dexamethasone sodium phosphate in bulk and pharmaceutical formulations. Optimum separation was achieved in less than 5 min using a C18 column (250 mmx4.6 mm i.d, 5μ particle size by isocratic elution. The mobile phase consisting of a mixture of mixed phosphate buffer (pH 4 and acetonitrile (65:35, v/v was used. Column effluents were monitored at 254 nm at a flow rate of 1ml/min. Retention times of ciprofloxacin hydrochloride and dexamethasone sodium phosphate were 2.0 and 3.16 min respectively. The linearity of ciprofloxacin hydrochloride and dexamethasone sodium phosphate was in the range of 3-18 μg/ml and 1-6 μg/ml respectively. Developed method was economical in terms of the time taken and amount of solvent consumed for each analysis. The method was validated and successfully applied to the simultaneous determination of ciprofloxacin hydrochloride and dexamethasone sodium phosphate in bulk and pharmaceutical formulations.

  18. Effects of low dose mitomycin C on experimental tumor radiotherapy

    International Nuclear Information System (INIS)

    Yang Jianzheng; Liang Shuo; Qu Yaqin; Pu Chunji; Zhang Haiying; Wu Zhenfeng; Wang Xianli

    2001-01-01

    Objective: To evaluate the possibility of low dose mitomycin C(MMC) as an adjunct therapy for radiotherapy. Methods: Change in tumor size tumor-bearing mice was measured. Radioimmunoassay was used to determine immune function of mice. Results: Low dose Mac's pretreatment reduced tumor size more markedly than did radiotherapy only. The immune function in mice given with low dose MMC 12h before radiotherapy was obviously higher than that in mice subjected to radiotherapy only (P<0.05), and was close to that in the tumor-bearing mice before radiotherapy. Conclusion: Low dose MMC could improve the radiotherapy effect. Pretreatment with low dose MMC could obviously improve the immune suppression state in mice caused by radiotherapy. The mechanism of its improvement of radiotherapeutic effect by low dose of MMC might be due to its enhancement of immune function and induction of adaptive response in tumor-bearing mice

  19. Enantioseparation of palonosetron hydrochloride by micellar electrokinetic chromatography with sodium cholate as chiral selector.

    Science.gov (United States)

    Tian, Kan; Chen, Hongli; Tang, Jianghong; Chen, Xingguo; Hu, Zhide

    2006-11-03

    The enantioseparation of four stereoisomers of palonosetron hydrochloride by micellar electrokinetic chromatography using sodium cholate as chiral surfactant was described. Sodium cholate was shown to be effective in separating palonosetron hydrochloride stereoisomers. For method optimization, several parameters such as sodium cholate concentration, buffer pH and concentration, the types and concentration of organic modifiers and applied voltage, on the enantioseparation were evaluated and the optimum conditions were obtained as follows: 30 mM borate buffer (pH 9.40) containing 70 mM sodium cholate and 20% (v/v) methanol with an applied voltage of 20 kV. Under these conditions, baseline separation of palonosetron hydrochloride stereoisomers was achieved within 18 min.

  20. Comparative study of encapsulated blebs following Ahmed glaucoma valve implantation and trabeculectomy with mitomycin-C.

    Science.gov (United States)

    Bae, Kunho; Suh, Wool; Kee, Changwon

    2012-08-01

    To compare the histopathologic and morphologic findings of encapsulated blebs following Ahmed glaucoma valve implantation and primary standard trabeculectomy with mitomycin-C. We reviewed the records of patients with otherwise uncontrollable glaucoma who had undergone Ahmed glaucoma valve implantation or trabeculectomy with mitomycin-C. Five eyes that underwent Ahmed valve implantation and three eyes that underwent trabeculectomy needed surgical revision of the initial surgery due to encapsulated bleb development with total loss of function. The surgically removed encapsulated blebs were analyzed macroscopically and microscopically. Removal of the encapsulated bleb was performed at a mean follow-up time of 26.6 ± 19.4 weeks in the Ahmed valve implantation group and 12.0 ± 11.4 weeks in the trabeculectomy group. The fibrotic wall of the encapsulated blebs had an overall thickness of 2.48 ± 0.42 mm in the Ahmed valve implantation group and 1.62 ± 0.37 mm in the trabeculectomy group. Macroscopically, the coconut flesh-like smooth surface was split into two layers, and the wall of the capsule was thicker in the Ahmed valve implantation group than in the trabeculectomy group. Histopathologically, the fibrotic capsule was composed of an inner fibrodegenerative layer and an outer fibrovascular layer, and there were no histopathological differences between the two groups. The fibrotic capsule wall was thicker in the Ahmed valve group, but there were no differences in histological findings between the two groups.

  1. Combination atovaquone and proguanil hydrochloride vs. halofantrine for treatment of acute Plasmodium falciparum malaria in children.

    Science.gov (United States)

    Anabwani, G; Canfield, C J; Hutchinson, D B

    1999-05-01

    Malaria is a major cause of pediatric mortality in sub-Saharan Africa. Worldwide estimates of mortality among children with Plasmodium falciparum malaria range from 1 to 2 million deaths per year. Management of malaria is increasingly difficult because of the global spread of drug-resistant strains of P. falciparum. There is an urgent need for safe and effective new therapies to treat multidrug-resistant malaria. This open label, randomized trial compared atovaquone and proguanil hydrochloride with halofantrine for treatment of acute, uncomplicated P. falciparum malaria in children age 3 to 12 years (84 patients per group). Study drug dosages were adjusted by weight (approximately 20 and 8 mg/kg daily for three doses for atovaquone and proguanil hydrochloride and 8 mg/kg every 6 h for three doses for halofantrine). Patients were monitored by serial clinical and laboratory assessments for 28 days after starting treatment. Both regimens were effective (cure rate, 93.8% for atovaquone and proguanil hydrochloride and 90.4% for halofantrine) and produced prompt defervescence. Mean parasite clearance times were 50.2 h for halofantrine and 64.9 h for atovaquone and proguanil hydrochloride. More adverse experiences were reported in children treated with halofantrine (119) than with atovaquone and proguanil hydrochloride (73). In Kenyan children the combination of atovaquone and proguanil hydrochloride has efficacy comparable with that of halofantrine for treatment of acute uncomplicated multidrug-resistant falciparum malaria and is associated with a lower rate of adverse events.

  2. Determination and correlation of pyridoxine hydrochloride solubility in different binary mixtures at temperatures from (278.15 to 313.15) K

    International Nuclear Information System (INIS)

    Han, Dandan; Li, Xiaona; Wang, Haisheng; Wang, Yan; Du, Shichao; Yu, Bo; Liu, Yumin; Xu, Shijie; Gong, Junbo

    2016-01-01

    Highlights: • Solubility of pyridoxine hydrochloride in three binary mixtures was determined. • Experimental solubility of pyridoxine hydrochloride was correlated by four models. • Mixing thermodynamics of pyridoxine hydrochloride were calculated and discussed. - Abstract: The solubility of pyridoxine hydrochloride in binary solvent mixtures, including (acetone + water), (methanol + water) and (ethanol + water), was measured over temperature range from (278.15 to 313.15) K by a gravimetric method at atmospheric pressure (P = 0.1 MPa). The solubility increased with increasing temperature in binary solvent mixtures at constant solvent composition. Besides, the dissolving capacity of pyridoxine hydrochloride in the three binary solvent mixtures at constant temperature ranked as (methanol + water > ethanol + water > acetone + water) in general, partly depending on the polarity of the solvents. Additionally, the modified Apelblat equation, van’t Hoff equation, CNIBS/R–K model and Jouyban–Acree model were used to correlate the solubility data in binary mixtures, it turned out that all the selected thermodynamic models could give satisfactory results. Furthermore, the mixing thermodynamic properties of pyridoxine hydrochloride in different binary solvent mixtures were also calculated and discussed. The results indicate that the mixing process of pyridoxine hydrochloride in the selected solvents is exothermic.

  3. Mitomycin-C-Induced TTP/HUS Treated Successfully with Rituximab: Case Report and Review of the Literature

    Directory of Open Access Journals (Sweden)

    Gunjan Shah

    2013-01-01

    Full Text Available Microangiopathic hemolytic anemia (MAHA, thrombocytopenia, fever, renal failure, and neurologic symptoms comprise the cardinal features of thrombotic thrombocytopenic purpura and hemolytic uremic syndrome. Etiologies can include medications, infections, cancers, or transplantation. We present a patient with a history of rectal cancer treated with mitomycin-C who developed MAHA, acute kidney injury, and thrombocytopenia 6 months after completing therapy and to did not respond the plasmapheresis or steroids. She was treated with four weekly doses of rituximab with full recovery.

  4. Preoperative infusion of mitomycin-C in the bronchial artery in squamous cell carcinoma of the lung

    Energy Technology Data Exchange (ETDEWEB)

    Hellekant, C; Boijsen, E; Svanberg, L [Departments of Diagnostic Radiology and Thoracic Sugery, Malmoe Allmaenna Sjukhus, Malmoe, Sweden

    1978-01-01

    Bronchial angiography was performed in 9 patients with squamous cell carcinoma of the lung. The tumour-feeding vessel was identified and infused with 10 mg of mitomycin-C (MMC) diluted in saline. At operation after 28 to 48 days complete remission of the tumour had occurred in 2 patients, almost complete in one, partial remission in 2 and a marked regression in 2. In 2 patients no change was noted. No side effects except moderate malaise and slight fever occurred.

  5. BCG+MMC trial: adding mitomycin C to BCG as adjuvant intravesical therapy for high-risk, non-muscle-invasive bladder cancer: a randomised phase III trial (ANZUP 1301)

    International Nuclear Information System (INIS)

    Hayne, Dickon; Stockler, Martin; McCombie, Steve P.; Chalasani, Venu; Long, Anne; Martin, Andrew; Sengupta, Shomik; Davis, Ian D.

    2015-01-01

    Despite adequate trans-urethral resection of the bladder tumour (TURBT), non-muscle-invasive bladder cancer (NMIBC) is associated with high rates of recurrence and progression. Instillation of Bacillus Calmette-Guérin (BCG) into the urinary bladder after TURBT (adjuvant intravesical administration) reduces the risk of both recurrence and progression, and this is therefore the standard of care for high-risk tumours. However, over 30 % of people still recur or progress despite optimal delivery of BCG. Our meta-analysis suggests that outcomes might be improved further by using an adjuvant intravesical regimen that includes both mitomycin and BCG. These promising findings require corroboration in a definitive, large scale, randomised phase III trial using standard techniques for intravesical administration. The BCG + MMC trial (ANZUP 1301) is an open-label, randomised, stratified, two-arm multi-centre phase III trial comparing the efficacy and safety of standard intravesical therapy (BCG alone) against experimental intravesical therapy (BCG and mitomycin) in the treatment of adults with resected, high-risk NMIBC. Participants in the control group receive standard treatment with induction (weekly BCG for six weeks) followed by maintenance (four-weekly BCG for ten months). Participants in the experimental group receive induction (BCG weeks 1, 2, 4, 5, 7, and 8; mitomycin weeks 3, 6, and 9) followed by four-weekly maintenance (mitomycin weeks 13, 17, 25, 29, 37, and 41; BCG weeks 21, 33, and 45). The trial aims to include 500 participants who will be centrally randomised to one of the two treatment groups in a 1:1 ratio stratified by T-stage, presence of CIS, and study site. The primary endpoint is disease-free survival; secondary endpoints are disease activity, time to recurrence, time to progression, safety, health-related quality of life, overall survival, feasibility, and resource use

  6. Management of attention-deficit hyperactivity disorder in adults: focus on methylphenidate hydrochloride

    Directory of Open Access Journals (Sweden)

    Rajasree Nair

    2009-08-01

    Full Text Available Rajasree Nair, Shannon B MossBaylor Family Medicine Residency at Garland, Garland, Texas, USAAbstract: Attention-deficit hyperactivity disorder (ADHD is one of the most common psychiatric disorders in young adults and causes significant psychosocial impairment and economic burden to society. Because of the paucity of long-term evidence and lack of national guidelines for diagnosis and management of adult ADHD, most of the data are based on experience derived from management of childhood ADHD. This article reviews the current evidence for the diagnosis and management of adult ADHD with special emphasis on the role of methylphenidate hydrochloride preparations in its treatment. Methylphenidate hydrochloride, a stimulant that acts through the dopaminergic and adrenergic pathways, has shown more than 75% efficacy in controlling the symptoms of adult ADHD. Although concern for diversion of the drug exists, recent data have shown benefits in preventing substance use disorders in patients with adult ADHD.Keywords: adult ADHD, treatment, stimulants, methylphenidate hydrochloride

  7. Spectrophotometric methods for simultaneous estimation of pantoprazole and itopride hydrochloride in capsules

    Directory of Open Access Journals (Sweden)

    Krishna R. Gupta

    2010-12-01

    Full Text Available Three simple, accurate and economical methods for simultaneous estimation of pantoprazole and itopride hydrochloride in two component solid dosage forms have been developed. The proposed methods employ the application of simultaneous equation method (Method A, absorbance ratio method (Method B and multicomponent mode of analysis method (Method C. All these methods utilize distilled water as a solvent. In distilled water pantoprazole shows maximum absorbance at a wavelength of 289.0 nm while itopride hydrochloride shows maximum absorbance at a wavelength of 258.0 nm also the drugs show an isoabsorptive point at a wavelength of 270.0 nm. For multicomponent method, sampling wavelengths 289.0 nm, 270.0 nm and 239.5 nm were selected. All these methods showed linearity in the range from 4-20 µg/mL and 15-75 µg/mL for pantoprazole and itopride hydrochloride respectively. The results of analysis have been validated statistically and by recovery studies.

  8. [Clinical observation of icotinib hydrochloride in first-line therapy for pulmonary adenocarcinoma].

    Science.gov (United States)

    Yang, Xinjie; Zhang, Hui; Qin, Na; Li, Xi; Nong, Jingying; Lv, Jialin; Wu, Yuhua; Zhang, Quan; Zhang, Shucai

    2013-07-01

    It has been proven that icotinib hydrochloride, as a molecule targeted drug, can be safely and efficiently used to treat advanced non-small cell lung cancer (NSCLC) for second-line or third-line. This research was aimed to investigate the efficacy and toxicity of icotinib hydrochloride as the first-line therapy for pulmonary adenocarcinoma. Among the 56 patients, the tumor objective response rate (ORR) and disease control rate (DCR) was 46.4% (26/56) and 78.6% (46/56), respectively. Among the 20 patients with EGFR analyses, 18 patients were positive for a mutation, ORR was 66.7% (12/18), DCR was 94.4% (17/18) respectively. The ORR with no history of smoke. EGFR positive mutation and appearance of rash were significantly higher than those with smoker, wild type EGFR, no information about EGFR and no appearance of rash (Picotinib hydrochloride is effective and tolerable in first-line therapy for pulmonary adenocarcinoma, especially with EGFR mutation.

  9. Atovaquone and proguanil hydrochloride: a review of nonclinical studies.

    Science.gov (United States)

    Pudney, M; Gutteridge, W; Zeman, A; Dickins, M; Woolley, J L

    1999-05-01

    Safe and effective antimalarial drugs are needed for treatment and prophylaxis of malaria. The combination of atovaquone and proguanil hydrochloride is a new antimalarial drug combination that has recently become available in many countries. Data were reviewed from nonclinical studies evaluating the microbiology, secondary pharmacology, pharmacokinetics, and toxicology of atovaquone and proguanil hydrochloride. Atovaquone is highly active against asexual erythrocytic stages of Plasmodium falciparum in vitro (IC50 0.7-6 nM) and in animal models. Proguanil per se has only weak antimalarial activity in vitro (IC50 2.4-19 microM), and its effectiveness depends on the active metabolite cycloguanil (IC50 0.5-2.5 nM). The combination of atovaquone and proguanil is synergistic in vitro. Both drugs also have activity against gametocytes and pre-erythrocytic (hepatic) stages of malaria parasites. Atovaquone is a ubiquinone antagonist that inhibits mitochondrial electron transport and collapses mitochondrial membrane potential. The proguanil metabolite cycloguanil is a dihydrofolate reductase inhibitor, but the mode of action of proguanil is unknown. In screening evaluations of secondary pharmacology, neither atovaquone nor proguanil had activity that adversely affected gastrointestinal, cardiovascular, or central or autonomic nervous system functions at clinically relevant concentrations. After oral administration, atovaquone exposure is extensive in rats but limited in dogs, while proguanil and cycloguanil exposure is extensive in dogs but limited in rats. In both species, toxicity was related to proguanil exposure, the principal manifestations being salivation, emesis, and loss of body weight. Neither atovaquone nor proguanil was teratogenic or mutagenic. An increased incidence of hepatic adenomas and adenocarcinomas was seen in mice, but not rats, after lifetime exposure to atovaquone, and appears to be related to species-specific differences in hepatic enzymatic activity

  10. Changes in biological markers, particularly hormone receptors, due to pre-operative chemotherapy (epirubicin/docetaxel in operable breast cancer

    Directory of Open Access Journals (Sweden)

    Rumiko Tashima

    2011-12-01

    Full Text Available We investigated the correlation between biological markers prior to pre-operative chemotherapy with epirubicin and docetaxel (ET therapy and the effect of treatment as well as the clinically significant changes in biological markers before and after chemotherapy. Since April 2002, 52 patients with tumors ≥3 cm in diameter or lymph node metastases have received pre-operative ET chemotherapy. The items investigated were ER/PgR, proliferative activity (MIB-1, etc. The correlation of changes in these factors between pre- and post-treatment status and the clinical and pathological responses was investigated. Clinical response was 82%, BCS rate was 67%. Pathological response was 31.4%. The ER/PgR positive cell rate significantly decreased from 48%/32% to 37%/14%. The MIB-1 decreased from 48% to 27%. The pathological response was significantly high in patients with low ER/PgR-positive rates and those with high MIB-1 values.

  11. Microparticulate drug delivery system containing tramadol hydrochloride for pain treatment.

    Science.gov (United States)

    Ciurba, Adriana; Todoran, Nicoleta; Vari, C E; Lazăr, Luminita; Al Hussein, Stela; Hancu, G

    2014-01-01

    The current trend of replacing conventional pharmaceutical forms is justified because most substances administered in this form give fluctuations of therapeutic concentrations and often outside the therapeutic range. In addition, these formulations offer a reduction in the dose or the number of administrations, thus increasing patient compliance. In the experiment, we developed an appropriate technology for the preparation of gelatin microspheres containing tramadol hydrochloride by emulsification/cross-linking method. The formulated microspheres were characterized by product yield, size distribution, encapsulation efficiency and in vitro release of tramadol hydrochloride. Data obtained from in vitro release studies were fitted to various mathematical models to elucidate the transport mechanisms. The kinetic models used were zero-order, first-order, Higuchi Korsmeyer-Peppas and Hopfenberg. Spherical microspheres were obtained, with free-flowing properties. The entrapment efficiency of tramadol hydrochloride in microparticles was 79.91% and product yield -94.92%. As the microsphere size was increased, the entrapment efficiency increased. This was 67.56, 70.03, 79.91% for formulations MT80-250, MT8-500 and, MT250-500. High entrapment efficiency was observed for MT250-500 formulation. The gelatin microspheres had particle sizes ranging from 80 to 500 microm. The drug was released for a period of 12 hours with a maximum release of 96.02%. Of the three proposed formulations, MT250-500 presented desirable properties and optimal characteristics for the therapy of pain. Release of tramadol hydrochloridi was best fitted to Korsmeyer-Peppas equation because the Akaike Information Criterion had the lowest values for this kinetic model. These results suggest the opportunity to influence the therapeutic characteristics of gelatin microspheres to obtain a suitable drug delivery system for the oral administration of tramadol hydrochloride.

  12. Amantadine hydrochloride in the treatment of parkinsonism: A ...

    African Journals Online (AJOL)

    Subjective mood elevation was not confirmed by statistical analysis. Gait, voice control, jaw tremor and salivation showed no statistical improvement, while eye convergence may be adversely affected. Side-effects were minimal. Amantadine hydrochloride (Symmetrel, Geigy) appears to have real value in the treatment of ...

  13. Amides and Hydrazides from Amine and Hydrazine Hydrochlorides.

    Science.gov (United States)

    Shama, Sami A.; Tran, Thuan L.

    1978-01-01

    This safe and efficient procedure for the synthesis of N-substituted amides and hydrazides is a modification of the Schotten-Bausmann procedure in which the amine or hydrazide is replaced by the corresponding hydrochloride salt, and the use of alkali is eliminated. (Author/BB)

  14. Cartap hydrochloride poisoning: a case report

    OpenAIRE

    Sumesh Raj; Sheetal S.

    2014-01-01

    Cartap hydrochloride is a thiocarbamate insecticide used for control of chewing and sucking insects of all stages of development, on many crops. It is an analogue of nereistoxin. Poisoning with cartap is very rarely reported from India. We report a 46 year old man who consumed cartap with alcohol, presented with nausea & vomiting and improved with supportive measures. [Int J Res Med Sci 2014; 2(1.000): 360-361

  15. Efficacy and influence factors of icotinib hydrochloride in treating advanced non-small cell lung cancer.

    Science.gov (United States)

    Ma, X-H; Tian, T-D; Liu, H-M; Li, Q-J; Gao, Q-L; Li, L; Shi, B

    2017-01-01

    To evaluate the efficacy and safety of icotinib hydrochloride in the treatment of patients with advanced non-small cell lung cancer (NSCLC) and discuss the influence factors on efficacy. 120 treatment-experienced patients confirmed by pathology or cytology with stage III B-IV non-small cell lung cancer took icotinib hydrochloride and erlotinib orally until the occurrence of disease progression or serious adverse reactions. Then, the efficacy of icotinib hydrochloride and the related influence factors were analyzed. In icotinib hydrochloride group, the response rate and the disease control rate were 30.00% and 65.00%, and the median progression-free survival time was 179 days (95% CI: 103.21-254.78); in erlotinib group, the response rate and the disease control rate were 25.00% and 56.70%, and the median progression-free survival time was 121 days (95% CI: 95.05-146.94). Moreover, the objective response rate and the disease control rate of second-line therapy were both superior to the third-line and above therapy. The objective response rate of patients with complete response/partial response/stable disease after the first-line therapy was higher than that of patients without response after the first-line therapy (picotinib hydrochloride is effective and safe in treating the treatment-experienced patients with advanced NSCLC, especially for patients with sensitive mutations.

  16. Effects of MK-467 hydrochloride and hyoscine butylbromide on cardiorespiratory and gastrointestinal changes induced by detomidine hydrochloride in horses.

    Science.gov (United States)

    Tapio, Heidi A; Raekallio, Marja R; Mykkänen, Anna; Mama, Khursheed; Mendez-Angulo, Jóse L; Hautajärvi, Heidi; Vainio, Outi M

    2018-04-01

    OBJECTIVE To compare the effects of MK-467 and hyoscine butylbromide on detomidine hydrochloride-induced cardiorespiratory and gastrointestinal changes in horses. ANIMALS 6 healthy adult horses. PROCEDURES Horses received detomidine hydrochloride (20 μg/kg, IV), followed 10 minutes later by MK-467 hydrochloride (150 μg/kg; DET-MK), hyoscine butylbromide (0.2 mg/kg; DET-HYO), or saline (0.9% NaCl) solution (DET-S), IV, in a Latin square design. Heart rate, respiratory rate, rectal temperature, arterial and venous blood pressures, and cardiac output were measured; blood gases and arterial plasma drug concentrations were analyzed; selected cardiopulmonary variables were calculated; and sedation and gastrointestinal borborygmi were scored at predetermined time points. Differences among treatments or within treatments over time were analyzed statistically. RESULTS With DET-MK, detomidine-induced hypertension and bradycardia were reversed shortly after MK-467 injection. Marked tachycardia and hypertension were observed with DET-HYO. Mean heart rate and mean arterial blood pressure differed significantly among all treatments from 15 to 35 and 15 to 40 minutes after detomidine injection, respectively. Cardiac output was greater with DET-MK and DET-HYO than with DET-S 15 minutes after detomidine injection, but left ventricular workload was significantly higher with DET-HYO. Borborygmus score, reduced with all treatments, was most rapidly restored with DET-MK. Sedation scores and pharmacokinetic parameters of detomidine did not differ between DET-S and DET-MK. CONCLUSIONS AND CLINICAL RELEVANCE MK-467 reversed or attenuated cardiovascular and gastrointestinal effects of detomidine without notable adverse effects or alterations in detomidine-induced sedation in horses. Further research is needed to determine whether these advantages are found in clinical patients and to assess whether the drug influences analgesic effects of detomidine.

  17. Spectrophotometric simultaneous determination of Rabeprazole Sodium and Itopride Hydrochloride in capsule dosage form

    Science.gov (United States)

    Sabnis, Shweta S.; Dhavale, Nilesh D.; Jadhav, Vijay. Y.; Gandhi, Santosh V.

    2008-03-01

    A new simple, economical, rapid, precise and accurate method for simultaneous determination of rabeprazole sodium and itopride hydrochloride in capsule dosage form has been developed. The method is based on ratio spectra derivative spectrophotometry. The amplitudes in the first derivative of the corresponding ratio spectra at 231 nm (minima) and 260 nm were selected to determine rabeprazole sodium and itopride hydrochloride, respectively. The method was validated with respect to linearity, precision and accuracy.

  18. Resistance to mitomycin C requires direct interaction between the fanconi anemia proteins FANCA and FANCG in the nucleus through an arginine-rich domain

    NARCIS (Netherlands)

    Kruyt, FAE; Abou-Zahr, F; Mok, H; Youssoufian, H

    1999-01-01

    Fanconi anemia (FA) is a genetically heterogeneous disorder characterized by bone marrow failure, birth defects, and chromosomal instability. Because FA cells are sensitive to mitomycin C (MMC), FA gene products could be involved in cellular defense mechanisms. The FANCA and FANCG proteins deficient

  19. A validated high performance thin layer chromatography method for determination of yohimbine hydrochloride in pharmaceutical preparations.

    Science.gov (United States)

    Badr, Jihan M

    2013-01-01

    Yohimbine is an indole alkaloid used as a promising therapy for erectile dysfunction. A number of methods were reported for the analysis of yohimbine in the bark or in pharmaceutical preparations. In the present work, a simple and sensitive high performance thin layer chromatographic method is developed for determination of yohimbine (occurring as yohimbine hydrochloride) in pharmaceutical preparations and validated according to International Conference of Harmonization (ICH) guidelines. The method employed thin layer chromatography aluminum sheets precoated with silica gel as the stationary phase and the mobile phase consisted of chloroform:methanol:ammonia (97:3:0.2), which gave compact bands of yohimbine hydrochloride. Linear regression data for the calibration curves of standard yohimbine hydrochloride showed a good linear relationship over a concentration range of 80-1000 ng/spot with respect to the area and correlation coefficient (R(2)) was 0.9965. The method was evaluated regarding accuracy, precision, selectivity, and robustness. Limits of detection and quantitation were recorded as 5 and 40 ng/spot, respectively. The proposed method efficiently separated yohimbine hydrochloride from other components even in complex mixture containing powdered plants. The amount of yohimbine hydrochloride ranged from 2.3 to 5.2 mg/tablet or capsule in preparations containing the pure alkaloid, while it varied from zero (0) to 1.5-1.8 mg/capsule in dietary supplements containing powdered yohimbe bark. We concluded that this method employing high performance thin layer chromatography (HPTLC) in quantitative determination of yohimbine hydrochloride in pharmaceutical preparations is efficient, simple, accurate, and validated.

  20. [Clinical observation of icotinib hydrochloride for patients with advanced non-small cell lung cancer].

    Science.gov (United States)

    Li, Xi; Yang, Xin-jie; Sun, Yi-fen; Qin, Na; Lü, Jia-lin; Wu, Yu-hua; Zhang, Hui; Zhang, Quan; Zhang, Shu-cai

    2012-08-01

    To explore the efficacy and side effects of icotinib hydrochloride in the treatment of patients with advanced non-small cell lung cancer (NSCLC). The efficacy and side effects of icotinib hydrochloride in treatment of 59 cases with stage IV NSCIC and followed-up from March 2009 to January 2012 were retrospectively analyzed. Twenty seven patients (45.8%) showed partial response (PR), 17 patients (28.8%) achieved SD, and 15 (25.4%) had progressive disease. The objective response rate (ORR) was 45.8% (27/59), and disease control rate (DCR) was 74.6% (44/59). Among the 23 patients with EGFR mutation, ORR was 73.9% (17/23), and DCR was 95.7% (22/23). Thirty six patients (61.0%) achieved remission of symptoms to varying degrees. The main symptoms relieved were cough, asthmatic suffocating, pain and hoarseness. The major adverse events were mild skin rash (35.6%) and diarrhea (15.3%). Others were dry skin, nausea and stomach problems. The efficacy of icotinib hydrochloride were related to the ECOG performance status, smoking history, EGFR mutation and rash significantly (P icotinib hydrochloride is effective and tolerable for patients with advanced NSCLC, especially with EGFR mutation.

  1. Micronucleus formation in cultured human keratinocytes following exposure to mitomycin C and cyclophosphamide.

    Science.gov (United States)

    van Pelt, F N; Haring, R M; Overkamp, M J; Weterings, P J

    1991-02-01

    A method is described to investigate the induction of micronuclei in cultured human keratinocytes after short-term exposure to known clastogenic agents. The cytokinesis-block method was applied to facilitate the scoring of micronucleated cells. Mitomycin C, a direct-acting compound, caused a 5-20-fold increase in micronuclei over the controls at the highest concentration tested (1 microgram/ml). Cyclophosphamide, an agent requiring metabolic activation, did not induce the formation of micronuclei in cultured keratinocytes. However, after pretreatment of the keratinocyte cultures with Aroclor 1254 for 72 h, exposure to cyclophosphamide resulted in a 3-fold increase in micronucleus frequency over the controls. No cytogenetic effect of Aroclor 1254 was observed in control experiments.

  2. DETERMINATION OF TAMSULOSIN HYDROCHLORIDE RELEASE PHARMACOKINETICS IN PROSTATE GLAND BY A RADIOTRACER METHOD

    Directory of Open Access Journals (Sweden)

    V. I. Grytsenko

    2013-10-01

    Full Text Available Introduction: recently in Ukraine prostate diseases have taken one of the leading places among male urological pathologies. Prostate gland hyperplasia is one of the most common ones. Causes of hyperplasia have not been reliably established so far, however, it has been proved that the poor state of androgen production in men is an integral condition for the development of benign prostatic hyperplasia. One of the urgent tasks of modern pharmaceutical science is to create new high-performance drugs in such dosage forms that provide optimal therapeutic effect with minimal adverse complications. Among a large number of drugs for the treatment of prostate diseases a prominent place is occupied by alpha-adrenoblockers – drugs of the first-line treatments that affect the α1А-adrenergic receptors, reduce or completely eliminate the muscle tone of the prostatic urethra and bladder neck. Tamsulosin hydrochloride is a selective and competitive blocker of postsynaptic α1А-adrenergic receptors. The selectivity of tamsulosin to α1А-adrenergic receptors, which are located in the bladder, is 20 times greater than its ability to interact with α1В-adrenoceptors that are located in vascular smooth muscles. Objective: to study the pharmacokinetics of tamsulosin hydrochloride release into prostate gland after oral and rectal administration by a radioactive-tracer technique. Materials and methods of research: tamsulosin hydrochloride substance and suppositories with this substance labeled by 14С with a specific activity of 3.7× 107Bq/mg. Pharmacokinetic studies of tamsulosin hydrochloride in the prostate were performed after oral and rectal administration. The experiments were carried out on white mature male rats of Wistar line weighing 210 ± 10 g. Pharmacokinetic studies were performed using a radioactive-tracer technique (tracers after oral and rectal administration of tamsulosin. Results and their discussion: after rectal administration the release of

  3. Quantitative analysis of Loperamide hydrochloride in the presence its acid degradation products

    Directory of Open Access Journals (Sweden)

    Savić Ivana M.

    2009-01-01

    Full Text Available The aim of this work was to develop a new RP-HPLC method for the determination of loperamide hydrochloride in the presence of its acid degradation products. Separation of loperamide from degradation products was performed using ZORBAX Eclipse XDB C-18, column with a mobile phase consisting of 0.1% sodium-octansulphonate, 0.05% triethylamine, 0.1% ammonium hydroxide in water:acetonitrile (45:55 v/v. The mobile phase was adjusted to pH 3.2 with phosphoric acid. The method showed high sensitivity with good linearity over the concentration range of 10 to 100 μg cm-3. The method was successfully applied to the analysis of a pharmaceutical formulation (Loperamide, Zdravlje-Actavis, Serbia containing loperamide hydrochloride with excellent recovery. The loperamide hydrochloride degradation during acid hydrolysis and kinetics investigation was carried out in hydrochloric acid solutions of 0.1, 1.0 and 1.5 mol dm-3, at different temperatures (25 and 40°C, by monitoring the parent compound itself. The first order reaction of loperamide degradation in acid solution was determined. The activation energy was estimated from the Arrhenius plot and it was found to be 38.81 kJ mol-1 at 40°C. The developed procedure was successfully applied for the rapid determination of loperamide hydrochloride in pharmaceutical formulation (Loperamide, Zdravlje-Actavis, Serbia and in the presence of its acid degradation products.

  4. Antinociceptive effects after oral administration of tramadol hydrochloride in Hispaniolan Amazon parrots (Amazona ventralis).

    Science.gov (United States)

    Sanchez-Migallon Guzman, David; Souza, Marcy J; Braun, Jana M; Cox, Sherry K; Keuler, Nicholas S; Paul-Murphy, Joanne R

    2012-08-01

    To evaluate antinociceptive effects on thermal thresholds after oral administration of tramadol hydrochloride to Hispaniolan Amazon parrots (Amazona ventralis). Animals-15 healthy adult Hispaniolan Amazon parrots. 2 crossover experiments were conducted. In the first experiment, 15 parrots received 3 treatments (tramadol at 2 doses [10 and 20 mg/kg] and a control suspension) administered orally. In the second experiment, 11 parrots received 2 treatments (tramadol hydrochloride [30 mg/kg] and a control suspension) administered orally. Baseline thermal foot withdrawal threshold was measured 1 hour before drug or control suspension administration; thermal foot withdrawal threshold was measured after administration at 0.5, 1.5, 3, and 6 hours (both experiments) and also at 9 hours (second experiment only). For the first experiment, there were no overall effects of treatment, hour, period, or any interactions. For the second experiment, there was an overall effect of treatment, with a significant difference between tramadol hydrochloride and control suspension (mean change from baseline, 2.00° and -0.09°C, respectively). There also was a significant change from baseline for tramadol hydrochloride at 0.5, 1.5, and 6 hours after administration but not at 3 or 9 hours after administration. Tramadol at a dose of 30 mg/kg, PO, induced thermal antinociception in Hispaniolan Amazon parrots. This dose was necessary for induction of significant and sustained analgesic effects, with duration of action up to 6 hours. Further studies with other types of noxious stimulation, dosages, and intervals are needed to fully evaluate the analgesic effects of tramadol hydrochloride in psittacines.

  5. An investigation on in vitro and in vivo antimicrobial properties of the antidepressant: amitriptyline hydrochloride

    Directory of Open Access Journals (Sweden)

    Anurup Mandal

    2010-10-01

    Full Text Available The antidepressant drug amitriptyline hydrochloride was obtained in a dry powder form and was screened against 253 strains of bacteria which included 72 Gram positive and 181 Gram negative bacteria and against 5 fungal strains. The minimum inhibitory concentration (MIC was determined by inoculating a loopful of an overnight peptone water culture of the organism on nutrient agar plates containing increasing concentrations of amitriptyline hydrochloride (0, 10 µg/mL, 25 µg/mL, 50 µg/mL, 100 µg/mL, 200 µg/mL. Amitriptyline hydrochloride exhibited significant action against both Gram positive and Gram negative bacteria at 25-200 µg/mL. In the in vivo studies it was seen that amitriptyline hydrochloride at a concentration of 25 µg/g and 30 µg/g body weight of mouse offered significant protection to Swiss strain of white mice when challenged with 50 median lethal dose (MLD of a virulent strain of Salmonella typhimurium NCTC 74. The in vivo data were highly significant (p<0.001 according to the chi-square test.

  6. Effect of N-hydroxyurea, mitomycin C and actinomycin D on tumour formation on the leaves of Kalanchoe daigremontiana

    Directory of Open Access Journals (Sweden)

    Józef Koawalczyk

    2014-01-01

    Full Text Available The leaves of Kalanchoe daigremontiana wounded and infected with Agrobacterium tumefaciens were treated with single doses of inhibitors (hydroxyurea - 190, mitomycin - 0.5, actinomycin - 2 µ,g per leaf. After delaying the time' of dosage of inhibitors during five days after inoculation, changes in susceptibility of the system to antitumorous activity of analysed compounds were observed. In several hours after inoculation (period of the bacteria metabolic activity in wounds all the inhibitors prevent strongly the tumour formation. At the time between 14 and 72 hours after inoculation, including the phase of tumour induction, the system becomes sensitive to the DNA synthesis inhibitors, particularly hydroxyurea. The intensified action of actinomycin appears again only about 60 hours after inoculation and lasts till the end of experiment (the initiation of the transformed plant cell proliferation. According to the literature the antitumorous effect of inhibitors could be connected with their action on the bacteria metabolism inside the host tissue. The activities of hydroxyurea and mitomycin in the second period correspond with the intensive DNA synthesis in plant cells, which is induced by wounding. The effect of actinomycin D in 60 hours after inoculation could depend upon the inhibition of the proliferation of the transformed host cells.

  7. Influence of stereoelectronic effects on the non-opioid analgesics gaboxadol and gaboxadol hydrochloride: Spectral and DFT study

    Science.gov (United States)

    Leenaraj, D. R.; Joe, I. Hubert

    2018-05-01

    The stereoelectronic properties of the molecular structure of most stable conformers of gaboxadol and gaboxadol hydrochloride have been studied using DFT/B3P86-LANL2DZ methodology. The energies of stable conformers of gaboxadol and gaboxadol hydrochloride are -494.2689 and -510.0117 hartrees, respectively. The stability of the molecules arising from stereoelectronic interactions, leading to its bioactivity, has been confirmed using natural bond orbital analysis. The natural bond orbital analysis of donor-acceptor (σ→σ* and n→σ*) interactions showed that the stereoelectronic hyperconjugative and anomeric interactions are exhibited in gaboxadol hydrochloride and gaboxadol, respectively. Lengthening of the axial and equatorial C-H bond lengths and natural population analysis support these results. Spectral features of gaboxadol hydrochloride have been explored by the Fourier transform infrared, Raman and Nuclear magnetic resonance spectroscopic techniques combined with density functional theory computations. NH+ … Cl- hydrogen bonding has been noticeable as a broad and strong absorption in the 2800-2400 cm-1 region. Broad peaks obtained by proton NMR are a result of the quadrupole effect of the N+ atom. Docking studies using representative GABA receptor crystal structures revealed that molecules containing azinane and isoxazole cores fit within the ligand binding domains, and the gaboxadol hydrochloride molecule shows the best binding energy with the 3D32 GABA receptor. Also, gaboxadol hydrochloride has obtained a high value of HOMO energy and a narrow HOMO- LUMO energy gap, which enhances reactivity.

  8. Physical and chemical stability of palonosetron hydrochloride with dacarbazine and with methylprednisolone sodium succinate during simulated y-site administration.

    Science.gov (United States)

    Trissel, Lawrence A; Zhang, Yanping; Xu, Quanyun A

    2006-01-01

    The objective of this study was to evaluate the physical and chemical stability of mixtures of undiluted palonosetron hydrochloride 50 micrograms/mL with dacarbazine 4 mg/mL and with methylprednisolone sodium succinate 5 mg/mL in 5% dextrose injection during simulated Y-site administration. Triplicate test samples were prepared by admixing 7.5 mL of palonosetron hydrochloride with 7.5 mL of dacarbazine solution and, separately, methylprednisolone sodium succinate solution. Physical stability was assessed by using a multistep evaluation procedure that included both turbidimetric and particulate measurement as well as visual inspection. Chemical stability was assessed by using stability-indicating high-performance liquid chromatographic analytical techniques that determined drug concentrations. Evaluations were performed immediately after mixing and 1 and 4 hours after mixing. The palonosetron hydrochloride-dacarbazine samples were clear and colorless when viewed in normal fluorescent room light and when viewed with a Tyndall beam. Measured turbidities remained unchanged; particulate contents were low and exhibited little change. High-performance liquid chromatography analysis revealed that palonosetron hydrochloride and dacarbazine remained stable throughout the 4-hour test with no drug loss. Palonosetron hydrochloride is, therefore, physically compatible and chemically stable with dacarbazine during Y-site administration. Within 4 hours, the mixtures of palonosetron hydrochloride and methylprednisolone sodium succinate developed a microprecipitate that became a white precipitate visible to the unaided eye. The precipitate was analyzed and identified as methylprednisolone. Palonosetron hydrochloride is incompatible with methylprednisolone sodium succinate.

  9. Stability studies of lincomycin hydrochloride in aqueous solution and intravenous infusion fluids

    Directory of Open Access Journals (Sweden)

    Czarniak P

    2016-03-01

    Full Text Available Petra Czarniak, Michael Boddy, Bruce Sunderland, Jeff D Hughes School of Pharmacy, Curtin University, Perth, WA, Australia Purpose: The purpose of this study was to evaluate the chemical stability of Lincocin® (lincomycin hydrochloride in commonly used intravenous fluids at room temperature (25°C, at accelerated-degradation temperatures and in selected buffer solutions.Materials and methods: The stability of Lincocin® injection (containing lincomycin 600 mg/2 mL as the hydrochloride stored at 25°C±0.1°C in sodium lactate (Hartmann’s, 0.9% sodium chloride, 5% glucose, and 10% glucose solutions was investigated over 31 days. Forced degradation of Lincocin® in hydrochloric acid, sodium hydroxide, and hydrogen peroxide was performed at 60°C. The effect of pH on the degradation rate of lincomycin hydrochloride stored at 80°C was determined.Results: Lincomycin hydrochloride was found to maintain its shelf life at 25°C in sodium lactate (Hartmann’s solution, 0.9% sodium chloride solution, 5% glucose solution, and 10% glucose solution, with less than 5% lincomycin degradation occurring in all intravenous solutions over a 31-day period. Lincomycin hydrochloride showed less rapid degradation at 60°C in acid than in basic solution, but degraded rapidly in hydrogen peroxide. At all pH values tested, lincomycin followed first-order kinetics. It had the greatest stability near pH 4 when stored at 80°C (calculated shelf life of 4.59 days, and was least stable at pH 2 (calculated shelf life of 0.38 days.Conclusion: Lincocin® injection was chemically found to have a shelf life of at least 31 days at 25°C when added to sodium lactate (Hartmann’s solution, 0.9% sodium chloride solution, 5% glucose solution, and 10% glucose solution. Solutions prepared at approximately pH 4 are likely to have optimum stability. Keywords: lincomycin, stability, pH, intravenous fluids, IV additives

  10. Compatibility and stability of aloxi (palonosetron hydrochloride) admixed with dexamethasone sodium phosphate.

    Science.gov (United States)

    Trissel, Lawrence A; Zhang, Yanping

    2004-01-01

    The purpose of this study was to evaluate the physical and chemical stability of palonosetron hydrochloride 0.25 mg admixed with dexamethasone (as sodium phophate) 10 mg or 20 mg in 5% dextrose injection or 0.9% sodium chloride injection in polyvinylchloride minibags, and also admixed with dexamethasone (as sodium phosphate) 3.3 mg in 5% dextrose injection or 0.9% sodium chloride injection in polypropylene syringes, at 4 deg C stored in the dark for 14 days, and at 23 deg C exposed to normal laboratory fluorescent light over 48 hours. Test samples of palonosetron hydrochloride 5 micrograms/mL with dexamethasone (as sodium phosphate) 0.2 mg/mL and also 0.4 mg/mL were prepared in polyvinylchloride minibags of each infusion solution. Additionally, palonosetron hydrochloride 25 micrograms/mL with dexamethasone (as sodium phosphate) 0.33 mg/mL in each infusion solution were prepared as 10 mL of test solution in 20-mL polypropylene syringes. Evaluations for physical and chemical stability were performed on samples taken initially and after 1, 3, 7 and 14 days of storage at 4 deg C and after 1, 4, 24 and 48 hours at 23 deg C. Physical stability was assessed using visual observation in normal room light and using a high-intensity monodirectional light beam. In addition, turbidity and particle content were measured electronically. Chemical stability of the drug was evaluated by using a stability-indicating high-performance liquid chromatographic analytical technique. All samples were physically compatible throughout the study. The solutions remained clear and showed little or no change in particulate burden and haze level. Additionally, little or no loss of palonosetron hydrochloride and dexamethasone occurred in any of the samples at either temperature throughout the entire study period. Admixtures of palonosetron hydrochloride with dexamethasone sodium phosphate in 5% dextrose injection or in 0.9% sodium chloride injection packaged in polyvinylchloride minibags or in

  11. Detecting Lactococcus lactis Prophages by Mitomycin C-Mediated Induction Coupled to Flow Cytometry Analysis

    Directory of Open Access Journals (Sweden)

    Joana Oliveira

    2017-07-01

    Full Text Available Most analyzed Lactococcus lactis strains are predicted to harbor one or more prophage genomes within their chromosome; however, the true extent of the inducibility and functionality of such prophages cannot easily be deduced from sequence analysis alone. Chemical treatment of lysogenic strains with Mitomycin C is known to cause induction of temperate phages, though it is not always easy to clearly identify a lysogenic strain or to measure the number of released phage particles. Here, we report the application of flow cytometry as a reliable tool for the detection and enumeration of released lactococcal prophages using the green dye SYTO-9.

  12. A validated HPTLC method for estimation of moxifloxacin hydrochloride in tablets.

    Science.gov (United States)

    Dhillon, Vandana; Chaudhary, Alok Kumar

    2010-10-01

    A simple HPTLC method having high accuracy, precision and reproducibility was developed for the routine estimation of moxifloxacin hydrochloride in the tablets available in market and was validated for various parameters according to ICH guidelines. moxifloxacin hydrochloride was estimated at 292 nm by densitometry using Silica gel 60 F254 as stationary phase and a premix of methylene chloride: methanol: strong ammonia solution and acetonitrile (10:10:5:10) as mobile phase. Method was found linear in a range of 9-54 nanograms with a correlation coefficient >0.99. The regression equation was: AUC = 65.57 × (Amount in nanograms) + 163 (r(2) = 0.9908).

  13. 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.

