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格列吡嗪 Eudragit 微球的设计、体外和体内评价。

Design, in vitro and in vivo evaluation of glipizide Eudragit microparticles.

机构信息

Department of Pharmacy, Annamalai University, Annamalai Nagar, India.

出版信息

J Microencapsul. 2010;27(4):281-91. doi: 10.3109/02652040903131319.

Abstract

Glipizide microparticles made with Eudragit (RS 100 and RL 100), prepared by emulsion solvent evaporation technique were evaluated for various in-vitro properties viz. encapsulation efficiency, particle size and surface morphology, drug release pattern and in-vivo hypoglycaemic activity. The optimized formulation parameters were used to prepare smooth and spherical microparticles (2-32 microm) with higher entrapment efficiency (67-89%). Drug release patterns of glipizide microparticles of Eudragit RS 100 and Eudragit RL 100 with drug-to-polymer ratio of 1 : 4 (i.e. EGM14 and ELGM14) have shown gradual and extended release for 24 h with cumulative release of glipizide to the extent of 72.3% and 83.9%, respectively. However, EGM14 showed a significant in-vivo hypoglycaemic effect up to 12 h in rabbits while ELGM14 showed for 9 h. Hence, glipizide microparticles of Eudragit RS 100 (glipizide: polymer 1 : 4) is better suited for oral sustained release formulation.

摘要

采用乳液溶剂蒸发技术制备的包封格列吡嗪的 Eudragit(RS 100 和 RL 100)微球,评价其各种体外性质,如包封效率、粒径和表面形态、药物释放模式和体内降血糖活性。优化的制剂参数用于制备具有较高包封效率(67-89%)的光滑、球形微球(2-32μm)。Eudragit RS 100 和 Eudragit RL 100 的格列吡嗪微球(药物-聚合物比为 1:4,即 EGM14 和 ELGM14)的药物释放模式显示出 24 小时内逐渐和延长释放,格列吡嗪的累积释放分别达到 72.3%和 83.9%。然而,EGM14 在兔子体内显示出显著的降血糖作用,持续 12 小时,而 ELGM14 则持续 9 小时。因此,Eudragit RS 100(格列吡嗪:聚合物 1:4)的格列吡嗪微球更适合口服缓释制剂。

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