目的 用液相色谱串联质谱法测定健康男性受试者单次空腹口服受试及参比盐酸特拉唑嗪片后的血药浓度,计算受试制剂和参比制剂的药动学参数,评价两种制剂是否生物等效。方法 采用随机、开放、双周期自身交叉试验设计,18例健康男性受试者随机分成2组,单剂量口服盐酸特拉唑嗪片受试制剂和参比制剂2 mg,用LC-MS/MS测定血浆中特拉唑嗪的浓度。药动学参数用DAS 2.0软件处理获得。结果 受试制剂和参比制剂t_max中位数(最小值,最大值)分别为1.00 (0.25, 2.00)h和0.75 (0.50, 4.00)h,ρ_max(平均值±SD)分别为(49.72±9.86)和(61.66±18.37)ng·mL^-1,AUC_0-t(平均值±SD)分别为(516.35±107.33)和(616.58±118.48)ng·h·mL^-1,AUC_0-∞(平均值±SD)分别为(532.62±112.42)和(634.99±122.49)ng·h·mL^-1,相对于参比制剂,受试制剂的相对生物利用度为(100.17±13.92)%。AUC_0-t、ρ_max 90%置信区间分别为93.8%~105.1%和88.3%~108.4%。试验期间未发生严重不良事件。结论 盐酸特拉唑嗪片受试制剂和参比制剂人体内具有生物等效性。

OBJECTIVE To evaluate the bioequivalence of test and reference preparation of terazosin hydrochloride tablets in healthy malevolunteers. METHODS This is openrandom and two-way crossover clinical trial involved 18 healthy male subjects. The volunteers were randomly divided into two groups. They were given single oral dose of test and reference preparation of terazosin hydrochloride tablets (each 2 mg). The plasma concentrations of terazosin were determined by LC-MS/MS. Pharmacokinetic parameters were obtained using DAS2.0 program. RESULTS The main pharmacokinetic parameters of terazosin hydrochloride tablets test and reference preparation were as follows:t_max were 1.00 (0.25, 2.00) h and 0.75 (0.50, 4.00)h, ρ_max were and (49.72±9.86) and (61.66±18.37) ng·mL^-1, AUC_0-t were (516.35±107.33) and (616.58±118.48) ng·h·mL^-1, AUC_0-∞ were (532.62±112.42) and (634.99±122.49) ng·h·mL^-1 respectively. The relative bioavailability was (100.17±13.92)%. And 90% confidence limit of test preparation of the logarithmic transformed parameters AUC_0-t and ρ_max were in 93.8%-105.1% and 88.3%-108.4% compared with reference preparation, respectively. No serious adverse events were observed during the trials. CONCLUSION Two kinds of terazosin hydrochloride tablets are bioequivalent.