草酸依地普仑片多次给药药动学研究

Pharmacokinetics of domestic escitalopram oxalate tablets after multiple doses to chinese healthy volunteers

目的探讨健康国人多次口服草酸依地普仑片10mg体内药动学特点。方法10名健康受试者,每日空腹口服草酸依地普仑片10mg,连续8d,采用高效液相色谱荧光检测法测定血浆中依地普仑浓度,并计算药动学参数。结果多次口服10mg草酸依地普仑片后药-时曲线符合二室模型,其Cmax,Tmax,T1/2,AUC0-132,AUC0-∞,AUCss,波动度DF,累积系数R分别为(38.00±6.40)μg·L-1,(3.1±1.2)h,(36.8±6.4)h,(1580.0±778.8)μg·h·L-1,(1772.0±804.0)μg·h·L-1,(598.5±124.4)μg·h·L-1,(79.18±27.51)%,(1.51±0.07)。结论健康国人多次口服草酸依地普仑药动学特点与国外研究结果基本接近,多次连续给药有蓄积趋势。

OBJECTIVE To study the pharmacokinetics of escitalopram oxalate tablets in Chinese healthy volunteers. METHODS 9 healthy subjects received a single oral dose of 10 mg escitalopram oxalate tablets. The plasma concentrations of escitalopram were determined by an improved HPLC method. Data of plasma level-time were disposed with 3P97 software. RESULTS The main pharmacokinetics parameters of escitalopram oxalate were as follow： Cmax（38.00±6.40）μg·L^-1,Tmax was（3.1±1.2）h,t1/2 was （36.8±6.4）h,AuC0-132 （1580.0±778.8）μg·L^-1,AUC0-∞ was （1772.0±804.0）μg·L^-1,AUCss was （598.5±124.4）μg·L^-1,（79.18±27.51）%,R was（1.51±0.07）.CONCLUSION The PK parameters of escitalopram oxalate tablets in Chinese was similar to that in Westener. There was a little cumulation when escitalopram oxalate tablets was given with multiple doses.