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Nano-composite formation for various pharmaceutical formulations.

Research Project

Project/Area Number 22790041
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeSingle-year Grants
Research Field Physical pharmacy
Research InstitutionOsaka University of Pharmaceutical Sciences (2012)
Gifu Pharmaceutical University (2010-2011)

Principal Investigator

TOZUKA Yuichi  大阪薬科大学, 薬学部, 教授 (50312963)

Project Period (FY) 2010 – 2012
Project Status Completed (Fiscal Year 2012)
Budget Amount *help
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2012: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2011: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2010: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Keywords製剤学 / ナノコンポジット / 機能性添加剤 / 糖転移ルチン / 溶解性改善 / 吸収性改善 / 糖転移化合物 / ナノ集合体 / 難水溶性薬物 / 分子間相互作用 / 機能性粒子
Research Abstract

A spray-dried powder (SDP) of trans-glycosylated materials and and poorly water soluble drugs were prepared by a spray-drying method. The SDPs resulted in pronounced improvementin both the dissolution rate and solubility of drugs. Hsp-G molecules self-associated into particular small micelles. Solubility enhancement was due to the incorporation of drugs into Hsp-G micelle. Fluorescence study revealed that the hydrophobic steviol-skeleton of Stevia-G made a hydrophobic core around a hydrophobic molecule, and the micellar aggregation number of Stevia-G was estimated as ca.15. This specific structure formed by Stevia-G molecules led to an enhancement of the apparent solubility of poorly water-soluble drugs. Rutin-G also showed pronounced improvement in both thedissolution rate and solubility of APIs, indicating the possibility of the new type nano-composite formation.

Report

(4 results)
  • 2012 Annual Research Report   Final Research Report ( PDF )
  • 2011 Annual Research Report
  • 2010 Annual Research Report
  • Research Products

    (33 results)

All 2012 2011 2010

All Journal Article (15 results) (of which Peer Reviewed: 7 results) Presentation (16 results) (of which Invited: 2 results) Patent(Industrial Property Rights) (2 results)

  • [Journal Article] Nanocomposite FormationBetween Alpha-glucosyl Stevia and Surfactant Improves the Dissolution Profile of Poorly Water-Soluble Drug, Int2012

    • Author(s)
      H. Uchiyama, Y. Tozuka, M. Nishikawa, H. Takeuchi
    • Journal Title

      J. Pharm

      Volume: 428 Pages: 183-186

    • Related Report
      2012 Final Research Report
  • [Journal Article] Transglycosylated Rutin-Specific Non-Surface-Active Nanostructure Affects Absorption Enhancement of Flurbiprofen, Euro2012

    • Author(s)
      Y. Tozuka, K. Higashi, T. Morita, M.Nishikawa, H. Uchiyama, J. Zhang, K. Moribe, K. Nishikawa, H. Takeuchi, K. Yamamoto
    • Journal Title

      J. Pharm. Biopharm

      Volume: 82 Pages: 120-126

    • Related Report
      2012 Final Research Report
  • [Journal Article] Nanocomposite Formation Between Alpha-glucosyl Stevia and Surfactant Improves the Dissolution Profile of Poorly Water-Soluble Drug2012

    • Author(s)
      Hiromasa Uchiyama
    • Journal Title

      International Journal of Pharmaceutics

      Volume: 428 Issue: 1-2 Pages: 183-186

    • DOI

      10.1016/j.ijpharm.2012.01.016

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Transglycosylated Rutin-Specific Non-Surface-Active Nanostructure Affects Absorption Enhancement of Flurbiprofen2012

    • Author(s)
      Yuichi Tozuka
    • Journal Title

      European Journal of Pharmaceutics and Biopharmaceutics

      Volume: 82 Issue: 1 Pages: 120-126

    • DOI

      10.1016/j.ejpb.2012.05.005

    • Related Report
      2012 Annual Research Report
    • Peer Reviewed
  • [Journal Article] α-Glucosyl Hesperidin Induced Improvement in Bioavailability of Pranlukast Hemihydrate Using High-Pressure Homogenization, Int2011

    • Author(s)
      H. Uchiyama, Y. Tozuka, F. Asamato, H.Takeuchi
    • Journal Title

      J. Pharm

      Volume: 410 Pages: 114-117

    • Related Report
      2012 Final Research Report
  • [Journal Article] Fluorescence Investigation of a Specific Structure Formed by Aggregation of Transglycosylated Stevias: Solubilizing Effect of Poorly Water-Soluble Drugs2011

    • Author(s)
      H. Uchiyama, Y. Tozuka, F. Asamato, H.Takeuchi
    • Journal Title

      Euro. J. Pharm. Sci

      Volume: 43 Pages: 71-77

    • Related Report
      2012 Final Research Report
  • [Journal Article] NMR Investigation of a Novel Excipient, α-Glicosylhesperidin as a Suitable Solubilizing Agent for Poorly Water-Soluble Drugs2011

