地芬尼多在健康人体内药动学研究

 目的研究盐酸地芬尼多片在健康人体中的药动学过程。方法采用双周期试验设计,12名健康志愿者单次和多次口服盐酸地芬尼多片50mg。建立GC-MS测定血药浓度,用DAS软件计算药动学参数,用AIC法结合F检验判别房室模型。结果盐酸地芬尼多片的药-时曲线符合一级吸收的二室开放模型,单次和多次给药主要药动学参数如下:ρ_max分别为(321.15±162.46)和(360.98±175.58)μg·L^-1,t_max分别为(2.25±0.62)和(1.75±0.54)h,t_1/2β分别为(21.22±22.30)和(29.27±49.65)h,AUC_0-36分别为(1052.75±596.25)和(2300.01±1533.73)μg·h·L^-1,AUC_0-∞分别为(1287.19±2931.36)和(2931.36±1668.27)μg·h·L^-1,ρ_ss-max为(360.98±175.58)μg·L^-1,ρ_ss-min为(127.23±61.22)μg·L^-1,ρ_ss-av为(129.12±136.36)μg·L^-1,DF为(1.10±0.39),AUC_SS为(1526.77±734.69)μg·h·L^-1。结论单次与多次给药,主要药动学参数ρ_max、AUC_0-36、AUC_0-∞统计学配对t检验呈极显著性差异。

Pharmacokinetics of Difenidol in Healthy Volunteers

OBJECTIVE To study the pharmacokinetics of difenidol hydrochloride tablets in healthy volunteers. METHODS In a crossover design study, 12 healthy volunteers received a single dose and multiple-dose regimen of diphenidol tablets 50 mg. The plasma concentrations were determined by GC-MS. The pharmacokinetic parameters were calculated by DAS software and the pharmacokinetic profile was fitted by AIC-F test method. RESULTS The concentration-time curve of a single dose and multiple-dose regimen were discribed with a two-compartment open model with first-order absorption. The main pharmacokinetic parameters of the single dose and multiple-dose regimen were as follows:ρ_max(321.15±162.46)and(360.98±175.58)μg·L^-1,t_max(2.25±0.62)and(1.75±0.54)h,t_1/2β(21.22±22.30)and(29.27±49.65)h, AUC_0-36(1 052.75±596.25)and (2 300.01±1 533.73)μg·h·L^-1,AUC_0-∞(1 287.19±2 931.36)and(2 931.36±1 668.27)μg·h·L^-1,ρ_SS-max(360.98±175.58)μg·L^-1,ρ_ss-min(127.23±61.22)μg·L^-1,ρ_ss-av(129.12±136.36)μg·L^-1, DF was(1.10±0.39), AUC_SS was(1 526.77±734.69)μg·h·L^-1. CONCLUSION The statistical analysis shows that there are significant difference between the single dose and multiple-does regimen