荧光法简单快速预测药物-血浆蛋白结合率

A Forecast of The Binding Rate of Drug to Plasma Protein by Fluorescence Quenching Method

以抗生素药物头孢匹胺钠(CPMS)为例,在模拟人体生理条件下,研究了不同温度下牛血清白蛋白(BSA)与CPMS的相互作用。由该反应的结合常数及结合位点数建立了预测该药物血浆蛋白结合率的理论模型,由实验数据分析了CPMS浓度与BSA浓度动态变化时药物蛋白结合率的全程规律。研究结果表明,药物与蛋白结合率随蛋白质与药物浓度的改变处于动态变化中。根据文献报道的药物与蛋白反应的结合常数及结合位点数预测了药物血浆蛋白结合率,并与文献数据进行了比较,结果满意。

Taking antibiotic medicine as an example, the interaction between bovine serum albumin （BSA） and cefpiramide sodium （CPMS） was researched at different temperatures in the simulation of the human body physiological conditions. A theoretical model of predicting the binding rate of drug to human plasma protein was estimated according to the binding constants and the number binding site in this reac- tion. Based on the experimental data, the regular pattern of the binding rate of drug to plasma protein was analyzed when the concentration of CPMS and BSA was dynamically changed. The results showed that the binding rate of drug to human plasma protein was dynamically changed in different concentration of protein and drug conditions. Besides, the binding rate of drug to plasma protein was forecasted on the basis of binding constants and the number binding site in the reaction of drug and protein in literature, and it showed a satisfied result compared with the data in literature.