ID | 64400 |
フルテキストURL | |
著者 |
Aikawa, Shohei
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Okayama University
Tanaka, Hironori
Formulation Research Department, Formulation R&D Laboratory, Shionogi & Co., Ltd.
Ueda, Hiroshi
Bioanalytical, Analysis and Evaluation Laboratory, Shionogi & Co., Ltd.
Maruyama, Masato
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Okayama University
Higaki, Kazutaka
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Okayama University
Kaken ID
publons
researchmap
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抄録 | Brick dust molecules are usually poorly soluble in water and lipoidal components, making it difficult to formulate them in dosage forms that provide efficient pharmacological effects. A co-amorphous system is an effective strategy to resolve these issues. However, their glass transition temperatures (Tg) are relatively lower than those of polymeric amorphous solid dispersions, suggesting the instability of the co-amorphous system. This study aimed to formulate a stable co-amorphous system for brick dust molecules by utilizing sodium taurocholate (NaTC) with a higher Tg. A novel neuropeptide Y-5 receptor antagonist (AntiY(5)R) and NaTC with Tg of 155 degrees C were used as the brick dust model and coformer, respectively. Ball milling formed a co-amorphous system for AntiY(5)R and NaTC (AntiY(5)R-NaTC) at various molar ratios. Deviation from the theoretical Tg value and peak shifts in Fourier-transform infrared spectroscopy indicated intermolecular interactions between AntiY(5)R and NaTC. AntiY(5)R-NaTC at equal molar ratios resulting in an 8.5-fold increase in AntiY(5)R solubility over its crystalline form. The co-amorphous system remained amorphous for 1 month at 25 degrees C and 40 degrees C. These results suggest that the co-amorphous system formed by utilizing NaTC as a coformer could stably maintain the amorphous state and enhance the solubility of brick dust molecules.
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キーワード | amorphous
co-amorphous
crystallization
sodium taurocholate
glass transition temperature
intermolecular interaction
dissolution testing
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発行日 | 2022-12-27
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出版物タイトル |
Pharmaceutics
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巻 | 15巻
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号 | 1号
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出版者 | MDPI
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開始ページ | 84
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ISSN | 1999-4923
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資料タイプ |
学術雑誌論文
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言語 |
英語
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OAI-PMH Set |
岡山大学
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著作権者 | © 2022 by the authors.
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論文のバージョン | publisher
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PubMed ID | |
DOI | |
Web of Science KeyUT | |
関連URL | isVersionOf https://doi.org/10.3390/pharmaceutics15010084
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ライセンス | https://creativecommons.org/licenses/by/4.0/
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