Design of drug amorphous nanosuspension to achieve a pharmaceutical formulation of poorly water-soluble drug

2020 Fiscal Year Final Research Report

• Project/Area Number: 18K06592
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 47020:Pharmaceutical analytical chemistry and physicochemistry-related
• Research Institution: Chiba University
• Principal Investigator: Higashi Kenjirou 千葉大学, 大学院薬学研究院, 准教授 (40451760)
• Co-Investigator(Kenkyū-buntansha): 植田 圭祐 千葉大学, 大学院薬学研究院, 助教 (40755972) ; 森部 久仁一 千葉大学, 大学院薬学研究院, 教授 (50266350)
• Project Period (FY): 2018-04-01 – 2021-03-31
• Keywords: 非晶質ナノ粒子 / Cryo-TEM / suspended-state NMR / 溶解性改善 / 非晶質固体分散体 / 固液界面

Outline of Final Research Achievements

Amorphous nanoparticles attract much attentions as a method for dramatically improving the solubility of poorly water-soluble drugs. However, amorphous nanosuspensions are not easy to prepare and the analytical methods to evaluate their structure and molecular state has not been established. In this study, we succeeded in preparing three types of amorphous nanosuspensions using the anti-solvent method, the wet grinding method, and the amorphous solid dispersion. Furthermore, by applying the advanced microscopy and spectroscopy techniques, the structure and molecular state of the obtained amorphous nanosuspensions were evaluated, and the formation and stabilization mechanism was analyzed precisely.

Free Research Field

製剤学

Academic Significance and Societal Importance of the Research Achievements

近年開発されている医薬品候補化合物の70％～90％は難水溶性であり、溶解性を改善する製剤技術が切望されている。本研究で得られた知見は、溶解性改善手法として期待されている非晶質ナノ懸濁液の形成・安定化メカニズムに新しい知見を与えるものである。今後益々求められていく非晶質ナノ懸濁液製剤の開発において本研究が新しい指針となり、高品質の医薬品製剤の創生に役立つものと期待される。