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Claims for Patent: 8,524,276

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Claims for Patent: 8,524,276

Title:Oral formulations and lipophilic salts of methylnaltrexone
Abstract: The present invention provides compositions comprising methylnaltrexone or a salt thereof, and compositions and formulations thereof, for oral administration.
Inventor(s): Shah; Syed M. (Delray Beach, FL), Diorio; Christopher Richard (Campbell Hall, NY), Ehrnsperger; Eric C. (New City, NY), Meng; Xu (San Diego, CA), Al Shareffi; Kadum A. (Greensboro, NC), Cohen; Jonathan Marc (Monroe, NY)
Assignee: Wyeth, LLC (Madison, NJ)
Application Number:13/045,108
Patent Claims: 1. A pharmaceutical composition for oral administration comprising a solid dosage of (i) methylnaltrexone, or a pharmaceutically acceptable salt thereof, and (ii) sodium dodecyl sulfate (SDS), wherein the composition is a tablet, and wherein the composition comprises from about 7% to about 75% methylnaltrexone cation and dodecyl sulfate anion, based upon the total weight of the composition.

2. The pharmaceutical composition of claim 1, wherein the methylnaltrexone, or a pharmaceutically acceptable salt thereof, and sodium dodecyl sulfate (SDS) form an ion pair when dissolved in solution.

3. The pharmaceutical composition of claim 2, wherein the ion pair is formed when the methylnaltrexone, or a pharmaceutically acceptable salt thereof, and sodium dodecyl sulfate (SDS) are dissolved in solution at a pH of greater than about 1 and less than about 4.

4. The pharmaceutical composition of claim 3, further comprising a disintegrant.

5. The pharmaceutical composition of claim 1, wherein at least 50% of the composition dissolves in a dissolution apparatus with paddles at 100 rpm in 900 mL of 0.1 N HCl at 37.degree. C. within about 15 minutes.

6. The composition of claim 5, wherein at least 75% of the composition dissolves in a dissolution apparatus with paddles at 100 rpm in 900 mL of 0.1 N HCl at 37.degree. C. within about 1.5 minutes.

7. The composition of claim 6, wherein at least 90% of the composition dissolves in a dissolution apparatus with paddles at 100 rpm in 900 mL of 0.1 N HCl at 37.degree. C. within about 10 minutes.

8. The composition of claim 1, wherein the composition in solution has an apparent octanol/water partition coefficient for methylnaltrexone of at least 0.25 at a pH between 1 and 4.

9. The composition according to claim 8, wherein the apparent partition coefficient is at least 1.

10. The composition according to claim 9, wherein the apparent partition coefficient is at least 10.

11. The composition according to claim 4, wherein the disintegrant is an effervescent disintegrant.

12. The composition according to claim 4, wherein the disintegrant is sodium bicarbonate.

13. The composition of claim 1, wherein the composition comprises at least one or more of a binder, a chelating agent, a wetting agent, a lubricant, a nonfunctional coating, or an antioxidant, and combinations thereof.

14. The composition according to claim 13, wherein the chelating agent is calcium EDTA disodium.

15. The composition according to claim 13, wherein the composition comprises a lubricant.

16. The composition according to claim 15, wherein the lubricant is magnesium stearate.

17. The composition according to claim 13, wherein the composition comprises an antioxidant.

18. The composition according to claim 17, wherein the antioxidant is ascorbic acid.

19. The composition according to claim 13, wherein the composition comprises: (a) about 7% to about 75% of methylnaltrexone bromide, based upon total weight of the composition; (b) about 5% to about 80% of sodium dodecyl sulfate (SDS), based upon total weight of the composition; (c) about 0.01% to about 5% of a chelating agent, based upon total weight of the composition; (d) about 1% to about 25% of a wetting agent, based upon total weight of the composition; (e) about 5% to about 90% of a binder, based upon total weight of the composition; (f) about 1% to about 25% of a disintegrant, based upon total weight of the composition; and (g) about 0.1% to about 7% of a lubricant, based upon total weight of the composition.

20. The composition according to claim 19, wherein the binder comprises a combination of microcrystalline cellulose and silicified microcrystalline cellulose.

21. The composition according to claim 19, wherein the disintegrant is crospovidone.

22. The composition according to claim 19, wherein the chelating agent is calcium EDTA.

23. The composition according to claim 19, wherein the wetting agent is polysorbate 80.

24. The composition according to claim 19, wherein the lubricant is magnesium stearate.

25. A multi-day pack comprising multiple unit dosage compositions of claim 10.

26. The composition according to claim 13, wherein the composition further comprises about 0.01% to about 5% of an antioxidant, based upon the total weight of the composition.

27. The composition according to claim 26, wherein the antioxidant is ascorbic acid.
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