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头孢呋辛酯胃内漂浮给药系统:体外评价

Intragastric floating drug delivery system of cefuroxime axetil: In vitro evaluation.

作者信息

Patel Viral F, Patel Natavarlal M

机构信息

Department of Pharmaceutics, Shri B. M. Shah College of Pharmacuetical Education and Research, Dhansura Road, 383315, Modasa, Gujarat, India.

出版信息

AAPS PharmSciTech. 2006 Mar;7(1):E118-E124. doi: 10.1208/pt070117. Epub 2017 Mar 8.

Abstract

This investigation describes the development of an intragastric drug-delivery system for cefuroxime axetil. The 3 full factorial design was employed to evaluate contribution of hydroxypropyl methyl cellulose (HPMC) K4M/HPMC K100 LV ratio (polymer blend) and sodium lauryl sulfate (SLS) on drug release from HPMC matrices. Tablets were prepared using direct compression technique. Formulations were evaluated for in vitro buoyancy and drug release study using United States Pharmacopeia (USP) 24 paddletype dissolution apparatus using 0.1N HCl as a dissolution medium. Multiple regression analysis was performed for factorial design batches to evaluate the response. All formulations had floating lag times below 2 minutes and constantly floated on dissolution medium for more than 8 hours. It was found that polymer blend and SLS significantly affect the time required for 50% of drug release, percentage drug release at 12 hours, release rate constant, and diffusion exponent (P<.05). Also linear relationships were obtained between the amount of HPMC K100 LV and diffusion exponent as well as release rate constant. Kinetic treatment to dissolution profiles revealed drug release ranges from anomalous transport to case 1 transport, which was mainly dependent on both the independent variables.

摘要

本研究描述了头孢呋辛酯胃内给药系统的研发情况。采用三因素全因子设计来评估羟丙基甲基纤维素(HPMC)K4M/HPMC K100 LV比例(聚合物共混物)和十二烷基硫酸钠(SLS)对HPMC基质药物释放的影响。采用直接压片技术制备片剂。使用美国药典(USP)24桨法溶出装置,以0.1N盐酸作为溶出介质,对制剂进行体外漂浮性和药物释放研究。对全因子设计批次进行多元回归分析以评估响应。所有制剂的漂浮滞后时间均低于2分钟,并在溶出介质上持续漂浮超过8小时。研究发现,聚合物共混物和SLS显著影响50%药物释放所需时间、12小时药物释放百分比、释放速率常数和扩散指数(P<0.05)。此外,HPMC K100 LV的用量与扩散指数以及释放速率常数之间存在线性关系。对溶出曲线的动力学处理表明,药物释放范围从非正规转运到1型转运,这主要取决于两个自变量。

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Floating drug delivery systems: a review.漂浮药物递送系统:综述
AAPS PharmSciTech. 2005 Oct 19;6(3):E372-90. doi: 10.1208/pt060347.

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