左乙拉西坦片在健康人体的药代动力学

目的研究中国健康志愿者口服不同剂量左乙拉西坦片(抗癫痫药)的药代动力学。方法 24名中国健康志愿者随机分为低,中,高3个剂量组,单次口服左乙拉西坦片(500,l000,1500 mg)。用高效液相色谱法测定血药浓度,用DAS 2.1.1软件计算药代动力学参数。结果左乙拉西坦片低,中,高剂量组的主要药代动力学参数分别如下:Cmax为(14.42±3.51),(26.73±6.22),(38.44±8.75)μg.L-1;Tmax为(1.31±0.58),(1.44±0.61),(1.19±0.51)h;t1/2为(6.19±1.18),(5.75±1.22),(5.87±1.55)h;AUC0-t为(130.43±23.43),(220.63±42.82),(316.93±76.58)μg.h.L-1。结论血浆中左乙拉西坦的Cmax和AUC显示线性药代动力学特征。受试者服用左乙拉西坦片500,l000,1500 mg后,药代动力学参数经单因素方差分析显示无性别差异。

Pharmacokinetics of levetiracetam tablets in healthy volunteers

Objective To investigate the pharmacokinetics of levetiracetam tablets in healthy volunteers.MethodsTwenty-four healthy volunteers were randomly divided into three groups receiving oral a single dose of 500,l000 and 1500 mg levetiracetam tablets respectively.The plasma concentration was determined by HPLC-UV method.ResultsThe main pharmacokinetics parameters of three different dosages(500,1000,1500 mg) were as follows:Cmax were(14.42±3.51),(26.73±6.22),(38.44±8.75) μg·L-1;Tmax were(1.31± 0.58),(1.44±0.61),(1.19±0.51) h;t1/2 were(6.19±1.18),(5.75±1.22),(5.87±1.55) h;AUC0-t were(130.43±23.43),(220.63±42.82),(316.92±76.58) μg·h·L-1.ConclusionThe pharmacokinetic characteristic of levetiracetam in Chinese healthy volunteers was fitted with linear kinetic model.It is showed that the sex-related differences did not exist in the main pharmacokinetic parameters between males and females by analysis of variance.