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在临床使用的化学合成药物中,约40%左右为手性药物,而其中绝大部分是以消旋体应用~([1])。近年来,随着高效液相色谱法及毛细管电泳等分析技术的发展和应用,消旋药物在药代及药效学上具有的立体选择性,这一观点逐渐为人们所认同,人们意识到只研究消旋体的药动学和生物利用度是有一定缺陷的,单一异构体的药动学研究越来越多引起重视。本文对手性药物对映体药代动力学立体选择性的过程和机理及相关影响因素作一综述。
About 40% of the chiral drugs used in clinical chemistry are chiral drugs, and most of them are used as racemates (1). In recent years, along with the development and application of analytical techniques such as high performance liquid chromatography and capillary electrophoresis, the stereoselectivity of racemic drugs in pharmacokinetics and pharmacodynamics has gradually become accepted by people and people are aware Only to study the racemate pharmacokinetics and bioavailability is a certain defect, single isomer of pharmacokinetic studies more and more attention. This review summarizes the process and mechanism of the stereoselectivity of the chiral drug enantiomer and its related influencing factors.