Effect of temperature on the binding of salicylate by human serum albumin

Effect of Temperature on Binding of Warfarin by Human Serum Albumin

“…Indeed, as shown in Table IV, these parameters are nearly identical for the small thiocyanate ion and the larger organic molecule of salicylate containing the aromatic ring. Despite this anomaly, it is possible to draw relevant conclusions from the strikingly different thermodynamic parameters recorded for warfarin and azo dyes (15) as contrasted with those for d-tryptophan (25), salicylate (5), and thiocyanate (26). The binding of the first group is characterized by a low negative enthalpy and a considerable positive entropy; the binding by the second group is characteristically enthalpy driven opposed by the negative entro-PY.…”

“…Some aspects of these interactions were discussed previously (7). EXPERIMENTAL Materials a n d Methods-Gel filtration frontal analysis chromatography, which was successfully employed in previous drug binding studies (5)(6)(7)(8), was used for the determination of bound warfarin. Various concentrations of drug were prepared in 0.067 M phosphate buffer, pH 7.4, containing 0.3 g/100 ml of crystalline human serum albumin'.…”

Interpretation of Protein-Drug Interaction through Fraction Bound and Relative Contribution of Secondary Sites

“…Two classes-of-sites resolution of the data ( Table I) The fraction bound-total drug interconversion program (Scheme I) was used to test the value of experimental binding constants in predicting binding information for protein levels other than those used to determine the constants (13). The binding constants from the 0.3 g % (P = 4.21 X M) albumin study for salicylate binding (Table I) were employed in the computer to determine the total drug concentrations for a given range of fraction bound a t the 3.0 g % level of albumin.…”

“…They also provide for changes in the level of protein, assuming that such changes do not influence the binding parameters. This was verified for the salicylate-albumin system in the range of 0.3-3.0 g 96 albumin (13). Partial Fraction Bound-Many drug-protein systems are appropriately resolved into two or more classes of binding sites (10,11,14,15).…”

Interspecies Difference in Drug Protein Binding - Temperature and Protein Concentration Dependency: Effect on Calculation of Effective Protein Fraction

“…In addition, they discussed in vivo situations based on the inadequate experimental data obtained in this way. BACKGROUND Recently, important critical information on these points was reported (4)(5)(6). Shen and Gibaldi (6) provided significant criticism on a previous report (7) that dealt with the application of in uitro drug protein binding data to the prediction of an in uiuo situation utilizing a physiologically based pharmacokinetic model.…”