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以酮基布洛芬 (ketoprofen)与人血清白蛋白为例 ,利用微透析取样技术建立了药物与蛋白质相互作用研究的新方法 .结果表明酮基布洛芬与人血清白蛋白的结合有两类非等价结合位点 ,以Scatchard方程拟合 ,一级结合的位点数和亲合常数分别为 0 .799,3.1 8× 1 0 6(mol·L-1) -1,二级结合的位点数和亲合常数分别为 2 .1 5 ,2 .0 1×1 0 5 (mol·L-1) -1.同时还考察了药物与人血清白蛋白结合的置换效应 ,表明布洛芬(ibuprofen)与酮基布洛芬的一级结合位点相同可使酮基布洛芬的结合率大大降低 ,两者间有较强的置换效应 .酮基布洛芬与华法令 (warfarin)的一级结合位点不同 ,彼此没有明显的置换效应 .采用液相色谱中的顶替吸附理论较好地表达了药物间的置换效应 .微透析取样技术测定药物与蛋白质相互作用具有简单、快速、易于自动化的优点 .
Taking ketoprofen and human serum albumin as an example, a new method of drug-protein interaction was established by using microdialysis sampling technique.The results showed that the combination of ketoprofen and human serum albumin had two Non-equivalent binding sites, using Scatchard equation fitting, the number of primary binding sites and affinity constants were 0.799, 3.1 8 × 10 6 (mol·L -1) -1, secondary binding sites The number of points and affinity constants were 2.15, 2.01 × 10 5 mol·L -1, respectively. The substitution effect of the drug and human serum albumin was also examined, indicating that ibuprofen ) And Ketoprofen the same primary binding site Ketoprofen binding rate can be greatly reduced, the two have a strong displacement effect.Ketoprofen and warfarin Level binding sites are different, there is no obvious displacement effect on each other.Using the displacement adsorption theory in liquid chromatography to better express the displacement effect between drugs.Micro-dialysis sampling technology to determine drug-protein interaction is simple, rapid and easy to automate The advantages .