High Concentration Olopatadine Ophthalmic Composition

Abstract

The present invention is an ophthalmic composition containing a relatively high concentration of olopatadine. The composition is typically an ophthalmic aqueous solution containing relatively high concentrations of olopatadine solubilized within the solution. The composition is preferably capable of providing enhanced relief from symptoms of ocular allergic conjunctivitis, particularly late phase symptoms of ocular allergic conjunctivitis.

We claim: 
     
         1 . An ophthalmic composition for treatment of ocular allergic conjunctivitis, the composition comprising:
 at least 0.67 w/v % olopatadine; and   water.   
     
     
         2 . A composition as in  claim 1  wherein the concentration of olopatadine is at least 0.7 w/v % and is dissolved in solution. 
     
     
         3 . A composition as in  claim 1  further comprising a γ-cyclodextrin derivative, a β-cyclodextrin derivative or both to aid in the solubility of the olopatadine. 
     
     
         4 . A composition as in  claim 1  further comprising a lactam polymer to aid in the solubility of the olopatadine. 
     
     
         5 . A composition as in  claim 4  wherein the lactam polymer is polyvinylpyrrolidone. 
     
     
         6 . A composition as in  claim 1  further comprising a polyether. 
     
     
         7 . A composition as in  claim 6  wherein the polyether is polyethylene glycol. 
     
     
         8 . A composition as in  claim 1  wherein the composition is disposed in an eyedropper, has a pH of 5.5 to 8.0 and an osmolality of 200 to 450. 
     
     
         9 . An ophthalmic composition for treatment of ocular allergic conjunctivitis, the composition comprising:
 at least 0.67 w/v % olopatadine dissolved in solution;   PEG having a molecular weight of 300 to 500;   polyvinylpyrrolidone; and   cyclodextrin derivative selected from β-cyclodextrin derivative, γ-cyclodextrin or both.   
     
     
         10 . A composition as in  claim 9  further comprising a preservative selected from a polymeric quaternary ammonium compound and benzalkonium chloride. 
     
     
         11 . A composition as in  claim 10  wherein the cyclodextrin derivative is hydroxypropyl-β-cyclodextrin or sulfoalkyl ether β-cyclodextrin. 
     
     
         12 . A composition as in  claim 11  wherein the β-cyclodextrin derivative is hydroxypropyl-β-cyclodextrin when the preservative is the benzalkonium chloride and the β-cyclodextrin derivative is sulfoalkyl ether β-cyclodextrin when the preservative is the polymeric quaternary ammonium compound. 
     
     
         13 . A composition as in  claim 10  wherein the preservative is benzalkonium chloride and the cyclodextrin derivative is hydroxypropyl-γ-cyclodextrin. 
     
     
         14 . A composition as in  claim 9  further comprising borate. 
     
     
         15 . A composition as in  claim 14  further comprising polyol. 
     
     
         16 . An ophthalmic composition for treatment of ocular allergic conjunctivitis, the composition comprising:
 at least 0.67 w/v % but no greater than 1.0 w/v % olopatadine dissolved in solution;   PEG having a molecular weight of 300 to 500 wherein the concentration of the PEG in solution is from about 2.0 w/v % to about 6.0 w/v %;   a lactam polymer wherein the lactam polymer is polyvinylpyrrolidone and the concentration of the polyvinylpyrrolidone in solution is from about 2.0 w/v % about 6.0 w/v %; and   a β-cyclodextrin derivative or a γ-cyclodextrin derivative selected from SAE-β-cyclodextrin, HP-γ-cyclodextrin and HP-β-cyclodextrin wherein the concentration of the β-cyclodextrin derivative or the γ-cyclodextrin derivative is at least 0.5 w/v % but no greater than 2.0 w/v %.   
     
     
         17 . A composition as in  claim 16  further comprising borate at a concentration of at least about 0.18 w/v % but less than about 0.5 w/v %. 
     
     
         18 . A composition as in  claim 17  further comprising polyol. 
     
     
         19 . A composition as in  claim 18  wherein the polyol include polyethylene glycol at a concentration of at least 0.4 w/v % but no greater than 2.2 w/v %. 
     
     
         20 . An ophthalmic composition for treatment of ocular allergic conjunctivitis, the composition comprising:
 at least 0.67 w/v % but no greater than 1.0 w/v % olopatadine dissolved in solution;   PEG having a molecular weight of 300 to 500 wherein the concentration of the PEG in solution is from about 2.0 w/v % to about 6.0 w/v %;   a lactam polymer wherein the lactam polymer is polyvinylpyrrolidone and the concentration of the polyvinylpyrrolidone in solution is from about 2.0 w/v % to about 6.0 w/v %; and   hydroxypropyl-γ-cyclodextrin in the composition at a concentration of at least 0.5 w/v % but no greater than 2.0 w/v %.   
     
     
         21 . A composition as in  claim 20  further comprising borate at a concentration of at least about 0.18 w/v % but less than about 0.5 w/v %. 
     
     
         22 . A composition as in  claim 21  further comprising polyol. 
     
     
         23 . A composition as in  claim 22  wherein the polyol include polyethylene glycol at a concentration of at least 0.4 w/v % but no greater than 2.2 w/v %. 
     
     
         24 . A method of treating ocular allergy symptoms, the method comprising:
 topically applying the composition of  claim 20  to an eye of a human.   
     
     
         25 . A method as in  claim 24  wherein the step of topically applying the composition includes dispensing an eyedrop from an eyedropper.