阿替洛尔对映体在12名中国健康男性中的药代动力学。

Pharmacokinetics of atenolol enantiomers in 12 Chinese healthy men.

作者信息

Wang X M, Yu X Y, Lin S G

机构信息

Division of Clinical Pharmacology, Guangdong Cardiovascular Institute, China.

出版信息

Zhongguo Yao Li Xue Bao. 1999 Apr;20(4):367-70.

PMID:10452127

Abstract

AIM

To study the pharmacokinetics of atenolol (Ate) stereoisomers in Chinese.

METHOD

A single oral dose of 100 mg of racemic Ate tablets were given to 12 healthy volunteers of Han nationality. Plasma and urine concentrations were determined by the reversed phase HPLC method.

RESULTS

The disposition of d-Ate and l-Ate was conformed to one-compartment model. Maximal plasma concentration (Cmax): l-Ate (331 +/- 79) micrograms.L-1, d-Ate (342 +/- 78) micrograms.L-1. Area under blood concentration-time curve (AUC): d-Ate (2635 +/- 610) micrograms.h.L-1, l-Ate (2442 +/- 588) micrograms.h.L-1. Renal clearance (Clr): l-Ate (6.9 +/- 1.2) L.h-1, d-Ate (6.5 +/- 1.3) L.h-1.

CONCLUSION

The disposition of Ate stereoisomers is of stereoselectivity.

摘要

目的

研究阿替洛尔（Ate）立体异构体在中国人群中的药代动力学。

方法

给予12名汉族健康志愿者单次口服100 mg消旋阿替洛尔片。采用反相高效液相色谱法测定血浆和尿液浓度。

结果

d-Ate和l-Ate的处置符合一室模型。最大血浆浓度（Cmax）：l-Ate为（331±79）μg·L-1，d-Ate为（342±78）μg·L-1。血药浓度-时间曲线下面积（AUC）：d-Ate为（2635±610）μg·h·L-1，l-Ate为（2442±588）μg·h·L-1。肾清除率（Clr）：l-Ate为（6.9±1.2）L·h-1，d-Ate为（6.5±1.3）L·h-1。