国产奈韦拉平片健康人体相对生物利用度研究

 目的研究国产奈韦拉平片健康人体相对生物利用度。方法采用双周期自身交叉对照试验设计,20名健康志愿者po国产和进口奈韦拉平片各200 mg后采用高效液相色谱法测定血浆药物浓度。用3P97药动学软件进行药动学参数计算及生物等效性评价。结果两种奈韦拉平片的药-时曲线均符合一房室模型,参比制剂、受试制剂的主要药动学参数如下：t_max分别为(3.50±1.05)和(4.20±1.24)h；ρ_max分别为(2394±392)和(2170±434)μg·L^-1。,t_1/2ka分别为(0.85±1.00)和(0.79±0.51)h,t_1/2ke分别为(52.30±13.82)和(55.59±10.51)h；AUC_0～t分别为(149.20±30.54)和(154.05±27.77)mg·h·L^-1,AUC_0-∞分别为(168.30±40.22)和(173.30±36.65)mg·h·L^-1。与标准参比制剂相比,受试制剂的相对生物利用度F_0-t为(104.97±16.51)%,F_0-∞为(105.21±18.93)%。对两制剂间的AUC_0～t,AUC_0～∞和ρ_max进行双向单侧t检验,表明两种制剂具有生物等效性。结论国产和进口奈韦拉平片具有生物等效性。

Pharmacokinetics and Relative Bioavailability Study of Nevirapine in Healthy Volunteers

OBJECTIVE To evaluate relative bioavailability of domestic nevirapine in healthy volunteers.METHODS A single oral dose of 200 mg nevirapine domestic and imported tablets,was given to 20 health volunteers in a randomized cross-over study.The nevirapine concentrations in plasma were determined by HPLC method.RESULTS The concentrations of two formulations were fitted to an one-com- partment open model.The main pharmacokinetic parameters of two nevirapine tablets were as follows:t_max(3.50±1.05)and(4.20±1.24) h;ρ_max were(2 394±392)and(2170±434)μg·L^-1;t_1/2ka(0.85±1.00)and(0.79±0.51)h;t_1/2ke(52.30±13.82)and(55.59±10.51)h;AUC_0～t(149.20±30.54)and(154.05±27.77)mg·h·L^-1;AUC_0～∞(168.30±40.22)and(173.30±36.65)mg·h·L^-1, respectiely.The relative bioavalability of F_0～t and F_0～∞(104.97±16.51)% and(105.21±18.93)%,respectively.CONCLUSION The ANOVA and two one-sided t test statistical analysis show that two formulations are bioequivalent.