五味子甲素4_℃条件下血浆蛋白结合率的测定

目的: 建立HPLC测定五味子甲素与大鼠血浆蛋白结合率的方法。 方法: 采用HPLC法测定大鼠血浆中五味子甲素的总浓度及游离药物浓度,色谱分离采用Agilent Zorbax SB-C₁₈(3.0 mm×100 mm,3.5 μm)色谱柱,以水-乙腈(40∶60)为流动相,流速0.8 mL·min^-1,柱温30 ℃,检测波长225 nm,进样量5 μL;应用平衡透析法测定4 ℃条件下五味子甲素与大鼠血浆蛋白的结合率。 结果: 低、中、高3种浓度下,五味子甲素的血浆蛋白结合率分别为(76.0±4.7)%、(87.1±3.2)%、(89.1±1.7)%。 结论: 在体外,五味子甲素与大鼠血浆蛋白结合率较高,不存在浓度依赖性。

Objective: To establish a method for the determination of the rat plasma protein binding rate of deoxyschisandrin. Methods: The total concentration of deoxyschisandrin and the free drug concentration were determined by HPLC.The separation was performed on an Agilent Zorbax SB-C₁₈(3.0 mm×100 mm,3.5 μm)column,the mobile phase consisted of water containing 0.1% formic acid and acetonitrile(40∶60)was used as isocratic elute at the flow rate of 0.8 mL·min^-1.The temperature of column was 30 ℃,the detective wavelength was 225 nm,and the injection volume was 5 μL.The rat plasma protein binding rate of deoxyschisandrin was determined by equilibrium dialysis method at 4 ℃. Results: The plasma protein binding rates of deoxyschisandrin at low,middle and high concentration was (76.0±4.7)%,(87.1±3.2)%,and (89.1±1.7)%,respectively. Conclusion: The in vitro binding power of deoxyschisandrin to rat plasma is high,without density dependence.

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