Controlled Release and Taste Masking Oral Pharmaceutical Composition

Abstract

Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

1 . A controlled release oral pharmaceutical composition in the form of a tablet, said tablet comprising:
 a) budesonide in an amount effective for treatment of inflammatory bowel disease in the gastrointestinal tract, and   b) a hydrophilic excipient capable of molecular relaxation in an amount effective to achieve said controlled release of said budesonide from said composition.   
     
     
         2 . A controlled release oral pharmaceutical composition according to  claim 1 , wherein said hydrophilic excipient is capable of swelling upon contact with water and said swelling is effective to control the release of said budesonide from said composition. 
     
     
         3 . A controlled release oral pharmaceutical composition according to  claim 1 , wherein said tablet is coated with a gastro-resistant film. 
     
     
         4 . A controlled release oral pharmaceutical composition according to  claim 1 , further comprising a surfactant. 
     
     
         5 . A controlled release oral pharmaceutical composition according to  claim 4 , wherein said surfactant is lecithin. 
     
     
         6 . A controlled release oral pharmaceutical composition according to  claim 1 , wherein said controlled release of said budesonide is achieved by the swelling and disintegration of said hydrophilic excipient. 
     
     
         7 . A method of treating inflammatory bowel disease comprising administering to a patient in recognized need thereof a controlled release oral pharmaceutical composition according to  claim 1 . 
     
     
         8 . A controlled release oral pharmaceutical composition in the form of a tablet, said tablet comprising:
 a) budesonide in an amount effective for treatment of inflammatory bowel disease in the gastrointestinal tract, and   b) a water-swellable hydrophilic excipient in an amount effective to achieve said controlled release of said budesonide from said composition.   
     
     
         9 . A controlled release oral pharmaceutical composition according to  claim 8 , wherein said water-swellable hydrophilic excipient swells upon contact with water to a degree sufficient to control the release of said budesonide from said composition. 
     
     
         10 . A controlled release oral pharmaceutical composition according to  claim 8 , wherein said tablet is coated with a gastro-resistant film. 
     
     
         11 . A controlled release oral pharmaceutical composition according to  claim 8 , wherein said hydrophilic excipient is chosen from acrylic acid polymers, methacrylic acid polymers, acrylic acid copolymers, methacrylic acid copolymers, alkylvinyl polymers, hydroxyalkyl celluloses, carboxyalkyl celluloses, polysaccharides, dextrins, pectins, starches, gums, and alginic acid. 
     
     
         12 . A controlled release oral pharmaceutical composition according to  claim 11 , wherein said hydrophilic excipient is chosen from hydroxyalkyl celluloses. 
     
     
         13 . A controlled release oral pharmaceutical composition according to  claim 12 , wherein said hydrophilic excipient is hydroxypropylcellulose. 
     
     
         14 . A controlled release oral pharmaceutical composition according to  claim 8 , further comprising a surfactant. 
     
     
         15 . A controlled release oral pharmaceutical composition according to  claim 14 , wherein said surfactant is lecithin. 
     
     
         16 . A controlled release oral pharmaceutical composition according to  claim 8 , wherein said controlled release of said budesonide is achieved by the swelling and disintegration of said hydrophilic excipient. 
     
     
         17 . A method of treating inflammatory bowel disease comprising administering to a patient in recognized need thereof a controlled release oral pharmaceutical composition according to  claim 7 .