Solutions containing epinastin

Abstract

Topically administered aqueous solutions containing epinastin, optionally in the form of its racemate or its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof.

1 .- 55 . (canceled)  
     
     
         56 . A method for inhibiting the influx of neutrophils and eosinophils into the tissue of the ocular conjunctiva of a host, comprising: 
 topically administering to the ocular conjunctiva of the host a solution comprising:    (a) epinastine, optionally in the form of its racemate, an enantiomer thereof, or a pharmacologically acceptable acid addition salt thereof, in a concentration of 0.005 to 0.5 mg/ml of solution;    (b) water or physiologically acceptable saline; and    (c) a preservative,    wherein the pH is adjusted to between 6.5 and 7.2 by means of a physiologically acceptable buffer, and    optionally also including one or more chelating agents, viscosity agents, penetration promoters, antioxidants, or substances to adjust the tonicity of the solution.    
     
     
         57 . The method according to  claim 56 , wherein the concentration of epinastine, optionally in the form of its racemate, an enantiomer thereof, or a pharmacologically acceptable acid addition salt thereof, in the solution is 0.02 to 0.5 mg/ml.  
     
     
         58 . The method according to  claim 56 , wherein the concentration of epinastine, optionally in the form of its racemate, an enantiomer thereof, or a pharmacologically acceptable acid addition salt thereof, in the solution is 0.02 to 0.1 mg/ml.  
     
     
         59 . The method according to  claim 56 , wherein the concentration of epinastine, optionally in the form of its racemate, an enantiomer thereof, or a pharmacologically acceptable acid addition salt thereof, in the solution is 0.03 to 0.07 mg/ml.  
     
     
         60 . The method according to  claim 56 , wherein the epinastine is epinastine hydrochloride.  
     
     
         61 . The method according to  claim 56 , wherein the preservative is selected from: benzalkonium chloride, chlorobutanol, thimerosal, phenyl mercury acetate, and phenyl mercury nitrate.  
     
     
         62 . The method according to  claim 56 , wherein the solution comprises a viscosity agent.  
     
     
         63 . The method according to  claim 62 , wherein the viscosity agent is selected from: polyvinyl alcohol, povidone, hydroxypropylmethylcellulose, poloxamers, carboxymethylcellulose, carbomers, and hydroxyethylcellulose.  
     
     
         64 . The method according to  claim 56 , wherein the solution comprises a penetration promoter.  
     
     
         65 . The method according to  claim 64 , wherein the penetration promoter is selected from: cationic, anionic, non-ionogenic, and amphoteric surfactants; dimethylsulfoxide and other sulfoxides; dimethylacetamide and pyrrolidone; amides of heterocyclic amines; glycols; propylene carbonate; oleic acid; and alkylamines and derivatives thereof.  
     
     
         66 . The method according to  claim 56 , wherein the solution further comprises a substance to adjust the tonicity of the solution selected from: sodium chloride, potassium chloride, mannitol, and glycerol.  
     
     
         67 . The method according to  claim 56 , wherein the solution comprises a buffer selected from: acetate buffer, citrate buffer, phosphate buffer, and borate buffer.  
     
     
         68 . The method according to  claim 56 , wherein the solution comprises an antioxidant selected from: sodium metabisulphite, sodium thiosulphate, acetylcysteine, butylated hydroxyanisole, and butylated hydroxytoluene.  
     
     
         69 . The method according to  claim 56 , wherein the solution further comprises the chelating agent disodium edetate.  
     
     
         70 . The method according to  claim 56 , wherein the solution comprises epinastine hydrochloride, water, sodium chloride, sodium hydrogen phosphate dihydrate, benzalkonium chloride, hydroxyethylcellulose, and optionally sodium EDTA and sodium hydroxide.