克拉霉素抗溃疡胃留置片的研制与表征

Rajesh Sharma, A. Mishra
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引用次数: 1

摘要

胃保留漂浮给药系统(GFDDS)用于延长口服给药后胃在特定部位的停留时间,并控制或修饰药物从制剂中的释放。本研究的目的是开发一种胃保留漂浮给药系统,以实现控释,从而提高制剂的生物利用度。基于克拉霉素生物制药特性的构效关系表明克拉霉素具有良好的生物制药特性。为治疗幽门螺杆菌引起的胃溃疡,设计了克拉霉素漂浮剂型。采用湿法制备颗粒,并对其流动性能、卡尔斯指数、容重、抽头密度和豪斯纳比进行了评价。以不同黏度的聚合物为胶凝剂,碳酸氢钠为生气剂和其他赋形剂设计剂型。进一步对颗粒进行片剂制备,并根据硬度、体外浮力、体外释药等不同评价参数对制备的片剂进行评价。优化配方(F7)含克拉霉素、HPMC、90sh、HPMC K4M、碳酸氢钠,10 h释药率约为86.6%。关键词:GFDDS,幽门螺杆菌,胶凝剂,体外浮力,HPMC,湿法造粒。
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DEVELOPMENT AND CHARACTERIZATION OF GASTRO RETENTIVE TABLETS OF CLARITHROMYCIN FOR ANTIULCER EFFECT
Gastroretentive floating drug delivery system (GFDDS) is used to prolong the gastric residence time after oral administration, at a particular site and controlled or modified the release of drug from the formulation.The purpose of the present study is to develop a gastro retentive floating drug delivery system to achieving controlled release so that is improves bioavailability of the formulation, Structure activity relationship based on Biopharmaceutical Properties of Clarithromycin indicates good biopharmaceutical Properties. Floating dosage form of Clarithromycin was designed for the treatment of gastric ulcer caused by Helicobacter pylori. The granules were prepared by wet granulation method and evaluated for flow property, Carrs' index, bulk density, tapped density and Hausner ratio. The dosage form was designed by using polymers of different viscosity as gelling agents, sodium bicarbonate as gas generating agent and other excipients. The granules were further subjected to tablet preparation and the prepared tablets were subjected for evaluated on the basis of different evaluation parameters like hardness, in vitro buoyancy, in vitro drug release. Incorporation of gas generating agent together with polymer improved drug release Optimized formulation (F7) containing Clarithromycin, HPMC, 90 SH , HPMC K4M , sodium bicarbonate, released approximately 86.6% drug in 10 hrs. and the floating lag time was found to be 25 sec. KEYWORDS: GFDDS, Helicobacter pylori, gelling agents, in vitro buoyancy, HPMC, wet granulation.
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