Controlled Release and Taste Masking Oral Pharmaceutical Compositions

Abstract

The invention relates to tablet comprising granules dispersed in at least one hydrophilic compound or matrix. The granules contain an active agent, at least one amphiphilic compound and at least one lipophilic compound. The tablet may include a gastro-resistant film coating.

1 . An oral dosage form for the controlled release of an active ingredient in the gastrointestinal tract of a human, said oral dosage form comprising:
 (i) an inert or lipophilic matrix comprising the active ingredient and an amphiphilic compound; and   (ii) a hydrophilic matrix,   
       wherein the inert or lipophilic matrix is dispersed in the hydrophilic matrix. 
     
     
         2 . The oral dosage form according to  claim 1 , wherein the active ingredient is budesonide. 
     
     
         3 . The oral dosage form according to  claim 1 , wherein said tablet further comprises a gastro-resistant coating. 
     
     
         4 . The oral dosage form according to  claim 1 , wherein the gastro-resistant coating comprises a compound selected from methacrylic acid polymers and cellulose derivatives. 
     
     
         5 . The oral dosage form according to  claim 4 , wherein the gastro-resistant coating comprises a methacrylic acid polymer. 
     
     
         6 . The oral dosage form according to  claim 1 , wherein the amphiphilic compound is selected from the group consisting of lecithin, phosphatidylcholine, phosphatidylethanolamine, ceramide, and a glycol alkyl ether. 
     
     
         7 . The oral dosage form according to  claim 6 , wherein the amphiphilic compound is lecithin. 
     
     
         8 . The oral dosage form according to  claim 1 , wherein the inert or lipophilic matrix comprises a compound selected from the group consisting of saturated or unsaturated fatty acid, salt, or alcohol thereof; a mono-, di-, or triglyceride, or polyethoxylated derivative thereof, a wax, ceramide, and cholesterol derivative. 
     
     
         9 . The oral dosage form according to  claim 8 , wherein the inert or lipophilic matrix comprises a saturated fatty acid. 
     
     
         10 . The oral dosage form according to  claim 9 , wherein the inert or lipophilic matrix comprises stearic acid. 
     
     
         11 . The oral dosage form according to  claim 1 , wherein the hydrophilic matrix comprises one or more water-swellable excipients. 
     
     
         12 . The oral dosage form according to  claim 1 , wherein the hydrophilic matrix comprises a compound selected from the group consisting of an acrylic or methacrylic acid polymer or copolymer, an alkylvinyl polymer, hydroxyalkyl cellulose, a carboxyalkyl cellulose, a polysaccharide, dextrin, pectin, starch, a natural or synthetic gum, and alginic acid. 
     
     
         13 . The oral dosage form according to  claim 12 , wherein the hydrophilic matrix comprises a hydroxyalkyl cellulose or a carboxylalkyl cellulose. 
     
     
         14 . The oral dosage form according to  claim 13 , wherein the hydrophilic matrix comprises a hydroxyalkyl cellulose. 
     
     
         15 . An oral dosage form for the controlled release of budesonide in the gastrointestinal tract of a human, said oral dosage form comprising:
 (i) an inert or lipophilic matrix comprising budesonide and an amphiphilic compound; and   (ii) a first matrix comprising a hydrophilic compound,   
       wherein the inert or lipophilic matrix is dispersed in the first matrix. 
     
     
         16 . The oral dosage form according to  claim 15 , wherein said tablet further comprises a gastro-resistant coating. 
     
     
         17 . The oral dosage form according to  claim 15 , wherein the gastro-resistant coating comprises a compound selected from methacrylic acid polymers and cellulose derivatives. 
     
     
         18 . The oral dosage form according to  claim 17 , wherein the gastro-resistant coating comprises a methacrylic acid polymer. 
     
     
         19 . The oral dosage form according to  claim 15 , wherein the amphiphilic compound is selected from the group consisting of lecithin, phosphatidylcholine, phosphatidylethanolamine, ceramide, and a glycol alkyl ether. 
     
     
         20 . The oral dosage form according to  claim 19 , wherein the amphiphilic compound is lecithin. 
     
     
         21 . The oral dosage form according to  claim 15 , wherein the inert or lipophilic matrix comprises a compound selected from the group consisting of saturated or unsaturated fatty acid, salt, or alcohol thereof; a mono-, di-, or triglyceride, or polyethoxylated derivative thereof, a wax, ceramide, and cholesterol derivative. 
     
     
         22 . The oral dosage form according to  claim 21 , wherein the inert or lipophilic matrix comprises a saturated fatty acid. 
     
     
         23 . The oral dosage form according to  claim 22 , wherein the inert or lipophilic matrix comprises stearic acid. 
     
     
         24 . The oral dosage form according to  claim 15 , wherein the hydrophilic compound is a water-swellable excipient. 
     
     
         25 . The oral dosage form according to  claim 15 , wherein the hydrophilic compound is selected from the group consisting of an acrylic or methacrylic acid polymer or copolymer, an alkylvinyl polymer, hydroxyalkyl cellulose, a carboxyalkyl cellulose, a polysaccharide, dextrin, pectin, starch, a natural or synthetic gum, and alginic acid. 
     
     
         26 . The oral dosage form according to  claim 25 , wherein the hydrophilic compound is hydroxyalkyl cellulose or carboxylalkyl cellulose. 
     
     
         27 . The oral dosage form according to  claim 26 , wherein the hydrophilic compound is hydroxyalkyl cellulose. 
     
     
         28 . An oral dosage form for the controlled release of budesonide in the gastrointestinal tract of a human, said oral dosage form comprising:
 a plurality of inert or lipophilic matrices dispersed in a hydrophilic matrix,   
       wherein each of the inert or lipophilic matrices incorporates a first matrix comprising budesonide and an amphiphilic compound. 
     
     
         29 . An oral dosage form for the controlled release of budesonide in the gastrointestinal tract of a human, said oral dosage form comprising:
 a plurality of inert or lipophilic matrices dispersed in a first matrix comprising a hydrophilic compound, wherein each of the inert or lipophilic matrices incorporates budesonide and an amphiphilic compound.   
     
     
         30 . The oral dosage form according to  claim 29 , wherein the first matrix is a hydrophilic matrix.