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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 ,M1与血浆蛋白结合的立体选择性不明显
Aim To study the plasma protein binding of trans-trans-T and its active metabolite oxygen-demethyl tramadol (M1) enantiomer. Methods The rats were intraperitoneally injected with a single dose of transT for 1 h, then the blood was collected and the ultrafiltrate was prepared by centrifugal ultrafiltration. The concentrations of transT and M1 enantiomers in plasma and ultrafiltrate were determined by high performance capillary electrophoresis. The t- Compare enantiomeric concentrations with plasma protein binding. Results The total and free concentrations of (+) - transT in plasma were higher than that of (-) - transT and the plasma protein binding of (+) - transT was lower than that of (-) - transT. M1 total enantiomer concentration, free concentration and plasma protein binding rate no significant difference. Conclusion The transT binding to plasma protein has stereoselectivity, and the stereoselectivity of M1 binding to plasma protein is not obvious