Methods of providing therapeutic effects using cyclosporin components

Abstract

Methods of treating an eye of a human or animal include administering to an eye of a human or animal a composition in the form of an emulsion including water, a hydrophobic component and a cyclosporin component in a therapeutically effective amount of less than 0.1% by weight of the composition. The weight ratio of the cyclosporin component to the hydrophobic component is less than 0.8.

1 - 36 . (canceled) 
     
     
         37 . A method of increasing tear production in a human eye, the method comprising topically administering to a human eye in need thereof a first topical ophthalmic emulsion at a frequency of twice a day. wherein the first topical ophthalmic emulsion comprises cyclosporin A in an amount of about 0.05% by weight, polysorbate 80, acrylate/C10-30 alkyl acrylate cross-polymer, water, and castor oil in an amount of about 1.25% by weight;
 wherein the method provides an overall increase in tear production substantially equal to administration of a second topical ophthalmic emulsion to a human eye in need thereof at a frequency of twice a day. the second emulsion comprising cyclosporin A in an amount of about 0.1% by weight and castor oil in an amount of about 1.25% by weight; and   wherein the method results in substantially no detectable concentration of cyclosporin A in the blood of the human.   
     
     
         38 . The method of  claim 37 , wherein the first topical ophthalmic emulsion further comprises a tonicity agent or a demulcent component. 
     
     
         39 . The method of  claim 38 , wherein the tonicity agent or the demulcent component is glycerine. 
     
     
         40 . The method of  claim 37 , wherein the first topical ophthalmic emulsion further comprises a buffer. 
     
     
         41 . The method of  claim 40 , wherein the buffer is sodium hydroxide. 
     
     
         42 . The method of  claim 37 , wherein the first topical ophthalmic emulsion further comprises glycerine and a buffer. 
     
     
         43 . The method of  claim 37 , wherein the first topical ophthalmic emulsion comprises polysorbate 80 in an amount of about 1.0% by weight. 
     
     
         44 . The method of  claim 37 , wherein the first topical ophthalmic emulsion comprises acrylate/C10-30 alkyl acrylate cross-polymer in an amount of about 0.05% by weight. 
     
     
         45 . The method of  claim 37 , wherein the first topical ophthalmic emulsion further comprises glycerine in an amount of about 2.2% by weight and a buffer. 
     
     
         46 . The method of  claim 45 , wherein the buffer is sodium hydroxide. 
     
     
         47 . The method of  claim 42 , wherein the first topical ophthalmic emulsion has a pH in the range of about 7.2 to about 7.6. 
     
     
         48 . The method of  claim 37 , wherein the method is therapeutically effective to treat dry eye disease. 
     
     
         49 . A method of increasing tear production in a human eye, the method comprising topically administering to a human eye in need thereof a first topical ophthalmic emulsion at a frequency of twice a day, wherein the first topical ophthalmic emulsion comprises:
 cyclosporin A in an amount of about 0.05% by weight;   castor oil in an amount of about 1.25% by weight;   polysorbate 80 in an amount of about 1.0% by weight;   acrylate/C10-30 alkyl acrylate cross-polymer in an amount of about 0.05% by weight;   a tonicity component or a demulcent component in an amount of about 2.2% by weight;   a buffer, and   water,   wherein the method achieves a substantially equal increase in tear production as administration of a second topical ophthalmic emulsion to a human eye in need thereof at a frequency of twice a day, the second emulsion being identical to the first topical ophthalmic emulsion except that the second topical ophthalmic emulsion comprises cyclosporin A in an amount of about 0.1% by weight, and   wherein the method results in substantially no detectable concentration of cyclosporin A in the blood of the human.   
     
     
         50 . The method of  claim 49 , wherein the first topical ophthalmic emulsion has a pH in the range of about 7.2 to about 7.6. 
     
     
         51 . The method of  claim 49 , wherein the method is effective in enhancing lacrimal gland tearing. 
     
     
         52 . The method of  claim 49 , wherein the method is therapeutically effective to treat dry eye disease.