Oral formulations and lipophilic salts of methylnaltrexone
AssigneeWyeth
InventorsSyed M. Shah, Christopher Richard Diorio, Eric C. Ehrnsperger, Xu Meng, Kadum A. Al Shareffi, Jonathan Marc Cohen
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Abstract
The present invention provides compositions comprising methylnaltrexone or a salt thereof, and compositions and formulations thereof, for oral administration.
Claims40
A pharmaceutical composition for oral administration comprising a solid dosage of (i) methylnaltrexone, or a pharmaceutically acceptable salt thereof, and (ii) and an amphiphilic pharmaceutically acceptable excipient comprising a saturated or unsaturated, branched or unbranched, cyclic or acyclic C4-30 aliphatic group that is optionally substituted, 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.
A pharmaceutical composition for oral administration comprising a solid dosage of a compound of formula (I):
- wherein A− is an anion of the amphiphilic pharmaceutically acceptable excipient comprising a saturated or unsaturated, branched or unbranched, cyclic or acyclic C4-30 aliphatic group that is optionally substituted, wherein when the compound of formula I is in solution, the apparent octanol/water partition coefficient is at least 0.25 at a pH between 1 and 4.
Dependencies are inferred from the claim text.