Details for Patent: 9,737,489

Title:	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.
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:	Dec 05, 2016
Application Number:	15/368,911
Claims:	1. A method of treating a human subject with ulcerative colitis, comprising administering to said human subject an oral pharmaceutical composition in the form of a tablet consisting essentially of: (a) a tablet core comprising granules, said 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 subject of about 1.35.+-.0.96 ng/mL following said administration of said oral pharmaceutical composition to said human subject. 2. The method according to claim 1, wherein said oral pharmaceutical composition further provides a T.sub.max of said budesonide in said human subject of about 13.3.+-.5.9 hours following administration of said oral pharmaceutical composition to said human subject. 3. The method according to claim 1, wherein said oral pharmaceutical composition further provides an AUC.sub.0-infinity of said budesonide in said human subject of about 16.43.+-.10.52 (ng)(hr)/mL following said administration of said oral pharmaceutical composition to said human subject. 4. The method according to claim 1, wherein said oral pharmaceutical composition further provides an AUC.sub.0-t of said budesonide in said human subject of about 13.56.+-.7.82 (ng)(hr)/mL in 36 hours following said administration of said oral pharmaceutical composition to said human subject. 5. The method according to claim 1, wherein said gastro-resistant film in said oral pharmaceutical composition comprises methacrylic acid copolymer type A. 6. The method according to claim 1, wherein said oral pharmaceutical composition further provides: (1) a T.sub.max of said budesonide in said human subject of about 13.3.+-.5.9 hours; and (2) an AUC.sub.0-infinity of said budesonide in said human subject of about 16.43.+-.10.52 (ng)(hr)/mL, following said administration of said oral pharmaceutical composition to said human subject. 7. A method of treating a human subject with ulcerative colitis, comprising administering to said human subject an oral pharmaceutical composition in the form of a tablet consisting essentially of: (a) a tablet core comprising granules, said 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 subject of from about 0.49 ng/mL to about 4.23 ng/mL following said administration of said oral pharmaceutical composition to said human subject. 8. The method according to claim 7, wherein said oral pharmaceutical composition further provides a T.sub.max of said budesonide in said human subject of about 13.3.+-.5.9 hours following administration of said oral pharmaceutical composition to said human subject. 9. The method according to claim 7, wherein said oral pharmaceutical composition further provides an AUC.sub.0-infinity of said budesonide in said human subject of about 16.43.+-.10.52 (ng)(hr)/mL following said administration of said oral pharmaceutical composition to said human subject. 10. The method according to claim 7, wherein said oral pharmaceutical composition further provides an AUC.sub.0-t of said budesonide in said human subject of about 13.56.+-.7.82 (ng)(hr)/mL in 36 hours following said administration of said oral pharmaceutical composition to said human subject. 11. The method according to claim 7, wherein in said oral pharmaceutical composition said gastro-resistant film comprises methacrylic acid copolymer type A. 12. The method according to claim 7, wherein said oral pharmaceutical composition further provides: (1) a T.sub.max of said budesonide in said human subject of about 13.3.+-.5.9 hours; and (2) an AUC.sub.0-infinity of said budesonide in said human subject of about 16.43.+-.10.52 (ng)(hr)/mL, following said administration of said oral pharmaceutical composition to said human subject. 13. A method of treating a human subject with ulcerative colitis, comprising administering to said human subject an oral pharmaceutical composition in the form of a tablet consisting essentially of: (a) a tablet core comprising granules, said 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 C.sub.max of said budesonide in said human subject of about 1.35.+-.0.96 ng/mL following said administration of said oral pharmaceutical composition to said human subject. 14. The method according to claim 13, wherein said oral pharmaceutical composition further provides a T.sub.max of said budesonide in said human subject of about 13.3.+-.5.9 hours following administration of said oral pharmaceutical composition to said human subject. 15. The method according to claim 13, wherein said oral pharmaceutical composition further provides an AUC.sub.0-infinity of said budesonide in said human subject of about 16.43.+-.10.52 (ng)(hr)/mL following said administration of said oral pharmaceutical composition to said human subject. 16. The method according to claim 13, wherein said oral pharmaceutical composition further provides an AUC.sub.0-t of said budesonide in said human subject of about 13.56.+-.7.82 (ng)(hr)/mL in 36 hours following said administration of said oral pharmaceutical composition to said human subject. 17. The method according to claim 13, wherein in said oral pharmaceutical composition said gastro-resistant film comprises methacrylic acid copolymer type A. 18. The method according to claim 13, wherein said oral pharmaceutical composition further provides: (1) a T.sub.max of said budesonide in said human subject of about 13.3.+-.5.9 hours; and (2) an AUC.sub.0-infinity of said budesonide in said human subject of about 16.43.+-.10.52 (ng)(hr)/mL, following said administration of said oral pharmaceutical composition to said human subject.