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Determination of pharmacokinetic properties of prohibited substances to optimize a process of doping test

Research Project

Project/Area Number 18K17840
Research Category

Grant-in-Aid for Early-Career Scientists

Allocation TypeMulti-year Fund
Review Section Basic Section 59020:Sports sciences-related
Research InstitutionHiroshima International University

Principal Investigator

Oda Keisuke  広島国際大学, 薬学部, 講師 (60712594)

Project Period (FY) 2018-04-01 – 2020-03-31
Project Status Completed (Fiscal Year 2019)
Budget Amount *help
¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000)
Fiscal Year 2019: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2018: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
Keywordsドーピング / 薬物動態 / 腎排泄 / LC-MS/MS / 1,3-dimethylamylamine / 尿中排泄 / 経皮吸収 / 尿細管再吸収 / Pharmacokinetics
Outline of Final Research Achievements

The fate of 1, 3-dimethylamylamine (DMAA), a prohibited substance to athletes, was evaluated by determining plasma concentrations, urinary excretion rate, and tissue distribution after intravenous, oral and transdermal administration in rats. DMAA administered intravenously disappeared from plasma according to a biexponential curve. During 6 h after intravenous administration, 35.2% of DMAA dose was excreted into urine as an intact form. Alkalized urine pH resulted in decreased urinary excretion rate and higher plasma concentrations of DMAA.The mean oral bioavailability of DMAA was 43.6%. When DMAA was applied to the skin, DMAA was recovered by 5.4% of dose in the urine for 7 days. In conclusion, DMAA was thought to be absorbed from anywhere, including the skin and distributed to various tissues. Long-term retention of DMAA in the body was, at least partly, due to the repeated reabsorption in renal tubules, though the extent of DMAA reabsorption depends on urine pH.

Academic Significance and Societal Importance of the Research Achievements

今回得られた知見は、ドーピング禁止物質の生体内運命を明らかにし、その制御因子を同定するものである。尿のpHが変化することにより、ドーピング禁止物質の尿中排泄が変化するため、検査時の「陽性・陰性」判断を誤ってしまう可能性が考えられる。また、DMAAのような塩基性の脂溶性低分子化合物の場合、皮膚などからも吸収されてしまうため、経口摂取以外の体内侵入経路を考慮する必要がある。このように、ドーピング禁止物質の体内動態変動要因を社会に広く周知させることにより、「うっかりドーピング」の回避、ドーピング検査の最適化に寄与できるものと考えられる。

Report

(3 results)
  • 2019 Annual Research Report   Final Research Report ( PDF )
  • 2018 Research-status Report
  • Research Products

    (1 results)

All 2020

All Presentation (1 results)

  • [Presentation] ラットにおけるドーピング禁止物質1,3-ジメチルアミルアミンの体内動態変動要因の探索2020

    • Author(s)
      大津 真依、小田 啓祐、麻生 進太朗、森 信博
    • Organizer
      日本薬学会 第140年会
    • Related Report
      2019 Annual Research Report

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Published: 2018-04-23   Modified: 2021-02-19  

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