Controlled-release granular compositions containing mesalazine and process for the manufacture thereof

摘要

The present invention refers to controlled release granular compositions of mesalazine and their use in the treatment of inflammatory pathologies of the intestinal tract. The aforesaid granular compositions comprise: a) a central core comprising an inert substrate; b) an intermediate layer comprising mesalazine and one or more physiologically acceptable excipients; c) a gastro-resistant coating. The present invention then refers to a process for obtaining the aforesaid granular compositions.

主权项

1. A granular composition with controlled release of mesalazine comprising:
a) a central core consisting of an inert substrate, wherein the inert substrate is microcrystalline cellulose and wherein said core contains 14.88% by weight of the microcrystalline cellulose with respect to the total weight of the composition; b) an intermediate layer comprising mesalazine, a plasticizer, a suspending agent and/or gliding agent and a film-forming agent, wherein the plasticizer is a polyalkylene glycol, the suspending agent and/or gliding agent is silicone dioxide and the film forming agent is a hydroxyalkylcellulose and wherein said intermediate layer b) contains 30% by weight of mesalazine, 3.26% by weight of polyethylene glycol 400, 0.79% by weight of colloidal silicon dioxide, 3.26% by weight of hydroxypropylmethylcellulose with respect to the total weight of the composition; and c) a gastro-resistant coating selected from among methacrylic and acrylic acid polymers and copolymers, wherein said gastro-resistant coatig c) contains 31.38% by weight of methacrvlic acid copolymer, 15.68% by weight of triethyl citrate and 0.75% by weight of colloidal silicon dioxide, with respect to the total weight of the composition.