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羟丙甲纤维素在口服药物递送中的应用。

The use of hypromellose in oral drug delivery.

作者信息

Li Chi L, Martini Luigi G, Ford James L, Roberts Matthew

机构信息

GlaxoSmithKline Pharmaceuticals, Pharmaceutical Development, New Frontiers Science Park South, Third Avenue, Harlow, Essex, CM19 5AW, UK.

出版信息

J Pharm Pharmacol. 2005 May;57(5):533-46. doi: 10.1211/0022357055957.

Abstract

Hypromellose, formerly known as hydroxypropylmethylcellulose (HPMC), is by far the most commonly employed cellulose ether used in the fabrication of hydrophilic matrices. Hypromellose provides the release of a drug in a controlled manner, effectively increasing the duration of release of a drug to prolong its therapeutic effect. This review provides a current insight into hypromellose and its applicability to hydrophilic matrices in order to highlight the basic parameters that affect its performance. Topics covered include the chemical, thermal and mechanical properties of hypromellose, hydration of the polymer matrices, the mechanism of drug release and the influence of tablet geometry on drug-release rate. The inclusion of drug-release modifiers within hypromellose matrices, the effects of dissolution media and the influence of both the external environment and microenvironment pH within the gel matrix on the properties of the polymer are also discussed.

摘要

羟丙甲纤维素,以前称为羟丙基甲基纤维素(HPMC),是目前在制备亲水性基质中最常用的纤维素醚。羟丙甲纤维素以可控方式实现药物释放,有效延长药物释放持续时间以增强其治疗效果。本综述提供了对羟丙甲纤维素及其在亲水性基质中的适用性的当前见解,以突出影响其性能的基本参数。涵盖的主题包括羟丙甲纤维素的化学、热和机械性能、聚合物基质的水化、药物释放机制以及片剂几何形状对药物释放速率的影响。还讨论了在羟丙甲纤维素基质中加入药物释放调节剂、溶出介质的影响以及凝胶基质内外部环境和微环境pH对聚合物性能的影响。

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