    • Author(s)
      J. Zhang, Y. Tozuka, H. Uchiyama, K.Higashi, K. Moribe, H. Takeuchi, K.Yamamoto
    • Journal Title

      J. Pharm. Sci

      Volume: 100 Pages: 4421-4431

    • Related Report
      2012 Final Research Report
  • [Journal Article] Fluorescence Investigation of a Specific Structure Formed by Aggregation of Transglycosylated Stevias : Solubilizing Effect of Poorly Water-Soluble Drugs2011

    • Author(s)
      H.Uchiyama, Y.Tozuka, F.Asamato, H.Takeuchi
    • Journal Title

      European journal of pharmaceutical sciences

      Volume: 43 Issue: 1-2 Pages: 71-77

    • DOI

      10.1016/j.ejps.2011.03.014

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] NMR investigation of a novel excipient, α-glucosylhesperidin, as a suitable solubilizing agent for poorly water-soluble drugs2011

    • Author(s)
      J.Zhang, Y.Tozuka, H.Uchiyama, K.Higashi, K.Moribe, H.Takeuchi, K.Yamamoto
    • Journal Title

      J.Pharm.Sci

      Volume: 100 Issue: 10 Pages: 4421-4431

    • DOI

      10.1002/jps.22606

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] A Novel Application of α-Glucosyl Hesperidin for Nanoparticle Formation of Active Pharmaceutical Ineredient by Dry-Grinding2011

    • Author(s)
      Y.Tozuka, M.Imono, H.Uchiyama, H.Takeuchi
    • Journal Title

      European journal of pharmaceutics and biopharm aceutics

      Volume: 79 Issue: 3 Pages: 559-565

    • DOI

      10.1016/j.ejpb.2011.07.006

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Anomalous Dissolution PropertyEnhancement of Naringenin fromSpray-Dried Powders withα-Glucosylhesperidin2010

    • Author(s)
      Y. Tozuka, J. Kishi, H. Takeuchi
    • Journal Title

      Adv. Powder.Tech

      Volume: 21 Pages: 305-309

    • Related Report
      2012 Final Research Report
  • [Journal Article] Improvement of Dissolution and Absorption Properties of Poorly Water-Soluble Drug by Preparing Spray-Dried Powders with α-Glucosyl Hesperidin2010

    • Author(s)
      H. Uchiyama, Y. Tozuka, H. Imono, H.Takeuchi
    • Journal Title

      Int. J. Pharm

      Volume: 392 Pages: 101-106

    • Related Report
      2012 Final Research Report
  • [Journal Article] Transglycosylated Stevia and Hesperidin as Pharmaceutical Excipients: Dramatic Improvement in Drug Dissolution and Bioavailability2010

    • Author(s)
      H. Uchiyama, Y. Tozuka, H. Imono, H.Takeuchi
    • Journal Title

      Euro J. Pharm. Biopharm

      Volume: 76 Pages: 238-244

    • Related Report
      2012 Final Research Report
  • [Journal Article] Improvement of Dissolution and Absorption Properties of Poorly Water-Soluble Drug by Preparing Spray-Dried Powders with α-Glucosyl Hesperidin2010

    • Author(s)
      内山博雅、戸塚裕一、鋳物将明、竹内洋文
    • Journal Title

      International journal of pharmaceutics

      Volume: 392 Pages: 101-106

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Transglycosylated Stevia and Hesperidin as Pharmaceutical Excipients : Dramatic Improvement in Drug Dissolution and Bioavailability2010

    • Author(s)
      内山博雅、戸塚裕一、鋳物将明、竹内洋文
    • Journal Title

      European journal of pharmaceutics and biopharm aceutics

      Volume: 76 Pages: 238-244

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Presentation] NMR 測定による Stevia-G の自己集合構造及び薬物溶解性改善メカニズムの解明2012

    • Author(s)
      東顕二郎、Junying Zhang、 戸塚 裕一 、 Limwikrant Waree、森部久仁一、竹内洋文、山本恵司
    • Organizer
      日本薬剤学会第27 年会
    • Related Report
      2012 Final Research Report
  • [Presentation] 糖転移させた食品添加剤のナノ集合体形成を利用した製剤設計2012

    • Author(s)
      戸塚裕一
    • Organizer
      創剤フォーラム第18回シンポジウム
    • Related Report
      2012 Annual Research Report 2012 Final Research Report
  • [Presentation] A strategic use of functional excipients to enhance the apparent solubility of API: a discovery of novel organic nanocomposite2012

    • Author(s)
      Yuichi Tozuka
    • Organizer
      ExAct Fair 2012
    • Place of Presentation
      Singapore
    • Related Report
      2012 Annual Research Report
    • Invited
  • [Presentation] Molecular Interaction-Mediated Particle Design for Improvement of Dissolution/Absorption Profile of Active Pharmaceutical Ingredient2012

    • Author(s)
      Yuichi Tozuka
    • Organizer
      The 2nd Advanced Study for Integrated Particle Science and Technology(ASIPST) Internatinal Symposium
    • Place of Presentation
      京都
    • Related Report
      2012 Annual Research Report
    • Invited
  • [Presentation] Dramatic Improvement of Dissolution and Absorption Properties of API by Spray-dried Powders with Transglycosylayed Materilas2011

