31 research outputs found
Fighting Antibiotic Resistance: New Pyrimidine-Clubbed Benzimidazole Derivatives as Potential DHFR Inhibitors
No full textThe present work describes the design and development of seventeen pyrimidine-clubbed benzimidazole derivatives as potential dihydrofolate reductase (DHFR) inhibitors. These compounds were filtered by using ADMET, drug-likeness characteristics calculations, and molecular docking experiments. Compounds 27, 29, 30, 33, 37, 38, and 41 were chosen for the synthesis based on the results of the in silico screening. Each of the synthesized compounds was tested for its in vitro antibacterial and antifungal activities using a variety of strains. All the compounds showed antibacterial properties against Gram-positive bacteria (Staphylococcus aureus and Staphylococcus pyogenes) as well as Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa). Most of the compounds either had a higher potency than chloramphenicol or an equivalent potency to ciprofloxacin. Compounds 29 and 33 were effective against all the bacterial and fungal strains. Finally, the 1,2,3,4-tetrahydropyrimidine-2-thiol derivatives with a 6-chloro-2-(chloromethyl)-1H-benzo[d]imidazole moiety are potent enough to be considered a promising lead for the discovery of an effective antibacterial agent
Development of validated RP-HPLC method for the simultaneous estimation of atenolol and chlorthalidone in combine tablet dosage form
No full textA RP-HPLC method for the estimation of ATN (Atenolol) and CTN (chlorthalidone) in combined dosage form was developed using Comosil RP-C18 (4.6 x 250mm, 5m) in an gradient mode with mobile phase comprising of Methanol: Water (pH 3 using OPA) The flow rate was 1 mL/ min and effluent was monitored at 226.0 nm. The retention times were found to be 2.2 min for ATN and 3.36 min for CTN. The assay exhibited a linear dynamic range of 40- 200 g/mL for ATN and 10- 50 g/mL for CTN. The calibration curves were linear (r 2 = 0.999 for ATN and r 2 = 0.999 for CTN) over the entire linear range. Mean % recovery was found to be 99.78 % for ATN and 99.30 % for CTN with % RSD was NMT 2 for both estimations which fully agrees with system suitability which is in good agreement with labeled amount of formulation. The % RSD for Intra- Day and Inter-Day Precision was NMT than 2 for both the drugs. The developed method was validated as per ICH guideline
DETERMINATION OF ATORVASTATIN CALCIUM IN PHARMACEUTICAL FORMULATIONS BY REVERSE PHASE-HIGH PERFORMANCE LIQUID CHROMATOGRAPHY
No full textA simple, sensitive and reproducible reverse-phase high performance liquid chromatographic (RP-HPLC) method has been developed for the quantitative estimation of Atorvastatin calcium in the pharmaceutical formulations. Chromatographic separation was achieved on a 250 × 4.6 mm, 5μ, Waters symmetry column. The flow rate was 1ml/min and eluent was monitored by absorbance at 246 nm using a mixture of Methanol and Acetonitrile (pH 3.
Development of stability indicating assay method for estimation of Ibuprofen and Famotidine in combined dosage form in tablet
No full textA simple, precise, accurate, simultaneous stability indicating RP-HPLC method for the estimation of IBU (Ibuprofen) and FMT (Famotidine) in combined dosage form was developed using Grace RP-C18 (4.6 x 250mm, 5m) in an gradient mode with mobile phase comprising of Methanol: Water (pH 2.5 using OPA) The flow rate was 0.7 mL/ min and effluent was monitored at 240.0 nm. The retention times were found to be 6.68 min for IBU and 1.76 min for FMT. The assay exhibited a linear dynamic range of 30- 150 g/mL for IBU and 1- 5 g/mL for FMT. The calibration curves were linear (r 2 = 0.994 for IBU and r 2 = 0.997 for FMT) over the entire linear range. Mean % recovery was found to be 99.82 % for IBU and 99.91 % for FMT with % RSD was NMT 2 for both estimations which fully agrees with system suitability which is in good agreement with labeled amount of formulation. The % RSD for Intra- Day and Inter-Day Precision was NMT than 2 for both the drugs. The developed method was validated as per ICH guideline
Phytochemical Screening & in vivo Fertility Enhancing Activity (Aphrodisiac) of Abutilon indicum Roots on Male Wistar Rats
No full textEVALUATION OF ANTI-ASTHMATIC ACTIVITY OF METHANOLIC EXTRACT OF BERLERIA PRIONITIS LINN. AERIAL PARTS
