Acidic drugs binding affinity

For the QSRR of reversed-phase liquid chromatography, the contact surface area is important, and the selection of a model phase is difficult, but a simple model phase is satisfactory for the measurement of albumin-acidic drug binding affinity in ion-exchange liquid chromatography/ ... 

Further analysis was performed to estimate the albumin-acidic drug binding affinity log oRT values. The albumin-acidic drug binding affinity was measured at pH 7.40. The log k values measured at pH 7.40 correlated with the predicted log tiK" values from the literature. The following relationship was obtained, log tiK = 1.597 x(log A )+ 5.808, r= 0.887, n = 13. The log nAT values may be derived from log k values measured on a guanidino phase at pH 7.40. Therefore, the addition of k measured by reversed-phase liquid chromatography improved the correlation, as previously described. ... 

Table 7.7 Molecular properties of some acidic compounds, logn represents the Human Serum Albumin (HSA)-drug binding affinity, from ref. 13. lognSf represents the HSA-drug binding affinity measured using a two-column system, from ref. 13. pKl are reference values, from ref. 13 TpKl values were measured by ion-exchange liquid chromatography. Mlm represents the molecular interaction eneigy calculated for the molecular-form compound, and Mlj the molecular interaction energy calculated for the ionic-form compound (kcal moP ).

Table 18 Human serum albumin-drug binding affinity and drug properties. rrSTi represents log k measured using an immobilized-HSA phase. nKa represents predicted log hsa-represents log k of acidic compounds at pH 7.4. k represents log k of basic compounds at pH 7.4. MIFa and MIFb represents the molecular interaction energy values of acidic and basic compounds, resepectively. nKs represents log nST measured using a modified Hummel-Dreyer method. nJQ, nKs, nSTg and nKj represent values. PB and PB2 represent the binding %. Log Pc are predicted log P values, and log Pm are measured values. 7.4 represents pH 7.4. Reproduced by permission of Bentham Science, ref. 20.

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