盐酸曲马多片人体药代动力学和生物等效性

Pharmacokinetics and relative bioequivalence of tramadol hydrochloride in healthy volunteers

目的 :比较国产和进口盐酸曲马多片在人体内的药物代谢动力学和生物等效度 ,确保临床用药质量 .方法 :1 8例男性健康受试者采用标准二阶段自身交叉对照试验法服用药物 ,以高效液相色谱荧光法测定受试者服药后 2 4h内血清中曲马多经时浓度 ,计算曲马多的药动学参数 ,并将数据作统计学处理 .结果 :国产和进口盐酸曲马多的血药达峰时间Tmax(实测值 )分别为 (2 .3± 0 .7)和 (2 .3± 0 .7)h ,峰值血清浓度Cmax(实测值 )分别为 (2 2 3± 79)和 (2 2 9± 6 5 ) μg·L-1 ,药时曲线下面积AUC(0 2 4h) 分别为 (2 1 73± 6 80 )和 (2 2 5 2± 5 97)μg·h·L-1 ,两种盐酸曲马多片上述药动学参数间均无统计学差异 (P >0 .0 5 ) ,国产对进口盐酸曲马多片的相对生物利用度为 96 .4 0 % .结论

AIM: To compare the pharmacokinetic parameters and relative bioavailability of domestic and imported tramadol hydrochloride tablets so as to ensure quality of the medicine. METHODS: An open, randomized, two period crossover study with a two week washout interval was performed in 18 healthy volunteers. Concentrations of tramadol in serum were assayed by HPLC FR method. The pharmacokinetics parameters, AUC, Cmax and Tmax, were analyzed by two one side t test. RESULTS: The concentration time course after medication conformed to a 1 compartment open model with a first order absorption. The AUC (0 24 h) , Cmax and Tmax of tramadol were (2173±680) and (2252±597) μg·h/L,(223±79) and (229±65)μg/L, (2.28±0.67) and (2.33±0.67)h respectively. The relative bioavailability of tramadol was 96.40%. CONCLUSION: Two tablets are bioequivalent.