提高难透膜水溶性药物口服生物利用度的方法研究进展

Approaches for improving oral bioavailability of soluble and poorly permeable drugs: research advances

难透膜水溶性药物多为基因工程药物或传统中药中水溶性活性成分,近年来该类药物发展迅速,但由于口服生物利用度低,在临床上往往需要注射给药,开发此类药物的口服制剂是近年来药剂学领域关注的热点和难点问题之一。本文综述了改善此类药物口服吸收的方法,包括利用化学修饰、载体主动转运吸收、吸收促进剂、微粒给药系统、生物黏附给药系统和酶抑制剂等方法。部分药物通过此类方法已经成功进入临床试验,个别药物已经上市。

Most soluble and poorly permeable drugs are genetically engineered drugs or soluble ingredients of Traditional Chinese Materia Medica.In recent years,this kind of drugs have enjoyed fast development,but they generally must be used as injections due to their poor oral bioavailability,thus it is very difficult to develop oral dosages of these drugs in pharmaceutical fields.This article provides a brief review of the approaches for improving oral bioavailability of this kind of drugs,including chemical modification,absorption via active transport carriers,absorption enhancers,particle carrier delivery system,mucoadhesive system,and enzyme inhibitors.Using the approaches mentioned above,some drugs have entered clinical trial successfully and a few drugs have been into the market.