パラオキシ安息香酸エステルとα-およびβ-シクロデキストリンとの包接化合物形成 : 溶解挙動および抗微生物活性

概要

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Complex formations of 12 p-hydroxybenzoic acid esters (alkylparabens) with α- and β-cyclodextrins (α-CyD, β-CyD) were studied in water and in solid state by solubility method, IR spectroscopy, thermal analyses, and X-ray diffractometry. Solid complexes for alkylparabens with α- and β-CyDs were obtained and their molar ratios were found to be 1 : 2 (alkylparaben/α-CyD) and 1 : 1 (alkylparaben/β-CyD), respectively, except methylparaben-α-CyD complex (1 : 1). The dissolution rate of the complex in water was significantly higher than that of alkylparaben itself, depending upon the magnitude of the stability of the complex. Alkylparaben molecule included within CyD cavity appeared to be inactive and antimicrobial activity was directly related to the concentration of free alkylparaben in aqueous solution. Upon addition of CyDs, a significant increase in inhibitory-zone diameter was observed by cup-plate method, suggesting improved solubility and diffusibility of the preservatives by inclusion complexation.
社団法人日本薬学会の論文
1980-10-25