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介绍手性药物对映体选择性，即对映异构体在生物环境中表现出的药物效应和药代动力学性质的特异性，包括药物效应的种类和强度，药物的吸收、分布、代谢、排泄等方面的立体选择性差异。着重讨论可能影响外消旋药物生物等效性评价的对映体选择性，如对映体优劣度差异较大，对映体的主动吸收和转化、非线性药代动力学特征、剂型差异、给药途径、给药速率、首过代谢和特异性蛋白结合等改变优／劣对映体浓度比值。因此，在对映体选择性差异较大的外消旋仿制或ＯＴＣ药物中，采用手性分析技术，开展对映体水平的生物等效性评价是必要的，也具有重要意义。
The enantioselectivity of chiral drugs is introduced, ie, the specificity of the pharmacodynamic and pharmacokinetic properties of the enantiomers in the biological environment, including the type and intensity of the drug effect, the absorption, distribution, and metabolism of the drug , Excretion and other aspects of the three-dimensional selective differences. The emphasis is placed on the enantioselectivities that may influence the bioequivalence assessment of racemic drugs, such as large differences in enantioselectivity, enantioselective uptake and conversion, non-linear pharmacokinetic profiles, dosage forms differences , Route of administration, rate of administration, first-pass metabolism, and specific protein binding, etc. to optimize the concentration ratio of superior / poor enantiomer. Therefore, it is necessary and significant to conduct enantiomeric bioequivalence assessment using chiral analytic techniques in racemic or OTC drugs with large enantioselectivity differences.