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Preparation and evaluation of injectable slow-release formulations of local anesthetics.

Research Project

Project/Area Number 20K17828
Research Category

Grant-in-Aid for Early-Career Scientists

Allocation TypeMulti-year Fund
Review Section Basic Section 55050:Anesthesiology-related
Research InstitutionGunma University

Principal Investigator

Matsui Yusuke  群馬大学, 医学部附属病院, 助教 (20805056)

Project Period (FY) 2020-04-01 – 2023-03-31
Project Status Completed (Fiscal Year 2022)
Budget Amount *help
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2022: ¥390,000 (Direct Cost: ¥300,000、Indirect Cost: ¥90,000)
Fiscal Year 2021: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Fiscal Year 2020: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Keywords局所麻酔薬徐放化 / レボブピバカイン / 温度応答性 / 居所麻酔薬徐放化 / 徐放 / 局所麻酔薬 / Drug Delivery System
Outline of Research at the Start

生体内で自然に分解され、温度に応答して性質が変わる物質を利用して、注射可能な局所麻酔薬の徐放製剤作成 (術後急性期痛の 鎮痛を念頭に48-78時間かけてのゆっくりとした放出を想定) を目指す。その後、同製剤を局所浸潤麻酔ならびに末梢神経ブロックへ応用する。

Outline of Final Research Achievements

An injectable slow-release formulation of levobupivacaine in the form of a temperature-responsive gel was prepared and evaluated in animals and humans. A slow-release formulation was successfully prepared in collaboration with Kansai University. For the slow release effect, the release rate in test tubes was evaluated. In an environment similar to that in vivo, the encapsulated levobupivacaine was released in approximately 48 hours. Pain threshold evaluation and safety evaluation were also conducted in rats. The results showed a prolonged analgesic effect time. Compared to the non-sustained release, pain thresholds were higher at 6 and 12 hours with statistically significant differences. No motor impairment remained for an extended period of time, and there were no obvious effects on nerves. The above information is currently being submitted to a scientific journal.

Academic Significance and Societal Importance of the Research Achievements

注射可能な局所麻酔薬は、今までの局所麻酔薬よりも作用時間の延長ができる。注射かなおうなため、現在局所麻酔薬が投与されている、局所麻酔、伝達麻酔、硬膜外麻酔など、幅広い状況で使用することが想定できる。これにより、オピオイドをはじめとした他の鎮痛薬減量による副作用軽減が期待でき、術後の回復促進をはかれる。それにより入院期間の短縮や医療費削減が期待される。また、鎮痛のために持続投与用カテーテルを留置しなくてもすむようになる可能性があり、患者や医療従事者の負担軽減、コスト削減の実現も期待される。

Report

(4 results)
  • 2022 Annual Research Report   Final Research Report ( PDF )
  • 2021 Research-status Report
  • 2020 Research-status Report
  • Research Products

    (2 results)

All 2022

All Presentation (2 results) (of which Int'l Joint Research: 2 results)

  • [Presentation] The history of local anesthesia multiple approaches to elongate the action2022

    • Author(s)
      Yusuke Matsui, Masaru Tobe, Takashi Suto, Shigeru Saito
    • Organizer
      The 10th International Symposium on The History of Anesthesia
    • Related Report
      2022 Annual Research Report
    • Int'l Joint Research
  • [Presentation] The history of local anesthesia: multiple approaches to elongate the action.2022

    • Author(s)
      Yusuke Matsui
    • Organizer
      10th International Symposium on the History of Anesthesia
    • Related Report
      2021 Research-status Report
    • Int'l Joint Research

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Published: 2020-04-28   Modified: 2024-01-30  

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