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目的：研究美托洛尔光学异构体在离体大鼠肝灌流上的药物动力学的立体选择性差异．方法：美托洛尔光学异构体在离体大鼠肝灌流中作循环式灌流，用高效液相色谱法进行定量分析．结果：０１６，０３２和０６４ｍｇ三种不同剂量的美托洛尔光学异构体在离体大鼠肝脏中消除过程，经叠加原则认为不存在饱和机制，符合单室模型一级动力学过程，在三种剂量下，两种异构体间的动力学参数Ｔ１／２，Ｋ和Ｃｌ均存在着显著性差异（Ｐ＜００１），其Ｓ（－）Ｍｅｔ／Ｒ（＋）Ｍｅｔ的Ｃｌ比值为０１４－０１７．结论：离体大鼠肝脏对美托洛尔两种光学异构体的代谢具有立体选择性，其肝消除符合线性动力学过程．
OBJECTIVE: To study the stereospecificity of the pharmacokinetics of metoprolol optical isomers on rat hepatic perfusion. METHODS: Metoprolol optical isomers were perfused circularly in isolated rat liver perfusion and quantified by high performance liquid chromatography. Results: Metoprolol optical isomers at three different dosages of 016, 032 and 064 mg were eliminated in isolated rat liver. According to the superposition principle, there was no saturation mechanism, which accorded with single-compartment model one At the three doses, there are significant differences in the kinetic parameters T1 / 2, K and Cl between the two isomers (P <001) and the S (-) Met / R (+) Met Cl ratio of 0 14-0 17. CONCLUSION: The isolated rat liver has stereoselectivity for the metabolism of the two optical isomers of metoprolol, and its liver elimination conforms to the linear kinetic process.