Details for Patent: 9,132,093

Title:	Controlled release and taste making 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.
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:	Aug 14, 2012
Application Number:	13/585,190
Claims:	1. An oral pharmaceutical composition administered to a human, wherein said oral pharmaceutical composition is in the form of a tablet, said tablet comprising: (a) a tablet core comprising: granules comprising 9 mg of budesonide, lipophilic or inert matrix, and at least one amphiphilic matrix, wherein said granules are dispersed in a composition comprising a hydrophilic matrix; and (b) a tablet coating comprising a gastro-resistant film, wherein said gastro-resistant film comprises: a plasticizer and at least one methacrylic acid copolymer, and wherein said oral pharmaceutical composition provides a mean C.sub.max of said budesonide in said human of about 1348.8.+-.958.8 pg/mL following said administration of said oral pharmaceutical composition to said human. 2. The oral pharmaceutical composition administered to a human according to claim 1, wherein said oral pharmaceutical composition further provides a mean T.sub.max of said budesonide in said human of about 13.3.+-.5.9 hours following administration of said oral pharmaceutical composition to said human. 3. The oral pharmaceutical composition administered to a human according to claim 1, wherein said oral pharmaceutical composition further provides a mean AUC.sub.0-infinity of said budesonide in said human of about 16431.2.+-.10519.8 (pg)(hr)/mL following said administration of said oral pharmaceutical composition to said human. 4. The oral pharmaceutical composition administered to a human according to claim 1, wherein said oral pharmaceutical composition further provides a mean AUC.sub.0-t of said budesonide in said human of about 13555.9.+-.7816.9 (pg)(hr)/mL in 36 hours following said administration of said oral pharmaceutical composition to said human. 5. The oral pharmaceutical composition administered to a human according to claim 1, wherein said gastro-resistant film comprises methacrylic acid copolymer type A. 6. The oral pharmaceutical composition administered to a human according to claim 1, wherein said oral pharmaceutical composition is in the form of a tablet that is swallowed whole without chewing by said human. 7. The oral pharmaceutical composition administered to a human according to claim 1 wherein said oral pharmaceutical composition further provides following administration of said oral pharmaceutical composition to said human: (1) a mean T.sub.max of said budesonide in said human of about 13.3.+-.5.9 hours; and (2) a mean AUC.sub.0-infinity of said budesonide in said human of about 16431.2.+-.10519.8 (pg)(hr)/mL. 8. The oral pharmaceutical composition administered to a human according to claim 1, wherein said gastro-resistant film further comprises talc. 9. An oral pharmaceutical composition administered to a human, wherein said oral pharmaceutical composition is in the form of a tablet, said tablet comprising: (a) a tablet core comprising: granules comprising 9 mg of budesonide, stearic acid, and lecithin, wherein said granules are dispersed in a composition comprising hydroxypropyl cellulose; and (b) a tablet coating comprising a gastro-resistant film, wherein said gastro-resistant film comprises: a plasticizer and at least methacrylic acid copolymer, and wherein said oral pharmaceutical composition provides a mean Cmax of said budesonide in said human of about 1348.8.+-.958.8 pg/mL following said administration of said oral pharmaceutical composition to said human. 10. An oral pharmaceutical composition administered to a human according to claim 9, wherein said oral pharmaceutical composition further provides a mean T.sub.max of said budesonide in said human of about 13.3.+-.5.9 hours following said administration of said oral pharmaceutical composition to said human. 11. An oral pharmaceutical composition administered to a human according to claim 9, wherein said oral pharmaceutical composition further provides a mean AUC.sub.0-infinity of said budesonide in said human of about 16431.2.+-.10519.8 (pg)(hr)/mL following said administration of said oral pharmaceutical composition to said human. 12. The oral pharmaceutical composition administered to a human according to claim 9, wherein said oral pharmaceutical composition further provides a mean AUC.sub.0-1 of said budesonide in said human of about 13555.9.+-.7816.9 (pg)(hr)/mL in 36 hours following said administration of said oral pharmaceutical composition to said human. 13. The oral pharmaceutical composition administered to a human according to claim 9, wherein said gastro-resistant film comprises methacrylic acid copolymer type A. 14. The oral pharmaceutical composition administered to a human according to claim 9, wherein said oral pharmaceutical composition is in the form of a tablet that is swallowed whole without chewing by said human. 