  14. SPECTROPHOTOMETRIC METHOD FOR SIMULTANEOUS ESTIMATION OF TOLPERISONE HYDROCHLORIDE AND DICLOFENAC SODIUM IN SYNTHETIC MIXTURE

    OpenAIRE

    Patel Satish A; Hariyani Kaushik P

    2012-01-01

    The present manuscript describes simple, sensitive, rapid, accurate, precise and economical spectrophotometric method for the simultaneous determination of Diclofenac sodium and Tolperisone hydrochloride in bulk and synthetic mixture. The method is based on the simultaneous equations for analysis of both the drugs using methanol as solvent. Diclofenac sodium has absorbance maxima at 281 nm and Tolperisone hydrochloride has absorbance maxima at 255 nm in methanol. The linearity was obtained in...

  15. SPECTROPHOTOMETRIC METHOD FOR SIMULTANEOUS ESTIMATION OF EPERISONE HYDROCHLORIDE AND DICLOFENAC SODIUM IN SYNTHETIC MIXTURE

    OpenAIRE

    Patel Paresh U; Patel Sejal K; Patel Umang J

    2012-01-01

    The present manuscript describes simple, sensitive, rapid, accurate, precise and economical spectrophotometric method for the simultaneous determination of diclofenac sodium and Eperisone hydrochloride in bulk and synthetic mixture. The method is based on the simultaneous equations for analysis of both the drugs using methanol as solvent. Diclofenac sodium has absorbance maxima at 281 nm and Eperisone hydrochloride has absorbance maxima at 255 nm in methanol. The linearity was obtained in the...

  16. Effect of mitomycin-c on biodistribution of 99 mTc-sodium pyrophosphate radiopharmaceuticals in mice; Efeito da mitomicina-c na biodistribuicao do radiofarmaco pirofosfato de sodio marcado com Tecnecio-99m em camundongos

    Energy Technology Data Exchange (ETDEWEB)

    Gomes, Maria L.; Braga, Ana C.S.; Gutfilen, Bianca; Bernardo-Filho, Mario [Instituto Nacional do Cancer, Rio de Janeiro, RJ (Brazil)

    1997-12-01

    The desirable characteristics of technetium-99 have stimulated the development of labeling techniques for different molecular and cellular. It is generally acceptable that a variety of factors other than disease can alter the biodistribution of radiopharmaceutical and one such factor is the drug therapy. The absence of knowledge of these factors may result in an unexpected behavior of the radiopharmaceutical. Since patients on chemotherapeutic treatment ca be submitted, for different reasons, to a nuclear medicine procedure, we have studied in mice, the effect of mitomycin-C on the biodistribution of the radiopharmaceutical {sup 99m} Tc-pyrophosphate ({sup 99m} Tc-PYP). Mitomycin-C is an antineoplastic agent obtained from Streptomyces caesptosus. It was administered 0,15 mg of mitomycin-C in Balb/c in Balb/c female mice with an interval of 72 hours. After one hour of the last dose, 0.3 ml of {sup 99m} Tc-PYP (7.4 MBq) were injected after 0.5 h the animals were sacrificed. The organs were isolated, weighted and counted in a well counter. The percentages of radioactivity per gran of organs (% rad/g) were calculated and statistics analyses were performed (wilcoxon). The results have shown that the % rad/g has increased in pancreas, stomach, bone and lungs. These increased of radioactivity can be justified by the metabolic process or the therapeutic effect of mitomycin-C. (author). 8 refs., 2 tabs.

  17. Pre- and intraoperative mitomycin C for recurrent pterygium associated with symblepharon

    Directory of Open Access Journals (Sweden)

    Mohammed I

    2013-01-01

    Full Text Available Isyaku MohammedDepartment of Ophthalmology, Aminu Kano Teaching Hospital, Kano, NigeriaBackground: Treatment of recurrent pterygium associated with symblepharon usually involves the use of tissue grafting and/or the intraoperative application of mitomycin C (MMC. For the graft, a conjunctival/limbal autograft and/or amniotic membrane may be used. This generally requires extra technical skills and assistance, an increase in the cost and duration of surgery, and a more extensive anesthesia (a complete eye block or general anesthesia. Although widely used, safety concerns have been raised over MMC in the treatment of pterygia.Objective: The objective of this case report is to report the successful use of preoperative subconjunctival injection of low-dose (0.02% MMC one month before bare sclera excision of a multirecurrent pterygium, as well as the concomitant intraoperative application of MMC to the conjunctival fornix of the same eye after the excision of an associated symblepharon.Case report: A 31-year-old man from Kano, Northern Nigeria, presented to the eye clinic with a recurrent pterygium associated with an upper lid symblepharon in his right eye. He has had five previous pterygium excisions, with the last surgery involving conjunctival autografting and subconjunctival steroid injection. He was subsequently given 0.1 mL of 0.02% MMC as a subpterygial injection; one month later he had an alcohol-assisted bare sclera pterygium excision and a symblepharolysis with the intraoperative application of 0.02% MMC for 1 minute to the upper conjunctival fornix. Except for a Tenon granuloma that was simply excised, there has been no recurrence or other complications up to a year after surgery.Conclusion: As a cheaper and technically easier treatment option, a preoperative subconjunctival MMC injection followed by bare sclera pterygium excision was found to be effective in this patient with a recurrent pterygium. As at one-year follow-up, low

  18. Application of Mitomycin C after dilation of an anastomotic stricture in a newborn with necrotizing enterocolitis

    Directory of Open Access Journals (Sweden)

    Jonathan Green

    2016-01-01

    Full Text Available Necrotizing enterocolitis (NEC is a common life-threatening condition in premature infants. Bacterial translocation, localized inflammation and subsequent perforation often require surgery for source control and definitive treatment. Small and large intestinal strictures may result from either creation of a surgical anastomosis or the disease process itself. Current methods to treat strictures include, balloon dilation and surgical resection with or without anastomosis. We report the diagnosis and surgical management of a premature infant treated for NEC, who developed an anastomotic stricture and was successfully treated with topical Mitomycin C after balloon stricturoplasty.

  19. In vitro release of metformin hydrochloride from sodium alginate/polyvinyl alcohol hydrogels.

    Science.gov (United States)

    Martínez-Gómez, Fabián; Guerrero, Juan; Matsuhiro, Betty; Pavez, Jorge

    2017-01-02

    Hydrogels, based on polysaccharides have found a number of applications as drug delivery carriers. In this work, hydrogels of full characterized sodium alginate (Mn 87,400g/mol) and commercial poly(vinyl alcohol) (PVA) sensitive to pH and temperature stimuli were obtained using a simple, controlled, green, low cost method based on freeze-thaw cycles. Stable hydrogels of sodium alginate/PVA with 0.5:1.5 and 1.0:1.0w/v concentrations showed very good swelling ratio values in distilled water (14 and 20g/g, respectively). Encapsulation and release of metformin hydrochloride in hydrogels of 1.0:1.0w/v sodium alginate/PVA was followed by UV spectroscopy. The hydrogel released a very low amount of metformin hydrochloride at pH 1.2; the highest release value (55%) was obtained after 6h at pH 8.0. Also, the release of metformin hydrochloride was studied by 1 H NMR spectroscopy, the temporal evolution of methyl group signals of metformin showed 30% of drug release after 3h. Copyright © 2016 Elsevier Ltd. All rights reserved.

  20. Surface properties of aqueous amino acid solutions II. Leucine-leucine hydrochloride and leucine-sodium leucinate mixtures.

    Science.gov (United States)

    Matubayasi, Norihiro; Matsuyama, Shohei; Akizuki, Ryosuke

    2005-08-15

    To understand the distinction between the effects of zwitterionic, anionic, and cationic l-leucine upon adsorption and lateral interactions at air/water surface, the surface tensions of aqueous solutions of l-leucine-l-leucine hydrochloride and l-leucine-sodium l-leucinate mixtures were measured as a function of concentration and composition at 25 degrees C. The surface activity decreases in the order l-leucine >l-leucine hydrochloride > sodium l-leucinate. Both l-leucine hydrochloride and sodium l-leucinate form gaseous adsorbed films through the experimentally accessible concentration range, while the adsorbed film of zwitterionic l-leucine shows a transition between gaseous and expanded film.

  1. Effect of mitomycin combined with Nd-YAG laser on cell proliferation and invasion as well as MEK/ERK signaling pathway in obstructive lacrimal duct model

    Directory of Open Access Journals (Sweden)

    Yu Yan

    2017-11-01

    Full Text Available Objective: To study the effect of mitomycin (MMC combined with Nd-YAG laser on cell proliferation and invasion as well as MEK/ERK signaling pathway in obstructive lacrimal duct model. Methods: New Zealand rabbits were selected as experimental animals and divided into model group, laser group and MMC + laser group; obstructive lacrimal duct model was established, then laser group were given Nd-YAG laser intervention, and MMC + laser group were given Nd-YAG laser combined with mitomycin intervention. 2 months after intervention, the expression of proliferation molecules, invasion molecules and MEK-ERK signaling molecules in lacrimal duct tissue were measured. Results: TGF-β, CTGF, PCNA, Ki-67, Col-I, Col-III, MEK, ERK1/2, MMP2 and MMP9 protein levels in lacrimal duct tissue of laser group were significantly higher than those of model group while TSG-6, Cthrc1 and TIMP1 protein levels were significantly lower than those of model group; TGF-β, CTGF, PCNA, Ki- 67, Col-I, Col-III, MEK, ERK1/2, MMP2 and MMP9 protein levels in lacrimal duct tissue of MMC + laser group were significantly lower than those of laser group while TSG-6, Cthrc1 and TIMP1 protein levels were significantly higher than those of laser group. Conclusion: Mitomycin can inhibit cell proliferation and invasion as well as MEK/ERK signaling pathway activation in obstructive lacrimal duct model after Nd-YAG laser treatment.

  2. The efficacy of two bupivacaine hydrochloride injection products

    African Journals Online (AJOL)

    1996-06-06

    Jun 6, 1996 ... stances majority of o the survey t the time hamstrung g staff. itive hes to ... hydrochloride injection products was investigated in patients who ... upon the concentration, dose, route of application, and ... Practice guidelines.~.5 .... GUIdelines on Ihe Qualoty. safety and efficacy Of mra.cmal prOducts for human.

  3. Evaluation of Epirubicin in Thermogelling and Bioadhesive Liquid and Solid Suppository Formulations for Rectal Administration

    Directory of Open Access Journals (Sweden)

    Yu-Li Lo

    2013-12-01

    Full Text Available Temperature sensitive Pluronic (Plu and pH-sensitive polyacrylic acid (PAA were successfully mixed in different ratios to form in situ gelling formulations for colon cancer therapy. The major formulations were prepared as the liquid and solid suppository dosage forms. Epirubicin (Epi was chosen as a model anticancer drug. In vitro characterization and in vivo pharmacokinetics and therapeutic efficacy of Epi in six Plu/PAA formulations were evaluated. Our in vitro data indicate that Epi in Plu 14%/PAA 0.75% of both solid and liquid suppositories possess significant cytotoxicity, strong bioadhesive force, long-term appropriate suppository base, sustained release, and high accumulation of Epi in rat rectums. These solid and liquid suppositories were retained in the upper rectum of Sprague-Dawley (SD rats for at least 12 h. An in vivo pharmacokinetic study using SD rats showed that after rectal administration of solid and liquid suppositories, Epi had greater area under the curve and higher relative bioavailability than in a rectal solution. These solid and liquid suppositories exhibited remarkable inhibition on the tumor growth of CT26 bearing Balb/c mice in vivo. Our findings suggest that in situ thermogelling and mucoadhesive suppositories demonstrate a great potential as colon anticancer delivery systems for protracted release of chemotherapeutic agents.

  4. Single-step transepithelial ASLA (SCHWIND with mitomycin-C for the correction of high myopia: long term follow-up

    Directory of Open Access Journals (Sweden)

    Aslanides IM

    2014-12-01

    Full Text Available Ioannis M Aslanides, Panagiotis N Georgoudis, Vasilis D Selimis, Achyut N Mukherjee Emmetropia Mediterranean Eye Institute, Heraklion, Crete, Greece Purpose: We wanted to compare the outcomes of single-step modified transepithelial photorefractive keratectomy (tPRK termed a SCHWIND all surface laser ablation (ASLA versus conventional alcohol-assisted photorefractive keratectomy (PRK and laser-assisted in situ keratomileusis (LASIK for the correction of higher myopia of 6.00 diopters (D or more, in an area with high risk of haze due to high intensity of sunlight.Methods: We used a prospective interventional cohort with matched retrospective control groups. Patients with >6 D myopia and <3.5 D of astigmatism were included. All treatments were performed with the SCHWIND Amaris system using aspheric ablation profiles. Mitomycin C was used in all PRK and ASLA cases. Outcomes were postoperative refraction, visual acuity, stability, and complications. The follow-up period was up to 12 months.Results: In total, 101 eyes were included after exclusions. Mean preoperative spherical equivalent refraction was −7.9 D, −8.2 D, and −7.4 D in the ASLA (n=41, PRK (n=29, and LASIK (n=31 groups. Mean postoperative spherical equivalent at 12 months postoperatively was −0.1 (standard deviation [SD]: 0.34, −0.2 (SD: 0.59, and −0.08 (SD: 0.36 in the ASLA, PRK, and LASIK groups, with 91.4%, 85.7%, and 83.9% within 0.5 D of target, respectively. Refractive outcomes and regression at 12 months did not vary among groups (P>0.05. Mean logMAR (logarithm of the minimum angle of resolution uncorrected distance visual acuity at 12 months was 0.00 (SD: 0.05, 0.06 (SD: 0.1, and 0.05 (SD: 0.09 in the ASLA, PRK, and LASIK groups, with significantly better vision in the tPRK group versus LASIK (P=0.01 and PRK (P=0.01 groups.Conclusion: ASLA (SCHWIND tPRK with mitomycin C for high myopia demonstrates comparable refractive outcomes to LASIK and PRK, with relatively

  5. Thiamine hydrochloride: An efficient catalyst for one-pot synthesis of ...

    Indian Academy of Sciences (India)

    thiamine hydrochloride (VB1) as an inexpensive, non-toxic and metal ion free catalyst at ambient temperature. Keywords. ... from practical applications due to environmental and economic ... filtered and purified by column chromatography on.

  6. Sustained transdermal release of diltiazem hydrochloride through electron beam irradiated different PVA hydrogel membranes

    Energy Technology Data Exchange (ETDEWEB)

    Bhunia, Tridib [Department of Polymer Science and Technology, University of Calcutta, 92 A.P.C. Road, Calcutta 700009 (India); Goswami, Luna [KIIT School of Biotechnology, KIIT University Campus XI, Patia, Bhubaneswar 751024, Orissa (India); Chattopadhyay, Dipankar [Department of Polymer Science and Technology, University of Calcutta, 92 A.P.C. Road, Calcutta 700009 (India); Bandyopadhyay, Abhijit, E-mail: abpoly@caluniv.ac.in [Department of Polymer Science and Technology, University of Calcutta, 92 A.P.C. Road, Calcutta 700009 (India)

    2011-08-15

    Extremely fast release of diltiazem hydrochloride (water soluble, anti anginal drug used to treat chest pain) together with its faster erosion has been the primary problem in conventional oral therapy. It has been addressed in this paper by encapsulating the drug in electron beam irradiated various poly (vinyl alcohol) hydrogel membranes and delivering it through transdermal route. Results show excellent control over the release of diltiazem hydrochloride through these membranes subject to their physico-mechanicals.

  7. Sustained transdermal release of diltiazem hydrochloride through electron beam irradiated different PVA hydrogel membranes

    Science.gov (United States)

    Bhunia, Tridib; Goswami, Luna; Chattopadhyay, Dipankar; Bandyopadhyay, Abhijit

    2011-08-01

    Extremely fast release of diltiazem hydrochloride (water soluble, anti anginal drug used to treat chest pain) together with its faster erosion has been the primary problem in conventional oral therapy. It has been addressed in this paper by encapsulating the drug in electron beam irradiated various poly (vinyl alcohol) hydrogel membranes and delivering it through transdermal route. Results show excellent control over the release of diltiazem hydrochloride through these membranes subject to their physico-mechanicals.

  8. Sustained transdermal release of diltiazem hydrochloride through electron beam irradiated different PVA hydrogel membranes

    International Nuclear Information System (INIS)

    Bhunia, Tridib; Goswami, Luna; Chattopadhyay, Dipankar; Bandyopadhyay, Abhijit

    2011-01-01

    Extremely fast release of diltiazem hydrochloride (water soluble, anti anginal drug used to treat chest pain) together with its faster erosion has been the primary problem in conventional oral therapy. It has been addressed in this paper by encapsulating the drug in electron beam irradiated various poly (vinyl alcohol) hydrogel membranes and delivering it through transdermal route. Results show excellent control over the release of diltiazem hydrochloride through these membranes subject to their physico-mechanicals.

  9. Disposable screen-printed sensors for determination of duloxetine hydrochloride

    Directory of Open Access Journals (Sweden)

    Alarfaj Nawal A

    2012-01-01

    Full Text Available Abstract A screen-printed disposable electrode system for the determination of duloxetine hydrochloride (DL was developed using screen-printing technology. Homemade printing has been characterized and optimized on the basis of effects of the modifier and plasticizers. The fabricated bi-electrode potentiometric strip containing both working and reference electrodes was used as duloxetine hydrochloride sensor. The proposed sensors worked satisfactorily in the concentration range from 1.0 × 10-6-1.0 × 10-2 mol L-1 with detection limit reaching 5.0 × 10-7 mol L-1 and adequate shelf life of 6 months. The method is accurate, precise and economical. The proposed method has been applied successfully for the analysis of the drug in pure and in its dosage forms. In this method, there is no interference from any common pharmaceutical additives and diluents. Results of the analysis were validated statistically by recovery studies.

  10. 3.3.1. Filtration properties of hydrochloride-acid pulps at reprocessingof nepheline syenites by baking method with calcium chloride

    International Nuclear Information System (INIS)

    Nazarov, Sh.B.; Safiev, Kh.S.; Mirsaidov, U.

    2008-01-01

    At hydrochloride-acid decomposition of solid residuum from the waterprocessing of cake obtained at baking of nepheline with calcium chloride into the liquid phase pass hydrochloride-acid of aluminium and iron

  11. Curcumin enhances the mitomycin C-induced cytotoxicity via downregulation of MKK1/2-ERK1/2-mediated Rad51 expression in non-small cell lung cancer cells

    International Nuclear Information System (INIS)

    Ko, Jen-Chung; Tsai, Min-Shao; Weng, Shao-Hsing; Kuo, Ya-Hsun; Chiu, Yu-Fan; Lin, Yun-Wei

    2011-01-01

    Curcumin (diferuloylmethane), a major active component of turmeric (Curcuma longa), has been reported to suppress the proliferation of a wide variety of tumor cells. Rad51 is a key protein in the homologous recombination (HR) pathway of DNA double-strand break repair, and HR represents a novel target for cancer therapy. A high expression of Rad51 has been reported in chemo- or radio-resistant carcinomas. Therefore, in the current study, we will examine whether curcumin could enhance the effects of mitomycin C (MMC), a DNA interstrand cross-linking agent, to induce cytotoxicity by decreasing Rad51 expression. Exposure of two human non-small lung cancer (NSCLC) cell lines (A549 and H1975) to curcumin could suppress MMC-induced MKK1/2-ERK1/2 signal activation and Rad51 protein expression. Enhancement of ERK1/2 activation by constitutively active MKK1/2 (MKK1/2-CA) increased Rad51 protein levels in curcumin and MMC co-treated human lung cells. Moreover, the synergistic cytotoxic effect induced by curcumin combined with MMC was decreased by MKK1-CA-mediated enhancement of ERK1/2 activation by a significant degree. In contrast, MKK1/2 inhibitor, U0126 was shown to augment the cytotoxicity of curcumin and MMC through downregulation of ERK1/2 activation and Rad51 expression. Depletion of endogenous Rad51 expression by siRad51 RNA transfection significantly enhanced MMC and/or curcumin induced cell death and cell growth inhibition. In contrast, an overexpression of Rad51 protected lung cancer cells from synergistic cytotoxic effects induced by curcumin and MMC. We concluded that Rad51 inhibition may be an additional action mechanism for enhancing the chemosensitization of MMC by curcumin in NSCLC. - Highlights: → Curcumin downregulates MKK-ERK-mediated Rad51 expression. → Curcumin enhances mitomycin C-induced cytotoxicity. → Rad51 protects cells from cytotoxic effects induced by curcumin and mitomycin C. → Rad51 inhibition enhances the chemosensitization of

  12. Surface tension of compositions of polyhexametyleneguanidine hydrochloride - surfactants

    Directory of Open Access Journals (Sweden)

    S. Kumargaliyeva

    2012-12-01

    Full Text Available We made up songs bactericidal polyhexamethyleneguanidine hydrochloride (metacyde with the surface-active substances - anionic sodium dodecylsulfate, cationic cetylpyridinium bromide, and nonionic Tween-80 and measured the surface tension of water solutions. The study showed that the composition metacyde with surface-active agents have a greater surface activity than the individual components.

  13. Effect of Magnesium Stearate Concentration on Dissolution Properties of Ranitidine Hydrochloride Coated Tablets

    Directory of Open Access Journals (Sweden)

    Alija Uzunović

    2007-08-01

    Full Text Available 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 pharmaco-peial 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.

  14. UPLC and LC-MS studies on degradation behavior of irinotecan hydrochloride and development of a validated stability-indicating ultra-performance liquid chromatographic method for determination of irinotecan hydrochloride and its impurities in pharmaceutical dosage forms.

    Science.gov (United States)

    Kumar, Navneet; Sangeetha, Dhanaraj; Reddy, Sunil P

    2012-10-01

    The objective of the current investigation was to study the degradation behavior of irinotecan hydrochloride under different International Conference on Harmonization (ICH) recommended stress conditions using ultra-performance liquid chromatography and liquid chromatography-mass spectrometry and to establish a validated stability-indicating reverse-phase ultra-performance liquid chromatographic method for the quantitative determination of irinotecan hydrochloride and its seven impurities and degradation products in pharmaceutical dosage forms. Irinotecan hydrochloride was subjected to the stress conditions of oxidative, acid, base, hydrolytic, thermal and photolytic degradation. Irinotecan hydrochloride was found to degrade significantly in oxidative and base hydrolysis and photolytic degradation conditions. The degradation products were well resolved from the main peak and its impurities, thus proving the stability-indicating power of the method. Chromatographic separation was achieved on a Waters Acquity BEH C8 (100 × 2.1 mm) 1.7-µm column with a mobile phase containing a gradient mixture of solvent A (0.02M KH(2)PO(4) buffer, pH 3.4) and solvent B (a mixture of acetonitrile and methanol in the ratio of 62:38 v/v). The mobile phase was delivered at a flow rate of 0.3 mL/min with ultraviolet detection at 220 nm. The run time was 8 min, within which irinotecan and its seven impurities and degradation products were satisfactorily separated. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision and robustness. This method was also suitable for the assay determination of irinotecan hydrochloride in pharmaceutical dosage forms.

  15. A novel drug delivery gel of terbinafine hydrochloride with high penetration for external use.

    Science.gov (United States)

    Yang, Yan; Ou, Rujing; Guan, Shixia; Ye, Xiaoling; Hu, Bo; Zhang, Yi; Lu, Shufan; Zhou, Yubin; Yuan, Zhongwen; Zhang, Jun; Li, Qing-Guo

    2015-12-01

    Terbinafine hydrochloride is an antifungal drug for onychomycosis. Poor permeability of its external preparation leads to poor curative effect. Transfersomes, also known as flexible liposome, could improve transmission of drug for local external use. Terbinafine hydrochloride-loaded liposome is expected to become a breakthrough on the treatment of onychomycosis. This study is aimed to prepare high skin penetration terbinafine hydrochloride transfersomes with high encapsulation efficiency, appropriate drug loading and good stability. Taking entrapment efficiency as the main indicator, the formulations and the processes of preparation were investigated. Transfersomes with different surfactants were prepared in the optimization processes, and the formulations were optimized through the transdermal test in vitro. As a result, a gel contained transfersomes was obtained with a brief evaluation. Its pharmacokinetic properties of going through the skin were studied by using the micro dialysis technology and liquid chromatography-mass spectrometry to assay the penetration behavior of terbinafine. Mean particle size of the terbinafine hydrochloride transfersomes was 69.6 ± 1.23 nm, and the entrapment efficiency was 95.4% ± 0.51. The content of the gel was 4.45 ± 0.15 mg/g. The accumulated permeation of the transfersomes gel in 12 h was 88.52 ± 4.06 µg cm -2 and the intracutaneous drug detention was 94.38 ± 5.26 µg cm -2 . The results of pharmacokinetic studies showed the C max and area under the curve (AUC) were apparently higher than the commercial cream. The terbinafine hydrochloride transfersomes was highly absorbed by the skin. The absorption rate was significantly higher than that of the commercial cream either in the transdermal test in vitro or in the pharmacokinetic studies in vivo.

  16. [Intraoperative chemotherapy against peritoneal dissemination of gastric cancer with intraperitoneal activated carbon particles adsorbing mitomycin C].

    Science.gov (United States)

    Hagiwara, A; Takahashi, T; Sawai, K; Yamaguchi, T; Iwamoto, A; Yoneyama, C

    1989-02-01

    For prevention and therapy of peritoneal dissemination, a new dosage from (MMC-CH) comprising carbon particles adsorbing mitomycin C was given to 44 patients (the MMC-CH group) undergoing gastrectomy for gastric cancer, of which advancing stage was classified into the category of H0, and S2 or S3, and P0, P1, P2 or P3 according to the General Rules for the Gastric Cancer Study. MMC-CH, principally at 50 mg person in terms of mitomycin C was administered intraperitoneally before the surgical wound was closed. Historical control group was composed of 53 patients not given MMC-CH, who underwent gastrectomy for gastric cancer in the same advancing stage as those of the 44 patients. There was statistically no significant difference of age, sex, depth of infiltration, macroscopically and microscopically defined progression of lymph-nodal metastases, between the MMC-CH group and the historical control group. The survival rate of the overall patients, and each group of the patients with the lesion defined as P0, P1, P2, or P3 was compared with Kaplan-Meier's method between the MMC-CH group and the historical control group. In the MMC-CH group, the survival rates of the overall patients and the patients with P0, P1, or P2 lesion were statistically significantly higher than those in the historical control group. However, the rate of the P3 patients in the MMC-CH group was statistically significantly lower than in the historical control group.

  17. Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

    Directory of Open Access Journals (Sweden)

    Mahmood S

    2014-09-01

    Full Text Available Syed Mahmood, Muhammad Taher, Uttam Kumar Mandal Department of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia (IIUM, Pahang Darul Makmur, Malaysia Abstract: Raloxifene hydrochloride, a highly effective drug for the treatment of invasive breast cancer and osteoporosis in post-menopausal women, shows poor oral bioavailability of 2%. The aim of this study was to develop, statistically optimize, and characterize raloxifene hydrochloride-loaded transfersomes for transdermal delivery, in order to overcome the poor bioavailability issue with the drug. A response surface methodology experimental design was applied for the optimization of transfersomes, using Box-Behnken experimental design. Phospholipon® 90G, sodium deoxycholate, and sonication time, each at three levels, were selected as independent variables, while entrapment efficiency, vesicle size, and transdermal flux were identified as dependent variables. The formulation was characterized by surface morphology and shape, particle size, and zeta potential. Ex vivo transdermal flux was determined using a Hanson diffusion cell assembly, with rat skin as a barrier medium. Transfersomes from the optimized formulation were found to have spherical, unilamellar structures, with a ­homogeneous distribution and low polydispersity index (0.08. They had a particle size of 134±9 nM, with an entrapment efficiency of 91.00%±4.90%, and transdermal flux of 6.5±1.1 µg/cm2/hour. Raloxifene hydrochloride-loaded transfersomes proved significantly superior in terms of amount of drug permeated and deposited in the skin, with enhancement ratios of 6.25±1.50 and 9.25±2.40, respectively, when compared with drug-loaded conventional liposomes, and an ethanolic phosphate buffer saline. Differential scanning calorimetry study revealed a greater change in skin structure, compared with a control sample, during the ex vivo drug diffusion study. Further, confocal laser

  18. HPMA copolymer conjugates of DOX and mitomycin C for combination therapy: physicochemical characterization, cytotoxic effects, combination index analysis, and anti-tumor efficacy

    Czech Academy of Sciences Publication Activity Database

    Kostková, Hana; Etrych, Tomáš; Říhová, Blanka; Kostka, Libor; Starovoytova, Larisa; Kovář, Marek; Ulbrich, Karel

    2013-01-01

    Roč. 13, č. 12 (2013), s. 1648-1660 ISSN 1616-5187 R&D Projects: GA ČR GAP301/11/0325; GA MŠk EE2.3.30.0029 Institutional support: RVO:61389013 ; RVO:61388971 Keywords : doxorubicin * HPMA copolymers * mitomycin C Subject RIV: CE - Biochemistry; FD - Oncology ; Hematology (MBU-M) Impact factor: 3.650, year: 2013

  19. Adsorption of dodecylamine hydrochloride on graphene oxide in water

    Directory of Open Access Journals (Sweden)

    Peng Chen

    Full Text Available Cationic surfactants in water are difficult to be degraded, leading to serious water pollution. In this work, graphene oxide (GO was used as an adsorbent for removing Dodecylamine Hydrochloride (DACl, a representative cationic surfactant. X-ray diffraction (XRD, FT-IR spectroscopy and atomic force microscope (AFM were used to characterize the prepared GO. The adsorption of DACl on GO have been investigated through measurements of adsorption capacity, zeta potential, FTIR, and X-ray photoelectron spectroscopy (XPS. The experimental results have shown that the adsorption kinetics could be described as a rate-limiting pseudo second-order process, and the adsorption isotherm agreed well with the Freundlich model. GO was a good adsorbent for DACl removal, compared with coal fly ash and powdered activated carbon. The adsorption process was endothermic, and could be attributed to electrostatic interaction and hydrogen bonding between DACl and GO. Keywords: Graphene oxide, Dodecylamine hydrochloride, Adsorption isotherm, Adsorption mechanisms

  20. Characterization of the effect of penehyclidine hydrochloride on muscarinic receptor subtypes mediating the contraction of guinea-pig isolated gastrointestinal smooth muscle.

    Science.gov (United States)

    Xiao, Hong-Tao; Liao, Zhi; Meng, Xian-Min; Yan, Xiao-Yan; Chen, Shu-Jie; Mo, Zheng-Ji

    2009-07-01

    The aim was to characterize the effect of penehyclidine hydrochloride, which mediates the relaxation of guinea-pig isolated gastrointestinal smooth muscle, on muscarinic receptor subtypes. Radioimmune assay was used to determine cAMP levels in isolated guinea-pig gastrointestinal smooth muscle to compare the selective effects of penehyclidine hydrochloride on muscarinic receptor subtypes. The results indicated that the relaxing effect of penehyclidine hydrochloride on isolated gastrointestinal smooth muscle contraction induced by acetylcholine was stronger than that of atropine (based on PA2 values). In the radioimmune assay, penehyclidine hydrochloride increased the cAMP content in isolated guinea-pig stomach smooth muscle and decreased the cAMP content in isolated guinea-pig intestinal smooth muscle, but the difference was not statistically significant at a dose of 10 mumol/l. The results suggest that penehyclidine hydrochloride has little or no effect on M2 receptor subtypes in guinea-pig gastrointestinal smooth muscle.

  1. Stability-Indicating RP-HPLC Method for Determination of Guanfacine Hydrochloride in Bulk Drugs and in Pharmaceutical Dosage Form

    Directory of Open Access Journals (Sweden)

    Vinod K. Ahirrao

    2011-04-01

    Full Text Available A novel stability-indicating RP-HPLC method was developed and validated for quantitative determination of guanfacine hydrochloride in bulk drug and in pharmaceutical dosage form. An isocratic, reversed phase HPLC method was developed to separate the drug from the degradation products, using Apollo, C18 (250mm x 4.6mm, 5µm column with mobile phase of 50mM Ammonium acetate (volatile buffer and acetonitrile (65:35, v/v. UV detection has been done at wavelength 220 nm. The guanfacine hydrochloride was subjected to the stress conditions of hydrolysis (acid, base, oxidation, photolysis and thermal degradation. The stressed samples were analyzed by the proposed method. The analyte peak shape was excellent. The described method shows excellent linearity over a range of 30 – 450 µg/mL. The correlation coefficient for guanfacine hydrochloride was 0.999. The limit of detection for Guanfacine hydrochloride is 0.011 µg/mL and the limit of quantification is 0.038 µg/mL respectively.Degradation was observed for guanfacine hydrochloride in base, thermal and in 30% H2O2 conditions. The drug was found to be stable in the other stress conditions attempted. The degradation products were well resolved from main peak. The percentage recovery of guanfacine hydrochloride was ranged from (99.2% to 100.5% in pharmaceutical dosage form. The developed method was validated with respect to the linearity, accuracy (recovery, precision, specificity and robustness. The forced degradation studies prove the stability indicating power of the method.

  2. Determination of in vivo behavior of mitomycin C-loaded o/w soybean oil microemulsion and mitomycin C solution via gamma camera imaging.

    Science.gov (United States)

    Kotmakçı, Mustafa; Kantarcı, Gülten; Aşıkoğlu, Makbule; Ozkılıç, Hayal; Ertan, Gökhan

    2013-09-01

    In this study, a microemulsion system was evaluated for delivery of mitomycin C (MMC). To track the distribution of the formulated drug after intravenous administration, radiochemical labeling and gamma scintigraphy imaging were used. The aim was to evaluate a microemulsion system for intravenous delivery of MMC and to compare its in vivo behavior with that of the MMC solution. For microemulsion formulation, soybean oil was used as the oil phase. Lecithin and Tween 80 were surfactants and ethanol was the cosurfactant. To understand the whole body localization of MMC-loaded microemulsion, MMC was labeled with radioactive technetium and gamma scintigraphy was applied for visualization of drug distribution. Radioactivity in the bladder 30 minutes after injection of the MMC solution was observed, according to static gamma camera images. This shows that urinary excretion of the latter starts very soon. On the other hand, no radioactivity appeared in the urinary bladder during the 90 minutes following the administration of MMC-loaded microemulsion. The unabated radioactivity in the liver during the experiment shows that the localization of microemulsion formulation in the liver is stable. In the light of the foregoing, it is suggested that this microemulsion formulation may be an appropriate carrier system for anticancer agents by intravenous delivery in hepatic cancer chemotherapy.

  3. Sustained release of verapamil hydrochloride from sodium alginate microcapsules.

    Science.gov (United States)

    Farhana, S Ayesha; Shantakumar, S M; Shyale, Somashekar; Shalam, Md; Narasu, Laxmi

    2010-04-01

    The objective of the present study was to develop sustained release microcapsules of verapamil hydrochloride (VH) using biodegradable polymers. For this purpose microcapsules embedded verapamil hydrochloride were prepared using sodium alginate alone and also by incorporating some co polymers like methyl cellulose (MC), sodium carboxy methyl cellulose (SCMC) , poly vinyl pyrollidone (PVP) and xanthan gum by employing complex emulsion method of microencapsulation. Microcapsules were prepared in various core: coat ratios to know the effect of polymer and co polymers on drug release. Overall ten formulations were prepared and evaluated for flow behaviour, sieve analysis, drug entrapment efficiency, in vitro dissolution studies, stability studies, including scanning electron microscopy and DSC. The resulting microcapsules were discrete, large, spherical and also free flowing. The drug content in all the batches of microcapsules was found to be uniform. The release was depended on core: coat ratio and nature of the polymers. FTIR analysis revealed chemical integrity between Verapamil hydrochloride (VH), sodium alginate and between the copolymers. Among the four copolymers used methyl cellulose retarded the drug release more than the other three, hence the same formulation was subjected for in vivo studies. The drug release from the microcapsules was found to be following non fickian diffusion. Mechanism of drug release was diffusion controlled first order kinetics. Drug diffusion co efficient and correlation co efficient were also assessed by using various mathematical models. In vivo result analysis of pharmacokinetic parameters revealed that t max of reference and test formulations were almost same. From the study it was concluded that, sustained release Verapamil hydro chloride microcapsules could be achieved with success using sodium alginate alone and also in combination with other biodegradable polymers.

  4. Synthesis of 1,5-Diaryl-1,4-pentadien-3-one Amidinohydrazone Hydrochloride Under Ultrasound Irradiation

    Directory of Open Access Journals (Sweden)

    Chao Du

    2012-01-01

    Full Text Available Synthesis of 1,5-diaryl-1,4-pentadien-3-one amidinohydrazone hydrochloride via the condensation of 1,5-diaryl-1,4-pentadien-3-one and aminoguanidine hydrochloride catalyzed by hydrochloric acid was carried out in 80-94% yield at 35-37°C within 1.5 h under ultrasound irradiation. Compared to the classical method, the advantages of this method are milder conditions, shorter reaction time and higher yield.

  5. Volumetric and viscometric studies of cefepime hydrochloride in water and normal saline from (278.15 to 313.15) K

    International Nuclear Information System (INIS)

    Li, Yu; Li, Yan-hong; Wang, Fu-an; Ren, Bao-zeng

    2013-01-01

    Graphical abstract: The limiting partial molar volume V ϕ 0 of cefepime hydrochloride in water are positive and increase with increasing temperature. The positive values of V ϕ 0 indicate that the solute–solvent interaction decreases as temperature increases. Highlights: • Density and viscosity of cefepime hydrochloride in water and normal saline has been obtained. • The results show that the model agrees well with the experimental data. • The nature of solute–solute and solute–solvent interactions has been probed. -- Abstract: Density (ρ) and viscosity (η) measurements were carried out for cefepime hydrochloride in water and 0.9 mass % normal saline from (278.15 to 313.15) K. The dependence of density and viscosity on temperature and concentration has been correlated. Apparent molar volumes, standard partial molar volumes, and the viscosity B-coefficient of cefepime hydrochloride were calculated from the experimental measurements. The results are used to establish the nature of solute–solute. Solute–solvent interactions and structure breaking effect of cefepime hydrochloride have been discussed using the Helper equation and the Jones–Dole equation. The relationship between relative changes in viscosity and solute-mixed solvent interaction has been probed

  6. Pharmacokinetic interaction of finasteride with tamsulosin hydrochloride: an open-label, randomized, 3-period crossover study in healthy Chinese male volunteers.

    Science.gov (United States)

    Chu, Nannan; Xu, Hongrong; Wang, Guoqin; Wang, Jiangdian; Chen, Weili; Yuan, Fei; Yang, Mengjie; Li, Xuening

    2015-02-01

    The primary aim of this study was to evaluate whether there was clinically significant pharmacokinetic (PK) interaction between finasteride and tamsulosin in healthy Chinese male subjects. This was an open-label, randomized, 3-period, crossover study. Subjects received single and multiple doses of 5 mg finasteride alone, single and multiple doses of 0.2 mg tamsulosin hydrochloride sustained-release capsule alone, and single and multiple doses of 5 mg finasteride with 0.2 mg tamsulosin hydrochloride, in an order determined by a computerized randomization schedule. Blood samples were collected up to 48 hours after dosing on study day 1 and up to 24 hours after dosing on study day 9 for determination of plasma concentrations with a validated LC-MS/MS method. Pharmacokinetic parameters were estimated via noncompartmental methods. Tolerability was evaluated by monitoring adverse events, laboratory assays, vital signs, and 12-lead ECG. Fifteen subjects were enrolled, and 14 completed the study. The geometric mean ratios (GMRs) (90% CIs) of AUC(τ,ss) and C(max,ss) values of finasteride at steady state between coadministration of finasteride and tamsulosin hydrochloride and finasteride alone were 1.14 (1.05-1.23) and 1.06 (0.99-1.14), respectively. The GMRs (90% CIs) for AUC(0-t) and C(max) values of finasteride for a single dose of coadministration of finasteride and tamsulosin hydrochloride and finasteride alone were 1.02 (0.94-1.11) and 1.06 (1.01-1.11), respectively. The GMRs (90% CIs) for AUC(τ,ss) and C(max,ss) values of tamsulosin at steady-state for coadministration of finasteride and tamsulosin hydrochloride and tamsulosin hydrochloride alone were 1.18 (1.05-1.33) and 1.23 (1.06-1.43), respectively. The GMRs (90% CIs) for AUC(0-t) and C(max) values of tamsulosin for a single dose of coadministration of finasteride and tamsulosin hydrochloride and tamsulosin hydrochloride alone were 1.04 (0.97-1.10) and 1.04 (0.98-1.11), respectively. Statistical analyses

  7. Effects of itopride hydrochloride and ranitidine in patients with functional dyspepsia: comparison between prokinetic and acid suppression therapies.

    Science.gov (United States)

    Chiba, Toshimi; Tokunaga, Yumi; Ikeda, Keisei; Takagi, Ryo; Chishima, Raita; Terui, Torahiko; Kudara, Norihiko; Endo, Masaki; Inomata, Masaaki; Orii, Seishi; Suzuki, Kazuyuki

    2007-09-01

    The effect of itopride hydrochloride or ranitidine on the health-related quality of life (HRQoL) of functional dyspepsia is not well known. Our aim was to assess the HRQoL before and after administration of itopride hydrochloride or ranitidine in patients with functional dyspepsia. A total of 18 functional dyspepsia patients (12 women, 6 men; mean age 52.5 y.o.) were enrolled. We determined the HRQoL using two different inquiry systems: the 36 item short form of the Medical Outcome Study Questionnaire (SF-36) and the Gastrointestinal Symptom Rating Scale (GSRS). The HRQoL was determined before administration of drug, and two, four, and eight weeks after administration of drug. After administration of itopride hydrochloride, the SF-36 mental health scale and GSRS indigestion syndrome score and constipation syndrome score were significantly improved compared to before administration (p Itopride hydrochloride would be useful for the treatment of dysmotility-type functional dyspepsia, whereas ranitidine would be beneficial for ulcer-type functional dyspepsia.

  8. The influence of family history of cancer, irradiation and anticancer medication (mitomycin C), on the occurrence of multiple primary neoplasms with breast cancer

    International Nuclear Information System (INIS)

    Yoshimoto, Masataka; Kasumi, Fujio; Fukami, Atsuo; Nishi, Mitsumasa; Kajitani, Tamaki; Sakamoto, Goi

    1985-01-01

    The influence of family history of cancer, radiation therapy and anticancer drug therapy (mitomycin C) on the occurrence of multiple primary neoplasms, following treatment of a first primary cancer of the breast, was analyzed by the person-year method in 1,359 patients, in Japan. During 14,371.8 person-years of observation, 111 multiple primary neoplasms including bilateral breast cancers were found in 109 patients. The incidence rate of multiple primary neoplasms were 0.00772 per person-year. The incidence in patients with a family history of cancer was 1.29 times greater than that in patients without such a family history, and the incidence in patients with a family history of breast cancer was about three times greater than that in those without it (p < 0.01). Radiation therapy raised the occurrence of subsequent primary neoplasms 1.28-fold (or 1.62 fold after 5 years), and mitomycin C (a total dose of 0.8 mg/kg) therapy caused no increase in the occurrence of subsequent primary cancers, after an observation of 10 years or so. (author)

  9. Preparation and the in vitro evaluation of nanoemulsion system for the transdermal delivery of granisetron hydrochloride.

    Science.gov (United States)

    Zheng, Wen-wu; Zhao, Ling; Wei, Yu-meng; Ye, Yun; Xiao, Shun-han

    2010-08-01

    The objective of this study was to develop and evaluate nanoemulsion system for transdermal delivery of granisetron hydrochloride. Pseudo-ternary phase diagram was constructed to ascertain the concentration range of components of nanoemulsion composed of isopropyl myristate (IPM) as an oil phase, tween 85 as surfactant, ethanol as cosurfactant, water as aqueous phase. The effects of the content of IPM as an oil phase and n-methyl pyrrolidone (NMP) as transdermal enhancer on rat skin permeation of granisetron hydrochloride nanoemulsion were studied in vitro. The results showed that the mean particle size of nanoemulsion ranged from 50.4+/-1.5 to 82.4+/-0.9 nm with homogeneous size distribution. The resulted optimum formulation composed of 2.5% granisetron hydrochloride, 4% IPM, 40% tween 85/ethanol (1 : 1) and 10% NMP showed that the skin permeation rate was the highest (85.39+/-2.90 microg/cm(2)/h) and enhancement of drug permeability was 4.1-fold for transdermal delivery of granisetron hydrochloridein comparison with the control group (20% of tween 85 and 20% of ethanol micelle solution containing 2.5% of granisetron hydrochloride without IPM), and cumulative permeation amount was the highest (891.8+/-2.86 microg/cm(2)) with the shortest lag time (0.11+/-0.02 h) and was stable for at least 12 months. Therefore, the nanoemulsion system developed in this study offers a promising vehicle for the transdermal delivery system of granisetron hydrochloride, which may be as effective as oral or intravenous dosage forms and avoid some difficulties associated with these dosage forms.

  10. Mitomycin-treated undifferentiated embryonic stem cells as a safe and effective therapeutic strategy in a mouse model of Parkinson's disease.

    Directory of Open Access Journals (Sweden)

    Mariana eAcquarone

    2015-04-01

    Full Text Available Parkinson’s disease (PD is an incurable progressive neurodegenerative disorder. Clinical presentation of PD stems largely from the loss of dopaminergic neurons in the nigrostriatal dopaminergic pathway, motivating experimental strategies aimed at replacing dopaminergic innervation by cellular therapy. Transplantation of dopaminergic neurons derived from embryonic stem cells significantly improves motor functions in rodent and non-human primate models of PD. However, protocols to generate dopaminergic neurons from embryonic stem cells generally meet with low efficacy and high risk of teratoma development upon transplantation. To address these issues, we have pre-treated undifferentiated mouse embryonic stem cells (mESCs with the DNA alkylating agent mitomycin C (MMC before transplantation. MMC treatment of cultures prevented tumor formation in a 12-week follow-up after mESCs were injected in nude mice. In 6-OH-dopamine-lesioned mice, intrastriatal injection of MMC-treated mESCs markedly improved motor function without tumor formation for as long as 15 months. Furthermore, we show that halting mitotic activity of undifferentiated mESCs induces a four-fold increase in dopamine release following in vitro differentiation. Our findings indicate that treating mESCs with mitomycin C prior to intrastriatal transplant is an effective strategy that could be further investigated as a novel alternative for treatment of Parkinson's disease.

