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Ex Vivo Intestinal Sacs to Assess Mucosal Permeability in Models of Gastrointestinal Disease
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Delivery and fate of oral mesalamine microgranules within the human small intestine

P H Layer1, H Goebell, J Keller

  • 1Department of Medicine, University of Essen, Germany.

Gastroenterology
|May 1, 1995
PubMed
Abstract

Insights

Slow-release mesalamine (5-ASA) effectively treats small intestinal Crohn's disease by achieving high luminal concentrations throughout the small intestine, despite most of the drug reaching the colon.

Area of Science:

  • Gastroenterology
  • Pharmacokinetics
  • Inflammatory Bowel Disease

Background:

  • Oral mesalamine (5-ASA) for inflammatory bowel disease necessitates slow-release formulations to prevent premature absorption.
  • Luminal concentrations of mesalamine in the human small intestine are not well-established.

Purpose of the Study:

  • To investigate the intestinal delivery patterns of mesalamine from a microgranule preparation (Pentasa).
  • To determine small intestinal luminal concentrations of mesalamine in healthy subjects.

Main Methods:

  • Six healthy subjects underwent multilumen tube placement for duodenal, jejunal, and ileal aspiration.
  • Luminal, plasma, and urinary levels of mesalamine and acetylmesalamine were measured for 7 hours post-ingestion of a 500 mg dose with a labeled meal.

Main Results:

  • Mesalamine release occurred throughout the small intestine, with 20% of the dose delivered cumulatively.
  • High luminal concentrations of mesalamine and acetylmesalamine were observed in the duodenum, jejunum, and ileum for up to 4 hours.
  • 82% of the mesalamine dose reached the colon, with only 7% dissolved.

Conclusions:

  • A significant portion of slow-release mesalamine is released in the small intestine.
  • High luminal concentrations in the small intestine likely contribute to the efficacy of mesalamine in Crohn's disease affecting this region.

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