水溶液中におけるインドメタシンおよびその関連化合物とシクロデキストリンとの包接複合体形成

概要

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Inclusion complexations of indomethacin (ID) and its related compounds with three cyclodextrins (α-, β-, and γ-CyDs) in aqueous solution were studied by solubility method, spectroscopies ultraviolet (UV), circular dichroism (CD), and ^1H-nuclear magnetic resonance (^1H-NMR), and kinetic method. A spatial relationship between host and guest molecules as well as hydrophobic nature in guest molecules was clearly reflected in the magnitude of the UV and CD spectral changes and the stability constants of inclusion complexes. The chemical shift measurements in ^1H-NMR spectra suggested that the chlorobenzene ring moiety of the ID molecule was predominantly included in the cavity of CyDs and that the γ-CyD cavity might be preferable to include the bulky ID molecule. The hydrolysis rates of ID and its related compounds in alkaline solution were affected by three CyDs, depending upon the cavity size of CyDs. The effective deceleration observed by γ-CyD may be due to the inclusion of active amide moiety of ID molecule.
公益社団法人日本薬学会の論文
1982-12-25