ID | JOS-s10847-014-0445-z |
著者:名前 | |
著者:別形式 | Inoue, Yutaka / Watanabe, Shota / Suzuki, Rina / Murata, Isamu / Kanamoto, Ikuo |
著者:カナ | |
著者:所属 | 城西大学薬学部医薬品安全性学研究室 / 城西大学薬学部医薬品安全性学研究室 / 城西大学薬学部医薬品安全性学研究室 / 城西大学薬学部医薬品安全性学研究室 / 城西大学薬学部医薬品安全性学研究室 |
著者:所属(別形式) | Josai University, Faculty of Pharmaceutical Sciences, Laboratory of Drug Safety Management / Josai University, Faculty of Pharmaceutical Sciences, Laboratory of Drug Safety Management / Josai University, Faculty of Pharmaceutical Sciences, Laboratory of Drug Safety Management / Josai University, Faculty of Pharmaceutical Sciences, Laboratory of Drug Safety Management / Josai University, Faculty of Pharmaceutical Sciences, Laboratory of Drug Safety Management |
著者版フラグ | author |
出版地 | Netherlands |
出版者 | Springer |
NCID | AA12422343 |
冊子ISSN | 13883127 |
電子ISSN | 15731111 |
掲載誌名 | |
巻 | 81 |
号 | 1-2 |
刊行年月 | 2015 |
開始ページ | 161 |
終了ページ | 168 |
コンテンツ作成日 | 2014-06-10 |
コンテンツ修正日 | 2014-08-25 |
コンテンツ登録日 | 2016-11-16 |
識別番号:URI | |
識別番号:DOI | info:doi/10.1007/s10847-014-0445-z |
識別番号:DOI(リンク) | |
抄録 | This study used actarit (ACT), an antirheumatic drug, to examine the molecular interaction of ACT and γ-CD in a solid state as a result of cogrinding or freeze-drying and it assessed the dissolution of ACT. Differential scanning calorimetry revealed that coground ACT and γ-CD at molar ratios of 1:2 and 1:3 and freeze-dried ACT and γ-CD at molar ratios of 1:1 and 1:2 lacked an endothermic peak due to melting of ACT crystals. Thus, coground ACT and γ-CD at a molar ratio of 1:2 had molecular interaction, as did freeze-dried ACT and γ-CD at a molar ratio of 1:1. Powder x-ray diffraction revealed that coground and humidified ACT and γ-CD at a molar ratio of 1:2 produced a characteristic diffraction peak at 2θ = 15.2° and 16.5° due to the cage structure of γ-CD. In addition, freeze-dried ACT and γ-CD at a molar ratio of 1:1 that had been humidified produced a diffraction peak at 2θ = 6.0° and 15.9° characteristic of a hexagonal structure with head-to-head channels due to γ-CD. Assessment of dissolution revealed that ground mixtures (GMs) and freeze-dried mixtures had improved dissolution of ACT compared to ACT, ground ACT alone, and physical mixtures. The mechanism for this is presumably the result of molecular interaction in a solid state or molecular interaction in an aqueous solution. 1H–1H NOESY NMR spectra suggested that in a GM of ACT and γ-CD the benzene ring and methyl group of ACT partially enter the CD cavity. In addition, spectra for freeze-dried ACT and γ-CD suggested that protons of the methylene group of ACT and the benzene ring of ACT partially enter the CD cavity. These findings indicate that ACT and γ-CD inclusion complexes feature different forms of inclusion depending on how they are prepared, e.g., cogrinding or freeze-drying. Findings also indicated that selection of a method of preparation may play a major role in drug development. |
キーワード | |
注記 | This is a post-peer-review, pre-copyedit version of an article published in Journal of Inclusion Phenomena and Macrocyclic Chemistry. The final authenticated version is available online at: http://dx.doi.org/10.1007/s10847-014-0445-z |
言語 | eng |
資源タイプ | text |
ジャンル | |
フォーマット | application/pdf |
このアイテムを表示する:本文(pdf) | ( 881.8KB) ダウンロード回数: 回 |
このアイテムを表示する:URI | |