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Gonciarz-Dytman, Anna
2018
Praca doktorska
Drug–protein binding is an important process affecting the pharmacokinetics and activity of drug, since only the free drug can pass across biological membranes and get to its site of action. In recent years, high-performance techniques have been sought to assess physicochemical properties and to study the ADME profile of compounds.The aim of this study was to develop, optimize and validate methods for separating and determining the free fraction of dexamethasone (DXM) and pravastatin (PRA) using capillary electrophoresis/frontal analysis (CE/FA) to assess their binding to plasma proteins. CE/FA has been compared with equilibrium dialysis (ED), considered as reference method. The thermodynamics of the binding process of DXM and PRA to bovine and human albumin were evaluated. CE/FA was used to study binding of compounds with endothelial activity to blood proteins, and the relationship between physicochemical properties of the tested compounds and the degree of their binding to studied proteins were evaluated.CE/FA can be used in high-throughput screening of drug-protein binding at the early stage of drug discovery. An advantage of CE/FA over ED is the ability to directly measure the concentration of free fraction of a compound in a sample, what significantly reduces costs and shortens the duration of the analysis. It can be use to evaluate the thermodynamics of binding process.
Kraków
2 - studia doktoranckie
farmacja
Wydział Farmaceutyczny
Walczak, Maria
2017
oai:dl.cm-uj.krakow.pl:4282
ZB-128499
pol
nieograniczony
Jun 26, 2023
May 7, 2019
115
112
http://dl.cm-uj.krakow.pl:8080/publication/4283
RDF
OAI-PMH
Szpyra, Bartłomiej
Małek, Agnieszka
Latacz, Gniewomir
Bajda, Marek
Godyń, Justyna
Citation style: chicago-author-date iso690-author-date
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