酒石酸唑吡坦口溶片的药动学及生物等效性研究

目的:研究酒石酸唑吡坦口溶片的药动学及生物等效性。方法:采用随机自身对照双周期交叉试验设计,18名健康受试者单剂量口服受试制剂7.5mg或参比制剂10mg后,用高效液相色谱-荧光法测定人血浆中的唑吡坦浓度,用非房室模型法估算唑吡坦的药动学参数。结果:受试制剂与参比制剂的主要药动学参数分别为:Cmax(117.62±24.39)、(126.30±35.27)μg·L-1,tmax(0.69±0.16)、(1.25±0.29)h,AUC0～τ(431.16±109.25)、(451.58±114.25)μg·h·L-1,AUC0～∞(450.79±108.03)、(465.34±121.89)μg·h·L-1。受试制剂相对于参比制剂的生物利用度为(97.9±10.7)%。结论:2种国产唑吡坦片剂吸收程度等效而吸收速度不等效。

Bioequivalence and Pharmacokinetics of Zolpidem Tartrate Mouth-dissolving Tablets

OBJECTIVE：To study the pharmacokinetics and bioequivalence of Zolpidem tartrate mouth-dissolving tablets in healthy volunteers.METHODS：In an open randomized controlled crossover design,18 healthy volunteers received single oral dose of either test preparation 7.5 mg or reference preparation 10 mg.The plasma concentration of zolpidem was determined by HPLC-fluorescence detection and pharmacokinetic parameters was calculated using non-compartment model.RESULTS：Main pharmacokinetic parameters of test preparation vs.reference preparation were as follows：Cmax（117.62±24.39）μg·L-1 vs.（126.30±35.27）μg·L-1;tmax（0.69±0.16）h vs.（1.25±0.29） h;AUC0～τ（431.16±109.25）μg·h·L-1 vs.（451.58±114.25）μg·h·L-1;AUC0～∞（450.79±108.03） μg·h·L-1 vs.（465.34±121.89） μg·h·L-1.The relative bioavailability of test preparation was（97.9±10.7）%.CONCLUSION：2 kinds of domestic Zolpidem tablets were bioequivalent in absorption level but not in absorption speed.