  11. On the guanidine hydrochloride method for determination of oxygen-18 content in orthophosphate

    International Nuclear Information System (INIS)

    Li Wenjun; Gu Zhennan

    1985-01-01

    The guanidine hydrochloride method is an accurate and simple procedure for oxygen-18 determination in KH 2 PO 4 and Ba 3 (PO 4 ) 2 . The method is based on heating the samples with guanidine hydrochloride at 300 deg C. Two Oxygen atoms per molecule of KH 2 PO 4 or Ba 3 (PO 4 ) 2 are converted into CO 2 which is then analysed by a mass spectrometer of model MAT-CH5. Only 5 mg of KH 2 PO 4 or Ba 3 (PO 4 ) 2 is required for each determination and reproducibility of assays is better than +-1%. (Author)

  12. Feasibility of ion-pair/supercritical fluid extraction of an ionic compound--pseudoephedrine hydrochloride.

    Science.gov (United States)

    Eckard, P R; Taylor, L T

    1997-02-01

    The supercritical fluid extraction (SFE) of an ionic compound, pseudoephedrine hydrochloride, from a spiked-sand surface was successfully demonstrated. The effect of carbon dioxide density (CO2), supercritical fluid composition (pure vs. methanol modified), and the addition of a commonly used reversed-phase liquid chromatographic ion-pairing reagent, 1-heptanesulfonic acid, sodium salt, on extraction efficiency was examined. The extraction recoveries of pseudoephedrine hydrochloride with the addition of the ion-pairing reagent from a spiked-sand surface were shown to be statistically greater than the extraction recoveries without the ion-pairing reagent with both pure and methanol-modified carbon dioxide.

  13. Denaturation/Renaturation of Organophosphorus Acid Anhydrolase (OPAA) Using Guanidinium Hydrochloride and Urea

    National Research Council Canada - National Science Library

    Ong, K. K; Sun, Z; Cheng, T. C; Wei, Y; Yuan, J. M; Yin, R

    2004-01-01

    .... Using organophosphorus acid anhydrolase (OPAA) as the model protein, a guanidinium hydrochloride and urea denaturation/renaturation study was conducted and measured both optically and enzymatically...

  14. Dehydration of detomidine hydrochloride monohydrate.

    Science.gov (United States)

    Veldre, K; Actiņš, A; Jaunbergs, J

    2011-10-09

    The thermodynamic stability of detomidine hydrochloride monohydrate has been evaluated on the basis of phase transition kinetics in solid state. A method free of empirical models was used for the treatment of kinetic data, and compared to several known solid state kinetic data processing methods. Phase transitions were monitored by powder X-ray diffraction (PXRD) and thermal analysis. Full PXRD profiles were used for determining the phase content instead of single reflex intensity measurements, in order to minimize the influence of particle texture. We compared the applicability of isothermal and nonisothermal methods to our investigation of detomidine hydrochlorine monohydrate dehydration. Copyright © 2011 Elsevier B.V. All rights reserved.

  15. A phase III trial of docetaxel/carboplatin versus mitomycin C/ifosfamide/cisplatin (MIC) or mitomycin C/vinblastine/cisplatin (MVP) in patients with advanced non-small-cell lung cancer: a randomised multicentre trial of the British Thoracic Oncology Group (BTOG1).

    Science.gov (United States)

    Booton, R; Lorigan, P; Anderson, H; Baka, S; Ashcroft, L; Nicolson, M; O'Brien, M; Dunlop, D; O'Byrne, K; Laurence, V; Snee, M; Dark, G; Thatcher, N

    2006-07-01

    Phase III studies suggest that non-small-cell lung cancer (NSCLC) patients treated with cisplatin-docetaxel may have higher response rates and better survival compared with other platinum-based regimens. We report the final results of a randomised phase III study of docetaxel and carboplatin versus MIC or MVP in patients with advanced NSCLC. Patients with biopsy proven stage III-IV NSCLC not suitable for curative surgery or radiotherapy were randomised to receive four cycles of either DCb (docetaxel 75 mg/m(2), carboplatin AUC 6), or MIC/MVP (mitomycin 6 mg/m(2), ifosfamide 3 g/m(2) and cisplatin 50 mg/m(2) or mitomycin 6 mg/m(2), vinblastine 6 mg/m(2) and cisplatin 50 mg/m(2), respectively), 3 weekly. The primary end point was survival, secondary end points included response rates, toxicity and quality of life. The median follow-up was 17.4 months. Overall response rate was 32% for both arms (partial response = 31%, complete response = 1%); 32% of MIC/MVP and 26% of DCb patients had stable disease. One-year survival was 39% and 35% for DCb and MIC/MVP, respectively. Two-year survival was 13% with both arms. Grade 3/4 neutropenia (74% versus 43%, P MVP. The MIC/MVP arm had significant worsening in overall EORTC score and global health status whereas the DCb arm showed no significant change. The combination of DCb had similar efficacy to MIC/MVP but quality of life was better maintained.

  16. Preparation and controlled release of mesoporous MCM-41/propranolol hydrochloride composite drug.

    Science.gov (United States)

    Zhai, Qing-Zhou

    2013-01-01

    This article used MCM-41 as a carrier for the assembly of propranolol hydrochloride by the impregnation method. By means of chemical analysis, powder X-ray diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared (FT-IR) spectroscopy and low-temperature N(2) adsorption-desorption at 77 K, the characterization was made for the prepared materials. The propranolol hydrochloride guest assembly capacity was 316.20 ± 0.31 mg/g (drug/MCM-41). Powder XRD test results indicated that during the process of incorporation, the frameworks of the MCM-41 were not destroyed and the crystalline degrees of the host-guest nanocomposite materials prepared still remained highly ordered. Characterization by SEM and TEM showed that the composite material presented spherical particle and the average particle size of composite material was 186 nm. FT-IR spectra showed that the MCM-41 framework existed well in the (MCM-41)-propranolol hydrochloride composite. Low-temperature nitrogen adsorption-desorption results at 77 K showed that the guest partially occupied the channels of the molecular sieves. Results of the release of the prepared composite drug in simulated body fluid indicated that the drug can release up to 32 h and its maximum released amount was 99.20 ± 0.11%. In the simulated gastric juice release pattern of drug, the maximum time for the drug release was discovered to be 6 h and the maximum cumulative released amount of propranolol hydrochloride was 45.13 ± 0.23%. The drug sustained-release time was 10 h in simulated intestinal fluid and the maximum cumulative released amount was 62.05 ± 0.13%. The prepared MCM-41 is a well-controlled drug delivery carrier.

  17. Evaluation of mitomycin-C effect on biodistribution of {sup 99m}Tc-dimercaptosuccinic acid in BALB/C mice; Avaliacao do efeito da mitomicina-c na biodistribuicao do radiofarmaco acido dimercaptosuccinico marcado com tecnecio-99m em camundongos BALB/C

    Energy Technology Data Exchange (ETDEWEB)

    Gomes, Maria Luisa; Britto, Deise Mara de M.; Freitas, Rosimeire de S.; Bernardo-Filho, Mario [Instituto Nacional do Cancer, Rio de Janeiro, RJ (Brazil). Centro de Pesquisa Basica; Braga, Ana Cristina de S.; Bezerra, Roberto Jose A.C. [Universidade do Estado, Rio de Janeiro, RJ (Brazil). Inst. de Biologia Roberto Alcantara Gomes. Dept. de Biofisica e Biometria

    1999-11-01

    The many desirable characteristics of technetium-99m have stimulated the development of labeling techniques for different molecular and cellular structures. It is accepted that a variety of factors such the drug chemotherapy can alter the biodistribution of radiopharmaceuticals. The unknowledge of these factor may result in an unexpected behavior of the radiopharmaceuticals. Since patients on chemotherapeutic treatment can be submitted to a nuclear medicine procedure, we have studied in mice, the effect of mitomycin-C on the {sup 99m} Tc-DMSA used for kidney scintigraphy. Mitomycin-C is an antineoplastic agent obtained from Streptomyces caesptosus. The metabolism of this drug produces different toxic and inactive metabolites. Mitomycin-C 0.15 mg was administered in Balb/c female with an interval of 72 hours. After one hour of the last dose, 0.3 ml of 9{sup 9m}c-DMSA (7.4 MBq) were injected and after 0.5 h the animals were sacrificed. The organs were isolated and counted in a well counter. The percentage of radioactivity (%ATI) were calculated and statistical analysis were performed (Wilcoxon Test). The results have shown that the %ATI: has increased in stomach and uterus, has decreased in kidney and ovary; has not altered in pancreas, spleen, lung, heart, liver, thymus, thyroid, bone and brain. The increase of % ATI could be justified by the metabolic process or the therapeutical effect of mitomycin-C. As an effect of this drug is observed in the uptake of the {sup 99m} Tc-DMSA by the kidney, probably an alteration in the kidney scintigraphy is expected. However, the increase of %ATI of this radiopharmaceutical in other organs by the mitomycin-C could be evaluated carefully. (author) 12 ref., 2 tabs.

  18. Treating Chronic Tension-type Headache Not Responding to Amitriptyline Hydrochloride With Paroxetine Hydrochloride: A Pilot Evaluation

    Science.gov (United States)

    Holroyd, Kenneth A.; Labus, Jennifer S.; O'Donnell, Francis J.; Cordingley, Gary E.

    2007-01-01

    Context In some individuals, chronic tension-type headache fails to respond to tricyclic antidepressant medications that often serve as first-line therapy. Objective To evaluate the clinical efficacy of paroxetine hydrochloride for chronic tension-type headache not responding to amitriptyline hydrochloride. Design and Setting Open-label trial of paroxetine conducted at 2 outpatient sites in Ohio. Participants and Intervention Thirty-one adults (mean age, 37 years; 20 women) with chronic tension-type headache (mean, 25 headache days per month) who had failed to respond (less than 30% improvement) to treatment with either amitriptyline (n = 13) or matched placebo (n = 18). All participants were treated with paroxetine (up to 40 mg per day) in a 9-month protocol. Outcome Measures Monthly headache index calculated as the mean of pain ratings (0 to 10 scale) recorded by participants in a diary 4 times per day, number of days per month with at least moderate pain (pain rating of 5 or greater), and analgesic medication use. Results In patients who had not responded to amitriptyline, paroxetine failed to reduce chronic tension-type headaches or analgesic medication use. In patients who had not responded to placebo, paroxetine produced modest reductions in chronic tension-type headaches and analgesic use. Conclusions We found no evidence that chronic tension-type headaches that failed to respond to tricyclic antidepressant therapy with amitriptyline improved when subsequently treated with paroxetine. More support was found for the efficacy of paroxetine in patients with chronic tension-type headaches who had failed to respond to placebo. PMID:14511278

  19. Preclinical Evaluation of Promitil, a Radiation-Responsive Liposomal Formulation of Mitomycin C Prodrug, in Chemoradiotherapy

    Energy Technology Data Exchange (ETDEWEB)

    Tian, Xi; Warner, Samuel B.; Wagner, Kyle T.; Caster, Joseph M. [Laboratory of Nano- and Translational Medicine, Department of Radiation Oncology, Lineberger Comprehensive Cancer Center, Carolina Center for Cancer Nanotechnology Excellence, Carolina Institute of Nanomedicine, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina (United States); Zhang, Tian [Division of Medical Oncology, Department of Medicine, Duke Cancer Institute, Duke University Medical Center, Durham, North Carolina (United States); Ohana, Patricia [Lipomedix Pharmaceuticals, Jerusalem (Israel); Gabizon, Alberto A. [Lipomedix Pharmaceuticals, Jerusalem (Israel); Shaare Zedek Medical Center, Jerusalem (Israel); Wang, Andrew Z., E-mail: zawang@med.unc.edu [Laboratory of Nano- and Translational Medicine, Department of Radiation Oncology, Lineberger Comprehensive Cancer Center, Carolina Center for Cancer Nanotechnology Excellence, Carolina Institute of Nanomedicine, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina (United States)

    2016-11-01

    Purpose: To examine the effect of radiation on in vitro drug activation and release of Promitil, a pegylated liposomal formulation of a mitomycin C (MMC) lipid-based prodrug; and examine the efficacy and toxicity of Promitil with concurrent radiation in colorectal cancer models. Methods and Materials: Promitil was obtained from Lipomedix Pharmaceuticals (Jerusalem, Israel). We tested the effects of radiation on release of active MMC from Promitil in vitro. We next examined the radiosensitization effect of Promitil in vitro. We further evaluated the toxicity of a single injection of free MMC or Promitil when combined with radiation by assessing the effects on blood counts and in-field skin and hair toxicity. Finally, we compared the efficacy of MMC and Promitil in chemoradiotherapy using mouse xenograft models. Results: Mitomycin C was activated and released from Promitil in a controlled-release profile, and the rate of release was significantly increased in medium from previously irradiated cells. Both Promitil and MMC potently radiosensitized HT-29 cells in vitro. Toxicity of MMC (8.4 mg/kg) was substantially greater than with equivalent doses of Promitil (30 mg/kg). Mice treated with human-equivalent doses of MMC (3.3 mg/kg) experienced comparable levels of toxicity as Promitil-treated mice at 30 mg/kg. Promitil improved the antitumor efficacy of 5-fluorouracil–based chemoradiotherapy in mouse xenograft models of colorectal cancer, while equitoxic doses of MMC did not. Conclusions: We demonstrated that Promitil is an attractive agent for chemoradiotherapy because it demonstrates a radiation-triggered release of active drug. We further demonstrated that Promitil is a well-tolerated and potent radiosensitizer at doses not achievable with free MMC. These results support clinical investigations using Promitil in chemoradiotherapy.

  20. Subconjunctival bevacizumab to augment trabeculectomy with mitomycin C in the management of failed glaucoma surgery

    Directory of Open Access Journals (Sweden)

    Saeed AM

    2014-09-01

    Full Text Available Ahmed M Saeed, Tarek Tawfeek AboulNasrOphthalmology Department, Benha University, Egypt Purpose: To provide a feasible solution to the problem of failed glaucoma surgery. The aim was to evaluate the efficacy and safety of the additional effects of a combined surgical approach. This approach augments the application of trabeculectomy with mitomycin C (MMC by adding subconjunctival bevacizumab injection. The results were compared with those of trabeculectomy with only adjunctive MMC. Methods: A randomized controlled prospective clinical trial included 28 eyes diagnosed with failed scarred bleb of a previous trabeculectomy. The eyes were divided into two equal groups: combined group A, “trabeculectomy with adjunctive MMC and subconjunctival bevacizumab,” and control group B, “trabeculectomy with adjunctive MMC only.” The main outcome results included the cumulative probability of surgical success, intraocular pressure (IOP values, and number of IOP-lowering medications needed to achieve the target IOP.Results: Group A achieved a cumulative probability of complete success of 0.769 and of qualified success of 0.231 at the end of the 24 month study period; group B achieved cumulative probabilities of 0.538 and 0.308, respectively. Group A achieved a lower mean IOP value than group B, with fewer antiglaucoma drugs at all postoperative visits, but this lower value did not reach a statistically significant level (P>0.05. There was no statistically significant difference between both groups regarding best corrected visual acuity, visual field parameters, operative and/or postoperative complications, and additional interventions. No significant adverse effects were caused by this combined approach.Conclusion: Bevacizumab was not found to add much to the favorable long-term outcome of conventional trabeculectomy with MMC as a solution to the problem of scarred failed bleb. Keywords: glaucoma, bevacizumab, mitomycin C, failed trabeculectomy

  1. Pharmacokinetic study of benfotiamine and the bioavailability assessment compared to thiamine hydrochloride.

    Science.gov (United States)

    Xie, Feifan; Cheng, Zeneng; Li, Sanwang; Liu, Xingling; Guo, Xin; Yu, Peng; Gu, Zhenkun

    2014-06-01

    Benfotiamine is a lipid-soluble thiamine precursor which can transform to thiamine in vivo and subsequently be metabolized to thiamine monophosphate (TMP) and thiamine diphosphate (TDP). This study investigated the pharmacokinetic profiles of thiamine and its phosphorylated metabolites after single- and multiple-dose administration of benfotiamine in healthy Chinese volunteers, and assessed the bioavailability of orally benfotiamine administration compared to thiamine hydrochloride. In addition, concentration of hippuric acid in urine which is produced in the transformation process of benfotiamine was determined. The results showed that thiamine and its phosphorylated metabolites exhibited different pharmacokinetic characteristics in plasma, blood and erythrocyte, and one-compartment model provided the best fit for pharmacokinetic profiles of thiamine. The transformation process of benfotiamine to thiamine produced large amount of hippuric acid. No accumulation of hippuric acid was observed after multiple-dose of benfotiamine. Compared to thiamine hydrochloride, the bioavailability of thiamine in plasma and TDP in erythrocyte after oral administration of benfotiamine were 1147.3 ± 490.3% and 195.8 ± 33.8%, respectively. The absorption rate and extent of benfotiamine systemic availability of thiamine were significantly increased indicating higher bioavailability of thiamine from oral dose of benfotiamine compared to oral dose of thiamine hydrochloride. © 2014, The American College of Clinical Pharmacology.

  2. Collagen matrix compared with mitomycin C for treatment of primary open-angle glaucoma with trabeculectomy performed

    Directory of Open Access Journals (Sweden)

    Lei Yu

    2017-09-01

    Full Text Available AIM:To evaluate the effectiveness and safety between trabeculectomy with collagen matrix versus trabeculectomy with mitomycin C(MMCfor patients with primary open-angle glaucoma(POAG.METHODS: In this prospective randomized comparative study from January 2015 to December 2016. Thirty-two eyes presented with POAG were included in this study, 14 eyes treated by trabeculectomy with subconjunctival implant of collagen matrix(study groupand the other 18 eyes treated by trabeculectomy with mitomycin C. Postoperative IOP, the success rate of operation, number of postoperative glaucoma medications and postoperative complications were recorded. Each patient was followed up at least 6mo. RESULTS: The mean postoperative IOP was statistically different between the study group and the control group after 1d(PP>0.05, and the mean postoperative IOP was statistically different between the two groups(PP>0.05. The IOP decreased at 1d after openations compared with before, kept stable at 1wk to 6mo. IOP of study group was lowen than control. IOP was controlled by glaucoma medications in the study group by 28% compared to control group by 33% at 6mo after operation, but there was no significant difference. There was no significant difference between the study group and the control group in complications(PCONCLUSION: Trabeculectomy with collagen matrix implant is comparable to the use of MMC with a similar success rate in open-angle glaucoma and the range in reducing intraocular pressure was significantly higher than that of MMC and it can significantly avoid the occurrence of low IOP postoperatively, transient anterior chamber, conjunctival wound leakage complications has no advantages compared with the use of MMC.

  3. Intra-arterial mitomycin C treatment of unresectable liver tumours

    International Nuclear Information System (INIS)

    Starkhammar, H.; Haakansson, L.; Morales, O.; Svedberg, J.; Linkoeping Univ.; Linkoeping Univ.

    1987-01-01

    Regional chemotherapy might be more efficient if the cytostatic drug is injected together with degradable starch microspheres (DSM), which induce temporary blockage of arterioles and trap the co-injected drug in tumour. Eighteen patients with non-resectable liver cancer were included. Mitomycin C (15 mg/m 2 ) was injected intra-arterially mixed with 900 mg of DSM every six weeks. For estimation of the effect of DSM in the liver a radiolabelled tracer was injected via the same route. Its passage through the liver to the systemic circulation was continuously measured by a detector situated over peripheral blood vessels. The effect of DSM on the tracer passage varied considerably between different patients. The study also indicated opening of new vascular pathways some minutes after the initial injection. The dose of DSM for total blockage of the arterial blood flow, indicated by angiography, also varied. In some patients 540 mg induced total occlusion. In others neither angiographic nor tracer passage were affected by the microspheres although 900 mg (or even more) were injected. Factors such as size of the vascular bed, portal and arterial blood flow and arterio-venous shunting seemed to be of great importance and should be controlled in order to optimize the use of DSM in conjunction with chemotherapy of liver tumours. (orig.)

  4. Determination of methadone hydrochloride in a maintenance dosage formulation.

    Science.gov (United States)

    Hoffmann, T J; Thompson, R D

    1975-07-01

    A colorimetric method for direct quantitative assay of methadone hydrochloride in liquid oral dosage forms is presented. The procedure involves the formation of a dye complex with bromothymol blue buffer solution. The resultant complex is extracted with benzene and measured spectrophotometrically. Duplicate tests on the formulation showed 99.2% of the labeled amount of methadone.

  5. Clinical Observation of Icotinib Hydrochloride in First-line Therapy 
for Pulmonary Adenocarcinoma

    Directory of Open Access Journals (Sweden)

    Xinjie YANG

    2013-07-01

    Full Text Available Background and objective It has been proven that icotinib hydrochloride, as a molecule targeted drug, can be safely and efficiently used to treat advanced non-small cell lung cancer (NSCLC for second-line or third-line. This research was aimed to investigate the efficacy and toxicity of icotinib hydrochloride as the first-line therapy for pulmonary adenocarcinoma. Results Among the 56 patients, the tumor objective response rate (ORR and disease control rate (DCR was 46.4% (26/56 and 78.6% (46/56, respectively. Among the 20 patients with EGFR analyses, 18 patients were positive for a mutation, ORR was 66.7% (12/18, DCR was 94.4% (17/18 respectively. The ORR with no history of smoke. EGFR positive mutation and appearance of rash were significantly higher than those with smoker, wild type EGFR, no information about EGFR and no appearance of rash (P<0.05. The most common drug-related adverse events were mild skin rash (28.5% and diarrhea (12%. Conclusion Single agent treatment with icotinib hydrochloride is effective and tolerable in first-line therapy for pulmonary adenocarcinoma, especially with EGFR mutation.

  6. Polymeric composite membranes for temperature and pH-responsive delivery of doxorubicin hydrochloride

    Directory of Open Access Journals (Sweden)

    Sahar Mohamaddoust Aliabadi

    2015-07-01

    Full Text Available Objective(s: Nowadays hydrogels are one of the upcoming classes of polymer-based controlled-release drug delivery systems. Temperature and pH-responsive delivery systems have drawn much attention because some diseases reveal themselves by a change in temperature and/or pH. The objective of this work is to prepare and characterize composite membrane using responsive nanoparticles into a polymer matrix. Materials and Methods: These nanoparticles were made of the copolymer poly (N-isopropylacrylamide-co-methaçrylic acid by an aqueous dispersion polymerization process and are responsible for dual sensitivity to temperature and pH. Morphology study with SEM, swelling behavior with Dynamic Light Scattering Technique, in vitro drug release behavior with side-by-side Diffusion Cells were also investigated in this paper. Doxorubicin hydrochloride was used as a model solute. Results:The study on the release of doxorubicin hydrochloride showed that the release rate was higher at pH 5 than pH 7.4, increased with the increase of temperature. Nevertheless, ionic strength only poses a minor direct effect at higher pH. Conclusion:Such system may be potentially used as a tumor-targeting doxorubicin hydrochloride delivery in the body.

  7. Stability of midazolam hydrochloride injection 1-mg/mL solutions in polyvinyl chloride and polyolefin bags.

    Science.gov (United States)

    Karlage, Kelly; Earhart, Zachary; Green-Boesen, Kelly; Myrdal, Paul B

    2011-08-15

    The stability of midazolam hydrochloride injection 1-mg/mL solutions in polyvinyl chloride (PVC) and polyolefin bags under varying conditions was evaluated. Triplicate solutions of midazolam hydrochloride 1-mg/mL were prepared in polyolefin and PVC i.v. bags by diluting midazolam hydrochloride injection 5 mg/mL with 5% dextrose injection. Bags were then stored under refrigeration (3-4 °C), exposed to light at room temperature (20-25 °C), or protected from light in amber bags at room temperature. Samples were taken immediately after preparation (day 0) and on days 1, 2, 3, 6, 13, 20, and 27 for analysis with a stability-indicating high-performance liquid chromatography assay in order to determine solution concentration. Stability was defined as retention of at least 90% of the initial drug concentration. The pH of each solution was also measured weekly. Sterility of the i.v. bags was determined at the end of the study by microbiological testing with culture in growth media. Differences in concentrations under the various storage conditions and bags used were analyzed using analysis of variance. All solutions retained over 98% of the initial midazolam hydrochloride concentration, with no statistically significant (p ≥ 0.05) change in concentration over the four-week period. Stability was not affected by temperature, exposure to light, or bag type. The pH of all solutions remained between 3.2 and 3.4 throughout the study. Sterility after 28 days was retained. Midazolam hydrochloride 1-mg/mL solutions diluted in 5% dextrose injection remained stable over 27 days in both polyolefin and PVC i.v. bags, regardless of storage condition.

  8. In vitro and in silico investigation of electrospun terbinafine hydrochloride-loaded buccal nanofibrous sheets.

    Science.gov (United States)

    Szabó, Péter; Daróczi, Tünde Beáta; Tóth, Gergő; Zelkó, Romána

    2016-11-30

    Terbinafine hydrochloride-loaded nanofibrous buccal films were formulated with the aim to improve the solubility and dissolution behavior; thus, the local effectiveness of the antifungal agent. Poly(vinyl alcohol) and chitosan polymer composites were selected as delivery base in order to enhance the mucoadhesion of the fibrous films. The dissolution of terbinafine hydrochloride was carried out applying a stainless steel disc assembly and the terbinafine concentration was determined by HPLC-MS in selective ion monitoring mode. The prediction of the absorption behavior of the prepared fibrous samples in the human oral cavity was modeled using GastroPlus™ software. The result indicates that the fibrous films enabled fast and complete dissolution of the active agent. The drug absorption from the oral cavity could be minimized by the employment of the proper oral transit model. Because of the limited absorption of terbinafine hydrochloride from the oral mucosa the formulation can be beneficial in local administration in the case of hold and expectorate administration mode. Copyright © 2016 Elsevier B.V. All rights reserved.

  9. Formulation, Development and Evaluation of delayed release capsules of Duloxetine Hydrochloride made of different Enteric Polymers

    OpenAIRE

    Pallavi Yerramsetty; J. Vijaya Ratna; Venkata Ramana Reddy; Praveen Kumar

    2012-01-01

    Delayed release systems have acquired a centre stage in the arena of pharmaceutical research and development. The present study involves formulation and evaluation of Duloxetine Hydrochloride delayed release capsules. Duloxetine Hydrochloride is an acid labile drug. It degrades in the acidic environment of the stomach thus leading to therapeutic inefficacy. Therefore it is necessary to bypass the acidic pH of the stomach which can be achieved by formulating delayed release dosage form by usin...

  10. Simultaneous Integrated Boost–Intensity Modulated Radiation Therapy With Concomitant Capecitabine and Mitomycin C for Locally Advanced Anal Carcinoma: A Phase 1 Study

    Energy Technology Data Exchange (ETDEWEB)

    Deenen, Maarten J. [Division of Clinical Pharmacology, Department of Medical Oncology, The Netherlands Cancer Institute, Amsterdam (Netherlands); Dewit, Luc [Department of Radiotherapy, The Netherlands Cancer Institute, Amsterdam (Netherlands); Boot, Henk [Division of Gastroenterology and Hepatology, Department of Medical Oncology, The Netherlands Cancer Institute, Amsterdam (Netherlands); Beijnen, Jos H. [Department of Pharmacy and Pharmacology, Slotervaart Hospital, Amsterdam (Netherlands); Faculty of Science, Department of Pharmaceutical Sciences, Division of Pharmaco-epidemiology and Clinical Pharmacology, Utrecht University, Utrecht (Netherlands); Schellens, Jan H.M. [Division of Clinical Pharmacology, Department of Medical Oncology, The Netherlands Cancer Institute, Amsterdam (Netherlands); Faculty of Science, Department of Pharmaceutical Sciences, Division of Pharmaco-epidemiology and Clinical Pharmacology, Utrecht University, Utrecht (Netherlands); Cats, Annemieke, E-mail: a.cats@nki.nl [Division of Gastroenterology and Hepatology, Department of Medical Oncology, The Netherlands Cancer Institute, Amsterdam (Netherlands)

    2013-04-01

    Purpose: Newer radiation techniques, and the application of continuous 5-FU exposure during radiation therapy using oral capecitabine may improve the treatment of anal cancer. This phase 1, dose-finding study assessed the feasibility and efficacy of simultaneous integrated boost–intensity modulated radiation therapy (SIB-IMRT) with concomitant capecitabine and mitomycin C in locally advanced anal cancer, including pharmacokinetic and pharmacogenetic analyses. Methods and Materials: Patients with locally advanced anal carcinoma were treated with SIB-IMRT in 33 daily fractions of 1.8 Gy to the primary tumor and macroscopically involved lymph nodes and 33 fractions of 1.5 Gy electively to the bilateral iliac and inguinal lymph node areas. Patients received a sequential radiation boost dose of 3 × 1.8 Gy on macroscopic residual tumor if this was still present in week 5 of treatment. Mitomycin C 10 mg/m{sup 2} (maximum 15 mg) was administered intravenously on day 1, and capecitabine was given orally in a dose-escalated fashion (500-825 mg/m{sup 2} b.i.d.) on irradiation days, until dose-limiting toxicity emerged in ≥2 of maximally 6 patients. An additional 8 patients were treated at the maximum tolerated dose (MTD). Results: A total of 18 patients were included. The MTD of capecitabine was determined to be 825 mg/m{sup 2} b.i.d. The predominant acute grade ≥3 toxicities included radiation dermatitis (50%), fatigue (22%), and pain (6%). Fifteen patients (83% [95%-CI: 66%-101%]) achieved a complete response, and 3 (17%) patients a partial response. With a median follow-up of 28 months, none of the complete responders, and 2 partial responders had relapsed. Conclusions: SIB-IMRT with concomitant single dose mitomycin C and capecitabine 825 mg/m{sup 2} b.i.d. on irradiation days resulted in an acceptable safety profile, and proved to be a tolerable and effective treatment regimen for locally advanced anal cancer.

  11. Simultaneous Integrated Boost–Intensity Modulated Radiation Therapy With Concomitant Capecitabine and Mitomycin C for Locally Advanced Anal Carcinoma: A Phase 1 Study

    International Nuclear Information System (INIS)

    Deenen, Maarten J.; Dewit, Luc; Boot, Henk; Beijnen, Jos H.; Schellens, Jan H.M.; Cats, Annemieke

    2013-01-01

    Purpose: Newer radiation techniques, and the application of continuous 5-FU exposure during radiation therapy using oral capecitabine may improve the treatment of anal cancer. This phase 1, dose-finding study assessed the feasibility and efficacy of simultaneous integrated boost–intensity modulated radiation therapy (SIB-IMRT) with concomitant capecitabine and mitomycin C in locally advanced anal cancer, including pharmacokinetic and pharmacogenetic analyses. Methods and Materials: Patients with locally advanced anal carcinoma were treated with SIB-IMRT in 33 daily fractions of 1.8 Gy to the primary tumor and macroscopically involved lymph nodes and 33 fractions of 1.5 Gy electively to the bilateral iliac and inguinal lymph node areas. Patients received a sequential radiation boost dose of 3 × 1.8 Gy on macroscopic residual tumor if this was still present in week 5 of treatment. Mitomycin C 10 mg/m 2 (maximum 15 mg) was administered intravenously on day 1, and capecitabine was given orally in a dose-escalated fashion (500-825 mg/m 2 b.i.d.) on irradiation days, until dose-limiting toxicity emerged in ≥2 of maximally 6 patients. An additional 8 patients were treated at the maximum tolerated dose (MTD). Results: A total of 18 patients were included. The MTD of capecitabine was determined to be 825 mg/m 2 b.i.d. The predominant acute grade ≥3 toxicities included radiation dermatitis (50%), fatigue (22%), and pain (6%). Fifteen patients (83% [95%-CI: 66%-101%]) achieved a complete response, and 3 (17%) patients a partial response. With a median follow-up of 28 months, none of the complete responders, and 2 partial responders had relapsed. Conclusions: SIB-IMRT with concomitant single dose mitomycin C and capecitabine 825 mg/m 2 b.i.d. on irradiation days resulted in an acceptable safety profile, and proved to be a tolerable and effective treatment regimen for locally advanced anal cancer

  12. Interactive effect of dietary protein level and zilpaterol hydrochloride ...

    African Journals Online (AJOL)

    Bonsmara type steers were used to determine the effect of dietary zilpaterol hydrochloride (ZH) in combination with different dietary crude protein (CP) levels (100, 120 and 140 g CP/kg) on growth performance and meat quality. Treatment groups (T) consisted of 12 steers each. T1 – 100 g CP/kg + 0.15 mg ZH/kg live weight ...

  13. Partial Tenon's capsule resection with adjunctive mitomycin C in Ahmed glaucoma valve implant surgery.

    Science.gov (United States)

    Susanna, R

    2003-08-01

    To verify if partial intraoperative Tenon's capsule resection (PTCR) with adjunctive mitomycin C is effective in developing thin, avascular blebs in eyes undergoing Ahmed glaucoma valve insertion, and to assess the efficacy and safety of this procedure. A multicentre, prospective, alternating case assignment, investigator unmasked, parallel group, comparative interventional study was conducted in four Latin American countries (Argentina, Brazil, Colombia, and Peru). Ahmed glaucoma valve implant insertion with PTCR (group A) and without PCTR (group B) was performed in neovascular glaucomatous eyes without previous surgery. Adjunctive mitomycin C (MMC) was used in both groups. Patients were examined 1 day, 10 days, 1 month, 2 months, 3 months, 6 months, and 1 year following the surgery. Intraocular pressure (IOP) and the appearance of the bleb were evaluated at each examination. Appearance of the bleb was classified at both the 1 month mark and last examinations into one of three groups: flat and vascularised; elevated avascular; or elevated and not avascular. 92 eyes from 92 patients were included in the study. The preoperative mean IOP was 50.0 (SD 10.5) mm Hg in group A and 48.4 (11.7) in group B (p>0.05). Statistically significant IOP reductions were observed at all periods of follow up. 12 months after surgery, the mean IOP was 17.2 (5.0) mm Hg in group A and 18.3 (8.7) mm Hg in group B (p>0.05). A hypertensive phase occurred in 40.0% in group A and in 46.8% in group B (p>0.05). At the 1 month and the final follow up, the blebs in all eyes were considered elevated and not avascular. The success rate (IOP0.05). Overall, 74.2% of the patients achieved an IOP glaucoma, PCTR with MMC augmentation showed no additional benefits or complications over MMC augmentation alone; no avascular bleb was obtained with this technique. The incidence of a hypertensive phase was lower than reported in previous studies.

  14. Trabeculectomy with double low dose of mitomycin C – two years of follow-up

    Directory of Open Access Journals (Sweden)

    Errico D

    2011-12-01

    Full Text Available Donato Errico1, Francesca Scrimieri1, Roberta Riccardi1, Romolo Fedeli1, Giancarlo Iarossi21Opthalmology Unit, Glaucoma Service, Azienda Ospedaliera, Cardinale G Panìco, Tricase (Le, Italy; 2Department of Opthalmology, Ospedale Pediatrico Bambino Gesù, Rome, ItalyPurpose: To evaluate the efficacy and the safety of a surgical technique in which classic trabeculectomy ab externo is performed with a double application of low-dose mitomycin C (MMC in uncontrolled open-angle glaucoma (OAG patients.Method: A consecutive series of 43 white patients (43 eyes with uncontrolled primary OAG underwent trabeculectomy surgery. A double application of MMC (0.1% was performed: the first under the Tenon's capsule for 3 minutes, and the second below the scleral flap for 1 or 2 minutes, according to the risk factors. Complete success was defined as intraocular pressure (IOP <14 mmHg without any additional glaucoma surgery or medication. Qualified success was defined as IOP <14 mmHg with additional needling revision.Results: Mean preoperative IOP was 29.9 mmHg (SD 3.8 for all eyes evaluated. At 1 day postoperative, mean IOP was 6.7 mmHg (SD 1.26. At the end of the first 2 weeks postoperative, mean IOP was 8.6 mmHg (SD 1.7, at 12 months mean IOP was 11.3 mmHg (SD 1.4; P < 0.0001 and at 24 months mean IOP was 11.4 mmHg (SD 1.5; P < 0.0001. At 3 months, two eyes (5.4% underwent needling of the bleb for cystic blebs formation.Conclusion: In this study we presented the results after 2 years of follow-up of OAG undergoing trabeculectomy with dual administration of MMC (0.1 mg/mL. After 24 months, complete success was achieved in 93% of patients and a qualified success in 100% of patients.Keywords: glaucoma, trabeculectomy, mitomycin C

  15. Comparison of the efficacy among multiple chemotherapeutic interventions combined with radiation therapy for patients with cervix cancer after surgery: A network meta-analysis.

    Science.gov (United States)

    Chang, Lei; Guo, Ruixia

    2017-07-25

    Cervix cancer was the second most common cancer in female. However, there was no network meta-analysis (NMA) comparing the efficacy of the multiple chemotherapeutic interventions combined with radiation therapy in patients after operation. Randomized controlled trials were retrieved from PubMed, Embase and Cochrane Library. Overall survival (OS), recurrence-free survival (RFS), incidence of recurrence and distant metastasis were the main outcomes, particularly 5-year OS and PFS were considered as primary outcomes. Furthermore, the hazard ratio (HR) or odds ratio (OR) and their 95% credible intervals (CrIs) were extracted. The surface under cumulative ranking curve (SUCRA) was also used in this NMA. A total of 39 eligible trials with 8,952 patients were included and 22 common chemotherapies were evaluated in this meta-analysis. For OS, cisplatin+fluorouracil+hydroxyurea, fluorouracil+mitomycin C, cisplatin and cisplatin+fluorouracil were better than placebo. As for RFS, cisplatin+fluorouracil, fluorouracil+mitomycin C, and cisplatin alone had the significant superiority compared with placebo. In terms of incidence of recurrence, the optimal drug combination was cisplatin+ifosfamide (0.93) based on SUCRA. Moreover, epirubicin (OR = 0.28, 95% CrI: 0.08-0.91) was the only one had the distinguished potency in reducing the occurrence of distant metastasis with a SUCRA rank probability of 0.88. We recommended cisplatin+fluorouracil+hydroxyurea and cisplatin+docetaxel for their good efficacy in long term survival. Meanwhile, the combination of multiple drugs with different mechanisms worked better.

  16. Quantitative estimation of itopride hydrochloride and rabeprazole sodium from capsule formulation.

    Science.gov (United States)

    Pillai, S; Singhvi, I

    2008-09-01

    Two simple, accurate, economical and reproducible UV spectrophotometric methods and one HPLC method for simultaneous estimation of two component drug mixture of itopride hydrochloride and rabeprazole sodium from combined capsule dosage form have been developed. First developed method involves formation and solving of simultaneous equations using 265.2 nm and 290.8 nm as two wavelengths. Second method is based on two wavelength calculation, wavelengths selected for estimation of itopride hydrochloride was 278.0 nm and 298.8 nm and for rabeprazole sodium 253.6 nm and 275.2 nm. Developed HPLC method is a reverse phase chromatographic method using phenomenex C(18) column and acetonitrile: phosphate buffer (35:65 v/v) pH 7.0 as mobile phase. All developed methods obey Beer's law in concentration range employed for respective methods. Results of analysis were validated statistically and by recovery studies.

  17. [The use of natural and synthetic hydrophilic polymers in the formulation of metformin hydrochloride tablets with different profile release].

    Science.gov (United States)

    Kołodziejczyk, Michał Krzysztof; Kołodziejska, Justyna; Zgoda, Marian Mikołaj

    2012-01-01

    Metformin hydrochloride after buformin and phenformin belongs to the group of biguanid derivatives used as oral anti-diabetic drugs. The object of the study is the technological analysis and the potential effect of biodegradable macromolecular polymers on the technological and therapeutic parameters of oral anti-diabetic medicinal products with metformin hydrochloride: Siofor, Formetic, Glucophage, Metformax in doses of 500mg and 1000mg and Glucophage XR in a dose of 500 mg of modified release. Market therapeutic products containing 500 and 1000 mg of metformin hydrochloride in a normal formulation and 500 mg of metformin hydrochloride in a formulation of modified release were analyzed. Following research methods were used: technological analysis of tablets, study of disintegration time of tablets, evaluation of pharmaceutical availability of metformin hydrochloride from tested therapeutic products, mathematical and kinetic analysis of release profiles of metformin hydrochloride, statistical analysis of mean differences of release coefficients. The percentage of excipients in the XR formulation is higher and constitutes 50.5% of a tablet mass. However, in standard formulations the percentage is lower, between 5.5% and 12.76%. On the basis of the results of disintegration time studies, the analysed therapeutic products can be divided into two groups, regardless the dose. The first one are preparations with faster (not fast!) disintegration: Glucophage i Metformax. The second group are preparations with slower disintegration, more balanced in the aspect of a high dose of the biologically active substance: Formetic and Siofor. Products with a lower content of excipients (Metformax, Glucophage) disintegrate in a faster way. The disintegration rate of the products with a higher content of excipients (Formetic, Siofor) is slower. The appearance of metformin hydrochloride concentration in the gastrointestinal contents, balanced in time, caused by a slower disintegration

  18. Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Proguanil Hydrochloride.

    NARCIS (Netherlands)

    Plöger, Gerlinde F; Abrahamsson, Bertil; Cristofoletti, Rodrigo; Groot, D I R K W; Langguth, Peter; Mehta, Mehul U; Parr, Alan; Polli, James E; Shah, Vinod P; Tajiri, Tomokazu; Dressman, Jennifer B

    2018-01-01

    Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To clarify the Biopharmaceutics Classification System (BCS) classification, experimental solubility and

  19. Combination chemotherapy versus single-agent therapy as first- and second-line treatment in metastatic breast cancer

    DEFF Research Database (Denmark)

    Joensuu, H; Holli, K; Heikkinen, M

    1998-01-01

    PURPOSE: We report results of a randomized prospective study that compared single agents of low toxicity given both as the first-line and second-line chemotherapy with combination chemotherapy in advanced breast cancer with distant metastases. PATIENTS AND METHODS: Patients in the single-agent arm...... (n = 153) received weekly epirubicin (E) 20 mg/m2 until progression or until the cumulative dose of 1,000 mg/m2, followed by mitomycin (M) 8 mg/m2 every 4 weeks, and those in the combination chemotherapy arm (n = 150) were first given cyclophosphamide 500 mg/m2, E 60 mg/m2, and fluorouracil 500 mg/m2...... younger than 50. RESULTS: An objective response (complete [CR] or partial [PR]) was obtained in 55%, 48%, 16%, and 7% of patients treated with CEF, E, M, and MV, respectively. A response to CEF tended to last longer than a response to E (median, 12 v 10.5 months; P = .07). Treatment-related toxicity...

  20. Nanosized complexation assemblies housed inside reverse micelles churn out monocytic delivery cores for bendamustine hydrochloride.

    Science.gov (United States)

    Singh, Yuvraj; Chandrashekhar, Anumandla; Meher, Jaya Gopal; Durga Rao Viswanadham, K K; Pawar, Vivek K; Raval, Kavit; Sharma, Komal; Singh, Pankaj K; Kumar, Animesh; Chourasia, Manish K

    2017-04-01

    We explore a plausible method of targeting bendamustine hydrochloride (BM) to circulatory monocytes by exploiting their intrinsic endocytic/phagocytic capability. We do so by complexation of sodium alginate and chitosan inside dioctyl sulfo succinate sodium (AOT) reverse micelles to form bendamustine hydrochloride loaded nanoparticles (CANPs). Dynamic light scattering, electrophoretic mobility and UV spectroscopy were used to detail intra-micellar complexation dynamics and to prove that drug was co-captured during interaction of carbohydrate polymers. A fluorescent conjugate of drug (RBM) was used to trace its intracellular fate after its loading into nanoparticles. CANPs were sized below 150nm, had 75% drug entrapment and negative zeta potential (-30mV). Confocal microscopy demonstrated that developed chitosan alginate nanoparticles had the unique capability to carry BM specifically to its site of action. Quantitative and mechanism based cell uptake studies revealed that monocytes had voracious capacity to internalize CANPs via simultaneous scavenger receptor based endocytic and phagocytic mechanism. Comparative in vitro pharmacokinetic studies revealed obtainment of significantly greater intracellular drug levels when cells were treated with CANPs. This caused reduction in IC 50 (22.5±2.1μg/mL), enhancement in G 2 M cell cycle arrest, greater intracellular reactive oxygen species generation, and increased apopotic potential of bendamustine hydrochloride in THP-1 cells. Selective monocytic targeting of bendamustine hydrochloride using carbohydrate constructs can prove advantageous in case of leukemic disorders displaying overabundance of such cells. Copyright © 2017 Elsevier B.V. All rights reserved.

  1. Study on the interaction of tropisetron hydrochloride and L-tryptophan by spectrofluorimetry and its analytical application

    International Nuclear Information System (INIS)

    Zhu Xiashi; Gong Aiqin; Wang Baosheng; Yu Suhai

    2008-01-01

    A new method to determine tropisetron hydrochloride with L-tryptophan in the medium with pH=9.0 was studied, which is based on the fluorescence quenching effect of tropisetron hydrochloride on L-tryptophan. The fluorescence quenching mechanism and various factors influencing fluorescence quenching were discussed. Under the optimum conditions, the linear range and detection limit were 0.03-12.0 and 0.01 μg/mL (correlation coefficient r=0.9970), respectively. The calibration curve equation was ΔF=6.17+12.56 C (μg/mL). RSD was 3.4% (c=4.0 μg/mL, n=5); the detection limit estimated (S/N=3) was 0.01 μg/mL. The proposed method had been successfully applied to determine tropisetron hydrochloride in real samples and the obtained results were in good agreement with the results of the official method

  2. Controlled delivery of ropinirole hydrochloride through skin using modulated iontophoresis and microneedles.

    Science.gov (United States)

    Singh, Neha D; Banga, Ajay K

    2013-05-01

    The objective of this study was to investigate the effect of modulated current application using iontophoresis- and microneedle-mediated delivery on transdermal permeation of ropinirole hydrochloride. AdminPatch® microneedles and microchannels formed by them were characterized by scanning electron microscopy, dye staining and confocal microscopy. In vitro permeation studies were carried out using Franz diffusion cells, and skin extraction was used to quantify drug in underlying skin. Effect of microneedle pore density and ions in donor formulation was studied. Active enhancement techniques, continuous iontophoresis (74.13 ± 2.20 µg/cm(2)) and microneedles (66.97 ± 10.39 µg/cm(2)), significantly increased the permeation of drug with respect to passive delivery (8.25 ± 2.41 µg/cm(2)). Modulated iontophoresis could control the amount of drug delivered at a given time point with the highest flux being 5.12 ± 1.70 µg/cm(2)/h (5-7 h) and 5.99 ± 0.81 µg/cm(2)/h (20-22 h). Combination of modulated iontophoresis and microneedles (46.50 ± 6.46 µg/cm(2)) showed significantly higher delivery of ropinirole hydrochloride compared to modulated iontophoresis alone (84.91 ± 9.21 µg/cm(2)). Modulated iontophoresis can help in maintaining precise control over ropinirole hydrochloride delivery for dose titration in Parkinson's disease therapy and deliver therapeutic amounts over a suitable patch area and time.

  3. [Clinical effect of atomoxetine hydrochloride in 66 children with narcolepsy].

