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Glucose and citrate reduce the permeability changes caused by indomethacin in humans

I Bjarnason1, P Smethurst, A Macpherson

  • 1Division of Clinical Biochemistry, King's College School of Medicine, London, England.

Gastroenterology
|May 1, 1992
PubMed

Insights

Coadministering glucose and citrate with nonsteroidal anti-inflammatory drugs (NSAIDs) may protect the intestines. This formulation prevented NSAID-induced increases in intestinal permeability, suggesting a new approach to reduce gastrointestinal side effects.

Area of Science:

  • Gastroenterology
  • Pharmacology
  • Biochemistry

Background:

  • Nonsteroidal anti-inflammatory drugs (NSAIDs) can increase intestinal permeability, a key factor in NSAID enteropathy.
  • Metabolic pathways like glycolysis and the tricarboxylic acid cycle may be inhibited by NSAIDs, leading to permeability changes.

Purpose of the Study:

  • To investigate whether coadministering glucose and citrate with indomethacin can prevent NSAID-induced increases in intestinal permeability.
  • To explore the protective mechanisms of glucose and citrate against NSAID enteropathy.

Main Methods:

  • Utilized a combined intestinal absorption-permeability test with multiple probes (3-O-methyl-D-glucose, D-xylose, L-rhamnose, [51Cr]EDTA).
  • Assessed intestinal permeability using the differential urine excretion ratio of [51Cr]-EDTA/L-rhamnose.
  • Conducted pharmacokinetic studies to evaluate drug absorption and the effects of glucose and citrate.

Main Results:

  • Indomethacin significantly increased intestinal permeability.
  • A formulation of indomethacin with both glucose and citrate (15 mg each per mg indomethacin) did not significantly increase intestinal permeability above baseline.
  • Neither glucose nor citrate alone, when given with indomethacin, showed protective effects.
  • Pharmokinetic data indicated that the protective effects were not due to altered indomethacin absorption.

Conclusions:

  • Coadministration of glucose and citrate with indomethacin formulations can prevent increased intestinal permeability.
  • This approach offers a potential strategy for mitigating the small intestinal side effects associated with NSAID use.
  • The findings suggest a metabolic basis for NSAID enteropathy and a novel therapeutic intervention.

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