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Polymorph control of pharmaceutical compounds

Research Project

Project/Area Number 15K14942
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Physical pharmacy
Research InstitutionOsaka University

Principal Investigator

YOSHIMURA MASASHI  大阪大学, レーザーエネルギー学研究センター, 教授 (60314382)

Co-Investigator(Kenkyū-buntansha) 高橋 晋  八戸工業大学, 大学院工学研究科, 准教授 (30337125)
Project Period (FY) 2015-04-01 – 2017-03-31
Project Status Completed (Fiscal Year 2016)
Budget Amount *help
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2016: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywords薬剤有機分子 / アセトアミノフェン / 準安定形選択晶出 / ソノクリスタリゼーション / ポリマー誘起核発生 / 溶液媒介相転移 / クラスター溶解制御 / レーザー誘起核発生
Outline of Final Research Achievements

We have developed an original method for selective crystallization of metastable phase acetaminophen form II by applied ultrasonic irradiation. In this research, we attempted to control the crystallinity in order to improve temporal stability of form II. We found that crystals of form II grown at low growth rate have high transparency and fewer defects. Powder X-ray diffraction measurement reveals that form II grown at low growth rate shows higher temporal stability than seed crystals nucleated by ultrasonic irradiation. We have also developed a new method of obtaining the metastable phase form II crystals of acetaminophen. Solution-mediated phase transformation (SMPT) from trihydrate into form II is utilized to obtain form II crystals. SMPT is triggered by seeding form II crystals into a saturated solution including trihydrate crystals, which are less stable than form II crystals.

Report

(3 results)
  • 2016 Annual Research Report   Final Research Report ( PDF )
  • 2015 Research-status Report
  • Research Products

    (17 results)

All 2017 2016 2015

All Journal Article (3 results) (of which Int'l Joint Research: 1 results,  Peer Reviewed: 3 results) Presentation (14 results) (of which Int'l Joint Research: 5 results)

  • [Journal Article] Crystallization of acetaminophen form II by plastic-ball-assisted ultrasonic irradiation2017

    • Author(s)
      Yo. Mori, M. Maruyama, Y. Takahashi, H. Y. Yoshikawa, S. Okada, H. Adachi, S. Sugiyama, K. Takano, S. Murakami, H. Matsumura, T. Inoue, M. Yoshimura, and Yu. Mori
    • Journal Title

      Applied Physics Express

      Volume: Vol.10, No.2 Issue: 2 Pages: 025501-025501

    • DOI

      10.7567/apex.10.025501

    • NAID

      210000135769

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Matastable crystal growth of acetaminophen using solution-mediated phase transformation2016

    • Author(s)
      Yo. Mori, M. Maruyama, Y. Takahashi, H. Y. Yoshikawa, S. Okada, H. Adachi, S. Sugiyama, K. Takano, S. Murakami, H. Matsumura, T. Inoue, M. Yoshimura, and Yu. Mori
    • Journal Title

      Applied Physics Express

      Volume: Vol.10, No.1 Issue: 1 Pages: 015501-015501

    • DOI

      10.7567/apex.10.015501

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Selective crystallization of metastable phase of acetaminophen by ultrasonic irradiation2015

    • Author(s)
      Y. Mori, M. Maruyama, Y. Takahashi, K. Ikeda, S. Fukukita, H. Y. Yoshikawa, S. Okada, H. Adachi, S. Sugiyama, K. Takano, S. Murakami, H. Matsumura, T. Inoue, M. Yoshimura, and Y. Mori
    • Journal Title

      Applied Physics Express

      Volume: Vol.8, No.6 Issue: 6 Pages: 065501-065501

    • DOI

      10.7567/apex.8.065501

    • NAID

      210000137563

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Int'l Joint Research
  • [Presentation] 溶液媒介相転移による医薬化合物アセトアミノフェンの準安定形成長(Ⅱ)2017

