A study for the development of the mesalazine multiparticulate dosage forms for colon delivery in paediatric patients.

Mesalazine (5-ASA) is an anti-inflammatory drug used for ulcerative colitis or Crohn's desease. Most of available oral 5-ASA dosage forms are modified release tablets targeting the colon. However, in paediatrics patient compliance would improve by avoiding dosage forms that channot be swallowed by children. The aim of this work was to develop gastro-resistant multiparticulate dosage forms for mesalazine colon delivery, for easier dose intake by children. Different granule formulations were considered starting from mesalazine granules prepared by kneading with an Eudragit S 100 solution and granulation (1 mm mesh sieve). Lipid coating was obtained by depositing melted stearic acid on 5-ASA granules. Lipid granules were also double coated by sprying on Eudragit FS suspension in a rotating glass pan. Agglomerates were prepared by blending mesalazine lipid microparticles (manufactured by spray-congealing) with excipient microparticles, which had been separately obtained by spray-drying