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Claims for Patent: 8,956,647

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Claims for Patent: 8,956,647

Title:Pellet formulation for the treatment of the intestinal tract
Abstract: An orally administrable pharmaceutical pellet formulation for the treatment of the intestinal tract is disclosed, which comprises a core and an enteric coating, the core including, as a pharmaceutical active compound, aminosalicylic acid or a pharmaceutically tolerable salt or a derivative thereof.
Inventor(s): Otterbeck; Norbert (Uberlingen, DE), Gruber; Peter (Merzhausen, DE)
Assignee: Dr. Falk Pharma GmbH (DE)
Application Number:13/951,951
Patent Claims: 1. An orally administrable pharmaceutical pellet formulation having a controlled release profile for the treatment of the intestinal tract, which comprises a core and an enteric coating, the core including aminosalicylic acid or a pharmaceutically acceptable salt thereof, wherein the aminosalicylic acid or pharmaceutically acceptable salt thereof is present in the core and homogenously dispersed in a non gel-forming polymer matrix comprising poly (ethylacrylate, methyl methacrylate) (2:1), wherein the polymer matrix is essentially insoluble in the intestinal tract and permeable to intestinal fluids and the aminosalicylic acid.

2. The pellet formulation of claim 1, wherein the poly (ethylacrylate, methyl methacrylate) (2:1) is present as a 40% strength aqueous dispersion.

3. The pellet formulation of claim 1, wherein the enteric coating comprises poly(methacrylic acid, methyl methacrylate) 1:1 or 1:2 with free carboxyl groups as functional groups.

4. The pellet formulation of claim 3, wherein the enteric coating comprises poly(methacylic acid-co-methyl methacrylate) 1:2 and poly(methacylic acid-co-methyl methacrylate) 1:1.

5. The pellet formulation of claim 1, wherein the matrix-forming polymer makes up at least 1% and up to approximately 21% by weight of the total weight of the core.

6. The pellet formulation of claim 1, wherein the pellet formulation is a capsule.

7. The pellet formulation of claim 1, wherein the pellets formulation is a tablet.

8. The pellet formulation of claim 1, wherein the pellets have a size of 0.1 to 3 mm.

9. The pellet formulation of claim 1, wherein the polymer matrix is water-insoluble in the intestinal tract.

10. An orally administrable pharmaceutical pellet formulation having a controlled release profile for the treatment of the intestinal tract, which comprises a core and an enteric coating, the core including aminosalicylic acid or a pharmaceutically acceptable salt thereof, wherein the aminosalicylic acid or pharmaceutically acceptable salt thereof is present in the core and homogenously dispersed in a polymer matrix comprising poly (ethylacrylate, methyl methacrylate) (2:1), wherein the polymer matrix is essentially insoluble in the intestinal tract and permeable to intestinal fluids and the aminosalicylic acid.

11. The pellet formulation of claim 10, wherein the poly (ethylacrylate, methyl methacrylate) (2:1) is present as a 40% strength aqueous dispersion.

12. The pellet formulation of claim 10, wherein the enteric coating comprises poly(methacrylic acid, methyl methacrylate) 1:1 or 1:2 with free carboxyl groups as functional groups.

13. The pellet formulation of claim 12, wherein the enteric coating comprises poly(methacylic acid-co-methyl methacrylate) 1:2 and poly(methacylic acid-co-methyl methacrylate) 1:1.

14. The pellet formulation of claim 10, wherein the matrix-forming polymer makes up at least 1% and up to approximately 21% by weight of the total weight of the core.

15. The pellet formulation of claim 10, wherein the polymer matrix comprises a non gel-forming polymer.

16. The pellet formulation of claim 10, wherein the matrix forming polymer makes up 10% by weight of the total weight of the core.

17. The pellet formulation of claim 10, wherein the polymer matrix is water-insoluble in the intestinal tract.

18. An orally administrable pharmaceutical pellet formulation having a controlled release profile for the treatment of the intestinal tract, which comprises a core and an enteric coating, the core including aminosalicylic acid or a pharmaceutically acceptable salt thereof, wherein the aminosalicylic acid or pharmaceutically acceptable salt thereof is present in the core and homogenously dispersed in a polymer matrix comprising poly (ethylacrylate, methyl methacrylate) (2:1), wherein the polymer matrix essentially insoluble in the intestinal tract and permeable to intestinal fluids and the aminosalicylic acid, and wherein the pellets have a size of 0.1 to 3 mm.

19. The pellet formulation of claim 18, wherein the poly (ethylacrylate, methyl methacrylate) (2:1) is present as a 40% strength aqueous dispersion.

20. The pellet formulation of claim 18, wherein the enteric coating comprises poly(methacrylic acid, methyl methacrylate) 1:1 or 1:2 with free carboxyl groups as functional groups.

21. The pellet formulation of claim 20, wherein the enteric coating comprises poly(methacylic acid-co-methyl methacrylate) 1:2 and poly(methacylic acid-co-methyl methacrylate) 1:1.

22. The pellet formulation of claim 18, wherein the matrix-forming polymer makes up at least 1% of the total weight of the core.

