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  

Pharmacokinetics of escitalopram in Chinese healthy volunteers after single and multiple oral administration

作　　者：司天梅[1] 刘薏[1] 赵振国[1] 孙丽丽[1] 苏允爱[1] 郭春梅[1] 张鸿燕[1] 舒良[1] 

机构地区：[1]北京大学精神卫生研究所,北京100191

出　　处：《中国临床药理学杂志》2009年第4期308-311,共4页The Chinese Journal of Clinical Pharmacology

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20mg;第1、14天服药后不同时间点,以及第12～14天每日服药前,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西酞普兰浓度,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41.1h;Cav为(76.4±26.8)μg.L-1;AUCss为(1832.4±642.4)μg.h.L-1;AUC0-t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5.0L.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。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. Eseitalopram 20 nag 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. Eseitalopram concentrations in plasma were determined by a validated HPLC fluorescence method. The pharmacokinetic parameters were calculated with DAS software. Results Escitalopram disposition on oral administration is characterized by a two - compartment pharmacokinetic model. The mean tl/2 is 41.09 h, Cav is （76.4±26.8）μg.L-1, AUCs8 is （1832.4±642.4） μg.L-1, AUC0-1 and AUC0-∞ are （4765.9±2171.0） and （5385.6 ＋2851.2）μg.L-1, respectively; tmax is （3.2±1.3） h;t1/2 is （41.1±17.7） h;CL is 5.0 L·h^-1. The mean accumulation index of AUC （RAuc ） is （ 1.2±0.3 ）. Conclusion Escitalopram pharmacokinetics in healthy Chinese subjects given 20 mg once daily dosing regimen were characterized by a two-compartment pharmacokinetie model. The state-concentration oecurre after 7 days of continuously dosing. There is no accumulation after continuously dosing.

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 

分 类 号：R971.43[医药卫生—药品] R969.1[医药卫生—药学]