Topical Brimonidine Tartrate Ophthalmic Solution

Abstract

The present invention provides an aqueous ophthalmic composition comprising an alpha-2 adrenergic receptor agonist and a non-ionic cellulosic polymer, the solution having a pH less than 6.5. The present invention also provides an aqueous ophthalmic composition comprising an alpha-2 adrenergic receptor agonist and a benzododecinium halide. Also provided are methods of manufacture, use and method of reducing intraocular pressure in the patient in need thereof.

1 . A method of reducing elevated intraocular pressure in a patient in need thereof, the method comprising administering a therapeutically effective amount of a composition comprising:
 0.05-0.2% (w/v) of brimonidine tartrate; and   about 0.1-1.0% (w/v) hydroxypropyl methyl cellulose;   wherein the composition is administered to at least one eye of the patient.   
     
     
         2 . (canceled) 
     
     
         3 . The method of  claim 1 , wherein the composition comprises 0.15% (w/v) of brimonidine tartrate. 
     
     
         4 . The method of  claim 1 , wherein the composition comprises 0.1% (w/v) of brimonidine tartrate. 
     
     
         5 - 8 . (canceled) 
     
     
         9 . The method of  claim 1 , wherein the composition is highly soluble at a pH of 6.5 or less. 
     
     
         10 . The method of  claim 1 , wherein the pH of the composition is in the range of 5.5-6.5. 
     
     
         11 . The method of  claim 1 , wherein the composition further comprises a quaternary ammonium compound as a preservative in the amount of 0.001-1.0% (w/v). 
     
     
         12 . (canceled) 
     
     
         13 . The method of  claim 11 , wherein the sole quaternary ammonium compound included in the composition id benzododecinium bromide. 
     
     
         14 . The method of  claim 1 , wherein the composition is further devoid of an oxidative preservative. 
     
     
         15 . A method of lowering the intraocular pressure in a patient with glaucoma or ocular hypertension, comprising administering to the patient a therapeutically effective amount of a composition comprising:
 0.05-0.2% (w/v) of brimonidine tartrate; and   about 0.1-1.0% (w/v) hydroxypropyl methyl cellulose.   
     
     
         16 - 24 . (canceled) 
     
     
         25 . The method of  claim 1 , wherein the composition is devoid of an anionic solubility enhancing component. 
     
     
         26 . (canceled) 
     
     
         27 . The method of  claim 1 , wherein the composition comprises:
 a) 0.1% (w/v) brimonidine tartrate;   b) 0.5% (w/v) hydroxypropyl methylcellulose; and   c) 0.012% (w/v) benzododecinium, and pharmaceutically acceptable excipients, wherein the composition is highly soluble at a pH of 6.5 or less.   
     
     
         28 - 30 . (canceled)