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Metformin in the digestive tract.

N Vidon1, S Chaussade, M Noel

  • 1INSERM U.290, Hôpital Saint-Lazare, Paris, France.

Diabetes Research and Clinical Practice
|February 19, 1988
PubMed
Summary
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Metformin absorption is limited in the stomach, with most occurring in the duodenum. This study explains gastrointestinal side effects and fecal recovery of metformin by examining drug absorption.

Area of Science:

  • Pharmacology
  • Gastroenterology
  • Drug Metabolism

Background:

  • Metformin, a biguanide drug, causes gastrointestinal issues like nausea and vomiting.
  • Approximately 30% of ingested metformin is eliminated in feces, necessitating an explanation for these phenomena.

Purpose of the Study:

  • To elucidate the mechanisms behind metformin-induced gastrointestinal effects.
  • To investigate the absorption of metformin in the gastroduodenal, jejunal, and ileal regions.
  • To understand the factors limiting metformin absorption and contributing to its fecal recovery.

Main Methods:

  • Study 1 used intubation in six healthy volunteers to assess gastroduodenal (GD) absorption of 1g metformin with a homogenized meal and markers.
  • Gastric emptying and duodeno-gastric reflux were monitored, with GD contents sampled over 4 hours.

Related Experiment Videos

  • Study 2 employed intestinal perfusion in six healthy volunteers to evaluate jejunal and ileal absorption of 400mg metformin.

    • Main Results:

    • Metformin exhibited poor absorption from the stomach (approx. 10% over 4 hours) and did not alter gastric emptying.
    • Duodeno-gastric reflux was observed in five of six subjects, and about 20% of the emptied metformin was absorbed from the duodenum.
    • The delivery process was identified as the rate-limiting step for duodenal metformin absorption, with increased absorption correlating to increased AUC/24h.

    Conclusions:

    • Metformin's limited gastric absorption and potential for duodeno-gastric reflux contribute to its gastrointestinal effects and fecal recovery.
    • Duodenal absorption plays a significant role, but is constrained by the drug's delivery rate.
    • Further investigation into jejunal and ileal absorption is warranted to fully understand metformin's pharmacokinetic profile.