Ophthalmic compositions comprising polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymers

Abstract

Compositions and methods related to ophthalmic use of polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymers and therapeutic uses are described herein.

What is claimed is: 
     
         1 . A topical ophthalmic composition comprising a polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymer. 
     
     
         2 . The composition of  claim 1 , wherein the polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymer has an average molecular weight of about 10,000 g/mol to about 500,000 g/mol. 
     
     
         3 . The composition of  claim 1  or  2 , further comprising a therapeutically active agent. 
     
     
         4 . The composition of  claim 3 , wherein the therapeutically active agent comprises an immunosuppressant, an alpha-adrenergic antagonist, a steroid, a prostaglandin EP2 agonist, a muscarinic, a prostaglandin, an alpha agonist, an antibiotic, an anti-infective agent, an anti-inflammatory, a beta blocker, or a combination thereof. 
     
     
         5 . The composition of  claim 3 , wherein the therapeutically active agent comprises one selected from the group consisting of cyclosporine A, a cyclosporine analog, phentolamine, testosterone, dexamethasone, prednisolone, bimatoprost, latanoprost, Compounds A. B, C, D, E, F, G, or H of Table 8, pilocarpine, brimonidine, gatifloxacin, ketorolac, a steroid, timolol, or a combination thereof. 
     
     
         6 . The composition of  claim 5 , wherein the composition is a solution. 
     
     
         7 . The composition of  claim 6 , further comprising a co-solubilizer. 
     
     
         8 . The composition of  claim 7 , wherein the co-solubilizer comprises sorbitan monostearate, a polyoxyethylene-polyoxypropylene block copolymer, polyoxyethyleneglyceroltriricinoleate 35, a cyclodextrin, or a combination thereof. 
     
     
         9 . The composition of  claim 6 , further comprising an osmolality agent. 
     
     
         10 . The composition of  claim 9 , wherein the osmolality agent comprises propylene glycol, glycerin, mannitol, sodium chloride, or a combination thereof. 
     
     
         11 . The composition of  claim 10 , further comprising a buffer. 
     
     
         12 . The composition of  claim 11 , wherein the buffer comprises phosphate, phosphate and citrate, trolamine, lactate, borate, borate and citrate, or a combination thereof. 
     
     
         13 . The composition of  claim 10  further comprising a preservative. 
     
     
         14 . The composition of  claim 13 , wherein the preservative comprises benzalkonium chloride, a stabilized oxychloro complex, or a combination thereof. 
     
     
         15 . A method of solubilizing a therapeutically active agent comprising providing a composition comprising the therapeutically active agent and a polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymer, wherein the therapeutically active agent is not completely soluble in the composition at room temperature without the polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymer. 
     
     
         16 . A method of solubilizing a therapeutically active agent comprising mixing the therapeutically active agent and a polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymer so that a composition according to  claims 5  is formed. 
     
     
         17 . A method of stabilizing a therapeutically active agent comprising combining the therapeutically active agent with a polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymer to thereby improve stability of the therapeutically active agent. 
     
     
         18 . A method of stabilizing a therapeutically active agent comprising combining the therapeutically active agent and a polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymer so that a composition according to  claim 5  is formed. 
     
     
         19 . A method of treating a disease affecting an eye comprising administering a composition according to  claim 11  to an eye in need thereof wherein one of the active agents is bimatoprost. 
     
     
         20 . The method of  claim 19  further comprising the active agent brimonidine.