国产氨氯吡咪片的相对生物利用度及其生物等效性评价

Relative Bioavailability and Bioequivalence Assessment of Domestic Amiloride Tablet

６名健康志愿者随机交叉ｐｏ单剂量１０ｍｇ氨氯吡咪国产或进口片。利用ＨＰＬＣ测得血浆中药物浓度分别在３．１２±０．５０和３．０７±０．７１ｈ达到峰值２５．４±５．３和２１．８±８．９ｎｇ／ｍｌ。血药浓度－时间曲线下面积分别为２５３±６６和２２６±５６ｎｇ·ｈ／ｍｌ。药－时曲线符合一级吸收的单室模型，国产氨氯吡咪片的相对生物利用度Ｆ为１．１４±０．３４，经统计分析两种制剂具有生物等效性。

The pharmacokinetics of amiloride was determined following a single oral dose of 10 mg given to each 6 volunteers in an open randomized crossover study. Drug concentration in plasma was assayed by HPLC methed. The peak levels in plasma averaged 25.4±5.3 and 21.8±8.9 ng/ml at 3.12±0.50,3.07±0.71 h,and the areas under the drug concentration cruves were 253±66 and 226±56ng·h/ml for domestic and imported tablet respectively. The concentration-time courses after medication conformed to a l-compartment open model with a first order absorption. The results of three factors analysis of variance showed that the two formulations were bioequivalent.