奈韦拉平2种片剂的人体生物等效性比较

Comparative bioequivalence of domestic and imported nevirapine tablets in human

目的:评价奈韦拉平国产片与进口片之间的人体生物等效性。方法:20名健康男性受试者,随机分为2组,分别于早晨空腹一次口服国产片或进口片200mg。1wk后再交叉服药。用HPLC法,以水∶甲醇=55∶45为流动相,蛋白沉淀后直接测定奈韦拉平血药浓度。结果:奈韦拉平国产片与进口片的主要药动学参数:tmax为(3.95±s0.22)h和(4.0±0.5)h,cmax为(13.8±1.9)mg·L-1和(14.0±2.1)mg·L-1,t1/2为(46±7)h和(42±8)h,AUC0～168为(765±198)mg·h·L-1和(779±132)mg·h·L-1,AUC0～∞为(839±230)mg·h·L-1和(840±150)mg·h·L-1。奈韦拉平国产片平均相对生物利用度为(97±14)%。结论:奈韦拉平国产片与进口片具有生物等效性。

AIM:To evaluate the bioequivalence of nevirapine between domestic and im ported tablets in human. METHODS:The study was performed with 20 healthy male volunteers according to a randomized 2-way crossover design. The plasma samples were collected at 1,2,3 ,4,6,8,12,24,48,72,120,168 h after taking 200 mg of domestic or importe d nevirapine tablet. The plasma-drug concentrations were determined by HPLC ass ay. RESULTS:The plasma concentration-time curves of domestic and imported nevirapi ne tablets showed as taking a nearly identical course. The main pharmacokinetic parameters o f domestic and imported nevirapine tablets were as follows:(3.95±(s 0.22 ) h) and((4.0±)0.5) h for t_(max),(13.8±(1.9) mg·)L^(-1) and ( (14.0±)2.1) mg·L^(-1) for c_(max),(46±7) h and (42±8) h for t_(1/2) ,(765±198) mg·h·L^(-1) and (779±132) mg·h·L^(-1) for AUC_( 0-168),(839±230) mg·h·L^(-1) and (840±150) mg·h·L^(-1) for AUC_(0-∞),respectively. The relative bioavailability of nevirapine was (97±14) %. CONCLUSION:The method is simple, reproducible and feasible to the pharmacokin etic studies of nevirapine showing bioequivalence of domestic and imported nevir apine tablet.