【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。更多还原

【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 were calculated with DAS software.Results Escitalopram disposition on oral administration is characterized by a two-compartment pharmacokinetic model.The mean t1/2 is 41.09 h,Cav is(76.4±26.8)μg·L-1,AUCss is(1832.4±642.4)μg·h·L-1,AUC0-t and AUC0-∞ are(4765.9±2171.0)and(5385.6±2851.2)μg·h·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 pharmacokinetic model.The state-concentration occurre after 7 days of continuously dosing.There is no accumulation after continuously dosing.更多还原