Determination and Comparison of the Solubility, Oil–Water Partition Coefficient, Intestinal Absorption, and Biliary Excretion of Carvedilol Enantiomers

Carvedilol is administered as a racemic mixture for the therapy of hypertension and heart failure. S-enantiomer is the dominant conformation of pharmacodynamics, but its further development was obstructed by its poor bioavailability. In this study, carvedilol and its enantiomers were compared in terms of solubility, permeability, and biliary excretion, and reasons for the poor bioavailability were discussed. Equilibrium solubility and log P were...