Ophthalmic formulation and method for ameliorating presbyopia

Abstract

An ophthalmic formulation having an effective amount of a parasympathomimetic agent comprising pilocarpine, or a pharmaceutically acceptable salt thereof, and one or more α1 adrenergic agonists or antagonists is disclosed. The ophthalmic formulation may enable treatment of conditions adversely affecting the visual acuity of a patient, including presbyopia. A method of using the disclosed ophthalmic formulation to treat or ameliorate symptoms of presbyopia is also disclosed.

1 .- 20 . (canceled) 
     
     
         21 . An ophthalmic formulation comprising an effective amount of about 0.1% to about 0.9% by weight pilocarpine or a pharmaceutically acceptable salt thereof, and about 0.3% to about 3% by weight phenylephrine or a pharmaceutically acceptable salt thereof. 
     
     
         22 . The ophthalmic formulation of  claim 21 , wherein the ophthalmic formulation comprises about 0.2% to about 0.7% by weight pilocarpine or a pharmaceutically acceptable salt thereof. 
     
     
         23 . The ophthalmic formulation of  claim 21 , wherein the ophthalmic formulation comprises about 0.6% to about 0.7% by weight phenylephrine or a pharmaceutically acceptable salt thereof. 
     
     
         24 . The ophthalmic formulation of  claim 21 , further comprising about 0.001% to about 0.020% by weight naphazoline or a pharmaceutically acceptable salt thereof. 
     
     
         25 . The ophthalmic formulation of  claim 24 , wherein the formulation comprises about 0.003% naphazoline or a pharmaceutically acceptable salt thereof. 
     
     
         26 . The ophthalmic formulation of  claim 21 , further comprising an anti-histamine selected from the group consisting of pheniramine, chlorpheniramine, dexchlorpheniramine, dexbrompheniramine, deschlorpheniramine, triprolidine, brompheniramine, iodopheniramine, fluorpheniramine, and a pharmaceutically acceptable salt thereof. 
     
     
         27 . The ophthalmic formulation of  claim 26 , wherein the anti-histamine is pheniramine or a pharmaceutically acceptable salt thereof. 
     
     
         28 . The ophthalmic formulation of  claim 27 , wherein the pheniramine is present in an amount of about 0.02% to about 0.2% by weight. 
     
     
         29 . The ophthalmic formulation of  claim 21 , further comprises a non-steroidal anti-inflammatory drug. 
     
     
         30 . The ophthalmic formulation of  claim 29 , wherein the non-steroidal anti-inflammatory drug is selected from the group consisting of nepafenac, meloxicam, diclofenac, bendazac, ketorolac, oxyphenbutazone, bromfenac, flurbiprofen, pranoprofen, surprofen, indomethacin, and a pharmaceutically acceptable salt thereof. 
     
     
         31 . The ophthalmic formulation of  claim 29 , wherein the non-steroidal anti-inflammatory drug is selected from the group consisting of nepafenac, bromfenac, ketorolac and meloxicam. 
     
     
         32 . The ophthalmic formulation of  claim 29 , wherein the non-steroidal anti-inflammatory drug is ketorolac. 
     
     
         33 . A method of ameliorating, reducing or treating presbyopia comprising administering an effective amount of an ophthalmic formulation of  claim 21  to an eye of a patient. 
     
     
         34 . The method of  claim 33 , wherein the ophthalmic formulation further comprises an anti-histamine selected from the group consisting of pheniramine, chlorpheniramine, dexchlorpheniramine, dexbrompheniramine, deschlorpheniramine, triprolidine, brompheniramine, iodopheniramine, fluorpheniramine, and a pharmaceutically acceptable salt thereof. 
     
     
         35 . The method of  claim 34 , wherein the ophthalmic formulation further comprises a non-steroidal anti-inflammatory drug selected from the group consisting of nepafenac, meloxicam, diclofenac, bendazac, ketorolac, oxyphenbutazone, bromfenac, flurbiprofen, pranoprofen, surprofen, indomethacin, and a pharmaceutically acceptable salt thereof.