Posted by admin on Nov 1, 2013 in |
The present study was carried out to assess the pharmacokinetic drug interaction between nebivolol and cefixime following single oral dose administration in hypertensive patients. Therapeutic dose of nebivolol alone and combination with cefixime were administered to a separate group of hypertensive patients. Serial blood samples were collected at pre-dose (0.0) to 48 h post-dose following each treatment to characterize the pharmacokinetic parameters. The plasma nebivolol concentrations were estimated by a sensitive liquid chromatographic mass spectrometry (LC-MS) method. Mean (SD) of AUC0-t (ng.h/mL) and AUC0–∞ (ng.h/mL) for nebivolol given as a combination versus nebivolol alone is 39.24 (6.96) vs. 17.29 (4.60) and 45.30 (6.70) vs. 24.42 (5.08) respectively. Corresponding values for Cmax (ng/mL) is 2.98 (0.47) vs. 3.09 (0.37). Cefixime significantly increased the extent of exposure of nebivolol when used in combination. There was minor change in the peak exposure and elimination parameters. The results indicate that there observed to be a pharmacokinetic interaction when nebivolol is administered in combination with cefixime. Hence, the combination is contraindicated or used with...
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Posted by admin on Nov 1, 2013 in |
The aim of the work is to formulate sustained release matrix tablets of simvastatin and to optimize them using Response Surface Methodology. The tablets were prepared by direct compression method and evaluated as per pharmacopoeia methodology. A central composite design for 2 factors at 3 levels each was employed to systematically optimize drug release profile. Concentration of HPMC K15M (X1) and PVP K30 (X2) were taken as the independent variables and the in vitro dissolution (Y1), t50% (Y2) and mean dissolution time (Y3) as dependent variables. Response surface plots and contour plots were drawn, and the optimum formulations were selected by feasibility and grid searches. Both the polymers had a significant effect on drug release from the tablets. The formulations were followed Higuchi drug kinetics and diffusion was the prime mechanism of drug release. The polynomial mathematical models produce for various response variables using the regression analysis and were found to be statistically significant (P< 0.05). Optimization study was validated using 8 confirmatory runs, indicated very high degree of...
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Posted by admin on Nov 1, 2013 in |
A liquid chromatographic method has been developed and validated for the determination of the clinical trial combination of Solifenacin succinate and Tamsulosin hydrochloride. Effective chromatographic separation was achieved on an eclipse XDB-C18 (4.6 mm X 150 mm, 5µm) column using isocratic reverse phase technique. The mobile phase employed was ACN: 20Mm sodium phosphate buffer (0.2% Triethylamine) (30:70), the pH was adjusted to 3.0 by ortho phosphoric acid. The flow rate was maintained at 1.0 mL/min and elutewasmonitoredat225nm. A linear response was observed over the concentration range 15-75 µg/mL (R2=0.999) of Solifenacin and the concentration range 1-5 µg/mL (R2=0.999) of Tamsulosin.The limit of quantitation (LOQ) and limit of detection (LOD) for Solifenacin were 0.04 and 0.14 µg/mL, respectively and for Tamsulosin were 0.05 and 0.1 µg/mL, respectively. The method was successfully validated in accordance to ICH guideline Q2. The RSD for intra-day and for inter-day precision were found to be lesser than 1.5% for Solifenacin. The RSD for intra-day and for inter-day precision were found to be lesser than 1%...
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Posted by admin on Nov 1, 2013 in |
Reaction of 4-fluorobenzylchloride with 2-thiouracil (1) gave 2-(4-fluorobenzylthio)pyrimidin-4(3H)-one (2), which on chlorination with POCl3 furnished 4-chloro-2-(4-fluorobenzylthio)-4-chloropyrimidine (3). This intermediate when treated with various substituted anilines gave desired targeted compounds 4(a-k) in 50-90% yield. Structural assignments of the synthesized compounds were based on their IR, 1H NMR, Mass and analytical data. The antimicrobial evaluation of newly synthesized compounds was carried out by cup-plate method. The investigation of antimicrobial screening reveals that the compounds 4b, 4g, 4c and 4f showed good activity against bacterial strain B. subtilis. Compounds4a, 4e, 4b, 4c, 4f, 4g and 4h wereactive against bacterial strain P. aeruginosa. Compounds 4a and 4c were active against fungul strain A. niger. Compounds 4e, 4b and 4j showed good activity against fungal strain A. flavus. All the synthesized compounds showed excellent antifungal activity against T.viridae. Remaining compounds exhibited moderate to poor activity against bacterial and fungal strains when compared to standard drugs Gentamycin and Fluconazole respectively. So, further we have carried out the antifungal screening of all the synthesized compounds at...
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Posted by admin on Nov 1, 2013 in |
The study was undertaken to compare the efficacy and safety of Glimepiride and Metformin in the management of patients with type 2 DM. The present invention is directed to a pharmaceutical composition in the form of a capsule with increased bioavailability as well as the process for obtaining said composition. The tablet of the present invention comprises two active ingredients comprising two oral hypoglycemic agents: one phase with a sulphonylurea, such as immediate release Glimepiride and second phase with a biguanide, such as extended release Metformin hydrochloride (Metformin HCL). This composition of capsule, which can include over 500mg of Metformin HCL (i.e. up to daily requirements of each patient), is to be orally administered once or twice a day. The combination of these hypoglycemic agents has a synergic effect.Finally we can explain that the availability of Metformin-Glimepiride combination can minimize the effects of diabetic conditions. From the complete work we assume that these hypoglycemic agents have a synergistic effect and therefore a greater effectiveness in controlling the blood glucose...
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