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Controls of Solution-mediated Polymorphic Transition and Crystal Growth Rate Utilizing Cyclodextrin Complexation

Research Project

Project/Area Number 23590063
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Physical pharmacy
Research InstitutionSojo University

Principal Investigator

HIRAYAMA Fumitoshi  崇城大学, 薬学部, 教授 (90094036)

Co-Investigator(Kenkyū-buntansha) IOHARA Daisuke  崇城大学, 薬学部, 助教 (40454954)
Project Period (FY) 2011 – 2013
Project Status Completed (Fiscal Year 2013)
Budget Amount *help
¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2013: ¥390,000 (Direct Cost: ¥300,000、Indirect Cost: ¥90,000)
Fiscal Year 2012: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2011: ¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Keywordsシクロデキストリン / アセトヘキサミド / アスピリン / 新規結晶多形 / 晶癖 / 溶液媒介性多形転移 / 結晶成長速度 / 包接複合体 / 結晶多形 / 米国
Research Abstract

The controls of solution-mediated polymorphic transition and crystal growth rate of drugs were conducted, utilizing inclusion complexations with cyclodextrins (CyDs). 1. A new polymorph of acetohexamide (Form VI) was prepared via the formation of a complex with 2-hydroxybutyl-b-cyclodextrin (HB-b-CyD) in aqueous solution. The new crystalline Form VI was highly soluble in water and physically and chemically stable, compared with other polymorphs (Forms I~V). 2. The crystal shape of aspirin was changed from plate to needle crystals, when the crystallizing solvent was changed from water to aqueous 2,6-dimethyl-b-CyD and 2-hydroxybutyl-b-CyD solutions. The results indicate that 2-hydroxybutyl-b-CyD is useful for preparation of metastable forms and control of crystal habit of solid drugs.

Report

(4 results)
  • 2013 Annual Research Report   Final Research Report ( PDF )
  • 2012 Research-status Report
  • 2011 Research-status Report
  • Research Products

    (26 results)

All 2013 2012 2011 Other

All Journal Article (14 results) (of which Peer Reviewed: 14 results) Presentation (9 results) (of which Invited: 2 results) Book (2 results) Remarks (1 results)

  • [Journal Article] Crystallization of A New Polymorph of Acetohexamide from 2-Hydroxybutyl-b- cyclodextrin Solution: Form VI with High Aqueous Solubility2013

    • Author(s)
      H. Aldawsari, A. Altaf, Z.M. Banjar, D. Iohara, M. Nakabayashi, M. Anraku, K. Uekama and F. Hirayama
    • Journal Title

      Int. J. Pharm.

      Volume: 453 Issue: 2 Pages: 315-321

    • DOI

      10.1016/j.ijpharm.2013.06.026

    • Related Report
      2013 Annual Research Report 2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Preparation of Soluble Stable C60/Human Serum Albumin Nanoparticles via Cyclodextrin Complexation and Their Reactive Oxygen Production Characteristics2013

    • Author(s)
      A. Altaf, H. Aldawsari, Z.M. Banjar, M. Anraku, D. Iohara, M. Otagiri, K. Uekama, F. Hirayama
    • Journal Title

      Life Sci

      Volume: 93 Issue: 7 Pages: 277-282

    • DOI

      10.1016/j.lfs.2013.06.021

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Preparation of Soluble Stable C60/Human Serum Albumin Nanoparticles via Cyclodextrin Complexation and Their Reactive Oxygen Production Characteristics2013

    • Author(s)
      A. Altaf, H. Aldawsari, Z.M. Banjar, M. Anraku, D. Iohara, M. Otagiri, K. Uekama and F. Hirayama
    • Journal Title

      Life Sci.

      Volume: 93 Pages: 277-282

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Antioxidant and Renoprotective Activity of Chitosan in Nephrectomizded Rat2013

    • Author(s)
      A. Hiraga, M. Anraku, D. Iohara, K. Uekama, M.Otagiri, F. Hirayama
    • Journal Title

      Chtin and Chitosan Research

      Volume: 19 Pages: 24-27

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Crystallization of A New Polymorph of Acetohexamide from 2-Hydroxybutyl-b-cyclodextrin Solution: Form VI with High Aqueous Solubility2013

    • Author(s)
      H. Aldawsari, A. Altaf, Z.M. Banjar, D. Iohara, M. Nakabayashi, M. Anraku, K. Uekama, F. Hirayama
    • Journal Title

      Int. J. Pham.

