反式曲马朵和反式氧去甲基曲马朵在大鼠胆汁中排泄的立体选择性  

Stereoselectivity in biliary excretion of trans tramadol and trans O-demethyltramadol in rats

作　　者：刘会臣[1] 于洋[2] 王娜[2] 侯艳宁[2] 王永利[1] 

机构地区：[1]河北医科大学药理教研室,河北石家庄050017 [2]白求恩国际和平医院临床药理室,河北石家庄050082

出　　处：《药学学报》2003年第6期412-415,共4页Acta Pharmaceutica Sinica

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 (- )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 Aft...

关 键 词：反式曲马朵 反式氧去甲基曲马朵 对映体 胆汁中排泄 立体选择性 

分 类 号：R965[医药卫生—药理学]