Correlation between reversed-phase high-performance liquid chromatography and plasma protein binding

Journal of Chromatography
J GanansiaJ P Thénot


As hydrophobic interactions are involved in both reversed-phase liquid chromatography and plasma protein binding, the relationship between retention time and binding was investigated experimentally in two series of compounds. For betaxolol and its O-alkyl analogues, the nature of the O-alkyl group strongly influences the retention time on a Spherisorb CN 5-microns column. With 0.03 M acetate buffer (pH 5.6)-acetonitrile (60:40) as the mobile phase, k' values increase from 1.8 to 8.3 with a concomitant increase in plasma protein binding from 0.5% (R = H) to 88.2% (R = cyclopentylmethyl). The relationship between the free fraction and log k' is sigmoidal. In the second example, structural changes in the propyl side-chain of alpidem (a new anxiolytic) lead to minor variations in the protein binding: 98.9 to 84.9%. This slight decrease with the more polar metabolite is correlated with a sharp decrease in the k' values from 14.7 to 0.94 on a Supelcosil LC 18 DB column. Based on retention times, it should be feasible to predict qualitatively, if not quantitatively in some instances, plasma protein binding in a series of structurally similar compounds.


Jan 20, 1995·Journal of Chromatography. B, Biomedical Applications·A van WaardeW Vaalburg
Apr 12, 1996·Journal of Chromatography. B, Biomedical Applications·A van WaardeW Vaalburg
Jan 1, 1993·European Journal of Clinical Pharmacology·R VanholderS Ringoir
Feb 13, 2001·Kidney International. Supplement·R VanholderN Lameire
Jun 15, 1990·Analytical Chemistry·J G DorseyH G Barth
Oct 12, 1990·Journal of Chromatography·C L Davies

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