Ophthalmic composition

Abstract

The present invention provides an ophthalmic composition comprising a hyperbranched polyester. The ophthalmic compositions may also comprise carbonic anhydrase inhibitors, wherein the hyperbranched polyester increases the aqueous solubility of the carbonic anhydrase inhibitor, and increases corneal permeation of the active agent. The ophthalmic compositions may also comprise non-ionic surfactants, such as PEG, Polysorbate, HPMC or HEC, and beta-blockers, such as Carteolol, Levobunolol, Betaxolol, Metipranolol, Timolol or Propranolol. The concentration of the hyperbranched polyester in the ophthalmic formulation should be less than or equal to 4% (w/v) in order to avoid any cytotoxic effects on human corneal cells and thus the eye irritation.

1 . An ophthalmic composition comprising a hyperbranched polymer, wherein the hyperbranched polymer comprises a terminal functional group selected from the group consisting of an amine group, a hydroxyl group, a fatty acid group, and PEG. 
     
     
         2 . The ophthalmic composition according to  claim 1 , further comprising a carbonic anhydrase inhibitor. 
     
     
         3 . The ophthalmic composition according to  claim 1 , further comprising a non-ionic surfactant. 
     
     
         4 . The ophthalmic composition according to  claim 2 , further comprising a non-ionic surfactant. 
     
     
         5 . The ophthalmic composition according to  claim 1 , wherein the average molecular weight of the hyperbranched polymer is in the range from 1,000 to 750,000 Daltons (M W ). 
     
     
         6 . The ophthalmic composition according to  claim 1 , wherein the hyperbranched polymer comprises a core selected from the group consisting of Polyethylenimine, Polypropylenimine, and polyester. 
     
     
         7 . The ophthalmic composition according to  claim 1 , wherein the pH is in the range from 3.0 to 8.0. 
     
     
         8 . The ophthalmic composition according to  claim 1 , wherein the concentration of the hyperbranched polymer is in the range from 0.01% to 5% (w/v). 
     
     
         9 . The ophthalmic composition according to  claim 2 , further comprising a beta-blocker. 
     
     
         10 . The ophthalmic composition according to  claim 2 , wherein the carbonic anhydrase inhibitor is selected from the group consisting of Dorzolamide, Brinzolamide and Acetazolamide. 
     
     
         11 . The ophthalmic composition according to  claim 3 , wherein the non-ionic surfactant is selected from the group consisting of PEG, polysorbate, Hydroxyl Propyl Methyl Cellulose, and Hydroxy Ethyl Cellulose. 
     
     
         12 . The ophthalmic composition according to  claim 4 , wherein the non-ionic surfactant is selected from the group consisting of PEG, Polysorbate, Hydroxyl Propyl Methyl Cellulose, and Hydroxy Ethyl Cellulose. 
     
     
         13 . The ophthalmic composition according to  claim 9 , wherein the beta-blocker is selected from the group consisting of Carteolol, Levobunolol, Betaxolol, Metipranolol, Timolol and Propranolol. 
     
     
         14 . The ophthalmic composition according to  claim 6 , wherein the hyperbranched polymer core is polyester, and wherein the hyperbranched polymer comprises a hydroxyl group, a fatty acid group, and PEG as terminal functional groups. 
     
     
         15 . The ophthalmic composition according to the  claim 14 , wherein the average molecular weight of the hyperbranched polymer is in the range from 1,000 to 12,000 Daltons (M W ). 
     
     
         16 . The ophthalmic composition according to  claim 14 , wherein the concentration of the hyperbranched polymer is in the range from 0.001 to 4% (w/v). 
     
     
         17 . An ophthalmic composition comprising a hyperbranched polyester, Timolol, Dorzolamide, and Polysorbate 80, wherein the hyperbranched polyester comprises a terminal functional group selected from the group consisting of a polyester hydroxyl group, a fatty acid group, and PEG. 
     
     
         18 . An ophthalmic composition comprising a hyperbranched polyester, Timolol, Brinzolamide, and Polysorbate 80, wherein the hyperbranched polyester comprises a terminal functional group selected from the group consisting of a polyester hydroxyl group, a fatty acid group, and PEG.