Disposition of mesalazine from mesalazine-delivering drugs in patients with inflammatory bowel disease, with and without diarrhoea

Scand J Gastroenterol. 1992 Oct;27(10):863-8. doi: 10.3109/00365529209000155.


The disposition of mesalazine from the azo compounds sulphasalazine and olsalazine (Dipentum) and from the slow-release mesalazine drugs Pentasa, Asacol, and Salofalk was studied in 20 patients with inflammatory bowel disease. Ten of them had diarrhoea, and 10 had normal stools. On the last 2 days of a 7-day maintenance treatment with each of the study drugs urine and faeces were collected for determination of mesalazine, acetyl-mesalazine, and unsplit azo compound. In patients with and without diarrhoea the urinary and the faecal excretion of acetyl-mesalazine was lowest during treatment with olsalazine. The proportion of acetyl-mesalazine in faeces was highest during treatment with Pentasa in both groups. The presence of diarrhoea was associated with a decrease in the proportion of acetyl-mesalazine in faeces during treatment with all drugs, not significant only for Pentasa. The proportion of unsplit azo compound in faeces increased in the case of diarrhoea to almost 50%. It is concluded that in patients with inflammatory bowel disease diarrhoea substantially influences the disposition from all these drugs except Pentasa.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Aged
  • Aminosalicylic Acids / chemistry
  • Aminosalicylic Acids / pharmacokinetics*
  • Aminosalicylic Acids / therapeutic use*
  • Aminosalicylic Acids / urine
  • Delayed-Action Preparations / standards
  • Diarrhea / etiology*
  • Drug Carriers
  • Feces / chemistry
  • Female
  • Gastrointestinal Transit
  • Humans
  • Inflammatory Bowel Diseases / complications
  • Inflammatory Bowel Diseases / drug therapy*
  • Inflammatory Bowel Diseases / urine
  • Male
  • Mesalamine
  • Middle Aged
  • Sulfasalazine / therapeutic use*


  • Aminosalicylic Acids
  • Delayed-Action Preparations
  • Drug Carriers
  • Sulfasalazine
  • Mesalamine
  • olsalazine