FORMULATIONS AND USES OF 2-HYDROXY-5-PHENYLAZOBENZOIC ACID DERIVATIVES FOR THE TREATMENT OF MALES

• US 20120058184A1
• Filed: 04/26/2011
• Published: 03/08/2012
• Est. Priority Date: 04/26/2010
• Status: Active Grant

• Current Assignee: Salix Pharmaceuticals Incorporated (Bausch Health Cos., Inc.)
• Original Assignee: Salix Pharmaceuticals Limited (Bausch Health Cos., Inc.)
• Inventors: Forbes, William, Bortey, Enoch, Johnson, Lorin
• Granted Patent: US 8,497,256 B2
• Time in patent office: Days
• US Class Current: 424/474
• CPC Class Codes: A61K 31/655 Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
• CPC Class Codes: A61K 9/28 Dragees; Coated pills or tablets , e.g. with film or compression coating A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209
• CPC Class Codes: A61K 9/50 Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals A61K9/2081 takes precedence; particles with a single coating comprising drug A61K9/167
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 1/06 Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia

Abstract

The instant application provides methods and compositions for the treatment of male subjects having ulcerative colitis.

Claims

1. A method treating a gastrointestinal disorder comprising administering to a male subject in need of treatment a therapeutically effective amount of balsalazide.

2. The method claim 1, wherein the therapeutically effective amount comprises about 6.5 to about 6.8 g per day.

3. The method claim 1, wherein the therapeutically effective amount comprises about 6.6 g per day.

4. The method claim 1, wherein the therapeutically effective amount comprises about 6.75 g per day.

5. The method of claim 1, wherein the therapeutically effective amount is a dosage regimen of three tablets of the formulation two times each day, wherein each tablet comprises about 1100 mg of balsalazide.

6. The method of claim 5, wherein the balsalazide tablet is a film-coated tablet.

7. The method of claim 1, wherein the therapeutically effective amount is a dosage regimen of three capsules of the formulation three times each day, wherein each capsule comprises about 750 mg of balsalazide.

8. The method of claim 1, wherein the administration to the subject occurs between about 30 minutes prior to about 1 hour after consuming food.

9. The method of claim 1, wherein the gastrointestinal disorder comprises ulcerative colitis.

10. The method of claim 9, wherein the ulcerative colitis is mild to moderately active ulcerative colitis.

11. A method of decreasing a MMDAI score in a male subject having ulcerative colitis comprising administering to the subject a therapeutically effective amount of balsalazide, thereby decreasing the MMDAI score.

12. The method claim 11, wherein the therapeutically effective amount comprises between about 6.5 to about 6.8 g per day.

13. The method claim 11, wherein the therapeutically effective amount comprises about 6.6 g per day.

14. The method claim 11, wherein the therapeutically effective amount comprises about 6.75 g per day.

15. The method of claim 12, wherein the therapeutically effective amount is a dosage regimen of three tablets of the formulation two times each day, wherein each tablet comprises about 1100 mg of balsalazide.

16. The method of claim 15, wherein the balsalazide tablet is a film-coated tablet.

17. The method of claim 11, wherein the therapeutically effective amount is a dosage regimen of three capsules of the formulation three times each day, wherein each capsule comprises about 750 mg of balsalazide.

18. The method of claim 11, wherein the MMDAI score is decreased by 3 or more points.

19. The method of claim 11, wherein the rectal bleeding component of the MMDAI score is decreased by 1 or more points.

20. A method of inducing clinical remission of ulcerative colitis in a male subject comprising;

administering to the subject a therapeutically effective amount of balsalazide, thereby inducing remission in the subject.

21. The method claim 20, wherein the therapeutically effective amount comprises between about 6.5 to about 6.8 g per day.

22. The method claim 20, wherein the therapeutically effective amount comprises about 6.6 g per day.

23. The method claim 20, wherein the therapeutically effective amount comprises about 6.75 g per day.

24. The method of claim 21, wherein the therapeutically effective amount is a dosage regimen of three tablets of the formulation two times each day, wherein each tablet comprises about 1100 mg of balsalazide.

25. The method of claim 24, wherein the balsalazide tablet is a film-coated tablet.

26. The method of claim 20, wherein the therapeutically effective amount is a dosage regimen of three capsules of the formulation three times each day, wherein each capsule comprises about 750 mg of balsalazide.

27. The method of claim 20, wherein remission is defined by MMDAI component scores of zero for rectal bleeding and a combined score of 2 or less for bowel frequency and physician'"'"'s assessment.

28. A method of inducing mucosal healing in a male subject having ulcerative colitis comprising administering to the subject a therapeutically effective amount of balsalazide, thereby inducing mucosal healing in the subject.

29. The method claim 28, wherein the therapeutically effective amount comprises between about 6.5 to about 6.8 g per day.

30. The method claim 28, wherein the therapeutically effective amount comprises about 6.6 g per day.

31. The method claim 28, wherein the therapeutically effective amount comprises about 6.75 g per day.

32. The method of claim 29, wherein the therapeutically effective amount is a dosage regimen of three tablets of the formulation two times each day, wherein each tablet comprises about 1100 mg of balsalazide.

33. The method of claim 32, wherein the balsalazide tablet is a film-coated tablet.

34. The method of claim 28, wherein the therapeutically effective amount is a dosage regimen of three capsules of the formulation three times each day, wherein each capsule comprises about 750 mg of balsalazide.

35. The method of claim 28, wherein the mucosal healing is defined as an improvement in endoscopy/sigmoidoscopy score to 0 or 1.