US2016206612A1PendingUtilityA1

Oral formulations and lipophilic salts of methylnaltrexone

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Assignee: WYETH LLCPriority: Mar 11, 2010Filed: Mar 15, 2016Published: Jul 21, 2016
Est. expiryMar 11, 2030(~3.6 yrs left)· nominal 20-yr term from priority
Inventors:Syed M. ShahChristopher DiorioEric C. EhrnspergerXu MengKadum A. Al ShareffiJonathan Marc Cohen
A61P 25/04A61P 1/10A61P 1/00A61P 1/14A61P 1/08A61K 47/20A61K 9/2013A61K 9/284A61K 9/2009A61K 9/2054A61K 47/12A61K 9/28A61K 31/485A61K 9/0053C07D 489/08A61K 9/2077
59
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Claims

Abstract

The present invention provides compositions comprising methylnaltrexone or a salt thereof, and compositions and formulations thereof, for oral administration.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A pharmaceutical composition for oral administration comprising a solid dosage of methylnaltrexone, or a pharmaceutically acceptable salt thereof, and an amphiphilic pharmaceutically acceptable excipient comprising (i) a saturated or unsaturated, branched or unbranched, cyclic or acyclic C 4-30  aliphatic group that is optionally substituted and that has a pKa of 3 or less; or (ii) a saturated, unbranched, acyclic, unsubstituted C 4-30  alkyl group; and wherein when the methylnaltrexone, or the pharmaceutically acceptable salt thereof, and the amphiphilic pharmaceutically acceptable excipient are in solution, the apparent octanol/water partition coefficient for methylnaltrexone is at least 0.25 at a pH between 1 and 4. 
     
     
         2 . The pharmaceutical composition of  claim 1 , wherein the methylnaltrexone, or a pharmaceutically acceptable salt thereof, and the amphiphilic pharmaceutically acceptable excipient 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 the amphiphilic pharmaceutically acceptable excipient 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 according to  claim 1 , wherein the pharmaceutically acceptable excipient comprises a sulfate (—OSO 3   − ) group. 
     
     
         6 . The pharmaceutical composition according to  claim 1 , wherein the pharmaceutically acceptable excipient comprises an acyclic C 4-30  aliphatic group that is optionally substituted. 
     
     
         7 . The pharmaceutical composition according to  claim 1 , wherein the pharmaceutically acceptable excipient comprises a saturated, unbranched, acyclic, unsubstituted C 7-15  alkyl group. 
     
     
         8 . The pharmaceutical composition according to  claim 1 , wherein the pharmaceutically acceptable excipient comprises a C 12  n-alkyl group. 
     
     
         9 . The pharmaceutical composition according to  claim 1 , wherein the pharmaceutically acceptable excipient is dodecyl sulfate. 
     
     
         10 . The pharmaceutical composition of  claim 9 , further comprising a disintegrant. 
     
     
         11 . 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° C. within about 15 minutes. 
     
     
         12 . The 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° C. within about 15 minutes. 
     
     
         13 . The composition of  claim 1 , wherein the composition in solution has an apparent octanol/water partition coefficient for methylnaltrexone of at least 1 at a pH between 1 and 4. 
     
     
         14 . The composition according to  claim 1 , wherein the apparent partition coefficient is at least 10, or at least 20. 
     
     
         15 . The composition according to  claim 1 , wherein the pharmaceutically acceptable excipient is an anionic surfactant. 
     
     
         16 . The composition according to  claim 10 , wherein the disintegrant is an effervescent disintegrant. 
     
     
         17 . The composition according to  claim 16 , wherein the disintegrant is a bicarbonate. 
     
     
         18 . The composition according to  claim 1 , wherein the composition is a tablet. 
     
     
         19 . 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. 
     
     
         20 . The composition according to  claim 19 , wherein the composition comprises a chelating agent. 
     
     
         21 . The composition according to  claim 20 , wherein the chelating agent is a salt of EDTA. 
     
     
         22 . The composition according to  claim 21 , wherein the chelating agent is calcium EDTA disodium. 
     
     
         23 . The composition according to  claim 19 , wherein the lubricant is magnesium stearate. 
     
     
         24 . The composition according to  claim 19 , wherein the antioxidant is ascorbic acid.

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