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 . A method for treating late phase reactions of 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, its enantiomers, or its pharmacologically acceptable acid addition salts, 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.    
     
     
         2 . The method according to  claim 1 , wherein the concentration of epinastine in the solution is 0.02 to 0.1 mg/ml of solution.  
     
     
         3 . The method according to  claim 2 , wherein the concentration of epinastine in the solution is 0.03 to 0.07 mg/ml of solution.  
     
     
         4 . The method according to  claim 1 , wherein the solution comprises epinastine hydrochloride.  
     
     
         5 . The method according to  claim 1 , wherein the preservative is selected from the group consisting of: benzalkonium chloride, chlorobutanol, thimerosal, phenyl mercury acetate, and phenyl mercury nitrate.  
     
     
         6 . The method according to  claim 4 , wherein the solution further comprises a viscosity agent.  
     
     
         7 . The method according to  claim 6 , wherein the viscosity agent is selected from the group consisting of: polyvinyl alcohol, povidone, hydroxypropylmethylcellulose, poloxamers, carboxymethylcellulose, carbomers, and hydroxyethylcellulose.  
     
     
         8 . The method according to  claim 4 , wherein the solution further comprises a penetration promoter.  
     
     
         9 . The method according to  claim 8 , wherein the penetration promoter is selected from the group consisting of: 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.  
     
     
         10 . The method according to  claim 1 , wherein the solution further comprises a substance to adjust the tonicity of the solution selected from the group consisting of: sodium chloride, potassium chloride, mannitol, and glycerol.  
     
     
         11 . The method according to  claim 1 , wherein the solution further comprises a buffer selected from the group consisting of: acetate buffer, citrate buffer, phosphate buffer, and borate buffer.  
     
     
         12 . The method according to  claim 1 , wherein the solution further comprises an antioxidant selected from the group consisting of: sodium metabisulphite, sodium thiosulphate, acetylcysteine, butylated hydroxyanisole, and butylated hydroxytoluene.  
     
     
         13 . The method according to  claim 1 , wherein the solution further comprises the chelating agent disodium edetate.  
     
     
         14 . The method according to  claim 1 , wherein the solution comprises epinastine hydrochloride, water, sodium chloride, sodium hydrogen phosphate dihydrate, benzalkonium chloride, hydroxyethylcellulose, and optionally sodium EDTA and sodium hydroxide.  
     
     
         15 . A method for treating late phase reactions of 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, its enantiomers, or its pharmacologically acceptable acid addition salts, in a concentration of 0.02 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.    
     
     
         16 . A method for treating late phase reactions of 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, its enantiomers, or its pharmacologically acceptable acid addition salts, in a concentration of 0.005 to 1.0 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.    
     
     
         17 . 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, its enantiomers, or its pharmacologically acceptable acid addition salts, 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.    
     
     
         18 . The method according to  claim 17 , wherein the concentration of epinastine in the solution is 0.02 to 0.1 mg/ml of solution.  
     
     
         19 . The method according to  claim 18 , wherein the concentration of epinastine in the solution is 0.03 to 0.07 mg/ml of solution.  
     
     
         20 . The method according to  claim 17 , wherein the solution comprises epinastine hydrochloride.  
     
     
         21 . The method according to  claim 17 , wherein the preservative is selected from the group consisting of: benzalkonium chloride, chlorobutanol, thimerosal, phenyl mercury acetate, and phenyl mercury nitrate.  
     
     
         22 . The method according to  claim 20 , wherein the solution further comprises a viscosity agent.  
     
     
         23 . The method according to  claim 22 , wherein the viscosity agent is selected from the group consisting of: polyvinyl alcohol, povidone, hydroxypropylmethylcellulose, poloxamers, carboxymethylcellulose, carbomers, and hydroxyethylcellulose.  
     
     
         24 . The method according to  claim 20 , wherein the solution further comprises a penetration promoter.  
     
     
         25 . The method according to  claim 24 , wherein the penetration promoter is selected from the group consisting of: 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.  
     
     
         26 . The method according to  claim 17 , wherein the solution further comprises a substance to adjust the tonicity of the solution selected from the group consisting of: sodium chloride, potassium chloride, mannitol, and glycerol.  
     
     
         27 . The method according to  claim 17 , wherein the solution further comprises a buffer selected from the group consisting of: acetate buffer, citrate buffer, phosphate buffer, and borate buffer.  
     
     
         28 . The method according to  claim 17 , wherein the solution further comprises an antioxidant selected from the group consisting of: sodium metabisulphite, sodium thiosulphate, acetylcysteine, butylated hydroxyanisole, and butylated hydroxytoluene.  
     
