人体卡托普利的药代动力学及其生物利用度

Pharmacokinetics and Bioavailability of Captopril in Healthy Volunteers

目的：比较Ａ、Ｂ两厂复方卡托普利片的生物利用度和药代动力学。方法：９名健康志愿者随机交叉口服单剂量３０ｍｇ复方卡托普利片，以对溴苯乙酰基溴（ＰＢＰＢ）为衍生化试剂，采用反相高效液相色谱法。结果：测得Ａ、Ｂ药厂生产的复方卡托普利片剂在血浆中Ｃａｐ浓度达峰时间分别为（０．９４±０．１３）ｈ和（１．００±０．１５）ｈ；达峰浓度Ｃｍａｘ分别为（９２．０３±２７．３６）ｎｇ／ｍｌ、（７４．６７±１９．２９）ｎｇ／ｍｌ；药时曲线下面积（ＡＵＣ）分别为（２５２．７８±６８．１４）ｎｇ／（ｈ·Ｌ）、（２５１．１９±５０．１３）ｎｇ／（ｈ·Ｌ）。血药浓度—时间曲线符合二房室模型。结论：以Ａ厂复方卡托普利片为标准算得Ｂ厂复方卡托普利片中卡托普利的相对生物利用度（Ｆ）为９９．３７％。

OBJECTIVES:To compare the bioavailability and pharmacokinetics of captopril between products of two factories.METHODS:An open randomized crossover study was carried out in 9 healthy volunteers who received a single oral dose of 30mg captopril,taking β bromophenacyl bromide as ramification.Drug concentrations in plasma were assayed by HPLC method.RESULTS:The concentration time course after medication conformed to a 2 compartment open model with a first order absorption.The pharmacokinetic parameters of Captopril of A and B medicine factories were:Tmax(0.94±0.13)h,(1.00±0.15)h,Cmax(92.03±27.36)ng/ml,(74.67±19.29)ng/ml,AUC(252.78±68.14)ng/(h·L),(251.19±50.13)ng/(h·L)respectively.CONCLUSIONS:The results showed that the bioavailability for the testing tablet was 99.37%,the two formulations were bioequivalent.