Ophthalmic Compositions

Abstract

The embodiments disclosed herein relate to ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors, and more particularly to methods for treating an ocular disease and/or condition using the disclosed compositions. According to aspects illustrated herein, there is provided a pharmaceutical composition that includes a calcineurin inhibitor or an mTOR inhibitor; a first surfactant with an HLB index greater than about 10; and a second surfactant with an HLB index of greater than about 13, wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3, and wherein the composition forms mixed micelles.

What is claimed is: 
     
         1 . A pharmaceutical composition, comprising:
 an effective amount of corticosteroid;   vitamin E tocopherol polyethylene glycol succinate (TPGS); and   octoxynol-40,   
       wherein the composition is in the form of mixed micelles having the vitamin E TPGS and the octoxynol-40 and is suitable for topical application. 
     
     
         2 . The pharmaceutical composition of  claim 1  wherein the corticosteroid includes prednisolone, hydrocortisone, triamcinolone, budesonide, or combinations thereof. 
     
     
         3 . The pharmaceutical composition of  claim 1  wherein the composition forms optically clear mixed micelles. 
     
     
         4 . The pharmaceutical composition of  claim 1  wherein the vitamin E TPGS is present in from about 0.01 wt % to about 20 wt % of a total volume of the composition. 
     
     
         5 . The pharmaceutical composition of  claim 1  wherein the octoxynol-40 is present in from about 0.001 wt % to about 10 wt % of a total volume of the composition. 
     
     
         6 . The pharmaceutical composition of  claim 1  further comprising one or more bioadhesive polymers selected from the group consisting of polyvinylpyrrolidone (PVP)-K-30, PVP-K-90, hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HEC), and polycarbophil. 
     
     
         7 . The pharmaceutical composition of  claim 1  wherein the composition is an aqueous solution. 
     
     
         8 . The pharmaceutical composition of  claim 1  wherein the corticosteroid is delivered to a back of an eye. 
     
     
         9 . A pharmaceutical composition, comprising:
 an effective amount of corticosteroid;   vitamin E tocopherol polyethylene glycol succinate (TPGS) with a hydrophilic/lipophilic balance (HLB) index greater than about 10; and   octoxynol-40 with an HLB index of greater than about 13,   
       wherein an absolute difference between the HLB index of the vitamin E TPGS and the HLB index of the octoxynol-40 is greater than about 3, and 
       wherein the composition is in the form of mixed micelles having the vitamin E TPGS and the octoxynol-40. 
     
     
         10 . The pharmaceutical composition of  claim 9  wherein the composition forms optically clear mixed micelles. 
     
     
         11 . The pharmaceutical composition of  claim 9  wherein the corticosteroid includes prednisolone, hydrocortisone, triamcinolone, budesonide, or combinations thereof. 
     
     
         12 . The pharmaceutical composition of  claim 9  wherein the vitamin E TPGS is present in from about 0.01 wt % to about 20 wt % of a total volume of the composition. 
     
     
         13 . The pharmaceutical composition of  claim 9  wherein the octoxynol-40 is present in from about 0.001 wt % to about 10 wt % of a total volume of the composition. 
     
     
         14 . The pharmaceutical composition of  claim 9  further comprising one or more bioadhesive polymers selected from the group consisting of polyvinylpyrrolidone (PVP)-K-30, PVP-K-90, hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HEC), and polycarbophil. 
     
     
         15 . The pharmaceutical composition of  claim 9  wherein the composition is an aqueous solution. 
     
     
         16 . The pharmaceutical composition of  claim 9  wherein the corticosteroid is delivered to a back of an eye. 
     
     
         17 . A pharmaceutical composition, comprising:
 an effective amount of corticosteroid selected from the group consisting of prednisolone, hydrocortisone, triamcinolone, budesonide, and any combinations thereof;   vitamin E tocopherol polyethylene glycol succinate (TPGS); and   octoxynol-40,   
       wherein the composition is in the form of mixed micelles having the vitamin E TPGS and the octoxynol-40 and is suitable for topical application. 
     
     
         18 . A method for treating an ocular disease in a patient in need thereof, the method comprising administering topically to an eye of the patient the pharmaceutical composition of  claim 1 . 
     
     
         19 . The method of  claim 18  wherein the ocular disease is an inflammatory ocular surface disease selected from the group consisting of dry eye syndrome (DES), Sjogren's syndrome, uveitis, conjunctivitis (pink eye), keratitis, keratoconjunctivitis, vernal keratoconjunctivitis (VKC), atopic keratoconjunctivitis (AKC), autoimmune disorders of the ocular surface, including cicatrizing conjunctivitis, blepharitis, and scleritis, or an immune rejection of a corneal allograft. 
     
     
         20 . A method for treating an ocular disease in a patient in need thereof, the method comprising administering topically to an eye of the patient the pharmaceutical composition of  claim 9 . 
     
     
         21 . The method of  claim 20  wherein the ocular disease is an inflammatory ocular surface disease selected from the group consisting of dry eye syndrome (DES), Sjogren's syndrome, uveitis, conjunctivitis (pink eye), keratitis, keratoconjunctivitis, vernal keratoconjunctivitis (VKC), atopic keratoconjunctivitis (AKC), autoimmune disorders of the ocular surface, including cicatrizing conjunctivitis, blepharitis, and scleritis, or an immune rejection of a corneal allograft. 
     
     
         22 . A method for treating an ocular disease in a patient in need thereof, the method comprising administering topically to an eye of the patient the pharmaceutical composition of  claim 17 . 
     
     
         23 . The method of  claim 22  wherein the ocular disease is an inflammatory ocular surface disease selected from the group consisting of dry eye syndrome (DES), Sjogren's syndrome, uveitis, conjunctivitis (pink eye), keratitis, keratoconjunctivitis, vernal keratoconjunctivitis (VKC), atopic keratoconjunctivitis (AKC), autoimmune disorders of the ocular surface, including cicatrizing conjunctivitis, blepharitis, and scleritis, or an immune rejection of a corneal allograft.