     
         29 . The method according to  claim 17 , wherein the solution further comprises the chelating agent disodium edetate.  
     
     
         30 . The method according to  claim 17 , wherein the solution comprises epinastine hydrochloride, water, sodium chloride, sodium hydrogen phosphate dihydrate, benzalkonium chloride, hydroxyethylcellulose, and optionally sodium EDTA and sodium hydroxide.  
     
     
         31 . A method for treating allergic rhinitis by topically administering to the nasal mucus membrane of a host in need of such treatment a solution comprising: 
 (a) epinastine, optionally in the form of its racemate, its enantiomers, or its pharmacologically acceptable acid addition salts, in a concentration of 0.005 to 1.0 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.    
     
     
         32 . 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.  
     
     
         33 . The method according to  claim 32 , wherein the solution comprises: 
 (a) epinastine, optionally in the form of its racemate, its enantiomers, or its pharmacologically acceptable acid addition salts, in a concentration of 0.005 to 0.5 mg/ml of solution;    (b) 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.    
     
     
         34 . The method according to  claim 33 , wherein the concentration of epinastine in the solution is 0.02 to 0.1 mg/ml of solution.  
     
     
         35 . The method according to  claim 34 , wherein the concentration of epinastine in the solution is 0.03 to 0.07 mg/ml of solution.  
     
     
         36 . The method according to  claim 32 , wherein the solution comprises epinastine hydrochloride.  
     
     
         37 . The method according to  claim 36 , wherein the solution further comprises a viscosity agent.  
     
     
         38 . The method according to  claim 36 , wherein the solution further comprises a penetration promoter.  
     
     
         39 . The method according to  claim 36 , wherein the solution further comprises a substance to adjust the tonicity of the solution selected from the group consisting of: sodium chloride, potassium chloride, mannitol, and glycerol.  
     
     
         40 . The method according to  claim 36 , wherein the solution further comprises a buffer selected from the group consisting of: acetate buffer, citrate buffer, phosphate buffer, and borate buffer.  
     
     
         41 . The method according to  claim 36 , wherein the solution further comprises an antioxidant selected from the group consisting of: sodium metabisulphite, sodium thiosulphate, acetylcysteine, butylated hydroxyanisole, and butylated hydroxytoluene.  
     
     
         42 . The method according to  claim 36 , wherein the solution further comprises the chelating agent disodium edetate.  
     
     
         43 . The method according to  claim 36 , wherein the solution comprises epinastine hydrochloride, water, sodium chloride, sodium hydrogen phosphate dihydrate, benzalkonium chloride, hydroxyethylcellulose, and optionally sodium EDTA and sodium hydroxide.  
     
     
         44 . A method for treating allergic rhinitis comprising: 
 (a) identifying a host suffering from or at risk for allergic rhinitis; and    (b) topically administering to the nasal mucus membrane of the host 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.    
     
     
         45 . The method according to  claim 44 , wherein the solution comprises: 
 (a) epinastine, optionally in the form of its racemate, its enantiomers, or its pharmacologically acceptable acid addition salts, 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    
     
     
         46 . The method according to  claim 45 , wherein the concentration of epinastine in the solution is 0.02 to 0.1 mg/ml of solution.  
     
     
         47 . The method according to  claim 46 , wherein the concentration of epinastine in the solution is 0.03 to 0.07 mg/ml of solution.  
     
     
         48 . The method according to  claim 44 , wherein the solution comprises epinastine hydrochloride.  
     
     
         49 . The method according to  claim 48 , wherein the solution further comprises a viscosity agent.  
     
     
         50 . The method according to  claim 48 , wherein the solution further comprises a penetration promoter.  
     
     
         51 . The method according to  claim 48 , wherein the solution further comprises a substance to adjust the tonicity of the solution selected from the group consisting of: sodium chloride, potassium chloride, mannitol, and glycerol.  
     
     
         52 . The method according to  claim 48 , wherein the solution further comprises a buffer selected from the group consisting of: acetate buffer, citrate buffer, phosphate buffer, and borate buffer.  
     
     
         53 . The method according to  claim 48 , wherein the solution further comprises an antioxidant selected from the group consisting of: sodium metabisulphite, sodium thiosulphate, acetylcysteine, butylated hydroxyanisole, and butylated hydroxytoluene.  
     
     
         54 . The method according to  claim 48 , wherein the solution further comprises the chelating agent disodium edetate.  
     
     
         55 . The method according to  claim 48 , wherein the solution comprises epinastine hydrochloride, water, sodium chloride, sodium hydrogen phosphate dihydrate, benzalkonium chloride, hydroxyethylcellulose, and optionally sodium EDTA and sodium hydroxide.