注射用盐酸帕洛诺司琼健康人体药动学研究  

Pharmacokinetic properties of palonosetron,a 5-hydroxytryptamine-3 receptor antagonist,in Chinese healthy subjects

作　　者：戴媛媛[1] 刘鹏[2] 陈喆[1] 汤致强[1] 冯凤仪[2] 

机构地区：[1]中国医学科学院肿瘤医院临床药理室,北京100021 [2]中国医学科学院肿瘤医院内科,北京100021

出　　处：《中国新药杂志》2009年第10期910-913,共4页Chinese Journal of New Drugs

摘　　要：目的:研究注射用盐酸帕洛诺司琼在健康受试者体内的药动学特征。方法:健康受试者静脉给与帕洛诺司琼,采集血样利用HPLC/MS测定药物浓度,进行数据分析计算药动学参数。结果:健康受试者静脉给与帕洛诺司琼0.25mg后,C0为(1.54±0.46)ng·mL-1,t1/2为(41.90±11.90)h,AUC0～t为(11.39±4.54)h.ng·mL-1,AUC0→∞为(14.44±5.45)h·ng·mL-1,Vd为(18.75±4.28)L·kg-1,CL为(5.68±2.56)mL·min·kg-1。结论:帕洛诺司琼体内分布广,清除较慢,体内半衰期长。健康受试者静脉注射帕洛诺司琼个体间存在着差异,性别间无差异。Objective： To determine the pharmacokinetic properties of intravenous （Ⅳ） palonosetron hydrochloride in healthy Chinese subjects. Methods： Twelve subjects were administered with a single IV dose of 0.25 mg palonosetron. Serial blood samples were obtained and the plasma concentration was determined by HPLC- MS to evaluate the pharmacokinetic properties of palonosetron. Results： After IV palonosetron, the values of AUC and Co were （14.44 ±5.45） h·ng·mL^-1 and （ 1.54 ± 0.46） ng·mL^-1 , respectively. Elimination half-life, body clearance, and apparent volume of distribution were （41.90 ± 11.90） h, （5.68 ± 2.56） mL. min·kg^-1 and （ 18.75 ± 4.28） L. kg^-1, respectively. Conclusion ： In healthy subjects, palonosetron is eliminated slowly from the body, with a long plasma elimination half-life time and a large volume of distribution; while the inter-subject variability is large.

关 键 词：盐酸帕洛诺司琼 药动学 HPLC/MS 

分 类 号：R969.1[医药卫生—药理学] R975.4[医药卫生—药学]