伊立替康及其主要活性代谢物血药浓度和药代动力学测定  

Detection of plasma concentrations and pharmacokinetics of irinotecan and its major active metabolites in man

作　　者：卢红文[1] 蔡东焱[1] 郁皓[1] 刘丽[2] 陶冠军 

机构地区：[1]苏州大学附属第四医院,无锡市214062 [2]江南大学信息工程学院 [3]江南大学仪器科学与技术国家重点实验室

出　　处：《江苏医药》2011年第23期2817-2820,共4页Jiangsu Medical Journal

基　　金：江苏省卫生厅临床药学科研课题[苏卫科基(2010)18]

摘　　要：目的测定抗癌药物伊立替康(CPT-11)及其主要活性代谢物SN-38,SN-38G的血药浓度和药代动力学指标。方法样品先经甲醇-乙腈(50∶50体积比)沉淀蛋白,并用盐酸酸化使内酯环开环。用高效液相色谱仪定量:以喜树碱作内标;Xterra RP18柱,激发波长370nm,检测波长为470nm和534nm。结果血浆CPT-11及其活性代谢物、酸性提取物在此条件下的稳定性较好。三种待测物线性范围皆为1～1000ng/ml,检测限都是1ng/ml。相对标准差为3.1%～11.7%的血浆。测定回收率为93.2%～109.8%。中位提取回收率为91%。结论所建立的方法可用于测定CPT-11,SN38和SN38-G在人血浆中的药物浓度,可满足临床进行CPT-11人体药代动力学研究。Objective To detect plasma concentrations and pharmacokinetics of irinotecan（CPT-11） and its major active metabolites SN-38 and SN-38G in man.Methods Protein precipitation of the sample was performed with methanol-acetonitrile（50∶50 by volume）,which was acidified by hydrochloric acid and quantified with high-performance liquid chromatography（Xterra RP18 column,excitation wave length 370 nm,the emission wave length 470 nm for the first 25 min and then 534 nm for the next 5 min）.Results The stability of CPT-11 and its major active metabolites SN-38 and SN-38G in plasma was good.The linear range tested was 1-1000 ng/L for the three analytes.The limit of quantification was 1 ng/ml,the interassay imprecision was 3.1%-11.7%.The assay recoveries ranged from 93.2% to 109.8%.Mean extraction recovery was 91%.Conclusion The technique mentioned above can be used to determine the pharmacokinetic parameters of CPT-11.

关 键 词：伊立替康 高效液相色谱 药代动力学 

分 类 号：R969[医药卫生—药理学]