Selective Preparation of Metastable Polymorphs Utilizing Inclusion Complexation with Cyclodextrins

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The selective crystallization of metastable forms and the control of crystal habits were conducted, utilizing inclusion complexations with cyclodextrins (CyDs). (1) Metastable forms of chlorpropamide were deposited from aqueous 2-hydroxy- butyl-β-CyD solutions, i.e. the metastable form II of the drug from lower CyD concentrations, whereas the most labile form III from higher CyD concentrations. (2) The crystal shape of aspirin was changed from plate to needle crystals, when the crystallizing solvent was changed from water to aqueous 2-hydroxybutyl-β-CyD solutions. The results indicate that 2-hydroxybutyl-β-CyD is useful for preparation of metastable forms and control of crystal habit of solid drugs.