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Claims for Patent: 8,956,651

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Claims for Patent: 8,956,651

Title:Oral formulations and lipophilic salts of methylnal trexone
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. (North Potomac, MD), Cohen; Jonathan Marc (Monroe, NY)
Assignee: Wyeth, LLC (Madison, NJ)
Application Number:13/966,779
Patent Claims: 1. A pharmaceutical composition for oral administration comprising a solid dosage of (i) methylnaltrexone, or a pharmaceutically acceptable salt thereof, and (ii) an amphiphilic pharmaceutically acceptable excipient, and wherein the composition comprises from about 7% to about 75% methylnaltrexone cation and an anion of the amphiphilic pharmaceutically acceptable excipient based upon the total weight of the composition and 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.

2. The pharmaceutical composition according to claim 1, wherein the amphiphilic pharmaceutically acceptable excipient has a pK.sub.a of 3 or less.

3. The pharmaceutical composition according to claim 1, wherein the amphiphilic pharmaceutically acceptable excipient comprises a sulfate (--OSO.sub.3.sup.-) group.

4. The pharmaceutical composition according to claim 1, wherein the amphiphilic pharmaceutically acceptable excipient comprises a saturated or unsaturated, branched or unbranched, cyclic or acyclic C.sub.4-30 aliphatic group that is optionally substituted.

5. The pharmaceutical composition according to claim 1, wherein the amphiphilic pharmaceutically acceptable excipient comprises a saturated, unbranched, acyclic, unsubstituted C.sub.4-30 alkyl group.

6. The pharmaceutical composition according to claim 1, wherein the amphiphilic pharmaceutically acceptable excipient comprises a saturated, unbranched, acyclic, unsubstituted C.sub.7-15 alkyl group.

7. The pharmaceutical composition according to claim 1, wherein the amphiphilic pharmaceutically acceptable excipient comprises a C.sub.12 n-alkyl group.

8. The pharmaceutical composition of claim 1, further comprising a disintegrant.

9. The pharmaceutical composition of claim 8, 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.

10. The composition of claim 8, 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 15 minutes.

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

12. The composition according to claim 11, wherein the apparent partition coefficient is at least 10.

13. The composition according to claim 12, wherein the apparent partition coefficient is at least 20.

14. The composition according to claim 1, wherein the amphiphilic pharmaceutically acceptable excipient is an anionic surfactant.

15. The composition according to claim 8, wherein the disintegrant is an effervescent disintegrant.

16. The composition according to claim 15, wherein the disintegrant is a bicarbonate.

17. The composition according to claim 1, wherein the composition is a tablet.

18. The composition according to claim 1, wherein the composition is a tablet comprising at least one or more of a binder, a chelating agent, a wetting agent, a lubricant, a non-functional coating, or an antioxidant, and combinations thereof.

19. The composition according to claim 18, wherein the composition comprises a chelating agent.

20. The composition according to claim 19, wherein the chelating agent is a salt of EDTA.

21. The composition according to claim 20, wherein the chelating agent is calcium EDTA disodium.

22. The composition according to claim 18, wherein the composition comprises a lubricant.

23. The composition according to claim 22, wherein the lubricant is magnesium stearate.

24. The composition according to claim 18, wherein the composition comprises an antioxidant.

25. The composition according to claim 24, wherein the antioxidant is ascorbic acid.

26. The composition according to claim 18, wherein the lubricant is magnesium stearate.

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

28. The pharmaceutical composition of claim 1, wherein the composition comprises a compound of formula (I): ##STR00006## wherein A.sup.- is an anion of the amphiphilic pharmaceutically acceptable excipient.

29. The pharmaceutical composition of claim 1, wherein the amphiphilic pharmaceutically acceptable excipient comprises dodecyl sulfate.

30. The pharmaceutical composition of claim 1, wherein the composition further comprises at least one or more of a binder, a chelating agent, a wetting agent, a lubricant, a non-functional coating, or an antioxidant, and combinations thereof.

31. The pharmaceutical composition of claim 30, wherein the composition further comprises a lubricant.
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