口服后莫达非尼及其代谢产物在汉族健康人体内的药物动力学

目的研究莫达非尼及其代谢产物(莫达非尼酸)在中国汉族健康人体内的药物动力学过程。方法10名健康志愿者口服莫达非尼片200 mg,采用HPLC法测定给药后不同时间点的莫达非尼及其代谢物的浓度,用DSA软件求算其药物动力学参数,并比较药物动力学参数在性别上的差异。结果莫达非尼及其代谢物莫达非尼酸的药物动力学过程符合二室模型拟合,其药物动力学参数分别为:莫达非尼tmax(1.69±0.70)h,ρmax(4.14±1.21)mg.L-1,AUC0-∞(65.96±11.69)mg.h.L-1;莫达非尼酸tmax(3.06±0.94)h,ρmax(3.19±0.95)mg.L-1,AUC0-∞(45.94±13.44)mg.h.L-1。结论口服莫达非尼在人体内其原形及代谢产物药物动力学均符合二室模型拟合,其药物动力学参数没有性别差异。

Pharmacokinetics of modafinil and its metabolite in Chinese healthy human subjects after a single dose oral administration

Objective To study the pharmacokinetics of modafinil and its metabolite modafinil acid in Chinese human subjects .Methods After oral administration of 200 mg modafinil tablets in 10 volunteers, the blood concentration of modafinil and modafinil acid in all volunteers were determined by HPLC-UV, and the concentration-time profiles were simulated and pharmacokinetic parameters were calculated by using DAS software, which was compared with the difference of gender effects. Results The pharmacokinetics of both modafinil and modafinil acid fitted the biphasic kinetic models. The parameters of modafinil were: tmax（1.69±0.70）h; ρmax（4.14±1.21）mg·L-1；AUC0-∞（65.96±11.69）mg·h·L-1.While those of modafinil acid were tmax (3.06±0.94)h，ρmax (3.19±0.95) mg·L-1 ， AUC0-∞（45.94±13.44）mg·h·L-1. Conclusion Pharmacokinetics of both modafinil and modafinil acid fit biphasic kinetic models. The pharmacokinetic parameters of modafinil and its metabolite are similar comparison and there was no difference between young males and young females.