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.

What is claimed is: 
     
         1 . A controlled release oral pharmaceutical composition in the form of a tablet consisting essentially of:
 (1) a tablet core consisting of a mixture of ingredients, said ingredients comprising:
 a) budesonide in an amount to treat intestinal inflammation; 
 b) hydroxyalkyl cellulose; 
 c) lactose; 
 d) colloidal silica; and 
 e) microcrystalline cellulose; and 
   (2) a gastro-resistant film coating on said tablet core, said coating comprising at least one methacrylic acid polymer or methacrylic acid copolymer.   
     
     
         2 . The controlled release oral pharmaceutical composition according to  claim 1 , wherein said mixture of ingredients in said tablet core further comprises a lubricant. 
     
     
         3 . The controlled release oral pharmaceutical composition according to  claim 1 , wherein said mixture of ingredients in said tablet core further comprises a lipophilic compound. 
     
     
         4 . The controlled release oral pharmaceutical composition according to  claim 3 , wherein said lipophilic compound is selected from the group consisting of palmitic, stearic, myristic, lauric, laurylic, or oleic acid or mixtures thereof, or salts or alcohols or mono-, di-, or triglycerides or ester derivatives thereof. 
     
     
         5 . The controlled release oral pharmaceutical composition according to  claim 4 , wherein said lipophilic compound comprises stearic acid, or salt, alcohol or ester derivative thereof. 
     
     
         6 . The controlled release oral pharmaceutical composition according to  claim 5 , wherein said lipophilic compound comprises the alcohol of stearic acid, or salt or ester derivative thereof. 
     
     
         7 . The controlled release oral pharmaceutical composition according to  claim 1 , wherein said mixture of ingredients in said tablet core further comprises an alcohol of stearic acid, or salt or ester derivative thereof. 
     
     
         8 . A controlled release oral pharmaceutical composition in the form of a tablet consisting essentially of:
 (1) a tablet core consisting of a mixture of ingredients, said ingredients comprising:
 a) 9 mg of budesonide; 
 b) hydroxypropyl cellulose; 
 c) lactose; 
 d) colloidal silica; and 
 e) microcrystalline cellulose; and 
   (2) a gastro-resistant film coating on said tablet core, said coating comprising at least one methacrylic acid polymer or methacrylic acid copolymer.   
     
     
         9 . The controlled release oral pharmaceutical composition according to  claim 8 , wherein said mixture of ingredients in said tablet core further comprises a lubricant. 
     
     
         10 . The controlled release oral pharmaceutical composition according to  claim 9 , wherein said mixture of ingredients in said tablet core further comprises a lipophilic compound. 
     
     
         11 . The controlled release oral pharmaceutical composition according to  claim 10 , wherein said lipophilic compound is selected from the group consisting of palmitic, stearic, myristic, lauric, laurylic, or oleic acid or mixtures thereof, or salts or alcohols or mono-, di-, or triglycerides or ester derivatives thereof. 
     
     
         12 . The controlled release oral pharmaceutical composition according to  claim 11 , wherein said lipophilic compound comprises stearic acid, or salt, alcohol or ester derivative thereof. 
     
     
         13 . The controlled release oral pharmaceutical composition according to  claim 12 , wherein said lipophilic compound comprises the alcohol of stearic acid, or salt or ester derivative thereof. 
     
     
         14 . The controlled release oral pharmaceutical composition according to  claim 8 , wherein said mixture of ingredients in said tablet core further comprises an alcohol of stearic acid, or salt or ester derivative thereof. 
     
     
         15 . The controlled release oral pharmaceutical composition according to  claim 8 , wherein said gastro-resistant film coating further comprises triethyl citrate, talc and titanium dioxide. 
     
     
         16 . The controlled release oral pharmaceutical composition according to  claim 13 , wherein said gastro-resistant film coating further comprises triethyl citrate, talc and titanium dioxide. 
     
     
         17 . A controlled release oral pharmaceutical composition in the form of a tablet consisting essentially of:
 (1) a tablet core consisting of a mixture of ingredients, said ingredients comprising:
 a) budesonide in an amount to treat intestinal inflammation; 
 b) hydroxyalkyl cellulose; and 
 c) stearic acid, or salt, alcohol or ester derivative thereof; and 
   (2) a gastro-resistant film coating on said tablet core, said coating comprising at least one methacrylic acid polymer or methacrylic acid copolymer.   
     
     
         18 . The controlled release oral pharmaceutical composition according to  claim 17 , wherein said mixture of ingredients in said tablet core further comprises microcrystalline cellulose, lactose, and colloidal silica. 
     
     
         19 . A controlled release oral pharmaceutical composition in the form of a tablet consisting essentially of:
 (1) a tablet core consisting of a mixture of ingredients, said ingredients comprising:
 a) 9 mg of budesonide; 
 b) hydroxypropyl cellulose; 
 c) stearic acid, or salt, alcohol or ester derivative thereof; and 
   (2) a gastro-resistant film coating on said tablet core, said coating comprising at least one methacrylic acid polymer or methacrylic acid copolymer.   
     
     
         20 . The controlled release oral pharmaceutical composition according to  claim 19 , wherein said mixture of ingredients in said tablet core further comprises microcrystalline cellulose, lactose, and colloidal silica. 
     
     
         21 . The controlled release oral pharmaceutical composition according to  claim 19 , wherein said gastro-resistant film coating further comprises triethyl citrate, talc and titanium dioxide. 
     
     
         22 . A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to  claim 1 . 
     
     
         23 . A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to  claim 2 . 
     
     
         24 . A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to  claim 6 . 
     
     
         25 . A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to  claim 7 . 
     
     
         26 . A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to  claim 8 . 
     
     
         27 . A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to  claim 9 . 
     
     
         28 . A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to  claim 13 . 
     
     
         29 . A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to  claim 17 . 
     
     
         30 . A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to  claim 19 .