Résumé
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 .