LC/MS/MS法测定比格犬血浆中埃克替尼及其在药动学研究中的应用  

Pharmacokinetics of icotinib in Beagle dog studied by using LC/MS/MS method

作　　者：关忠民[1] 陈笑艳[2] 钟大放[1,2] 王印祥[3] 

机构地区：[1]沈阳药科大学 [2]中国科学院上海药物研究所,上海201203 [3]浙江贝达药业

出　　处：《中国临床药理学与治疗学》2008年第10期1158-1162,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：目的:建立灵敏、快速的液相色谱-串联质谱(LC/MS/MS)法测定比格犬血浆中埃克替尼,并用于药动学研究。方法:健康比格犬32只,随机分成4组后,静脉(10mg/kg)或灌胃(10,20和40mg/kg)给予埃克替尼。采用LC/MS/MS法测定血药浓度,并计算出药动学参数。结果:测定埃克替尼的线性范围是0.5～10000ng/mL,日内和日间精密度(RSD)均小于10。静脉给药后AUC0-t为(27.3±15.3)μg.mL-1.h。灌胃给药后AUC0-t分别为(7.47±3.30)、(23.5±11.5)、(54.5±24.9)μg.mL-1.h,埃克替尼在犬体内的绝对生物利用度是27.4。结论:该分析方法选择性好、灵敏度高、操作简便,并成功应用于埃克替尼的比格犬药动学研究。AIM:To develop an LC/MS/MS method for the determination of icotinib in dog plasma and study the pharmacokinetics of icotinib.METHODS:Icotinib was administered to 32 Beagle dogs via intravenous bolus(10 mg/kg) or oral dosing(10,20 or 40 mg/kg) administration after randomly dividing into 4 groups.The concentrations of icotinib in dog plasma were detected by using LC/MS/MS method,and the pharmacokinetic parameters were calculated.RESULTS:The linear calibration curves were obtained in the concentration range of...

关 键 词：埃克替尼 药动学 LC/MS/MS法 比格犬 

分 类 号：R969.1[医药卫生—药理学]