【摘要】 目的　研究反式曲马朵 (transT)及反式氧去甲基曲马朵 (M1 )在大鼠胆汁中排泄的立体选择性。　方法高效毛细管电泳法测定大鼠ivtransT或M1后胆汁和血浆中transT ,M1和与葡糖醛酸结合M1 (M1 c)的对映体。结果　大鼠ivtransT后 ,胆汁中 (+) transT水平较 (- ) transT高 ,(+) (- ) transT较血浆中 (+) (- ) transT的比值小。大鼠ivM1后 ,胆汁中 (+) M1水平较 (- ) M1高 ,(+) M1 c 较 (- ) M1 c 低 ,(+) M1与葡糖醛酸的结合率较(- ) M1低。结论　TransT和M1在大鼠胆汁中排泄具立体选择性 ,(+) transT和 (- ) M1被优先排泄更多还原

【Abstract】 Aim To investigate the stereoselectivity in biliary excretion of trans tramadol (trans T) and trans O-demethyltramadol (M1) in rats. Methods After a single intravenous dose of trans T hydrochloride (10 mg·kg -1 ) or M1 (2.5 mg·kg -1 ) to rats, the bile was collected for 30 min, then, blood was obtained from the heart. The enantiomers of trans T, M1 and M1 conjugated with glucuronic acid (M1 c) in the bile and plasma were analyzed by high performance capillary electrophoresis (HPCE). Results After the rats were given trans T, the bile concentrations of (+)-trans T were higher than those of (-)-trans T, and the (+)/(-)- trans T ratios were lower compared with those in the plasma. After the rats were given M1, the bile concentrations of (+)-M1 were higher than those of (-)-M1, and the bile concentrations of (+)-M1 c were lower than those of (-)-M1 c. The glucuronidation rate of (+)-M1 was lower than that of (-)-M1 in the bile. Conclusion The biliary excretion of trans T and M1 was stereoselective, (+)-trans T and (-)-M1 being preferentially excreted.更多还原