Separation of Drug Stereoisomers by the Formation of β-Cyclodextrin Inclusion Complexes

• DOI: 10.1126/science.3704640
• Publication Date: 2006-10-05T20:28:52Z
• Authors: Daniel W. Armstrong; Timothy J. Ward; R. Douglas Armstrong; Thomas E. Beesley
• Keywords: Diastereomer; Inclusion compound; Chiral resolution; Stereoisomerism

For many drugs, only racemic mixtures are available for clinical use. Because different stereoisomers of drugs often cause physiological responses, the use pure isomers could elicit more exact therapeutic effects. Differential complexation a variety drug by immobilized β-cyclodextrin was investigated. Chiral recognition and resolution were observed with number compounds from such clinically useful classes as β-blockers, calcium-channel blockers, sedative hypnotics, antihistamines, anticonvulsants, diuretics, synthetic opiates. Separation diastereomers cardioactive antimalarial cinchona alkaloids two antiestrogens demonstrated well. Three dimensional projections complexes propanolol, which is resolved this technique, warfarin, not, compared. These studies have improved understanding application chiral interactions β-cyclodextrin, they means to measure optical purity isolate or produce enantiomers drugs. In addition, highly specific technique also be used in pharmacological evaluation enantiomeric