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Potential Use of Cyclodextrins in the Development of Patient-Friendly Super-Generic Preparations

Research Project

Project/Area Number 19590169
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Medical pharmacy
Research InstitutionSojo University

Principal Investigator

UEKAMA Kaneto  Sojo University, 薬学部, 教授 (90040328)

Co-Investigator(Kenkyū-buntansha) HIRAYAMA Fumitoshi  崇城大学, 薬学部, 教授 (90094036)
MATSUKURA Makoto  崇城大学, 薬学部, 教授 (70238997)
SEO Hakaru  崇城大学, 薬学部, 教授 (20435142)
TSURUTA Satoshi  崇城大学, 薬学部, 教授 (50412739)
Project Period (FY) 2007 – 2008
Project Status Completed (Fiscal Year 2008)
Budget Amount *help
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2008: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2007: ¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Keywords親水性シクロデキストリン / 包接複合体 / フラーレンC60 / ナノ粒子 / PEG化インスリン / Polypseudorotaxane / 放出制御 / 結晶形態の制御 / スーパージェネリック製剤 / ナノ粒子化 / 抗酸化物質 / ナノ粒子形成 / バイオアベイラビリティ改善 / 標的指向化 / 製剤設計
Research Abstract

生体適合性に優れる各種シクロデキストリン(CyDs)を用いてスーパージェネリック製剤の開発を企図した基礎研究を実施し、以下の知見を得た。(1)HP-β-CyDを用いて抗酸化物質フラーレン(C60)のナノ粒子粉末の調製法と凝集安定性に優れる懸濁製剤の処方を構築した。(2)コエンザイムQ10/γ-CyD 系ではpseudorataxane 様の超分子複合体を形成し、親水軟膏からの CoQ10 放出が有意に増大した。(3)γ-CyD を用いてPEG化インスリンの製剤特性(安定性、バイオアベイラビリティ、徐放出など)を改善し、蛋白質性薬物の高品位化の新手法を開発した。(4)両親媒性 β-CyDsを用いてインドメタシンの非晶質化やアスピリンの晶癖を制御すると、製剤の品質向上が可能なことを明らかにした。

Report

(3 results)
  • 2008 Annual Research Report   Final Research Report ( PDF )
  • 2007 Annual Research Report
  • Research Products

    (27 results)

All 2009 2008 2007 Other

All Journal Article (12 results) (of which Peer Reviewed: 12 results) Presentation (7 results) Book (6 results) Remarks (2 results)

  • [Journal Article] Slow Release System of Randomly-Pegylated Insulin by Polypseudorotaxane Formation with Cyclodextrins2009

    • Author(s)
      T. Higashi, F. Hirayama, S. Misumi, K. Motoyama, H. Arima, K. Uekama
    • Journal Title

      Chem. Pharm. Bull 56

      Pages: 541-544

    • Related Report
      2008 Final Research Report
    • Peer Reviewed
  • [Journal Article] Design and Evaluation of Polypseudorotaxanes of Pegylated Insulin with Cyclodextrins as Sustained Release System2008

    • Author(s)
      T. Higashi, F. Hirayama, S. Misumi, H. Arima, K. Uekama
    • Journal Title

      Biomaterials 29

      Pages: 3866-3871

    • Related Report
      2008 Final Research Report
    • Peer Reviewed
  • [Journal Article] Pseudorotaxane-like Supramolecular Complex of Coenzyme Q10 with γ-Cyclodextrin Formed by Solubility Method2008

    • Author(s)
      K. Nishimura, T. Higashi, A. Yoshimatsu, F. Hirayama, K. Uekama, H. Arima
    • Journal Title

      Chem. Pharm. Bull 56

      Pages: 701-706

    • NAID

      110006663996

    • Related Report
      2008 Final Research Report
    • Peer Reviewed
  • [Journal Article] Prominent Inhibitory Effect of 2-Hydroxybutyl-β-cyclodextrin on Solution-mediated Polymorphic Transition of Chlorpropamide2008

    • Author(s)
      T. Ishiguro, F. Hirayama, D. Iohara, K. Uekama
    • Journal Title

