Studies on stereoselective separations of the 'azole' antifungal drugs ketoconazole and itraconazole using HPLC and SFC on silica-based polysaccharides

Abstract

The resolution of ketoconazole and itraconazole enantiomers has been studied in HPLC and SFC on chiral stationary phases based upon substituted polysaccharides with different groups such as 3,5-dimethylphenylcarbamates and (R)-phenylethylcarbamate. The separations have been studied particularly in SFC (influence of pressure, temperature, as well as type and percentage of organic modifier). This study shows the advantages of SFC over HPLC for the enantiomeric separation of these antifungal agents.