| 論文名 |
Crystallization of a new polymorph of acetohexamide from 2-hydroxybutyl-β-cyclodextrin solution: form VI with a high aqueous solubility. |
| 著者 |
Hibah Aldawsari
Abdulmalik Altaf
Zainy M Banjar
Daisuke Iohara
Mami Nakabayashi
Makoto Anraku
Kaneto Uekama
Fumitoshi Hirayama
|
| キーワード |
|
| 出版年月 |
1970年1月 |
| 発表先 |
Int J Pharm. 2013 Sep 10;453(2):315-21. |
| WEBサイト |
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| 論文概要（和文） |
2-ヒドロキシブチル-β-シクロデキストリン溶液からのアセトヘキサミドの新しい多形の結晶化：高い水溶性を持つフォームVI。 |
| 論文概要（英文） |
A new polymorph of acetohexamide (Form VI) was prepared via the formation of a complex with 2-hydoxybutyl-β-cyclodextrin (HB-β-CD) in aqueous solution. An alkaline solution of acetohexamide and HB-β-CD was adjusted to pH 4.0 by titration with hydrochloric acid. The resulting opaque solution was filtered through paper and allowed to stand at 4°C for 24h. The resulting precipitate was isolated on a filter and analyzed for polymorph content by powder X-ray diffractometry and thermal analysis. The diffraction pattern and thermal behavior of the precipitate was different from those of previously reported acetohexamide polymorphs (Forms I, III, IV and V), indicating that a new polymorph of the drug, i.e. Form VI was produced. This new polymorph was fairly stable against conversion to a stable form even at accelerated storage conditions. Crystalline Form VI was highly soluble in water and dissolved more rapidly than the other known polymorphs. This property was reflected in the blood concentrations of the drug after oral administration to rats. |
