Claims for Patent: 10,307,417

Summary for Patent: 10,307,417

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:	16/219,681
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,307,417
Patent Claims:	1. A pharmaceutical composition for oral administration comprising a solid dosage of (i) methylnaltrexone bromide, and (ii) sodium dodecyl sulfate (SDS), wherein the composition is a tablet, wherein methylnaltrexone bromide is the sole active agent, wherein the tablet is not enterically coated, and 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. 2. The pharmaceutical composition of claim 1, further comprising a rapid-acting disintegrant. 3. The pharmaceutical composition of claim 2, wherein the rapid-acting disintegrant is an effervescent disintegrant. 4. The pharmaceutical composition of claim 2, wherein the rapid-acting disintegrant is sodium bicarbonate. 5. The pharmaceutical composition of claim 1, 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. 6. The pharmaceutical composition of claim 5, 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 15 minutes. 7. The pharmaceutical composition of claim 1, wherein an ion pair forms when the methylnaltrexone bromide and sodium dodecyl sulfate (SDS) are dissolved in solution. 8. The pharmaceutical composition of claim 7, wherein the solution is at a pH of about 1 to about 4. 9. The pharmaceutical composition of claim 2, wherein an ion pair forms when the methylnaltrexone bromide and sodium dodecyl sulfate (SDS) are dissolved in solution. 10. The pharmaceutical composition of claim 9, wherein the solution is at a pH of about 1 to about 4. 11. The pharmaceutical 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. 12. The pharmaceutical composition of claim 11, wherein the apparent octanol/water partition coefficient for methylnaltrexone is at least 0.5. 13. The pharmaceutical composition of claim 11, wherein the apparent octanol/water partition coefficient for methylnaltrexone is at least 1. 14. The pharmaceutical composition of claim 1, wherein the ratio of methylnaltrexone bromide to sodium dodecyl sulfate in the tablet is about 3:1 by weight. 15. The pharmaceutical composition of claim 14, 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. 16. The pharmaceutical composition of claim 15, 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 15 minutes. 17. The pharmaceutical composition of claim 14, wherein an ion pair forms when the methylnaltrexone bromide and sodium dodecyl sulfate (SDS) are dissolved in solution. 18. The pharmaceutical composition of claim 17, wherein the solution is at a pH of about 1 to about 4. 19. The pharmaceutical composition of claim 1 made with methylnaltrexone bromide and sodium dodecyl sulfate in a ratio of about 3:1 by weight. 20. The pharmaceutical composition of claim 1, further comprising a chelating agent. 21. The pharmaceutical composition of claim 20, wherein the chelating agent is calcium EDTA disodium. 22. The pharmaceutical composition of claim 14, further comprising a chelating agent. 23. The pharmaceutical composition of claim 22, wherein the chelating agent is calcium EDTA disodium. 24. The pharmaceutical composition of claim 14, wherein the amount of methylnaltrexone bromide is about 150 mg. 25. The pharmaceutical composition of claim 24, wherein the amount of methylnaltrexone bromide is 150 mg and the amount of sodium dodecyl sulfate (SDS) is 50 mg. 26. The pharmaceutical composition of claim 17, wherein the amount of methylnaltrexone bromide is about 150 mg. 27. The pharmaceutical composition of claim 26, wherein the amount of methylnaltrexone bromide is 150 mg and the amount of sodium dodecyl sulfate (SDS) is 50 mg. 28. The pharmaceutical composition of claim 19, wherein the amount of methylnaltrexone bromide is about 150 mg. 29. The pharmaceutical composition of claim 28, wherein the amount of methylnaltrexone bromide is 150 mg and the amount of sodium dodecyl sulfate (SDS) is 50 mg.