    Science.gov (United States)

    Zhang, Shen; Ding, Changhong; Wu, Husheng; Fang, Fang; Wang, Xiaohui; Ren, Xiaotun

    2015-10-01

    To observe the efficacy and safety of atomoxetine hydrochloride in children with narcolepsy. Totally 66 patients with narcolepsy who were conformed international classification of sleep disturbances (ICSD-2) diagnostic criteria treated with atomoxetine hydrochloride seen from November 2010 to December 2014 were enrolled into this study, 42 of them were male and 24 female, mean age of onset was 7.5 years (3.75-13.00 years), mean duration before diagnosis was 1.75 years (0.25-5.00 years). Complete blood count, liver and kidney function, multiple sleep latency test (MSLT), polysomnography (PGS), neuroimaging and electroencephalography (EEG) were performed for each patient. For some of the children HLA-DR2 gene and serum markers of infection were tested. The 66 cases were followed up from 2 to 49 months (average 18 months) to observe the clinical efficacy and adverse reactions. In 62 cases excessive daytime sleepiness was improved, in 11 cases (16.7%) it was controlled (16.7%), in 29 cases (43.9%) the treatment was obviously effective and in 22 (33.3%) it was effective; cataplexy occurred in 54 cases, in 18 (33.3%) it was controlled, in 19 (35.2%) the treatment was obviously effective and in 10 (18.5%) effective; night sleep disorders existed in 55 cases, in 47 cases it was improved, in 14 (25.5%) it was controlled, in 20 (36.4%) the treatment was obviously effective and in 13 (23.6%) effective; hypnagogic or hypnopompic hallucination was present in 13 cases, in only 4 these symptoms were controlled. Sleep paralysis existed in 4 cases, it was controlled in only 1 case. In 18 cases attention and learning efficiency improved.Anorexia occurred in 18 cases, mood disorder in 5 cases, depression in 2 cases, nocturia, muscle tremors, involuntary tongue movement each occurred in 1 case. P-R interval prolongation and atrial premature contraction were found in 1 case. Atomoxetine hydrochloride showed good effects in patients with narcolepsy on excessive daytime sleepiness

  4. Thermodynamic characteristics of the acid dissociation of dopamine hydrochloride in water-ethanol solutions

    Science.gov (United States)

    Ledenkov, S. F.; Vandyshev, V. N.; Molchanov, A. S.

    2012-06-01

    Enthalpies of the interaction of protonated dopamine with a hydroxide ion in water-ethanol mixtures in the concentration range of 0-0.8 EtOH mole fractions are measured calorimetrically. The neutralization process of dopamine hydrochloride is shown to occur endothermally in solvents with an ethanol concentration of ≥0.5 mole fractions. Standard thermodynamic characteristics (Δr H ○, Δr G ○, and Δr S ○) of the first-step acid dissociation of dopamine hydrochloride in solutions are calculated with regard to the autoprotolysis enthalpy of binary solvents. It is found that dissociation enthalpies vary within 9.1-64.8 kJ/mol, depending on the water-ethanol solvent composition.

  5. Pharmaceutical development of an intravenous dosage form of diacetylmorphine hydrochloride

    NARCIS (Netherlands)

    Klous, Marjolein G.; Nuijen, Bastiaan; van den Brink, Wim; van Ree, Jan M.; Beijnen, Jos H.

    2004-01-01

    A solid dosage form for multiple use was developed for parenteral administration of diacetylmorphine in a clinical trial on co-prescription of heroin to heroin addicts. A 300-mg/mL diacetylmorphine hydrochloride solution was lyophilised as 10-mL aliquots in 30-mL glass vials, to be reconstituted to

  6. Enantiospecific synthesis of (1- sup 3 H)-(+)-pseudoephedrine hydrochloride

    Energy Technology Data Exchange (ETDEWEB)

    Hill, J.A.; Scharver, J.D. (Burroughs Wellcome Co., Research Triangle Park, North Carolina (USA). Chemical Development Labs.)

    1990-06-01

    The naturally occurring dextrorotary enantiomer (+)-pseudoephedrine was synthesized in the ({sup 3}H)-labelled form with specific activity 17.5 Ci/mmol suitable for development of a radioimmunoassay procedure. The chirally specific route from L-alanine to (1-{sup 3}H)-d-pseudoephedrine hydrochloride was based on the use of {alpha}-amino acids as chiral educts for asymmetric products. (author).

  7. Stability-Indicating Validated HPLC Method for Analysis of Berberine Hydrochloride and Trimethoprim in Pharmaceutical Dosage Form

    Directory of Open Access Journals (Sweden)

    Jing-Chun Wang

    2013-01-01

    Full Text Available A stability-indicating HPLC method was developed and validated for the determination of berberine hydrochloride and trimethoprim in pharmaceutical dosage form in the presence of degradation products. The proposed RP-HPLC method utilizes an Agilent TC-C18, 4.6 mm × 250 mm, 5 μm, column using a mobile phase consisting of acetonitrile-50 mM potassium dihydrogen phosphate (30 : 70, v/v, pH adjusted to 3 with orthophosphoric acid at a flow rate of 1.0 mL/min and UV detection at 271 nm. The linearity of berberine hydrochloride and trimethoprim was in the range of 2 to 60 μg/mL (r=0.9996 and 1 to 30 μg/mL (r=0.9995, respectively. Repeatability and intermediate precisions were also determined with percentage relative standard deviation (% RSD less than 2.0%. The limits of detection were found to be 9.8 ng/mL for berberine hydrochloride and 2.5 ng/mL for trimethoprim. The mean recoveries for berberine hydrochloride and trimethoprim were 99.8 and 98.8%, respectively. The stability of the two drugs was determined under different conditions and the proposed method has shown effective separation for their degradation products. And the proposed assays method can thus be considered stability-indicating.

  8. The influence of stachydrine hydrochloride on the reperfusion model of mice with repetitive cerebral ischemia

    Directory of Open Access Journals (Sweden)

    Mingsan Miao

    2017-03-01

    Full Text Available To study the influence of stachydrine hydrochloride on the inflammatory cytokines and tissue morphology of the re-perfusion model of mice with repetitive cerebral ischemia and probe into the protection mechanism of stachydrine hydrochloride for cerebral ischemia reperfusion impairment. Build a repetitive cerebral ischemia reperfusion model by first blocking the common carotid artery on both sides for 10 min, then resuming perfusion for 10 min and then blocking the common carotid artery on both sides again for 10 min. Before the operation, all the mice in the Nimodipine group, and the big, medium and small stachydrine hydrochloride dose groups were given corresponding gastric perfusion, the mice in the sham operation group and the modeled groups were at the same time given 0.5% sodium carboxymethyl cellulose for gastric perfusion of the same volume. The medicine was fed daily for 7 consecutive days. The model was built 1 h after the last feed and the perfusion continued for 24 h after the operation. Then the death rate of the mice was calculated. The mouse brains were taken out to test the ICAM-1 level and the TNF-α level, and the serum was taken out to test the NSE level and the MPO level. The tissue morphology changes were also observed. All the repetitive cerebral ischemia reperfusion models were successfully duplicated. The stachydrine hydrochloride in all the dose groups significantly reduced the death rates of big and small mice, reduced the level of ICAM-1 and the level of TNF-α in the brain tissues and the NSE level and the MPO level in the serum, significantly alleviating the pathological impairment in the hippocampus. Stachydrine hydrochloride can significantly reduce the death rate of mice, improve the pathological changes in the hippocampus, inhibit inflammatory reactions after ischemia, thus reducing the re-perfusion impairment after cerebral ischemia.

  9. Efficacy of Icotinib Hydrochloride in the Treatment of Advanced Non-small Cell Lung Cancer

    Directory of Open Access Journals (Sweden)

    Xianglei Ma

    2013-09-01

    Full Text Available Objective: To observe and evaluate the efficacy and adverse responses of icotinib hydrochloride in the treatment of advanced non-small cell lung cancer (NSCLC, and analyze the relative factors impacting its efficacy and prognosis. Methods: The clinical data of 260 patients with advanced NSCLC treated with icotinib hydrochloride in Jiangsu Cancer Hospital was retrospectively analyzed. Results: Four weeks after initial administration, 256 patients were evaluable for efficacy except 4 who withdrew the drug due to intolerable adverse responses. Among the 256 patients, there were 0 complete response (CR, 96 partial response (PR, 37.5%, 97 stable disease (SD, 37.9% and 63 progression disease (PD, 24.6%, with the objective remission rate (ORR and disease control rate (DCR being 37.6% and 75.4% respectively. However, in all patients, the median progression-free survival (PFS was 7 (0.4 - 16.3 months, and were 11 (1 - 16.3, 6 (0.4 - 11.3 and 5 (1 - 13.5 months in those treated with first-line, second-line, and ≥third-line treatments, respectively. Conclusion: Icotinib hydrochloride has significant efficiency and better safety for treating advanced NSCLC.

  10. 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.

  11. Effect of hydroxylamine hydrochloride on the floral decoration of zinc oxide synthesized by solution method

    International Nuclear Information System (INIS)

    Wahab, Rizwan; Ansari, S.G.; Kim, Young Soon; Khang, Gilson; Shin, Hyung-Shik

    2008-01-01

    Effect of the structure-directing agent on the floral (depicting flower) morphological variation of ZnO is systematically studied and presented here. Flowery decorated (resembling flower) zinc oxide structure composed of hexagonal nanorods (sharp tips and wider bases) was synthesized at 90 deg. C using zinc acetate dihydrate and sodium hydroxide at various concentrations of hydroxylamine hydrochloride for 12 h by solution method. Single crystalline nature with the wurtzite hexagonal phase remained unaltered with increasing concentration of hydroxylamine hydrochloride while the morphology changes from nanorod to plate like structure. Photoelectron spectroscopic measurement presented spectra close to the standard bulk ZnO, with an O 1s peak composed of surface adsorbed O-H group, O 2- in the oxygen vacancies on ZnO structure and ZnO. At higher concentration (0.8 M), surface adsorbed O-H group increases while other component decreases because of the changes in the nucleation and surface energy. Results clearly indicate that hydroxylamine hydrochloride works as a structure-directing agent without affecting other properties

  12. Development and validation of a dissolution test for diltiazem hydrochloride in immediate release capsules

    Directory of Open Access Journals (Sweden)

    Taciane Ferreira Mendonça

    2011-01-01

    Full Text Available This work describes the development and validation of a dissolution test for 60 mg of diltiazem hydrochloride in immediate release capsules. The best dissolution in vitro profile was achieved using potassium phosphate buffer at pH 6.8 as the dissolution medium and paddle as the apparatus at 50 rpm. The drug concentrations in the dissolution media were determined by UV spectrophotometry and HPLC and a statistical analysis revealed that there were significant differences between HPLC and spectrophotometry. This study illustrates the importance of an official method for the dissolution test, since there is no official monograph for diltiazem hydrochloride in capsules.

  13. [The determination of pyridoxine hydrochloride (vitamin B6) according to European Pharmacopoeia 4.0].

    Science.gov (United States)

    Kos, N; Surmann, J P

    2006-05-01

    Determination of pyridoxine hydrochloride according to the European Pharmacopoeia 4.0 In the Ph.Eur. 4.0 assay pyridoxine hydrochloride is titrated by sodium hydroxide 0.1 mol x 1(-1) in ethanolic solution. The impossibility of a correct evaluation of the titration curve is shown both in theory and practice. The new method in Ph.Eur. 4.04 is an acidimetric titration of the base chloride. In a mixture of formic acid/acetic anhydride the titration is made by perchloric acid. Because some critical points in this assay an alternative method is developed. This method is robust and should give results with high accuracy.

  14. Polymeric matrix membrane sensors for stability-indicating potentiometric determination of oxybutynin hydrochloride and flavoxate hydrochloride urogenital system drugs.

    Science.gov (United States)

    Heba, Mohamed; Ramadan, Nesrin; El-Laithy, Moustafa

    2008-01-01

    Four polyvinyl chloride (PVC) matrix membrane electrodes responsive to 2 drugs affecting the urogenital system--oxybutynin hydrochloride (OX) and flavoxate hydrochloride (FX)--were developed, described, and characterized. A precipitation-based technique with tungstophosphate (TP) and ammonium reineckate (R) anions as electroactive materials in a PVC matrix with an OX cation was used for electrode 1 and 2 fabrication, respectively. Electrode 3 and 4 fabrication was based on use of the precipitation technique of FX cation with tetrakis (4-chlorophenyl) borate and R anions as electroactive materials. Fast and stable Nernstian responses in the range 1 x 10(-2)-1 x 10(-6) M for the 2 drugs over the pH range 5-8 revealed the performance characteristics of these electrodes, which were evaluated according to International Union of Pure and Applied Chemistry recommendations. The method was applied to FX and OX in their pharmaceutical formulations and in human plasma samples. The 4 proposed sensors were found to be specific for the drugs in the presence of up to 60% of their degradation products. Validation of the method according to the quality assurance standards showed suitability of the proposed electrodes for use in the quality control assessment of these drugs. The recoveries for determination of the drugs by the 4 proposed selective electrodes were 99.5 +/- 0.5, 100.0 +/- 0.4, 99.9 +/- 0.4, and 100.1 +/- 0.4% for sensors 1-4, respectively. Statistical comparison between the results obtained by this method and the official method of the drugs was done, and no significant difference found.

  15. Comparison on Anticoagulation and Antiplatelet Aggregation Effects of Puerarin with Heparin Sodium and Tirofiban Hydrochloride: An In Vitro Study.

    Science.gov (United States)

    Li, Si-Wei; Feng, Xue; Xu, Hao; Chen, Ke-Ji

    2018-02-01

    To detect the anticoagulation and antiplatelet effects of different concentrations of puerarin, heparin sodium and tirofiban hydrochloride on the blood samples of healthy volunteers by Sonoclot coagulation and platelet function analyzer. Peripheral blood samples were extracted from 20 healthy volunteers, followed by adding different concentrations of puerarin, heparin sodium and tirofiban hydrochloride. Samples were detected for activated clotting time (ACT), clot rate (CR) and platelet function (PF) by Sonoclot coagulation and platelet function analyzer instrument. For puerarin and heparin sodium, the values of ACT gradually increased, and the values of CR and PF gradually decreased with increasing in drug concentration. There was a linear (or log linear) relationship between ACT, CR, PF value and drug concentration (Phydrochloride, the values of ACT and CR had no significant changes, while PF values gradually decreased with concentration increasing. There was also a linear relationship between PF values and concentrations of tirofiban hydrochloride (Psodium. For high concentrations of puerarin (e.g. 3.8 mg/600 μL) and tirofiban hydrochloride (e.g. 0.8 μg/600 μL), PF values had no significant difference. However, PF values for high puerarin concentration had a larger variance. Puerarin has similar anticoagulant and antiplatelet effects with the heparin sodium, and may have a lower hemorrhage risk than heparin sodium when obtained the same anticoagulation effect in the concentration range of this experiment. In addition, for high concentration, puerarin had the same antiplatelet function as tirofiban hydrochloride but with a larger individual variability.

  16. Chemoreactomic analysis of thiamine disulfide, thiamine hydrochloride, and benfotiamine molecules

    Directory of Open Access Journals (Sweden)

    O. A. Gromova

    2017-01-01

    Full Text Available Objective: to analyze the interactions that could indicate the potential pharmacological properties of the molecules of thiamin, thiamine disulfide, and others.Material and methods. The investigators simulated the properties of thiamine disulfide (bistiamin versus those of the reference molecules of thiamin hydrochloride and benfotiamine. The study was performed using chemoreactomic simulation that is the newest area in post-genome pharmacology.Results and discussion. Chemoreactomic analysis has shown that thiamine disulfide can inhibit the molecular receptors involved in blood pressure regulation: adrenoceptors, vasopressin receptor, and angiotensin receptor. Thiamine disulfide can inhibit the reuptake of serotonin, increase its levels, inhibit benzodiazepine receptor and dopamine reuptake, and enhance neuronal acetylcholine release to a large extent than benfotiamine. These molecular effects are consistent with the sedative and anticonvulsant action profile of thiamine disulfide. Simulation has indicated that thiamine disulfide has neuroprotective, anti-inflammatory, normolipidemic, and antitumor activities.Conclusion. The simulation results are confirmed by the available clinical and experimental findings and indicate the virtually unstudied molecular mechanisms of action of thiamine disulfide, benfotiamine, and thiamin hydrochloride

  17. Transepithelial transport of biperiden hydrochloride in Caco-2 cell monolayers.

    Science.gov (United States)

    Abalos, Ivana S; Rodríguez, Yanina I; Lozano, Verónica; Cereseto, Marina; Mussini, Maria V; Spinetto, Marta E; Chiale, Carlos; Pesce, Guido

    2012-09-01

    The aim of this research has been to determine the biperiden hydrochloride permeability in Caco-2 model, in order to classify it based on the Biopharmaceutics Classification System (BCS). The World Health Organization (WHO) as well as many other authors have provisionally assigned the drug as BCS class I (high solubility-high permeability) or III (high solubility-low permeability), based on different methods. We determined biperiden BCS class by comparing its permeability to 5 pre-defined compounds: atenolol and ranitidine hydrochloride (low permeability group) and metoprolol tartrate, sodium naproxen and theophylline (high permeability group). Since biperiden permeability was higher than those obtained for high permeability drugs, we classified it as a BCS class I compound. On the other hand, as no differences were obtained for permeability values when apical to basolateral and basolateral to apical fluxes were studied, this drug cannot act as a substrate of efflux transporters. As a consequence of our results, we suggest that the widely used antiparkinsonian drug, biperiden, should be candidate for a waiver of in vivo bioequivalence studies. Copyright © 2012 Elsevier B.V. All rights reserved.

  18. Use of 8.4% Sodium Bicarbonate in Buffering Commonly Administered Vancomycin Hydrochloride Solutions for Use with Midline or Peripheral Line Catheters.

    Science.gov (United States)

    Puertos, Enrique; Spencer, Melissa

    2015-01-01

    The primary objective of this study was to evaluate the use of 8.4% sodium bicarbonate in the buffering of commonly administered vancomycin hydrochloride solutions for use with midline or peripheral line catheters. Nine admixtures of vancomycin hydrochloride were aseptically prepared for this study. Vancomycin hydrochloride solutions were prepared in triplicates in the following strengths, 1 gram, 2 grams, and 3 grams, which were added to 250-mL bags of sodium chloride 0.9% injection (with overfill). To each prepared solution of vancomycin hydrochloride, 0.5 mL of 8.4% sodium bicarbonate was added. The pH was measured to obtain a baseline level. At day 9, the pH of each sample was measured and compared to those at baseline. The osmolality of each sample was also measured. There was no statistical difference in the pH at baseline and at day 9 (α = 0.05, P = 0.347). A solution of vancomycin hydrochloride that is compounded in 250 mL of sodium chloride 0.9% injection (including overfill) and buffered with 0.5 mL of 8.4% sodium bicarbonate maintained a pH in the range of 5 to 9 and an osmolality in the range of 150 mOsm/kg to 500 mOsm/kg.

  19. Extended Stability of Epinephrine Hydrochloride Injection in Polyvinyl Chloride Bags Stored in Amber Ultraviolet Light-Blocking Bags.

    Science.gov (United States)

    Van Matre, Edward T; Ho, Kang C; Lyda, Clark; Fullmer, Beth A; Oldland, Alan R; Kiser, Tyree H

    2017-09-01

    Objective: The objective of this study was to evaluate the stability of epinephrine hydrochloride in 0.9% sodium chloride in polyvinyl chloride bags for up to 60 days. Methods: Dilutions of epinephrine hydrochloride to concentrations of 16 and 64 µg/mL were performed under aseptic conditions. The bags were then placed into ultraviolet light-blocking bags and stored at room temperature (23°C-25°C) or under refrigeration (3°C-5°C). Three samples of each preparation and storage environment were analyzed on days 0, 30, 45, and 60. Physical stability was performed by visual examination. The pH was assessed at baseline and upon final degradation evaluation. Sterility of the samples was not assessed. Chemical stability of epinephrine hydrochloride was evaluated using high-performance liquid chromatography. To determine the stability-indicating nature of the assay, degradation 12 months following preparation was evaluated. Samples were considered stable if there was less than 10% degradation of the initial concentration. Results: Epinephrine hydrochloride diluted to 16 and 64 µg/mL with 0.9% sodium chloride injection and stored in amber ultraviolet light-blocking bags was physically stable throughout the study. No precipitation was observed. At days 30 and 45, all bags had less than 10% degradation. At day 60, all refrigerated bags had less than 10% degradation. Overall, the mean concentration of all measurements demonstrated less than 10% degradation at 60 days at room temperature and under refrigeration. Conclusion: Epinephrine hydrochloride diluted to 16 and 64 µg/mL with 0.9% sodium chloride injection in polyvinyl chloride bags stored in amber ultraviolet light-blocking bags was stable up to 45 days at room temperature and up to 60 days under refrigeration.

  20. Investigation of ability of serum albumin to bind the tritium labeled drotaverine hydrochloride at virus hepatitis

    International Nuclear Information System (INIS)

    Kim, A.A.; Mavlyanov, I.R.; Shukurov, B.V.; Djuraeva, G.T.

    2005-01-01

    The most of pathological conditions, and especially liver pathologies, proceeds on the background of intoxication syndromes. One of universal mechanisms of reaction of an organism on increase of concentration of toxic metabolites is removing of metabolites with the help of one of the basic protein of blood plasma - serum albumin. The purpose of the present research was studying of serum albumin ability to bind drotaverine hydrochloride at virus hepatitis in dynamics of traditional therapy. This parameter is rather important for therapy as it is known, that serum albumin is a carrier of pharmaceutical preparations. At intoxication of organism the toxic metabolites can reduce the binding capacity of serum albumin due to competitive binding and by that to reduce efficiency of carry of pharmaceutical preparations. Application of a radiochemical method with use of tritium labeled drotaverine hydrochloride in the given research it is represented to the most effective. The method of tritium labeling of pharmacological preparation of drotaverine hydrochloride was developed. Drotaverine hydrochloride was labeled by thermally activated tritium. The system of purification of tritium labeled drotaverine hydrochloride by thin layer chromatography (TLC) has been developed. Tritium labeled preparation of drotaverine hydrochloride was purified by TLC on silica gel in system isopropanol : ammonia : water (8:1:1). The output of purified tritium labeled preparation of drotaverine hydrochloride was about 25 %. The received preparation had specific radioactivity - 3,2 MBq/mg (37,4 mCi/mmol), radiochemical purity of a preparation was 95 %. We had been developed a micromethod of definition of binding ability of albumin, allowing analyze 20 microliters of blood serum. The method consists in incubation of tritium labeled drotaverine hydrochloride with blood serum in vitro, the following fractionation of serum proteins by gel - filtration on a microcolumn with Sephadex G-25, and direct

  1. Thermal stability study of crystalline and novel spray-dried amorphous nilotinib hydrochloride

    NARCIS (Netherlands)

    Herbrink, Maikel; Vromans, Herman; Schellens, Jan Hm; Beijnen, Jos H; Nuijen, Bastiaan

    2018-01-01

    The thermal characteristics and the thermal degradation of crystalline and amorphous nilotinib hydrochloride (NH) were studied. The spray drying technique was successfully utilized for the amorphization of NH and was evaluated by spectroscopic techniques and differential scanning calorimetry (DSC).

  2. [Correlation of single-cell gel electrophoresis and mitomycin C-induced chromosomal breakage for chromosomal instabiligy in children with Fanconi anemia].

    Science.gov (United States)

    Zhang, Li; Liu, Qiang; Zou, Yao; Liu, Xiao-ming; Zhang, Jia-yuan; Wang, Shu-chun; Chen, Xiao-juan; Guo, Ye; Yang, Wen-yu; Ruan, Min; Liu, Tian-feng; Liu, Fang; Cai, Xiao-jin; Chen, Yu-mei; Zhu, Xiao-fan

    2013-02-01

    Fanconi anemia (FA) is characterized by bone marrow failure, congenital abnormalities and predisposition to neoplasia. Hypersensitivity of FA cells to the clastogenic effect of mitomycin C (MMC) provides a unique marker for the diagnosis before the beginning of hematological manifestations. The aim of this study was to evaluate the relationship between Single-Cell Gel Electrophoresis (SCGE) and mitomycin C-induced chromosomal breakage in children with FA. Between January 2007 and June 2011, 248 children (results of the two methods and compared with each other. The receiver operating characteristic (ROC) curve was used to evaluate the parameters in SCGE. Seventeen patients were diagnosed as FA and 231 as non-FA. Chromosomal breakage was found to be significantly higher in FA patients [(32.2 ± 4.8)%] than non-FA [(19.9 ± 3.0)%] and controls[(21.6 ± 4.8)%] when induced by MMC 80 ng/ml. The parameters of SCGE were significantly different between FA patients and non-FA or controls. All the parameters were rectilinearly correlated with MMC (P = 0.000). The most closely correlated parameter was the rate of comet cell (r = 0.848, P = 0.000). The results of ROC curves suggested the comet cell rate (0.999) was more important. SCGE might be used to discriminate between FA and non-FA individuals. The relationship between SCGE and MMC-induced chromosomal breakage was significant. The rate of comet cell was the important parameter.

  3. Resultados refractivos en pacientes operados por LASIK versus LASEK con mitomicina C Refractive results in patients operated by LASIK versus LASEK with Mitomycin C

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    Abel Cabrera Martínez

    2009-06-01

    Full Text Available OBJETIVO: Evaluar comparativamente los resultados refractivos obtenidos en ojos operados con el uso de la keratomileusis in situ asistida con láser (LASIK contra la keratomileusis subepitelial asistida con láser combinándosele a esta última el uso de la mitomicina C (LASEK+MC. MÉTODOS: Se realizó un estudio prospectivo, experimental, comparativo en un total de 210 ojos de pacientes que acudieron a consulta para ser operados por algún defecto refractivo. Un total de 104 ojos fueron intervenidos por LASIK y 106 por LASEK+MC. Para comparar los resultados del estudio se realizaron varios exámenes antes y después de operados los pacientes. RESULTADOS: Los defectos refractivos fueron superiores con significación estadística (pOBJECTIVE: Evaluating comparatively the refractive results obtained in eyes operated by keratomileusis in situ assisted with laser (LASIK versus keratomileusis subepithelial assisted with laser plus Mitomycin C (LASEK + MC. METHODS: A prospective, experimental and comparative study was performed in 210 eyes of patients who went to see the specialist to be operated from some refractive defect. A total of 104 eyes were operated by LASIK and 106 by LASEK + MC. In order to compare the results of study, several tests were made before and after surgery. RESULTS: The refractive defects were greater with statistical significance (p< 0,05, for Student's t for the eyes operated by LASEK + MC. The visual result of the LASEK with MC surgery was better than that of LASIK. Haze was a problem resolved for the LASEK when included Mitomycin C in patients with high myopia, in addition to improvement of quality of life of the patients. CONCLUSIONS: The corneal surgery with laser through the LASEK technique plus use of Mitomycin C demonstrated being as reliable as that with LASIK for ametropy correction, since it provides additional advantages that increases the quality of life of patient, with less postoperative risks.

  4. 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.

  5. Study of the β-Cyclodextrin Imipramine Hydrochloride Inclusion Complex and Determination of its Stability Constant (K by UV-Visible Spectroscopy

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    Alamdar Ashnagar

    2007-01-01

    Full Text Available In this research, the interactions of imipramine hydrochloride drug with β- cyclodextrin and the stability constant (K of the inclusion complex formed between them were investigated by using UV-visible spectroscopy. Solutions consisting of a known and constant amount of imipramine hydrochloride and varying amounts of β- cyclodextrin were prepared in 0.1 M phosphate buffer (pH 7.4. The final solutions had cyclodextrin concentrations between 0.0011 and 0.0153 M. UV-visible spectra of each solution was taken at λmax= 250 nm. The absorbances at this wavelength were recorded and plotted against cyclodextrin concentrations. From the graph, the concentrations of free and bound imipramine hydrochloride and free β-cyclodextrin were calculated using the Beer-Lambert law. From these data, the stability constant was calculated and a value of K=52.26±11.41 mol-1L was obtained. The magnitude of the stability constant is discussed in terms of the relative sizes and the chemical natures of β-cyclodextrin and imipramine hydrochloride.

  6. Prophylactic Effects of Mitomycin-C on Regression and Haze Formation in Photorefractive Keratectomy

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    Hassan Hashemi

    2008-12-01

    Full Text Available

    PURPOSE: To study the effect of prophylactic application of mitomycin-C on regression and corneal haze formation after photorefractive keratectomy (PRK for high myopia. METHODS: Fifty-four eyes of 28 high myopic patients were enrolled in this prospective study. All eyes underwent PRK with application of 0.02% mitomycin-C for two minutes and irrigation with 15-20 ml of normal saline. Follow-up visits were scheduled for the first 7 days and 1, 3 and 6 months after surgery. Hanna grading (in the scale of 0 to 4+ was used to assess corneal haze. RESULTS: Mean spherical equivalent refraction (SE was -7.08 ± 1.11 diopters (D, preoperatively. All eyes were examined on the first 7 days and one month after surgery; 48 eyes (88.9% were evaluated 3 and 6 months post-surgery. Six months after surgery, all eyes had uncorrected visual acuity (UCVA of 20/40 or better and 37 eyes (77.1 % achieved UCVA of 20/20 or better, 45 eyes (93.7% had SE within ±1.00D of emmetropia. One month postoperatively, 2 eyes (3.7% had grade 0.5 haze, while at 3 and 6 months after surgery no visited eye had haze at all. There was no decrease in best corrected visual acuity after 6 months. In spatial frequencies of 6 and 12 cycle/degree, contrast sensitivity decreased immediately after PRK but increased to the preoperative values by the 6th postoperative month

  7. 78 FR 66263 - New Animal Drugs; Afoxolaner; Carprofen; Ceftiofur Hydrochloride; Monensin

    Science.gov (United States)

    2013-11-05

    ... DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and Drug Administration 21 CFR Parts 510, 520, 522, and 558 [Docket No. FDA-2013-N-0002] New Animal Drugs; Afoxolaner; Carprofen; Ceftiofur Hydrochloride... transferred ownership of, and all rights and interest in, ANADA 200-555 for LIBREVIA (carprofen) Soft Chewable...

  8. 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.

  9. Sensitivity to mitomycin-C and radiation of cells derived from patients with familial colon polyposis: an autosomal dominant hereditary disease

    International Nuclear Information System (INIS)

    Ban, Sadayuki; Iida, Shozo; Tamura, Taizo.

    1984-04-01

    This study was undertaken to investigate the sensitivity to mitomycin-C (MMC) of skin fibroblasts derived from patients with adenomatosis coli (AC), especially familial colon polyposis. The sensitivity to X rays and ultraviolet rays of AC cells cultured at RERF was similar to that of normal human diploid cells. However, there were large individual differences in sensitivity to MMC. DNA elongation in cells sensitive to MMC was found to be inhibited after MMC treatment. Sites highly sensitive to MMC were considered to be involved in the initial stages of DNA synthesis. (author)

  10. Application of mitomycin C after endoscopic lysis of congenital laryngeal web combined with epiglottic hypoplasia in a middle-aged man.

    Science.gov (United States)

    Roh, Jong-Lyel

    2006-04-01

    Laryngeal webs and epiglottic hypoplasias are uncommon congenital anomalies. Anterior glottic web combined with epiglottic hypoplasia was found in a middle-aged man presenting with hoarseness and dyspnea on exertion. This can be considered as a unique isolated defect of the larynx during early fetal development. The laryngeal web can be successfully treated in a single stage with endoscopic lysis and topical application of mitomycin C for prevention of anterior glottic restenosis. This case and prior reports suggest that the novel approach may be effective in the treatment of laryngeal webs.

  11. HER-2, p53, p21 and hormonal receptors proteins expression as predictive factors of response and prognosis in locally advanced breast cancer treated with neoadjuvant docetaxel plus epirubicin combination

    International Nuclear Information System (INIS)

    Tiezzi, Daniel G; Andrade, Jurandyr M; Ribeiro-Silva, Alfredo; Zola, Fábio E; Marana, Heitor RC; Tiezzi, Marcelo G

    2007-01-01

    Neoadjuvant chemotherapy has been considered the standard care in locally advanced breast cancer. However, about 20% of the patients do not benefit from this clinical treatment and, predictive factors of response were not defined yet. This study was designed to evaluate the importance of biological markers to predict response and prognosis in stage II and III breast cancer patients treated with taxane and anthracycline combination as neoadjuvant setting. Sixty patients received preoperative docetaxel (75 mg/m 2 ) in combination with epirubicin (50 mg/m 2 ) in i.v. infusion in D1 every 3 weeks after incisional biopsy. They received adjuvant chemotherapy with CMF or FEC, attaining axillary status following definitive breast surgery. Clinical and pathologic response rates were measured after preoperative therapy. We evaluated the response rate to neoadjuvant chemotherapy and the prognostic significance of clinicopathological and immunohistochemical parameters (ER, PR, p51, p21 and HER-2 protein expression). The median patient age was 50.5 years with a median follow up time 48 months after the time of diagnosis. Preoperative treatment achieved clinical response in 76.6% of patients and complete pathologic response in 5%. The clinical, pathological and immunohistochemical parameters were not able to predict response to therapy and, only HER2 protein overexpression was associated with a decrease in disease free and overall survival (P = 0.0007 and P = 0.003) as shown by multivariate analysis. Immunohistochemical phenotypes were not able to predict response to neoadjuvant chemotherapy. Clinical response is inversely correlated with a risk of death in patients submitted to neoadjuvant chemotherapy and HER2 overexpression is the major prognostic factor in stage II and III breast cancer patients treated with a neoadjuvant docetaxel and epirubicin combination

  12. Compatibility and Stability of VARUBI (Rolapitant) Injectable Emulsion Admixed with Intravenous Granisetron Hydrochloride.

    Science.gov (United States)

    Wu, George; Powers, Dan; Yeung, Stanley; Chen, Frank; Neelon, Kelly

    2018-01-01

    Prophylaxis or therapy with a combination of a neurokinin 1 (NK-1) receptor antagonist (RA), a 5-hydroxytryptamine- 3 (5-HT3) RA, and dexamethasone is recommended by international antiemesis guidelines for the prevention of chemotherapy-induced nausea and vomiting for patients receiving highly emetogenic chemotherapy and for select patients receiving moderately emetogenic chemotherapy. VARUBI (rolapitant) is a substance P/NK-1 RA that was recently approved by the U.S. Food and Drug Administration as an injectable emulsion in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. Granisetron Hydrochloride Injection USP is one of the 5-HT3 RAs indicated for the prevention of nausea and/or vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin. Herein, we describe the physical and chemical compatibility and stability of VARUBI (rolapitant) injectable emulsion (166.5 mg/92.5 mL [1.8 mg/mL], equivalent to 185 mg of rolapitant hydrochloride) admixed with Granisetron Hydrochloride Injection USP (1.0 mg/mL, equivalent to 1.12 mg/mL hydrochloride). Binary admixtures of VARUBI injectable emulsion and Granisetron Hydrochloride Injection USP were prepared and stored in VARUBI ready-to-use glass vials and in four types of commonly used intravenous administration (tubing) sets. Evaluation of the physical and chemical compatibility and stability of the admixtures in the VARUBI ready-to-use vials stored at room temperature (20°C to 25°C) under fluorescent light and under refrigeration (2°C to 8°C protected from light) was conducted at 0, 1, 6, 24, and 48 hours, and that of the admixtures in the intravenous tubing sets was evaluated at 0, 2, and 6 hours of storage at 20°C to 25°C. Physical stability was evaluated by visual examination

  13. The effect of mitomycin-c in keloid fibroblast cultures

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    Ishandono Dachlan

    2016-12-01

    Full Text Available ABSTRACT Keloid occurs due to hyperactivity of keloid fibroblast (KF in proliferation, migration, collagen deposition, together with low rates of collagen degradation. These are under the responsibility of TGF-b. Mitomycin C (MC is used for treating keloid by a topical application during surgery at the level of 0.02% to 0.08%. Unfortunately, the lowest effective level of MC for keloid has not been determined yet. We aimed to determine the lowest effective level of MC in the suppression of KF activities. Various levels of MC diluted in growth medium were administered on KF that were isolated from six patients. After 24 hours and 72 hours of incubation, cellular proliferation, collagen deposition, cellular migration and level of TGF-b, were analyzed. Application of 120 uM MC on KF culture for 24 hours could significantly reduce TGF-b production from 1265.74 ± 274.81 pg/mL to 265.17 ± 12.20 pg/mL; proliferation index from 100% to 84.01 ± 12.91%; inhibit cellular migration to 64.38 ± 3.66%; but reduce collagen depositions from 100% to only 91.13 ± 10.19%. The lowest MC level is on 30 uM or equal with 0.001%. In conclusion, the lowest level of MC can suppress the activities of KF is 0.001%. Moreover, due to low activity in inhibiting collagen deposition, MC would be better as an adjuvant drug for keloid surgery.

  14. The efficacy of cetirizine hydrochloride on the pruritus of cats with atopic dermatitis: a randomized, double-blind, placebo-controlled, crossover study.

    Science.gov (United States)

    Wildermuth, Kerstin; Zabel, Sonja; Rosychuk, Rod A W

    2013-12-01

    Various antihistamines have been used in the management of feline atopic dermatitis, with variable reported benefit. To date, there have been no randomized, double-blind, placebo-controlled, crossover clinical trials on the use of this drug class in cats. To evaluate the clinical efficacy of cetirizine hydrochloride for the control of pruritus and dermatitis in cats diagnosed with atopic dermatitis. In this randomized, double-blind, placebo-controlled crossover clinical trial, 21 client-owned cats diagnosed with mild to moderate nonseasonal atopic dermatitis were randomly assigned to two groups. Cats in each group received either 1 mg/kg cetirizine hydrochloride or placebo once daily per os for 28 days followed by a 14 day wash-out period. Treatments were then crossed over, and cats received placebo or cetirizine hydrochloride for another 28 days. Owners marked a pruritus severity scale before inclusion in the study and weekly throughout the entire study period. Lesions were scored by the clinician using a Canine Atopic Dermatitis Extent and Severity Index (CADESI)-03 modified for the cat before enrolment and at day 28 of each treatment. Nineteen cats completed the study. There were no statistically significant differences between treatment with cetirizine hydrochloride and placebo for modified CADESI-03 or pruritus scores. This study suggests that cetirizine hydrochloride cannot be recommended for the management of feline atopic dermatitis. © 2013 ESVD and ACVD.

  15. Semiquantitative regional cerebral blood flow evaluation by the sup 123 I-IMP SPECT before and during medication of bifemelane hydrochloride in patients with cerebrovascular diseases

    Energy Technology Data Exchange (ETDEWEB)

    Tsuda, Yoshiyasu; Ayada, Yoshihide; Kitadai, Masaya; Tanabe, Masatada; Matsuo, Hirohide (Kagawa Medical School, Miki (Japan))

    1992-04-01

    Regional cerebral blood flow (rCBF) by {sup 123}I-IMP SPECT was measured before and 2.8, 10.3 months during medication of bifemelane hydrochloride in 10 patients with cerebrovascular diseases and compared with 5 control patients without medication. Semiquantitative rCBF indices of asymmetry and redistribution (AI, RI) were calculated from mean regional counts/pixel of each region of interest (ROI) in the early and delayed images of IMP SPECT. Before medication, no significant differences of RI and AI were observed between patients with and without medication of bifemelane hydrochloride. Significantly higher RI was observed in the second measurement 2.8 months in mean during medication of bifemelane hydrochloride, while AI was less in patients medicated with bifemelane hydrochloride. In the third measurement 10.3 months in mean during medication of bifemelane hydrochloride, RI was kept to be higher than that in the second measurement of the control patients without medication. The ratio of the number of ROI, where the redistribution being observed, was significantly higher in patients medicated than in control patients. From the results, medication of bifemelane hydrochloride might keep the redistribution phenomenon, which may indicate reversible cerebral ischemia, more persistently and intensively in patients with cerebrovascular diseases. (author).

  16. SPECTROPHOTOMETRIC, ATOMIC ABSORPTION AND CONDUCTOMETRIC ANALYSIS OF TRAMADOL HYDROCHLORIDE

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    Sara M. Anis

    2011-09-01

    Full Text Available Six simple and sensitive spectroscopic and conductometric procedures (A-F were developed for the determination of tramadol hydrochloride. Methods A, B and C are based on the reaction of cobalt (II thiocyanate with tramadol to form a stable ternary complex, which could be measured by spectrophotometric (method A, atomic absorption (method B or conductometric (method C procedures. Methods D and E depend on the reaction of molybdenum thiocyanate with tramadol to form a stable ternary complex, measured by spectrophotometric means (method D or by atomic absorption procedures (method E, while method F depends on the formation of an ion pair complex between the studied drug and bromothymol blue which is extractable into methylene chloride. Tramadol hydrochloride could be assayed in the range of 80-560 and 40-–220 μg ml-1, 1-15 mg ml-1 and 2.5-22.5, 1.25-11.25 and 5-22 μg ml-1 using methods A,B,C,D,E and F, respectively. Various experimental conditions were studied. The results obtained showed good recoveries. The proposed procedures were applied successfully to the analysis of tramadol in its pharmaceutical preparations and the results were favorably comparable with the official method.

  17. Oxymetazoline hydrochloride cream for facial erythema associated with rosacea.

    Science.gov (United States)

    Patel, Nupur U; Shukla, Shweta; Zaki, Jessica; Feldman, Steven R

    2017-10-01

    Rosacea is a chronic skin condition characterized by transient and persistent erythema of the central face. The symptom of persistent erythema can be particularly frustrating for both patients and physicians as it is difficult to treat. Areas covered: Current treatment options for the treatment of rosacea include metronidazole, azelaic acid, sodium sulfacetamide-sulfur, and brimonidine. Until recently, brimonidine gel was the only option approved specifically for the treatment of facial erythema. However, oxymetazoline hydrochloride 1% cream is a newly FDA approved topical medication for adult rosacea patients. A primarily alpha-1a agonist, oxymetazoline hydrochloride (HCl) is thought to diminish erythema through vasoconstriction. Our paper seeks to evaluate evidence for topical oxymetazoline HCl with respect to its efficacy and safety for its approved indication of treating the persistent erythema associated with rosacea. Expert commentary: While assessment of available clinical trial data indicates that the medication is as effective as other available treatment for controlling rosacea-associated erythema with minimal risk of adverse effects, studies of long-term duration and direct comparison will be necessary to establish its place in treatment guidelines and clinical practice. As further evidence becomes available, the real-world clinical potential of topical oxymetazoline cream will become clearer.

  18. Sensitivity of Phytophthora infestans (Mont. de Bary Isolates to Fluazinam, Fosetyl-Al and Propamocarb-hydrochloride

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    Emil Rekanović

    2011-01-01

    Full Text Available A survey of in vitro sensitivity of twelve isolates of the Phytophthora infestans to the fluazinam,fosetyl-Al and propamocarb-hydrochloride was conducted. The isolates were isolated from infeceted potato leaves collected from eight different localities in Serbia during 2005-2007. All P. infestans isolates were sensitive to tested fungicides. The obtained values of resistance factor were in the range from 1.0 to 2.8. The EC50 values of fluazinam were from0.14 to 0.27 mg l-1, fosetyl-Al from 30.2 to 85.8 mg l-1, propamocarb-hydrochloride between 12.1 and 31.1 mg l-1, respectively.

  19. Synthesis of 7-[α-(2-amino-[2-14C]thiazol-4-yl)-α-(Z)-methoxyimin oacetamido]-3-(1-methylpyrrolidinio)methyl-3-cephem-4-carboxylate hydrochloride ([14C]cefepime hydrochloride)

    International Nuclear Information System (INIS)

    Standridge, R.T.; Swigor, J.E.

    1993-01-01

    The title compound ([ 14 C]cefepime hydrochloride) was prepared as follows:- [ 14 C]Thiourea was condensed with ethyl 4-bromo-3-oxo-2-methoxyimino-acetate providing ethyl 2-(2-amino-4-[2- 14 C] thiazolyl)-2-methoxyi-minoacetate as the pure Z-isomer. Saponification gave the amino acid this was reacted with 1-hydroxybenzotriazole to give the activated ester. Condensation in situ with 7-amino-3-(1-methylpyrrolidinio) methyl-3-cephem-4-carboxylate yielded the product as the pure sulfate salt. Treatment of the sulfate salt with base provided the zwitterion isolated as the stable N-methyl-2-pyrrolidinone adduct. An aqueous solution of the adduct was converted to the crystalline title compound, [ 14 C]Cefepime hydrochloride hydrate, with hydrochloric acid/acetone. Radiochemical purity was 99.0% and specific activity, 34.2 μCi/mg. Overall yield from [ 14 C]thiourea was 18%. (Author)

  20. Stable RNA interference of ErbB-2 gene synergistic with epirubicin suppresses breast cancer growth in vitro and in vivo

    International Nuclear Information System (INIS)

    Hu Xiaoqu; Su Fengxi; Qin Li; Jia Weijuan; Gong Chang; Yu Fengyan; Guo Jujiang; Song Erwei

    2006-01-01

    Overexpression of human epidermal growth factor receptor-2 (Her2, ErbB-2) contributes to the progression and metastasis of breast cancer, implying that Her2 gene is a suitable target of RNA interference (RNAi) for breast cancer therapy. Here, we employed plasmid-mediated expression of 2 different Her2-shRNAs (pU6-Her2shRNAs) efficiently silenced the target gene expression on Her2 expressing SKBR-3 breast cancer cells in both mRNA and protein levels. Consequently, pU6-Her2shRNA increased apoptosis and reduced proliferation of SKBR-3 cells assayed by TUNEL and MTT, respectively. In vivo, intra-tumor injection of pU6-Her2shRNA inhibited the growth of SKBR-3 tumors inoculated subcutaneously in nude mice. Furthermore, pU6-Her2shRNA synergized the tumor suppression effect of epirubicin to SKBR-3 cells in vitro and implanted subcutaneously in nude mice. Therefore, we concluded that stable silencing of Her2 gene expression with plasmid expressing shRNA may hold great promise as a novel therapy for Her2 expressing breast cancers alone or in combination with anthracycline chemotherapy

  1. Ocular pharmacokinetics comparison between 0.2% olopatadine and 0.77% olopatadine hydrochloride ophthalmic solutions administered to male New Zealand white rabbits.

