Compositions containing quaternary ammonium compounds

Abstract

This invention relates to compositions containing quaternary ammonium compounds in which the nitrogen atom is substituted by at least one alkyl group having at least 12 carbon atoms, characterized in that the composition includes at least 20% in weight by weight of the total composition, of ammonium halides in which the nitrogen atom is substituted by at least one alkyl group having at least 14 carbon atoms and more than 5%, preferably more than 7% in weight by weight of the total composition, of ammonium halides in which the nitrogen atom is substituted by at least one alkyl group having at least 16 carbon atoms. This invention also relates to ophthalmic oil-in-water emulsions containing such compositions, said ophthalmic emulsions being useful for eye care or for the treatment of eye conditions.

1 . Composition comprising at least one quaternary ammonium halide in which the nitrogen atom is substituted by at least one alkyl group having at least 12 carbon atoms, characterized in that said composition includes:
 a) at least 20% in weight by weight of the total composition, of quaternary ammonium halides in which the nitrogen atom is substituted by at least one alkyl group having at least 14 carbon atoms and   b) more than 5%, preferably more than 7% in weight by weight of the total composition, of quaternary ammonium halides in which the nitrogen atom is substituted by at least one alkyl group having at least 16 carbon atoms.   
     
     
         2 . Composition according to  claim 1 , wherein said composition includes
 a) at least 20% in weight by weight of the total composition, of quaternary ammonium halides in which the nitrogen atom is substituted by at least one alkyl group having at least 14 carbon atoms and   b) at least 10%, preferably at least 15%, more preferably at least 20% in weight by weight of the total composition, of quaternary ammonium halides in which the nitrogen atom is substituted by at least one alkyl group having at least 16 carbon atoms.   
     
     
         3 . Composition according to  claim 1 , wherein said quaternary ammonium halides are benzyl dimethyl ammonium chlorides or bromides, wherein the nitrogen atom is further substituted by an alkyl group having at least 12 carbon atoms. 
     
     
         4 . Composition according to  claim 1 , comprising C14- and C16-alkyl benzyl dimethyl ammonium chlorides. 
     
     
         5 . Composition according to  claim 1 , wherein said quaternary ammonium halide is a trimethyl ammonium chloride or bromide, wherein the nitrogen atom is further substituted by an alkyl group having at least 12 carbon atoms. 
     
     
         6 . Composition according to  claim 1 , wherein the amount of ammonium halides in which the nitrogen atom substituted by at least one alkyl group having 14 or 16 carbon atoms represents at least 50% w/w in dry weight of the weight of all ammonium halides present in the composition. 
     
     
         7 . Composition according to  claim 1 , wherein the dry weight ratio of C12-alkyl ammonium halides to the sum of C14-alkyl ammonium halides and C16-alkyl ammonium halides, is less than 1.5, preferably less than 1.35, more preferably less than 1.20. 
     
     
         8 . Oil-in-water emulsion comprising a composition according to  claim 1 , said emulsion comprising 0.0005 to 0.1% of quaternary ammonium halides. 
     
     
         9 . Oil-in-water emulsion according to  claim 8 , further comprising hydroxypropyl guar, polyethylene glycol-400 or a mixture of both. 
     
     
         10 . Oil-in-water emulsion according to  claim 8 , further comprising an oil phase comprising MCT, castor oil or mineral oil, surfactants preferably chosen among at least one of tyloxapol, poloxamer, tocopherol polyethyleneglycol succinate and polysorbate, and optionally antioxidants and/or isotonicity agents preferably chosen among at least one of glycerol and mannitol. 
     
     
         11 . Oil-in-water emulsion according to  claim 8 , said emulsion having a positive zeta potential. 
     
     
         12 . Oil-in-water emulsion according to  claim 8 , said emulsion having a droplet size of 100 to 500 nm. 
     
     
         13 . Oil-in-water emulsion according to  claim 8 , said emulsion being preserved. 
     
     
         14 . Oil-in-water emulsion according to  claim 8 , said emulsion being unpreserved. 
     
     
         15 . Oil-in-water emulsion according to  claim 8 , said emulsion comprising C16-alkyl quaternary ammonium halide as only source of quaternary ammonium halide. 
     
     
         16 . Oil-in-water emulsion according to  claim 8 , further comprising an active principle. 
     
     
         17 . Medicament comprising of an oil-in-water emulsion according to  claim 8 . 
     
     
         18 . Use of an oil-in-water emulsion according to  claim 8  for the manufacture of a medicament or an ophthalmic composition for the treatment of an eye condition or disease. 
     
     
         19 . Cosmetic composition comprising an oil-in-water emulsion according to  claim 8 . 
     
     
         20 . A non-therapeutical process for caring for, removing makeup from and/or cleansing the skin, the lips and/or the eyes, and/or for hair care, comprising applying an oil-in-water emulsion according to  claim 8 .