校正超滤法测定川芎嗪硝酮衍生物MPI-01的血浆蛋白结合率  

Determination of plasma protein binding rate of tetramethylpyrazine-nitrone derivative MPI-01 by rectified ultrafiltration

作　　者：廖凯谊[1] 孙业伟[1] 于沛[1] 程俊辉 张高小[1] 

机构地区：[1]暨南大学新药研究所,广州510632 [2]广州喜鹊医药有限公司,广州510530

出　　处：《中国新药杂志》2013年第16期1890-1894,共5页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2012ZX09103-101-055);广东省重大科技专项(2012A080201009);广东省企业科技特派员工作站建设项目(2011B090600033)

摘　　要：目的:测定川芎嗪硝酮衍生物MPI-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MPI-01与血浆蛋白结合程度低。Objective： To determinate tetramethylpyrazine-nitrone derivative MPI-01 plasma protein bind- ing rate in rat and human plasma. Methods： The plasma ultrafihrate was firstly chosen to determine drug＇s nonspe- cific 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 MPI- 01 was low.

关 键 词：校正超滤法 川芎嗪硝酮衍生物 血浆蛋白结合率 

分 类 号：R969.1[医药卫生—药理学]