盐酸帕洛诺司琼在健康人体的药动学研究

Study on pharmacokinetics of palonosetron hydrochloride in healthy volunteers

目的:研究盐酸帕洛诺司琼注射液在健康志愿者体内的药动学。方法:24名健康志愿者按随机数字表法分成3组,每组8人,男女不限,分别单剂量静脉注射0.25、0.50和0.75mg 3种剂量的盐酸帕洛诺司琼注射液后,采用HPLC-MS/MS法测定人血浆中帕洛诺司琼的浓度,用DAS 2.0软件计算药动学参数。结果:3组受试者的主要药动学参数如下:cmax(5.57±2.97)、(6.84±5.48)和(9.75±5.78)μg/L;AUC0～t(24.3±7.6)、(48.3±14.6)和(74.7±25.4)μg.h.L-1;t1/2β(31.0±5.6)、(33.5±5.6)和(31.1±5.0)h。结论:在0.25～0.75mg剂量范围内帕洛诺司琼在健康志愿者体内呈线性药动学特征。本研究建立的帕洛诺司琼测定方法灵敏、准确、简便。

Objective： To study the pharmacokinetics of palonosetron hydrochloride injection in healthy volunteers.Methods： Twenty-four healthy volunteers were divided into three groups by random digital table（8 volunteers in each group） to receive a single dose of 0.25,0.50 and 0.75 mg palonosetron hydrochloride injection by intravenous infusion,respectively.The plasma concentration of palonosetron was determined by HPLC-MS/MS method and the pharmacokinetic parameters were calculated by software DAS 2.0.Results：The main pharmacokinetic parameters of palonosetron in the three groups were as follows： cmax was（5.57±2.97）,（6.84±5.48） and（9.75±5.78） μg/L;AUC0-t was（24.3±7.6）,（48.3±14.6） and（74.7±25.4） μg·h·L-1;t1/2β was（31.0±5.6）,（33.5±5.6） and（31.1±5.0） h.Conclusion： The metabolism of palonosetron in the dosage range of 0.25-0.75 mg exhibits linearity character.This method for determination of palonosetron is simple,accurate and sensitive.