Controls of Solution-mediated Polymorphic Transition and Crystal Growth Rate Utilizing Cyclodextrin Complexation

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The controls of solution-mediated polymorphic transition and crystal growth rate of drugs were conducted, utilizing inclusion complexations with cyclodextrins (CyDs). 1. A new polymorph of acetohexamide (Form VI) was prepared via the formation of a complex with 2-hydroxybutyl-b-cyclodextrin (HB-b-CyD) in aqueous solution. The new crystalline Form VI was highly soluble in water and physically and chemically stable, compared with other polymorphs (Forms I~V). 2. The crystal shape of aspirin was changed from plate to needle crystals, when the crystallizing solvent was changed from water to aqueous 2,6-dimethyl-b-CyD and 2-hydroxybutyl-b-CyD solutions. The results indicate that 2-hydroxybutyl-b-CyD is useful for preparation of metastable forms and control of crystal habit of solid drugs.