    • Author(s)
      Yuichi Tozuka
    • Organizer
      Particulate Processes in the Pharmaceutical Industry III
    • Place of Presentation
      Australia
    • Year and Date
      2011-07-29
    • Related Report
      2011 Annual Research Report
  • [Presentation] NMR 測定を用いた水溶液中でのα-glycosyl hesperidin の構造評価2011

    • Author(s)
      張峻頴、内山博雅、東顕二郎、戸塚裕一、森部久仁一、竹内洋文、山本恵司
    • Organizer
      日本薬学会 131 年会
    • Related Report
      2012 Final Research Report
  • [Presentation] 糖転移ステビアと界面活性剤のナノコンポジットの製剤学的利用2011

    • Author(s)
      内山博雅、鋳物将明、西川真紘、 戸塚裕 一 、竹内洋文
    • Organizer
      日本薬剤学会第26 年会
    • Related Report
      2012 Final Research Report
  • [Presentation] 糖転移ヘスペリジンとのナノ 複合体形成による難水溶性化合物の溶解性および吸収性改善2011

    • Author(s)
      戸塚裕一
    • Organizer
      第3回糖転移ヘス ペリジン・ビタミン P 研究会
    • Related Report
      2012 Final Research Report
  • [Presentation] 分子間相互作用を利用した新規粒子設計2010

    • Author(s)
      戸塚裕一
    • Organizer
      日本薬剤学会第25年会
    • Place of Presentation
      徳島市
    • Year and Date
      2010-05-12
    • Related Report
      2010 Annual Research Report
  • [Presentation] 分子間相互作用を利用した新規粒子設計.日本薬剤学会奨励賞受賞講演2010

    • Author(s)
      戸塚裕一
    • Organizer
      日本薬剤学会第25 年会講演要旨集
    • Related Report
      2012 Final Research Report
  • [Presentation] 糖転移化合物を用いた難水溶性薬物の溶解性及び吸収性改善に関する製剤設計2010

    • Author(s)
      内山博雅、 戸塚裕一 、鋳物将明、竹内洋 文
    • Organizer
      日本薬剤学会第25 年会講演要旨集
    • Related Report
      2012 Final Research Report
  • [Presentation] 糖転移化合物を用いた難水溶性化合物の溶解性/吸収性改善に関 する研究2010

    • Author(s)
      内山博雅、浅本房俊、鋳物将明、 戸塚裕 一 、竹内洋文
    • Organizer
      第45回技術討論会テキスト
    • Related Report
      2012 Final Research Report
  • [Presentation] 糖転移化合物を用いた難水溶性成分の溶解性及び吸収性改善手法に関する研究2010

    • Author(s)
      鋳物将明、内山博雅、 戸塚裕一、竹内洋 文
    • Organizer
      平成 22 年度粉体工学会中部談話会
    • Related Report
      2012 Final Research Report
  • [Presentation] NMR 測定によるα-Gヘスペリジンの薬物可溶化メカニズムの解明2010

    • Author(s)
      東顕二郎、張峻頴、内山博雅、戸塚裕一 、森部久仁一、竹内洋文、山本恵司
    • Organizer
      第27回製剤と粒子設計シンポジウム
    • Related Report
      2012 Final Research Report
  • [Presentation] 蛍光物質を用いた糖転移ステビアが示す溶解性改善メカニズムの解明2010

    • Author(s)
      内山博雅、鋳物将明、浅本房俊、戸塚裕 一、竹内洋文
    • Organizer
      粉体工学会 2010 年度秋期研究発表会
    • Related Report
      2012 Final Research Report
  • [Presentation] 糖転移ヘスぺリジン及びステビアを用いた難水溶性薬物の溶解性及び吸収性改善2010

    • Author(s)
      内山博雅、鋳物将明、 戸塚裕一、竹内洋文
    • Organizer
      2010 年度秋期研究発表会
    • Related Report
      2012 Final Research Report
  • [Patent(Industrial Property Rights)] 難水溶性物質の溶解方法およびその利用2012

    • Inventor(s)
      戸塚裕一, 内山博雅, 竹内洋文, 相澤 恭、飯田純久
    • Industrial Property Rights Holder
      東洋精糖株式会社
    • Patent Publication Number
      2012-240949
    • Acquisition Date
      2012-12-10
    • Related Report
      2012 Final Research Report
  • [Patent(Industrial Property Rights)] 高吸収性薬剤組成物およびその製造方法2011

    • Inventor(s)
      戸塚裕一, 内山博雅, 竹内洋文, 飯田純久, 米谷俊
    • Industrial Property Rights Holder
      東洋精糖株式会社
    • Patent Publication Number
      2011-051938
    • Acquisition Date
      2011-03-17
    • Related Report
      2012 Final Research Report

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Published: 2010-08-23   Modified: 2019-07-29  

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