    • Author(s)
      藤本吏輝, 森陽一朗, 高橋義典, 丸山美帆子, 吉川洋史, 岡田詩乃, 安達宏昭, 杉山成, 高野和文, 村上聡, 松村浩由, 井上豪, 塚本勝男, 吉村政志, 森勇介
    • Organizer
      第64回応用物理学会春季学術講演会
    • Place of Presentation
      パシフィコ横浜, 神奈川
    • Year and Date
      2017-03-14
    • Related Report
      2016 Annual Research Report
  • [Presentation] Metastable crystal growth of acetaminophen using solvent-mediated phase transformation2016

    • Author(s)
      R. Fujimoto, Yo. Mori, Y. Takahashi, M. Maruyama, H. Yoshikawa, S. Okada, H. Adachi, S. Sugiyama, K. Takano, S. Murakami, H. Matsumura, T. Inoue, K. Tsukamoto, M. Yoshimura, and Yu. Mori
    • Organizer
      The 5th China-Japan Symposium on Crystal Growth and Crystal Technology
    • Place of Presentation
      Fuzhou, China
    • Year and Date
      2016-11-21
    • Related Report
      2016 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Metastable crystal growth of acetaminophen in low supersaturated solution2016

    • Author(s)
      K. Nii, M. Maruyama, Y. Takahashi, H. Yoshikawa, S. Okada, H. Adachi, S. Sugiyama, K. Takano, S. Murakami, H. Matsumura, T. Inoue, K. Tsukamoto, M. Yoshimura, and Yu. Mori
    • Organizer
      The 5th China-Japan Symposium on Crystal Growth and Crystal Technology
    • Place of Presentation
      Fuzhou, China
    • Year and Date
      2016-11-21
    • Related Report
      2016 Annual Research Report
    • Int'l Joint Research
  • [Presentation] 超音波結晶化法におけるアセトアミノフェンΙΙ形結晶の経時安定性向上2016

    • Author(s)
      藤原慎, 森陽一朗, 高橋義典, 丸山美帆子, 吉川洋史, 岡田詩乃, 安達宏昭, 杉山成, 高野和文, 村上聡, 松村浩由, 井上豪, 吉村政志, 森勇介
    • Organizer
      第77回応用物理学会秋季学術講演会
    • Place of Presentation
      朱鷲メッセ, 新潟
    • Year and Date
      2016-09-14
    • Related Report
      2016 Annual Research Report
  • [Presentation] 溶媒媒介相転移による医薬化合物アセトアミノフェンの準安定形成長2016

    • Author(s)
      藤本吏輝, 森陽一朗, 高橋義典, 丸山美帆子, 吉川洋史, 岡田詩乃, 安達宏昭, 杉山成, 高野和文, 村上聡, 松村浩由, 井上豪, 吉村政志, 森勇介
    • Organizer
      第77回応用物理学会秋季学術講演会
    • Place of Presentation
      朱鷲メッセ, 新潟
    • Year and Date
      2016-09-14
    • Related Report
      2016 Annual Research Report
  • [Presentation] 徐冷法を用いた医薬化合物アセトアミノフェンの準安定形成長2016

    • Author(s)
      仁井滉允, 森陽一郎, 高橋義典, 丸山美帆子, 吉川洋史, 岡田詩乃, 安達宏昭, 杉山成, 高野和文, 村上聡, 松村浩由, 井上豪, 塚本勝男, 吉村政志, 森勇介
    • Organizer
      第77回応用物理学会秋季学術講演会
    • Place of Presentation
      朱鷲メッセ, 新潟
    • Year and Date
      2016-09-14
    • Related Report
      2016 Annual Research Report
  • [Presentation] Growth of acetaminophen form Ⅱ by using solven-mediated phase transformation2016

    • Author(s)
      Yo. Mori, M. Maruyama, Y. Takahashi, H. Yoshikawa, S. Okada, H. Adachi, S. Sugiyama, K. Takano, S. Murakami, H. Matsumura, T. Inoue, K. Tsukamoto, M. Yoshimura, and Yu. Mori
    • Organizer
      The 18th International Conference on Crystal Growth and Epitaxy (ICCGE-18)
    • Place of Presentation
      Nagoya, Aichi
    • Year and Date
      2016-08-11
    • Related Report
      2016 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Temporal stability improvement of the metastable phase of acetaminophen using low supersaturated solution growth2016

