Delayed-release mesalazine (5-aminosalicylic acid): coat dissolution and excretion in ileostomy subjects

Br J Clin Pharmacol. 1988 Aug;26(2):173-7. doi: 10.1111/j.1365-2125.1988.tb03383.x.

Abstract

1. Delayed-release mesalazine has been formulated to deliver 5-aminosalicylic acid to the colon. We have therefore studied the ileostomy excretion and coat dissolution of this preparation. 2. Following ingestion of a single tablet 88% (range 69-114%) of the 400 mg dose appeared unchanged in the ileosomy effluent over the subsequent 12 h. 3. Ileostomy effluent pH appeared to be a major determinant of 5-aminosalicylic acid release. 4. In vitro studies revealed rapid coat dissolution above pH 7.0, slow dissolution between pH 6.0 and 7.0 and non-dissolution at pH 2.0 and 4.0.

MeSH terms

  • Adult
  • Aminosalicylic Acids / administration & dosage
  • Aminosalicylic Acids / pharmacokinetics*
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations
  • Female
  • Humans
  • Hydrogen-Ion Concentration
  • Ileostomy*
  • Male
  • Mesalamine
  • Middle Aged
  • Solubility

Substances

  • Aminosalicylic Acids
  • Delayed-Action Preparations
  • Mesalamine