Abstract
Several chiral stationary phases based on polysaccharide derivatives and proteins were evaluated for the resolution of some chiral drugs and their metabolites. The polysaccharide-based stationary phases CHIRALCEL OD-H, CHIRALCEL OB-H, CHIRALCEL OJ, CHIRALPAK AD and CHIRALPAK AS were evaluated under normal phase conditions, using hexane:2-propanol or hexane:ethanol as mobile phase. Diethylamine and trifluoracetic acid were also added to improve peak shape. The CHIRALCEL OJ-R, CHIRALCEL OD-R and CHIRALCEL OD-H columns were evaluated under reversed-phase conditions, using acetonitrile:H2O or acetonitrile:NaClO4 solution. The protein- based stationary phases, CHIRAL AGP and ULTRON ES-OVM columns were used with mobile phases consisting of a buffer solution supplemented with an organic modifier. Among the polysaccharide-based stationary phases, CHIRALPAK AD provided better resolution for almost all drugs and metabolites studied. The ULTRON ES-OVM column was particularly suitable for the resolution of the four enantiomers of thioridazine-2-sulfoxide.
Highlights
IntroductionOver the last two decades a large number of chiral stationary phases have been described in the literature and some of them are commercially available
Stereoselectivity in drug disposition and drug action is a well established issue and plays an important role in drug development both from the viewpoint of theVol 13, No 2, 2002 Enantiomeric Resolution of Drugs and Metabolites in Polysaccharide- and Protein-BasedOver the last two decades a large number of chiral stationary phases have been described in the literature and some of them are commercially available
The mobile phases used were different for which drug and type of stationary phase and were selected among the mobile phases that resulted in better resolution
Summary
Over the last two decades a large number of chiral stationary phases have been described in the literature and some of them are commercially available. Among them, those based on polysaccharides[4,5] and proteins[6] have broad application due to their stability, efficiency and high resolving ability. Polysaccharide phases are well suited for preparative scale enantiomeric separations.[7] Polysaccharide phases are prepared by coating cellulose or amylose derivatives (acetates, benzoates or carbamates) on a pretreated silica gel matrix and could be used under normal or reversed phase conditions. Differences in the higher-order structures among cellulose and amylose are responsible for differences in chiral discrimination.[8,9,10]
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
