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目的综述手性药物经皮吸收与代谢的立体选择性及其影响因素。方法分析评述近年来国内、外相关文献资料。结果皮肤的组成潜在地提供了一个手性环境,手性药物对映体与皮肤手性物质的选择性结合会引起对映体间渗透性的不同。除皮肤手性环境外,其他一些因素如对映体与消旋体熔点的差异、手性促进剂的构象、手性辅料的对映体选择性吸附、前体药物的对映体选择性皮肤代谢等均可能引起对映体选择性皮肤渗透。结论手性药物皮肤吸收与代谢的对映体选择性及其影响因素研究可为其经皮给药制剂的研制及其前体药物的设计提供理论与技术支持。
Objective To summarize the stereoselectivity of percutaneous absorption and metabolism of chiral drugs and its influencing factors. Methods Analysis and comment on domestic and foreign literature in recent years. As a result, the composition of the skin potentially provides a chiral environment in which selective binding of the chiral drug enantiomer to the skin chiral substance causes a difference in the enantiomeric permeability. In addition to the skin’s chiral environment, other factors such as differences in the melting points of enantiomers and racemates, conformations of chiral promoters, enantioselective adsorption of chiral excipients, enantioselective skin of prodrugs Metabolism and so may cause enantioselective skin penetration. Conclusion The enantioselectivity and its influencing factors of skin absorption and metabolism of chiral drugs may provide theoretical and technical support for the preparation of transdermal drug delivery agents and the design of prodrugs.