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理解吸收:监管方面以及应对溶解性和渗透性障碍的当代方法。

Understanding absorption: regulatory aspects and contemporary approaches to tackling solubility and permeability hurdles.

作者信息

B Shekhawat Prachi, B Pokharkar Varsha

机构信息

Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Kothrud, Pune 411038, India.

出版信息

Acta Pharm Sin B. 2017 May;7(3):260-280. doi: 10.1016/j.apsb.2016.09.005. Epub 2016 Nov 2.

Abstract

Oral drug absorption is a process influenced by the physicochemical and biopharmaceutical properties of the drug and its inter-relationship with the gastrointestinal tract. Drug solubility, dissolution and permeability across intestinal barrier are the key parameters controlling absorption. This review provides an overview of the factors that affect drug absorption and the classification of a drug on the basis of solubility and permeability. The biopharmaceutical classification system (BCS) was introduced in early 90׳s and is a regulatory tool used to predict bioavailability problems associated with a new entity, thereby helping in the development of a drug product. Strategies to combat solubility and permeability issues are also discussed.

摘要

口服药物吸收是一个受药物物理化学和生物药剂学性质及其与胃肠道相互关系影响的过程。药物的溶解度、溶出度以及穿过肠道屏障的通透性是控制吸收的关键参数。本综述概述了影响药物吸收的因素以及基于溶解度和通透性的药物分类。生物药剂学分类系统(BCS)于20世纪90年代初引入,是一种用于预测与新药物相关的生物利用度问题的监管工具,从而有助于药物产品的开发。文中还讨论了解决溶解度和通透性问题的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b7a6/5430883/bc35aaf8b4b8/fx1.jpg

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