      Chem. Lett 37

      Pages: 816-817

    • NAID

      10024281162

    • Related Report
      2008 Final Research Report
    • Peer Reviewed
  • [Journal Article] Preparation of Amorphous Indomethacin from Aqueous 6-Di-O-methyl-β-cyclodextrin Solution2008

    • Author(s)
      D. Iohara, F. Hirayama, T. Ishiguro, H. Arima, K., Uekama
    • Journal Title

      Int.J.Pharmaceut 354

      Pages: 70-76

    • Related Report
      2008 Final Research Report
    • Peer Reviewed
  • [Journal Article] Improved Stability of OPALMONR Tablets under HumidConditions IV :Formulation Development Study2008

    • Author(s)
      N. Sekiya, A. Nishiwaki, A. Nishiura, M. Yamamoto, K. Takeda, D. Iohara, F. Hirayama, H. Arima, K. Uekama
    • Journal Title

      Chem. Pharm. Bull 56

      Pages: 7-11

    • Related Report
      2008 Final Research Report
    • Peer Reviewed
  • [Journal Article] Pseudorotaxane-like Supramolecular Complex of Coenzyme Q10 with γ-Cyclodextrin Formed by Solubility Method2008

    • Author(s)
      K. Nishimura, T. Higashi, A. Yoshimatsu, F. Hirayama, K. Uekama, H. Arima
    • Journal Title

      Chem. Pharm. Bull. 56

      Pages: 7-11

    • NAID

      110006663996

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Prominent Inhibitory Effect of 2-Hydroxybutyl-β-cyclodextrin on Solution-mediated Polymorphic Transition of Chlorpropamide2008

    • Author(s)
      T. Ishiguro, F. Hirayama, D. Iohara, K. Uekama
    • Journal Title

      Chem. Lett. 37

      Pages: 816-817

    • NAID

      10024281162

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Design and Evaluation of Polypseudorotaxanes of Pegylated Insulin with Cyclodextrins as Sustained Releas System.2008

    • Author(s)
      T. Higashi, F. Hirayama, S. Misumi, H. Arima, K. Uekama
    • Journal Title

      Biomaterials 29

      Pages: 3866-3871

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Improved Stability of OPALMON[○!R] Tablets under Humid Conditions IV:Formulation Development Study2008

    • Author(s)
      N.Sekiya, A.Nishiwaki, A.Nishiura, M.Yamamoto, K.Takeda, D.Iohara, F.Hirayama, H.Anima, K.Uekama
    • Journal Title

      Chem, Pharm. Bull 56

      Pages: 7-11

    • Related Report
      2007 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Preparation of Amorphous Indomethacin from Aqueous 2,6-di-O-methyl-β-cyclodextrin Solution2008

    • Author(s)
      D.Iohara, F.Hirayama, T.Ishiguro, H.Arima, K.Uekama
    • Journal Title

      Int.J.Pharm. 354

      Pages: 70-76

    • Related Report
      2007 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Pseudorotaxane-like Supramolecular Complex of Coenzyme Q_<10> with γ-Cyclodextrin Formed by Solubility Method2008

    • Author(s)
      K.Nishimura, T.Higashi, A.Yoshimatsu, F.Hirayama, K.Uekama, H.Arima
    • Journal Title

      Chem.Pharm.Bull 56

    • Related Report
      2007 Annual Research Report
    • Peer Reviewed
  • [Presentation] シクロデキストリン誘導体を用いたアスピリンの面選択的な結晶成長制御2009

    • Author(s)
      吉田賢史, 平山文俊, 庵原大輔, 山口幸樹, 吉武康之, 原野一誠, 本山敬一 有馬英俊, 上釜兼人
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      京都
    • Related Report
      2008 Final Research Report
  • [Presentation] Preparation of Water-Soluble C60 Nanoparticles by Co-grinding with Hydrophilic Cyclodextrin Derivatives2008

