ID JOS-acsomega.5c07202
著者：名前 著者：別形式 Ohtsu, Akiteru / Uchimura, Mione / Tomita, Junki / Ishida, Yoshiyuki / Nakata, Daisuke / Terao, Keiji / Inoue, Yutaka
著者：カナ 著者：所属 城西大学薬学部薬学科栄養治療学研究室 / 城西大学薬学部薬学科栄養治療学研究室 / 城西大学機器分析センター / 株式会社シクロケム / 株式会社シクロケム / 株式会社シクロケム / 城西大学薬学部薬学科栄養治療学研究室
著者：所属(別形式） Josai University, Faculty of Pharmacy and Pharmaceutical Sciences, Laboratory of Nutri-Pharmacotherapeutics Management / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences, Laboratory of Nutri-Pharmacotherapeutics Management / Josai University, Instrument Analysis Center / CycloChem Bio Co., Ltd. / CycloChem Bio Co., Ltd. / CycloChem Bio Co., Ltd. / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences, Laboratory of Nutri-Pharmacotherapeutics Management
著者版フラグ publisher
出版者 ACS Publications
電子ISSN 24701343
掲載誌名 巻 10
号 43
刊行年月 2025-10
開始ページ 51545
終了ページ 51558
コンテンツ作成日 2025-10-10
コンテンツ登録日 2025-12-02
識別番号：DOI info:doi/10.1021/acsomega.5c07202
識別番号：DOI（リンク） PubMed番号 41210774
抄録 In this study, stearyl glycyrrhetinate (SG), a poorly water-soluble derivative of glycyrrhetinic acid, was formulated into inclusion complexes with γ-cyclodextrin (γCD) and cyclodextrin-based metal–organic frameworks (CD-MOF-1) using the evaporation method (EVP) in the solid state. Powder X-ray diffraction and differential scanning calorimetry analyses confirmed the disappearance of SG’s crystalline and melting peaks, suggesting complexation and amorphization. Meanwhile, solid-state 13C CP/MAS NMR and near-infrared spectroscopy revealed chemical shift alternation and peak broadening in C–H and carbon signals. This demonstrates clear molecular interactions and differences in inclusion modes between the SG and the host materials. In solubility tests using fasted-state simulated intestinal fluid, EVP (SG/γCD = 1/2) and EVP (SG/CD-MOF-1 = 1/2) significantly increased in SG solubility by approximately 194-fold and 193-fold, respectively, compared with intact SG. Both complexes achieved rapid release from the early stages of testing. CD-MOF-1 showed unique dissolution behavior attributed to its rigid three-dimensional framework. These findings suggest that forming inclusion complexes with γCD or CD-MOF-1 can enhance the aqueous solubility and dissolution performance of SG, offering promising potential for the development of oral SG formulations.
キーワード 注記 Funding: This research was supported by Josai University. γ-Cyclodextrin was received from CycloChem Co., Ltd.; however, the company was not involved in the study design, collection, analysis, interpretation of data, writing of this article, or the decision to submit it for publication. The authors declare no competing financial interest.
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権利 Copyright: © 2025 The Authors. Published by American Chemical Society. This publication is licensed under CC-BY-NC-ND 4.0 .
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