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Enhancement of oral absorption of biological medicines through co-encapsulation with oligoarginine-linked polymers

Research Project

Project/Area Number 25670016
Research Category

Grant-in-Aid for Challenging Exploratory Research

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

Principal Investigator

SAKUMA Shinji  摂南大学, 薬学部, 教授 (80388644)

Co-Investigator(Kenkyū-buntansha) KAWAKAMI Kohsaku  物質材料研究機構, 生体機能材料ユニット, 主幹研究員 (00455271)
Project Period (FY) 2013-04-01 – 2015-03-31
Project Status Completed (Fiscal Year 2014)
Budget Amount *help
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2014: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2013: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywords吸収促進 / バイオ医薬 / オリゴアルギニン / オリゴアルギニン固定化高分子 / エレクトロスプレー / 腸溶性
Outline of Final Research Achievements

There are a couple of problems that should be solved to develop oral formulations of biological medicines: safety of absorption enhancers and a reduction of efficacy of the enhancers through dilution in the gastrointestinal tract. We designed enteric-coated particles containing drugs and absorption enhancers. Electrospray deposition was applied for particle preparation. When both a drug and an absorption enhancer were organic compounds with low molecular weights, absorption-enhancing functions was boosted through their co-encapsulation. This was presumably because the drug was always accompanied by the enhancer during the gastrointestinal transit. Oral absorption of insulin was enhanced when it was co-administered with oligoarginine-linked polymers in a solution. When the dosage form was substituted with enteric-coated particles, insulin absorption was considerably reduced. This probably resulted from interactions between formulated substances.

Report

(3 results)
  • 2014 Annual Research Report   Final Research Report ( PDF )
  • 2013 Research-status Report
  • Research Products

    (2 results)

All 2015 2014

All Journal Article (1 results) (of which Peer Reviewed: 1 results,  Open Access: 1 results,  Acknowledgement Compliant: 1 results) Presentation (1 results)

  • [Journal Article] Enhanced boosting of oral absorption of lopinavir through electrospray co-encapsulation with ritonavir2015

    • Author(s)
      Shinji Sakuma, Satoshi Matsumoto, Narimoto Ishizuka, Kohta Mohri, Mayuko Fukushima, Chie Ohba, Kohsaku Kawakami
    • Journal Title

      Journal of Pharmaceutical Sciences

      Volume: 印刷中

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Presentation] 薬物/吸収促進剤-包含型腸溶性微粒子を用いた経口吸収改善2014

    • Author(s)
      松本諭、石塚就元、川上亘作、佐久間信至
    • Organizer
      日本薬剤学会第29年会
    • Place of Presentation
      大宮
    • Year and Date
      2014-05-20 – 2014-05-22
    • Related Report
      2014 Annual Research Report

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Published: 2014-07-25   Modified: 2019-07-29  

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