Quantitative study of competitive binding of drugs to protein by microdialysis/high-performance liquid chromatography.
A displacement equation describing competitive binding of drugs to protein in solution is derived and examined with four nonsteroidal anti-inflammatory drugs and human serum albumin as model drugs and protein, respectively. Microdialysis/high-performance liquid chromatography was adopted to determine simultaneously the unbound solute and displacing agent in drug-protein solutions. The method is able to locate the binding site and determine affinity constants even up to 10(7) L/mol accurately. A comparison of association constants determined by this method and from capacity factors on HSA-CSP is given.
Wang
H
H
National Chromatographic R.&A. Centre, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, China.
Zou
H
H
Zhang
Y
Y
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000097:blood; D001667:Binding, Competitive; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D066298:In Vitro Techniques; D017551:Microdialysis; D010599:Pharmacokinetics; D011485:Protein Binding; D012709:Serum Albumin / Q000378:metabolism
D000894:Anti-Inflammatory Agents, Non-Steroidal; D012709:Serum Albumin