2023 Fiscal Year Final Research Report
Optimization of three-component amorphous formulations with using co-amorphous system
| Project/Area Number |
18K06610
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Review Section |
Basic Section 47020:Pharmaceutical analytical chemistry and physicochemistry-related
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| Research Institution | Aichi Gakuin University |
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Principal Investigator |
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| Project Period (FY) |
2018-04-01 – 2024-03-31
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| Keywords | 共非晶質 / 非晶質製剤 / 溶解性改善 |
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| Outline of Final Research Achievements |
Improvement of the dissolution rate and enhancement of the solubility of drugs is required to improve the bioavailability of poorly water-soluble drugs. We focused on co-amorphous formulations that contain a poorly soluble drug and a low molecular-weight compound to improve solubility and stability. In the present study, a co-amorphous model drug was prepared by spray-drying of probucol (PC) and atorvastatin calcium trihydrate salt (ATO) as lower water solubility and co-former components, respectively. The co-amorphization of PC and ATO prepared can be stored for 35 days without crystallization and improve the solubility of PC in water. Furthermore, we prepared three-component amorphous formulations with several kinds of poorly water-soluble model drugs and obtained useful knowledge about the relationship between formulations and solubility improvement of the drugs.
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| Free Research Field |
製剤学、物理化学
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| Academic Significance and Societal Importance of the Research Achievements |
本研究では、難溶性薬物モデルであるプロブコールにアトルバスタチンカルシウム三水和物を適用することで共非晶質を形成できることを明らかとし、さらにその物理化学的特性に関する知見を得ることができた。共非晶質中の薬物と添加薬の分子状態の解析結果は、共非晶質を形成する化合物の配合比率の最適化と結晶抑制メカニズムの解明をもたらす。また、処方と製剤特性の関係性の解明は、難溶性薬物のより効率的な製剤設計に貢献できる。さらに、水への溶解性が低いために十分な薬理作用が発揮できず上市に至っていない既存の医薬品の有効性の再発見につながり、医療の向上に寄与することができると考える。
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