【摘要】 本文首次报道合成α-细辛脑的人体各项药物动力学参数。10名健康志愿者单剂量口服“α-细辛脑120mg,采用静脉置留针取血,反相高效液相色谱法测定α-细辛脑血中浓度。药时曲线呈二室模型,其清除半衰期3.5±1.0h,达峰时0.91±0.29h,峰浓度120±116ng/ml,药时曲线下面积149±95ng·h/ml,吸收速度常数4.1±2.8h^-1。结果表明,该药口服吸收快,在人体内分布广泛,并提示存在个体差异。更多还原

【Abstract】 α-Asaronum（1-Propaylene-2,4,5-Trimethoxy Benzen）is one of composition in Acorus gramineus Soland（Chineseherbal medicine）.This paper first reported the pharmacokinetic study of synthetic α-Asaronum in human body.5 males and5 females of healthy volunteers were tested,age 32±14 years and bodyweight 54±6kg.After 120mg of α-Asaronum wastaken by oral adiministration,the serum sample was run assay for drug concentration within 12h by High Performance LiquidChromatography.The serum concentration-time relationship was compatible with a two compartmental model.Thepharmacokinetic equation is 563e^-2.08t+11.4e^-0.21t-574.4e^-4.1t,α=2.1±0. 7h^-1,β=0.21±0.05h^-1,Ka=4.1±2.8h^-1,K₂₁=0.31±0. 07h^-1,K₁₂=0. 52±0.15h^-1,K₁₀=1.5±0. 6h^-1,T_1/2β=3.5±1.0h,T_max=0.91±0.29h,C_max=120±116ng/ml,AUC 0→12=149±95ng·h/ml,Vd/F=126±133L/kg.The results showed that α-Asaronum was widelydistributed in body and absorbed rapidly by human body.It indicated that individual difference of Vd is existent.更多还原