    • Author(s)
      K. Nii, M. Maruyama, Y. Takahashi, H. Yoshikawa, S. Okada, H. Adachi, S. Sugiyama, K. Takano, S. Murakami, H. Matsumura, T. Inoue, K. Tsukamoto, M. Yoshimura, and Y. Mori
    • Organizer
      The 18th International Conference on Crystal Growth and Epitaxy (ICCGE-18)
    • Place of Presentation
      Nagoya, Aichi
    • Year and Date
      2016-08-09
    • Related Report
      2016 Annual Research Report
    • Int'l Joint Research
  • [Presentation] 溶媒媒介相転移を用いたアセトアミノフェンⅡ形の結晶化2016

    • Author(s)
      森陽一朗, 高橋義典, 丸山美帆子, 岡田詩乃, 安達宏昭, 吉村政志, 森勇介
    • Organizer
      日本薬剤学会第31年会
    • Place of Presentation
      長良川国際会議場, 岐阜
    • Year and Date
      2016-05-19
    • Related Report
      2016 Annual Research Report
  • [Presentation] 低過飽和育成によるアセトアミノフェンⅡ形結晶の経時安定性向上2016

    • Author(s)
      仁井滉允, 森陽一郎, 高橋義典, 丸山美帆子, 岡田詩乃, 安達宏昭, 吉村政志, 森勇介
    • Organizer
      日本薬剤学会第31年会
    • Place of Presentation
      長良川国際会議場, 岐阜
    • Year and Date
      2016-05-19
    • Related Report
      2016 Annual Research Report
  • [Presentation] 超音波結晶化法におけるアセトアミノフェンⅡ形結晶の経時安定性向上2016

    • Author(s)
      藤原慎, 森陽一朗, 高橋義典, 丸山美帆子, 岡田詩乃, 安達宏昭, 吉村政志, 森勇介
    • Organizer
      日本薬剤学会第31年会
    • Place of Presentation
      長良川国際会議場, 岐阜
    • Year and Date
      2016-05-19
    • Related Report
      2016 Annual Research Report
  • [Presentation] 超音波印加で得たアセトアミノフェンⅡ形の安定性に及ぼす過飽和度の影響2015

    • Author(s)
      福喜多俊, 丸山美帆子, 森陽一朗, 高橋義典, 吉川洋史, 岡田詩乃, 安達宏昭, 杉山成, 高野和文, 村上聡, 松村浩由, 井上豪, 吉村政志, 森勇介
    • Organizer
      第45回結晶成長国内会議(NCCG-45)
    • Place of Presentation
      北海道大学学術交流会館(北海道・札幌市)
    • Year and Date
      2015-10-19
    • Related Report
      2015 Research-status Report
  • [Presentation] 医薬化合物アセトアミノフェンの結晶多形制御2015

    • Author(s)
      森陽一朗, 丸山美帆子, 髙橋義典, 吉川洋史, 岡田詩乃, 安達宏昭, 杉山成, 高野和文, 村上聡, 松村浩由, 井上豪, 吉村政志, 森勇介
    • Organizer
      第39回結晶成長討論会
    • Place of Presentation
      同志社びわこリトリートセンター(滋賀県・大津市)
    • Year and Date
      2015-09-24
    • Related Report
      2015 Research-status Report
  • [Presentation] SELECTIVE CRYSTALLIZATION OF ACETAMINOPHEN POLYMORPH WITH HIGH SOLUBILITY2015

    • Author(s)
      Y. Mori, M. Maruyama, Y. Takahashi, H. Yoshikawa, S. Okada, H. Adachi, S. Sugiyama, K. Takano, S. Murakami, H. Matsumura, T. Inoue, M. Yoshimura, and Y. Mori
    • Organizer
      20th American Conference on Crystal Growth and Epitaxy (ACCGE-20)
    • Place of Presentation
      Big Sky Resort(Big Sky, Montana, USA)
    • Year and Date
      2015-08-03
    • Related Report
      2015 Research-status Report
    • Int'l Joint Research

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Published: 2015-04-16   Modified: 2018-03-22  

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