    • Author(s)
      D. Iohara, F. Hirayama, K. Uekama
    • Organizer
      2008 American Association of Pharmaceutical Scientists Annual Meeting and Exposition
    • Place of Presentation
      Atlanta, U.S.A.
    • Year and Date
      2008-11-19
    • Related Report
      2008 Annual Research Report
  • [Presentation] Preparation of Water-Soluble C60 Nanoparticles by Co-grinding with Hydrophilic Cyclodextrin Derivatives2008

    • Author(s)
      D. Iohara, F. Hirayama, K. Uekama
    • Organizer
      2008 American Association of Pharmaceutical Scientists Annual Meeting and Exposition
    • Place of Presentation
      Atlanta, U.S.A
    • Related Report
      2008 Final Research Report
  • [Presentation] ジメチル-β-シクロデキストリンを利用した水溶液からの非晶質性インドメタシンの調製とその溶解挙動2008

    • Author(s)
      庵原大輔, 平山文俊, 上釜兼人
    • Organizer
      日本薬剤学会第23年会
    • Place of Presentation
      札幌
    • Related Report
      2008 Final Research Report
  • [Presentation] Change in Crystal Habit of Aspirin by the Addition of Cyclodextrins in Aqueous Solution2008

    • Author(s)
      K. Yoshida, F. Hirayama, D. Iohara, K. Yamaguchi, Y. Yoshitake, K. Harano, H.Arima, K. Uekama
    • Organizer
      14th International Cyclodextirn Symposium
    • Place of Presentation
      Kyoto
    • Related Report
      2008 Final Research Report
  • [Presentation] Effects of 2-Hydroxybutyl-β-cyclodextrin on Solution-mediated Transformation of Chlorpropamide2008

    • Author(s)
      T. Ishiguro, F. Hirayama, D. Iohara, K. Uekama
    • Organizer
      14th International Cyclodextirn Symposium
    • Place of Presentation
      Kyoto
    • Related Report
      2008 Final Research Report
  • [Presentation] Effects of β-Cyclodextrin Derivatives on Polymorphic Transition and Crystal Habit of Typical NSAIDs,Indomethacin and Aspirin2007

    • Author(s)
      D.Iohara, F.Hirayama, K.Uekama
    • Organizer
      4th Asian Cyclodextrin Conference
    • Place of Presentation
      京都
    • Year and Date
      2007-05-19
    • Related Report
      2007 Annual Research Report
  • [Book] The Practice of Medicinal Chemistry2008

    • Author(s)
      K. Uekama and F. Hirayama
    • Publisher
      C.G. Wermuth, AcademicPress
    • Related Report
      2008 Final Research Report
  • [Book] シクロデキストリンの応用技術-Drug Delivery System-2008

    • Author(s)
      上釜兼人. 小宮山 真,寺尾啓二(編)
    • Publisher
      シーエムシー出版
    • Related Report
      2008 Final Research Report
  • [Book] Improvement of Drug Properties by Cyclodextrills., in "The Practice of Medicinal Chemistry (3rd Edition)"2008

    • Author(s)
      K. Uekama, F. Hirayama
    • Total Pages
      23
    • Publisher
      Academic Press, London
    • Related Report
      2008 Annual Research Report
  • [Book] シクロデキストリンの応用技術2008

    • Author(s)
      上釜 兼人
    • Total Pages
      329
    • Publisher
      シーエムシー出版(東京)
    • Related Report
      2007 Annual Research Report
  • [Book] Biotechnology: Pharmaceutical Aspect2007

    • Author(s)
      F. Hirayama and K. Uekama
    • Publisher
      AAPS Press
    • Related Report
      2008 Final Research Report
  • [Book] Prodrugs:Vhallenges and Rewards(Part 1)2007

    • Author(s)
      F.Hirayama and K.Uekama
    • Total Pages
      734
    • Publisher
      AAPS Press,New York
    • Related Report
      2007 Annual Research Report
  • [Remarks]

    • URL

      http://www.pharm.ph.sojo-u.ac.jp/~dio

    • Related Report
      2008 Final Research Report
  • [Remarks]

    • URL

      http://www.pharm.ph.sojo~u.ac.jp/~dio/

    • Related Report
      2008 Annual Research Report

URL: 

Published: 2007-04-01   Modified: 2016-04-21  

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