两种盐酸特拉唑嗪片的人体生物等效性研究

Bioequivalence study on two terazosin hydrochloride tablets

目的：评价单剂量口服国产和进口盐酸特拉唑嗪片的人体生物等效性。方法采用单中心、随机、开放、双周期交叉试验设计，21名受试者在不同周期分别空腹口服国产和进口盐酸特拉唑嗪片2mg，于给药前0h及给药后60h内不同时间点采集静脉血4 ml ，采用液-质联用（LC-MS／MS）法测定受试者血浆中特拉唑嗪的浓度。结果国产和进口盐酸特拉唑嗪片的 t1／2分别为（13.2±2.39）和（12.5±1.93） h；tmax分别为（1.01±0.83）和（1.08±0.69） h；Cmax分别为（40.1±10.6）和（37.3±9.57） ng／ml；AUC0-∞分别为（428±82.1）和（426±85.2） ng · h／ml。国产盐酸特拉唑嗪片的相对生物利用度为（101.2±14.7）％。国产与进口盐酸特拉唑嗪片 AUC0-t和Cmax几何均值比的90％置信区间（CI）均落在80％～125％之间。结论国产和进口盐酸特拉唑嗪片具有生物等效性。

Objective To evaluate the bioequivalence of domestic and imported terazosin hydrochloride tablets after single oral dose .Methods It was a single center ,randomized ,open ,cross-over trail design ,21 subjects were fasting oral adminis-tered of 2 mg domestic and imported terazosin hydrochloride tablets in different periods ,venous blood 4 ml were collected in different time points before and 60 h after administration ,plasma concentration of terazosin was determined by LC-MS/MS . Results The main pharmacokinetic parameters of domestic and imported terazosin hydrochloride tablets were as follows ：t1/2 ：（13.2± 2.39）hvs（12.5±1.93）h,tmax ：（1.01±0.83）hvs（1.08±0.69）h,Cmax ：（40.1±10.6）ng/mlvs（37.3± 9 .57） ng/ml;AUC0- ∞ ：（428 ± 82 .1） ng · h/ml vs （426 ± 85 .2） ng · h/ml .The relative bioavailability of domestic terazosin hydrochloride tablets was （101 .2 ± 14 .7）% .90% CI of domestic and imported terazosin hydrochloride tablets AUC0-t and Cmax geometric mean ratio fell between 80% -125% .Conclusion The domestic tablets are bioequivalent to the imported tablets .