平衡透析法测定具栖冬青苷和毛冬青酸的大鼠血浆蛋白结合率

摘要

Objective To create an assay method for determining the concentration of pedunculoside and ilexolic acid in rats plasma , and to determine the plasma protein binding rate by an in vitro method . Methods High performance liquid chromatography (HPLC) and equilibrium dialysis were used to determine the plasma protein binding rate of pedunculoside and ilexolic acid in vitro .Results The protein binding ratios of pedunculoside with low ,moderate and high concentration in vitro were 39 .72% ± 2 .68% ,52 .05% ± 3 .35% and 52 .32% ± 0 .76% ,respectively ;the protein binding ratios of ilexolic acid in vitro were 55 .18% ± 3 .66% ,60 .79% ± 2 .20% and 47 .00% ± 1 .59% ,respectively .Conclusion The HPLC method used to separate pedunculoside and ilexolic acid in rats plasma was simple and convenient .The binding of pedunculoside and ilexolic acid with plasma of rats was moderate and protein binding ratio did not affect the drug concentration .%目的：建立测定具栖冬青苷、毛冬青酸血药质量浓度的方法，并测定其大鼠体外血浆蛋白结合率。方法采用高效液相色谱法和平衡透析法测定具栖冬青苷、毛冬青酸在大鼠体外血浆中的血浆蛋白结合率。结果低、中、高3种质量浓度，具栖冬青苷在大鼠体外血浆中的蛋白结合率分别为39．72％±2．68％，52．05％±3．35％和52．32％±0．76％；毛冬青酸在大鼠体外血浆中的蛋白结合率分别为55．18％±3．66％，60．79％±2．20％和47．00％±1．59％。结论建立 HPLC 法对具栖冬青苷和毛冬青酸进行分离，方法简便。体外实验，具栖冬青苷和毛冬青酸与大鼠血浆属中等结合型药物，且蛋白结合率与药物质量浓度无关。