Ophthalmic compound with extended dwell time on the eye

Abstract

Ophthalmic composition with prolonged residence time on the eye, in particular in the form of a gel which can be administered as drops, of an ointment or the like, containing a free-flowing vehicle with increased viscosity and a preservative, and, where appropriate, one or more active ingredients and conventional additives such as tonicity agents, substances to adjust the pH etc. The preservative is essentially formed according to the invention by a benzyllauryldimethylammonium salt. The invention furthermore relates to the use of a benzyllauryldimethylammonium salt as preservative for producing ophthalmic compositions intended for repeated use over lengthy periods and/or formulated for a lengthy residence time on the eye after each use, whereby irritation and/or damage to the tissue of the eye are avoided.

1 . Ophthalmic composition with prolonged residence time on the eye, in particular in the form of a gel which can be administered as drops, of an ointment or the like, containing a free-flowing vehicle with increased viscosity and a preservative, and, where appropriate, one or more active ingredients and conventional additives such as tonicity agents, substances to adjust the pH etc., characterized in that the preservative is essentially formed by a benzyllauryldimethylammonium salt.  
     
     
         2 . Ophthalmic composition according to  claim 1 , characterized in that the composition has as vehicle an aqueous base for a gel which can be administered as drops.  
     
     
         3 . Ophthalmic composition according to  claim 1  or  2 , characterized in that the vehicle of the composition contains at least one viscosity-increasing synthetic or natural polymer in aqueous solution or dispersion.  
     
     
         4 . Ophthalmic composition according to  claim 3 , characterized in that the polymer comprises a carboxyvinyl polymer, in particular a carboxypolymethylene, or an ethylene/maleic anhydride copolymer.  
     
     
         5 . Ophthalmic composition according to  claim 3 , characterized in that the polymer comprises a cellulose derivative, a natural gum such as xanthan, a dextran derivative or the like.  
     
     
         6 . Ophthalmic composition according to any of  claims 1  to  5 , characterized in that the liquid portion of the composition is in the form of a single-phase aqueous liquid.  
     
     
         7 . Ophthalmic composition according to any of  claims 1  to  5 , characterized in that the liquid portion of the composition is in the form of a two-phase liquid, preferably as O/W emulsion.  
     
     
         8 . Ophthalmic composition according to any of  claims 1  to  7 , characterized in that the preservative is benzyllauryldimethylammonium chloride.  
     
     
         9 . Ophthalmic composition according to any of  claims 1  to  8 , characterized in that the concentration of the preservative based on the total amount of the composition is between 0.001% by weight and 0.5% by weight, preferably between 0.01% by weight and 0.05% by weight.  
     
     
         10 . Ophthalmic composition according to any of  claims 1  to  9 , characterized in that the composition contains vitamin A as active ingredient.  
     
     
         11 . Ophthalmic composition according to any of  claims 1  to  10 , characterized in that the composition comprises 0.001 to 1% by weight, preferably 0.1 to 0.5% by weight, of carboxypolyethylene, 0.0005 to 0.05% by weight, preferably 0.001 to 0.01% by weight, of benzyllauryldimethylammonium chloride, 0.1 to 10% by weight, preferably 1 to 5% by weight, of sorbitol, and alkali metal hydroxide or acid to adjust a physiologically acceptable pH and otherwise water.  
     
     
         12 . Use of a benzyllauryldimethylammonium salt as preservative for producing ophthalmic compositions intended for repeated use over lengthy periods and/or formulated for a lengthy residence time on the eye after each use, whereby irritation and/or damage to the tissue of the eye are avoided.  
     
     
         13 . Use of benzyllauryldimethylammonium chloride according to  claim 12 .  
     
     
         14 . Use of the preservative according to  claim 12  or  13  for eye drops having a least one active ingredient.  
     
     
         15 . Use of the preservative according to  claim 12  or  13  for a simulated tear fluid.