Ophthalmic formulation

Abstract

Disclosed herein is an ophthalmic formulation comprising a compound of formula (I) wherein R1 is a linear or branched C9-C33 alkyl or a linear or branched C9-C33 alkenyl with 1 to 4 double bonds; R2 is a linear or branched C9-C19 alkyl or a linear or branched C9-C19 alkenyl with 1 to 4 double bonds; and an ophthalmologically acceptable carrier.

1 . An ophthalmic formulation comprising a compound of formula (I): 
       
         
           
           
               
               
           
         
       
       wherein
 R 1  is a linear or branched C 9 -C 33  alkyl or a linear or branched C 9 -C 33  alkenyl 
 
       with 1 to 4 double bonds;
 R 2  is a linear or branched C 9 -C 19  alkyl or a linear or branched C 9 -C 19  alkenyl with 1 to 4 double bonds; 
 and an ophthalmologically acceptable carrier. 
 
     
     
         2 . An ophthalmic formulation according to  claim 1 , wherein HOOC—R 1 — is selected from the group consisting of: capryl (C10:0), lauryl (C12:0), myristyl (C14:0), palmityl (C16:0), stearyl (C18:0), oleoyl (C18:1), linoleoyl (ω6) (C18:2), and linoleoyl (ω3) (C18:3). 
     
     
         3 . An ophthalmic formulation of  claim 1 , wherein R 2  is linear or branched C 17  alkyl or linear or branched C 17  alkenyl with 1 or 2 double bonds. 
     
     
         4 . An ophthalmic formulation of  claim 1 , wherein R 2  is linear or branched C 19  alkenyl with 4 double bonds. 
     
     
         5 . An ophthalmic formulation of  claim 1 , wherein the compound of formula (I) is selected from the group consisting of: 
       
         
           
           
               
               
           
         
       
     
     
         6 . (canceled) 
     
     
         7 . An ophthalmic formulation according to  claim 1 , wherein the ophthalmologically acceptable carrier is, or comprises, water. 
     
     
         8 . An ophthalmic formulation of  claim 1 , wherein the ophthalmic formulation further comprises an ophthalmologically acceptable excipient. 
     
     
         9 . An ophthalmic formulation according to  claim 8 , wherein the ophthalmologically acceptable excipient is selected from the group consisting of demulcents, emollients, hypertonicity agents, preservatives, buffers and pH adjusting agents. 
     
     
         10 . An ophthalmic formulation of  claim 1 , wherein the ophthalmic formulation is an oil in water emulsion. 
     
     
         11 . An ophthalmic formulation of  claim 1 , wherein the ophthalmic formulation comprises liposomes. 
     
     
         12 . An ophthalmic formulation comprising a compound of formula (I) as defined in  claim 1 , water, and an emulsifying agent. 
     
     
         13 . An ophthalmic formulation comprising a compound of formula (I) as defined in  claim 1 , water, and one or more ophthalmologically acceptable excipients selected from the group consisting of polyethylene glycol, propylene glycol, glycerin, polyvinyl alcohol, povidone, polysorbate 80, hydroxypropyl methylcellulose, carmellose, carbomer 980, sodium hyaluronate and dextran. 
     
     
         14 . An ophthalmic formulation of  claim 1 , further comprising an active pharmaceutical ingredient for treating a condition or disease of the eye. 
     
     
         15 . A method for the treatment of dry eye comprising topically administering to the eye of a subject in need thereof a therapeutically effective amount of an ophthalmic formulation of  claim 1 . 
     
     
         16 . (canceled) 
     
     
         17 . An ophthalmic formulation of  claim 1 , wherein the compound of formula (I) is a compound of the following formula: 
       
         
           
           
               
               
           
         
       
     
     
         18 . An ophthalmic formulation of  claim 1 , wherein the compound of formula (I) is a compound of the following formula: 
       
         
           
           
               
               
           
         
       
     
     
         19 . An ophthalmic formulation of  claim 1 , wherein the compound of formula (I) is a compound of the following formula: 
       
         
           
           
               
               
           
         
       
     
     
         20 . An ophthalmic formulation of  claim 1 , wherein the compound of formula (I) is a compound of the following formula: 
       
         
           
           
               
               
           
         
       
     
     
         21 . An ophthalmic formulation of  claim 1 , wherein the compound of formula (I) is a compound of the following formula: 
       
         
           
           
               
               
           
         
       
     
     
         22 . An ophthalmic formulation of  claim 1 , wherein the compound of formula (I) is a compound of the following formula: 
       
         
           
           
               
               
           
         
       
     
     
         23 . An ophthalmic formulation of  claim 1 , wherein the compound of formula (I) is a compound of the following formula: 
       
         
           
           
               
               
           
         
       
     
     
         24 . (canceled)