4.7 Article

Plateau hypoxia attenuates the metabolic activity of intestinal flora to enhance the bioavailability of nifedipine

期刊

DRUG DELIVERY
卷 25, 期 1, 页码 1175-1181

出版社

TAYLOR & FRANCIS LTD
DOI: 10.1080/10717544.2018.1469687

关键词

Nifedipine; gut microbiota; metabolic activity; plateau hypoxia; bioavailability; pharmacokinetics

资金

  1. National Natural Science Foundation of China [81403004]
  2. Major project of Twelfth Five-Year Plan Military Logistics research [AWS14L005]

向作者/读者索取更多资源

Nifedipine is completely absorbed by the gastrointestinal tract and its pharmacokinetics and metabolism may be influenced by microorganisms. If gut microbes are involved in the metabolism of nifedipine, plateau hypoxia may regulate the bioavailability and the therapeutic effect of nifedipine by altering the metabolic activity of the gut microbiota. We herein demonstrated for the first time that gut flora is involved in the metabolism of nifedipine by in vitro experiments. In addition, based on the results of 16S rRNA analysis of feces in rats after acute plateau, we first confirmed that the plateau environment could cause changes in the number and composition of intestinal microbes. More importantly, these changes in flora could lead to a slower metabolic activity of nifedipine in the body after an acute plateau, resulting in increased bioavailability and therapeutic efficacy of nifedipine. Our research will provide basis and new ideas for changes in the fecal flora of human acutely entering the plateau, and contribute to rational drug use of nifedipine.

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