      Volume: in press

    • Related Report
      2012 Research-status Report
    • Peer Reviewed
  • [Journal Article] Cyclodextrin-induced change in crystal habit of acetylsalicylic acid in aqueous solution2012

    • Author(s)
      D. Iohara, K. Yoshida, K. Yamaguchi, M. Anraku, K. Motoyama, H. Arima, K. Uekama, F.Hirayama
    • Journal Title

      Cryst. Growth Des.

      Volume: 12 Issue: 4 Pages: 1985-1991

    • DOI

      10.1021/cg201691c

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Evaluation of photodynamic activity ofC/2-hydroxypropyl-β-cyclodextrinNanoparticles.2012

    • Author(s)
      Daisuke Iohara, Masaaki Hiratsuka,Fumitoshi Hirayama, Keizo Takeshita, KeiichiMotoyama, Hidetoshi Arima, Kaneto Uekama;
    • Journal Title

      J. Pharm. Sci.

      Volume: 101(9) Issue: 9 Pages: 3390-3397

    • DOI

      10.1002/jps.23045

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Antioxidant and Renoprotec- tive Activity of Chitosan in Nephrecto- mized Rats2012

    • Author(s)
      M. Anraku, H. Tomida, A. Michihara, A. Tsuchiya, D. Iohara, Y. Maezaki, K. Uekama, T. Maruyama, M. Otagiri, F. 2 Hirayama
    • Journal Title

      Carbohydr. Polymers

      Volume: 89 Issue: 1 Pages: 302-304

    • DOI

      10.1016/j.carbpol.2012.03.014

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Cyclodextrin-induced Change in Crystal Habit of Acetylsalicylic Acid in Aqueous Solution2012

    • Author(s)
      D. Iohara, K. Yoshida, K. Yamaguchi, M. Anraku, K. Motoyama, H. Arima, K. Uekama and F. Hirayama
    • Journal Title

      Crystal Growth & Design

      Volume: 12 Pages: 1985-1991

    • Related Report
      2011 Research-status Report
    • Peer Reviewed
  • [Journal Article] Some pharmaceutical and inclusion properties of 2-hydroxybutyl-β-cyclodextrin derivative2011

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

      J. Pharm.

      Volume: 419 Issue: 1-2 Pages: 161-169

    • DOI

      10.1016/j.ijpharm.2011.07.044

    • Related Report
      2013 Final Research Report 2011 Research-status Report
    • Peer Reviewed
  • [Journal Article] Improvement of Some Physicochemical Properties of Arundic Acid, (R)-(-)-2-Propyloctanonic Acid, by Complexation with Hydrophilic Cyclodextrins2011

    • Author(s)
      Y.Miyamoto, M.Nakahara, K.Motoyama, T.Ishiguro, Y.Oda, T.Yamanoi, I.Okamoto, A.Yagi, H.Nishimura, F.Hirayama, K.Uekama, H.Arima
    • Journal Title

      International Journal of Pharmaceutics

      Volume: 413 Issue: 1-2 Pages: 63-71

    • DOI

      10.1016/j.ijpharm.2011.04.022

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Reduction of bitterness of antihistaminic drugs by com-plexation with β-cyclodextrin2011

    • Author(s)
      N. Ono, Y. Miyamoto, T. Ishiguro, K.Motoyama, F. Hirayama, D. Iohara, H. Seo, S.Tsuruta, H. Arima, K. Uekama
    • Journal Title

      J. Pharm. Sci.

      Volume: 100 Issue: 5 Pages: 1935-1943

    • DOI

      10.1002/jps.22417

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Formation of Stable Hydrophilic C_<60> Nanoparticles by Hdroxypropyl-β-cyclodextrin2011

    • Author(s)
      D.Iohara, F.Hirayama, K.Higashi, K.Yamamoto, K.Uekama
    • Journal Title

      Molecular Pharmaceutics

      Volume: 8 Issue: 4 Pages: 1276-1284

    • DOI

      10.1021/mp200204v

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Effect of Sulfobutyl ether-β-cyclodextrin on Bio- availability of Insulin Glargine and Blood Glucose Level after Subcuta- neous Injection to Rats2011

    • Author(s)
      K. Uehata, T. Anno, K. Hayashida, K. Motoyama, F. Hirayama, N. Ono, J.D. Pipkin, K. Uekama, H. Arima
    • Journal Title

