盐酸格拉司琼胶囊健康人体药代动力学研究  

Pharmacokinetics of granisetron hydrocloride capsule in healthy volunteers

作　　者：李珍[1] 杨武云[1] 范国荣[2] 闻俊[2] 王法财[1] 唐世新[1] 计一平[1] 

机构地区：[1]第二军医大学长海医院临床药理研究室,上海200433 [2]第二军医大学药学院药物分析学教研室,上海200433

出　　处：《第二军医大学学报》2008年第11期1395-1397,共3页Academic Journal of Second Military Medical University

摘　　要：目的:建立测定人血浆中格拉司琼浓度的LC/MS/MS法,并应用于健康人体药代动力学研究。方法:12例健康受试者单剂量口服2mg盐酸格拉司琼胶囊,LC/MS/MS法测定血浆中格拉司琼浓度,采用非房室模型统计矩法计算药代动力学参数。结果:单剂量口服2mg盐酸格拉司琼胶囊后,主要的药代动力学参数Cmax、tmax、t1/2、MRT、Cl/F、AUC0-24和AUC0-∞分别为(6.93±1.90)ng/ml,(1.35±0.29)h,(5.59±1.87)h,(8.05±1.84)h,(54.23±16.08)L/h,(36.61±8.87)ng·h·ml-1和(39.32±9.36)ng·h·ml-1。结论:本分析方法的准确度、灵敏度、专属性及定量线性范围等均符合生物样品的分析要求,适用于盐酸格拉司琼胶囊的人体药代动力学研究。Objective： To establish a sensitive and specific LC/MS/MS method for the determination of granisetron in human plasma,and to apply it in investigating the pharmacokinetics of granisetron hydrocloride capsule in healthy volunteers. Methods： Twelve healthy male volunteers were given single oral dose of 2 mg granisetron hydrocloride capsules. The plasma concentrations of granisetron were determined by LC/MS/MS method after liquid-liquid extraction. The pharmacokinetic parameters were calculated by noncompartment model. Results： The calibration curve was linear within a concentration range of 0. 501-20.04 ng/ml,with the limit of quantification being 0. 501 ng/ml. The main pharmacokinetic parameters of granisetron in the volunteers were as following： Cmax（6. 93±1. 90） ng/ml,tmax（1. 35±0. 29） h,t1/2 （5.59±1.87） h,MRT （8.05±1.84） h, Cl/F（54.23±16.08） L/h,AUC024 （36.61±8.87） ng · h · ml^-1 and AUC0-∞（39.32±9.36） ng · h· ml^-1. Conclusion： The present method is accurate,sensitive and reproducible for the determination of granisetron levels in human plasma. It is suitable for pharmacokinetic study of granisetron hydrochloride capsule in human.

关 键 词：盐酸格拉司琼 LC/MS/MS法 药代动力学 

分 类 号：R975.4[医药卫生—药品]