6533b82bfe1ef96bd128e1b5

RESEARCH PRODUCT

Quantitative structure-retention and retention-activity relationships of beta-blocking agents by micellar liquid chromatography.

D.l. MassartA DetroyerY. Vander HeydenMaría Celia García-alvarez-coqueSamuel Carda-broch

subject

ChromatographyChemistryOrganic ChemistryAdrenergic beta-AntagonistsQuantitative Structure-Activity RelationshipGeneral MedicineBiochemistryMicelleAcebutololMicellar electrokinetic chromatographyAnalytical ChemistryPartition coefficientchemistry.chemical_compoundMicellar liquid chromatographyOxprenololmedicineAlprenololSodium dodecyl sulfateMicellescirculatory and respiratory physiologymedicine.drugChromatography Liquid

description

Abstract Sixteen β-blocking agents (acebutolol, alprenolol, atenolol, bisoprolol, carteolol, celiprolol, esmolol, labetalol, metoprolol, nadolol, oxprenolol, pindolol, practolol, propranolol, sotalol and timolol) showing a large range of hydrophobicity (octanol–water partition coefficients, log P between −0.026 and 2.81) were subjected to micellar liquid chromatography with sodium dodecyl sulfate as micelle forming agent, and n-propanol as organic modifier. The correlation between log P and the retention factor extrapolated to a mobile phase free of micelles and organic modifier was investigated. The use of an interpolated retention factor or the retention factor for specific individual experimental mobile phases was however advantageous since the retention factors of all β-blocking agents were measurable in the selected mobile phases. Good correlations with log P and with in vitro biological parameters (cellular permeability coefficients in Caco-2 monolayers and apparent permeability coefficients in rat intestinal segments) were found.

10.1016/s0021-9673(01)00577-5https://pubmed.ncbi.nlm.nih.gov/11330791