盐酸曲马多胶囊在汉族健康人体内的药动学研究

 目的研究盐酸曲马多胶囊在汉族健康人体内的药动学。方法选择10名健康受试者口服盐酸曲马多胶囊100 mg后,于不同时间点分别从受试者静脉取血4 mL,用高效液相色谱荧光检测法测定血浆中盐酸曲马多浓度。用3P97药动学软件进行房室模型判断并计算药动学参数。结果口服盐酸曲马多胶囊后,曲马多的药-时曲线符合一级吸收二室模型,t_max为(2.4±0.7)h,ρ_max为(401.4±77.9)μg·L^-1,t_1/2α为(2.1±1.8)h,t_1/2β为(6.6±1.2)h,AUC_0-36为(4 249±1 290)μg·h·L^-1,AUC_0-∞(4 370±1 347)μg·h·L^-1。结论健康受试者单剂量po盐酸曲马多胶囊的药动学参数与文献报道基本一致。不同性别受试者药动学参数的差异无统计学意义。

Pharmacokinetics of Tramadol Hydrochloride in Chinese Han Healthy Volunteers

OBJECTIVE To investigate the pharmacokinetics of tramadol hydrochloride in Chinese Han healthy volunteers.METHODS 10 Healthy volunteers were given with a single oral dose(100 mg) of Tramadol Hydrochloride Capsule.Blood samples were collected from vein at certain sampling times.Tramadol hydrochloride in plasma were determined by HPLC-fluorescence method,and the pharmacokinetic parameters were calculated by 3P97 software.RESULTS The plasma concentration-time curves of tramadol were fitted to a two-compartment model with a first order absorption.The main pharmacokinetic parameters were as follows: t_max(2.4±0.7) h,ρ_max(401.4±77.9) μg·L^-1,t_1/2α(2.1±1.8)h,t_1/2β(6.6±1.2)h,AUC_0-36(4 249±1 290)μg·h·L^-1,AUC_0-∞(4 370±1 347)μg·h·L^-1.CONCLUSION The pharmacokinetic parameters of tramadol in healthy volunteers after an oral single dose of tramadol hydrochloride capsule is concordant with that of the literature.There is no significant difference in the pharmacokinetic parameters between female and male subjects.