Details for Patent: 9,532,954

Title:	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.
Inventor(s):	Villa; Roberto (Lecco, IT), Pedrani; Massimo (Gignese, IT), Ajani; Mauro (Milan, IT), Fossati; Lorenzo (Milan, IT)
Assignee:	COSMO TECHNOLOGIES LIMITED (Dublin, IE)
Filing Date:	Jun 18, 2014
Application Number:	14/308,305
Claims:	1. A tablet consisting essentially of (a) a tableted core and (b) a gastro-resistant film coating on the tableted core, wherein the tableted core comprises granules dispersed in a composition comprising at least a first hydrophilic compound, wherein the granules comprise: (a) budesonide; (b) at least one amphiphilic compound; and (c) at least one lipophilic compound. 2. The tablet according to claim 1, wherein the first hydrophilic compound is water-swellable. 3. The tablet according to claim 1, wherein the first hydrophilic compound is selected from the group consisting of an acrylic or methacrylic acid polymer or copolymer, an alkylvinyl polymer, a hydroxyalkyl cellulose, a carboxyalkyl cellulose, a polysaccharide, dextrin, pectin, starch, a natural or synthetic gum, and alginic acid. 4. The tablet according to claim 1, wherein the first hydrophilic compound is a hydroxyalkyl cellulose or a carboxyalkyl cellulose. 5. The tablet according to claim 4, wherein the first hydrophilic compound is a hydroxyalkyl cellulose. 6. The tablet according to claim 1, wherein the at least one amphiphilic compound is selected from the group consisting of lecithin, phosphatidylcholine, phosphatidylethanolamine, ceramide, and a glycol alkyl ether. 7. The tablet according to claim 1, wherein the at least one amphiphilic compound is lecithin. 8. The tablet according to claim 1, wherein the at least one lipophilic compound is selected from the group consisting of an unsaturated or hydrogenated alcohol or fatty acid, salt, ester, or amide thereof, a fatty acids mono-, di- or triglyceride, or a polyethoxylated derivative thereof, a wax, ceramide, and a cholesterol derivative. 9. The tablet according to claim 1, wherein the at least one lipophilic compound is stearic acid. 10. The tablet according to claim 1, wherein the gastro-resistant film coating comprises acrylic and/or methacrylic acid polymers, or copolymers, or cellulose derivatives. 11. The tablet according to claim 1, wherein the granules further comprise at least a second hydrophilic compound, wherein the second hydrophilic compound is the same or different than the first hydrophilic compound. 12. The tablet according to claim 11, wherein the second hydrophilic compound is selected from the group consisting of an acrylic or methacrylic acid polymer or copolymer, an alkylvinyl polymer, a hydroxyalkyl cellulose, a carboxyalkyl cellulose, a polysaccharide, dextrin, pectin, starch, a natural or synthetic gum, and alginic acid. 13. The tablet according to claim 11, wherein the second hydrophilic compound is a hydroxyalkyl cellulose or a carboxyalkyl cellulose. 14. The tablet according to claim 11, wherein the second hydrophilic compound is a hydroxyalkyl cellulose. 15. A tablet consisting essentially of (a) a tableted core and (b) a gastro-resistant film coating on the tableted core, wherein the tableted core comprises granules dispersed in at least one hydrophilic matrix, wherein the granules comprise: (a) budesonide; (b) at least one amphiphilic compound; and (c) at least one lipophilic compound. 16. The tablet according to claim 15, wherein the at least one hydrophilic matrix is water-swellable. 17. The tablet according to claim 15, wherein the at least one hydrophilic matrix comprises at least one hydrophilic compound selected from the group consisting of an acrylic or methacrylic acid polymer or copolymer, an alkylvinyl polymer, a hydroxyalkyl cellulose, a carboxyalkyl cellulose, a polysaccharide, dextrin, pectin, starch, a natural or synthetic gum, and alginic acid. 18. The tablet according to claim 15, wherein the at least one hydrophilic matrix comprises a hydroxyalkyl cellulose or a carboxyalkyl cellulose. 19. The tablet according to claim 18, wherein the at least one hydrophilic matrix comprises hydroxyalkyl cellulose. 20. The tablet according to claim 15, wherein the at least one amphiphilic compound is selected from the group consisting of lecithin, phosphatidylcholine, phosphatidylethanolamine, ceramide, and a glycol alkyl ether. 21. The tablet according to claim 15, wherein the at least one amphiphilic compound is lecithin. 22. The tablet according to claim 15, wherein the at least one lipophilic compound is selected from the group consisting of an unsaturated or hydrogenated alcohol or fatty acid, salt, ester, or amide thereof, a fatty acids mono-, di- or triglyceride, or a polyethoxylated derivative thereof, a wax, ceramide, and a cholesterol derivative. 23. The tablet according to claim 15, wherein the at least one lipophilic compound is stearic acid. 24. The tablet according to claim 15, wherein the gastro-resistant film coating comprises acrylic and/or methacrylic acid polymers, or copolymers, or cellulose derivatives. 25. The tablet according to claim 15, wherein the granules further comprise at least one hydrophilic compound. 26. The tablet according to claim 25, wherein the at least one hydrophilic compound in the granules is selected from the group consisting of an acrylic or methacrylic acid polymer or copolymer, an alkylvinyl polymer, a hydroxyalkyl cellulose, a carboxyalkyl cellulose, a polysaccharide, dextrin, pectin, starch, a natural or synthetic gum, and alginic acid. 27. The tablet according to claim 25, wherein the at least one hydrophilic compound in the granules is a hydroxyalkyl cellulose or a carboxyalkyl cellulose. 28. The tablet according to claim 25, wherein the hydrophilic compound in the granules is a hydroxyalkyl cellulose. 29. A tablet consisting essentially of (a) a tableted core and (b) a gastro-resistant film coating on the tableted core, wherein the gastro-resistant film comprises methacrylic acid polymers and/or copolymers, wherein the tableted core comprises: (i) a matrix comprising a hydroxyalkyl cellulose and/or a carboxyalkyl cellulose; and (ii) granules dispersed in the matrix, wherein the granules comprise: (a) budesonide; (b) lecithin; and (c) stearic acid. 30. The tablet of claim 1, wherein the tableted core further comprises at least one compound selected from the group consisting of a chitosan, a polyacrylamide, a natural or synthetic gum, and an acrylic acid polymer. 31. The tablet of claim 15, wherein the tableted core further comprises at least one compound selected from the group consisting of a chitosan, a polyacrylamide, a natural or synthetic gum, and an acrylic acid polymer. 32. The tablet of claim 29, wherein the tableted core further comprises at least one compound selected from the group consisting of a chitosan, a polyacrylamide, a natural or synthetic gum, and an acrylic acid polymer. 33. The tablet of claim 1, wherein the tableted core further comprises microcrystalline cellulose. 34. The tablet of claim 15, wherein the tableted core further comprises microcrystalline cellulose. 35. The tablet of claim 29, wherein the tableted core further comprises microcrystalline cellulose. 36. A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to claim 1. 37. A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to claim 15. 38. A method for treating intestinal inflammatory disease comprising administering to a patient the controlled release oral pharmaceutical composition according to claim 29.