Absorption of Oral Mesalazine-Containing Preparations and the Influence of Famotidine on the Absorption

Abstract

The mesalazine-containing preparations Asacol^®, Pentasa^®, and Salofalk^® (= Cla-versal^®) are frequently used in the treatment of inflammatory bowel disease. The release patterns of these formulations are time- and/or pH-dependent. The aim of this study was to investigate the patterns of absorption of these preparations and the influence of raised intragastric pH on absorption. Gastric pH was raised by simultaneous administration of famotidine. Absorption was determined by assaying with a high-performance liquid chromatography method the urinary excretion of acetylmesalazine, the major metabolite of mesalazine. A large intra- and inter-individual variability in absorption was found for all three formulations, both with and without concomitant famotidine administration. Asacol and Pentasa were significantly less absorbed than Salofalk. A significant lower absorption of mesalazine was seen when Asacol was combined with famotidine. Variations in gastric pH have negligible effect on the bioavailability of mesalazine in vivo.

Key Words:

• Absorption
• Asacol^®
• famotidine
• oral mesalazine
• Pentasa^®
• Salofalk^®