国产盐酸特拉唑嗪片在人体内的药动学研究及生物等效性评价

Pharmacokinetics and Bioavailability of Domestic Terazosin in Healthy Volunteers

目的对两种盐酸特拉唑嗪片在健康青年志愿者体内的药代动力学和相对生物利用度进行研究,并评价其生物等效性。方法单剂量口服盐酸特拉唑嗪片剂2 mg后,用HPLC法测定血药浓度,所得数据用BECS软件计算药动力学参数并进行等效性评价。结果两种盐酸特拉唑嗪片剂的药动学参数分别为:T1/213.39±1.89和13.00±2.32 h,Tmax 1.33±0.30和1.36±0.29 h,Cmax27.83±5.34μg.L-1,和28.62±5.35μg.L-1,AUC0→t342.31±61.18和334.93±73.08μg.h.L。两种特拉唑嗪片剂的相对生物利用度F1(AUC0→t)=96.92%±0.21,F2(AUC0→∞)=96.41%±0.21。结论经统计学分析,两种特拉唑嗪片剂的药动学参数之间差异均无显著性(P>0.05),两种制剂生物等效。

Objective To study the pharmacokinetics and bioavailability of two brand domestic Terazosin tablets.Methods The blood level of two brand Terazosin tablets were determined by RP - HPLC after administering single-dose oral adm 2mg. The BECS program was used for the calculation of pharmacokinetic and bioavailability parameters. Results The pharmacokinetic parameters of two brand Terazosin tablets were ： Ke 0.053 ± 0.008 and 0.055 ± 0.011 h^-1 ,T1/2 13.39 ± 1.89 and 13.00 ± 2.32 h,Tmax 1.33± 0.30 and 1.36 ± 0.29 h, Cmax 27.83 ± 5.34 and 28.62 ± 5.35 μg/L, AUC0→t 342.31 ± 61.18 and 334.93 ± 73.08 μg.h.L.F1（AUC0→t） =96.92% ±0.21,F2（AUC0→∞） =96.41% ± 0.21.Conclusion There is no signifi- cant difference between the two products. The results demonstrate that the two preparations are bioequivalent.