论文部分内容阅读
目的:研究反式曲马多对映体:(+ )反式曲马多和( - )反式曲马多的人体药代动力学。方法:12 名受试者po 多剂量盐酸反式曲马多缓释片,用高效毛细管电泳法测定人血清中反式曲马多对映体的浓度,配对t检验比较两对映体的血药浓度和药代动力学参数。结果:血药浓度达稳态后不同时间血清中( + )反式曲马多的浓度均明显高于( -)反式曲马多的浓度,两对映体的Cmax ,Cmin ,Cav,AUC0 →∞,T1/2 等药代动力学参数均有显著性差异。结论:人体对(+ )反式曲马多比对( -)反式曲马多吸收完全、消除慢,反式曲马多对映体有药代动力学立体选择性。
OBJECTIVE: To study human pharmacokinetics of trans-tramadol enantiomers: (+) trans-tramadol and (-) trans-tramadol. Methods: Twelve subjects were given po multi-dose trans-tramadol hydrochloride sustained release tablets. The concentration of trans-tramadol in human serum was determined by high performance capillary electrophoresis. The t-test was used to compare the two enantiomers Blood concentration and pharmacokinetic parameters. Results: The concentrations of (+) - trans-tramadol in serum at different time after the steady-state plasma concentrations were significantly higher than those of (-) - trans-tramadol. The Cmax, Cmin, Cav , AUC0 → ∞, T1 / 2 and other pharmacokinetic parameters were significantly different. CONCLUSION: The human body is completely abolished by (+) - trans-tramadol (-) - trans-tramadol and has the pharmacokinetic stereoselectivity of eliminating the slow and trans-tramadol enantiomers.