    Science.gov (United States)

    Iyer, Ganesh R; Cason, Marita M; Womble, Scott W; Li, Guangming; Chastain, James E

    2015-05-01

    The primary objective of this study was to compare uptake and distribution of the commercially available formulation of 0.2% olopatadine and the newly developed 0.77% olopatadine hydrochloride ophthalmic solution formulation with improved solubility following a single (30 μL), bilateral topical ocular dose in male New Zealand white rabbits. Each animal received a single 30-μL topical ocular dose (0.2% olopatadine or 0.77% olopatadine hydrochloride ophthalmic solution) to the right (OD) eye followed by the left (OS) eye for a total dose of 60 μL. Olopatadine concentrations were measured in ocular tissues (cornea, bulbar, conjunctiva, choroid, iris-ciliary body, whole lens, retina), aqueous humor, and plasma at prespecified time points over 24 h using a qualified liquid chromatography coupled with mass spectrometry (LC-MS/MS) analytical method. Olopatadine was absorbed into the eye and reached maximal levels (Cmax) within 30 min (0.5 h) to 2 h (Tmax) in ocular tissues and plasma for both treatment groups, except for the lens in which the Tmax was 4 h in the 0.2% olopatadine group and 8 h in the 0.77% olopatadine hydrochloride group, respectively. Tissues associated with the site of dosing, that is, the conjunctiva and cornea, had the highest concentrations of olopatadine in both the 0.2% olopatadine (609 and 720 ng/g) and 0.77% olopatadine hydrochloride (3,000 and 2,230 ng/g) dose groups. The greatest differences between 0.2% olopatadine and 0.77% olopatadine hydrochloride were associated with the overall duration and level of ocular exposures. The newly developed 0.77% olopatadine hydrochloride ophthalmic solution formulation resulted in a higher and more prolonged olopatadine concentration in the target tissue, that is, conjunctiva compared to the commercial formulation of 0.2% olopatadine ophthalmic solution.

  2. A validated stability-indicating HPLC method for the simultaneous determination of pheniramine maleate and naphazoline hydrochloride in pharmaceutical formulations.

    Science.gov (United States)

    Huang, Taomin; Chen, Nianzu; Wang, Donglei; Lai, Yonghua; Cao, Zhijuan

    2014-02-01

    A simple, rapid, and accurate stability-indicating reverse phase liquid chromatographic method was developed and validated for the simultaneous determination of pheniramine maleate and naphazoline hydrochloride in bulk drugs and pharmaceutical formulations. Optimum chromatographic separations among pheniramine maleate, naphazoline hydrochloride and stress-induced degradation products have been achieved within 10 minutes by using an Agilent zorbax eclipse XDB C18 column (150 mm × 4.6 mm, 5 μm) as the stationary phase with a mobile phase consisted of 10 mM phosphate buffer pH 2.8 containing 0.5% triethlamine and methanol (68:32, v/v) at a flow rate of 1 mL min-1. Detection was performed at 280 nm using a diode array detector. Theoretical plates for pheniramine maleate and naphazoline hydrochloride were calculated to be 6762 and 6475, respectively. The method was validated in accordance with ICH guidelines with respect to linearity, accuracy, precision, robustness, specificity, limit of detection and quantitation. Regression analysis showed good correlations (R2 > 0.999) for pheniramine maleate in the concentration range of 150-1200 μg mL-1 and naphazoline hydrochloride in 12.5-100 μg mL-1. The method results in excellent separation of both the analytes and degradation products. The peak purity factor is ≥980 for both analytes after all types of stress, indicating complete separation of both analyte peaks from the stress induced degradation products. Overall, the proposed stability-indicating method was suitable for routine quality control and drug analysis of pheniramine maleate and naphazoline hydrochloride in pharmaceutical formulations.

  3. Eradication of Biofilm-like Microcolony Structures of Borrelia burgdorferi by Daunomycin and Daptomycin but not Mitomycin C in Combination with Doxycycline and Cefuroxime

    Directory of Open Access Journals (Sweden)

    Jie eFeng

    2016-02-01

    Full Text Available Lyme disease, caused by Borrelia burgdorferi, is the most common vector-borne disease in the United States and Europe. While the majority of Lyme disease patients can resolve their symptoms if treated promptly, 10-20% of patients suffer from prolonged symptoms called post-treatment Lyme disease syndrome (PTLDS. Although the cause for PTLDS is unclear, one possibility is the presence of bacterial persisters not effectively cleared by the current Lyme antibiotics. Recent studies identified several drug candidates including daptomycin, daunomycin, doxorubicin, and mitomycin C that had good activity against B. burgdorferi persisters. However, their relative activities against B. burgdorferi persisters have not been evaluated under the same conditions. In this study, we tested the anti-persister activities of these drugs against both 7-day and 15-day old stationary phase cultures of B. burgdorferi individually as well as in combination with Lyme antibiotics doxycycline and cefuroxime (Ceftin. Our findings demonstrate daunomycin and daptomycin were more active than mitomycin C in single drug comparison at 10 and 20 µM, as well as in drug combinations with doxycycline and cefuroxime. In addition, daunomycin was more active than doxorubicin which correlated with their ability to stain and accumulate in B. burgdorferi. The two drug combination of doxycycline and cefuroxime was unable to eradicate biofilm-like microcolonies of B. burgdorferi persisters. However, the addition of either daunomycin or daptomycin to the doxycycline + cefuroxime combination completely eradicated the biofilm-like structures and produced no visible bacterial regrowth after 7 days and 21 days, while the addition of doxorubicin was unable to prevent regrowth at either 7 day or 21 day subculture. Mitomycin C in combination with doxycycline and cefuroxime caused no regrowth at 7 days but visible spirochetal regrowth occurred after 21 day subculture. Furthermore, we found that

  4. Association between Chemotherapy-Response Assays and Subsets of Tumor-Infiltrating Lymphocytes in Gastric Cancer: A Pilot Study.

    Science.gov (United States)

    Lee, Jee Youn; Son, Taeil; Cheong, Jae-Ho; Hyung, Woo Jin; Noh, Sung Hoon; Kim, Choong-Bai; Park, Chung-Gyu; Kim, Hyoung-Il

    2015-12-01

    The purpose of this pilot study was to evaluate the association between adenosine triphosphate-based chemotherapy response assays (ATP-CRAs) and subsets of tumor infiltrating lymphocytes (TILs) in gastric cancer. In total, 15 gastric cancer tissue samples were obtained from gastrectomies performed between February 2007 and January 2011. Chemotherapy response assays were performed on tumor cells from these samples using 11 chemotherapeutic agents, including etoposide, doxorubicin, epirubicin, mitomycin, 5-fluorouracil (5-FU), oxaliplatin, irinotecan, docetaxel, paclitaxel, methotrexate, and cisplatin. TILs in the tissue samples were evaluated using antibodies specific for CD3, CD4, CD8, Foxp3, and Granzyme B. The highest cancer cell death rates were induced by etoposide (44.8%), 5-FU (43.1%), and mitomycin (39.9%). Samples from 10 patients who were treated with 5-FU were divided into 5-FU-sensitive and -insensitive groups according to median cell death rate. No difference was observed in survival between the two groups (P=0.216). Only two patients were treated with a chemotherapeutic agent determined by an ATP-CRA and there was no significant difference in overall survival compared with that of patients treated with their physician's choice of chemotherapeutic agent (P=0.105). However, a high number of CD3 TILs was a favorable prognostic factor (P=0.008). Pearson's correlation analyses showed no association between cancer cell death rates in response to chemotherapeutic agents and subsets of TILs. Cancer cell death rates in response to specific chemotherapeutic agents were not significantly associated with the distribution of TIL subsets.

  5. Simultaneous radiochemotherapy in cervical cancer: recommendations for chemotherapy

    International Nuclear Information System (INIS)

    Dunst, J.; Haensgen, G.

    2001-01-01

    Background: Simultaneous radiochemotherapy has recently been demonstrated to be superior to radiation alone in the treatment of cervical cancer. The objective of this article is to summarize the data of major randomized trials and to derive recommendations for daily clinical practice. Materials and Methods: We have analyzed the data from seven randomized trials in the recent literature in which radiotherapy alone as standard treatment has been compared to simultaneous radiochemotherapy. Four trials used cisplatin-based chemotherapy regimens, 5-FU, mitomycin C and epirubicin were used each in one trial. Results: All trials demonstrated some improvement in survival which was significant in the studies with cisplatin-based chemotherapy regimens. The survival benefit resulted mainly from an improvement in local control whereas chemotherapy had only a small and insignificant effect on distant metastases. Thus, the main action of chemotherapy is ''radiosensitization''. Cisplatin as single drug yielded comparable results as compared to combined regimens although the cisplatin dose was lower in the studies with combination chemotherapy. For the definitive treatment of locally advanced cancers, monotherapy with cisplatin can be recommended. Mitomycin C offers an attractive alternative to cisplatin in patients with contraindications for cisplatin. For postoperative radiochemotherapy, a combination of cisplatin/5-FU should be used because data with cisplatin alone are lacking so far. Simultaneous radiochemotherapy should also be considered for the curative treatment of local recurrences. Conclusions: The addition of simultaneous chemotherapy to radiotherapy is indicated in the vast majority of patients with cervical cancers who are treated with curative intent. (orig.) [de

  6. [Determination of metformin hydrochloride, melamine and dicyandiamide in metformin hydrochloride preparations by tandem dual solid phase extraction cartridges-high performance liquid chromatography-electrospray ionization multi-stage mass spectrometry].

    Science.gov (United States)

    Zhou, Yanfen; Wang, Fanghuan; Wang, Zelan; Zhan, Haijuan; Liu, Wanyi; Meng, Zhe

    2018-02-08

    A method for the confirmation and quantification of metformin hydrochloride and its relative substances melamine and dicyandiamide using tandem dual solid phase extraction (SPE) cartridges and high performance liquid chromatography-electrospray ionization multi-stage mass spectrometry (HPLC-ESI-MS n ) was developed. The samples were extracted with anhydrous ethanol containing 0.1% (v/v) acetic acid under ultrasound-assisted conditions. The extracts were concentrated and purified using Cleanert PCX and C18 tandem dual solid phase extraction cartridges, and eluted with 5% (v/v) ammonia methanol solution. The separation was performed on a Kromasil-C18 column (100 mm×4.6 mm, 3.5 μm) with gradient elution. The detection was performed in selected ion monitoring (SIM) mode using electrospray ionization multi-stage mass spectrometry. The external standard method was used for quantification. The extraction solvents, types of SPE cartridges and eluents were optimized by comparing the recoveries under different conditions. The results showed that the detector response of each target compound was linear in corresponding mass concentration ranges with the correlation coefficients ( r 2 ) ≥ 0.9992. The limits of detection (LODs) and the limits of quantification (LOQs) of the three analytes were 1.48-13.61 μg/kg and 5.96-45.67 μg/kg, respectively. The recoveries of the three analytes were 65.02%-118.33% spiked at low, medium and high levels. The relative standard deviations (RSDs) were no more than 13.41%. The method is reliable, easy, and has a better purification effect. The method can be applied to the routine analysis of metformin hydrochloride and its relative substances melamine and dicyandiamide in different preparations of metformin hydrochloride.

  7. RP-HPLC Determination of Atomoxetine Hydrochloride in Bulk and Pharmaceutical Formulations

    Directory of Open Access Journals (Sweden)

    H. R. Prajapati

    2011-01-01

    Full Text Available A reversed phase high performance liquid chromatographic (RP–HPLC method was developed and subsequently validated for the determination of atomoxetine hydrochloride in bulk and pharmaceutical formulation. The separation was done by a PerkinElmer Brownlee analytical C8 column (260 mm x 4.6 mm, 5 µm using methanol: 50 mM KH2PO2 buffer (PH adjusted to 6.8 with 0.1 M NaOH, 80:20 v/v as an eluent. UV detection was performed at 270 nm at a flow rate 1.0 mL/min. The validation of the method was performed, and specificity, reproducibility, precision accuracy and ruggedness were confirmed. The correlation coefficient was found to be 0.997 for atomoxetine hydrochloride. The recovery was in the range of 99.94 to 100.98% and limit of quantification was found to be 5.707 µg/mL. The method is simple, rapid, selective and economical too and can be used for the routine analysis of drug in pharmaceutical formulations.

  8. Spectrophotometric assay of phenylephrine hydrochloride using 4-aminoantipyrine and copper (II)

    International Nuclear Information System (INIS)

    Theia'a, N.; Sabha, A.

    2010-01-01

    A new spectrophotometric method is proposed for determination of phenylephrine hydrochloride. The method is based on the coupling of 4-aminoantipyrine (4-AAP) with phenylephrine hydrochloride (PEH) to give a new ligand that reacts with copper (II) in the presence of sodium tetraborate buffer solution of pH 9.00 at 50 deg. C to give an intense red colored chelate having maximum absorption at 480 nm. The optimization of the experimental conditions is described. The method has been used for the determination of 2.0 - 50.0 mu g/ml of PEH. The molar absorptivity is 5.34 X 103 L. mol/sup -1/cm /sup- 1/ and the accuracy of the method is achieved by the value of average recovery (101.28 %) and the precision is supported by relative standard deviation (RSD=1.25 %) values. The results of the method was compared with those of the standard method. The interference of excipients was studied. The mechanism of the chemical reaction has been proposed. The proposed method was successfully applied for the determination of the PEH in pharmaceutical syrup formulations. (author)

  9. Spectrophotometric Assay of Phenylephrine Hydrochloride Using 4-Aminoantipyrine and Copper (II

    Directory of Open Access Journals (Sweden)

    Theia'a N. Al-Sabha

    2010-06-01

    Full Text Available A new spectrophotometric method is proposed for determination of phenylephrine hydrochloride. The method is based on the coupling of 4-aminoantipyrine (4-AAP with phenylephrine hydrochloride (PEH to give a new ligand that reacts with copper (II in the presence of sodium tetraborate buffer solution of pH 9.00 at 50 °C to give an intense red colored chelate having maximum absorption at 480 nm. The optimization of the experimental conditions is described. The method has been used for the determination of 2.0–50.0 μg/ml of PEH. The molar absorptivity is 5.34×103 L.mol.-1cm.-1 and the accuracy of the method is achieved by the value of average recovery (101.28 % and the precision is supported by relative standard deviation (RSD=1.25 % values. The results of the method was compared with those of the standard method. The interference of excipients was studied. The mechanism of the chemical reaction has been proposed. The proposed method was successfully applied for the determination of the PEH in pharmaceutical syrup formulations.

  10. Benazepril hydrochloride improves diabetic nephropathy and decreases proteinuria by decreasing ANGPTL-4 expression.

    Science.gov (United States)

    Xue, Lingyu; Feng, Xiaoqing; Wang, Chuanhai; Zhang, Xuebin; Sun, Wenqiang; Yu, Kebo

    2017-10-04

    This study aimed to investigate the effects of benazepril hydrochloride (BH) on proteinuria and ANGPTL-4 expression in a diabetic nephropathy (DN) rat model. A total of 72 Wistar male rats were randomly divided into three groups: normal control (NC), DN group and BH treatment (BH) groups. The DN model was induced by streptozotocin (STZ). Weight, glucose, proteinuria, biochemical indicators and the kidney weight index were examined at 8, 12 and 16 weeks. In addition, ANGPTL-4 protein and mRNA expressions were assessed by immunohistochemistry and qRT-PCR, respectively. Relationships between ANGPTL-4 and biochemical indicators were investigated using Spearman analysis. Weight was significantly lower but glucose levels were significantly higher in both the DN and BH groups than in the NC group (P Benazepril hydrochloride improves DN and decreases proteinuria by decreasing ANGPTL-4 expression.

  11. Chemoreactomic analysis of thiamine disulfide, thiamine hydrochloride, and benfotiamine molecules

    OpenAIRE

    O. A. Gromova; I. Yu. Torshin; L. V. Stakhovskaya; L. E. Fedotova

    2017-01-01

    Objective: to analyze the interactions that could indicate the potential pharmacological properties of the molecules of thiamin, thiamine disulfide, and others.Material and methods. The investigators simulated the properties of thiamine disulfide (bistiamin) versus those of the reference molecules of thiamin hydrochloride and benfotiamine. The study was performed using chemoreactomic simulation that is the newest area in post-genome pharmacology.Results and discussion. Chemoreactomic analysis...

  12. Efficacy and tolerability of itopride hydrochloride in patients with non-ulcer dyspepsia.

    Science.gov (United States)

    Shenoy, K T; Veenasree; Leena, K B

    2003-06-01

    To document the clinical efficacy and tolerability of itopride hydrochloride in patients with non-ulcer dyspepsia an open-label, non-comparative study, was undertaken at the Medical College, Thiruvananthapuram, among patients with endoscopically confirmed diagnosis of non-ulcer dyspepsia or chronic gastritis. Itopride hydrochloride 50 mg (1 tablet) thrice a day for 2 weeks was administered among them. Relief of symptoms at the end of two weeks treatment, assessed as marked/complete, moderate, slight, none or worse; QT interval on ECG; adverse events; haemogram; serum chemistry for hepatic and renal functions. None had QT prolongation on ECG. At the end of 2 weeks' treatment, moderate to complete relief of symptoms was reported by 22 patients (73%), whereas 5 (17%) reproted slight improvement, and 3 (10%) reported no improvement. Clinical tolerability was excellent in 28 patients (93%) and good in 2 (7%). None of the patients had any prolongation of QT on ECG, nor did any patient show any abnormality in haemogram or serum chemistry during the treatment.

  13. Cost-effectiveness Analysis of Fluorouracil, Leucovorin, and Irinotecan versus Epirubicin, Cisplatin, and Capecitabine in Patients with Advanced Gastric Adenocarcinoma

    Science.gov (United States)

    Wen, Feng; Zheng, Hanrui; Wu, Yifan; Wheeler, John; Zeng, Xiaoxi; Fu, Ping; Li, Qiu

    2016-01-01

    No standard treatment has been accepted widely for the first-/second-line therapy for advanced gastric cancer (AGC). The current study aimed to determine a preferred strategy between FOLFIRI (fluorouracil, leucovorin, and irinotecan) and ECX (epirubicin, cisplatin,and capecitabine) for AGC from the cost-effectiveness perspective. According to a French intergroup study, two groups (ECX arm and FOLFIRI arm) and three health states (progression-free survival (PFS), progressive disease (PD) and death) were analyzed in the current Markov model. All the medical costs were calculated from a Chinese societal perspective. Although FOLFIRI was an acceptable first-line therapy in the treatment of AGC with a better time-to treatment failure (TTF) compared to ECX, ECX arm (ECX followed by FOLFIRI) gained 0.08 quality-adjusted life months (QALMs) more effectiveness benefit compared with FOLFIRI arm (FOLFIRI followed by ECX). Additionally, a lower cost was found in ECX arm ($23,813.13 versus $24,983.70). Hence, the strategy of FOLFIRI arm is dominated by ECX arm ($4,125.8 per QALM in FOLIRI arm; $3,879.724 per QALM in ECX arm). ECX followed by FOLFIRI was a preferred strategy with more effectiveness and lower cost compared with FOLFIRI followed by ECX for the treatment of AGC. PMID:27824060

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

    Science.gov (United States)

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

    2015-01-01

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

  15. Influence of Sodium Alginate on Hypoglycemic Activity of Metformin Hydrochloride in the Microspheres Obtained by the Spray Drying

    Directory of Open Access Journals (Sweden)

    Marta Szekalska

    2016-01-01

    Full Text Available Alginate microspheres with metformin hydrochloride were prepared by the spray drying method in order to improve residence time of drug in the stomach. Nine formulations (F1–F9 with various drug : polymer ratio (1 : 2, 1 : 1, and 2 : 1 and different sodium alginate concentration (1%, 2%, and 3% were evaluated for size, morphology, drug loading, Zeta potential, and swelling degree. In vitro drug release, mathematical release profile, and physical state of microspheres were also evaluated. Optimal formulation characterized by the highest drug loading was formulation F6 (drug : polymer ratio 2 : 1 and 2% alginate solution. Based on glucose uptake in Saccharomyces cerevisiae cells and α-amylase inhibition tests, it could be concluded that alginate microspheres enhance hypoglycemic activity of metformin hydrochloride evaluated in vitro. Designed microspheres are promising as alternative, multicompartment dosage form for metformin hydrochloride delivery.

  16. Modulation of mitomycin C-induced genotoxicity by acetyl- and thio- analogues of salicylic acid.

    Science.gov (United States)

    Pawar, Amol Ashok; Vikram, Ajit; Tripathi, Durga Nand; Padmanabhan, Shweta; Ramarao, Poduri; Jena, Gopabandhu

    2009-01-01

    Recent reports regarding acetylsalicylic acid (ASA) and its metabolites suggest suppressive effects against mitomycin C (MMC)-induced genotoxicity in a mice chromosomal aberration assay. Keeping this in mind, the potential anti-genotoxic effect of the thio-analogue of salicylic acid namely thio-salicylic acid (TSA) was speculated upon. The present study investigated and compared the anti-genotoxic potential of ASA and TSA. The study was performed in male swiss mice (20+/-2 g) using single-cell gel electrophoresis and a peripheral blood micronucleus assay. ASA and TSA (5, 10 or 20 mg/kg) were administered 15 minutes after MMC (1 mg/kg) once daily for 3 or 7 days. Both ASA and TSA significantly decreased the DNA damage induced by MMC as indicated by a decrease in the comet parameters in bone marrow cells and decreased frequencies of micronucleated reticulocytes in peripheral blood. The results clearly demonstrate the anti-genotoxic potential of ASA and TSA.

  17. Mitomycin-C in dacryocystorhinostomy: From experimentation to implementation and the road ahead: A review

    Directory of Open Access Journals (Sweden)

    Akshay Gopinathan Nair

    2015-01-01

    Full Text Available Dacryocystorhinostomy (DCR is the procedure of choice in patients with epiphora due to primary acquired nasolacrimal duct obstruction. The evolution of surgical tools, fiber-optic endoscopes, effective anesthesia techniques, and the adjunct use of antimetabolites intraoperatively; namely mitomycin-C (MMC have significantly contributed to the advancement of DCR surgery. MMC is a systemic chemotherapeutic agent derived from Streptomyces caespitosus that inhibits the synthesis of DNA, cellular RNA, and protein by inhibiting the synthesis of collagen by fibroblasts. Even the cellular changes in the human nasal mucosal fibroblasts induced by MMC at an ultrastructural level have been documented. There, however, seems to be a lack of consensus regarding MMC: The dosage, the route of delivery/application, the time of exposure and subsequently what role each of these variables plays in the final outcome of the surgery. In this review, an attempt is made to objectively examine all the evidence regarding the role of MMC in DCR. MMC appears to improve the success rate of DCR.

  18. 76 FR 17336 - New Animal Drugs; Amikacin Sulfate, Ampicillin Trihydrate, Ceftiofur Hydrochloride, Cephapirin...

    Science.gov (United States)

    2011-03-29

    ..., Ceftiofur Hydrochloride, Cephapirin Benzathine, Chlortetracycline, Fenbendazole, Formalin, Furosemide... (e)(3)(iii) to read as follows: Sec. 520.905a Fenbendazole suspension. * * * * * (e) * * * (2.... 520.905c, revise paragraph (e)(2)(iii) to read as follows: Sec. 520.905c Fenbendazole paste...

  19. Corneal haze following PRK with mitomycin C as a retreatment versus prophylactic use in the contralateral eye.

    Science.gov (United States)

    Netto, Marcelo V; Chalita, Maria Regina; Krueger, Ronald R

    2007-01-01

    To report photorefractive keratectomy (PRK) treated with mitomycin C (MMC) for previous corneal haze in one eye and PRK with MMC to prevent corneal haze formation in the fellow eye. A 40-year-old woman underwent PRK with MMC to treat previous corneal haze (secondary to previous PRK without MMC) for residual refractive error of +0.50 +0.25 x 165 in the left eye and PRK with MMC to prevent corneal haze in the right eye. Postoperative slit-lamp examination revealed no haze in the right eye, but continued mild haze in the left eye. Treatment with PRK and MMC for previous corneal haze is not as effective as primary PRK with MMC in preventing postoperative corneal haze formation.

  20. Plasma lipid levels in Alzheimer's disease patients treated by Donepezil hydrochloride: a cross-sectional study.

    Science.gov (United States)

    Adunsky, Abraham; Chesnin, Vladimir; Ravona, Ramit; Harats, Dror; Davidson, Michael

    2004-01-01

    Donepezil hydrochloride is a central acetylcholine esterase inhibitor that is widely used in Alzheimer disease (AD). We have recently observed some differences in lipid profile between occasional cases of Donepezil hydrochloride users (DU) and non-users (DNU). This prompted us to study the levels of plasma lipids in these two groups, cross-sectionally. The medical charts of patients with probable AD were screened for current use of Donepezil hydrochloride and lipids profile, along with other clinical and demographic data. A total number of 105 patients were identified and included in the final analysis. Patients were divided into two groups (DU and DNU). Plasma levels of lipids were recorded. Mann-Whitney or t-test for continuous variables and Fisher exact test for categorical variables were used to test for significant differences between the groups. Regression analysis was applied to identify independently the factors associated with lipid levels. Thirty-three patients were DU and 72 DNU. The two groups differed in terms of age, lipid levels and cognitive level. DU had statistically significant higher levels of triglycerides compared with those not using the drug (P=0.036), higher total cholesterol (Phydrochloride. Alternatively, this may indicate that the effect of the medication may involve lipid metabolism, rather than other proposed mechanisms.

  1. BUSPIRONE HYDROCHLORIDE EFFECTS ON HOSPITALIZATIONS FREQUENCY IN PATIENTS WITH CHRONIC HEART FAILURE AND MIXED ANXIETY-DEPRESSIVE DISORDER

    Directory of Open Access Journals (Sweden)

    M. A. Khristichenko

    2017-01-01

    Full Text Available Aim. Assessing the impact of buspirone hydrochloride on hospitalizations frequency in patients  with chronic heart failure (CHF and mixed anxietydepressive disorder (MADD. Materials and methods.  The study involved 49 patients  with heart failure of ischemic etiology and MADD. Patients in Group 1 (n = 25 received buspirone hydrochloride (in the starting dose of 15 mg/day with a gradual (within 2 weeks increasing to the effective (30 mg/day in addition to standard  CHF therapy and coronary heart disease (CHD. Patients in group 2 (n = 24 received standard  therapy of CHF and CHD. After 6 months, we evaluated hospitalizations frequency and duration in patients from both groups. Results. The risk of hospitalization for heart failure decompensation was significantly lower in patients  from group 1 compared with patients  from group 2 (HR 0.333, 95% CI 1,12-8,05, p = 0.035.Conclusions. Buspirone hydrochloride admission in addition to standard  therapy  is associated  with reduced risk of hospitalization for decompensation of chronic heart failure in patients with MADD.

  2. Genome-Wide Mutational Signature of the Chemotherapeutic Agent Mitomycin C in Caenorhabditis elegans.

    Science.gov (United States)

    Tam, Annie S; Chu, Jeffrey S C; Rose, Ann M

    2015-11-12

    Cancer therapy largely depends on chemotherapeutic agents that generate DNA lesions. However, our understanding of the nature of the resulting lesions as well as the mutational profiles of these chemotherapeutic agents is limited. Among these lesions, DNA interstrand crosslinks are among the more toxic types of DNA damage. Here, we have characterized the mutational spectrum of the commonly used DNA interstrand crosslinking agent mitomycin C (MMC). Using a combination of genetic mapping, whole genome sequencing, and genomic analysis, we have identified and confirmed several genomic lesions linked to MMC-induced DNA damage in Caenorhabditis elegans. Our data indicate that MMC predominantly causes deletions, with a 5'-CpG-3' sequence context prevalent in the deleted regions of DNA. Furthermore, we identified microhomology flanking the deletion junctions, indicative of DNA repair via nonhomologous end joining. Based on these results, we propose a general repair mechanism that is likely to be involved in the biological response to this highly toxic agent. In conclusion, the systematic study we have described provides insight into potential sequence specificity of MMC with DNA. Copyright © 2016 Tam et al.

  3. Genome-Wide Mutational Signature of the Chemotherapeutic Agent Mitomycin C in Caenorhabditis elegans

    Directory of Open Access Journals (Sweden)

    Annie S. Tam

    2016-01-01

    Full Text Available Cancer therapy largely depends on chemotherapeutic agents that generate DNA lesions. However, our understanding of the nature of the resulting lesions as well as the mutational profiles of these chemotherapeutic agents is limited. Among these lesions, DNA interstrand crosslinks are among the more toxic types of DNA damage. Here, we have characterized the mutational spectrum of the commonly used DNA interstrand crosslinking agent mitomycin C (MMC. Using a combination of genetic mapping, whole genome sequencing, and genomic analysis, we have identified and confirmed several genomic lesions linked to MMC-induced DNA damage in Caenorhabditis elegans. Our data indicate that MMC predominantly causes deletions, with a 5′-CpG-3′ sequence context prevalent in the deleted regions of DNA. Furthermore, we identified microhomology flanking the deletion junctions, indicative of DNA repair via nonhomologous end joining. Based on these results, we propose a general repair mechanism that is likely to be involved in the biological response to this highly toxic agent. In conclusion, the systematic study we have described provides insight into potential sequence specificity of MMC with DNA.

  4. Growth of glycine ethyl ester hydrochloride and its characterizations

    Energy Technology Data Exchange (ETDEWEB)

    Venkatesan, G.; Pari, S., E-mail: sparimyur@gmail.com

    2016-11-15

    Single crystal of glycine ethyl ester hydrochloride by slow evaporation method is reported. The grown crystal characterized by single crystal X-ray diffraction, FT-IR, UV–Vis–NIR and fluorescence spectroscopy. It is established that the crystal falls under the monoclinic system and space group P21/c with the cell parameters as: a=8.565 Å, b=12.943 Å, c=6.272 Å, α=γ=90°, β=103.630º. UV–Vis–NIR spectrum shows indirect allowed transition with a band gap of 5.21 eV and other optical properties are measured. The crystal is also shown to have a high transmittance in the visible region. The third order nonlinear property and optical limiting have been investigated using Z-Scan technique. Complex impedance spectrum measured at the dc conductivity. Dependence of dielectric constant, dielectric loss and ac conductivity on frequency at different temperature of applied ac field is analyzed. The mechanical behavior has been assessed by Vickers microhardness indenter. The thermal behavior of glycine ethyl ester hydrochloride was analyzed using TG/DTA thermal curves. From the thermal study, the material was found to possess thermal stability up to 174 °C. The predicted NLO properties, UV–Vis transmittance and Z-scan studies indicate that is an attractive material for photonics optical limiting applications.

  5. Immediate acid-suppressing effects of ranitidine hydrochloride and rabeprazole sodium following initial administration and reintroduction: A randomized, cross-over study using wireless pH monitoring capsules.

    Science.gov (United States)

    Ono, Shouko; Kato, Mototsugu; Ono, Yuji; Imai, Aki; Yoshida, Takeshi; Shimizu, Yuichi; Asaka, Masahiro

    2009-04-01

    Histamine 2 receptor antagonists and proton-pump inhibitors, drugs that are widely used for the treatment of acid-related diseases, have different clinical characteristics. The objective of this study was to compare the acid-suppressing effects of ranitidine hydrochloride and those of rabeprazole sodium at the first administration and re-administration after withdrawal. The study was designed as an open-label, randomized, two-way cross-over trial. Seven Helicobacter pylori-negative healthy volunteers were enrolled in this study. Ranitidine hydrochloride (300 mg/day) or rabeprazole sodium (20 mg/day) was administered from days 1 to 7 and from days 11 to 13. The percentage of time with gastric pH sodium maintained a potent and stable effect from days 2 to 7 (ranitidine vs rabeprazole: P hydrochloride was attenuated after day 4. In addition, the effect of ranitidine hydrochloride at re-administration was attenuated (days 11, 12, and 13 vs pre-administration: not significant). In view of our observations, we expect symptoms associated with gastric acidity to be more adequately controlled with rabeprazole sodium in the short term when compared to ranitidine hydrochloride.

  6. Development of radiochemical method of analysis of binding of tritium labeled drotaverine hydrochloride with human blood serum albumin

    International Nuclear Information System (INIS)

    Kim, A.A.; Djuraeva, G.T.; Shukurov, B.V.; Mavlyanov, I.R.

    2004-01-01

    Full text: The albumin, being a basic functional linkage of numerous endogenous and exogenous substances is the most important protein of blood plasma. At the diseases connected to liver disfunction, collected in blood metabolite reduce connecting ability of albumino. The aim of the present research was a development of radiochemical method of determination of ability of albumin to bind the tritium labeled preparation drotaverine hydrochloride (no - spa). We had developed a micromethod of definition of connecting ability of albumin, allowing to analyse 20 mkl of blood serum. The method consists in incubation of tritium labeled drotaverine hydrochloride with blood serum in vitro, the following fractionation of serum proteins by gel - filtration on a microcolumn with Sephadex G-25, and direct measurement of the radioactivity connected to fraction of proteins of blood serum. The method has been tested on a series of blood serum of control group of healthy people and on a series of blood serum of patients with hepatitis B. We received quantitative characteristics of binding of drotaverine hydrochloride with albumin of patients with hepatitis B. It was preliminary established that binding ability of serum albumin of children with various forms of acute virus hepatitis tends to decrease in comparison with group of the control. Advantage of the developed radiochemical method is high precision and the high sensitivity of detection of infringement of binding ability of albumin. Application of tritium labeled drotaverine hydrochloride allows to measure directly levels of binding of a preparation with albumin

  7. Mitomycin C induced alterations in antioxidant enzyme levels in a model insect species, Spodoptera eridania.

    Science.gov (United States)

    Batcabe, J P; MacGill, R S; Zaman, K; Ahmad, S; Pardini, R S

    1994-05-01

    1. An insect species, the southern armyworm Spodoptera eridania, was used as an in vivo model to examine mitomycin C's (MMC) pro-oxidant effect reflected in alterations of antioxidant enzymes. 2. Following a 2-day exposure to 0.01 and 0.05% w/w dietary concentrations, MMC only induced superoxide dismutase activity. All other enzyme activities were not affected, indicating oxidative stress was mild. 3. Following a 5-day exposure to 0.05% w/w dietary MMC, the activities of superoxide dismutase, glutathione-S-transferase and its peroxidase activity and DT-diaphorase were induced. GR activity was not altered. The high constitutive catalase activity was also not affected. These responses of S. eridania's antioxidant enzymes are analogous to those of mammalian systems in alleviating MMC-induced oxidative stress. 4. S. eridania emerges as an appropriate non-mammalian model for initial and cost-effective screening of drug-induced oxidative stress.

  8. Use of transmission electron microscope to assess the damage to Sarcoma 180 ascites tumour cells following in vivo treatment of mitomycin-C and gamma radiation

    International Nuclear Information System (INIS)

    Majumdar, S.K.; Bhattacharya, S.; Mitra, A.; Mukherji, S.

    1991-01-01

    Five day old Sarcoma 180 tumour bearing mice were exposed to different doses of mitomycin-C (4 mg or 7 mg per kg body weight of mouse) and gamma radiation (400 R or 800 R) applied singly or in combination. Surviving populations were collected after 5 days of treatment and processed for transmission electron microscopy. The control Sarcoma 180 tumour cells has the following characteristics: profused microvilli, different sized mitochondria with poorly developed internal structure, distinct endoplasmic reticulum studded with ribosomes, the large nucleus rich in chromatin materials and distinct nucleolus containing closely interwined granular and fibrillar components with associated chromatins. Damage to treated cells were ascertained by the reduction in microvilli, swelling of mitochondria with cloudy appearance, dilation and fragmentation of endoplasmic reticulum, blebbing of nuclear membrane, condensation of heterochromatin, appearance of perichromatin granules, segregation and fragmentation of nucleolus and invagination of plasma memebrane with increased intracellular spaces. With the help of transmission electron microscope it is thus possible to assess the nature of damage to organelles effected by mitomycin C and radiation both singly and in combination. Growth inhibition and damage in the cellular ultrastructure were maximum among tumour cells which survived with concomitant treatment with 7 mg MMC and 800 R. (author). 7 refs., 4 figs., 1 tab

  9. Lidocaine Hydrochloride Compared with MS222 for the Euthanasia of Zebrafish (Danio rerio)

    Science.gov (United States)

    Collymore, Chereen; Banks, E Kate; Turner, Patricia V

    2016-01-01

    Despite several shortcomings, MS222 is the most commonly used chemical agent for euthanasia of zebrafish. Although lidocaine hydrochloride has some advantages over MS222, its effectiveness as a euthanasia agent for zebrafish is unknown. Larvae at 9 to 16 d postfertilization were exposed to 250 mg/L MS222 or 400, 500, 600, 700, 800, 900, or 1000 mg/L lidocaine and observed for cessation of heartbeat. Adult zebrafish were exposed to 250 mg/L MS222 or 400, 500, or 600 mg/L lidocaine; times to loss of righting reflex, cessation of opercular movement, and complete recovery; body length; aversive behavior; and gross and microscopic evidence of acute toxicity were evaluated. The heartbeat was not lost from any larvae in any group, regardless of drug or dosage. For adults, time to loss of righting reflex was greatest in the 500-mg/L lidocaine group. Opercular movement ceased earlier in all lidocaine groups compared with the MS222 group. Fish in the 500-mg/L lidocaine group were smaller than those in other groups. Fewer fish in the lidocaine groups displayed aversive behavior (erratic swimming and piping) compared with the MS222 group. No fish in the lidocaine hydrochloride groups (n = 30) recovered from euthanasia, whereas one fish in the MS222 group did (n = 10). Neither the MS222 nor lidocaine groups showed any gross or histologic changes suggestive of acute toxicity. Our results suggest that lidocaine hydrochloride may be an effective alternative chemical euthanasia agent for adult zebrafish but should not be used in larval fish. PMID:27931323

  10. Development and Validation of a Rapid RP-UPLC Method for the Simultaneous Estimation of Bambuterol Hydrochloride and Montelukast Sodium from Tablets.

    Science.gov (United States)

    Yanamandra, R; Vadla, C S; Puppala, U M; Patro, B; Murthy, Y L N; Parimi, A R

    2012-03-01

    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 2-8°. 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.

  11. Influence of insecticidal derivative (cartap hydrochloride) from the marine polycheate on certain enzyme systems of the fresh water fish Oreochromis mossambicus.

    Science.gov (United States)

    Palanivelu, V; Vijayavel, K; Balasubramanian, S Ezhilarasi; Balasubramanian, M P

    2005-04-01

    The activities of phosphatases and transaminases were studied in muscle and liver of the fresh water fish, Oreochromis mossambicus on exposure to different sublethal concentrations (0.25, 0.5, 0.75 and 1 mgl(-1)) of cartap hydrochloride (insecticidal derivative from marine polycheate) for 96 h. There was an overall decrease in phosphatases and transaminases activity in muscle and liver of the fish subjected to cartap hydrochloride.

  12. Abnormal sensitivity of diploid skin fibroblasts from a family with Gardner's syndrome to the lethal effects of X-irradiation, ultraviolet light and mitomycin-C

    International Nuclear Information System (INIS)

    Little, J.B.; Nove, J.; Weichselbaum, R.R.

    1980-01-01

    Skin fibroblasts isolated from two members of the same family with the cancer-prone disease Gardner's Syndrome (intestinal polyposis, colon cancer, bone and soft tissue tumors) showed enhanced sensitivity to the lethal effects of X-irradiation, ultraviolet light and mitomycin-C. These cells showed no liquid-holding type recovery following UV-irradiation of confluent cultures, but were normal in their capacity for UV-induced unscheduled DNA synthesis. UV survival was not influenced by post-irradiation incubation with caffeine. (orig.)

  13. Atovaquone and proguanil hydrochloride compared with chloroquine or pyrimethamine/sulfadoxine for treatment of acute Plasmodium falciparum malaria in Peru

    OpenAIRE

    Llanos-Cuentas, A.; Campos, P.; Clendenes, M.; Canfield, C. J.; Hutchinson, D. B. A.

    2001-01-01

    The efficacy and safety of a fixed-dose combination of atovaquone and proguanil hydrochloride (MalaroneTM) were compared with chloroquine or pyrimethamine/sulfadoxine in patients with acute falciparum malaria in northern Peru. Patients were initially randomized to receive 1,000 mg atovaquone and 400 mg proguanil hydrochloride daily for 3 days (n=15) or 1,500 mg chloroquine (base) over a 3 day period (n=14) (phase 1). The cure rate with chloroquine was lower than expected and patients were sub...

  14. Epirubicin is not Superior to Doxorubicin in the Treatment of Advanced Soft Tissue Sarcomas.The Experience of the EORTC Soft Tissue and Bone Sarcoma Group

    DEFF Research Database (Denmark)

    Nielsen, Ole Steen; Dombernowsky, Per; Mouridsen, Henning T

    2000-01-01

    studies the EORTC STBSG tested whether epirubicin (epi) is an alternative to standard dose dox in the treatment of chemonaive patients with advanced soft tissue sarcoma. The present report gives the final results of these studies.Patients/Methods. In the first study 210 patients were randomized to receive...... either dox or epi both at a dose of 75 mg/m(2) given as bolus injection at 3-week intervals. In the second study 334 patients were randomized to dox 75 mg/m(2), epi 150 mg/m(2) or epi 50 mg/m(2) days 1-3, all given as bolus injection at 3-week intervals.Results. In the first study no differences...... in median survival and duration of response were found. Of 167 evaluable patients the response rate was slightly in favour of dox (23% vs 18%) but at the expense of more toxicity.These data could suggest that increasing the epi dose may lead to a greater antineoplastic effect with acceptable toxicity...

  15. Determination of antihypertensive drug moexipril hydrochloride based on the enhancement effect of sodium dodecyl sulfate at carbon paste electrode.

    Science.gov (United States)

    Attia, Ali K

    2010-04-15

    Herein, an electrochemical differential pulse voltammetric method was developed for the determination of moexipril hydrochloride based on the enhancement effect of sodium dodecyl sulfate. The oxidation process has been carried out in Britton-Robinson buffer. Moexipril hydrochloride exhibits a well-defined irreversible oxidation peak over the entire pH range (2-11). The peak current varied linearly over the range from 4.0 x 10(-7) to 5.2 x 10(-6) mol L(-1). The limits of detection and quantification were 6.87 x 10(-8) mol L(-1) and 2.29 x 10(-7) mol L(-1), respectively. The recovery was found in the range from 99.65% to 100.76%. The relative standard deviation was found in the range from 0.429% to 0.845%. The proposed method possesses high sensitivity, accuracy and rapid response. Finally, this method was successfully used to determine moexipril hydrochloride in tablets. (c) 2009 Elsevier B.V. All rights reserved.

  16. Guanidine hydrochloride embedded polyurethanes as antimicrobial and absorptive wound dressing membranes with promising cytocompatibility

    Energy Technology Data Exchange (ETDEWEB)

    Sahraro, Maryam; Yeganeh, Hamid, E-mail: h.yeganeh@ippi.ac.ir; Sorayya, Marziyeh

    2016-02-01

    Preparation and assessments of novel absorptive wound dressing materials with efficient antimicrobial activity as well as very good cytocompatibility were described in this work. An amine terminated poly(hexamethylene guanidine hydrochloride) was prepared and used as curing agent of different epoxy-terminated polyurethane prepolymers. The structures of prepared materials were elucidated by evaluation of their {sup 1}H NMR and FTIR spectra. The recorded tensile strength of membranes confirmed the excellent dimensional stability of the film type dressings even at fully hydrated conditions. Therefore, these dressings could protect the wound bed from external forces during the healing period. The structurally optimized dressing membranes could preserve the desired moist environment over the wounded area, as a result of their balanced equilibrium, water absorption and water vapor transmission rate. Therefore, a very good condition for stimulation of self-healing of wound bed was attained. Also, owing to the presence of guanidine hydrochloride moieties embedded into the structure of dressings, efficient antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans were detected. In vitro cytotoxicity assay of the prepared dressings revealed cytocompatibility of these materials against fibroblast cells. Therefore, they could support cell growth and proliferation at the wounded area. - Highlights: • New polyurethane wound dressings with guanidine hydrochloride based antimicrobials • Maintaining moist and warm wound environment for accelerating healing • Proper tensile strength of dressings even at fully hydrated state • Excellent biocompatibility index due to proper selection of starting materials.

  17. Effect of Mitomycin C on Myopic versus Astigmatic Photorefractive Keratectomy

    Directory of Open Access Journals (Sweden)

    Ashwag A. Almosa

    2017-01-01

    Full Text Available Purpose. Long-term mitomycin C (MMC effects on photorefractive keratectomy (PRK were compared in simple myopic and astigmatic patients. Methods. In this observational cohort study, subjects were selected based on preoperative and postoperative data collected from medical records; they were divided into simple myopia with/without MMC and myopic astigmatism with/without MMC groups. Haze, uncorrected visual acuity (UCVA, best-corrected visual acuity (BCVA, subjective refraction, and K-reading were evaluated at 1-, 3-, 6-, and 12-month follow-ups. Results. One hundred fifty-nine eyes of 80 subjects (34 women and 46 men; mean age, 26.81 ± 7.74 years; range, 18–53 years; spherical powers, −0.50 to −8.00 DS; and cylindrical powers, −0.25 to −5.00 DC were enrolled. One year postoperatively, the simple myopia with/without MMC groups showed no difference in UCVA (P=0.187, BCVA (P=0.163, or spherical equivalent (P=0.163 and a significant difference (P=0.0495 in K-reading; the haze formation difference was nonsignificant (P=0.056. Astigmatic groups with/without MMC showed a significant difference in K-reading (P<0.0001. MMC groups had less haze formation (P<0.0001. Conclusion. PRK with intraoperative MMC application showed excellent visual outcomes. MMC’s effect on astigmatic patients was significantly better with acceptable safety and minimal side effects.

  18. An experimental and theoretical investigation of loperamide hydrochloride-glutaric acid cocrystals.

    Science.gov (United States)

    Bruni, Giovanna; Maietta, Mariarosa; Maggi, Lauretta; Mustarelli, Piercarlo; Ferrara, Chiara; Berbenni, Vittorio; Freccero, Mauro; Scotti, Federico; Milanese, Chiara; Girella, Alessandro; Marini, Amedeo

    2013-07-11

    Cocrystallization is a powerful method to improve the physicochemical properties of drugs. Loperamide hydrochloride is a topical analgesic for the gastrointestinal tract showing low and pH-dependent solubility; for this reason, an enhancement of its solubility or dissolution rate, particularly at the pH of the intestinal tract, could improve its local efficacy. Here we prepared cocrystals of this active principle with glutaric acid and so obtained a new crystalline solid representing a viable alternative to improve the physicochemical properties and thus the pharmaceutical behavior of the drug. Differential scanning calorimetry, X-ray powder diffraction, Fourier infrared spectroscopy, solid-state NMR, and scanning electron microscopy coupled to the energy-dispersive X-ray spectrometry were used to investigate the new solid-phase formation. DFT calculations at B3LYP/6-31G(d) level of theory, in the gas phase, including frequencies computation, provided a rationale for the interaction between loperamide hydrochloride and glutaric acid. The cocrystals showed improved water solubility in comparison with loperamide HCl, and the pharmaceutical formulation proposed was able to release the drug more rapidly in comparison with three reference commercial products when tested at neutral pH values.

  19. Calorimetric, FTIR and 1H NMR measurements in combination with DFT calculations for monitoring solid-state changes of dynamics of sibutramine hydrochloride.

