DR VACHASPATI DUBEY,DR RASHMI KUMARI,Bhuneshwar Dutta Tripathi
申请号：
IN201831002434
公开号：
IN201831002434A
申请日:
2018.01.21
申请国别(地区):
IN
年份:
2018
代理人:
摘要：
The present invention relates to development of coated pharmaceutical dosage forms of extended release of HMG CoA reductase inhibitor and immediate release of Antihyperlipidemic drug using different polymers by wet granulation techniques for the management hypercholesterolemia and hyperlipidaemia. Invention is aimed at controlling the absolute oral bioavailability and high hepatic extraction of HMG CoA reductase inhibitor due to its consistent first-pass uptake into the liver after oral dosing. The main aim is to minimize the liver extraction ratio by controlling the release of drug from the dosage form. Granules were characterized by Fourier transformed Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Powder X-Ray Diffractometry (XRD) as well as by content uniformity, in vitro dissolution studies and release kinetics. Selected granular system was compressed by direct compression. Compressed disc were evaluated for drugs content, weight variation, friability, hardness, thickness, % assay and in-vitro dissolution studies. Prepared disc were then coated and evaluated for drugs content, weight variation, friability, hardness, thickness, % assay and in-vitro dissolution studies. Cellulose polymers, MCC and HPMC K4M, showed better control over drug(s) release. Formulated disc gave satisfactory results for various physicochemical evaluations like weight variation, content uniformity and in vitro drug release. Developed dosage form best fitted to korsmeyer peppas and first order model rate kinetics. Formulations are optimized on the basis of IR/CR release of drugs. In vitro study showed that optimized disc formulation released immediate dose of antihyperlipidemic drug and then sustained release of HMG CoA reductase inhibitor for more than twelve hours. Thus the objective of the work is to formulate a coated disc dosage form of antihyperlipidemic and HMG CoA reductase inhibitor to minimize hepatic extraction has been achieved with succe
