白芍总苷在CCl_4肝损伤大鼠和正常大鼠血浆中蛋白结合率的比较

Study on plasma protein binding rates of total glucosides of paeony in liver injury rats induced by CCl_4 and in normal rats

目的 :以芍药苷和芍药内酯苷为指标成分,建立白芍总苷血浆蛋白结合率的测定方法,比较其在CCl4肝损伤大鼠及正常大鼠血浆中蛋白结合率的异同。方法 :采用大鼠血浆平衡透析法,HPLC法测定透析袋两侧溶液中芍药苷和芍药内酯苷的质量浓度,分别计算其在CCl4肝损伤大鼠血浆中和正常大鼠血浆中的蛋白结合率。结果 :白芍总苷血浆浓度为50,100和200μg/ml时,芍药苷与肝损伤大鼠血浆的蛋白结合率分别为(15.5±0.4)%、(16.5±1.4)%、(27.9±1.6)%,与正常大鼠血浆的蛋白结合率分别为(12.7±1.6)%、(13.5±0.8)%、(15.6±0.6)%;芍药内酯苷与肝损伤大鼠血浆的蛋白结合率分别为(12.4±1.5)%、(13.2±1.6)%、(20.2±2.1)%,与正常大鼠血浆的蛋白结合率分别为(8.1±0.9)%、(9.7±2.3)%、(14.7±1.4)%。结论 :白芍总苷中主要成分芍药苷和芍药内酯苷与CCl4肝损伤大鼠及正常大鼠血浆的蛋白结合均属低度结合,且与血药浓度有一定的依赖性,CCl4肝损伤后大鼠血浆蛋白结合率较正常大鼠提高,提示白芍总苷临床应用时可能受患者肝功能状态的影响。

Aim： To determine the plasma protein binding rates of Total Glucosides of Paeony（TGP）in liver injury rats induced by CCl4 and in normal rats,using paeoniflorin and albiflorin as the indicator composition.Methods： The equilibrium dialysis method and HPLC were employed to determine the plasma protein binding rates of paeoniflorin and albiflorin in TGP in liver injury rats induced by CCl4 and in rat plasma.The plasma protein binding rates of high,middle and low groups were calculated using standard curves.Results ： At the concentration of 50,100,200 μg/ml of TGP,the plasma protein binding rates of Paeoniflorin with liver injury rat plasma were（15.5±0.4）%,（16.5±1.4）%,（27.9±1.6）% and with normal rat plasma were（12.7±1.6）%,（13.5±0.8）%,（15.6±0.6）%.the plasma protein binding rates of albiflorin with liver injury rat plasma were（12.4±1.5）%,（13.2±1.6）%,（20.2±2.1）% and with normal rat plasma were（8.1±0.9）%,（9.7±2.3）%,（14.7±1.4）%.Conclusions： Paeoniflorin and albiflorin in TGP had low protein binding capacities with the two kinds of rat plasma.Moreover,the binding rates are proportionally dependent on plasma concentration of TGP.The binding rates are increased dramatically in liver injury rats induced by CCl4 compared with the normal rats.