Steady-state pharmacokinetics of enteric coated 5-amino-salicylic acid tablets in healthy volunteers and in patients with Crohn's disease or ulcerative colitis.

An Eudragit-L coated oral 5-aminosalicylic acid (5-ASA; mesalazine) product (Mesasal), has been formulated to deliver 5-ASA to the distal small bowel and colon for the treatment of inflammatory bowel disease. The purpose of this study was to compare the pharmacokinetic profile of this product at steady-state between healthy volunteers and two different patient groups with inflammation of either the small or the large bowel. Two carefully selected groups of patients, nine with Crohn's disease restricted to the small intestine and ten with total ulcerative colitis and one group of ten healthy volunteers received two 250 mg Mesasal tablets three times daily for 10 days to reach steady-state. Plasma 5-ASA and acetyl-5-ASA concentrations were followed for 48 h and urinary excretion for 72 h. There was a great variation in most pharmacokinetic parameters within each group and no significant differences were noticed between the groups. The location of the inflammatory process probably does not influence the pharmacokinetics of 5-ASA in any significant way in patients with either Crohn's disease in the small bowel or total ulcerative colitis.