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单次和连续口服艾司西酞普兰在中国健康志愿者的药代动力学
引用本文:司天梅,刘薏,赵振国,孙丽丽,苏允爱,郭春梅,张鸿燕,舒良.单次和连续口服艾司西酞普兰在中国健康志愿者的药代动力学[J].中国临床药理学杂志,2009,25(4).
作者姓名:司天梅  刘薏  赵振国  孙丽丽  苏允爱  郭春梅  张鸿燕  舒良
作者单位:北京大学精神卫生研究所,北京,100191
摘    要:目的 研究中国健康志愿者单次和连续口服艾司西酞普兰(抗抑郁药)的体内药代动力学特点.方法 12名健康受试者在第1、8~14天,每日1次空腹口服艾司西酞普兰20 mg;第1、14天服药后不同时间点,以及第12~14天每13服药前,取肘静脉血肝素抗凝,用高效液相色谱-荧光检测法测定血浆中的艾司两酞普兰浓度,用DAS软件计算药代动力学参数.结果 艾司西酞普兰的药代动力学特点符合二房室模型,平均t1/2为41.1 h;Cav为(76.4±26.8)μg·L-1;AUCss为(1832.4±642.4)μg·h·L-1;AUC0-∞和AUC0-∞分别为(4765.9±2171.0)和(5385.6±2851.2)μg·h·L-1;tmax为(3.2±1.3)h;t1/2为(41.1±17.7)h;CL为5.0 L·h-1;AUC的平均累积常数RAUC为(1.2±0.3).结论 艾司西酞普兰连续服药7天可以达稳态,体内无蓄积.

关 键 词:艾司西酞普兰  高效液相色谱-荧光检测法  药代动力学

Pharmacokinetics of escitalopram in Chinese healthy volunteers after single and multiple oral administration
SI Tian-mei,LIU Yi,ZHAO Zhen-guo,SUN Li-li,SU Yun-ai,GUO Chun-mei,ZHANG Hong-yan,SHU Liang.Pharmacokinetics of escitalopram in Chinese healthy volunteers after single and multiple oral administration[J].The Chinese Journal of Clinical Pharmacology,2009,25(4).
Authors:SI Tian-mei  LIU Yi  ZHAO Zhen-guo  SUN Li-li  SU Yun-ai  GUO Chun-mei  ZHANG Hong-yan  SHU Liang
Institution:Peking University Institute of Mental Health;Beijing 100191;China
Abstract:Objective To explore the pharmacokinetics of single and multiple oral 20 mg escitalopram in healthy Chinese volunteers.Methods A total of 12 subjects participated in the study.Escitalopram 20 mg was given orally once on day 1 and days 8 to 14 in the fast condition.Sequential blood samples were collected over 144 hours on day 1 and 14 and a predose sample was obtained on day 12 to 14.Escitalopram concentrations in plasma were determined by a validated HPLC fluorescence method.The pharmacokinetic parameters w...
Keywords:escitalopram  HPLC-fluorescence  pharmacokinetics
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