盐酸特拉唑嗪在健康人体内的药物动力学

Pharmacokinetics of terazosin in healthy volunteers

目的：在８名健康志愿者体内研究了国产盐酸特拉唑嗪胶囊和进口片剂的药物动力学和生物利用度。方法：受试者交叉口服单剂量（２ｍｇ）盐酸特拉唑嗪胶囊和片剂后，采用高效液相色谱法和荧光检测器测定血药浓度。结果：胶囊和片剂的药时曲线均符合二室模型，其Ｔｍａｘ分别为１．３±０．６ｈ和１．３±０．４ｈ，Ｃｍａｘ分别为４９．５±８．６ｎｇ·ｍｌ－１和５０．３±５．２ｎｇ·ｍｌ－１，ＡＵＣ０→∞分别为５３６．５±３９．８ｎｇ·ｍｌ－１和５８６．６±５２．８ｎｇ·ｍｌ－１·ｈ，测试药品的相对生物利用度为９２．３０％±１２．９１％。结论：经方差分析两药药物动力学参数间差异均无显著性（Ｐ＞０．０５）；结果表明两药具有生物等效性。

OBJECTIVE :The pharmacokinetics and bioavailability of terazosin was studied in 8 healthy male volunteers. METHODS :After a single oral dose of 2mg terazosin capsule and tablet was given to 8 volunteers in a randomized cross over study, the terazosin concentration in serum was determined by high performance liquid chromatography with fluorescence detection. RESULTS :The concentrationtime curves of terazosin capsules and tablets were fitted to a twocompartment model.Tmax of capsules and tablets were 1.30.6h and 1.30.4h,Cmax 49.58.6ngml-1 and 50.35.2ngml-1,AUC0 536.539.8ngml-1h and 586.652.8ngml-1h,respectively.The relative bioavailability of the tablets was 92.30%12.91%. CONCLUSIONS :There was no significant difference in each pharmacokinetics parameters between the two preparations. The results suggested that the two preparations were bioequivalent.