Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane

Abstract

A method for treating allergic rhinitis, comprising topically administering to the nasal mucus membrane of a host in need of such treatment a solution comprising: epinastine, optionally in the form of its racemate, its enantiomers, or its pharmacologically acceptable acid addition salts, in a pharmacologically acceptable carrier.

1 - 55 . (canceled)  
     
     
         56 . A method for treating allergic rhinitis comprising: 
 topically administering to the nasal mucous membrane of a host in need thereof, a solution comprising epinastine, optionally in the form of its racemate, an enantiomer thereof, or a pharmacologically acceptable acid addition salt thereof, in a pharmacologically acceptable carrier.    
     
     
         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 0.005 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 solution further comprises a viscosity agent.  
     
     
         62 . The method according to  claim 56 , wherein the solution further comprises a penetration promoter.  
     
     
         63 . 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.  
     
     
         64 . The method according to  claim 56 , wherein the solution further comprises a buffer selected from: acetate buffer, citrate buffer, phosphate buffer, and borate buffer.  
     
     
         65 . The method according to  claim 56 , wherein the solution further comprises an antioxidant selected from: sodium metabisulphite, sodium thiosulphate, acetylcysteine, butylated hydroxyanisole, and butylated hydroxytoluene.  
     
     
         66 . The method according to  claim 56 , wherein the solution further comprises the chelating agent disodium edetate.  
     
     
         67 . 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.  
     
     
         68 . The method according to  claim 56 , wherein the method is for treating late phase reactions of allergic rhinitis.  
     
     
         69 . A method for treating allergic rhinitis by topically administering to the nasal mucous membrane of a host in need of such treatment 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.    
     
     
         70 . The method according to  claim 69 , 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.  
     
     
         71 . The method according to  claim 69 , 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.  
     
     
         72 . The method according to  claim 69 , wherein the solution comprises epinastine hydrochloride.  
     
     
         73 . The method according to  claim 69 , wherein the preservative is selected from: benzalkonium chloride, chlorobutanol, thimerosal, phenyl mercury acetate, and phenyl mercury nitrate.  
     
     
         74 . The method according to  claim 69 , wherein the solution comprises a viscosity agent selected from: polyvinyl alcohol, povidone, hydroxypropylmethylcellulose, poloxamers, carboxymethylcellulose, carbomers, and hydroxyethylcellulose.  
     
     
         75 . The method according to  claim 69 , wherein the solution comprises a penetration promoter 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.  
     
     
         76 . The method according to  claim 69 , wherein the solution further comprises a substance to adjust the tonicity of the solution selected from: sodium chloride, potassium chloride, mannitol, and glycerol.  
     
     
         77 . The method according to  claim 69 , wherein the solution comprises a buffer selected from: acetate buffer, citrate buffer, phosphate buffer, and borate buffer.  
     
     
         78 . The method according to  claim 69 , wherein the solution comprises an antioxidant selected from: sodium metabisulphite, sodium thiosulphate, acetylcysteine, butylated hydroxyanisole, and butylated hydroxytoluene.  
     
     
         79 . The method according to  claim 69 , wherein the solution further comprises the chelating agent disodium edetate.  
     
     
         80 . The method according to  claim 69 , wherein the method is for treating late phase reactions of allergic rhinitis.  
     
     
         81 . The method of  claim 56 , further comprising identifying a host suffering from or at risk for allergic rhinitis and topically administering the solution to the nasal mucous membrane of such host.  
     
     
         82 . The method of  claim 69 , further comprising identifying a host suffering from or at risk for allergic rhinitis and topically administering the solution to the nasal mucous membrane of such host.