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羟丙基淀粉,不同直链淀粉含量,作为片剂的控释基质。

Hydroxypropylated starches of varying amylose contents as sustained release matrices in tablets.

机构信息

Department of Food Science, University of Arkansas, 2650 N. Young Ave., Fayetteville, AR 72704, USA.

出版信息

Int J Pharm. 2010 Jan 29;385(1-2):104-12. doi: 10.1016/j.ijpharm.2009.10.038. Epub 2009 Oct 30.

DOI:10.1016/j.ijpharm.2009.10.038
PMID:19879935
Abstract

Waxy corn, Hylon VII, and common corn starches were hydroxypropylated to low and high levels, and their sustained release properties and matrix characteristics were studied. Hydroxypropylation had a stronger impact on Hylon VII and common corn starch matrices than on waxy corn ones, suggesting that the behavior of starch tablet was dominated by its amylose content. The introduction of hydroxypropyl groups increased the water holding capacity of all starches and resulted in more fluid-like and softer matrices with increased chain mobility for amylose-containing starches. There was a decrease in the tablet porosity and in the storage modulus of swollen tablets of Hylon VII and common corn starches after hydroxypropylation. Microscopic analyses revealed smoother and less porous tablet structure upon hydroxypropylation of all starches. Hydroxypropylation improved the sustained release ability of amylose-containing starch matrices, and conferred additional resistance to the hydrolytic action of pancreatin under simulated gastrointestinal conditions. However, hydroxypropylation had a detrimental impact on drug release from waxy corn starch matrices.

摘要

糯玉米、Hylon VII 和普通玉米淀粉被低水平和高水平羟丙基化,研究了它们的持续释放性能和基质特性。羟丙基化对 Hylon VII 和普通玉米淀粉基质的影响比对蜡质玉米淀粉基质的影响更强,这表明淀粉片的行为主要由其直链淀粉含量决定。引入羟丙基基团增加了所有淀粉的持水能力,导致含有直链淀粉的淀粉基质更具流动性和柔软性,链迁移性增加。Hylon VII 和普通玉米淀粉经羟丙基化后,片剂的孔隙率和溶胀片剂的储能模量降低。微观分析表明,所有淀粉羟丙基化后,片剂结构更加光滑,孔隙率更低。羟丙基化提高了含有直链淀粉的淀粉基质的持续释放能力,并在模拟胃肠道条件下赋予了对胰蛋白酶水解作用的额外抗性。然而,羟丙基化对蜡质玉米淀粉基质的药物释放有不利影响。

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