23. The pellet formulation of claim 18, wherein the polymer matrix comprises a non gel-forming polymer.

24. The pellet formulation as claimed in claim 18, wherein the pellets have a size of 0.5 to 1 mm.

25. The pellet formulation as claimed in claim 18, wherein the pellet formulation is a capsule.

26. The pellet formulation as claimed in claim 18, wherein the pellet formulation is a tablet.

27. The pellet formulation of claim 18, wherein the polymer matrix is water-insoluble in the intestinal tract.

28. A controlled release pellet formulation, comprising 1) homogeneously dispersed 5-aminosalicylic acid in a core comprising a polymer matrix comprising poly (ethylacrylate, methyl methacrylate) (2:1), wherein the polymer matrix is essentially insoluble in the intestinal tract and permeable to artificial intestinal juice, and wherein the polymer matrix comprises at least 1% by weight of the total weight of the core; and 2) an enteric coating; wherein, when administered to humans, the mean maximal plasma concentration of the 5-aminosalicylic acid is reached at about 4 hours after administration.

29. The controlled release pellet formulation of claim 28, wherein about 10-30% of the 5-aminosalicyclic acid is released from the formulation in 30 minutes at 37.degree. C. in artificial intestinal juice at a pH of about 6.8.

30. The controlled release pellet formulation of claim 28, wherein, when administered to humans, the mean maximal plasma concentration of acetyl-5-aminosalicylic acid is at about 5 hours after administration.

31. The controlled release pellet formulation of claim 28, wherein, when administered to humans, the ratio of the mean plasma concentration of 5-aminosalicyclic acid to the mean plasma concentration of acetyl-5-aminosalicylic acid at about 4 hours after administration is about 1:2.

32. The controlled release pellet formulation of claim 28, wherein, when administered to humans, the ratio of the mean plasma concentration of 5-aminosalicyclic acid to the mean plasma concentration of acetyl-5-aminosalicylic acid at about 6 hours after administration is about 1:3.

33. The controlled release pellet formulation of claim 28, wherein, when administered to humans, the ratio of the mean plasma concentration of 5-aminosalicyclic acid to the mean plasma concentration of acetyl-5-aminosalicylic acid at about 8 hours after administration is about 1:5.

34. The controlled release pellet formulation of claim 28, wherein, when the controlled release pellet formulation is administered to humans, the mean plasma concentration of 5-aminosalicyclic acid is less than about 1564 ng/ml at about 5 hours after administration.

35. The controlled release pellet formulation of claim 28, wherein, when administered to humans, the mean plasma concentration of 5-aminosalicyclic acid is less than about 924 ng/ml at about 6 hours after administration.

36. The controlled release pellet formulation of claim 28, wherein, when the controlled release pellet formulation is administered to humans, the mean plasma concentration of acetyl-5-aminosalicylic acid is less than about 2511 ng/ml at about 5 hours after administration.

37. The controlled release pellet formulation of claim 28, wherein, when administered to humans, the mean plasma concentration of acetyl-5-aminosalicylic acid is less than about 2243 ng/ml at about 6 hours after administration.

38. A controlled release pellet formulation comprising: homogeneously dispersed 5-aminosalicyclic acid in a polymer matrix comprising poly (ethylacrylate, methyl methacrylate) (2:1), wherein the polymer matrix is essentially insoluble in the intestinal tract and permeable to intestinal fluid; and an enteric coating; wherein, when administered to humans, the average cumulative fecal excretion of 5-aminosalicyclic acid is greater than 250 mg.

39. The controlled release pellet formulation of claim 38, wherein the average cumulative fecal excretion is measured approximately 72 hours after administration.

40. The controlled release pellet formulation of claim 39, wherein the average cumulative fecal excretion of 5-aminosalicyclic acid is greater than 280 mg.

41. The controlled release formulation of claim 40, wherein the polymer matrix comprises at least 1% by weight of the total weight of the core.

42. An orally administrable pharmaceutical pellet formulation having a controlled release profile for the treatment of the intestinal tract, which comprises a core and an enteric coating, the core including aminosalicylic acid or a pharmaceutically acceptable salt thereof, wherein the aminosalicylic acid or pharmaceutically acceptable salt thereof is present in the core and homogenously dispersed in a non gel-forming polymer matrix comprising poly (ethylacrylate, methyl methacrylate) (2:1), wherein the polymer matrix is essentially insoluble in the intestinal tract and permeable to intestinal fluids and the aminosalicylic acid, and wherein the matrix-forming polymer makes up at least 1% and up to approximately 21% by weight of the total weight of the core.

43. The pellet formulation of claim 42, wherein, when administered to humans, the mean maximal plasma concentration of the 5-aminosalicylic acid is reached at about 4 hours after administration.

44. The pellet formulation of claim 42, wherein the pellet formulation is a capsule.

45. The pellet formulation of claim 42, wherein the pellets formulation is a tablet.

46. The pellet formulation of claim 42, wherein the pellets have a size of 0.1 to 3 mm.

47. The pellet formulation of claim 42, wherein the polymer matrix is water-insoluble in the intestinal tract.

48. The pellet formulation of claim 42, wherein, when the controlled release pellet formulation is administered to humans, the mean plasma concentration of 5-aminosalicyclic acid is less than about 1564 ng/ml at about 5 hours after administration.

49. The pellet formulation of claim 42, wherein, when administered to humans, the average cumulative fecal excretion of 5-aminosalicyclic acid is greater than 250 mg.
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