    Science.gov (United States)

    Pajzderska, Aleksandra; Chudoba, Dorota M; Mielcarek, Jadwiga; Wąsicki, Jan

    2012-10-01

    Two forms of sibutramine hydrochloride, monohydrate and anhydrous, have been investigated by calorimetric methods, Fourier transform infrared (FTIR) absorption and (1) H nuclear magnetic resonance (NMR) measurements as well as by density functional theory (DFT) of vibrational frequencies and infrared intensities, calculations of steric hindrances and Monte Carlo simulations. The results of FTIR spectra combined with DFT calculations permitted identification of the bands corresponding to the dynamics and vibrations of water molecules. NMR study and Monte Carlo simulations revealed the occurrence of reorientation jumps of the methyl groups in sibutramine cation and also revealed that the reorientation of isopropyl group is possible only in sibutramine monohydrate hydrochloride. The hydration of sibutramine hydrochloride causes a change in the conformation of sibutramine cation. Copyright © 2012 Wiley-Liss, Inc.

  20. In vivo cell kinetic measurements in a randomized trial of continuous hyperfractionated accelerated radiotherapy with or without mitomycin C in head-and-neck cancer

    International Nuclear Information System (INIS)

    Dobrowsky, Werner; Dobrowsky, Eva; Wilson, George D.

    2003-01-01

    Purpose: Tumor cell repopulation is still considered to be a major cause of failure in radiotherapy. In this study, we investigated the influence of cell kinetic parameters on the outcome of patients treated in a randomized trial of accelerated fractionation, with or without mitomycin C, vs. conventional fractionation. Methods and Materials: Sixty-two patients were studied using administration of bromodeoxyuridine (BrdUrd), and cell kinetic parameters were measured using flow cytometry. The patients were treated with either 70 Gy for 7 weeks or 55.3 Gy for 17 continuous days (V-CHART) with or without 20 mg/m 2 mitomycin C on day 5. Results: The potential doubling time (Tpot) and labeling index (LI) failed to provide any prognostic information with regard to local control or survival. However, the duration of the S phase (Ts) revealed patients whose tumors had a long Ts had significantly worse local control (p = 0.028) and survival (p = 0.034) irrespective of treatment. A similar trend was evident within the different treatment arms particularly associated with overall survival. Conclusions: The Ts values of head-and-neck squamous cell cancers provided prognostic information that predicted clinical outcome irrespective of treatment schedule in this study. This neglected parameter of the Tpot method might provide information related to redistribution of cells during fractionated radiotherapy

  1. [Influence of polymer type on the physical properties and the release study of papaverine hydrochloride from tablets].

    Science.gov (United States)

    Kasperek, Regina; Polski, Andrzej; Sobótka-Polska, Karolina; Poleszak, Ewa

    2014-01-01

    Polymers are widely used in drug manufacturing. Researchers studied their impact on the bioavailability of active substances or on physical properties of tablets for many years. To study the influence of polymer excipients, such as microcrystalline cellulose (Avicel PH 101, Avicel PH 102), croscarmellose sodium, crospovidone or polyvinylpyrrolidone, on the release profile of papaverine hydrochloride from tablets and on the physical properties of tablets. Six series of uncoated tablets were prepared by indirect method, with previous wet granulation. Tablets contained papaverine hydrochloride and various excipients. The physical properties of the prepared granules, tablets and the release profile of papaverine hydrochloride from tablets were examined. The content of papaverine hydrochloride from the release study were determined spectrophotometrically. All tablets met the pharmacopoeia requirements during following tests: the disintegration time of tablets, uncoated tablets resistance to abrasion, the weight uniformity and dose formulations, their dimensions, the resistance to crushing of tablets and the drug substance content in the tablet. In four cases more than 80% of papaverine was released up to 2 min, in one formula it was up to 5 min, and in last one up to 10 min. Tablets containing crospovidone disintegrated faster than tablets with croscarmellose sodium. Adding gelatinized starch to the tablet composition increased the disintegration time, hardness and delayed the release of papaverine. During the wet granulation process, granules containing polyvinylpyrrolidone were characterized by a suitable flow properties and slightly prolonged disintegration time. Tablets containing Avicel PH 102 compared to tablets with Avicel PH 101 had less weight loss during the test of mechanical resistance, improved hardness and faster release profile of papaverine from tablets.

  2. Oxidation of Tetracaine Hydrochloride by Chloramine-B in Acid Medium: Kinetic Modeling

    Directory of Open Access Journals (Sweden)

    Jayachamarajapura Pranesh Shubha

    2014-01-01

    Full Text Available Tetracaine hydrochloride (TCH is one of the potent local anaesthetics. A kinetic study of oxidation of tetracaine hydrochloride by sodium N-chlorobenzenesulfonamide (chloramine-B or CAB has been carried in HClO4 medium at 303 K. The rate shows first-order dependence on [CAB]o, shows fractional–order dependence on [substrate]o, and is self-governing on acid concentration. Decrease of dielectric constant of the medium, by adding methanol, increased the rate. Variation of ionic strength and addition of benzenesulfonamide or NaCl have no significant effect on the rate. The reaction was studied at different temperatures and the activation parameters have been evaluated. The stoichiometry of the reaction was found to be 1 : 5 and the oxidation products were identified by spectral analysis. The conjugate free acid C6H5SO2NHCl of CAB is postulated as the reactive oxidizing species. The observed results have been explained by plausible mechanism and the related rate law has been deduced.

  3. Alfuzosin hydrochloride transdermal films: evaluation of physicochemical, in vitro human cadaver skin permeation and thermodynamic parameters

    Directory of Open Access Journals (Sweden)

    Satyanarayan Pattnaik

    2009-12-01

    Full Text Available Purpose: The main objective of the investigation was to develop a transdermal therapeutic system for alfuzosin hydrochloride and to study the effects of polymeric system and loading dose on the in vitro skin permeation pattern. Materials and methods: Principles of experimental design have been exploited to develop the dosage form. Ratio of ethyl cellulose (EC and polyvinyl pyrrolidone (PVP and loading dose were selected as independent variables and their influence on the cumulative amount of alfuzosin hydrochloride permeated per cm2 of human cadaver skin at 24 h (Q24, permeation flux (J and steady state permeability coefficient (P SS were studied using experimental design. Various physicochemical parameters of the transdermal films were also evaluated. Activation energy for in vitro transdermal permeation has been estimated. Results: Ratio of EC and PVP was found to be the main influential factor for all the dependent variables studied. Drug loading dose was also found to influence the dependent variables but to a lesser extent. Physicochemical parameters of the prepared films were evaluated and found satisfactory. Activation energy for alfuzosin permeation has also been estimated and reported. Conclusion: The therapeutic system was found to be dermatologically non-irritant and hence, a therapeutically effective amount of alfuzosin hydrochloride can be delivered via a transdermal route.

  4. [Clinical effects for patients with recurrent advanced non-small cell lung cancer treated with icotinib hydrochloride].

    Science.gov (United States)

    Nong, Jingying; Qin, Na; Wang, Jinghui; Yang, Xinjie; Zhang, Hui; Wu, Yuhua; Lv, Jialin; Zhang, Quan; Zhang, Shucai

    2013-05-01

    Icotinib hydrochloride is the third single target EGFR-TKI used in clinical treatment of advanced non-small cell lung cancer (NSCLC). Clinical research reports on its efficacy and survival in patients with Recurrent Advanced NSCLC are still little.The aim of this study is to evaluate the efficacy and survival of Icotinib hydrochloride for patients with advanced non-small cell lung cancer who failed to previous chemotherapy and explore the association of clinical features with the efficacy and survival. The clinical data of 60 NSCLC patients referred to the Beijing Chest Hospital, Capital Medical University from March 2009 to July 2012 were retrospectively analyzed. The overall response rate (ORR) was 45.0% and the disease control rate (DCR) was 80.0%. The median progression-free survival (PFS) time was 6.7 months. RR and PFS in female were superior to male (P=0.014, 0.013, respectively). RR, DCR in 2nd-line subgroup were superior to ≥3rd-line subgroup (P=0.020, 0.024, respectively). RR, DCR and PFS in EGFR mutation carriers were significantly superior to wild-type patients (P=0.006, Icotinib hydrochloride is effective especially in EGFR mutation carriers and well tolerated in patients with recurrent advanced non-small-cell lung cancer.

  5. Effect of humidity on the hydration behaviour of prazosin hydrochloride polyhydrate: Thermal, sorption and crystallographic study

    International Nuclear Information System (INIS)

    Kumar, Lokesh; Bansal, Arvind K.

    2011-01-01

    Highlights: → Utility of TGA to differentiate between unbound and bound water was demonstrated. → Nature of the lattice arrangement in prazosin hydrochloride polyhydrate was confirmed to be expanded (non-stoichiometric) type hydrate. → Correlation of the DSC, TGA, PXRD and DVS for dehydration of prazosin hydrochloride polyhydrate was delineated. - Abstract: In this study, hydration behaviour of prazosin hydrochloride polyhydrate was assessed using differential scanning calorimetry, thermogravimetric analysis, powder X-ray diffraction and dynamic vapour sorption techniques. Differential scanning calorimetry and thermogravimetric analysis at faster heating rate (20 o C/min) showed single step water loss, attributed to both dihydrate and unbound water. In contrast, thermogravimetric analysis at slower heating rate (1 o C/min) showed unbound and dihydrate lattice water separately, with unbound water being lost initially, followed by loss of dihydrate water. Variable vacuum and variable humidity PXRD study revealed shift in diffraction peaks to higher values on removal of unbound water. Initial PXRD patterns were regained when kept again at ambient conditions. Dynamic vapour sorption depicted type I sorption isotherm with interstitial water, indicating that polyhydrate form show reversible behaviour with change in humidity. Correlation between thermal, sorption and crystallographic data established hydration behaviour to be characteristic of expanded channel type (non-stoichiometric) hydrate.

  6. Antibiofilm Effect of Octenidine Hydrochloride on Staphylococcus aureus, MRSA and VRSA

    OpenAIRE

    Amalaradjou, Mary Anne Roshni; Venkitanarayanan, Kumar

    2014-01-01

    Millions of indwelling devices are implanted in patients every year, and staphylococci (S. aureus, MRSA and vancomycin-resistant S. aureus (VRSA)) are responsible for a majority of infections associated with these devices, thereby leading to treatment failures. Once established, staphylococcal biofilms become resistant to antimicrobial treatment and host response, thereby serving as the etiological agent for recurrent infections. This study investigated the efficacy of octenidine hydrochlorid...

  7. Protective Effect of Melatonin Against Mitomycin C-Induced Genotoxic Damage in Peripheral Blood of Rats

    Directory of Open Access Journals (Sweden)

    S. Ortega-Gutiérrez

    2009-01-01

    Full Text Available Mitomycin C (MMC generates free radicals when metabolized. We investigated the effect of melatonin against MMC-induced genotoxicity in polychromatic erythrocytes and MMC-induced lipid peroxidation in brain and liver homogenates. Rats (N = 36 were classified into 4 groups: control, melatonin, MMC, and MMC + melatonin. Melatonin and MMC doses of 10 mg/kg and 2 mg/kg, respectively, were injected intraperitoneally. Peripheral blood samples were collected at 0, 24, 48, 72, and 96 hours posttreatment and homogenates were obtained at 96 hours posttreatment. The number of micronucleated polychromatic erythrocytes (MN-PCE per 1000 PCE was used as a genotoxic marker. Malondialdehyde (MDA plus 4-hydroxyalkenal (4-HDA levels were used as an index of lipid peroxidation. The MMC group showed a significant increase in MN-PCE at 24, 48, 72, and 96 hours that was significantly reduced with melatonin begin coadministrated. No significant differences were found in lipid peroxidation. Our results indicate that MMC-induced genotoxicity can be reduced by melatonin.

  8. Determination of Dyclonine Hydrochloride by a HPLC Method and Camphor and Menthol by a GC Method in Compound Lotion

    Directory of Open Access Journals (Sweden)

    Suying Ma

    2013-01-01

    Full Text Available A high performance liquid chromatographic (HPLC method with UV detector for the determination of dyclonine hydrochloride and a gas chromatography (GC method with flame ionization detector (FID for the determination of camphor and menthol in lotion were developed. The developed HPLC method involved using a SinoChoom ODS-BP C18 reversed-phase column (5 μm, 4.6 mm × 200 mm and mobile phase consisting of acetonitrile : water : triethylamine in a ratio of 45 : 55 : 1.0; pH was adjusted to 3.5 with glacial acetic acid. The developed GC method for determination of camphor and menthol involved using an Agilent 19091J-413 capillary chromatographic column (30 m × 320 μm × 0.25 μm. The two methods were validated according to official compendia guidelines. The calibration of dyclonine hydrochloride for HPLC method was linear over the range of 20–200 μg/mL. The retention time was found at 6.0 min for dyclonine hydrochloride. The calibration of camphor and menthol of GC method was linear over the range of 10–2000 μg/mL. The retention time was found at 2.9 min for camphor and 3.05 min for menthol. The proposed HPLC and GC methods were proved to be suitable for the determination of dyclonine hydrochloride, camphor, and menthol in lotion.

  9. Effect of hydromorphone hydrochloride combined with ropivacaine for PCEA after transurethral resection of prostate on pain mediators and stress response

    Directory of Open Access Journals (Sweden)

    Yu-Lin Ma

    2017-08-01

    Full Text Available Objective: To study the effect of hydromorphone hydrochloride combined with ropivacaine for patient-controlled epidural analgesia (PCEA after transurethral resection of prostate on pain mediators and stress response. Methods: A total of 138 patients who received transurethral resection of prostate in Ankang Central Hospital between May 2014 and October 2016 were selected and randomly divided into group A and group B, group A received postoperative hydromorphone hydrochloride combined with ropivacaine for PCEA, and group B received postoperative morphine hydrochloride combined with ropivacaine for PCEA. The serum contents of pain mediators, inflammatory response cytokines and stress hormones of the two groups were detected before surgery as well as 12 h, 24 h and 48 h after surgery. Results: 12 h, 24 h and 48 h after surgery, serum SP, BK, HIS, CX3CL1, CCL2, IL-1β, TNF-α, IL-10, ACTH, CORT, TSH, FT3, FT4 and GH levels of both groups of patients were significantly higher than those before surgery, and serum SP, BK, HIS, CX3CL1, CCL2, IL-1β, TNF-α, IL-10, ACTH, CORT, TSH, FT3, FT4 and GH levels of group A were significantly lower than those of group B. Conclusion: Hydromorphone hydrochloride combined with ropivacaine for PCEA can effectively reduce the pain and stress after transurethral resection of prostate.

  10. Clinical efficacy of efonidipine hydrochloride, a T-type calcium channel inhibitor, on sympathetic activities. Examination using spectral analysis of heart rate/blood pressure variabilities and 123I-Metaiodobenzylguanidine myocardial scintigraphy

    International Nuclear Information System (INIS)

    Harada, Kenji; Nomura, Masahiro; Nishikado, Akiyoshi; Uehara, Kouzoh; Nakaya, Yutaka; Ito, Susumu

    2003-01-01

    Dihydropyridine Ca antagonists cause reflex tachycardia related to their hypotensive effects. Efonidipine hydrochloride has inhibitory effects on T-type Ca channels, even as it inhibits reflex tachycardia. In the present study, the influence of efonidipine hydrochloride on heart rate and autonomic nervous function was investigated. Using an electrocardiogram and a tonometric blood pressure measurement, autonomic nervous activity was evaluated using spectral analysis of heart rate/systolic blood pressure variability. Three protocols were used: a single dose of efonidipine hydrochloride was administered orally to healthy subjects with resting heart rate values of 75 beats/min or more (high-heart rate (HR) group) and to healthy subjects with resting heart rate values less than 75 beats/min (low-HR group); efonidipine hydrochloride was newly administered to untreated patients with essential hypertension, and autonomic nervous activity was investigated after a 4-week treatment period; and patients with high heart rate values (≥75 beats/min) who had been treated with a dihydropyridine L-type Ca channel inhibitor for 1 month or more were switched to efonidipine hydrochloride and any changes in autonomic nervous activity were investigated. In all protocols, administration of efonidipine hydrochloride decreased the heart rate in patients with a high heart rate, reduced sympathetic nervous activity, and enhanced parasympathetic nervous activity. In addition, myocardial scintigraphy with 123 I-metaiodobenzylguanidine showed significant improvement in the washout rate and heart to mediastinum (H/M) ratio of patients who were switched from other dihydropyridine Ca antagonists to efonidipine hydrochloride. Efonidipine hydrochloride inhibits increases in heart rate and has effects on the autonomic nervous system. It may be useful for treating hypertension and angina pectoris, and may also have a cardiac protective function. (author)

  11. Sinomenine Hydrochloride Protects against Polymicrobial Sepsis via Autophagy

    Directory of Open Access Journals (Sweden)

    Yu Jiang

    2015-01-01

    Full Text Available Sepsis, a systemic inflammatory response to infection, is the major cause of death in intensive care units (ICUs. The mortality rate of sepsis remains high even though the treatment and understanding of sepsis both continue to improve. Sinomenine (SIN is a natural alkaloid extracted from Chinese medicinal plant Sinomenium acutum, and its hydrochloride salt (Sinomenine hydrochloride, SIN-HCl is widely used to treat rheumatoid arthritis (RA. However, its role in sepsis remains unclear. In the present study, we investigated the role of SIN-HCl in sepsis induced by cecal ligation and puncture (CLP in BALB/c mice and the corresponding mechanism. SIN-HCl treatment improved the survival of BALB/c mice that were subjected to CLP and reduced multiple organ dysfunction and the release of systemic inflammatory mediators. Autophagy activities were examined using Western blotting. The results showed that CLP-induced autophagy was elevated, and SIN-HCl treatment further strengthened the autophagy activity. Autophagy blocker 3-methyladenine (3-MA was used to investigate the mechanism of SIN-HCl in vitro. Autophagy activities were determined by examining the autophagosome formation, which was shown as microtubule-associated protein light chain 3 (LC3 puncta with green immunofluorescence. SIN-HCl reduced lipopolysaccharide (LPS-induced inflammatory cytokine release and increased autophagy in peritoneal macrophages (PM. 3-MA significantly decreased autophagosome formation induced by LPS and SIN-HCl. The decrease of inflammatory cytokines caused by SIN-HCl was partially aggravated by 3-MA treatment. Taken together, our results indicated that SIN-HCl could improve survival, reduce organ damage, and attenuate the release of inflammatory cytokines induced by CLP, at least in part through regulating autophagy activities.

  12. Temporal effects of intramuscular administration of medetomidine hydrochloride or xylazine hydrochloride to healthy dogs on tear flow measured by use of a Schirmer tear test I.

    Science.gov (United States)

    Kanda, Teppei; Ishihara, Satoko; Oka, Miina; Sako, Kaori; Sato, Yoko; Maeta, Noritaka; Tamura, Katsutoshi; Furumoto, Kayo; Furukawa, Toshinori

    2016-04-01

    To determine the temporal effects on tear flow measurements obtained by use of a Schirmer tear test (STT) I after IM administration of various doses of medetomidine or xylazine to healthy dogs. 5 healthy purpose-bred male Beagles. Each dog received IM injections of 2.0 mL of physiologic saline (0.9% NaCl) solution (control treatment); 0.1% medetomidine hydrochloride (5, 10, 20, and 40 μg/kg), and 2.0% xylazine hydrochloride (0.5, 1.0, 2.0, and 4.0 mg/kg). Treatments were injected into the semimembranosus muscles; there was at least a 1-week interval between successive injections. Order of treatments was determined via a randomized Latin square crossover design. The STT I was performed on both eyes before (baseline) and 0.25, 0.50, 0.75, 1, 2, 3, 4, 5, 6, 7, 8, and 24 hours after each injection. STT I values decreased significantly within 45 minutes after injection of medetomidine or xylazine, which was followed by gradual recovery. The lowest mean STT I value was tear flow in a dose-related manner. Artificial tear solution or ophthalmic ointment should be used to protect the ocular surface when these drugs are administered to dogs.

  13. In vitro interactions of amantadine hydrochloride, R-(-)-deprenyl hydrochloride and valproic acid sodium salt with antifungal agents against filamentous fungal species causing central nervous system infection.

    Science.gov (United States)

    Galgóczy, L; Tóth, Liliána; Virágh, M; Papp, T; Vágvölgyi, C S

    2012-12-01

    The mortality rates of fungal infections that affect the central nervous system are high in consequence of the absence of effective antifungal drugs with good penetration across the blood-brain barrier and the blood-cerebrospinal fluid barrier. In the present work in vitro antifungal activities of three good penetrating non-antifungal drugs (amantadine hydrochloride, R-(-)-deprenyl hydrochloride, valproic acid sodium salt) and their combinations with three antifungal agents (amphotericin B, itraconazole, terbinafine) were tested with broth microdilution method against eight fungal isolates belonging to Zygomycetes (Lichtheimia corymbifera, Rhizomucor miehei, Rhizopus microsporus var. rhizopodiformis, Saksenaeavasiformis) and Aspergillus genus (A. flavus, A. fumigatus, A. nidulans, A. terreus). These are known to be possible agents of central nervous fungal infections (CNFI). When used alone, the investigated nonantifungal drugs exerted slight antifungal effects. In their combinations with antifungal agents they acted antagonistically, additively and synergistically against zygomyceteous isolates. Primarily antagonistic interactions were revealed between the investigated drugs in case of Aspergilli, but additive and synergistic interactions were also observed. The additive and synergistic combinations allowed the usage of reduced concentrations of antifungal agents to inhibit the fungal growth in our study. These combinations would be a basis of an effective, less toxic therapy for treatment of CNFI.

  14. Results of third-generation epirubicin/cisplatin/xeloda adjuvant chemotherapy in patients with radically resected gastric cancer.

    Science.gov (United States)

    Cainap, Calin; Nagy, Viorica; Seicean, Andrada; Gherman, Alexandra; Laszlo, Istvan; Lisencu, Cosmin; Nadim, Al Hajar; Constantin, Anne-Marie; Cainap, Simona

    2016-01-01

    The purpose of this study was to evaluate the efficacy and toxicity of a third-generation chemotherapy regimen in the adjuvant setting to radically operated patients with gastric cancer. This proposed new adjuvant regimen was also compared with a consecutive retrospective cohort of patients treated with the classic McDonald regimen. Starting in 2006, a non-randomized prospective phase II study was conducted at the Institute of Oncology of Cluj-Napoca on 40 patients with stage IB-IV radically resected gastric adenocarcinoma. These patients were administered a chemotherapy regimen already considered to be standard treatment in the metastatic setting: ECX (epirubicin, cisplatin, xeloda) and were compared to a retrospective control group consisting of 54 patients, treated between 2001 and 2006 according to McDonald's trial. In a previous paper, we reported toxicities and the possible predictive factors for these toxicities; in the present article, we report on the results concerning predictive factors on overall survival (OS) and disease free survival (DFS). The proposed ECX treatment was not less effective than the standard suggested by McDonald's trial. Age was an independent prognostic factor in multivariate analysis. N3 stage was an independent prognostic factor for OS and DFS. N ratio >70% was an independent predictive factor for OS and locoregional disease control. The resection margins were independent prognostic factors for OS and DFS. The proposed treatment is not less effective compared with the McDonald's trial. Age was an independent prognostic factor in multivariate analysis. N3 stage represented an independent prognostic factor and N ratio >70% was a predictive factor for OS and DFS. The resection margins were proven to be independent prognostic factors for OS and DFS.

  15. Monoclonal antibody Zt/g4 targeting RON receptor tyrosine kinase enhances chemosensitivity of bladder cancer cells to Epirubicin by promoting G1/S arrest and apoptosis.

    Science.gov (United States)

    Chen, Jun-Feng; Yu, Bi-Xia; Yu, Rui; Ma, Liang; Lv, Xiu-Yi; Cheng, Yue; Ma, Qi

    2017-02-01

    Epirubicin (EPI) is one of the most used intravesical chemotherapy agents after transurethral resection to non-muscle invasive bladder tumors (NMIBC) to prevent cancer recurrence and progression. However, even after resection of bladder tumors and intravesical chemotherapy, half of them will recur and progress. RON is a membrane tyrosine kinase receptor usually overexpressed in bladder cancer cells and associated with poor pathological features. This study aims to investigate the effects of anti-RON monoclonal antibody Zt/g4 on the chemosensitivity of bladder cells to EPI. After Zt/g4 treatment, cell cytotoxicity was significantly increased and cell invasion was markedly suppressed in EPI-treated bladder cancer cells. Further investigation indicated that combing Zt/g4 with EPI promoted cell G1/S-phase arrest and apoptosis, which are the potential mechanisms that RON signaling inhibition enhances chemosensitivity of EPI. Thus, combing antibody-based RON targeted therapy enhances the therapeutic effects of intravesical chemotherapy, which provides new strategy for further improvement of NMIBC patient outcomes.

  16. 1,2-Bis (pyridin-2-ylmethyl)sulfanyl ethane and its dimorphic hydrochloride salt

    DEFF Research Database (Denmark)

    Lennartson, A.; McKenzie, C. J.

    2011-01-01

    and are held together by C-H center dot center dot center dot N and C-H center dot center dot center dot S interactions, resulting in the formation of a three-dimensional network structure. In addition, two polymorphs of the corresponding hydrochloride salt, 2-[(2-[(pyridin-1-ium-2-ylmethyl...

  17. Replication of simian virus 40 in simian virus 40-transformed hamster kidney cells induced by mitomycin C or 60Co γ irradiation

    International Nuclear Information System (INIS)

    Rakusanova, T.; Smales, W.P.; Kaplan, J.C.; Black, P.H.

    1978-01-01

    Several clones of simian virus 40 (SV40)-transformed hamster kidney cells, which are heterogeneous for induction of infectious SV40, have been studied. SV40 yields are low after induction with 60 Co γ irradiation or mitomycin C. In order to clarify the mechanism(s) by which virus is produced in induced cells, we analyzed the replication of viral DNA and production of virion (V) antigen and infectious virus after induction in various clones as well as in lytically infected permissive cells. Cells replicating SV40 DNA or synthesizing V antigen were visualized by in situ hybridization and immunofluorescence techniques, respectively. Only some cells in induced cultures were found to produce SV40 and those which did were less efficient than lytically infected monkey cells. Mitomycin C or 60 Co γ irradiation acted by inducing more cells to replicate virus rather than by increasing the amount of SV40 released from individual cells. A greater proportion of cells could be induced to replicate SV40 DNA than to synthesize V antigen in all induced clones studied. Also, SV40 DNA replication was induced at lower doses of γ irradiation than the production of either V antigen or infectious virus suggesting that synthesis of late virus protein is more restricted in induced cells than is replication of SV40 DNA. These findings indicate that one of the effects of induction treatments on SV40-transformed hamster cells is an enhancement of the cells' capacity to support SV40 replication

  18. The 5-year incidence of bleb-related infection and its risk factors after filtering surgeries with adjunctive mitomycin C: collaborative bleb-related infection incidence and treatment study 2.

    Science.gov (United States)

    Yamamoto, Tetsuya; Sawada, Akira; Mayama, Chihiro; Araie, Makoto; Ohkubo, Shinji; Sugiyama, Kazuhisa; Kuwayama, Yasuaki

    2014-05-01

    To report the 5-year incidence of bleb-related infection after mitomycin C-augmented glaucoma filtering surgery and to investigate the risk factors for infections. Prospective, observational cohort study. A total of 1098 eyes of 1098 glaucoma patients who had undergone mitomycin C-augmented trabeculectomy or trabeculectomy combined with phacoemulsification and intraocular lens implantation performed at 34 clinical centers. Patients were followed up at 6-month intervals for 5 years, with special attention given to bleb-related infections. The follow-up data were analyzed via Kaplan-Meier survival analysis and the Cox proportional hazards model. Incidence of bleb-related infection over 5 years and risk factors for infections. Of the 1098 eyes, a bleb-related infection developed in 21 eyes. Kaplan-Meier survival analysis revealed that the incidence of bleb-related infection was 2.2±0.5% (cumulative incidence ± standard error) at the 5-year follow-up for all cases, whereas it was 7.9±3.1% and 1.7±0.4% for cases with and without a history of bleb leakage, respectively (P = 0.000, log-rank test). When only eyes with a well-functioning bleb were counted, it was 3.9±1.0%. No differences were found between the trabeculectomy cases and the combined surgery cases (P = 0.398, log-rank test) or between cases with a fornix-based flap and those with a limbal-based flap (P = 0.651, log-rank test). The Cox model revealed that a history of bleb leakage and younger age were risk factors for infections. The 5-year cumulative incidence of bleb-related infection was 2.2±0.5% in eyes treated with mitomycin C-augmented trabeculectomy or trabeculectomy combined with phacoemulsification and intraocular lens implantation in our prospective, multicenter study. Bleb leakage and younger age were the main risk factors for infections. Copyright © 2014 American Academy of Ophthalmology. Published by Elsevier Inc. All rights reserved.

  19. Quantitative estimation of itopride hydrochloride and rabeprazole sodium from capsule formulation

    OpenAIRE

    Pillai S; Singhvi I

    2008-01-01

    Two simple, accurate, economical and reproducible UV spectrophotometric methods and one HPLC method for simultaneous estimation of two component drug mixture of itopride hydrochloride and rabeprazole sodium from combined capsule dosage form have been developed. First developed method involves formation and solving of simultaneous equations using 265.2 nm and 290.8 nm as two wavelengths. Second method is based on two wavelength calculation, wavelengths selected for estimation of itopride hydro...

  20. SIMULTANEOUS SPECTROPHOTOMETRIC DETERMINATION OF MONTELUKAST SODIUM AND BAMBUTEROL HYDROCHLORIDE IN TABLETS

    OpenAIRE

    Patel Satish A; Patel Dhara J; Patel Natavarlal J.

    2011-01-01

    The present manuscript describe simple, sensitive, rapid, accurate, precise and economical first derivative spectrophotometric method for the simultaneous determination of montelukast sodium and bambuterol hydrochloride in combined tablet dosage form. The derivative spectrophotometric method was based on the determination of both the drugs at their respective zero crossing point (ZCP). The first order derivative spectra was obtained in chloroform and the determinations were made at 241 nm (ZC...

  1. Simultaneous determination of hydrochlorothiazide and benazepril hydrochloride or amiloride hydrochloride in presence of hydrochlorothiazide impurities: chlorothiazide and salamide by HPTLC method.

    Science.gov (United States)

    Naguib, Ibrahim A; Abdelaleem, Eglal A; Zaazaa, Hala E; Draz, Mohammed E

    2015-01-01

    Simple, selective and sensitive high-performance thin layer chromatographic (HPTLC) method has been developed and validated for the simultaneous determination of hydrochlorothiazide (HCZ) in the presence of its impurities (chlorothiazide (CT) and salamide (DSA)), in two quaternary mixtures with benazepril hydrochloride (BZ) or amiloride hydrochloride (AM). The separation was carried out on HPTLC silica gel 60 F254 using ethyl acetate-methanol-glacial acetic acid (85:2:0.3 v/v/v) followed by densitometric measurement of bands at 240 nm for the first mixture containing HCZ, CT, DSA, BZ and by using ethyl acetate-methanol-water-ammonia (90:10:5:3 v/v/v) followed by densitometric measurement at 278 nm for the second mixture containing HCZ, CT, DSA, AM. Calibration curves were constructed in the range of (0.2-1.8 µg/band) and (0.4-2.2 µg/band) with good accuracy for HCZ and BZ, respectively, for the first mixture and in the range of (0.6-1.8 µg/band) and (0.4-2.4 µg/band) with good accuracy for HCZ and AM, respectively, for the second mixture. The developed method was validated according to ICH guidelines and demonstrated good accuracy and precision. Moreover, the methods were successfully applied for the determination of HCZ and BZ and AM in pure form and pharmaceutical dosage forms. The results were statically compared with the reported methods with no significant difference, indicating the ability of the proposed method to be used for routine analysis of drug product. © The Author [2014]. Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

  2. Fate and transport of the ß-adrenergic agonist ractopamine hydrochloride in soil-water systems

    Science.gov (United States)

    The feed additive ractopamine hydrochloride was fortified at four concentrations into batch vials containing soils that differed in both biological activity and organic matter (OM). Sampling of the liquid layer for 14 d demonstrated that ractopamine rapidly dissipated from the liquid layer. Less t...

  3. Relationship between icotinib hydrochloride exposure and clinical outcome in Chinese patients with advanced non-small cell lung cancer.

    Science.gov (United States)

    Ni, Jun; Liu, Dong-Yang; Hu, Bei; Li, Chen; Jiang, Ji; Wang, Han-Ping; Zhang, Li

    2015-09-01

    The current study was conducted to explore the relationship between icotinib hydrochloride exposure and therapeutic effects in Chinese patients with advanced non-small cell lung cancer (NSCLC) who were treated with icotinib hydrochloride. A total of 30 patients with NSCLC who were treated with icotinib hydrochloride were chosen from a single-center, open-label, phase 1 dose escalation clinical trial. Different doses of icotinib hydrochloride were administered orally for 28 consecutive days in different groups until disease progression or unacceptable toxicities occurred. Blood samples were collected during the first treatment cycle (day 1-28) for the pharmacokinetic analysis. Tumor responses were assessed according to the Response Evaluation Criteria in Solid Tumors (RECIST). The plasma concentrations of icotinib hydrochloride were assessed by liquid chromatography-mass spectrometry. Thirty patients with a median age of 56 years old (50% of whom were female) were enrolled. For single-dose treatment, the plasma pharmacokinetics demonstrated a median time to maximum concentration of 0.5 to 4 hours and a mean terminal elimination half-life of 6.21±3.44 hours at the 150-mg dose and 10.1±12.18 hours at the 200-mg dose. For multiple-dose treatment, the last measurable concentration (Clast ) was 708±368.67 ng/mL at the 150-mg every 12 hours, 782.73±618.18 ng/mL at the 200-mg every 12 hours, and 1162±658.44 ng/mL at the 125-mg every 8 hours; the under the concentration curve from time 0 to Clast was 14.5±2.43 hour*mg/mL, 13.2±2.5 hour*mg/mL, and 12.19±2.47 hour*mg/mL, respectively. At the dose of 150 mg every 12 hours, 1 patient with an epidermal growth factor receptor (EGFR) exon 19 deletion achieved a complete response for 10 months; another patient who carried the EGFR exon 19 deletion achieved stable disease for 6 months. Univariate analysis demonstrated that the time to maximum plasma concentration (Tmax ) after a single dose of icotinib hydrochloride was

  4. 53BP1 loss suppresses the radiosensitizing effect of icotinib hydrochloride in colorectal cancer cells.

    Science.gov (United States)

    Huang, Ai; Yao, Jing; Liu, Tao; Lin, Zhenyu; Zhang, Sheng; Zhang, Tao; Ma, Hong

    2018-04-01

    This study aimed to investigate the influence of the expression of P53-binding protein 1 (53BP1), a key component in DNA damage repair pathways, on the radiosensitizing effect of icotinib hydrochloride in colorectal cancer and to elucidate the mechanisms underlying this influence. Real-time RT-PCR and Western blotting were performed to verify the gene-knockout effect of 53BP1 small hairpin RNA (ShRNA), and colony formation assay was employed to investigate the influence of 53BP1 downregulation on the radiosensitizing effect of icotinib hydrochloride in HCT116 cells. Cell apoptosis, cell cycle distributions, and histone H2AX (γ-H2AX) fluorescence foci after 53BP1 knockdown were evaluated. Relative protein expression in the ataxia telangiectasia mutated kinase (ATM)-checkpoint kinase-2 (CHK2)-P53 pathway was measured by Western blot analysis to unravel the molecular mechanisms linking the pathway to the above phenomena. Icotinib hydrochloride increased the radiosensitivity of HCT116 cells; however, this effect was suppressed by the downregulation of 53BP1 expression, a change that inhibited cell apoptosis, increased the percentage of HCT116 cells arrested in S-phase and inhibited the protein expression of key molecules in the ATM-CHK2-P53 apoptotic pathway. Our studies confirmed that the loss of 53BP1 serves as a negative regulator of the radiosensitizing effect of icotinib in part by suppressing the ATM-CHK2-P53 apoptotic pathway.

  5. Effects of 1% cyclopentolate hydrochloride on anterior segment parameters obtained with Pentacam in young adults

    Directory of Open Access Journals (Sweden)

    Ceyhun Arici

    2014-08-01

    Full Text Available Purpose: To investigate the effects of topically applied 1% cyclopentolate hydrochloride on anterior segment parameters obtained with a Pentacam rotating Scheimpflug camera in healthy young adults. Methods: Anterior segment analyses of 25 eyes from 25 young adults (Group 1, before and after 45 min of 1% cyclopentolate hydrochloride application, were performed. For a control group (cycloplegia-free, Group 2, 24 eyes of 24 age- and sex-matched healthy cases were evaluated twice at 45 min intervals. The results obtained from the groups were compared statistically. Results: The mean ages of the groups were 23.04 ± 3.42 (range, 18-29 and 22.4 ± 2.05 (range, 18-27 years for Groups 1 and 2, respectively (p=0.259. In Group 1, measurements between the two analyses were significantly different for the values of anterior chamber depth (ACD, anterior chamber angle (ACA, and anterior chamber volume (ACV (p<0.05, whereas no statistical difference was found for the central corneal thickness (CCT and keratometry (K1, K2 measurements. In Group 2, none of these parameters were statistically different between the two analyses. Conclusions: Topically applied 1% cyclopentolate hydrochloride caused an increase in the ACD and ACV values, and a decrease in the ACA value. However, it had no significant effect on the CCT and keratometry measurements. It is important to consider these effects when using the Pentacam device on young adults with cycloplegia and when applying it for various reasons.

  6. Partial Tenon’s capsule resection with adjunctive mitomycin C in Ahmed glaucoma valve implant surgery

    Science.gov (United States)

    Susanna, R

    2003-01-01

    Aim: To verify if partial intraoperative Tenon’s capsule resection (PTCR) with adjunctive mitomycin C is effective in developing thin, avascular blebs in eyes undergoing Ahmed glaucoma valve insertion, and to assess the efficacy and safety of this procedure. Methods: A multicentre, prospective, alternating case assignment, investigator unmasked, parallel group, comparative interventional study was conducted in four Latin American countries (Argentina, Brazil, Colombia, and Peru). Ahmed glaucoma valve implant insertion with PTCR (group A) and without PCTR (group B) was performed in neovascular glaucomatous eyes without previous surgery. Adjunctive mitomycin C (MMC) was used in both groups. Patients were examined 1 day, 10 days, 1 month, 2 months, 3 months, 6 months, and 1 year following the surgery. Intraocular pressure (IOP) and the appearance of the bleb were evaluated at each examination. Appearance of the bleb was classified at both the 1 month mark and last examinations into one of three groups: flat and vascularised; elevated avascular; or elevated and not avascular. Results: 92 eyes from 92 patients were included in the study. The preoperative mean IOP was 50.0 (SD 10.5) mm Hg in group A and 48.4 (11.7) in group B (p>0.05). Statistically significant IOP reductions were observed at all periods of follow up. 12 months after surgery, the mean IOP was 17.2 (5.0) mm Hg in group A and 18.3 (8.7) mm Hg in group B (p>0.05). A hypertensive phase occurred in 40.0% in group A and in 46.8% in group B (p>0.05). At the 1 month and the final follow up, the blebs in all eyes were considered elevated and not avascular. The success rate (IOP⩽21 mm Hg) at 1 year after surgery was 70.4% in group A and 77.7% in group B (p>0.05). Overall, 74.2% of the patients achieved an IOP ⩽21 mm Hg and 55.2% an IOP⩽17 mm Hg, with or without additional medication administered to lower IOP. The incidence of complications was similar in both groups. Conclusions: In eyes undergoing Ahmed

  7. Self-assembled nanoparticles of cholesterol-conjugated carboxymethyl curdlan as a novel carrier of epirubicin

    International Nuclear Information System (INIS)

    Li Lei; Gao Fuping; Tang Hongbo; Ba, Yonggang; Li Ruifeng; Li Xuemin; Liu Lingrong; Wang Yinsong; Zhang Qiqing

    2010-01-01

    The purpose of this study was to develop nanoparticles made of cholesterol-conjugated carboxymethyl curdlan (CCMC) entrapping epirubicin (EPB) and establish their in vitro and in vivo potential. CCMC was synthesized and characterized by Fourier transform infrared spectra (FT-IR) and proton nuclear magnetic resonance spectra ( 1 H NMR). The degrees of substitution (DS) of the cholesterol moiety were 2.3, 3.5 and 6.4, respectively. EPB-loaded CCMC-3.5 nanoparticles were prepared by the remote loading method. The physicochemical characteristics, drug loading efficiency and drug release kinetics of EPB-loaded CCMC-3.5 nanoparticles were characterized. The in vitro release profiles revealed that EPB release was sensitive to the pH as well as the drug loading contents. The cellular cytotoxicity and cellular uptake were accessed by using human cervical carcinoma (HeLa) cells. The EPB-loaded CCMC-3.5 nanoparticles were found to be more cytotoxic and have a broader distribution within the cells than the free EPB. The in vivo pharmacokinetics and biodistribution were investigated after intravenous injection in rats. Promisingly, a 4.0-fold increase in the mean residence time (MRT), a 4.31-fold increase in the half-life time and a 6.69-fold increase in the area under the curve (AUC 0→∞ ) of EPB were achieved for the EPB-loaded CCMC-3.5 self-assembled nanoparticles compared with the free EPB. The drug level was significantly increased in liver at 24 and 72 h; however, it decreased in heart at 8 and 24 h compared with the free EPB. The in vivo anti-tumor study indicated that the EPB-loaded CCMC-3.5 self-assembled nanoparticles showed greater anti-tumor efficacy than the free EPB. Taken together, the novel CCMC self-assembled nanoparticles might have potential application as anti-cancer drug carriers in a drug delivery system due to good results in vitro and in vivo.

  8. Formulation, preparation, and evaluation of novel orally disintegrating tablets containing taste-masked naproxen sodium granules and naratriptan hydrochloride.

    Science.gov (United States)

    Stange, Ulrike; Führling, Christian; Gieseler, Henning

    2014-04-01

    The purpose of this study was to develop and manufacture novel freeze-dried orally disintegrating tablets (ODTs) for migraine therapy containing taste-masked naproxen sodium and naratriptan hydrochloride. The formulation was optimized based on freeze-drying of sucrose solutions with different binders (hydroxyethylstarch, sodium alginate, methylcellulose, and gelatin) and varying amounts of Eudragit® E-coated naproxen sodium granules. Excellent product performance of the ODTs in terms of hardness and disintegration time (hydrochloride, and taste-masked naproxen sodium granules corresponding to 200 mg of naproxen were then added, and the final batches of ODTs for migraine therapy were produced. The ODTs were fully characterized, and subsequently stored for 1 month at room temperature and at 40°C. The amount of free naproxen sodium after freeze-drying and storage was below the threshold bitterness value, and the coating remained intact. Additionally, the particle size distribution of taste-masked granules was preserved, and more than 90 % naproxen sodium was released after 30 min. Naratriptan hydrochloride was dissolved immediately after disintegration, hence facilitating buccal absorption of the active pharmaceutical ingredient. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.

  9. Ractopamine hydrochloride on performance and carcass traits of confined Nellores cattle

    Directory of Open Access Journals (Sweden)

    João Luis Kill

    2015-10-01

    Full Text Available The effect of four levels of inclusion (0; 450; 900 and 1,350g T-1 of Ractopamine hydrochloride was assessed concerning weight gain, feed conversion, dry matter intake, carcass traits and quality of castrated male cattle meat in confinement. Forty Nellore steers were used, with an average age of 26 months and initial average weight of 423.4±2.7kg, in a randomized block experimental design with four treatments and ten replications. The diet was fixed with the ratio of forage to concentrate dry matter of 75.3:24.7. A Linear positive effect observed was the inclusion of Ractopamine on daily weight gain and linear negative effect on feed conversion, highlighting the improvements with the increasing inclusion of Ractopamine hydrochloride. In relation to carcass traits, the linear effect was negative for fat thickness and no differences were found regarding the hot carcass weight ; carcass yield; area, width and depth of rib eye area of the Longissimus dorsi muscle, and noble courts. In relation to dry matter intake, the comparison of the treatments demonstrated that Ractopamine didn't influence negatively, which highlights its positive effect on the animal performance. The use of Ractopamine improves performance and decreases de amount of superficial fat in male nellore carcass in confinement.

  10. Evaluating tamsulosin hydrochloride-released microparticles prepared using single-step matrix coating.

    Science.gov (United States)

    Maeda, Atsushi; Shinoda, Tatsuki; Ito, Naoki; Baba, Keizo; Oku, Naoto; Mizumoto, Takao

    2011-04-15

    The objective of the present study was to determine the optimum composition for sustained-release of tamsulosin hydrochloride from microparticles intended for orally disintegrating tablets. Microparticles were prepared from an aqueous ethylcellulose dispersion (Aquacoa®), and an aqueous copolymer based on ethyl acrylate and methyl methacrylate dispersion (Eudragit®) NE30D), with microcrystalline cellulose as core particles with a fluidized bed coating process. Prepared microparticles were about 200 μm diameter and spherical. The microparticles were evaluated for in vitro drug release and in vivo absorption to assess bioequivalence in a commercial product, Harnal® pellets. The optimum ratio of Aquacoat® and Eudragit® NE30D in the matrix was 9:1. We observed similar drug release profiles in microparticles and Harnal® pellets. Higuchi model analysis of the in vitro drug release from microparticles was linear up to 80% release, typical of Fickian diffusion sustained-release profile. The in vivo absorption properties from microparticles were comparable to Harnal® pellets, and there was a linear relationship between in vitro drug release and in vivo drug release. In conclusion, this development produces microparticles in single-step coating, that provided a sustained-release of tamsulosin hydrochloride comparable to Harnal® pellets. Copyright © 2011 Elsevier B.V. All rights reserved.

  11. Effect of budesonide and cetirizine hydrochloride on neurotrophic factor, airway function and chemokines CCL17 and CCL22 in patients with allergic rhinitis

    Directory of Open Access Journals (Sweden)

    Xiang Xu

    2017-11-01

    Full Text Available Objective: To investigate the effect of budesonide combined with cetirizine hydrochloride on neurotrophic factor, airway function and chemokines CCL17 and CCL12 in patients with allergic rhinitis. Methods: A total of 123 patients with Allergic Rhinitis were randomly divided into three groups, A group treated with budesonide nasal spray, B group treated with cetirizine hydrochloride, C group treated with budesonide combined with cetirizine hydrochloride, then the Neurotrophic factors, airway function indexes and chemokines CCL17 and CCL12 levels in three groups were compared. Results: Before the treatments, the three groups of patients in neurotrophic factor, airway function index and chemokines CCL17, CCL22 have no differences, Compared with before the treatments, after receiving different treatments, the three groups of patients in all indicators were Showed significant differences. In the indexes of neurotrophic factor (NGF, BDNF, NT-3mRNA expression, there was no significant difference between group A and group B, and group C was lower than group A and B. In airway function indexes (FVC, FEV1 and PEF, A group was significantly higher than B group, C group was significantly higher than A group; In the chemokines CCL17 and CCL22 indicators, C group was lower than A group, A group was lower than B group, the difference was significant. Conclusions: Budesonide combined with cetirizine hydrochloride in the treatment of Allergic Rhinitis, can effectively control the patients' neurotrophic factor, pulmonary ventilation and chemokine CC17, CCL22 indicators, the effect is better than Budesonide alone or Cetirizine hydrochloride.

