Relationship between lipophilicity and binding to human serum albumin of arylpropionic acid non-steroidal anti-inflammatory drugs

A possible relationship between lipophilicity and binding to human serum albumin was investigated for 11 arylpropionate non-steroidal anti-inflammatory drugs. The lipophilic parameter was determined by a reversed-phase high-performance liquid chromatographic procedure as the capacity factor ( k′). T...

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Veröffentlicht in:Journal of pharmaceutical and biomedical analysis 1997-10, Vol.16 (2), p.223-229
Hauptverfasser: Deschamps-Labat, Laurence, Péhourcq, Fabienne, Jagou, Maryline, Bannwarth, Bernard
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Sprache:eng
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Zusammenfassung:A possible relationship between lipophilicity and binding to human serum albumin was investigated for 11 arylpropionate non-steroidal anti-inflammatory drugs. The lipophilic parameter was determined by a reversed-phase high-performance liquid chromatographic procedure as the capacity factor ( k′). The binding of arylpropionic acids to human serum albumin was studied in vitro by equilibrium dialysis. For each compound, a Scatchard analysis was performed considering two classes of binding sites characterized by high- and low-affinity constants, K 1 and K 2, respectively. A linear relationship was found between lipophilicity and binding parameters, n 1 K 1 ( r=0.88, P
ISSN:0731-7085
1873-264X
DOI:10.1016/S0731-7085(97)00017-4