      Int. J. Pharm

      Volume: 419 Issue: 1-2 Pages: 71-76

    • DOI

      10.1016/j.ijpharm.2011.07.018

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Presentation] Cyclodextrin/Sangelose系の解離平衡に基づく温度感受性sol-gel変換システムの徐放性点眼剤への応用2013

    • Author(s)
      大久保尚徳、庵原大輔、安楽誠、平山文俊、上釜兼人
    • Organizer
      第30回シクロデキストリンシンポジウム
    • Place of Presentation
      くまもと県民交流館パレア(熊本県熊本市)
    • Related Report
      2013 Annual Research Report
  • [Presentation] 親水性シクロデキストリン/水酸化フラーレンナノ粒子の調製と抗酸化能評価2013

    • Author(s)
      梅崎至高、庵原大輔、安楽誠、上釜兼人、平山文俊
    • Organizer
      第30回シクロデキストリンシンポジウム
    • Place of Presentation
      くまもと県民交流館パレア(熊本県熊本市)
    • Related Report
      2013 Annual Research Report
  • [Presentation] 慢性腎不全モデルラットにおける2-ヒドロキシプロピル-b-シクロデキストリンの抗酸化および腎保護効果の検討2013

    • Author(s)
      石田裕太郎、梅崎至高、和田幸樹、庵原大輔、安楽誠、小田切優樹、上釜兼人、平山文俊
    • Organizer
      第30回シクロデキストリンシンポジウム
    • Place of Presentation
      くまもと県民交流館パレア(熊本県熊本市)
    • Related Report
      2013 Annual Research Report
  • [Presentation] 2-ヒドロキシブチル-β-シクロデキストリンを用いたアセトヘキサミド新規結晶多形の調製2011

    • Author(s)
      中林磨実、庵原大輔、安楽誠、上釜兼人、平山文俊
    • Organizer
      第28回日本薬学会九州支部大会
    • Place of Presentation
      福岡大学薬学部、福岡
    • Related Report
      2013 Final Research Report
  • [Presentation] アセトヘキサミドの結晶化に及ぼす2-ヒドロキシブチル-β-シクロデキストリンの影響2011

    • Author(s)
      中林磨実、庵原大輔、平山文俊、上釜兼人、安楽誠
    • Organizer
      第28回シクロデキストリンジンポジウム
    • Place of Presentation
      秋田ビューホテル、秋田
    • Related Report
      2013 Final Research Report
  • [Presentation] シクロデキストリンによる薬物の結晶化および晶癖の制御2011

    • Author(s)
      平山文俊
    • Organizer
      第36回製剤セミナー
    • Place of Presentation
      ヤマハリゾートつま恋、静岡
    • Related Report
      2013 Final Research Report
    • Invited
  • [Presentation] シクロデキストリンによる薬物の結晶多形転移の制御2011

    • Author(s)
      平山文俊
    • Organizer
      日本薬剤学会第26年会
    • Place of Presentation
      タワーホール船橋、埼玉
    • Related Report
      2013 Final Research Report
    • Invited
  • [Presentation] シクロデキストリンによる薬物の結晶多形転移の制御2011

    • Author(s)
      平山文俊
    • Organizer
      日本薬剤学会第26年会(招待講演)
    • Place of Presentation
      タワーホール船橋(東京)
    • Related Report
      2011 Research-status Report
  • [Presentation] シクロデキストリンによる薬物の結晶化および晶癖の制御2011

    • Author(s)
      平山文俊
    • Organizer
      第36回製剤セミナー(招待講演)
    • Place of Presentation
      ヤマハリゾートつま恋(静岡)
    • Related Report
      2011 Research-status Report
  • [Book] 各種薬物の製剤特性改善におけるシクロデキストリンの有用性.in"シクロデキストリンの科学と技術"2013

    • Author(s)
      上釜兼人、平山文俊、安楽誠、庵原大輔
    • Total Pages
      314
    • Publisher
      シーエムシー出版
    • Related Report
      2013 Final Research Report
  • [Book] 各種薬物の製剤特性改善におけるシクロデキストリンの有用性 in “シクロデキストリンの科学と技術”2013

    • Author(s)
      上釜兼人、平山文俊、安楽誠、庵原大輔
    • Publisher
      シーエムシー出版
    • Related Report
      2013 Annual Research Report
  • [Remarks]

    • URL

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

    • Related Report
      2013 Final Research Report

URL: 

Published: 2011-08-05   Modified: 2019-07-29  

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