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 tablet for the treatment of ulcerative colitis consisting essentially of (1) a tableted core, and (2) a coating on said tableted core, wherein said tableted core consists of a compressed blend of ingredients, said ingredients comprising:
 (a) 9 mg of budesonide;   (b) hydroxypropyl cellulose; and   (c) starch or starch derivative;   wherein said coating on said tableted core comprises methacrylic acid copolymer type A and methacrylic acid copolymer type B in a weight to weight ratio of from 1:5 to 5:1;   wherein following oral administration of the tablet to a human, the tablet provides a T max  of said budesonide in said human of about 13.3±5.9 hours;   and wherein said tablet provides extended release of budesonide in the colon of said human effective to treat ulcerative colitis in said human.   
     
     
         2 . The tablet of  claim 1 , wherein said ingredients further comprise lactose. 
     
     
         3 . The tablet of  claim 1 , wherein said ingredients further comprise all of hydroxypropyl cellulose, silicon dioxide, lactose, microcrystalline cellulose and lecithin. 
     
     
         4 . The tablet of  claim 1 , wherein said ingredients further comprise magnesium stearate. 
     
     
         5 . The tablet of  claim 2 , wherein said ingredients further comprise magnesium stearate. 
     
     
         6 . The tablet of  claim 3 , wherein said ingredients further comprise magnesium stearate. 
     
     
         7 . The tablet of  claim 1 , wherein said ingredients do not comprise stearic acid. 
     
     
         8 . The tablet of  claim 2 , wherein said ingredients do not comprise stearic acid. 
     
     
         9 . The tablet of  claim 5 , wherein said ingredients do not comprise stearic acid. 
     
     
         10 . The tablet of  claim 1 , wherein the weight to weight ratio of methacrylic acid copolymer type A to methacrylic acid copolymer type B in said mixture of methacrylic acid copolymer type A and methacrylic acid copolymer type B in said coating on said tableted core is 1:1. 
     
     
         11 . The tablet of  claim 1 , wherein said coating on said tableted core further comprises triethylcitrate. 
     
     
         12 . The tablet of  claim 10 , wherein said coating on said tableted core further comprises triethylcitrate. 
     
     
         13 . A method of treating a human subject with ulcerative colitis, comprising administering to said human subject a tablet consisting essentially of (1) a tableted core, and (2) a coating on said tableted core, wherein said tableted core consists of a compressed blend of ingredients, said ingredients comprising:
 (a) 9 mg of budesonide;   (b) hydroxypropyl cellulose; and   (c) starch or starch derivative;   wherein said coating on said tableted core comprises methacrylic acid copolymer type A and methacrylic acid copolymer type B in a weight to weight ratio of from 1:5 to 5:1;   wherein following oral administration of the tablet to a human, the tablet provides a T max  of said budesonide in said human of about 13.3±5.9 hours;   and wherein said tablet provides extended release of budesonide in the colon of said human effective to treat ulcerative colitis in said human.   
     
     
         14 . The method of  claim 13 , wherein the weight to weight ratio of methacrylic acid copolymer type A to methacrylic acid copolymer type B in said mixture of methacrylic acid copolymer type A and methacrylic acid copolymer type B in said coating on said tableted core is 1:1. 
     
     
         15 . The method of  claim 14 , wherein said coating on said tableted core further comprises triethylcitrate.