  12. A comparative study on the aggregating effects of guanidine thiocyanate, guanidine hydrochloride and urea on lysozyme aggregation

    Energy Technology Data Exchange (ETDEWEB)

    Emadi, Saeed, E-mail: emadi@iasbs.ac.ir; Behzadi, Maliheh

    2014-08-08

    Highlights: • Lysozyme aggregated in guanidine thiocyanate (1.0 and 2.0 M). • Lysozyme aggregated in guanidine hydrochloride (4 and 5 M). • Lysozyme did not aggregated at any concentration (0.5–5 M) of urea. • Unfolding pathway is more important than unfolding per se in aggregation. - Abstract: Protein aggregation and its subsequent deposition in different tissues culminate in a diverse range of diseases collectively known as amyloidoses. Aggregation of hen or human lysozyme depends on certain conditions, namely acidic pH or the presence of additives. In the present study, the effects on the aggregation of hen egg-white lysozyme via incubation in concentrated solutions of three different chaotropic agents namely guanidine thiocyanate, guanidine hydrochloride and urea were investigated. Here we used three different methods for the detection of the aggregates, thioflavin T fluorescence, circular dichroism spectroscopy and atomic force microscopy. Our results showed that upon incubation with different concentrations (0.5, 1.0, 2.0, 3.0, 4.0, 5.0 M) of the chemical denaturants, lysozyme was aggregated at low concentrations of guanidine thiocyanate (1.0 and 2.0 M) and at high concentrations of guanidine hydrochloride (4 and 5 M), although no fibril formation was detected. In the case of urea, no aggregation was observed at any concentration.

  13. Simple spectrophotometric methods for determination of fluoxetine and clomipramine hydrochlorides in dosage forms and in some post-mortem biological fluids samples

    Directory of Open Access Journals (Sweden)

    Emam A. Ali

    2016-12-01

    Full Text Available Sensitive, simple and rapid spectrophotometric methods for micro determination of fluoxetine hydrochloride (FLU and clomipramine hydrochloride (CLO. The methods are based on the reaction between the examined drugs and acid dyes, namely; bromocresol green (BCG, phenol red (PhR and metanil yellow (MY producing yellow ion-pair complexes followed by their extraction with methylene chloride and measured at 412, 407 and 409 nm for FLU with BCG, PhR and MY, respectively; whereas for CLO at 409, 406 and 407 nm, respectively. All variables that affect the performance of the proposed methods were carefully studied and optimized. Beer’s law was obeyed in the concentration ranges 0.86–24.32 μg/mL, 8.64–41.30 μg/mL, 0.86–34.76 μg/mL for FLU and 1.75–24.55 μg/mL, 7.0–50 μg/mL, 1.65–34.78 μg/mL for CLO using BCG, PhR and MY respectively. The methods were validated in terms of accuracy and precision. The proposed methods were successfully applied to the determination of fluoxetine hydrochloride and clomipramine hydrochloride in pure samples, pharmaceutical formulations, spiked post-mortem urine and blood samples.

  14. Short-term therapeutic effects of combined therapy with metformin hydrochloride for aplastic anemia

    Directory of Open Access Journals (Sweden)

    Xue-chun LU

    2012-03-01

    Full Text Available Objective To screen and select new drugs for aplastic anemia (AA and evaluate their clinical efficacy by clinical bioinformatics methods. Methods First, we established genome expression profiles of AA patients, and conducted similarity analyses with the pharmacogenomics database to screen and select drugs with possible efficacy. Intractable AA patients who received immunosuppressors and/or androgen for more than six months showing no clinical efficacy were enrolled in the study to evaluate therapeutic effects of the therapeutic regime. Clinical efficacy and adverse effects were evaluated after six months. Results The clinical bioinformatics results showed therapeutic effects of metformin hydrochloride on AA. Forty-three intractable AA patients (15 with severe AA were treated with metformin hydrochloride combined with cyclosporin A (CsA and stanozolol. Twenty-seven transfusion-dependent patients (100% became transfusion independent after a 6-month therapy. The hemoglobin level completely returned to normal in 37 out of 40 anemia patients (92.5%. In the 40 patients with platelet count lower than 20×109/L, the platelet count of 28 patients (90.3% increased to higher than 50×109/L. The white cell count increased to higher than 3.5×109/L in 30 out of 35 patients (88.6% with white cell count lower than 2.5×109/L. Among 40 anemic patients, 1 was found to have abnormal renal function, but it recovered to the normal range after ending CsA treatment. Eighteen patients were found to have elevated transaminase levels which were lowered to normal range after using liver protectants and reducing the dosage of stanozolol. There were no instances of hypoglycemia in all patients throughout the treatment. Conclusion Combination of metformin hydrochloride, CsA and stanozolol is effective in refractory aplastic anemia with acceptable toxicity.

  15. Topical Mitomycin C and Radiation Induce Conjunctival DNA-Polyploidy

    Directory of Open Access Journals (Sweden)

    Olaf Cartsburg

    2001-01-01

    Full Text Available Introduction: Atypical cell changes often occur following treatment of premalignant or malignant conjunctival neoplasias with topical mitomycin C (MMC and/or radiation. These reactive, non‐neoplastic alterations of the conjunctival epithelium can be a differential diagnostic problem. Our aim was to investigate changes in the nuclear DNA‐distribution of conjunctival epithelial cells after MMC‐ and radiation therapy by DNA‐image‐cytometry. Methods: Conjunctival brush smears were obtained from 13 patients (13 eyes with squamous cell carcinomas and six patients (6 eyes with conjunctival malignant melanomas in situ before, during and after treatment. The patients were treated with MMC‐drops (0.02% or 0.04% alone (n=12, with radiation therapy (n=3 or both (n=4. At first, the obtained brush smears were evaluated by cytology. Secondly, after Feulgen restaining, the DNA content of reactively changed cells was determined using the AutoCyte‐QUIC‐DNA® workstation. Results: We observed euploid DNA‐polyploidy and cytomorphological changes in all patients (19/19. We considered these alterations as reactive to treatment. Four patients showed their greatest DNA‐stemline at 4c and 15 patients at 8c. This effect was observed during and following MMC‐drops and/or radiation and remained stable in 94% of all patients after a mean follow‐up of 22.5 months (SD 15.4. In five cases image cytometry additionally demonstrated DNA‐stemline aneuploidy as an evidence of tumor recurrence. Conclusion: Measurements of DNA‐content revealed euploid polyploidisation of morphological suspicious but benign squamous cells which is the biologic correlate of well known secondary morphologic changes following topical chemotherapy and/or radiation. DNA‐image‐cytometry is a useful tool in the differention of euploid polyploidization as a sign of reactive cell changes following treatment and tumor recurrences.

  16. A study of selective spectrophotometric methods for simultaneous determination of Itopride hydrochloride and Rabeprazole sodium binary mixture: Resolving sever overlapping spectra

    Science.gov (United States)

    Mohamed, Heba M.

    2015-02-01

    Itopride hydrochloride (IT) and Rabeprazole sodium (RB) are co-formulated together for the treatment of gastro-esophageal reflux disease. Three simple, specific and accurate spectrophotometric methods were applied and validated for simultaneous determination of Itopride hydrochloride (IT) and Rabeprazole sodium (RB) namely; constant center (CC), ratio difference (RD) and mean centering of ratio spectra (MCR) spectrophotometric methods. Linear correlations were obtained in range of 10-110 μg/μL for Itopride hydrochloride and 4-44 μg/mL for Rabeprazole sodium. No preliminary separation steps were required prior the analysis of the two drugs using the proposed methods. Specificity was investigated by analyzing the synthetic mixtures containing the two cited drugs and their capsules dosage form. The obtained results were statistically compared with those obtained by the reported method, no significant difference was obtained with respect to accuracy and precision. The three methods were validated in accordance with ICH guidelines and can be used for quality control laboratories for IT and RB.

  17. Hydrostatic pressure enhances mitomycin C induced apoptosis in urothelial carcinoma cells.

    Science.gov (United States)

    Chen, Shao-Kuan; Chung, Chih-Ang; Cheng, Yu-Che; Huang, Chi-Jung; Ruaan, Ruoh-Chyu; Chen, Wen-Yih; Li, Chuan; Tsao, Chia-Wen; Hu, Wei-Wen; Chien, Chih-Cheng

    2014-01-01

    Urothelial carcinoma (UC) of the bladder is the second most common cancer of the genitourinary system. Clinical UC treatment usually involves transurethral resection of the bladder tumor followed by adjuvant intravesical immunotherapy or chemotherapy to prevent recurrence. Intravesical chemotherapy induces fewer side effects than immunotherapy but is less effective at preventing tumor recurrence. Improvement to intravesical chemotherapy is, therefore, needed. Cellular effects of mitomycin C (MMC) and hydrostatic pressure on UC BFTC905 cells were assessed. The viability of the UC cells was determined using cellular proliferation assay. Changes in apoptotic function were evaluated by caspase 3/7 activities, expression of FasL, and loss of mitochondrial membrane potential. Reduced cell viability was associated with increasing hydrostatic pressure. Caspase 3/7 activities were increased following treatment of the UC cells with MMC or hydrostatic pressure. In combination with 10 kPa hydrostatic pressure, MMC treatment induced increasing FasL expression. The mitochondria of UC cells displayed increasingly impaired membrane potentials following a combined treatment with 10 μg/ml MMC and 10 kPa hydrostatic pressure. Both MMC and hydrostatic pressure can induce apoptosis in UC cells through an extrinsic pathway. Hydrostatic pressure specifically increases MMC-induced apoptosis and might minimize the side effects of the chemotherapy by reducing the concentration of the chemical agent. This study provides a new and alternative approach for treatment of patients with UC following transurethral resection of the bladder tumor. Copyright © 2014 Elsevier Inc. All rights reserved.

  18. Use of an in vitro human skin permeation assay to assess bioequivalence of two topical cream formulations containing butenafine hydrochloride (1%, w/w).

    Science.gov (United States)

    Mitra, Amitava; Kim, Nanhye; Spark, Darren; Toner, Frank; Craig, Susan; Roper, Clive; Meyer, Thomas A

    2016-12-01

    The primary objective of this work was to investigate, using an in vitro human skin permeation study, whether changes in the excipients of butenafine hydrochloride cream would have any effect on bioperformance of the formulation. Such in vitro data would be a surrogate for any requirement of a bioequivalence (BE) study to demonstrate formulation similarity. A LC-MS/MS method for quantitation of butenafine in various matrices was developed and validated. A pilot study was performed to validate the in vitro skin permeation methodology using three cream formulations containing butenafine hydrochloride at concentrations of 0.5, 1.0 and 1.5% (w/w). Finally, a definitive in vitro human skin permeation study was conducted, comparing the extent of butenafine hydrochloride permeation from the new formulation to that from the current formulation. The results of the study comparing the two formulations showed that there was no statistically significant difference in the extent of butenafine permeation into human skin. In conclusion, these in vitro data demonstrated that the formulation change is likely to have no significant impact on the bioperformance of 1% (w/w) butenafine hydrochloride cream. Copyright © 2016 Elsevier Inc. All rights reserved.

  19. Effect of venlafaxine hydrochloride in different preparations of isolated guinea-pig and rat organ tissues.

    Science.gov (United States)

    Velasco, A; Arruza, A; Maroto, M; Carvajal, A; Fernández del Busto, E; García del Pozo, J

    1999-04-01

    A study was undertaken to know better the effects of venlafaxine hydrochloride on the responses of isolated rat vas deferens to noradrenaline and dopamine, those of isolated rat uterus to serotonin and histamine, and those of isolated guinea-pig ileum to acetylcholine and histamine. Venlafaxine hydrochloride increased the response of rat vas deferens to noradrenaline but not to dopamine. Venlafaxine did not alter the response of rat isolated uterus to serotonin. In rat uterus, venlafaxine did not modify the response to histamine but was able to increase it in guinea-pig ileum. An anticholinergic effect was observed with the lowest concentration tested. Although venlafaxine is a selective serotonine reuptake inhibitor in the central nervous system, serotonin uptake was not seen in the rat uterus. The anticholinergic effects observed in the present study might be consistent with some of the side-effects associated with venlafaxine.

  20. Simultaneous determination of eperisone hydrochloride and paracetamol in mouse plasma by high performance liquid chromatography-photodiode array detector.

    Science.gov (United States)

    Locatelli, Marcello; Cifelli, Roberta; Di Legge, Cristina; Barbacane, Renato Carmine; Costa, Nicola; Fresta, Massimo; Celia, Christian; Capolupo, Carlo; Di Marzio, Luisa

    2015-04-03

    This paper reports the validation of a quantitative high performance liquid chromatography-photodiode array (HPLC-PDA) method for the simultaneous analysis, in mouse plasma, of eperisone hydrochloride and paracetamol by protein precipitation using zinc sulphate-methanol-acetonitrile. The analytes were resolved on a Gemini C18 column (4.6 mm × 250 mm; 5 μm particle size) using a gradient elution mode with a run time of 15 min, comprising re-equilibration, at 60°C (± 1°C). The method was validated over the concentration range from 0.5 to 25 μg/mL for eperisone hydrochloride and paracetamol, in mouse plasma. Ciprofloxacin was used as Internal Standard. Results from assay validations show that the method is selective, sensitive and robust. The limit of quantification of the method was 0.5 μg/mL for eperisone hydrochloride and paracetamol, and matrix-matched standard curves showed a good linearity, up to 25 μg/mL with correlation coefficients (r(2))≥ 0.9891. In the entire analytical range the intra and inter-day precision (RSD%) values were ≤ 1.15% and ≤ 1.46% for eperisone hydrochloride, and ≤ 0.35% and ≤ 1.65% for paracetamol. For both analytes the intra and inter-day trueness (bias%) values ranged, respectively, from -5.33% to 4.00% and from -11.4% to -4.00%. The method was successfully tested in pharmacokinetic studies after oral administration in mouse. Furthermore, the application of this method results in a significant reduction in terms of animal number, dosage, and improvement in speed, rate of analysis, and quality of pharmacokinetic parameters related to serial blood sampling. Copyright © 2015 Elsevier B.V. All rights reserved.

  1. Safety and efficacy of atovaquone and proguanil hydrochloride for the prophylaxis of Plasmodium falciparum malaria in South Africa.

    Science.gov (United States)

    van der Berg, J D; Duvenage, C S; Roskell, N S; Scott, T R

    1999-04-01

    The objective of this study was to determine the safety and efficacy of atovaquone and proguanil hydrochloride combination therapy for the prophylaxis of Plasmodium falciparum malaria in at-risk nonimmune subjects in South Africa. This open-label trial was conducted at research sites in South Africa during the main malaria transmission season, February through July. The study volunteers were temporarily living in, or traveling to, a malaria-endemic area. They received I tablet of 250 mg atovaquone and 100 mg proguanil hydrochloride once daily for up to 10 weeks. Subjects were monitored using sequential clinical and laboratory assessments. Thick blood smears were stained and evaluated by a central laboratory. An immunochromatographic test for P. falciparum was also used for on-site patient management. Prophylactic success was summarized using a 95% confidence interval for the proportion of subjects who did not develop parasitemia or who withdrew due to a treatment-related adverse event. A total of 175 subjects (15% women) were enrolled in the trial. The mean duration of drug exposure was 8.9 weeks. The combination of atovaquone and proguanil hydrochloride was well tolerated. The most frequently reported adverse events considered possibly related to study treatment were headache (7%), abdominal pain (2%), increased cough (2%), and skin disorder (2%). No serious adverse events were reported, and no treatment-emergent effects were noted for any laboratory variables. One subject who was noncompliant with therapy developed parasitemia, and 3 subjects withdrew due to a treatment-related adverse event (2 subjects with headache and 1 with nausea and dizziness). The prophylaxis success rate was 97%. In this study, atovaquone and proguanil hydrochloride combination therapy had an excellent safety and efficacy profile for prophylaxis of P. falciparum malaria in nonimmune subjects.

  2. Cytostatic action of aspirin and its effect on mitomycin C activity. A study in vitro under irradiation

    International Nuclear Information System (INIS)

    Kammerer, Cornelia; Getoff, Nikola

    2001-01-01

    Experiments in vitro using E. coli bacteria (AB 1157) proved that aspirin possesses a cytostatic ability under various experimental condition (pH=7.4) in airfree, aerated as well as in media containing N 2 O (converting e aq - into OH- radicals). In the last case the highest effect of aspirin was observed. The combination of aspirin with the well-known cytostaticum, mitomycin C (MMC) leads in airfree as well as in aerated media to a significant decrease of the MMC activity. However, the mixture of aspirin and MMC in the presence of N 2 O causes a synergistic effect, resulting in an enhancement of the MMC activity by a factor of 1.5. Probable reaction steps are presented and discussed. Using the pulse radiolysis method the rate constants for the reactions of e aq - , H and OH- species with aspirin were also determined

  3. Cytostatic action of aspirin and its effect on mitomycin C activity. A study in vitro under irradiation

    Energy Technology Data Exchange (ETDEWEB)

    Kammerer, Cornelia; Getoff, Nikola E-mail: nikola.getoff@univie.ac.at

    2001-04-01

    Experiments in vitro using E. coli bacteria (AB 1157) proved that aspirin possesses a cytostatic ability under various experimental condition (pH=7.4) in airfree, aerated as well as in media containing N{sub 2}O (converting e{sub aq}{sup -} into OH- radicals). In the last case the highest effect of aspirin was observed. The combination of aspirin with the well-known cytostaticum, mitomycin C (MMC) leads in airfree as well as in aerated media to a significant decrease of the MMC activity. However, the mixture of aspirin and MMC in the presence of N{sub 2}O causes a synergistic effect, resulting in an enhancement of the MMC activity by a factor of 1.5. Probable reaction steps are presented and discussed. Using the pulse radiolysis method the rate constants for the reactions of e{sub aq}{sup -}, H and OH- species with aspirin were also determined.

  4. Synthesis and Characterization of New 3-(4-Arylpiperazin-1-yl-2-hydroxypropyl 4-Propoxybenzoates and Their Hydrochloride Salts

    Directory of Open Access Journals (Sweden)

    Pavlina Marvanova

    2016-06-01

    Full Text Available Five new 3-(4-arylpiperazin-1-yl-2-hydroxypropyl 4-propoxybenzoates were designed and synthesized as potential dual antihypertensive agents. The compounds were prepared as free bases and subsequently transformed to hydrochloride salts. The position of protonation of nitrogen atoms in the piperazine ring of hydrochloride salts was determined by means of 13C-CP/MAS and 15N-CP/MAS NMR and IR spectroscopy. Using these solid-state analytical techniques, it was found that both nitrogen atoms were protonated when excess hydrogen chloride was used for preparation of salts. On the other hand, when the equimolar amount of hydrogen chloride was used, piperazine nitrogen substituted by aryl was protonated.

  5. Development and validation of an HPTLC method for the simultaneous estimation of Clonazepam and Paroxetine hydrochloride using a DOE approach

    Directory of Open Access Journals (Sweden)

    Purvi Shah

    2017-01-01

    Full Text Available The present study examines simultaneous multiple response optimization using Derringer's desirability function for the development of an HPTLC method to detect Clonazepam and Paroxetine hydrochloride in pharmaceutical dosage form. Central composite design (CCD was used to optimize the chromatographic conditions for HPTLC. The independent variables used for the optimization were the n-butanol content in the mobile phase, the chamber saturation time and the distance travelled. HPTLC separation was performed on aluminium plates pre-coated with silica gel 60 F254 as the stationary phase using n-butanol:glacial acetic acid:water (9:2:0.5% v/v/v as the mobile phase. Quantification was achieved based on a densitometric analysis of Clonazepam and Paroxetine hydrochloride over the concentration range of 40–240 ng/band and 300–1800 ng/band, respectively, at 288 nm. The method yielded compact and well-resolved bands at Rf of 0.77 ± 0.02 and 0.34 ± 0.02 for Clonazepam and Paroxetine hydrochloride, respectively. The linear regression analysis for the calibration plots produced r2 = 0.9958 and r2 = 0.9989 for Clonazepam and Paroxetine hydrochloride, respectively. The precision, accuracy, robustness, specificity, limit of detection and limit of quantitation of the method were validated according to the ICH guidelines. The factors evaluated in the robustness test were determined to have an insignificant effect on the selected responses. The results indicate that the method is suitable for the routine quality control testing of marketed tablet formulations.

  6. [Clinical Observation of Icotinib Hydrochloride for Advanced Non-small Cell Lung Cancer Patients with EGFR Status Identified].

    Science.gov (United States)

    Li, Xi; Qin, Na; Wang, Jinghui; Yang, Xinjie; Zhang, Xinyong; Lv, Jialin; Wu, Yuhua; Zhang, Hui; Nong, Jingying; Zhang, Quan; Zhang, Shucai

    2015-12-01

    Icotinib is the first self-developed small molecular drug in China for targeted therapy of lung cancer. Compared to the other two commercially available epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors, gefitinib and erlotinib, icotinib is similar to them in chemical structure, mechanism of activity and therapeutic effects. To explore the efficacy and side effects of icotinib hydrochloride in the treatment of the advanced non-small cell lung cancer (NSCLC) patients with EGFR mutation and wild-type. Patients with advanced NSCLC who were treated with icotinib hydrochloride in Beijing Chest Hospital were retrospective analyzed from March 2009 to December 2014. The clinical data of 124 patients (99 with EGFR mutation and 25 with wild type) with advanced NSCLC were enrolled in this study. The patients' overall objective response rate (ORR) was 51.6 % and the disease control rate (DCR) was 79.8%; The patients with EGFR mutation, ORR was 63.6%, DCR was 93.9%. The ORR was 4.0% and the DCR was 24.0% in the wild-type patients. Median progression-free survival (PFS) with icotinib treatment in EGFR mutation patients was 10.5 months and 1.0 month in wild-type patients. The major adverse events were mild skin rash (30.6%) and diarrhea (16.1%). Monotherapy with icotinib hydrochloride is effective and tolerable for the advanced NSCLC EGFR mutation patients.


  7. Mitomycin C-augmented trabeculectomy: subtenon injection versus soaked sponges: a randomised clinical trial.

    Science.gov (United States)

    Pakravan, Mohammad; Esfandiari, Hamed; Yazdani, Shahin; Douzandeh, Azadeh; Amouhashemi, Nassim; Yaseri, Mehdi; Pakravan, Parto

    2017-09-01

    To compare the efficacy and safety of subtenon injection of mitomycin C (MMC) with that of conventional application of MMC-soaked sponges in trabeculectomy. In this multicentre randomised clinical trial, 80 consecutive open-angle glaucoma cases were randomised into two groups; group 1 received a subtenon injection of 0.1 mL of 0.01% MMC, while group 2 received 0.02% MMC-soaked sponges. Primary outcome measure was intraocular pressure (IOP), and secondary outcome measures were endothelial cell count (ECC) changes and bleb morphology according to the Indiana Bleb Appearance Grading Scale. Outcome measures were compared at 1, 3 and 6 months postoperatively. Complete and qualified success was defined as IOP within 6-15 mm Hg without and with medications at month 6, respectively. Mean preoperative IOP was 21.8±5.1 in group 1, which reduced to 10.3±3.7 mm Hg at final visit (pinjection of MMC is a safe and effective alternative to the conventional soaked sponge method. This method produces more favourable bleb morphology after trabeculectomy. NCT02385370, Post-results. Published by the BMJ Publishing Group Limited. For permission to use (where not already granted under a licence) please go to http://www.bmj.com/company/products-services/rights-and-licensing/.

  8. Solid Microneedles for Transdermal Delivery of Amantadine Hydrochloride and Pramipexole Dihydrochloride

    Directory of Open Access Journals (Sweden)

    Mylien T. Hoang

    2015-09-01

    Full Text Available The aim of this project was to study the influence of microneedles on transdermal delivery of amantadine hydrochloride and pramipexole dihydrochloride across porcine ear skin in vitro. Microchannel visualization studies were carried out and characterization of the microchannel depth was performed using confocal laser scanning microscopy (CLSM to demonstrate microchannel formation following microneedle roller application. We also report, for the first time, the use of TA.XT Plus Texture Analyzer to characterize burst force in pig skin for transdermal drug delivery experiments. This is the force required to rupture pig skin. The mean passive flux of amantadine hydrochloride, determined using a developed LC–MS/MS technique, was 22.38 ± 4.73 µg/cm2/h, while the mean flux following the use of a stainless steel microneedle roller was 49.04 ± 19.77 µg/cm2/h. The mean passive flux of pramipexole dihydrochloride was 134.83 ± 13.66 µg/cm2/h, while the flux following the use of a stainless steel microneedle roller was 134.04 ± 0.98 µg/cm2/h. For both drugs, the difference in flux values following the use of solid stainless steel microneedle roller was not statistically significantly (p > 0.05. Statistical analysis was carried out using the Mann–Whitney Rank sum test.

  9. Inference of some pharmacokinetic parameters of the C mitomycin, through the analysis of its micro nucleate polychromatic erythrocytes induction kinetics

    International Nuclear Information System (INIS)

    Morales R, P.; Vallarino K, T.; Cruz V, V.; Delgadillo H, A.

    2003-01-01

    The objective of the present work was to establish pharmacokinetic parameters of the C Mitomycin (MMC) in vivo, comparing its kinetics of induction of polychromatic micro nucleate erythrocytes (EPGMN) with that of the gamma radiation. The used doses were of 0.75; 1.5 and 3. 0 μmoles/kg of MMC. It was observed that the MMC produces MN in the first cycle of cellular division and it is independent of the cytotoxic effect. This agent requires of a relatively long period of latency that is not compatible with her great reactivity, for what the pharmacokinetic values obtained in fact reflect the time that takes the processing of leisure in the DNA and the subsequent induction of ruptures that produce MN. (Author)

  10. 77 FR 16036 - Determination That CITANEST (Prilocaine Hydrochloride) Injection, 1%, 2%, and 3%, and CITANEST...

    Science.gov (United States)

    2012-03-19

    ... marketing for reasons other than safety or effectiveness. ANDAs that refer to CITANEST (prilocaine HCl... Hydrochloride) Injection, 4%, Were Not Withdrawn From Sale for Reasons of Safety or Effectiveness AGENCY: Food... (prilocaine HCl) Injection, 4%, were not withdrawn from sale for reasons of safety or effectiveness. This...

  11. 78 FR 27971 - Determination That REV-EYES (Dapiprazole Hydrochloride Ophthalmic Solution), 0.5%, Was Not...

    Science.gov (United States)

    2013-05-13

    ...] Determination That REV-EYES (Dapiprazole Hydrochloride Ophthalmic Solution), 0.5%, Was Not Withdrawn From Sale... ophthalmic solution), 0.5%, was not withdrawn from sale for reasons of safety or effectiveness. This... ophthalmic solution, 0.5%, if all other legal and regulatory requirements are met. FOR FURTHER INFORMATION...

  12. Multiple-dose pharmacokinetic study of proguanil and cycloguanil following 12-hourly administration of 100 mg proguanil hydrochloride.

    Science.gov (United States)

    Jamaludin, A; Mohamad, M; Navaratnam, V; Yeoh, P Y; Wernsdorfer, W H

    1990-09-01

    A pharmacokinetic study with 12-hourly doses of 100 mg proguanil hydrochloride over 15 days has been conducted in six adult male Malaysian volunteers. Steady state for proguanil was established after the fourth dose on Day 2, for the active metabolite cycloguanil as from Day 3 inclusive. The steady state mean peak concentration of proguanil was 1201.6 +/- 132.4 nmol/l, the mean trough concentration 650.0 +/- 58.1 nmol/l. The corresponding values for cycloguanil were 317.0 +/- 44.4 nmol/l (mean peak) and 230.8 +/- 35.1 nmol/l (mean trough). The profiles and peak/trough ratios of proguanil and cycloguanil with 12-hourly dosing offer better prospects for protection against malaria than those obtained with 24-hourly doses of 200 mg proguanil hydrochloride, the current routine in malaria chemoprophylaxis.

  13. Stimulatory action of itopride hydrochloride on colonic motor activity in vitro and in vivo.

    Science.gov (United States)

    Tsubouchi, Tadashi; Saito, Takaharu; Mizutani, Fujie; Yamauchi, Toshie; Iwanaga, Yuji

    2003-08-01

    We investigated the effects of itopride hydrochloride (itopride, N-[4-[2-(dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide hydrochloride), a gastroprokinetic agent, on the colonic motor activity in vitro and in vivo, in comparison with benzamides, cisapride hydrate (cisapride), and mosapride citrate (mosapride). Itopride stimulated both peristaltic and segmental motility induced by applying intraluminal pressure to the isolated guinea pig colon. Although cisapride and mosapride enhanced the segmental motility, they markedly reduced the peristaltic motility. In conscious dogs with implanted strain gauge force transducers, itopride stimulated contractile activity in the gastrointestinal tract from the stomach to the colon. Cisapride stimulated contractile activity in the gastric antrum, ileum, and ascending colon. Mosapride stimulated contractile activity only in the gastric antrum and ileum. In guinea pigs and rats, itopride accelerated colonic luminal transit. On the other hand, cisapride and mosapride failed to enhance colonic transit. These results demonstrate that itopride has a stimulatory action on colonic peristalsis, propelling colonic luminal contents, different from that of cisapride and mosapride. Therefore, itopride may be a useful drug for the treatment of functional bowel disorders such as functional constipation.

  14. Microwave-Assisted Hydrolysis of Chitosan from Shrimp Shell Waste for Glucosammine Hydrochlorid Production

    International Nuclear Information System (INIS)

    Zaeni, Ahmad; Safitri, Endang; Fuadah, Badrotul; Sudiana, I Nyoman

    2017-01-01

    Chitin is the most widespread renewable natural sources following cellulose as the main source of chitosan. Chitin is isolated from crustacean waste and shrimp shells. Chitosan is derived from chitin throuhgt demineralisation, deproteination, decolorisation and deacetylation process using chemicals such as sodium hydroxide, hydrogen chloride and acetone. Glucosamine hydrochloride (GlcN-Cl) can be produced by hydrolysis of chitosan by using hydrogen chloride. During deacetylation and hydrolysis the solution is heated by hotplate or furnace. In this paper we use microwave instead of hotplate for production chitosan and GlcN-Cl. The research investigates effect of microwaves to amount of rendemen and their property. The chitosan was characterized its moisture content, solubility, and degree of deacetylation (DDA). Whereas the glucosammine hydrochloride characterized its functional groups using FTIR and crystallization by using X-Ray Difraction (XRD). The experimental results show that the use of microwave energy on deacetilation of chitosan and hydrolisis processes can decrease time consuming and reactant concentration during production. the DDA value obtained was very high from 70 to 85%. The results also show that microwaves meet chitosan and GlcN-Cl standards. (paper)

  15. Microwave-Assisted Hydrolysis of Chitosan from Shrimp Shell Waste for Glucosammine Hydrochlorid Production

    Science.gov (United States)

    Zaeni, Ahmad; Safitri, Endang; Fuadah, Badrotul; Nyoman Sudiana, I.

    2017-05-01

    Chitin is the most widespread renewable natural sources following cellulose as the main source of chitosan. Chitin is isolated from crustacean waste and shrimp shells. Chitosan is derived from chitin throuhgt demineralisation, deproteination, decolorisation and deacetylation process using chemicals such as sodium hydroxide, hydrogen chloride and acetone. Glucosamine hydrochloride (GlcN-Cl) can be produced by hydrolysis of chitosan by using hydrogen chloride. During deacetylation and hydrolysis the solution is heated by hotplate or furnace. In this paper we use microwave instead of hotplate for production chitosan and GlcN-Cl. The research investigates effect of microwaves to amount of rendemen and their property. The chitosan was characterized its moisture content, solubility, and degree of deacetylation (DDA). Whereas the glucosammine hydrochloride characterized its functional groups using FTIR and crystallization by using X-Ray Difraction (XRD). The experimental results show that the use of microwave energy on deacetilation of chitosan and hydrolisis processes can decrease time consuming and reactant concentration during production. the DDA value obtained was very high from 70 to 85%. The results also show that microwaves meet chitosan and GlcN-Cl standards.

  16. Determination of Degradation Products of Cyclobenzaprine Hydrochloride, Lidocaine and Piroxicam in a Semi-Topical Formulation: MS-MS Confirmation of Unknown Impurities.

    Science.gov (United States)

    Cioroiu, Bogdan Ionel; Grigoriu, Ioana Cezara; Cioroiu, Mona Elisabeta; Niculaua, Marius; Lupuleasa, Roxana; Lazar, Mihai Ioan

    2016-07-01

    Association of cyclobenzaprine hydrochloride, piroxicam and lidocaine in a topical formulation is one of the newest innovations in the pharmaceutical formulary field. In this study, a reversed-phase liquid chromatographic method was developed for the establishment of the impurities of cyclobenzaprine hydrochloride, lidocaine and piroxicam in the semisolid topical formulation. In this study, we not only determined 2,6-dimethylaniline, 2-pyrydilamine but also specified impurities of cyclobenzaprine hydrochloride (dibenzosuberenone, amitriptyline, carbinole, cyclobenzaprine N-oxide and anthrachinone). The target compounds were determined using a mobile phase that consisted of a mixture of phosphate buffer (0.025 M; pH 6.2)-acetonitrile-methanol (60 : 13 : 27, v/v/v). A minimum of three supplementary possible degradation products were determined. Using mass spectrometry, the unspecified impurities were identified and the use of correlation matrices permitted the association with the possible source compounds. The chromatographic conditions were qualified and validated according to ICH guideline requirements to confirm specificity, linearity, accuracy and precision. © The Author 2016. Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

  17. Stability of i.v. admixture containing metoclopramide, diphenhydramine hydrochloride, and dexamethasone sodium phosphate in 0.9% sodium chloride injection.

    Science.gov (United States)

    Kintzel, Polly E; Zhao, Ting; Wen, Bo; Sun, Duxin

    2014-12-01

    The chemical stability of a sterile admixture containing metoclopramide 1.6 mg/mL, diphenhydramine hydrochloride 2 mg/mL, and dexamethasone sodium phosphate 0.16 mg/mL in 0.9% sodium chloride injection was evaluated. Triplicate samples were prepared and stored at room temperature without light protection for a total of 48 hours. Aliquots from each sample were tested for chemical stability immediately after preparation and at 1, 4, 8, 24, and 48 hours using liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis. Metoclopramide, diphenhydramine hydrochloride, and dexamethasone sodium phosphate were selectively monitored using multiple-reaction monitoring. Samples were diluted differently for quantitation using three individual LC-MS/MS methods. To determine the drug concentration of the three compounds in the samples, three calibration curves were constructed by plotting the peak area or the peak area ratio versus the concentration of the calibration standards of each tested compound. Apixaban was used as an internal standard. Linearity of the calibration curve was evaluated by the correlation coefficient r(2). Constituents of the admixture of metoclopramide 1.6 mg/mL, diphenhydramine hydrochloride 2 mg/mL, and dexamethasone sodium phosphate 0.16 mg/mL in 0.9% sodium chloride injection retained more than 90% of their initial concentrations over 48 hours of storage at room temperature without protection from light. The observed variability in concentrations of these three compounds was within the limits of assay variability. An i.v. admixture containing metoclopramide 1.6 mg/mL, diphenhydramine hydrochloride 2 mg/mL, and dexamethasone sodium phosphate 0.16 mg/mL in 0.9% sodium chloride injection was chemically stable for 48 hours when stored at room temperature without light protection. Copyright © 2014 by the American Society of Health-System Pharmacists, Inc. All rights reserved.

  18. The Th1/Th2/Th17/Treg paradigm induced by stachydrine hydrochloride reduces uterine bleeding in RU486-induced abortion mice.

    Science.gov (United States)

    Li, Xia; Wang, Bin; Li, Yuzhu; Wang, Li; Zhao, Xiangzhong; Zhou, Xianbin; Guo, Yuqi; Jiang, Guosheng; Yao, Chengfang

    2013-01-09

    The Th1/Th2/Th17/Treg paradigm plays an important role in achieving maternal-fetal immunotolerance and participates in RU486-induced abortion. Excessive uterine bleeding is the most common side effect of RU486-induced abortion; however, its etiopathogenesis has not been fully understood. Therefore, elucidating the correlation between the Th1/Th2/Th17/Treg paradigm and the volume of uterine bleeding may offer novel therapeutic target for reducing uterine bleeding in RU486-induced abortion. Leonurus sibiricus has been used in clinics to reduce postpartum hemorrhage with low toxicity and high efficiency; however, the effective constituents and therapeutic mechanism have not been described. Stachydrine hydrochloride is the main constituent of L. sibiricus, therefore L. sibiricus is regarded as a candidate for reducing uterine bleeding in RU486-induced abortion mice by regulating the Th1/Th2/Th17/Treg paradigm. The purpose of this study was to determine the Th1/Th2/Th17/Treg paradigm in uterine bleeding of RU486-induced abortion mice and to elucidate the immunopharmacologic effects of stachydrine hydrochloride on inducing the Th1/Th2/Th17/Treg paradigm in reducing the uterine bleeding volume in RU486-induced abortion mice. To investigate the Th1/Th2/Th17/Treg paradigm in uterine bleeding during RU486-induced abortion mice, pregnant BALB/c mice were treated with high- and low-dose RU486 (1.5mg/kg and 0.9 mg/kg, respectively), and the serum progesterone (P(4)) protein level, uterine bleeding volume, and proportions of Th1/Th2/Th17/Treg cells in mice at the maternal-fetal interface were detected by ELISA assay, alkaline hematin photometric assay, and flow cytometry, respectively. To determine the regulatory effect of stachydrine hydrochloride on the Th1/Th2/Th17/Treg paradigm in vitro, splenocytes of non-pregnant mice were separated and treated with P(4,) RU486, and/or stachydrine hydrochloride (10(-5)M, 10(-4)M, and 10(-3)M, respectively). The proportions of Th1/Th2/Th17

  19. Effect of oxycodone hydrochloride combined with flurbiprofen axetil for intravenous patient-controlled analgesia in lower abdominal patients: A randomized trial.

    Science.gov (United States)

    Xiang, Xiaobing; Yuan, Xiaohong; Lian, Yanhong; Fang, Jun; Wu, Yingli

    2018-02-01

    Problems like postoperative pain are still common phenomena after general anesthesia. Oxycodone hydrochloride is a semisynthetic opioid with a safe and excellent therapeutic effect on visceral pain. Flurbiprofen axetil has the efficacy of targeted analgesia. We hypothesize that different doses of oxycodone hydrochloride combined with flurbiprofen axetil would generate great results on postoperative intravenous analgesia in lower abdominal patients. In the clinical trial, 90 American Society of Anesthesiologists I or II patients scheduled for elective general anesthesia were randomly divided into 3 groups, 30 cases in each group. Group I: oxycodone hydrochloride 0.5 mg/kg + flurbiprofen axetil 150 mg, group II: oxycodone hydrochloride 0.75 mg/kg + flurbiprofen axetil 150 mg, group III: oxycodone hydrochloride 1.0 mg/kg + flurbiprofen axetil 150 mg. Dilute them with 0.9% saline to 150 mL, respectively, with the background dose of 2 mL/h, patient-controlled analgesia 2 mL per time, with an interval of 10 min, and the loading dose of 0.1 mL/kg. Record the preoperative situation, 24 h (T0) before surgery, postoperative situation, 1 h (T1), 4 h (T2), 8 h (T3), 12 h (T4), 24 h (T5), 48 h (T6), 72 h (T7) after the surgery, including the mean arterial pressure, heart rate, saturation of pulse oximetry, static and dynamic pain rating (NRS) and Ramsay sedation score, effective pressing and total pressing ratio (referred to as the pressing ratio), patient satisfaction, and occurrence of adverse reactions. There was no significant statistic difference in mean arterial blood pressure, heart rate, arterial oxygen saturation, and adverse reactions among the 2 groups at each time point (P > .05). Compared with group I, the static NRS rating in group II and group III were significantly lower than that in group I (P  .05). Compared with group III, the Ramsay sedation scores of group I and group II were significantly lower from T1 to T4 (P

  20. LC-ESI-MSD fast determination of residual mitomycin C in hen aqueous humour after corneal refractive surgery.

    Science.gov (United States)

    Nozal, M J; Bernal, J L; Martín, M T; Bernal, J; Torres, R M; Merayo, J

    2006-01-23

    A simple, fast and reliable method has been developed for the assay of traces of mitomycin C (MMC) in hen aqueous humour samples. The determination was carried out by high-performance liquid chromatography with electrospray ionization mass spectrometric detection. In isocratic elution analysis, the mobile phase was a mixture of water-acetonitrile (78:22, v/v) and the chromatographic column was C(18) at 35 degrees C. The method has been validated over a range from 0.1 to 250 microg L(-1) in hen aqueous humour with correlation coefficients higher than 0.999. Limit of detection and limit of quantification for MMC based in signal to noise ratio of 3 and 10, respectively, were 20 and 71 ng L(-1). The developed method allows the analysis of MMC in hen aqueous humour samples obtained at different times and conditions in order to evaluate and compare the efficacy of the drug administration.

  1. The effect of polymorphism on powder compaction and dissolution properties of chemically equivalent oxytetracycline hydrochloride powders.

    Science.gov (United States)

    Liebenberg, W; de Villiers, M M; Wurster, D E; Swanepoel, E; Dekker, T G; Lötter, A P

    1999-09-01

    In South Africa, oxytetracycline is identified as an essential drug; many generic products are on the market, and many more are being developed. In this study, six oxytetracycline hydrochloride powders were obtained randomly from manufacturers, and suppliers were compared. It was found that compliance to a pharmacopoeial monograph was insufficient to ensure the optimum dissolution performance of a simple tablet formulation. Comparative physicochemical raw material analysis showed no major differences with regard to differential scanning calorimetry (DSC), infrared (IR) spectroscopy, powder dissolution, and particle size. However, the samples could be divided into two distinct types with respect to X-ray powder diffraction (XRD) and thus polymorphism. The two polymorphic forms had different dissolution properties in water or 0.1 N hydrochloride acid. This difference became substantial when the dissolution from tablets was compared. The powders containing form A were less soluble than that containing form B.

  2. Amifostine Protection Against Mitomycin-induced Chromosomal Breakage in Fanconi Anaemia Lymphocytes

    Directory of Open Access Journals (Sweden)

    Miriam T. P. Lopes

    2008-08-01

    Full Text Available Fanconi anaemia (FA is a rare genetic chromosomal instability syndrome caused by impairment of DNA repair and reactive oxygen species (ROS imbalance. This disease is also related to bone marrow failure and cancer. Treatment of these complications with radiation and alkylating agents may enhance chromosomal breakage. We have evaluated the effect of amifostine (AMF on basal and mitomycin C (MMC-induced chromosomal breakage in FA blood cells using the micronucleus assay. The basal micronuclei count was higher among FA patients than healthy subjects. Pre-treatment with AMF significantly inhibited micronucleation induced by MMC in healthy subjects (23.4 ± 4.0 – MMC vs 12.3 ± 2.9 – AMF →MMC MN/1000CB, p < 0.01, one way ANOVA as well as in FA patients (80.0 ± 5.8 – MMC vs 40.1 ± 5.8 – AMF →MMC MN/1000CB, p < 0.01, ANOVA. Release of ROS by peripheral blood mononuclear cells treated with AMF →MMC and measured by chemoluminometry showed that AMF-protection was statistically higher among FA patients than in healthy individuals. Based on these results we suggest that AMF prevents chromosomal breakage induced by MMC, probably by its antioxidant effect.

  3. Clinical study on photorefractive keratectomy for high myopia with mitomycin C

    Directory of Open Access Journals (Sweden)

    Hao-Jiang Yang

    2013-06-01

    Full Text Available AIM: To evaluate the efficacy, safety and stability of photorefractive keratectomy(PRKfor high myopia with 0.2g/L mitomycin C(MMC. METHODS: Totally 109 patients(201 eyesafter PRK were treated with intraoperative application of 0.2g/L MMC for 20 seconds. The recovery of cornea epithelium after surgery was regularly observed. The uncorrected visual acuity(UCVA, corrected distance visual acuity(CDVA, refraction, haze, complications and endothelial cell counts 1 month, 3, 6, 12 months after PRK were compared. RESULTS:The time of corneal epithelium recovery was 3.68±0.35 days. All eyes had a significant increase in UCVA. 12 months after surgery, 189 eyes(94%achieved UCVA better than 1.0 and 153 eyes(76%had a spherical equivalent(SEwithin±0.5D. 7 eyes(3%lost one line of CDVA. No one lost 2 or more lines of CDVA. Ninety-six percent eyes changed within±0.5D when comparing 3 month and 12 month. Postoperative endothelial cell density and coefficient of variability(CVdid not show a significant difference from preoperative measurements(P1=0.71; P2=0.83. Haze of grade 1 occurred in 12 eyes(6%and haze between grade 0.5 and 1 existed in 189 eyes(94%at 12 months. No eye developed haze over grade 2. No toxic effect and complications of MMC were found after surgery. CONCLUSION: PRK with intraoperative application of MMC for 20 seconds appears to be a safe and effective method for correction of high myopia.

  4. Efficacy and safety of terbinafine hydrochloride 1% cream vs eberconazole nitrate 1% cream in localised tinea corporis and tinea cruris

    Directory of Open Access Journals (Sweden)

    Sanjiv V Choudhary

    2014-01-01

    Full Text Available Aims: To study and compare the efficacy and safety of topical terbinafine hydrochloride 1% cream and eberconazole nitrate 1% cream in localized tinea corporis and cruris. Methods and Materials: Patients were randomized after considering various inclusion and exclusion criteria into two groups. Group A (treated with terbinafine 1% cream for 3 weeks and group B (treated with eberconazole 1% cream for 3 weeks. The sample size was of 30 patients with 15 patients in each group. Assessment of clinical improvement, KOH mount and culture was done weekly up to 3 weeks to assess complete cure. Results: On comparison between the two groups, it was observed that eberconazole nitrate 1% cream was as effective as terbinafine hydrochloride 1% cream at the end of first (Non-sisgnificant (NS; P = 0.608, 1.00, second (NS; P = 0.291,0.55, and third (P = 1.00, 1.00 weeks with statistically nonsignificant clinical and mycological values. In both the groups, clinically no significant local side effects were noticed. Conclusions: The newer fungistatic eberconazole nitrate 1% cream was as effective as the fungicidal terbinafine hydrochloride 1% cream. Both the drugs showed good tolerability with no adverse effects.

  5. Determination of antazoline hydrochloride in rat plasma and excreta by reversed-phase ion-pair chromatography and its application to pharmacokinetics.

