冬凌草甲素在不同种属血浆中蛋白结合率的HPLC法测定

HPLC determination of protein binding rates of oridonin different plasma*

目的:建立冬凌草甲素在大鼠血浆、人血浆和牛血清白蛋白中蛋白结合率的测定方法,并计算不同种属血浆蛋白的相关参数。方法:采用HPLC法测定血浆中药物总浓度及游离药物浓度,应用平衡透析法测定蛋白结合率。结果:大鼠血浆中冬凌草甲素高、中、低3个浓度的血浆蛋白结合率分别为(69.66±12.8)%,(59.62±12.6)%,(57.94±4.1)%;人血浆中冬凌草甲素高、中、低3个浓度的血浆蛋白结合率分别为(78.15±3.6)%,(77.92±8.8)%,(76.72±7.3)%;牛血清白蛋白中冬凌草甲素高、中、低3个浓度的血浆蛋白结合率分别为(35.58±7.2)%,(34.59±10.8)%,(32.03±6.0)%。结论:在体外冬凌草甲素与大鼠血浆、人血浆和牛血清白蛋白属中等结合型药物,且蛋白结合率随着药物血浆浓度的增加无明显的浓度依赖性。

Objective：To develop an HPLC method to determine the protein binding rates of oridonin in human plasma,rat plasma and bovine serum albumin（BSA）,and to calculate related parameters of oridonin to different genera plasma proteins.Methods： The binding rates of oridonin with different genera plasma proteins were determined by equilibrium dialysis method.The concentrations of oridonin were assayed by HPLC.Results：The binding rates of oridonin with rat,human plasma and BSA at three concentrations levels were（69.66±12.8）%,（59.62±12.6）%,（57.94±4.1）%;（78.15±3.6）%,（77.92±8.8）%,（76.72±7.3）% and（35.58±7.2）%,（34.59±10.8）%,（32.03±6.0）%,respectively.Conclusion：The binding rates of oridonin with human,rat plasma and BSA are middle.Moreover,the binding rates are not dependent proportionally to plasma concentration of oridonin.