NDLI: Evaluation of actarit/γ-cyclodextrin complex prepared by different methods

Content Provider	Springer Nature Link
Author	Iue, Yutaka Watanabe, Shota Suzuki, Rina Murata, Isamu Kanamoto, Ikuo
Copyright Year	2014
Abstract	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. $^{1}$H–$^{1}$H 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.
Starting Page	161
Ending Page	168
Page Count	8
File Format	PDF
ISSN	13883127
Journal	Journal of Inclusion Phenomena and Macrocyclic Chemistry
Volume Number	81
Issue Number	1-2
e-ISSN	15731111
Language	English
Publisher	Springer Netherlands
Publisher Date	2014-09-07
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Molecular interaction Ground mixture Freeze dried γ-Cyclodextrin Actarit Organic Chemistry Food Science Crystallography
Content Type	Text
Resource Type	Article
Subject	Chemistry Condensed Matter Physics Food Science

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