| 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2 mg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2 mg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。 |
| 关键词: 盐酸格拉司琼 LC/MS/MS法 药代动力学 |
| DOI：10.3724/SP.J.1008.2008.01395 |
| 投稿时间：2007-07-24修订日期：2008-09-29 |
| 基金项目: |
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| Pharmacokinetics of granisetron hydrocloride capsule in healthy volunteers |
| LI Zhen1*,YANG Wu-yun1,FAN Guo-rong2,WEN Jun2 ,WANG Fa-cai1,TANG Shi-xin1,JI Yi-ping1 |
| (1.Department of Clinical Pharmacology,Changhai Hospital,Second Military Medical University,Shanghai 200433,China;2.Department of Drug Analysis,School of Pharmacy,Second Military Medical University,Shanghai 200433) |
| Abstract: |
| 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,AUC0-24 (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. |
| Key words: granisetron hydrocloride LC/MS/MS pharmacokinetics |
