Posted by admin on Dec 31, 2016 in |
Background: Antimicrobials are used for bacterial infections & has a great benefits in health related problems of human life. The main objectives of medicinal chemistry is synthesising and producing newer molecules having a valuable significant therapeutic action. Quinolones has a considerable scientific and clinical interest since their discovery. Objective: Quinolones class of drugs are useful in the treatment of serious bacterial infections thus keeping in view a potential approach is made for synthesising & characterizing of newer quinolone derivatives for their biological activity. Method: Quinolone ester was synthesised from Gould-Jacob reaction by using substituted aniline & diethylethoxymethelene malonate (EMME) Results: Solubility of all synthesised compounds were checked in various solvents & were characterized by FT-IR, 1H-NMR. Conclusion: The result of the present study thus demonstrates the anti-microbial activity against gram positive (Bacillus subtilis) & gram negative (Escherichia coli)...
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Posted by admin on Dec 31, 2016 in |
Increasing use of bioinformatics made very easy to researchers in biological and drug discovery field. Bioinformatics is involved at each and every step of drug discovery to drug development. The first step of the drug discovery is a question about disease and the treatment by drugs and whenever term drug comes, means something has to be given and the second question arises the given compound is drugable or not. To check any drugable compound the compound has to be cleared by the ADME studies and the main sensitive parameter blood brain barrier. Bioinformatics made it easy without use of model organism and waste of time. In this study we aimed to predict the blood brain barrier parameters on 87 drugs about their drug...
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Posted by admin on Dec 31, 2016 in |
Diclofenac Sodium, being NSAID, its oral administration restricted due to its inherent problems. Hence in the present study, attempt has been made to design oral sustained release once daily matrix tablets of Diclofenac Sodium using combination of hydroxyl propyl methyl cellulose (HPMC) & PEG 6000 and to study the effect of various process and formulation variables like polymer properties and polymer viscosity on in-vitro release of drug. Sustained release tablets of Diclofenac sodium were prepared using different proportion of HPMC 4000 cps and PEG 6000 (F1, F2, F3……..F6). The physical properties of prepared tablets like hardness, friability, weight variation, thickness and drug content were studied and were found to be within the acceptable limits. In-vitro release studies were performed in Simulated Gastric Fluid (SGF) pH-1.2 for two hours and Simulated Intestinal Fluid (SIF) pH-6.8 for subsequent 10 hours by USP-I dissolution apparatus, in 900 ml at 37.5±0.5oC (stirring speed was 70 rpm). As amount of HPMC was increased from 5% to 30%, released rate was decreased. However, no appreciable...
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Posted by admin on Dec 31, 2016 in |
Extended release hydrophilic matrix tablet formulations of cefuroxime axetil were developed and evaluated to observe the effect of different high viscosity hydroxypropyl methylcellulose (Methocel® K100M, K100M CR and K100LV CR) polymers on in vitro drug release. Fifteen different formulations (F1-F15) were prepared by direct compression. The results of the physical parameters and assay were found to be within the acceptable range of USP 36/NF 31. In vitro dissolution of each formulation, suitably compressed with 9.50±1.10 to 13.47±1.29 Kg hardness were performed in 0.07N HCl, distilled water, 0.1N HCl of pH 1.2 and phosphate buffers of pH 4.5 and 6.8 to observe the drug release. The drug release was higher with K100 LV CR polymer (F14, F15) as compare to K100M and K100M CR in 0.07N HCl (74.22%±0.69 for F14 and 83.57%±0.71 for F15) and in distilled water medium (65.19%±0.78 for F14 and 79.66%±1.05 for F15). The drug release rate from tablets containing K100LV CR was effectively controlled by decreasing the polymer concentration from 30-10%. Model-dependent method were used for...
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Posted by admin on Dec 31, 2016 in |
This present work is on method development of assay and related substances of Vardenafil HCl and degradation of drug substance under acid, base hydrolysis and oxidation conditions. Identification of the impurities were done by the UPLC-TOF. Waters LCT Premier time of flight HRMS instrument with 5 ppm accuracy employed for degradation impurity identification. The validation of the method for its impurities was done in RP-UPLC chromatography as per the ICH Q2(R1) guidelines and the validation parameters such as specificity with all the process and degradation impurities, linearity, precision, accuracy, solution stability, mobile phase stability, robustness and ruggedness parameters met acceptance criteria as per ICH...
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