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烯丙雌醇片在健康人体的药代动力学研究

Pharmacokinetic Study of Allylestrenol Tablets in Healthy Volunteers
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摘要 目的:建立准确、灵敏的液相色谱—串联质谱法(LC-MS/MS)测定人血浆中烯丙雌醇的浓度,并评价中国健康女性受试者单剂量口服烯丙雌醇片后的药动学特征。方法:20例女性健康受试者单剂量口服20mg烯丙雌醇片后按时采集血样,以米非司酮为内标,采用APCI正离子选择性反应监测测定烯丙雌醇血浆浓度,计算药动学参数。结果:单剂量口服20mg烯丙雌醇后,烯丙雌醇的主要药动学参数Cmax为(12.48±4.18)ng·ml^(-1),Tmax为(1.9±0.8)h,t1/2为(8.4±3.2)h,MRT0-∞为(6.7±2.6)h,AUC0-36为(41.29±14.83)h·ng·ml^(-1),AUC0∞为(42.72±15.33)h·ng·ml^(-1)。结论:建立的LC-MS/MS测定法结果准确可靠,灵敏度高。 Objective:To estabhsh an accurate and sensitive LC-MS/MS method for the determination of allylestrenol in plasma and to evaluate its pharmacokinetic study in healthy Chinese women volunteers after po the altylestrenol tablets.Methods:The 20 healthy women volunteers received allylestrenot tablet respectively for a single oral dose of allylestrenol 20mg.The plasma concentrations of allylestrenol were determined by a validated LC-APCI-MS/MS method with positive ion SRM mode using mifepristone as internal standard.The pharmaeokinetie parameters were calculated.Results:The main pharmaeokinetic parameters after the single oral dose of allylestrenol tablet(20mg)were as follows:Cmax was(12.48±4.18)ng·ml^-1,Tmax was (1.9±0.8)h,t1/2 was(8.4±3.2)h, MRT0-∞ was(6.7±2.6)h,AUC0-36 was(41.29±14.83)h·ng·ml^-1,AUC0-∞ was (42.72±15.33)h·ng·ml^-1. Conelusions:The validated LC-MS/MS for the determination of allylestrenol in human plasma is accurate,sensitive and reliable.
出处 《中国医药导刊》 2009年第11期1870-1872,共3页 Chinese Journal of Medicinal Guide
关键词 烯丙雌醇 药代动力学 LC-MS/MS 大气压化学离子化 Allylestrenol Pharmacokinetics LC-MS/MS APCI(atmospheric pressure chemical ionization)
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