超滤法结合替代对照品HPLC测定大蒜辣素与大鼠及人血浆的蛋白结合率

Determination of Human and Rat Plasma Protein Binding of Allicin by Ultrafiltration and HPLC with Alternative Reference

目的:测定大蒜辣素与大鼠及人血浆的蛋白结合率,为大蒜辣素的成药性研究提供参考。方法:以羟苯乙酯为替代对照品,采用C_(18)色谱柱,流动相甲醇-1%甲酸梯度洗脱,流速1.0 m L·min^(-1),检测波长254 nm,结合超滤法对大蒜辣素与大鼠及健康人血浆的蛋白结合率进行测定。结果:测得75,150,300 mg·L^(-1)大蒜辣素溶液与大鼠和人血浆蛋白结合率分别为23.2%,19.8%,28.1%及15.5%,25.8%,40.0%。结论:大蒜辣素与大鼠及人的血浆蛋白结合率均较低,替代对照品HPLC可用于测定大蒜辣素的血浆蛋白结合率。

Objective： To Detemine human and rat plasma protein binding rate of allicin,and provide a reference for research of allicin into medicinal properties. Method： With ethylparaben as an alternative reference, C18 column was used,mobile phase was methanol-1% formic acid for gradient elution in a flow rate of 1.0 mL · min^-1 and detection wavelength was 254 nm. Result： With different concentration of allicin including 75,150,300 mg · L^-1, protein binding rates of allicin in rat and human plasma were 23.2%,19.8%,28.1% and 15.5%,25.8%,40.0%,respectively. Conclusion： Allicin has low level in binding to plasma protein of human and rat.HPLC with ethylparaben as alternative reference can be used to determine plasma protein binding rate of allicin.