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目的:测定川芎嗪硝酮衍生物M PI-01在大鼠及人血浆中的蛋白结合率.方法:采用血浆超滤液测定超滤管与药物的非特异吸附系数,对超滤法进行校正,并验证校正超滤法的准确性.利用校正超滤法测定MPI-01血浆蛋白结合率,将所得结果与平衡透析法进行比较.结果:MPI-01与人及大鼠血浆蛋白结合率分别为8.3％～8.7％,7.5％～8.2％.结论:校正后的超滤法测定药物血浆蛋白结合率较为准确,尤其适于蛋白结合率低的药物.该法成功应用于MPI-01的血浆蛋白结合率测定,实验证明MPl-01与血浆蛋白结合程度低.“,”Objective:To determinate tetramethylpyrazine-nitrone derivative MPI-01 plasma protein binding rate in rat and human plasma.Methods:The plasma uhrafihrate was firstly chosen to determine drug's nonspecific binding coefficient with the ultrafiltration device,and the accuracy of this method was validated.Then it was applied to determine the plasma protein binding rate of MPI-01,and the results were compared with the equilibrium dialysis method.Results:The plasma protein binding rate of MPI-01 in human and rat plasma was 8.3％ ～ 8.7％,7.5％ ～ 8.2％,respectively.Conclusion:The rectified ultrafiltration method was accurate in determining plasma protein binding of drugs,especially to the low binding drugs.As a result,the plasma protein binding rate of MPI01 was low.