Claims for Patent: 10,660,858

Summary for Patent: 10,660,858

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)
Application Number:	16/263,223
Patent Claims:	1. A tablet for the treatment of ulcerative colitis consisting essentially of (1) a tableted core, and (2) a coating on said tableted core, wherein said tableted core consists of a mixture comprising: (a) 9 mg of budesonide; (b) hydroxypropyl cellulose; and (c) starch or starch derivative; wherein said coating on said tableted core comprises a mixture of methacrylic acid copolymer type A and methacrylic acid copolymer type B in a weight to weight ratio of 1:1; wherein following oral administration of the tablet to a human, the tablet provides a C.sub.max of said budesonide in said human of about 1.35.+-.0.96 ng/mL; and wherein said tablet provides extended release of budesonide in the colon of said human effective to treat ulcerative colitis in said human. 2. The tablet of claim 1, wherein said mixture further comprises lactose. 3. The tablet of claim 1, wherein said mixture further comprises magnesium stearate. 4. The tablet of claim 2, wherein said mixture further comprises magnesium stearate. 5. The tablet of claim 1, wherein said mixture does not comprise stearic acid. 6. The tablet of claim 2, wherein said mixture does not comprise stearic acid. 7. The tablet of claim 3, wherein said mixture does not comprise stearic acid. 8. The tablet of claim 4, wherein said mixture does not comprise stearic acid. 9. The tablet of claim 1, wherein said coating on said tableted core further comprises triethylcitrate. 10. The tablet of claim 1, wherein following oral administration of the tablet to a human, the tablet provides a T.sub.max of said budesonide in said human of about 13.3.+-.5.9 hours. 11. The tablet of claim 2, wherein following oral administration of the tablet to a human, the tablet provides a T.sub.max of said budesonide in said human of about 13.3.+-.5.9 hours. 12. The tablet of claim 7, wherein following oral administration of the tablet to a human, the tablet provides a T.sub.max of said budesonide in said human of about 13.3.+-.5.9 hours. 13. The tablet of claim 4, wherein following oral administration of the tablet to a human, the tablet provides a T.sub.max of said budesonide in said human of about 13.3.+-.5.9 hours. 14. A tablet consisting essentially of (1) a tableted core, and (2) a gastro-resistant coating on said tableted core, wherein said tableted core consists of a compressed blend of ingredients, said ingredients comprising: (a) 9 mg of budesonide; (b) hydroxypropyl cellulose; and (c) magnesium stearate; wherein said gastro-resistant coating comprises a mixture of methacrylic acid copolymer type A, methacrylic acid copolymer type B and triethylcitrate, wherein said methacrylic acid copolymer type A and said methacrylic acid copolymer type B are present in said mixture in a weight to weight ratio of 1:1; wherein following oral administration of the tablet to a human, the tablet provides an AUC of said budesonide in said human of about 16.43.+-.10.52 (ng).times.(h)/mL, a C.sub.max of said budesonide in said human of about 1.35.+-.0.96 ng/mL, and a T.sub.max of said budesonide in said human of about 13.3.+-.5.9 hour; and wherein said tablet provides extended release of budesonide in the colon of said human effective to treat ulcerative colitis in said human. 15. The tablet of claim 14, wherein said ingredients further comprise starch or starch derivative. 16. The tablet of claim 15, wherein said ingredients comprise starch. 17. The tablet of claim 15, wherein said ingredients comprise starch derivative. 18. The tablet of claim 16, wherein said ingredients further comprise lactose. 19. The tablet of claim 17, wherein said ingredients further comprise lactose.