Evaluation of actarit/γ-cyclodextrin complex prepared by different methods
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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.
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
identifier:JOS-s10847-014-0445-z
identifier:http://link.springer.com/article/10.1007/s10847-014-0445-z/fulltext.html
収録刊行物
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- Journal of inclusion phenomena and macrocyclic chemistry
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Journal of inclusion phenomena and macrocyclic chemistry 81 (1-2), 161-168, 2015
Springer
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詳細情報 詳細情報について
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- CRID
- 1050001202786794624
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- NII論文ID
- 120005867444
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- NII書誌ID
- AA12422343
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- ISSN
- 13883127
- 15731111
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- 本文言語コード
- en
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- 資料種別
- journal article
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- データソース種別
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- IRDB
- CiNii Articles