Prominent Inhibitory Effect of 2-Hydroxybutyl-β-cyclodextrin on Solution-mediated Polymorphic Transition of Chlorpropamide

The effects of cyclodextrins on crystallization of chlorpropamide from aqueous solutions were investigated. Parent α-, β-, and γ-cyclodextrins and 2-hydroxypropyl-α-, and -β-cyclodextrins and glucose did not change the crystallization of the drug, providing the stable Form A crystal. On the other ha...

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Bibliographic Details
Published in:Chemistry letters Vol. 37; no. 8; pp. 816 - 817
Main Authors: Ishiguro, Takako, Hirayama, Fumitoshi, Iohara, Daisuke, Uekama, Kaneto
Format: Journal Article
Language:English
Published: The Chemical Society of Japan 05-08-2008
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Summary:The effects of cyclodextrins on crystallization of chlorpropamide from aqueous solutions were investigated. Parent α-, β-, and γ-cyclodextrins and 2-hydroxypropyl-α-, and -β-cyclodextrins and glucose did not change the crystallization of the drug, providing the stable Form A crystal. On the other hand, 2-hydroxybutyl-β-cyclodextrin inhibited the solution-mediated polymorphic transition of the drug, providing the metastable Form II at higher cyclodextrin concentrations and Form III at lower cyclodextrin concentrations. The results suggested that 2-hydoxybutyl-β-cyclodextrin is useful for preparing metastable crystals during crystallization according to the Ostwald rule.
ISSN:0366-7022
1348-0715
DOI:10.1246/cl.2008.816