微透析法测定虎杖苷的体外血浆蛋白结合率及与超滤法的比较

    Comparison of Microdialysis and Ultrafiltration Methods for Determination of Plasma Protein Binding Rate of Polydatin in Vitro

    • 摘要: 目的 采用微透析技术研究虎杖苷的体外血浆蛋白结合率,并与超滤法比较。 方法 微透析探针依次浸入含虎杖苷20,60,200 μg·mL-1的大鼠、人血浆中,灌注器以2.5 μg·min-1的流速依次灌注含虎杖苷0,10,30,100,300 μg·mL-1的生理盐水,每15 min收集1次样品,HPLC分析虎杖苷浓度。以灌注液与透析液中虎杖苷的浓度差对灌注液浓度进行线性回归,计算血浆中游离虎杖苷的浓度,进而计算虎杖苷的血浆蛋白结合率,并与超滤法进行比较。 结果 微透析测定虎杖苷与大鼠、人血浆蛋白结合率平均值分别为86.15%,89.08%,超滤法分别为85.60%和87.24%,两种方法结果比较接近。 结论 虎杖苷与大鼠、人血浆蛋白有较高的结合率,微透析法和超滤法结果一致。

       

      Abstract: OBJECTIVE The microdialysis method was used to study the plasma protein binding rate of polydatin, and the obtained results were compared with those of the conventional ultrafiltration method. METHODS The microdialysis- HPLC method was applied to dialysis the difference of concentration between dialysis fluid and perfusion fluid concentration on linear regression analysis, so the concentration of free polydatin in drug-containing plasma could be calculated, then the binding rate of polydatin with rat and human plasma can be calculated, and compared with ultrafiltration method. RESULTS The plasma protein binding rate of polydatin of rat and human plasma were about 86.15% and 89.08% respectively for microdialysis method, and were around 86.15% and 89.08% for ultrafiltration method. There was no significant difference between the two methods. CONCLUSION The binding percentage of polydatin with rat and human plasma is relative high, and results of the two methods are consistent.

       

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