Release of 5-ASA from Pentasa in patients with Crohn's disease of the small intestine.

Abstract

BACKGROUND:

Pentasa is a controlled-release tablet made from semipermeable microspheres and designed to continuously deliver therapeutic quantities of 5-ASA (5-aminosalicylic acid) throughout the gastrointestinal tract. Scintigraphic studies in healthy subjects have documented that 5-ASA release could occur in the small intestine. We tested here the disintegration of Pentasa in the digestive tract of nine patients with Crohn's disease of the small intestine.

MATERIALS:

Each patient was given, after breakfast, a 250 mg tablet of Pentasa containing samarium-153 oxide. For 8 h the progression of the isotope in the gastrointestinal tract was followed using gamma camera scintigraphy. Plasma measurement of 5-ASA and acetylated 5-ASA was used to verify the liberation and absorption of 5-ASA.

RESULTS:

The Pentasa tablet appeared completely dissolved in the stomach by 117 +/- 18 min. Samarium oxide was first detected in the small intestine 60 +/- 5 min after its ingestion; it reached the colon after 280 +/- 13 min and it was completely absent from the small intestine at 360 +/- 26 min. Plasma concentrations of 5-ASA started to rise after 67 +/- 7 min and were maximal at 222 +/- 25 min.

CONCLUSION:

In patients with Crohn's disease of the small intestine, Pentasa microgranules start releasing 5-ASA in the proximal small intestine, acting locally to exert its beneficial effect.

• Authors: J Larouche, J Morais, M Picard, C Lambert, J Spénard, H Landriault, G Kennedy, P Poitras
• Journal: Alimentary pharmacology & therapeutics (Aliment Pharmacol Ther) Vol. 9 Issue 3 Pg. 315-20 (Jun 1995) ISSN: 0269-2813 [Print] England
• PMID: 7654894 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Aminosalicylic Acids
• Tablets
• Samarium
• Mesalamine

Topics

• Adult
• Aminosalicylic Acids (administration & dosage, pharmacokinetics)
• Crohn Disease (diagnostic imaging, drug therapy, metabolism)
• Humans
• Mesalamine
• Middle Aged
• Radionuclide Imaging
• Samarium
• Tablets