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健康人单次口服不同剂量依地普仑片的药动学

Pharmacokinetics of escitalopram in Chinese healthy volunteers after oral administration of different doses

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【作者】 司天梅邱健文刘薏孙丽丽苏允爱郭春梅张鸿燕舒良

【Author】 SI Tian-mei QIU Jian-wen LIU Yi SUN Li-li SU Yun-ai GUO Chun-mei ZHANG Hong-yan SHU Liang (Institute of Mental Health,Key Laboratory of Mental Health,Ministry of Health,Peking University,Beijing 100083,China)

【机构】 北京大学精神卫生研究所卫生部精神卫生学重点实验室北京大学精神卫生研究所卫生部精神卫生学重点实验室 北京 100083北京 100083

【摘要】 目的:研究中国健康志愿者单次口服不同剂量依地普仑草酸盐片的体内药动学特点。方法:32例受试者单次空腹口服依地普仑草酸盐片,剂量分别为10(n=10),20(n=12),30 mg(n=10)。用HPLC荧光检测法测定血浆中的依地普仑浓度,用DAS统计软件进行数据处理,计算药动学参数。结果:草酸依地普仑片药动学特点符合二房室模型,为线性药动学特点,单次口服依地普仑10,20和30 mg的主要药动学参数是:Cmax分别为(20.91±4.94),(40.28±10.13)和(57.66±10.51)μg·L-1;Tmax分别为(3.80±1.23),(4.18±0.98)和(4.00±1.49)h;t1/2分别为(34.08±26.58),(36.02±23.68)和(36.95±11.58)h;AUC0~t分别为(846.8±466.7),(1437.5±535.5)和(2277.5±506.5)μg·h·L-1,AUC0~∞分别为(975.7±622.4),(1587.1±731.2)和(2496.6±707.4)μg·h·L-1。药动学参数的个体间差异较大,CV%最大值为77.99%。女性受试者和男性受试者的血浆清除率(CL/F)及单位剂量的AUC0~t和AUC0~∞值相似。结论:中国健康受试者单次口服不同剂量草酸依地普仑的药动学参数具有线性药动学特点。

【Abstract】 Objective:To explore the pharmacokinetics of escitalopram tablets after single oral administra- tion of different doses in healthy Chinese volunteers.Methods:A total of 32 subjects participated in the study.Es- citalopram 10 mg,20 mg and 30 mg were given orally to 10,12 and 10 volunteers,respectively.Sequential blood samples were collected and escitalopram concentrations in plasma were determined by a validated high performance liquid chromatography with fluorescence detection.The pharmacokinetic parameters were calculated with DAS soft- ware.Results:Escitalopram disposition in oral administration was characterized by a two-compartment pharmacoki- netic and linear model.The main pharmacokinetic parameters after single doses of 10 mg,20 mg and 30 mg of es- citalopram were:Cmax (20.91±4.94),(40.28±10.13),and (57.66±10.51)μg·L-1;Tmax(3.80±1.23), (4.18±0.98),and (4.00±1.49)h;t1/2(34.08±26.58),(36.02±23.68) and (36.95±11.58) h;AUC0~t, (846.8±466.7),(1437.5±535.5),and (2277.5±506.5)μg·h·L-1;AUC0~∞ (975.7±622.4), (1587.1±731.2) and (2496.6±707.4)μg·h·L-1,respectively.Individual variability was relatively large. The largest CV% value is 77.99%.The CL/F,AUC0~t,and AUC0~∞ on single dose were not significantly different (P>0.05) between male and female subjects.Conclusion:Escitalopram pharmacokinetics in healthy Chinese subjects at three different doses is characteristic of linear pharmacokinetics.

  • 【文献出处】 中国新药杂志 ,Chinese Journal of New Drugs , 编辑部邮箱 ,2008年09期
  • 【分类号】R96
  • 【被引频次】1
  • 【下载频次】110
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