Ophthalmic compositions containing galactomannan polymers and borate

Abstract

The present invention is directed to ophthalmic compositions containing a gelling amount of a combination of galactomannan polysaccharides and borates. The compositions gel or partially gel upon administration to the eye. The present invention also discloses methods of topical ophthalmic administration of the compositions to the eye.

1 . A topical ophthalmic composition comprising one or more galactomannan(s) and one or more borate compound(s), wherein the galactomannan and the borate compound are contained in the composition in concentrations effective to create a gel or partial gel when the composition is administered to an eye.  
     
     
         2 . A composition of  claim 1 , wherein the concentration of the galactomannan is about 0.1 to 5% (w/v) and the concentration of the borate compound is about 0.05 to 5.0% (w/v).  
     
     
         3 . A composition of  claim 1 , wherein the galactomannan is selected from the group consisting of guar gum, locust bean gum, tara gum and chemically modified derivatives thereof.  
     
     
         4 . A composition of  claim 1 , wherein the borate compound is selected from the group consisting of boric acid, sodium borate, potassium borate and combinations thereof.  
     
     
         5 . A composition of  claim 1 , wherein the galactomannan is hydroxypropyl guar and the borate compound is boric acid.  
     
     
         6 . A composition of  claim 1 , wherein the galactomannan is guar gum and the borate compound is boric acid.  
     
     
         7 . A composition of  claim 5 , wherein the composition comprises hydroxypropyl guar in a concentration of 0.2 to 2.0% (w/v) and boric acid in a concentration of 0.1 to 2.0% (w/v).  
     
     
         8 . A composition of  claim 6 , wherein the composition comprises guar gum in a concentration of 0.2 to 2.0% (w/v) and boric acid in a concentration of 0.1 to 2.0% (w/v).  
     
     
         9 . A composition of  claim 1 , further comprising one or more pharmaceutically active agent(s).  
     
     
         10 . A composition of  claim 9 , wherein the concentration of the galactomannan is about 0.1 to 5% (w/v) and the concentration of the borate compound is about 0.05 to 5.0% (w/v).  
     
     
         11 . A composition of  claim 9 , wherein the pharmaceutically active agent(s) is/are selected from the group consisting of: anti-hypertensive, anti-glaucoma, neuro-protective, anti-allergy, muco-secretagogue, angiostatic, anti-microbial, pain relieving and anti-inflammatory agents.  
     
     
         12 . A composition of  claim 9 , wherein the pharmaceutically active agent is selected from the group consisting of: betaxolol, timolol, pilocarpine, carbonic anhydrase inhibitors, prostglandins; post-surgical antihypertensive agents, apraclonidine; ciprofloxacin, tobramycin; naproxen, diclofenac, suprofen, ketorolac, tetrahydrocortisol, dexamethasone; proteins and growth factors.  
     
     
         13 . A method of delivering a pharmaceutical agent to the eye which comprises topically administering to the eye a composition comprising one or more pharmaceutically active agent(s), one or more galactomannan(s) and one or more borate compound(s), wherein the galactomannan and the borate compound are contained in the composition in concentrations effective to create a gel or partial gel when the composition is administered to the eye.  
     
     
         14 . A method of  claim 13 , wherein the composition comprises the galactomannan in a concentration of about 0.1 to 5% (w/v) and the borate compound in a concentration of about 0.05 to 5% (w/v).  
     
     
         15 . A method of  claim 13 , wherein the galactomannan is selected from the group consisting of guar gum, locust bean gum, tara gum and chemically modified derivatives thereof.  
     
     
         16 . A method of  claim 13 , wherein the borate compound is selected from the group consisting of boric acid, sodium borate, potassium borate and combinations thereof.  
     
     
         17 . A method of  claim 13 , wherein the galactomannan is hydroxypropyl guar and the borate compound is boric acid.  
     
     
         18 . A method of  claim 13 , wherein the galactomannan is guar gum and the borate compound is boric acid.  
     
     
         19 . A method of  claim 17 , wherein the composition comprises hydroxypropyl guar in a concentration of 0.2 to 2.0% (w/v) and boric acid in a concentration of 0.1 to 2.0% (w/v).  
     
     
         20 . A method of  claim 18 , wherein the composition comprises guar gum in a concentration of 0.2 to 2.0% (w/v) and boric acid in a concentration of 0.1 to 2.0% (w/v).  
     
     
         21 . A composition of  claim 13 , wherein the pharmaceutically active agent(s) is/are selected from the group consisting of: anti-hypertensive, anti-glaucoma, neuro-protective, anti-allergy, muco-secretagogue, angiostatic, anti-microbial, pain relieving and anti-inflammatory agents.  
     
     
         22 . A composition of  claim 13 , wherein the pharmaceutically active agent is selected from the group consisting of: betaxolol, timolol, pilocarpine, carbonic anhydrase inhibitors, prostglandins; post-surgical antihypertensive agents, apraclonidine; ciprofloxacin, tobramycin; naproxen, diclofenac, suprofen, ketorolac, tetrahydrocortisol, dexamethasone; proteins and growth factors.