洛哌丁胺胶囊在健康中国志愿者体内的药动学研究

Study on the Pharmacokinetics of Loperamide Capsule in Healthy Chinese Volunteers

目的:建立人血浆中洛哌丁胺的HPLC-MS/MS测定方法,研究洛哌丁胺在健康中国人体内的药动学特征。方法:10名健康受试者口服易蒙停(洛哌丁胺胶囊)4mg后,采用HPLC-MS/MS测定其血浆药物浓度,并计算主要药动学参数。结果:洛哌丁胺在10.50～3150pg.mL-1内线性关系良好,最低定量限为10.50pg.mL-1。洛哌丁胺血药达峰浓度为(927±354)pg.mL-1,达峰时间为(3.0±1.2)h,AUC0～72h为(15487±4242)pg.h.mL-1,消除半衰期为(19.1±4.9)h。结论:洛哌丁胺在中国人体内的药动学参数与文献报道的其在德国人体内的药动学参数基本一致,但与其在韩国人体内的药动学参数有明显的差异。

Objective：To establish an LC-MS/MS method for the determination of loperamide in human plasma and investigate the pharmacokinetics of loperamide capsule in healthy Chinese volunteers.Methods：A single oral dose of 4mg loperamide capsule was given to 10 health Chinese volunteers.The loperamide concentrations in plasma were determined by HPLC-MS/MS method.The pharmacokinetic parameters of loperamide in the volunteers were evaluated.Results：The calibration curve of loperamide in human plasma was linear over the concentration rang of 10.50～3150 pg·mL^-1.The lower limit of quantitation was 10.50 pg·mL^-1.The pharmacokinetic parameters Cmax,tmax,AUC0～72h and t1/2 of loperamide were（927±354） pg·mL^-1,（3.0 ±1.2）h,（15487 ±4242）pg·h·mL^-1 and（19.1 ±4.9）h,respectively.Conclusion：The pharmacokinetic parameters of loperamide in healthy Chinese volunteers are consistent with those in Germanys reported in literatures,but are apparently different from those in Koreans reported in literatures.