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Claims for Patent: 9,192,581

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Claims for Patent: 9,192,581

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 (Milano, IT), Fossati; Lorenzo (Milano, IT)
Assignee: COSMO TECHNOLOGIES LIMITED (Dublin, IE)
Application Number:14/491,363
Patent Claims: 1. An oral dosage form being in the form of a tablet comprising: an extended release core comprising a homogeneous dispersion of granules in a hydrophilic matrix, wherein said granules comprise 9 mg of budesonide, at least one lipophilic or inert component, and at least one amphiphilic component; and a gastro-resistant coating to control the release of said budesonide from said dosage form, wherein following oral administration of a single dose, the dosage form provides an AUC.sub.0-infinity of said budesonide in said human of about 16431.2 (mean).+-.10519.8 (pg)(hr)/mL, and wherein said dosage form provides extended release of budesonide in the colon effective to treat ulcerative colitis in the human.

2. The oral dosage form of claim 1, wherein following oral administration of a single dose, the dosage form provides a systemic availability of budesonide in the colon (AUC.sub.colon) of said human that accounts for between 84.93% and 100% of the total systemic availability (AUC.sub.t) of budesonide in the human.

3. The oral dosage form of claim 1, wherein following oral administration of a single dose, the dosage form provides a mean systemic availability of budesonide in the colon (AUC.sub.colon) of said human of about 95.88.+-.4.19% of the total systemic availability (AUC.sub.t) of budesonide in the human.

4. The oral dosage form of claim 1, wherein following oral administration of a single dose, the dosage form provides a T.sub.max of budesonide in said human of about 13.3.+-.5.9 hours.

5. The oral dosage form of claim 1, wherein following oral administration of a single dose, the dosage form achieves a Xu.sub.0-36 h of 6-.beta.-hydroxy-budesonide from said human of about 111061.9.+-.53992.6 ng.

6. The oral dosage form of claim 1, wherein said gastro-resistant coating dissolves at a pH of 7.2.

7. The oral dosage form of claim 6, wherein said gastro-resistant coating contains a mixture of methacrylic acid copolymers type A and type B.

8. The oral dosage form of claim 7, wherein said gastro-resistant coating further contains triethylcitrate.

9. The oral dosage form of claim 8, wherein said gastro-resistant coating further contains talc.

10. The oral dosage form of claim 9, wherein said gastro-resistant coating further contains titanium dioxide.

11. The oral dosage form of claim 1, wherein said extended release core incorporates budesonide-containing granules in a hydrogel composition, said hydrogel composition comprising hydroxypropylcellulose.

12. The oral dosage form of claim 11, wherein within the granules, budesonide is at least partially incorporated in lecithin and stearic acid.

13. The oral dosage form of claim 12, wherein within the granules, budesonide is wholly contained in lecithin and stearic acid.

14. The oral dosage form of claim 12, wherein said granules further comprise hydroxylpropylcellulose.

15. A method of treating a human subject with ulcerative colitis comprising administering the oral dosage form according to claim 1 to the human subject.

16. The oral dosage form of claim 11, wherein said extended release core further comprises microcrystalline cellulose, lactose, silicon-dioxide, and magnesium stearate.

17. An oral dosage form being in the form of a tablet comprising: an extended release core comprising a homogeneous dispersion of granules in a hydrophilic matrix, wherein said granules comprise 9 mg of budesonide, at least one lipophilic or inert component, and at least one amphiphilic component; and a gastro-resistant coating to control the release of said budesonide from said dosage form, wherein following oral administration of a single dose, the dosage form provides an AUC0-t of said budesonide in said human of about 13555.9.+-.7816.9 (pg).times.(h)/mL, and wherein said dosage form provides extended release of budesonide in the colon effective to treat ulcerative colitis in the human.

18. The oral dosage form of claim 17, wherein following oral administration of a single dose, the dosage form provides a systemic availability of budesonide in the colon (AUC.sub.colon) of said human that accounts for between 84.93% and 100% of the total systemic availability (AUC.sub.t) of budesonide in the human.

19. The oral dosage form of claim 17, wherein following oral administration of a single dose, the dosage form provides a mean systemic availability of budesonide in the colon (AUC.sub.colon) of said human of about 95.88.+-.4.19% of the total systemic availability (AUC.sub.t) of budesonide in the human.

20. The oral dosage form of claim 17, wherein following oral administration of a single dose, the dosage form provides a T.sub.max of budesonide in said human of about 13.3.+-.5.9 hours.

21. The oral dosage form of claim 17, wherein following oral administration of a single dose, the dosage form achieves a Xu.sub.0-36 h of 6-.beta.-hydroxy-budesonide from said human of about 111061.9.+-.53992.6 ng.

22. The oral dosage form of claim 17, wherein said gastro-resistant coating dissolves at a pH of 7.2.

23. The oral dosage form of claim 22, wherein said gastro-resistant coating contains a mixture of methacrylic acid copolymers type A and type B.

24. The oral dosage form of claim 23, wherein said gastro-resistant coating further contains triethylcitrate.

25. The oral dosage form of claim 24, wherein said gastro-resistant coating further contains talc.

26. The oral dosage form of claim 25, wherein said gastro-resistant coating further contains titanium dioxide.

27. The oral dosage form of claim 17, wherein said extended release core incorporates budesonide-containing granules in a hydrogel composition, said hydrogel composition comprising hydroxypropylcellulose.

28. The oral dosage form of claim 27, wherein within the granules, budesonide is at least partially incorporated in lecithin and stearic acid.

29. The oral dosage form of claim 28, wherein said granules further comprise hydroxylpropylcellulose.

30. A method of treating a human subject with ulcerative colitis comprising administering the oral dosage form according to claim 17 to the human subject.

31. The oral dosage form of claim 1, wherein said granules comprise 9 mg of budesonide, at least one lipophilic component, and at least one amphiphilic component.

32. The oral dosage form of claim 17, wherein said granules comprise 9 mg of budesonide, at least one lipophilic component, and at least one amphiphilic component.
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