中国药理学通报2016，Vol.32Issue(7)：1017-1021,1022,6.DOI:10.3969/j.issn.1001-1978.2016.07.025
LC-MS／MS法测定人血浆中甲磺酸雷沙吉兰的浓度及其体内药动学研究
Determination of rasagiline mesylate in human plasma by LC-MS/MS and its pharmacokinetics study
刘泽娟 1赵萍 1陈娟 1赵佳佳 1华晶 1王凌 1蒋学华1
作者信息
- 1. 四川大学华西药学院，四川成都 610041
- 折叠
摘要
Abstract
Aim To develop LC-MS/MS method to de-termine rasagiline mesylate in human plasma and its application in a pharmacokinetics study .Methods Plasma samples were extracted using liquid-liquid ex-traction with clopidogrel as internal standard .The con-tent of rasagiline mesylate in human plasma was detec-ted by selectivelypositive ion reaction monitoring on a triple quadrupoles tandem mass spectrometer .The de-tected ions were m/z 172.3→117.1 ( rasagiline ) , m/z 322.3 →184.0 ( clopidogrel ) .The linear calibration curve was obtained in the concentration range of 0.1047~20.93 μg · L-1 .The lower limit of quantifi-cation was 0.1047 μg · L-1 .Indicators of the method validation were in line with requirements .The method was used to determine the concentration of rasagiline in human plasma after oral administration of rasagiline mesylate capsule to 24 healthy Chinese volunteers ( with half males and females ) and the results were compared statistically .Results The single oral dose of 0.5 ,1.0 and 2.0 mg presented linear pharmacokinetics in the health volunteers .No accumulation was observed with multiple doses .Meanwhile , no significant difference was identified between the gender groups . High fat postprandial has obvious effects on the peak serum con-centration of rasagiline , but there was no effect on the absorption amount and cumulative excretion .Conclu-sion The LC-MS/MS method is specific and sensi-tive, and can be successfully applied to the pharmaco-kinetic study of Rasagiline mesylate tablets in healthy Chinese volunteers .关键词
甲磺酸雷沙吉兰/药代动力学/血药浓度/LC-MS/MS/人血浆/测定Key words
rasagiline mesylate/pharmacokinetics/plasma concentration/LC-MS/MS/human Plasma/de-termine分类
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刘泽娟,赵萍,陈娟,赵佳佳,华晶,王凌,蒋学华..LC-MS／MS法测定人血浆中甲磺酸雷沙吉兰的浓度及其体内药动学研究[J].中国药理学通报,2016,32(7):1017-1021,1022,6.
