N-ethyl-n-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide, preparation and uses thereof

Abstract

The subject invention provides a pharmaceutical composition containing laquinimod or a pharmaceutically acceptable salt thereof, and a compound of N-ethyl-N-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide or a salt thereof.

What is claimed is: 
     
         1 - 21 . (canceled) 
     
     
         22 . A pharmaceutical composition comprising laquinimod or a pharmaceutically acceptable salt thereof, at least one pharmaceutically acceptable carrier, and a light-resistant coating wherein the coating is resistant to light with wavelength in the range of 310-400 nm. 
     
     
         23 . The pharmaceutical composition of  claim 22 , wherein the light-resistant coating is a coating comprising titanium dioxide. 
     
     
         24 . The pharmaceutical composition of  claim 22  which is a solid pharmaceutical composition. 
     
     
         25 . The pharmaceutical composition of  claim 22 , in the form of a tablet. 
     
     
         26 . The pharmaceutical composition of  claim 22 , in the form of a capsule. 
     
     
         27 . The pharmaceutical composition of  claim 22 , in light-resistant packaging. 
     
     
         28 . The pharmaceutical composition of  claim 27 , wherein the light-resistant packaging is an opaque blister pack or an opaque high density polyethylene (HPDE) container. 
     
     
         29 - 56 . (canceled) 
     
     
         57 . The pharmaceutical composition of  claim 27 , wherein the light-resistant packaging is a sealed package. 
     
     
         58 . The pharmaceutical composition of  claim 27 , wherein the light-resistant packaging is an opaque ampule, an opaque bag, an opaque blister pack, an opaque bottle, an opaque can, an opaque carton, an opaque drum, an opaque jar, an opaque pouch or an opaque tube. 
     
     
         59 . (canceled) 
     
     
         60 . The pharmaceutical composition of  claim 28 , wherein the opaque blister pack comprises a blend of aluminum and aluminum-silver. 
     
     
         61 . The pharmaceutical composition of  claim 28 , wherein the opaque blister pack comprises a blend of aluminum and poly-chloro-trifluoro-ethylene. 
     
     
         62 . The pharmaceutical composition of  claim 28 , wherein the opaque blister pack comprises a blend of two or more of polyvinyl chloride, polyethylene, polycarbonate, polyvinylidene chloride and ethylene vinyl alcohol. 
     
     
         63 . The pharmaceutical composition of  claim 28 , wherein the opaque high density polyethylene (HPDE) container is an opaque high density polyethylene (HPDE) bottle. 
     
     
         64 . The pharmaceutical composition of  claim 63 , wherein the opaque high density polyethylene (HPDE) bottle is an opaque high density polyethylene bottle capped with polypropylene child-resistant screw caps fitted with a silica desiccant insert. 
     
     
         65 . The pharmaceutical composition of  claim 63 , wherein the opaque high density polyethylene (HPDE) bottle is an opaque high density polyethylene bottle capped with polypropylene child-resistant screw caps with aluminum induction seal. 
     
     
         66 . The pharmaceutical composition of  claim 22 , further comprising N-ethyl-N-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide in an amount greater than about 0.02% and less than about 0.50%, by weight, relative to the amount of laquinimod, based on a determination by an HPLC method. 
     
     
         67 . The pharmaceutical composition of  claim 66 , wherein the amount of N-ethyl-N-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide in the composition is greater than about 0.02% and less than about 0.10% by weight relative to the amount of laquinimod. 
     
     
         68 . The pharmaceutical composition of  claim 66 , wherein the amount of N-ethyl-N-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide is greater than about 0.05% and less than about 0.50% by weight relative to the amount of laquinimod. 
     
     
         69 . The pharmaceutical composition of  claim 22 , wherein the pharmaceutically acceptable salt of laquinimod is a sodium salt. 
     
     
         70 . The pharmaceutical composition of  claim 22 , wherein the at least one pharmaceutically acceptable carrier is magnesium stearate.