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目的:研究阿替洛尔对映体在中国人体内的药物动力学,方法:12名男性汉族健康志愿者单剂量口服阿替洛尔片剂100 mg后,用高效液相-荧光法测定血浆和尿液药物浓度。结果:血药浓度-时间曲线拟合表明阿替洛尔对映体的体内过程符合口服一室开放模型,l-Ate和d-Ate的主要药代动力学参数:C_(max) (331±79)and(342±78)μg·L~(-1);AUC(2442±588)and(2635±610)μg·h·L~(-1);Cl_r:(6.9±1.2)and(6.5±1.3)L·h~(-1)。结论:阿替洛尔对映体的药代动力学过程具有明显的立体选择性差异。
AIM: To study the pharmacokinetics of atenolol enantiomers in Chinese human.Methods: A total of 12 male Han volunteers were given 100 mg oral administration of atenolol tablets, and the plasma levels of plasma And urine drug concentration. Results: The plasma concentration-time curve fitting showed that the in vivo process of the atenolol enantiomer was consistent with the oral, open-chamber model with the main pharmacokinetic parameters of l-Ate and d-Ate: C max (331 ± 79 and 342 ± 78 μg · L -1; AUC (2442 ± 588) and (2635 ± 610) μg · h · L -1; ± 1.3) L · h ~ (-1). Conclusion: The pharmacokinetics of atenolol enantiomers have obvious stereoselective differences.