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Claims for Patent: 8,496,965

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Claims for Patent: 8,496,965

Title:Pellet formulation for the treatment of the intenstinal tract
Abstract: An orally adminsterable 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)
Assignee: Dr. Falk Pharma GmbH (Freiburg, DE)
Application Number:13/586,585
Patent Claims: 1. A controlled release pellet formulation, comprising 1) homogeneously dispersed 5-aminosalicylic acid in a core comprising a polymer matrix, 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.

2. The controlled release pellet formulation of claim 1, 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.

3. The controlled release pellet formulation of claim 1, wherein about 40-60% of the 5-aminosalicyclic acid is released from the formulation in about 2 hours at 37.degree. C. in artificial intestinal juice at a pH of about 6.8.

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

5. The controlled release pellet formulation of claim 1, 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.

6. The controlled release pellet formulation of claim 1, 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.

7. The controlled release pellet formulation of claim 1, 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.

8. The controlled release pellet formulation of claim 1, 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.

9. The controlled release pellet formulation of claim 1, 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.

10. The controlled release pellet formulation of claim 1, 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.

11. The controlled release pellet formulation of claim 1, 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.

12. A controlled release pellet formulation comprising: 1) 5-aminosalicyclic acid in a core comprising a polymer matrix, wherein the polymer matrix is essentially insoluble in the intestinal tract and permeable to intestinal fluid, and wherein the polymer matrix comprises at least 1% by weight of the total weight of the core; and an enteric coating; wherein about 10-30% of the 5-aminosalicyclic acid is released from the formulation in about 30 minutes at 37.degree. C. in artificial intestinal juice at a pH of about 6.8.

13. The controlled release pellet formulation of claim 12, wherein about 40-60% of the 5-aminosalicyclic acid is released from the formulation in about 2 hours.

14. The controlled release pellet formulation of claim 12, wherein the 5-aminosalicyclic acid is homogeneously dispersed in the polymer matrix.

15. The controlled release pellet formulation of claim 12, 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.

16. The controlled release pellet formulation of claim 12, 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.

17. The controlled release pellet formulation of claim 12, 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.

18. The controlled release pellet formulation of claim 12, wherein, when administered to humans, the mean plasma concentration of 5-aminosalicyclic acid is less than about 1293 ng/ml at about 4 hours after administration.

19. The controlled release pellet formulation of claim 12, wherein, when administered to humans, the mean plasma concentration of 5-aminosalicyclic acid is less than about 1564 ng/ml at about 5 hours after administration.

20. The controlled release pellet formulation of claim 12, 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.

21. The controlled release pellet formulation of claim 12, wherein, when administered to humans, the mean plasma concentration of acetyl-5-aminosalicylic acid is less than about 1651 ng/ml at about 4 hours after administration.

22. The controlled release pellet formulation of claim 12, wherein, when 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.

23. The controlled release pellet formulation of claim 12, 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.

24. A controlled release pellet formulation comprising: 1) 5-aminosalicyclic acid in a core comprising a polymer matrix, wherein the polymer matrix is essentially insoluble in the intestinal tract and permeable to intestinal fluid, and wherein the polymer matrix comprises at least 1% by weight of the total weight of the core; and 2) an enteric coating; wherein the pellets have a particle size of 0.1 mm to 3 mm.

25. The controlled release pellet formulation of claim 24, wherein the pellets have a particle size of about 0.5 to about 1.0 mm.

26. The controlled release pellet formulation of claim 24, wherein the pellets have a particle size of about 1 mm.

27. The controlled release pellet formulation, of claim 1, wherein the pellets have a particle size of 0.1 mm to 3 mm.

28. The controlled release pellet formulation of claim 1, wherein the pellets have a particle size of about 1 mm.

29. The controlled release pellet formulation, of claim 12, wherein the pellets have a particle size of 0.1 mm to 3 mm.

30. The controlled release pellet formulation of claim 12, wherein the pellets have a particle size of about 1 mm.
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