反式曲马朵及其活性代谢物氧去甲基曲马朵对映体的血浆蛋白结合  

Plasma Protein Binding of the Enantiomers of trans Tramadol and Its Active Metabolite, O-Demethyltramadol

作　　者：刘会臣[1] 胡玉钦 刘长锁 王娜 刘建芳 赵春丽 侯艳宁 

机构地区：[1]中国人民解放军白求恩国际和平医院临床药理室,河北石家庄050082

出　　处：《解放军药学学报》2001年第6期301-302,共2页Pharmaceutical Journal of Chinese People's Liberation Army

摘　　要：目的　研究反式曲马朵 (transT)及其活性代谢物氧去甲基曲马朵 (M1)对映体的血浆蛋白结合。方法　大鼠腹腔注射单剂量盐酸transT ,1h后取血 ,离心超滤法制备血浆超滤液 ,高效毛细管电泳法测定血浆及其超滤液中transT和M1对映体的浓度 ,配对 t-检验比较对映体间的浓度与血浆蛋白结合率。结果　血浆中 (+) - transT的总浓度和游离浓度均高于(- ) -transT ,(+) -transT的血浆蛋白结合率低于 (- ) -transT。M1两对映体的总浓度、游离浓度和血浆蛋白结合率无明显区别。结论　transT与血浆蛋白结合具有立体选择性 。Aim To study the plasma protein binding of the enantiomers of trans tramadol (trans T) and its active metabolite, O-demethyltramadol (M 1). Methods Blood samples were taken 1h after a single ip dose of trans T hydrochloride. The ultrafiltrate of plasma was gotten by centrifugation with means of a Microcon centrifugal filter device. The concent rations of the enantiomers of trans T and M 1 in plasma and its ultrafiltrate were determined by high performance capillary electrophoresis (HPCE). The concentrations and plasma protein binding ratio between the two enantiomers of trans T and M 1 were compared through paired t-test. Results The total and free concentrations of (+)-trans T were higher than those of (-)-trans T; But the plasma protein binding ratio of (+)-trans T were lower than that of (-)-trans T. Between the two enantiomers of M 1, there were no significant differences in total concentrations, free concentrations and plasma protein binding ratio. Conclusion The plasma protein binding of trans T showed marked stereoselectivity. While the plasma protein binding of M 1 didn't exhibit obvious stereoselectivity.

关 键 词：反式曲马朵 氧去甲基曲马朵 对映体 血浆蛋白结合 

分 类 号：R971.1[医药卫生—药品]