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Claims for Patent: 7,452,872

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Claims for Patent: 7,452,872

Title:Formulations and uses of 2-hydroxy-5-phenylazobenzoic acid derivatives
Abstract:A method of increasing the bioavailability of balsalazide by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of balsalazide in a suitable container and associated with printed labeling which describes the increased bioavailability of the medication in the container when taken with food.
Inventor(s): Johnson; Lorin (Palo Alto, CA)
Assignee: Salix Pharmaceuticals, Inc. (Morrisville, NC)
Application Number:11/835,897
Patent Claims: 1. A method of increasing the bioavailability of balsalazide and metabolites 5-aminosalicylic acid (5-ASA) and N-acetyl-5-ASA (NASA) comprising administering to a subject a therapeutically effective amount of a solid dosage form of balsalazide with food, wherein the solid dosage form is a tablet or capsule, wherein administering with food comprises administering the solid dosage form within 15 minutes after eating a meal, wherein the bioavailability of balsalazide, 5-ASA or NASA is increased compared to administering balsalazide without food, and wherein the method decreases the systemic adsorption of the 5-ASA and NASA metabolites.

2. The method of claim 1, wherein the bioavailability increase is due to: a delay of the transit of the balsalazide, 5-ASA or NASA in the colon of a subject; a decrease in the systemic level of 5-ASA or NASA in a subject; increasing conversion of balsalazide to 5-ASA and 5-ASA to NASA in a subject; increasing the systemic ratio of NASA to 5-ASA in a subject; a decrease in the maximal plasma concentration (C.sub.max) of balsalazide by a ratio of from between about 0.497 to about 1 .048, or to 5-ASA by a ratio of from between about 0.292 and about 0.620 or to NASA by a ratio of from between about 0.473 and about 0.809 in a subject; or , delaying T.sub.max of balsalazide to from between about 0.09 to about 2.31 hours, 5-ASA to from between about 13.77 to about 30.23 hours or NASA to from between about 11.26 to about 29.14 hours in a subject; or decreasing the extent of absorption (AUC.sub.last) of 5-ASA to from between about -480.91 to about 4673.71 nghr/mL or by a ratio of from between about 0.401 to about 0.864 or NASA to from between about 4006.69 to about 31447.71 nghr/mL or by a ratio of from between about 0.649 to about 1 .034 in a subject.

3. The method of claim 1, wherein the therapeutically effective amount comprises from between about 6.25 mg to about 14000 mg/day.

4. The method of claim 1, wherein the therapeutically effective amount comprises from between about 750 mg to about 6750 mg/day.

5. The method of claim 1, wherein the therapeutically effective amount comprises from between about 1100 mg to about 13200 mg/day.

6. 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.

7. 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.

8. The method of claim 1, wherein the food comprises high-fat meal.

9. A method of increasing the bioavailability of balsalazide and metabolites 5-aminosalicylic acid (5-ASA) and N-acetyl-5-ASA (NASA) comprising administering to a subject a therapeutically effective amount of a solid dosage form of balsalazide with food, wherein the solid dosage form is a tablet or capsule, wherein with food comprises administering the balsalazide immediately after the consumption of food, wherein the bioavailability of balsalazide, 5-ASA or NASA is increased compared to administering balsalazide without food, and wherein the method decreases the systemic adsorption of the 5-ASA and NASA metabolites.

10. A method for increasing the time to maximum plasma concentration (T.sub.max) of a metabolite of balsalazide in a subject comprising administering to the subject a solid dosage form of balsalazide with food wherein the solid dosaQe form is a tablet or capsule, wherein the T.sub.max of the metabolite is increased as compared to administering the solid dosage form of balsalazide without food.

11. The method of claim 10, wherein the metabolite is 5-aminosalicylic acid (5-ASA) and the T.sub.max is reached at about 22 hours after the administration.

12. The method of claim 10, wherein the metabolite is N-acetyl-5-aminosalicylic acid (NASA), and the Tmax is reached at about 20 hours after the administration.

13. The method of claim 10, wherein the balsalazide is administered in a dose of three tablets, each tablet comprising about 1100 mg of balsalazide.

14. The method of claim 10, wherein the balsalazide is administered in a dose of three capsules, each capsule comprising about 750 mg of balsalazide.

15. The method of claim 14, wherein the about 750 mg capsules of balsalazide comprise propylene glycol.

16. The method of claim 10, wherein the subject is a healthy subject.

17. The method of claim 10, wherein the administration results in a T.sub.max, C.sub.max and AUC of the metabolite in the subject substantially according to Table 1, Treatment B (High-fat Diet).

18. The method of claim 10, wherein the food comprises a high-fat meal.

19. The method of claim 10, wherein the balsalazide is taken within 15 minutes of a meal.

20. The method of claim 10, wherein the balsalazide is taken immediately following a meal.
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