高效液相色谱法测定美林洛尔与人血浆蛋白的结合率

High performance liquid chromatographic determination MELE concentration and the binding rate of MELE to human plasma proteins

目的：建立人标准血浆中美林洛尔（MELE）浓度的测定方法，测定美林洛尔在人标准血浆中的蛋白结合率，并计算相关参数。方法：用平衡透析法测定血浆蛋白结合率，用高效液相-荧光检测法测定血浆中药物总浓度及游离药物浓度。结果；美林洛尔与人标准血浆的蛋白结合率随药物浓度发生变化约为7．02％～18．75％。MELE与白蛋白结合的表观最大能力岛为0.016μmol·g^-1,药物-蛋白复合物的解离常数Kdp为1．734μmol·g^-1,结合常数Kp为1．2719×10μmol·g^-1,结合位点n为0.0016。结论：在体外美林洛尔与人标准血浆的蛋白结合率较低，并随着药物浓度的增加结合率下降。

OBJECTIVE To develop a high-performance liquid chromatographie（HPLC）method to determine the concentration of MELE in human plasma. To study the binding rate of MELE to plasma proteins, and to calculate the binding parameters of MELE to plasma proteins. METHODS The binding rate of MELE to human plasma proteins was determined by equilibrium dialysis method, Concentration of MELE was assayed by HPLC with fluorescent detection. RESULTS The binding rate of MELE to plasma protein was found to be 7.02%-18.75%, varying with the concentration of MELE. The binding parameters were 0.016 μmol·g^-1 for βp;1.734 μmol·g^-1 for Kdp ; 1.271 9×10^3 L. mol^-1 for Kp and 0.001 6 for n. CONCLUSION The binding rate of MELE to human plasma protein was very low. Moreover plasma concentration of MELE was inversely proportional to the binding rate.