15. The oral pharmaceutical composition administered to a human according to claim 9, wherein said gastro-resistant film further comprises talc. 16. An oral pharmaceutical composition administered to a human, wherein said oral pharmaceutical composition is in the form of a tablet, said tablet comprising: (a) a tablet core comprising: granules comprising 9 mg of budesonide, at least one lipophilic or inert matrix, and at least one amphiphilic matrix, wherein said granules are dispersed in a composition comprising at least one hydrophilic matrix; and (b) a tablet coating comprising a gastro-resistant film, wherein said gastro-resistant film comprises: a plasticizer and at least one methacrylic acid copolymer, and wherein said oral pharmaceutical composition provides a C.sub.max of said budesonide in said human of from about 485 pg/mL to about 4227 pg/mL following said administration of said oral pharmaceutical composition to said human. 17. The oral pharmaceutical composition administered to a human according to claim 16, wherein said oral pharmaceutical composition provides a T.sub.max of said budesonide in said human of from about 6 hours to about 24 hours following said administration of said oral pharmaceutical composition to said human. 18. The oral pharmaceutical composition administered to a human according to claim 16, wherein said oral pharmaceutical composition further provides a mean AUC.sub.0-infinity of said budesonide in said human of about 16431.2.+-.10519.8 (pg)(hr)/mL following said administration of said oral pharmaceutical composition to said human. 19. The oral pharmaceutical composition administered to a human according to claim 16, wherein said oral pharmaceutical composition further provides a mean AUC.sub.0-1 of said budesonide in said human of about 13555.9.+-.7816.9 (pg)(hr)/mL in 36 hours following said administration of said oral pharmaceutical composition to said human. 20. The oral pharmaceutical composition administered to a human according to claim 16, wherein said gastro-resistant film comprises methacrylic acid copolymer type A. 21. The oral pharmaceutical composition administered to a human according to claim 16, wherein said oral pharmaceutical composition is in the form of a tablet that is swallowed whole without chewing by said human. 22. The oral pharmaceutical composition administered to a human according to claim 16, wherein said gastro-resistant film further comprises talc. 23. An oral pharmaceutical composition administered to a human, wherein said oral pharmaceutical composition is in the form of a tablet, said tablet comprising: (a) a tablet core comprising: granules comprising 9 mg of budesonide, stearic acid, and lecithin, wherein said granules are dispersed in a composition comprising hydroxypropyl cellulose; and (b) a tablet coating comprising a gastro-resistant film, wherein said gastro-resistant film comprises: a plasticizer and at least one methacrylic acid copolymer, and wherein said oral pharmaceutical composition provides a C.sub.max of said budesonide in said human of from about 485 pg/mL to about 4227 pg/mL following said administration of said oral pharmaceutical composition to said human. 24. The oral pharmaceutical composition administered to a human according to claim 23, wherein said oral pharmaceutical composition provides a T.sub.max of said budesonide in said human of from about 6 hours to about 24 hours following said administration of said oral pharmaceutical composition to said human. 25. The oral pharmaceutical composition administered to a human according to claim 23, wherein said oral pharmaceutical composition further provides a mean AUC.sub.0-infinity of said budesonide in said human of about 16431.2.+-.10519.8 (pg)(hr)/mL following said administration of said oral pharmaceutical composition to said human. 26. The oral pharmaceutical composition administered to a human according to claim 23, wherein said oral pharmaceutical composition further provides a mean AUC.sub.0-1 of said budesonide in said human of about 13555.9.+-.7816.9 (pg)(hr)/mL in 36 hours following said administration of said oral pharmaceutical composition to said human. 27. The oral pharmaceutical composition administered to a human according to claim 23, wherein said gastro-resistant film comprises methacrylic acid copolymer type A. 28. The oral pharmaceutical composition administered to a human according to claim 23, wherein said oral pharmaceutical composition is in the form of a tablet that is swallowed whole without chewing by said human. 29. The oral pharmaceutical composition administered to a human according to claim 23, wherein said gastro-resistant film further comprises talc.