卡维地洛在健康人体的生物等效性

Bioequivalence of carvedilol in healthy volunteers

目的研究中国健康志愿者单次口服卡维地洛片(抗高血压药)的药代动力学。方法20名健康志愿者随机分成2组,分别单次口服试验与参比卡维地洛20 mg。用LC-MS法测定给药后不同时间点血浆中的卡维地洛浓度,并用DAS Ver 2.0软件计算其药代动力学参数。结果卡维地洛试验与参比制剂主要药代动力学参数如下:tm ax分别为(0.69±0.24)和(0.76±0.39)h,t1/2分别为(7.21±5.10)和(7.99±4.70)h,Cm ax分别为(63.70±21.45)和(60.02±22.34)μg.L-1,AUC0-t分别为(161.98±62.24)和(168.15±64.09)μg.h.L-1,AUC0-∞分别为(173.30±78.42)和(179.49±72.84)μg.h.L-1;卡维地洛的相对生物利用度为(99.3±25.9)%。结论2种制剂具有生物等效性。

Objective To study the pharmacokinetics of a single dose carvedilol tablets in Chinese healthy volunteers. Methods Twenty healthy volunteers were divided into 2 groups. Twenty mg single oral dose of carvedilol tablets was given to 20 healty volunteers. The concentrations of plasma samples collected from the volunteers respectively were determined by LC-MS. The pharmacokinetic parameters were calaulated by DAS Ver 2. 0 software. Results The main pharmacokinetic parameters of carvedilol test and reference tablets were as follow ： tmax were （ 0. 69 ±0. 24）and（0. 76 ±0.39） h,t1/2were （7.21 ±5.10）and（7.99 ±4.70） h,Cmax were （ 63.70 ± 21.45 ） and （ 60. 02 ± 22.34 ） μg .L^-1 , AUC0-t were （161.98±62.24）and（168.15 ±64.09） μg.h.L^-1, AUC0-∞ were （ 173.30 ±78.42） and （ 179.49 ± 72.84 ） μg.h. L^-1. The relative bioavailability of drug was （99. 3 ± 25.9） %. Conclusion The two carvedilol tablets are bioequivalent.