    Science.gov (United States)

    Wang, Rui; Chu, Yanle; Li, Xiaotian; Wan, Baoluo; Yu, Tong; Wang, Linxi; Hao, Lianqi; Guo, Maowen

    2013-12-01

    A reversed-phase ion pair chromatography method with liquid-liquid extraction analytical method was developed and validated for the determination of antazoline hydrochloride in plasma and excreta of rat. The aim of our study was to characterize the preclinical pharmacokinetics and excretion profiles of antazoline hydrochloride in rats after intravenous injection at the dose of 10 mg/kg. Plasma and excreta samples were extracted with ethyl acetate, and phenacetin was used as the internal standard. The result showed that the method is suitable for the quantification of antazoline hydrochloride in plasma and excreta samples. Analysis of accuracy (90.89-112.33%), imprecision (82.5%) showed adequate values. After a single intravenous administration at 10 mg/kg to rats, plasma concentration profile showed a relative fast elimination proceeding with a terminal elimination half-life of 3.53 h. Approximately 61.8 and 14.2% of the administered dose were recovered in urine and bile after 72 and 24 h post-dosing respectively; 5.9% of the administered dose was recovered in feces after 72 h post-dosing. The above results show that the major elimination route is urinary excretion. Copyright © 2013 John Wiley & Sons, Ltd.

  6. NTP toxicity studies of dimethylaminopropyl chloride, hydrochloride (CAS No. 5407-04-5) administered by Gavage to F344/N rats and B6C3F1 mice.

    Science.gov (United States)

    Abdo, Km

    2007-07-01

    Dimethylaminopropyl chloride, hydrochloride is used primarily as an industrial and research organic chemical intermediate acting as an alkylating reagent in Grignard and other types of reactions. It is also used as a pharmaceutical intermediate for the synthesis of many types of drugs, as an agricultural chemical intermediate, as a photographic chemical intermediate, and as a biochemical reagent for enzyme and other studies. Human occupational or other accidental exposure can occur by inhalation, ingestion, or skin absorption. Male and female F344/N rats and B6C3F1 mice received dimethylaminopropyl chloride, hydrochloride (greater than 99% pure) in water by gavage for 2 weeks or 3 months. Genetic toxicology studies were conducted in Salmonella typhimurium and mouse peripheral blood erythrocytes. In the 2-week toxicity studies, groups of five male and five female F344/N rats and B6C3F1 mice were administered doses of 0, 6.25, 12.5, 25, 50, or 100 mg dimethylaminopropyl chloride, hydrochloride/kg body weight in deionized water by gavage, 5 days per week for 16 days. All dosed male and female rats and mice survived until the end of the 2-week study; one vehicle control female mouse died early. Mean body weights of all dosed groups of rats and mice were similar to those of the vehicle control groups. No gross or microscopic lesions were considered related to dimethylaminopropyl chloride, hydrochloride administration. In the 3-month toxicity studies, groups of 10 male and 10 female F344/N rats and B6C3F1 mice were administered doses of 0, 6.25, 12.5, 25, 50, or 100 mg/kg in deionized water by gavage, 5 days per week for 3 months. One male rat in the 50 mg/kg group died during week 12 of the study, and one female mouse in the 100 mg/kg group died during week 9 and another during week 13. The final mean body weights of 50 mg/kg male rats and 50 mg/kg female mice were significantly less than those of the vehicle controls. Possible chemical-related clinical findings in rats

  7. In vitro evaluation of extemporaneously compounded slow-release capsules containing morphine sulfate or oxycodone hydrochloride.

    Science.gov (United States)

    Glowiak, Dana L; Green, Julie L; Bowman, Bill J

    2005-01-01

    The in vitro performance of extemporaneously compounded morphine sulfate and oxycodone hydrochloride slow-release capsules was evaluated. Capsules containing varying amoutns of morphine sulfate (15, 60, 200 mg) or oxycodone hydrochloride (10, 80, 200 mg) were prepared and provided by a Phoenix, Arizona, pharmacy. The capsules also contained 40% Methocel E4M Premium to slow the release of their active ingredient and sufficient lactose to fill the capsules. Three batches of each capsule strength were prepared, and replicates from each batch were evlauated using United Stated Pharmacopeia dissolution apparatus II. Samples were taken at regular time intervals over 24 hours. After 1 hour the pH of the dissolution medium was adjusted form 1.2 to 4.0, and after 2 hours the pH was adjusted to 6.8. The amount of drug released at each time point was determined spectrophotometrically. The compounded capsules released 14% to 23%, 67% to 85% and 93% to 98% of their active ingredient after 0.5, 4 and 12 hours, respectively. The relative standard deviations between the replicates from each batch were less than 10% for most time points. The percent of drug released over the first 4 hours was linear (r squared = 0.9409-0.9999) when plotted versus time 1/2, indicating adherence to the simplified Higuchi model. Statistical analysis of the Higuchi dissolution constants indicated a significant difference (P less than 0.05) between batch No.3 and the other two batches of 200-mg oxycodone hydrochloride capsules. There was also a statistical difference between most of the Higuchi dissolution constants for the different-strength slow-release capsules and most slow-release capsules and equivalent strength controlled-release manufactured tablets (P less than 0.05). Using 40% Methocel E4M Premium slowed the release of morphine sulfate and oxycodone hydrochloride from extemporaneously compounded capsules. The in vitro performance of the slow-release capsules showed little intrabatch variation

  8. Formulation of bi-layer matrix tablets of tramadol hydrochloride: Comparison of rate retarding ability of the incorporated hydrophilic polymers.

    Science.gov (United States)

    Arif, Hasanul; Al-Masum, Abdullah; Sharmin, Florida; Reza, Selim; Sm Islam, Sm Ashraful

    2015-05-01

    Bi-layer tablets of tramadol hydrochloride were prepared by direct compression technique. Each tablet contains an instant release layer with a sustained release layer. The instant release layer was found to release the initial dose immediately within minutes. The instant release layer was combined with sustained release matrix made of varying quantity of Methocel K4M, Methocel K15MCR and Carbomer 974P. Bi-layer tablets were evaluated for various physical tests including weight variation, thickness and diameter, hardness and percent friability. Drug release from bi-layer tablet was studied in acidic medium and buffer medium for two and six hours respectively. Sustained release of tramadol hydrochloride was observed with a controlled fashion that was characteristic to the type and extent of polymer used. % Drug release from eight-hour dissolution study was fitted with several kinetic models. Mean dissolution time (MDT) and fractional dissolution values (T25%, T50% and T80%) were also calculated as well, to compare the retarding ability of the polymers. Methocel K15MCR was found to be the most effective in rate retardation of freely water-soluble tramadol hydrochloride compared to Methocel K4M and Capbomer 974P, when incorporated at equal ratio in the formulation.

  9. Clinical Observation of Icotinib Hydrochloride for Advanced Non-small Cell Lung Cancer Patients with EGFR Status Identified

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    Xi LI

    2015-12-01

    Full Text Available Background and objective Icotinib is the first self-developed small molecular drug in China for targeted therapy of lung cancer. Compared to the other two commercially available epidermal growth factor receptor (EGFR tyrosine kinase inhibitors, gefitinib and erlotinib, icotinib is similar to them in chemical structure, mechanism of activity and therapeutic effects. To explore the efficacy and side effects of icotinib hydrochloride in the treatment of the advanced non-small cell lung cancer (NSCLC patients with EGFR mutation and wild-type. Methods Patients with advanced NSCLC who were treated with icotinib hydrochloride in Beijing Chest Hospital were retrospective analyzed from March 2009 to December 2014. Results The clinical data of 124 patients (99 with EGFR mutation and 25 with wild type with advanced NSCLC were enrolled in this study. The patients’ overall objective response rate (ORR was 51.6 % and the disease control rate (DCR was 79.8%; The patients with EGFR mutation, ORR was 63.6%, DCR was 93.9%. The ORR was 4.0% and the DCR was 24.0% in the wild-type patients. Median progression-free survival (PFS with icotinib treatment in EGFR mutation patients was 10.5 months and 1.0 month in wild-type patients. The major adverse events were mild skin rash (30.6% and diarrhea (16.1%. Conclusion Monotherapy with icotinib hydrochloride is effective and tolerable for the advanced NSCLC EGFR mutation patients.

  10. Development and validation of new analytical methods for simultaneous estimation of Drotaverine hydrochloride in combination with Omeprazole in a pharmaceutical dosage form

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    Smita Sharma

    2017-02-01

    Full Text Available A rapid and precise method (in accordance with ICH guidelines is developed for the quantitative simultaneous determination of Drotaverine hydrochloride and Omeprazole in a combined pharmaceutical dosage form. Three methods are described for the simultaneous determination of Drotaverine hydrochloride and Omeprazole in a binary mixture. The first method was based on UV-Spectrophotometric determination of two drugs, using Vierordt!s simultaneous equation method. It involves absorbance measurement at 226.8 nm (λmax of Drotaverine hydrochloride and 269.4 nm (λmax of Omeprazole in methanol; linearity was obtained in the range of 5–30 μg ml−1 for both the drugs. The second method was based on HPLC separation of the two drugs using potassium dihydrogen phosphate buffer pH 5.0: Acetonitrile: Triethylamine (60:40:0.5, v/v as a mobile phase. Areas were recorded at 260 nm for both the drugs and retention time was found to be 2.71 min. and 3.87 min for Drotaverine hydrochloride and Omeprazole, respectively at 1.0 mL/min flow rate. The selected chromatographic conditions were found to determine Drotaverine hydrochloride and Omeprazole quantitatively in a combined dosage form without any physical separation. The method has been validated for linearity, accuracy and precision. Linearity was found over the range of 5–30 μg mL−1 for both drugs. The third method was based on HPTLC method for simultaneous quantification of these compounds in pharmaceutical dosage forms. Precoated silica gel 60 F254 plate was used as stationary phase. The separation was carried out using Glacial acetic acid:Cyclohexane:Methanol:(80:15:5 v/v/v as mobile phase. The proposed method was found to be fast, accurate, precise, reproducible and rugged and can be used for a simultaneous analysis of these drugs in combined formulations.

  11. Development of analytical method for the determination of carbinoxamine maleate, dextromethorphan hydrobromide and pseudoephedrine hydrochloride by HPLC

    International Nuclear Information System (INIS)

    Mahfoud, J.

    2007-01-01

    A simple and accurate method was developed for the analysis of carbinoxamine maleate, dextromethorphan hydrobromide and pseudoephedrine hydrochloride content in pure form and pharmaceutical preparations using HPLC. Analysis was conducted on a silica column (6 μm) with mobile phase consisting of ethanol - ammonium acetate (0.05 M) in rate [85:15] respectively, and at detection wavelength of 276 nm and flow rate 1 ml/min. Results were linear (correlation coefficient R > 0.9996) in the range of the studied concentrations for the active materials. The relative standard deviations (n=6) of intra and interday assay were 0.931%, 1.527% for carbinoxamine maleate and 0.717%, 1.058% for dextromethorphan hydrobromide and 0.309%, 0.891% for pseudoephedrine hydrochloride, respectively. This method, proved to be easy, precise and economical, is useful for quality control of pharmaceutical drugs industrial samples. (author)

  12. Neuroprotective effects of the antioxidant action of 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride against ischemic neuronal damage in the brain

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    Soo Young Choi

    2013-07-01

    Full Text Available Ischemia is characterized by oxidative stress and changes in theantioxidant defense system. Our recent in vitro study showedthat 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochlorideprotects cortical astrocytes against oxidative stress. In the currentstudy, we examined the effects of 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride on ischemia-induced neuronaldamage in a gerbil ischemia/reperfusion models. Extensive neuronaldeath in the hippocampal CA1 area was observed 4 daysafter ischemia/reperfusion. Intraperitoneal injection of 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride (0.3 mg/kgbody weight significantly prevented neuronal death in the CA1region of the hippocampus in response to transient forebrainischemia. 2-Cyclopropylimino-3-methyl-1,3-thiazoline hydrochlorideadministration reduced ischemia-induced increases inreactive oxygen species levels and malondialdehyde content. Italso attenuated the associated reductions in glutathione level andsuperoxide dismutase, catalase, and glutathione peroxidaseactivities. Taken together, our results suggest that 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride protects againstischemia-induced neuronal damage by reducing oxidative stressthrough its antioxidant actions. [BMB Reports 2013; 46(7:370-375

  13. High-Resolution Infrared and Raman Spectra of the Polycrystalline Sinomenine Hydrochloride

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    Liu Xiao-Dong

    2016-01-01

    Full Text Available High-resolution infrared and Raman spectra of the polycrystalline sinomenine (SM hydrochloride have been measured to work out its whole really existing vibrational spectral bands. Except for the hydroxyl stretching modes and IR active bands less than 400 cm−1, most normal modes (about 34 are both IR and Raman active. In addition, 8 Raman bands less than 400 cm−1 are tentatively assigned, for the first time to our knowledge, to stretching/bending modes of the aromatic-ring−methoxyls and (SMH+–Cl− ions, respectively.

  14. Ocular and systemic pharmacokinetics of lidocaine hydrochloride ophthalmic gel in rabbits after topical ocular administration.

    Science.gov (United States)

    Liu, Bing; Ding, Li; Xu, Xiaowen; Lin, Hongda; Sun, Chenglong; You, Linjun

    2015-12-01

    Lidocaine hydrochloride ophthalmic gel is a novel ophthalmic preparation for topical ocular anesthesia. The study is aimed at evaluating the ocular and systemic pharmacokinetics of lidocaine hydrochloride 3.5 % ophthalmic gel in rabbits after ocular topical administration. Thirty-six rabbits were randomly placed in 12 groups (3 rabbits per group). The rabbits were quickly killed according to their groups at 0 (predose), 0.0833, 0.167, 0.333, 0.667, 1, 1.5, 2, 3, 4, 6, and 8 h postdose and then the ocular tissue and plasma samples were collected. All the samples were analyzed by a validated LC-MS/MS method. The test result showed that the maximum concentration (C max) of lidocaine in different ocular tissues and plasma were all achieved within 20 min after drug administration, and the data of C max were (2,987 ± 1814) μg/g, (44.67 ± 12.91) μg/g, (26.26 ± 7.19) μg/g, (11,046 ± 2,734) ng/mL, and (160.3 ± 61.0) ng/mL for tear fluid, cornea, conjunctiva, aqueous humor, and plasma, respectively. The data of the elimination half-life in these tissues were 1.5, 3.2, 3.5, 1.9, and 1.7 h for tear fluid, cornea, conjunctiva, aqueous humor, and plasma, respectively. The intraocular lidocaine levels were significantly higher than that in plasma, and the elimination half-life of lidocaine in cornea, conjunctiva, and aqueous humor was relatively longer than that in tear fluid and plasma. The high intraocular penetration, low systemic exposure, and long duration in the ocular tissues suggested lidocaine hydrochloride 3.5 % ophthalmic gel as an effective local anesthetic for ocular anesthesia during ophthalmic procedures.

  15. Stability indicating high performance thin-layer chromatographic method for simultaneous estimation of pantoprazole sodium and itopride hydrochloride in combined dosage form

    Directory of Open Access Journals (Sweden)

    Deepak Bageshwar

    2011-11-01

    Full Text Available A specific, precise and stability indicating high-performance thin-layer chromatographic method for simultaneous estimation of pantoprazole sodium and itopride hydrochloride in pharmaceutical formulations was developed and validated. The method employed TLC aluminium plates precoated with silica gel 60F254 as the stationary phase. The solvent system consisted of methanol:water:ammonium acetate; 4.0:1.0:0.5 (v/v/v. This system was found to give compact and dense spots for both itopride hydrochloride (Rf value of 0.55±0.02 and pantoprazole sodium (Rf value of 0.85±0.04. Densitometric analysis of both drugs was carried out in the reflectance–absorbance mode at 289 nm. The linear regression analysis data for the calibration plots showed a good linear relationship with R2=0.9988±0.0012 in the concentration range of 100–400 ng for pantoprazole sodium. Also, the linear regression analysis data for the calibration plots showed a good linear relationship with R2=0.9990±0.0008 in the concentration range of 200–1200 ng for itopride hydrochloride. The method was validated for specificity, precision, robustness and recovery. Statistical analysis proves that the method is repeatable and selective for the estimation of both the said drugs. As the method could effectively separate the drug from its degradation products, it can be employed as a stability indicating method. Keywords: Gastroesophageal reflux disease (GERD, Itopride hydrochloride, Pantoprazole sodium, High performance thin layer chromatography (HPTLC, Stability indicating, Forced degradation

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

    NARCIS (Netherlands)

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

    2017-01-01

    Objective: 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. Significance: Elacridar is highly demanded for

  17. Multifunctional liposomes for nasal delivery of the anti-Alzheimer drug tacrine hydrochloride

    DEFF Research Database (Denmark)

    Corace, Giuseppe; Angeloni, Cristina; Malaguti, Marco

    2014-01-01

    . This approach was chosen in order to obtain at the same time two positive results: an enhanced drug permeation through nasal mucosa and a concomitant neuroprotective effect. Several liposome formulations were prepared using the Reverse Phase Evaporation technique followed by membrane filter extrusion......Abstract The purpose of this study was the development of multifunctional liposomes for nasal administration of tacrine hydrochloride. Liposomes were prepared using traditional excipients (cholesterol and phosphatidylcholine), partly enriched with α-tocopherol and/or Omega3 fatty acids...

  18. Investigations of genotoxic potential of levamisole hydrochloride in bone marrow cells of Wistar rats

    Directory of Open Access Journals (Sweden)

    Kulić Milan

    2006-01-01

    Full Text Available An experiment was performed under in vivo conditions on bone marrow cells of Wistar rats. The following doses of levamisole hydrochloride were tested: a therapeutic dose of 2.2 mg/kg bm, a dose of 4.4 mg/kg bm, LD50 -25% mg/kg bm, and LD50 -75% mg/kg bm. We followed the effect of levamisole hydrochloride on kinetics of the cell cycle and the appearance of structural and numeric changes in chromosomes in bone marrow cells. The therapeutic dose of levamisole of 2.2 mg/kg bm exhibited a capability to increase mitotic activity in the observed cells, thus confirming knowledge of the immunostimulative effect of this dose of the medicine under in vivo conditions. The other tested doses of levamisole in this experiment, observed in comparison with the control group, had an opposite effect, namely, they caused a reduction in the mitotic activity of bone marrow cells. All the examined doses in vivo exhibited the ability to induce numeric (aneuploid and polyploid and structural (lesions, breaks and insertions chromosomal aberrations. It can be concluded on the grounds of these findings that the examined doses have a genotoxic effect.

  19. Determination of itopride hydrochloride by high-performance liquid chromatography with Ru(bpy)3(2+) electrogenerated chemiluminescence detection.

    Science.gov (United States)

    Sun, Yonghua; Zhang, Zhujun; Xi, Zhijun; Shi, Zuolong; Tian, Wei

    2009-08-26

    In this work, a stable electrogenerated chemiluminescence (ECL) detector was developed. The detector was prepared by packing cation-exchanged resin particles in a glass tube, followed by inserting Pt wires (working electrode) in this tube and sealing. The leakage of Ru(bpy)(3)(2+) can be compensated by adding a small amount of Ru(bpy)(3)(2+) into solution phase. Coupled with high-performance liquid chromatography separation, the detector has been used for determination of itopride hydrochloride in human serum. Under the optimal conditions, the ECL intensity has a linear relationship with the concentration of itopride hydrochloride in the range of 1.0 x 10(-8) g mL(-1) to 1.0 x 10(-6) g mL(-1) and the detection limit was 3 x 10(-9) g mL(-1) (S/N=3). The as-prepared ECL detector displayed good sensitivity and stability.

  20. [Intraoperative chemotherapy with intraperitoneal activated carbon particles adsorbing mitomycin C against peritoneal dissemination of gastric cancer].

    Science.gov (United States)

    Iwamoto, A; Takahashi, T; Sasabe, T; Itoh, M; Kondoh, S; Seiki, K; Yoneyama, C; Shimotsuma, M; Hagiwara, A; Yamaguchi, T

    1989-08-01

    A new form of dosage (MMC-CH) was composed of activated carbon particles adsorbing mitomycin C. Intraperitoneal administration of MMC-CH was tested clinically for prophylactic and therapeutic effects on peritoneal carcinomatosis of gastric cancer. The criteria of MMC-CH's administration were equal or less than 70 years old, more than 40 kg in body weight, no disfunction of liver and kidney, no particular findings in electrocardiography, S2 or S3 in the grade of serosal invasion, P0, P1, P2 or P3 in the grade of peritoneal dissemination, according to the General Rules for the Gastric Cancer Study in Surgery and Pathology by the Japanese Research Society for Gastric Cancer. MMC-CH was given to 44 patients undergoing gastrectomy for gastric cancer in our department from 1985 to 1988. The 44 patients were composed of 12 patients with P0 findings (P0 patients), 8 patients with P1 findings (P1 patients), 12 patients with P2 findings (P2 patients), and 12 patients with P3 findings (P3 patients). MMC-CH at 50 mg/person in terms of mitomycin C was administered intraperitoneally before the operation wound was closed. Fifty-seven patients in our department from 1983 to 1987 for whom the same criteria were applicable and did not receive MMC-CH therapy, served as the control group. The 57 patients were composed of 23 P0 patients, 21 P1 patients, 10 P2 patients, and 3 P3 patients. There was statistically with chi 2 test no significant difference of age, sex, depth of infiltration macroscopically and microscopically defined progression of lymph-nodal metastases between the MMC-CH group and the control group. Survival rate was calculated with Kaplan-Meier's method in the overall patients in each of the MMC-CH group or the control group. The overall survival rate in the MMC-CH group was statistically significantly (p less than 0.01-0.05) higher from day 460 to day 552 and from day 736 to day 800 than that in the control group. Next, the patients were classified into two subgroups

  1. Pediatric PRK (PhotoRefractive Keratectomy) with Mitomycin C (MCC) for Persistent Anisometropic Amblyopia. A Case Report.

    Science.gov (United States)

    Crawford, Courtney M; Frazier, Travis C; Torres, Mark F; Arnold, Robert W; Mazzoli, Robert A; Raymond, William R

    2012-01-01

    To evaluate the safety and efficacy of photorefractive keratectomy (PRK) with Mitomycin C (MMC) for the treatment of severe pediatric anisometropia and amblyopia resistant to more conservative treatment modalities. A 3 year-old-child, who at 18 months old underwent unilateral diode laser treatment for threshold ROP, developed 11 diopters of anisometropic myopia and secondary dense amblyopia of the Right Eye. Only after all conservative treatment options failed was he treated with PRK and MMC. Principal outcome measures included cycloplegic refraction, the amount of refractive correction, degree of corneal haze and change in visual acuity. On presentation: BCVA: 20/CF OD; 20/30 OS. CRNS: -11.50 diopters sphere OD; -0.50 diopters sphere OS. Unilateral PRK followed by application of MMC (0.2 mg/ml) for 1 min was performed under general anesthesia. Three-month postoperative findings include: VA: 20/30 OD; 20/25 OS. CRNS: +0.25 diopters sphere OD. At one year, the BCVA remained equal at the 20/30 level despite mild myopic regression OD. CRNS OD at one year was -1.25 +050 x 116. No corneal haze was appreciated. In this child, treatment with PRK and MMC safely reduced the anisometropia thus facilitating his visual rehabilitation. While encouraging, further study is required to verify the longer term results of this single case. To evaluate the safety and efficacy of photorefractive keratectomy (PRK) with Mitomycin C (MMC) for the treatment of severe pediatric anisometropia and amblyopia resistant to more conservative treatment modalities. A 3 year-old-child, who at 18 months old underwent unilateral diode laser treatment for threshold ROP, developed 11 diopters of anisometropic myopia and secondary dense amblyopia of the Right Eye. Only after all conservative treatment options failed was he treated with PRK and MMC. Principal outcome measures included cycloplegic refraction, the amount of refractive correction, degree of corneal haze and change in visual acuity. On

  2. Clinical study of 3g/L sodium hyaluronate eye drops with bromhexine hydrochloride tablets for dry eye

    Directory of Open Access Journals (Sweden)

    Hui-Qun Xu

    2018-04-01

    Full Text Available AIM:To investigate the clinical efficacy of 3g/L sodium hyaluronate eye drops combined with bromhexine hydrochloride tablets on the treatment of dry eye. METHODS:Totally 200 patients with dry eye were randomly divided into the control group(n=100and observation group(n=100. Patients in two groups were given 3g/L sodium hyaluronate eye drops and physiotherapy. On the basis of this, the observation group were treated with bromhexine hydrochloride tablets. The inflammatory factors(IL-6, IL-10, TNF-α and IL-1βlevels and ocular symptom scores(OSDI, BUT, SⅠt, FLin the two groups were compared between before and after treatment. And the clinical efficacy and adverse reactions were evaluated. RESULTS: After treatment, the IL-6, IL-10, TNF-α, IL-1β, OSDI and FL scores in two groups were significantly lower than those before treatment, and BUT and SⅠt were significantly higher than those before treatment. Moreover, the improvement degree of the above indexes in the observation group were better than those in the control group, showing statistically significant difference(Pχ2=5.531, P=0.019, but there was no significant difference in the incidence of adverse reactions between the two groups(χ2=0.307, P=0.579. CONCLUSION:As for the patients with dry eye, the combination of 3g/L sodium hyaluronate eye drops with bromhexine hydrochloride tablets can significantly decrease the level of inflammatory factors, improve the eye symptoms and the clinical total efficiency, without increasing treatment-related adverse effects.

  3. Determination of itopride hydrochloride in human plasma by RP-HPLC with fluorescence detection and its use in bioequivalence study.

    Science.gov (United States)

    Ma, Jing; Yuan, Li-Hua; Ding, Mei-Juan; Zhang, Jun; Zhang, Qing; Xu, Qun-Wei; Zhou, Xue-Min

    2009-03-01

    A sensitive, selective and simple method using a precipitation of protein with 10% perchloric acid, followed by high-performance liquid chromatography (HPLC) with fluorescence detection was developed for the determination of itopride hydrochloride in human plasma, using levofloxacin as the internal standard (IS). Chromatographic separation was obtained within 7.0 min using a reverse phase Hypersil BDS C(18) (250 mm x 4.6 mm, 5 microm) column and an isocratic mobile phase, constituting of a mixture of 0.1 mol/l ammonium acetate-methanol (30:70, v/v) flowing at 1.1 ml/min. The excitation and emission wavelengths were set at 304 and 344 nm, respectively. The method was validated over the concentration range of 5 ng/ml to 1000.0 ng/ml. The lower limit of quantitation (LLOQ) was 5 ng/ml. The extractive recovery of itopride hydrochloride from the biological matrix was more than 80.77%. The intra-day accuracy of the drug containing serum samples was more than 82.94% with a precision of 2.81-4.37%. The inter-day accuracy was 82.91% or more, with a precision of 6.89-9.54%. The limit we have used (70-143%) is based on the local regulatory authority (SFDA). The developed method was validated and successfully applied to bioequivalence studies of itopride hydrochloride in healthy male volunteers.

  4. Effect of donepezil hydrochloride on brain perfusion in patients with dementia of Alzheimer type, evaluated by I-123-IMP SPECT

    International Nuclear Information System (INIS)

    Ogura, Y.; Narabayashi, I.; Utsunomiya, K.; Komori, T.; Adachi, I.; Sugino, M.; Sakai, J.

    2002-01-01

    Aim: To evaluate the effects of donepezil hydrochloride on brain perfusion in patients with dementia of Alzheimer type (DAT). Materials and Methods: I-123-IMP SPECT was performed on 12 controls (5 males and 7 females, mean age 69.7±6.4) and 30 consecutive patients with DAT (9 males and 21 females, mean age 71.0±5.1) to assess regional cerebral blood flow (rCBF) using the I-123-IMP autoradiography method. All 30 patients were diagnosed as having DAT by Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition criteria. In 23 of the 30 DAT patients, rCBF in the parietal, occipital, temporal cortex, or hippocampus was decreased more than the control rCBF by 1 SD. These 23 patients were enrolled in this study and received 5 mg/day of donepezil hydrochloride after breakfast. Treatment was continued for 3 to 12 months. At 3 to 6 (DAT/3-6M group) and/or 6 to 12 months (DAT/6-12M group) after the start of the treatment, I-123-IMP SPECT was performed again to obtain the rCBF. Regions of interest were set at the same position in a same patient pair of SPECT images before and after the treatment using an automatic registration tool (ART software, Toshiba, Tokyo, Japan). Results: 10 of the 23 patients in the DAT/3-6M group exhibited improved rCBF. 15 of the 23 patients in the DAT/6-12M group exhibited improved rCBF. These findings were not correlated with the neuropsychological score. Statistically, the rCBF showed no significant difference in the DAT/3-6M group. However, in the DAT/6-12M group, donepezil hydrochloride significantly improved rCBF in the frontal, parietal, and occipital cortices from 25.7±8.7 to 29.3±6.9, 20.6±7.9 to 24.9±6.2, and 27.2±6.0 to 35.0±7.6 [ml/100g/min] respectively. No change, either an increase or a decrease in rCBF was observed in any other regions. Conclusion: Some cases were improved and some cases were not recovered without relationship to the neuropsychological score. Statistically, donepezil hydrochloride did increase r

  5. Simultaneous determination of rabeprazole sodium and itopride hydrochloride in capsule dosage form by spectrophotometry.

    Science.gov (United States)

    Sabnis, Shweta S; Gandhi, Santosh V; Madgulkar, A R; Bothara, K G

    Three methods viz. Absorbance Ratio Method (I), Dual Wavelength Method (II) and First Order Derivative Spectroscopic Method (III) for simultaneous estimation of Rabeprazole sodium and Itopride hydrochloride have been developed. The drugs obey Beer's law in the concentration range 2-20 microg/ml for RAB and 5-75 microg/ml for ITO. The results of analysis of drugs have been validated statistically and by recovery studies.

  6. Physical and Chemical Characterization of Poly(hexamethylene biguanide Hydrochloride

    Directory of Open Access Journals (Sweden)

    Luiz Henrique C. Mattoso

    2011-06-01

    Full Text Available We present the characterization of commercially available Poly(hexamethylene biguanide hydrochloride (PHMB, a polymer with biocidal activity and several interesting properties that make this material suitable as a building block for supramolecular chemistry and “smart” materials. We studied polymer structure in water solution by dynamic light scattering, surface tension and capacitance spectroscopy. It shows typical surfactant behavior due to amphiphilic structure and low molecular weight. Spectroscopic (UV/Vis, FT-NIR and thermal characterization (differential scanning calorimetry, DSC, and thermogravimetric analysis, TGA were performed to give additional insight into the material structure in solution and solid state. These results can be the foundation for more detailed investigations on usefulness of PHMB in new complex materials and devices.

  7. N-hydroxyurea, mitomycin C and actinomycin D activity in the process of tumour formation on the primary leaves of the 'Pinto' bean

    Directory of Open Access Journals (Sweden)

    Aldona Rennert

    2014-01-01

    Full Text Available Mitomycin C (MC, N-hydroxyurea (HU and actinomycin D (AD inhibit tumour formation on the primary leaves of Pinto beans. Agrobacterium tumefaciens was inoculated into bean leaves with application of the above named inhibitors at various times. It was found that MC action is strongest during inoculation and immediately after it, the maximal effect of HU take place within 12 h after inoculation, whereas the antitumour action of AD starts as late as 12 h after leaf inoculation. In view of the different degree of susceptibility of bacteria and plant cells to the inhibitors applied, the above described results allowed to distinguish three critical periods in the process of tumour formation in the tested host-pathogen system.

  8. Comparison of the antifungal efficacy of terbinafine hydrochloride and ciclopirox olamine containing formulations against the dermatophyte Trichophyton rubrum in an infected nail plate model.

    Science.gov (United States)

    Täuber, Anja; Müller-Goymann, Christel C

    2014-07-07

    Onychomycosis is a fungal infection mostly induced by dermatophytes such as Trichophyton rubrum. Due to slow nail growth, the treatment takes 3-9 months depending on the nail size and infected area. Hence, high efficacy of the active ingredient without systemic side effects is of major interest. To test the efficacy of an antifungal formulation, an appropriate in vitro model reflecting the in vivo situation as close as possible is required. In this study, a variety of antifungal formulations, i.e., commercial ones (Ciclopoli and Lamisil cream), those used in compounding pharmacies (Pentravan) as well as poloxamer 407-based systems, have been evaluated in an infected nail plate model. The active pharmaceutical ingredients (APIs) were ciclopirox olamine and terbinafine hydrochloride. The poloxamer 407-based formulations consisted of poloxamer 407, double distilled water, propylene glycol, isopropyl alcohol, medium chain triglycerides and either 1% ciclopirox olamine or 1% terbinafine hydrochloride as API, respectively. Former studies have shown high permeation rates of terbinafine hydrochloride from similar poloxamer 407-based formulations with dimethyl isosorbide instead of propylene glycol. The present contribution shows superior inhibition of T. rubrum growth from poloxamer 407-based formulations in comparison to the commercial Lamisil cream. Moreover, poloxamer 407-based formulations were equally effective as the nail lacquer Ciclopoli even though the poloxamer formulations contained only 1% of the drug instead of 8% in the marketed lacquer. Poloxamer 407-based systems containing ciclopirox olamine proved to be about as effective as similar terbinafine hydrochloride systems.

  9. Improved antitumor activity and reduced cardiotoxicity of epirubicin using hepatocyte-targeted nanoparticles combined with tocotrienols against hepatocellular carcinoma in mice.

    Science.gov (United States)

    Nasr, Magda; Nafee, Noha; Saad, Hoda; Kazem, Amani

    2014-09-01

    Hepatocellular carcinoma (HCC) is the third most common cause of cancer death worldwide. Epirubicin (EPI), an anthracycline derivative, is one of the main line treatments for HCC. However, serious side effects including cardiomyopathy and congestive heart failure limit its long term administration. Our main goal is to develop a delivery strategy that ensures improved efficacy of the chemotherapeutic agent together with reduced cardiotoxicity. In this context, EPI was loaded in chitosan-PLGA nanoparticles linked with asialofetuin (EPI-NPs) selectively targeting hepatocytes. In an attempt to reduce cardiotoxicity, targeted EPI-NPs were coadministered with tocotrienols. EPI-NPs significantly enhanced the antiproliferative effect compared to free EPI as studied on Hep G2 cell line. Nanoencapsulated EPI injected in HCC mouse model revealed higher p53-mediated apoptosis and reduced angiogenesis in the tumor. Combined therapy of EPI-NPs with tocotrienols further enhanced apoptosis and reduced VEGF level in a dose dependent manner. Assessment of cardiotoxicity indicated that EPI-NPs diminished the high level of proinflammatory cytokine tumor necrosis factor-α (TNF-α) as well as oxidative stress-induced cardiotoxicity as manifested by reduced level of lipid peroxidation products (TBARS) and nitric oxide (NO). EPI-NPs additionally restored the diminished level of superoxide dismutase (SOD) and reduced glutathione (GSH) in the heart. Interestingly, tocotrienols provided both antitumor activity and higher protection against oxidative stress and inflammation induced by EPI in the heart. This hepatocyte-targeted biodegradable nanoparticle/tocotrienol combined therapy represents intriguing therapeutic strategy for EPI providing not only superior efficacy but also higher safety levels. Copyright © 2014 Elsevier B.V. All rights reserved.

  10. Pressure injection of methyl 2-benzimidazole carbamate hydrochloride solution as a control for Dutch elm disease

    Science.gov (United States)

    Garold F. Gregory; Thomas W. Jones

    1973-01-01

    A preliminary evaluation of the effectiveness of injecting methyl 2-benzimidazole carbamate hydrochloride solution into elms for prevention or cure of Dutch elm disease is reported. Symptom development was diminished or prevented in elms injected with fungicide before inoculation. Symptom development was arrested in all crown-inoculated diseased trees injected with the...

  11. A chiral capillary electrophoresis method for ropivacaine hydrochloride in pharmaceutical formulations : Validation and comparison with chiral liquid chromatography

    NARCIS (Netherlands)

    Sänger-Van De Griend, C. E.; Wahlström, H.; Gröningsson, K.; Widahl-Näsman, Monica E.

    A capillary electrophoresis method for the determination of the enantiomeric purity of the local anaesthetic ropivacaine hydrochloride in injection solutions has been validated. The method showed the required limit of quantitation of 0.1% enantiomeric impurity. Good performances were shown for

  12. One-year outcomes of a bilateral randomised prospective clinical trial comparing PRK with mitomycin C and LASIK.

    Science.gov (United States)

    Wallau, A D; Campos, M

    2009-12-01

    To compare 1-year follow-up results of photorefractive keratectomy (PRK) with mitomycin C (MMC) and laser in situ keratomileusis (LASIK) for custom correction of myopia. Eighty-eight eyes of 44 patients with moderate myopia were randomised to PRK with 0.002% MMC for 1 min in one eye and LASIK in the fellow eye. The 1-year follow-up was evaluated. There were no differences between LASIK and MMC-PRK eyes preoperatively. Forty-two patients completed the 1-year follow-up. MMC-PRK eyes achieved better uncorrected visual acuity (p = 0.03) and better best-spectacle-corrected visual acuity (pPRK eyes postoperatively. Excellent vision was reported in 64% of LASIK and 74% of MMC-PRK eyes 1 year after surgery. The corneal resistance factor and corneal hysteresis (ORA, Reichert) were higher in LASIK than in MMC-PRK eyes (pPRK with 0.002% MMC was more effective than wavefront-guided LASIK for correction of moderate myopia. Further research is necessary to determine the optimal concentration, exposure time and long-term corneal side effect of MMC.

  13. A validated stability-indicating high performance liquid chromatographic method for moxifloxacin hydrochloride and ketorolac tromethamine eye drops and its application in pH dependent degradation kinetics

    Directory of Open Access Journals (Sweden)

    Jayant B Dave

    2013-01-01

    Full Text Available Background and Aim: A fixed dose combination of moxifloxacin hydrochloride and ketorolac tromethamine is used in ratio of 1:1 as eye drops for the treatment of the reduction of post operative inflammatory conditions of the eye. A simple, precise, and accurate High Performance Liquid Chromatographic (HPLC method was developed and validated for determination of moxifloxacin hydrochloride and ketorolac tromethamine in eye drops. Materials and Methods: Isocratic HPLC separation was achieved on a ACE C 18 column (C 18 (5 μm, 150 mm×4.6 mm, i.d. using the mobile phase 10 mM potassium di-hydrogen phosphate buffer pH 4.6-Acetonitrile (75:25 v/v at a flow rate of 1.0 mL/min. The detection was performed at 307 nm. Drugs were subjected to acid, alkali and neutral hydrolysis, oxidation and photo degradation. Moreover, the proposed HPLC method was utilized to investigate the pH dependent degradation kinetics of moxifloxacin hydrochloride and ketorolac tromethamine in buffer solutions at different pH values like 2.0, 6.8 and 9.0. Results and Conclusion: The retention time (t R of moxifloxacin hydrochloride and ketorolac tromethamine were 3.81±0.01 and 8.82±0.02 min, respectively. The method was linear in the concentration range of 2-20 μ/mL each for moxifloxacin hydrochloride and ketorolac tromethamine with a correlation coefficient of 0.9996 and 0.9999, respectively. The method was validated for linearity, precision, accuracy, robustness, specificity, limit of detection and limit of quantitation. The drugs could be effectively separated from different degradation products and hence the method can be used for stability analysis. Different kinetics parameters like apparent first-order rate constant, half-life and t 90 (time for 90% potency left were calculated.

  14. Thermodynamics of mixing of sodium naproxen and procaine hydrochloride in ethanol + water cosolvent mixtures

    OpenAIRE

    Mora Guerrero, Carolina Del Pilar

    2010-01-01

    Thermodynamic functions Gibbs energy, enthalpy, and entropy of mixing of sodium naproxen and procaine hydrochloride were evaluated. Mixing quantities were calculated based on fusion calorimetric values obtained from differential scanning calorimetry measurements and equilibrium solubility values reported in the literature for both drugs in ethanol + water mixtures. By means of enthalpy-entropy compensation analysis, non-linear ΔH°mix vs. ΔG°mix plots were obtained which indicates different me...

  15. Enhancement of antibacterial activity of ciprofloxacin hydrochloride by complexation with sodium cholate

    Directory of Open Access Journals (Sweden)

    Uduma E. Osonwa

    2017-12-01

    Full Text Available Ciprofloxacin is a broad spectrum bactericidal anti-infective agent of the fluoroquinolones class used in treatment of many bacterial infections. In recent times, there has been increasing resistance to the antibiotic. In this work, we investigated the effect of making an ion- pair complex of Ciprofloxacin – hydrochloride with Sodium cholate on bacterial activity. The optimal ratio of the reactants and pH were determined using UV spectrometry. The complex was characterized by octanol-water partitioning, melting point, and IR spectrometry. The antibacterial activity of the complex was determined against Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae, and Streptococcus pneumoniae by the agar-well diffusion method. The complex was whitish to off-white in color and crystalline, with a melting point of 238 °C. The stoichiometry of the complex shows a molar ratio of 1:1 of sodium cholate to ciprofloxacin. The best pH for complexation was pH 9. The complex partitioned 3.38 times into octanol than in water. The FTIR revealed interaction between the 4-nitrogen atom in the 7-piperazinyl group of ciprofloxacin and the carbonyl of the cholate. The drug in complex form gave double the antibacterial activity of the uncomplexed drug. This study showed that development of hydrophobic ion pair complex enhances antibacterial activity of ciprofloxacin hydrochloride. Keywords: Ciprofloxacin, Sodium cholate, Ion-pair complex, Antibacterial activity, Enhanced activity

  16. Formulation and evaluation of bilayer tablets of metoclopramide hydrochloride and diclofenac sodium.

    Science.gov (United States)

    Gattani, Surendra G; Khabiya, Sohan S; Amrutkar, Jitendra R; Kushare, Sachin S

    2012-01-01

    The main objective of the present research work was to develop a bilayer tablet of metoclopramide hydrochloride (MTH) and diclofenac sodium (DS) in separate layers to avoid incompatibility and thus to maximize the efficacy of both drugs in combination for the effective treatment of migraine headaches. MTH and DS were formulated as immediate and sustained release layers respectively. In vitro dissolution kinetic studies of an optimized (D10) batch of DS in both sustained release layer and bilayer tablet forms show good linearity of regression coefficient 0.9773 (first order equation). The results reveal that an optimized immediate release layer (M5) of MTH and a sustained release layer (D10) of DS might be suitable for the treatment of migraine by sequential release of the two drugs in a bilayer tablet. Migraine is a type of recurring headache of moderate to severe intensity associated with gastrointestinal, neurological, and autonomic symptoms. In migraine, a combination of pretreatment with antiemetics is required for symptomatic treatment, when nausea and vomiting are severe. In our present research, we have selected the metoclopramide hydrochloride (MTH) active ingredient for study because it has an antiemetic effect and is a prokinetic agent. MTH is more effective to counteract gastric stasis associated with migraine, and it enhances the rate of absorption of non-steroidal anti-inflammatory drugs (NSAIDs). In the present investigation we combine MTH and a second active ingredient, diclofenac sodium, as a formulated bilayer tablet to prevent degradation of MTH.

  17. Clinical Effects for Patients with Recurrent Advanced Non-small Cell Lung Cancer Treated with Icotinib Hydrochloride

    Directory of Open Access Journals (Sweden)

    Jingying NONG

    2013-05-01

    Full Text Available Background and objective Icotinib hydrochloride is the third single target EGFR-TKI used in clinical treatment of advanced non-small cell lung cancer (NSCLC. Clinical research reports on its efficacy and survival in patients with Recurrent Advanced NSCLC are still little.The aim of this study is to evaluate the efficacy and survival of Icotinib hydrochloride for patients with advanced non-small cell lung cancer who failed to previous chemotherapy and explore the association of clinical features with the efficacy and survival. Methods The clinical data of 60 NSCLC patients referred to the Beijing Chest Hospital, Capital Medical University from March 2009 to July 2012 were retrospectively analyzed. Results The overall response rate (ORR was 45.0% and the disease control rate (DCR was 80.0%. The median progression-free survival (PFS time was 6.7 months. RR and PFS in female were superior to male (P=0.014, 0.013, respectively. RR, DCR in 2nd-line subgroup were superior to ≥3rd-line subgroup (P=0.020, 0.024, respectively. RR, DCR and PFS in EGFR mutation carriers were significantly superior to wild-type patients (P=0.006, <0.001, 0.002, respectively . There was no statistical difference in RR and PFS between those age <65 and ≥65 or PS<2 and PS≥2. There was no statistical difference in RR and DCR between exon 19 deletion and exon 21 mutations, while the former had much longer PFS (P=0.020. EGFR mutation and exon 19 deletion are the independent prognostic factors to significantly improve the PFS (P=0.009, 0.012, respectively. The side effects were generally mild and consisted of rash and diarrhea. Conclusion Icotinib hydrochloride is effective especially in EGFR mutation carriers and well tolerated in patients with recurrent advanced non-small-cell lung cancer.

  18. Single dose pharmacokinetics of fenspiride hydrochloride: phase I clinical trial.

    Science.gov (United States)

    Montes, B; Catalan, M; Roces, A; Jeanniot, J P; Honorato, J M

    1993-01-01

    The absolute bioavailability of fenspiride has been studied in twelve healthy volunteers. It was administered IV and orally in single doses of 80 mg fenspiride hydrochloride according to a randomised crossover pattern. Following IV administration, the plasma clearance of fenspiride was about 184 ml.min-1, and its apparent volume of distribution was moderately large (215 l). When given orally as a tablet, fenspiride exhibited fairly slow ab- sorption; the maximum plasma concentration (206 ng.ml-1) was achieved 6 h after administration. The absolute bioavailability was almost complete (90%). The tablet had slow release characteristics. The elimination half-life obtained from the plasma data was 14 to 16 h independent of the route of administration.

  19. Multilayer Films and Capsules of Sodium Carboxymethylcellulose and Polyhexamethylenguanidine Hydrochloride

    Science.gov (United States)

    Guzenko, Nataliia; Gabchak, Oleksandra; Pakhlov, Evgenij

    The complexation of polyhexamethylenguanidine hydrochloride (PHMG) and sodium carboxymethylcellulose (CMC) was investigated for different conditions. Mixing of equiconcentrated aqueous solutions of the polyelectrolytes was found to result in the formation of an insoluble interpolyelectrolyte complex with an overweight of carboxymethylcellulose. A step-by-step formation of stable, irreversibly adsorbed multilayer film of the polymers was demonstrated using the quartz crystal microbalance method. Unusually thick polymer shells with a large number of loops and tails of the polyanion were formed by the method of layer-by-layer self-assembly of PHMG and CMC on spherical CaCO3 particles. Hollow multilayer capsules stable in neutral media were obtained by dissolution of the inorganic matrix in EDTA solution.

  20. 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. Copyright © 2010 John Wiley & Sons, Ltd.