Massolini G, De Lorenzi E, Ponci M C, Caccialanza G
Department of Pharmaceutical Chemistry, University of Pavia, Italy.
Boll Chim Farm. 1996 Jun;135(6):382-6.
Immobilized serum albumins (rat and human) HPLC stationary phases have been used to investigate and to compare the binding sites of a number of analytes of pharmaceutical interest assessing the retention time as the chromatographic parameter which correlates the percentage of drug-binding of the corresponding free protein. Anti-inflammatory drugs with different molecular structure were chromatographed and the k' values were determined with a mobile phase based on 100 mM sodium phosphate buffer (pH 6.9) containing 6% n-propanol (v/v). The effect of the addition to the mobile phase of octanoic, decanoic and dodecanoic acids on the k' values enabled to elucidate the site of interaction between the solutes and the two albumins. The results indicate that there are some structural differences in the binding sites of the two albumins and also some quantitative differences with respect to the extent of drug-binding. Moreover the different stereoselective behaviour of the two albumins was studied by analysing some chiral anti-inflammatory drugs much as aryl-propionic acids.
固定化血清白蛋白（大鼠和人）高效液相色谱固定相已用于研究和比较多种具有药物活性的分析物的结合位点，以保留时间作为色谱参数来评估相应游离蛋白质的药物结合百分比。对具有不同分子结构的抗炎药物进行了色谱分析，并使用基于100 mM磷酸钠缓冲液（pH 6.9）且含有6%正丙醇（v/v）的流动相测定了k'值。向流动相中添加辛酸、癸酸和十二烷酸对k'值的影响有助于阐明溶质与两种白蛋白之间的相互作用位点。结果表明，两种白蛋白的结合位点存在一些结构差异，在药物结合程度方面也存在一些定量差异。此外，通过分析一些手性抗炎药物（如芳基丙酸）研究了两种白蛋白不同的立体选择性行为。
