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2013 Fiscal Year Final Research Report

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

Research Project

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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
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
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.

  • Research Products

    (16 results)

All 2013 2012 2011 Other

All Journal Article (10 results) (of which Peer Reviewed: 10 results) Presentation (4 results) (of which Invited: 2 results) Book (1 results) Remarks (1 results)

  • [Journal Article] Crystallization of A New Polymorph of Acetohexamide from 2-Hydroxybutyl-β-cyclodextrin So- lution : 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. Pharm

      Volume: 453 Pages: 315-321

    • DOI

      10.1016/j.ijpharm.2013.06.026

    • 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 Pages: 277-282

    • DOI

      10.1016/j.lfs.2013.06.021

    • 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

      Crystal Growth & Design

      Volume: 12 Pages: 1985-1991

    • DOI

      10.1021/cg201691c

    • Peer Reviewed
  • [Journal Article] Evaluation of Photodynamic Activity of C60/2-Hydroxypropyl-β-cyclo- dextrin Nanoparticles2012

    • Author(s)
      D. Iohara, M. Hiratsuka, F. Hirayama, K. Takeshita, K. Motoyama, H. Arima, K. Uekama
    • Journal Title

      J. Pharm. Sci

      Volume: 101 Pages: 3390-3397

    • DOI

      10.1002/jps.23045

    • 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 Pages: 302-304

    • DOI

      10.1016/j.carbpol.2012.03.014

    • Peer Reviewed
  • [Journal Article] Some Pharma- ceutical and Inclusion Properties of 2-Hydroxybutyl-β-cyclodextrin Derivative2011

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

      Int. J. Pharm

      Volume: 419 Pages: 161-169

    • DOI

      10.1016/j.ijpharm.2011.07.044

    • Peer Reviewed
  • [Journal Article] Improvement of Some Physico- chemical Properties of Arundic Acid, (R)-(-)-2-Propyloctanonic Acid, by Complexation with Hydrophilic Cyclo- dextrins2011

    • 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

      Int. J. Pharm

      Volume: 413 Pages: 63-72

    • DOI

      10.1016/j.ijpharm.2011.04.022

    • Peer Reviewed
  • [Journal Article] Reduction of Bitterness of Antihistaminic Drugs by Complexation withβ-Cyclodextrins2011

    • 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 Pages: 1935-1943

    • DOI

      10.1002/jps.22417

    • Peer Reviewed
  • [Journal Article] Formation of Stable Hydrophilic C60 Nanoparticles by 2-Hydroxypropyl-β-cyclodextrin2011

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

      Mol. Pharm

      Volume: 8 Pages: 1276-1284

    • DOI

      10.1021/mp200204v

    • 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 Pages: 71-76

    • DOI

      10.1016/j.ijpharm.2011.07.018

    • Peer Reviewed
  • [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
    • Year and Date
      20111210-11
  • [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
    • Year and Date
      20110908-09
  • [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
    • Year and Date
      20110720-21
    • 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
    • Year and Date
      20110529-31
    • Invited
  • [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(124-133)
    • Publisher
      シーエムシー出版
  • [Remarks]

    • URL

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

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Published: 2015-07-16  

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