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Research Article Open Access
Enalapril is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension, diabetic nephropathy, and some types of chronic heart failure. The serum concentration profile of Enalapril exhibits a prolonged terminal phase apparently representing a small fraction of the administered dose that has been bound to ACE.The amount bound does not increase with dose, indicating a saturable site of binding. The effective half-life for accumulation of enalapril following multiple doses of enalapril maleate is 11 hours. The aim of the present investigation is to increase the gastric residence time by preparing gastro retentive floating bilayered tablet thereby by improving bioavailability. Fourier transform Infrared spectroscopy confirmed the absence of any drug/polymer interactions. Eight formulations (FE1 to FE8) were prepared using various polymers such as HPMC K15M, Sodium Carboxymethylcellulose in different ratios. Direct compression was adapted to compress bilayer floating tablet. The prepared bilayer floating tablet were evaluated for hardness, weight variation, thickness, Friability, drug content, buoyancy lag time, total floating time and in- vitro dissolution studies. Drug content (98.23-99.75%) was found uniform for all batches. percentage drug release was found to be 87.84 % to 97.27 % after 12 hours. Release of bi layered formulations follows zero order kinetics (0.8661 to 0.9649) except formulation FE1. When drug release data fitted to Korsmeyer equation, the values of slope ‘n’ (0.603 to 0.6981) indicated that the drug release was by non-fickian mechanism. FE4 was considered as optimized formulation which exhibited 84.91% of drug releases in 14 hours. The values were within the permissible limits.
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Author(s): Anil Kumar AP, Felix Joe V., Vishwanath B. A