The effective concentration of a drug in the blood, i.e. the concentration of a free drug in the blood, is influenced by the strength of drug binding onto plasma proteins. Besides its efficacy, these interactions subsequently influence the liberation, absorption, distribution, metabolism, excretion, and toxicological properties of the drug. It is important to not only determine the binding strength and stoichiometry, but also the binding site of a drug on the plasma protein molecule, because the co-administration of drugs with the same binding site can affect the above-mentioned concentration and as a result the pharmacological behavior of the drugs and lead to side effects caused by the change in free drug concentration, its toxicity. In this study, the binding characteristics of six drugs with human serum albumin, the most abundant protein in human plasma, were determined by capillary electrophoresis-frontal analysis, and the obtained values of binding parameters were compared with the literature data. The effect of several drugs and site markers on the binding of l-tryptophan and lidocaine to human serum albumin was investigated in subsequent displacement studies which thus demonstrated the usability of capillary electrophoresis as an automated high-throughput screening method for drug-protein binding studies.
- MeSH
- chlorpropamid analýza farmakologie MeSH
- diklofenak analýza farmakologie MeSH
- elektroforéza kapilární MeSH
- fenylbutazon analýza farmakologie MeSH
- flurbiprofen analýza farmakologie MeSH
- ibuprofen analýza farmakologie MeSH
- lidé MeSH
- lidokain antagonisté a inhibitory chemie MeSH
- lidský sérový albumin chemie MeSH
- tolbutamid analýza farmakologie MeSH
- tryptofan antagonisté a inhibitory chemie MeSH
- vazebná místa účinky léků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
