Quantitative structure-retention and retention-activity relationships of beta-blocking agents by micellar liquid chromatography.
Sixteen beta-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 beta-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.
Detroyer
A
A
Department of Pharmaceutical and Biomedical Analysis, Pharmaceutical Institute, Vrije Universiteit Brussel, Belgium.
Vander Heyden
Y
Y
Carda-Broch
S
S
García-Alvarez-Coque
M C
MC
Massart
D L
DL
D000319:Adrenergic beta-Antagonists / Q000737:chemistry*; D002853:Chromatography, Liquid / Q000379:methods*; D008823:Micelles; D021281:Quantitative Structure-Activity Relationship
D000319:Adrenergic beta-Antagonists; D008823:Micelles