盐酸阿呋唑嗪片剂的人体生物等效性研究

Bioavailability of Alfzosin Hydrochloride Tablets in Healthy Subjects

１２名健康志愿者采用交叉给药方法，分别单剂量口服５ｍｇ国产盐酸阿呋唑嗪片及进口盐酸阿呋唑嗪片，进行两种制剂的生物等效性研究。采用ＨＰＬＣ荧光检测法测定血浆中阿味唑嗪的浓度，血药浓度－时间数据经３ｐ９７生物利用度计算程序处理拟合，符合血管外给药二室开放模型，试验结果表明：单次口服５ｍｇ国产盐酸阿呋唑嗪片和进口盐酸阿呋唑嗪片后，达峰时间分别为１４６ ± ０．５４ｈ和１．４２ ±０．２９ ｈ，峰浓度分别为 ３９．７９ ± ５，２９ μ ｇ· Ｌ^（－１）和 ４０．０５ ± ５．８８ μ ｇ· Ｌ^（－１），０－ ２４ｈ的药时曲线下面积分别为２２５．４０ ± ２６．６６μｇ·ｈ· Ｌ^（－１）和２３５．０４±２４．１３ μ ｇ·ｈ· Ｌ^（－１）、其主要药代动力学参数经方差分析和双单侧ｔ检验，无显著性差异（Ｐ＞０．０５），两种制剂具有生物等效性。国产盐酸阿呋唑嗪片的相对生物利用度为９６．９０／±１５．８％。

The relative bioavailability and pharmacokinetics of domestic alfuzosin tablets were studied in 12 healthy male volunteers.A dose of sing of domestic or imported alfuzosin hydrochloride was given according to a randomized 2 cross-over design,blood samples were withdrawn up to 24 hours post administration,and plasma concentration of alfuzosin was determined by high performance liquid chromatography (HPLC) flavoxate.The concentration-time curves of two preparations were fitted to a two-compartment model.The peak plasma levels(C_(max))of alfuzosin hydrochloride domestic drug and imported drug were 39.79 ± 5.29 and 40.05 ± 5.88 p g·L^(-1) respectively,the peak time (T_(max))were 1.46 ± 0.54h and 1.42 ± 0.29h respectively,and AUC(O-24) were 225.40 ± 26.66 and 235.04 ± 24. 13 μg· h·L^(-1)respectively.The pharmacokinetics and relative bioavailability data obtained in the study furnished definite proof of bioequivalence of both domestic and imported alfuzosin hydrochloride tablets.