No full textObjective: The aim of the present study is to evaluate the aerial parts of a plant of Barleria prionitis Linn., for its antiasthmatic activity with the separation of active moieties.Methods: Adult wistar albino rats were used for the anti-inflammatory study. Histamine-induced bronchospasm was conducted on isolated goat trachea.Results: The dried and powdered aerial parts of Berleria prionitis was extracted with continuous soxhlet extraction with Petroleum ether (40-60 ° C), Chloroform, Ethyl acetate, Acetone, Methanol, and Hydroalcoholic solvents. Preliminary phytochemical screening of all extracts was done. Preliminary animal studies by In vitro isolated goat trachea chain preparation of all extracts were done to find out the potent extract. In this study, the methanolic extract of aerial parts of Berleria prionitis was found to be potent comparative to another extract. The results of carrageenan induced rat paw oedema model indicated the dose-dependant anti-inflammatory activity. As compared to standard drug (Indomethacin), methanolic extract showed similar activity which was found to be statistically significant (P<0.0001). The extent of DPPH radical scavenging was determined by calculated the IC50 value of methanolic extract Berleria prionitis (133.5) compared with the Ascorbic acid (114.7) taken as standard. In the present study, the histamine-induced dose-dependent contraction of goat tracheal chain was significantly inhibited (p<0.001) by methanolic extract of aerial parts of Berleria prionitis (200 μg/ml). Thus the present study revealed that the methanolic extract of Berleria prionitis (MEBP) has significant antihistaminic (H1 receptor antagonist) activity.Conclusion: In view the fact that tribal have well experienced the antiasthmatic effects of the roots of Barleria prionitis Linn. The results of our study, for the first time, show that the methanolic extract of aerial parts of Berleria prionitis Linn. possesses antioxidant, anti-inflammatory, Bronchodilator properties and therefore can be used for the antiasthmatic treatment
FORMULATION AND EVALUATION OF IMMEDIATE RELEASE TABLETS OF METFORMIN HYDROCHLORIDE ON LABORATORY SCALE
No full textThe purpose of this research is to prepare metformin hydrochloride immediate release tablets by wet granulation technique. In order to obtain the best, optimized product ten different formulations were developed. Different binder, disintegrants and lubricants taken as variables. Weight variation, thickness, hardness, friability, disintegration time, in-vitro release and pharmaceutical assay were studied as response variables. Capping was observed in formulation containing PVP K-30. However, in the remaining formulation containing PVP K-90, no capping was observed. The formulation A7 was selected as optimized formulation. The different physical properties and in-vitro release profile showed best comparable with the reference product. Optimization has proven an effective tool in product development
Chromatographic Development of validated analytical method for the estimation of tapentadol and paracetamol in combined dosage form
No full textA simple, sensitive an isocratic RP-HPLC method for the estimation of TAP (Tapentadol) and PARA (Paracetamol) in combined dosage form using Inertsil ODS C-18 column (250.6 mm, 5 ) in an isocratic mode with mobile phase comprising Buffer (1mL TEA) : ACN : MeOH in the ratio of (75:20:5 v/v/v). The flow rate was 1.2 mL/ min and effluent was monitored at 220 nm. The retention times were found to be 6.88 min for TAP and 3.78 min for PARA. The assay exhibited a linear dynamic range of 11.89- 28.55 g/mL for TAP and 64.95- 155.90 g/mL for PARA .The calibration curves were linear (r = 0.999 for TAP and r = 0.9996 for PARA) over the entire linear range
DETERMINATION OF TELMISARTAN AND FORCED DEGRADATION BEHAVIOR BY RP-HPLC IN TABLET DOSAGE FORM
No full textA simple, rapid, precise, rapid, sensitive and reproducible reverse phase high performance liquid chromatographic (RP-HPLC) method for determination of Telmisartan in tablet dosage form was developed and validated. Chromatographic separation was achieved on a 250 × 4.6 mm, 5μ, Waters symmetry column in gradient mode, with mobile phase consisting of a mixture of solution (10 mM potassium dihydrogen phosphate, pH 3.
