单剂量口服盐酸曲马多在维吾尔族和汉族健康受试者体内的药代动力学研究

Pharmacokinetics study of a single oral dose tramadol hydrochloride in uigur and han healthy volunteers

目的:研究盐酸曲马多在中国维吾尔族和汉族健康受试者体内的药动学。方法:选择维吾尔族和汉族健康志愿者各10名(5男5女),每名口服盐酸曲马多100mg后,用高效液相色谱荧光检测法测定受试者血浆中盐酸曲马多的血药浓度,研究其药代动力学过程,用DasVer2.0药动学软件进行数据处理。结果:汉族、维吾尔族两个民族口服盐酸曲马多后药时曲线均符合一室开放模型。主要药代动力学参数分别为:t1/(26.2±1.0)和(7.1±1.9)h,tma(x2.4±0.7)和(2.6±0.6)h,Cma(x401.4±78)和(350.6±46)μg·L-1,AUC0-3(64297.1±1261.8)和(4111.6±1336.0)μg·h·L-1,AUC0-∞(4456.1±1318.5)和(4368.5±1603.5)μg·h·L-1。结论:服用盐酸曲马多后,汉族、维吾尔族健康受试者的Cmax,AUC0-t,AUC0-∞个体间差异较大,同一民族受试者单剂量口服盐酸曲马多后的药动学参数无明显差异(P>0.05),男女受试者单剂量口服盐酸曲马多后的药动学参数在统计学上有显著性差异(P<0.05)。

Objective： To investigate the pharmacokinetics of tramadol hydrochloride in uigur and han healthy volunteers. Methods： 10 healthy volunteers （5 males, 5 females） in both nation were given a single oral dose （100 mg） of tramadol hydrochloride capsules respectively. Blood samples were determined by HPLC-fluorescent detection method and the pharmacokinetics parameters were calculated by Das Ver 2.0 software. Results： The plasma concentration-time curves of tramadol are both fitted to one-compartment model after an oral tramadol capsule in single dose. The main pharmacokinetic parameters of han and uigur were as follows： t1/2 （6.2 ± 1.0） and （7.1 ± 1.9） h, tmax （2.4 ± 0.7） and （2.6 ± 0.6） h, Cmax （401.4 ± 78） and （350.6 ± 46） μg · L^-1, AUC0-36 （4 297.1 ± 1 261.8） and （4 111.6 ± 1 336.0） μg · h · L^-1, AUC0-∞ （4 456.1 ± 1 318.5） and （4 368.5 ± 1 603.5） μg · h · L^-1 respectively. Conclusion： Individual differences were significant in Cmax, AUC0-1 AUC0-∞ with a single oral dose of tramadol hydrochloride capsules. The pharmacokinetics parameters obtained from our study showed no significant differences between uigur and ban （P 〉 0.05）. In contrast, the pharmacokinetics parameters showed obvious differences between the males and the females （P 〈 0.05）.