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Optimization of three-component amorphous formulations with using co-amorphous system

Research Project

Project/Area Number 18K06610
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Review Section Basic Section 47020:Pharmaceutical analytical chemistry and physicochemistry-related
Research InstitutionAichi Gakuin University

Principal Investigator

Ozeki (Ogawa) Noriko  愛知学院大学, 薬学部, 准教授 (80409359)

Project Period (FY) 2018-04-01 – 2024-03-31
Project Status Completed (Fiscal Year 2023)
Budget Amount *help
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2020: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2019: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2018: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Keywords共非晶質 / 非晶質製剤 / 溶解性改善
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.

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。

Report

(7 results)
  • 2023 Annual Research Report   Final Research Report ( PDF )
  • 2022 Research-status Report
  • 2021 Research-status Report
  • 2020 Research-status Report
  • 2019 Research-status Report
  • 2018 Research-status Report
  • Research Products

    (13 results)

All 2024 2023 2022 2021 2020 2019 2018

All Journal Article (1 results) (of which Peer Reviewed: 1 results,  Open Access: 1 results) Presentation (12 results) (of which Int'l Joint Research: 3 results)

  • [Journal Article] Improved Dissolution Properties of Co-amorphous Probucol with Atorvastatin Calcium Trihydrate Prepared by Spray-Drying2024

    • Author(s)
      Oyama Shinji、Ogawa Noriko、Kawai Kaori、Iwai Kanako、Yasunaga Toshiya、Yamamoto Hiromitsu
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 72 Issue: 2 Pages: 190-199

    • DOI

      10.1248/cpb.c23-00673

    • ISSN
      0009-2363, 1347-5223
    • Year and Date
      2024-02-16
    • Related Report
      2023 Annual Research Report
    • Peer Reviewed / Open Access
  • [Presentation] プロブコールとスタチン類からなる共非晶質の調製と安定性評価2023

    • Author(s)
      大山晋司,小川法子,河合かおり,安永峻也,山本浩充
    • Organizer
      第48回 製剤・創剤セミナー
    • Related Report
      2023 Annual Research Report
  • [Presentation] ニフェジピンによるニモジピンの共非晶質化と三成分系固体分散体の調製2023

    • Author(s)
      草野真奈、小川法子、安永峻也、山本浩充
    • Organizer
      日本薬学会第143年会
    • Related Report
      2022 Research-status Report
  • [Presentation] Preparation and evaluation of three-component solid dispersion particles with using hydrophilic cyclodextrin derivative2022

    • Author(s)
      Noriko Ogawa, Ayumi Nishikata, Toshiya Yasunaga, Hiromitsu Yamamoto
    • Organizer
      International Conference on the Characterization and Control of Interfaces for High Quality Advanced Materials 2022 (ICCCI2022)
    • Related Report
      2022 Research-status Report
    • Int'l Joint Research
  • [Presentation] プロブコールとスタチン類からなる共非晶質の物性検討2022

    • Author(s)
      大山晋司、河合かおり、小川法子、安永峻也、山本浩充
    • Organizer
      第68回日本薬学会東海支部大会
    • Related Report
      2022 Research-status Report
  • [Presentation] プロブコールとスタチン類から成る共非晶質の設計2022

    • Author(s)
      大山晋司、河合かおり、小川法子、安永峻也、山本浩充
    • Organizer
      日本薬剤学会第37年会
    • Related Report
      2022 Research-status Report
  • [Presentation] Formulation design of three-component solid dispersion particles with using hydroxy propyl-beta-cyclodextrin and their drug release profiles2022

    • Author(s)
      Noriko Ogawa, Ayumi Nishikata, Kosuke Fujita, Ryohei Yasue, Toshiya Yasunaga, Hiromitsu Yamamoto
    • Organizer
      4th International Symposium on BA/BE of Oral Drug Products, 2022 (BABE2022)
    • Related Report
      2022 Research-status Report
    • Int'l Joint Research
  • [Presentation] プロブコールと共結晶/共非晶質を形成する添加物の探索2022

    • Author(s)
      大山 晋司、小川 法子、安永 峻也、山本 浩充
    • Organizer
      日本薬学会第142年会
    • Related Report
      2021 Research-status Report
  • [Presentation] Preparation of solid dispersion particles with using co-amorphous of probucol and atorvastatin2021

    • Author(s)
      Noriko Ogawa, Shinji Oyama, Kaori Kawai, Toshiya Yasunaga, Hiromitsu Yamamoto
    • Organizer
      8th Asian Particle Technology Symposium (APT2021)
    • Related Report
      2021 Research-status Report
    • Int'l Joint Research
  • [Presentation] アトルバスタチンとの共非晶質を利用したプロブコールの三成分系固体分散体の設計2021

    • Author(s)
      大山晋司、河合かおり、小川法子、安永峻也、山本浩充
    • Organizer
      日本病院薬剤師会東海ブロック・日本薬学会東海支部 合同学術大会2021
    • Related Report
      2021 Research-status Report
  • [Presentation] 共非晶質を利用したプロブコールの三成分系固体分散体の設計2020

    • Author(s)
      大山晋司, 小川法子, 安永峻也, 山本浩充
    • Organizer
      日本薬学会第140年会
    • Related Report
      2019 Research-status Report
  • [Presentation] 難溶性薬物の溶解性改善を目的とした三成分系固体分散体の設計2019

    • Author(s)
      小川法子, 大山晋司, 藤尾和紀, 藤田浩輔, 安永峻也, 山本浩充
    • Organizer
      粉体工学会 春期研究発表会
    • Related Report
      2019 Research-status Report
  • [Presentation] アミノ酸を添加した三成分系固体分散体の設計2018

    • Author(s)
      小川法子、藤尾和紀、藤田浩輔、安永峻也、山本浩充
    • Organizer
      日本薬学会第139年会
    • Related Report
      2018 Research-status Report

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Published: 2018-04-23   Modified: 2025-01-30  

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