GC-MS研究不同给药途径复方麝香注射液中β-细辛醚在大鼠体内的药代动力学  

Pharmacokinetic study ofβ-asarone in compound Shexiang injection in rats with different administration routes by GC-MS method

作　　者：彭敏[1] 邓楠[1] 刘文[1] 邓银华[1] 戴迎春[1] 颜笑 陈丽[1] 李威 PENG Min;DENG Nan;LIU Wen;DENG Yin-hua;DAI Ying-chun;YAN Xiao;CHEN Li;LI Wei(Department of Pharmacy,Hunan Provincial People’s Hospital,Changsha 410005,Hunan Province,China;Department of Pharmacy,Hunan Cancer Hospital,Changsha 410005,Hunan Province,China)

机构地区：[1]湖南省人民医院药学部,湖南长沙410005 [2]湖南省肿瘤医院药学部,湖南长沙410005

出　　处：《中国临床药理学杂志》2021年第12期1590-1593,共4页The Chinese Journal of Clinical Pharmacology

基　　金：湖南省自然科学基金资助项目(2018JJ6032);湖南省人民医院仁术基金资助项目(RS201915)。

摘　　要：目的比较复方麝香注射液经不同途径给药后大鼠体内β-细辛醚的药代动力学特征。方法用尾静脉注射(对照组)和肌内注射(实验组)2种给药方式给予SD大鼠复方麝香注射液2.50 m L·kg^(-1)。以β-细辛醚为特征成分,建立气质联用测定大鼠血浆中β-细辛醚的浓度,并计算药代动力学(PK)参数。结果对照组和实验组的β-细辛醚的血药浓度-时间曲线分别符合一级动力学开放性二室模型和一级动力学开放性一室模型。对照组和实验组主要PK参数:AUC0-t分别为(172.00±28.57)和(88.69±14.58)μg·min·m L-1,t1/2分别为(51.13±11.54)和(57.75±9.77)min,CL分别为(2.00×10^(-3)±0.93×10^(-3))和(4.00×10^(-3)±1.37×10^(-3))m L·kg^(-1)·min-1。大鼠肌内注射复方麝香注射液后β-细辛醚的生物利用度为51.56%。结论复方麝香注射液经2种途径给药后大鼠体内β-细辛醚的药代动力学参数基本相似。Objective To compare the pharmacokinetic characteristics ofβ-asarone in rats after administration of compound Shexiang injection by different routes.Methods Sprague Dawley rats were given compound Shexiang injection by tail intravenous injection(control group)and intramuscular injection(experimental group)at dose of 2.50m L·kg^(-1)respectively.Gas chromatography-mass spectrometry was used to determine the concentrations ofβ-asarone as a characteristic component in rat plasma,and the pharmacokinetic parameters were calculated.Results The drug-time curves ofβ-asarone in the control group and experimental group were in accordance with two compartment open model and a dynamic one compartment open model of the firstorder kinetics,respectively.The main PK parameters of the control and experimental groups:AUC0-t were(172.00±28.57)and(88.69±14.58)μg·min·m L-1,t1/2 were(51.13±11.54)and(57.75±9.77)min,CL were(2.00×10^(-3)±0.93×10^(-3))and(4.00×10^(-3)±1.37×10^(-3))m L·kg^(-1)·min-1,respectively.The bioavailability of intramuscular injection was 51.56%.Conclusion Pharmacokinetic parameters ofβ-asarone in compound Shexiang injection in rats by tail vein injection and intramuscular injection were basically similar.

关 键 词：复方麝香注射液 Β-细辛醚 药代动力学 气质联用 

分 类 号：R97[医药卫生—药品]