氨酚曲马多胶囊的Ⅰ期临床药动学

Phase Ⅰ pharmakinetics of tramadol hydrochloride paracetamol capsules in Chinese healthy volunteers

目的:研究氨酚曲马多胶囊在健康人体内的药动学过程。方法:10名健康志愿者,男女各半,单剂量口服氨酚曲马多(盐酸曲马多37.5mg+对乙酰氨基酚325mg)2粒,用高效液相色谱法测定血浆中对乙酰氨基酚和曲马多的浓度,并采用PKS药动学程序对试验数据进行处理,求算有关药动学参数。结果:单剂量口服受试制剂2片后,其药-时曲线经拟合对乙酰氨基酚和曲马多均符合二室模型,其中Cmax,tmax,t1/2,AUC0-24,AUC0-∞对乙酰氨基酚分别为(9.5±2.4)mg.L-1,(0.68±0.24)h,(6.0±1.6)h,(30.9±8.5)mg.L-1.h,(32.1±8.7)mg.L-1.h;曲马多分别为(247.0±45.1)μg.L-1,(1.6±0.8)h,(5.5±1.4)h,(1 712.6±556.3)μg.L-1.h,(1 872.8±623.3)μg.L-1.h。结论:氨酚曲马多胶囊单剂量给药后在中国健康人体内耐受良好,人体内的药动学行为与文献报道基本一致。

OBJECTIVE To investigate the pharmacokinetics of tramadol hydrochloride paracetamol capsules after oral administration in Chinese healthy volunteers, METHODS 10 heathy volunteers （5 men and 5 women） were given with 2 capsules. The plasma concentrations of tramadot were determined by HPLC-FLD and paracetamol by HPLC-UV. RESULTS Phannacokineties profiles were fitted to a one compartment model calculated using PKS software. Pharmaeokinetics parameters were as followings： paraeetamol Cmax was（9. 5 ± 2. 4） mg· L^-1, tmax was （0. 68 ± 0. 24） h, t1/2 was（6.0 ± 1.6） h, AUG0-24 was（ 30.9 ±8. 5）mg·L ^-1·h,AUC,0-∞ was （32. 1±8. 7）mg·L^-1·h; tramadol Cmax was （247.0±45. 1）μg·L^-1 ,tmax was （1.6±0.8）h,t1/2 was（5.5±1.4）h,AUQ0-24 was（1712.6± 556.3）μg·L^-1·h, AUG0-∞ was （1 872. 8±623. 3）μg·L^-1·h. CONCLUSION The pharmacokinetics parameters of tramadol hydrochloride paracetamol capsules in Chinese healthy volunteers show no difference to those reported in the literature