US2022040152A1PendingUtilityA1

Compositions and methods for treating presbyopia, mild hyperopia, and irregular astigmatism

Assignee: ALLERGAN INCPriority: Sep 20, 2011Filed: Mar 17, 2021Published: Feb 10, 2022
Est. expirySep 20, 2031(~5.2 yrs left)· nominal 20-yr term from priority
A61K 31/4178A61K 45/06A61K 9/0048A61K 31/325A61P 27/06A61K 31/27A61K 31/4164A61K 31/4174A61K 31/16A61P 27/10A61K 31/5415A61K 31/541A61P 27/02
70
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Claims

Abstract

The present invention is directed to compositions and methods for treating ocular conditions, including presbyopia, mild hyperopia, irregular astigmatism, hyperopic accommodative esotropia, and glaucoma. The compositions can also be used to potentiate or enhance interventions that retard, reverse, or modify the aging process of the crystalline lens and its surrounding tissues. The compositions include a cholinergic agent, such as a muscarinic acetylcholine receptor M 3 agonist, and an alpha agonist having an imidazoline group or a non-steroidal anti-inflammatory agent (NSAID) having COX-2 selectivity. It has been found that an alpha agonist having an imidazoline group or non-steroidal anti-inflammatory agent (NSAID) having COX-2 selectivity in combination with a cholinergic agent, such as pilocarpine, act synergistically to improve the accommodative and focusing ability of the eye while minimizing the side effects from each compound.

Claims

exact text as granted — not AI-modified
1 - 31 . (canceled) 
     
     
         32 . A composition for treatment of an ocular condition comprising presbyopia, comprising
 a muscarinic acetylcholine receptor M 3  agonist comprising pilocarpine,   an alpha-stimulant agonist having an imidazoline group comprising oxymetazoline, and   an NSAID comprising one or more of meloxicam, celecoxib, rofecoxib, valdecoxib, parecoxib, etoricoxib, nimesulide, etodolac, and nabumetone,   
       wherein the composition is therapeutically effective in the treatment of the ocular condition for at least six hours. 
     
     
         33 . The composition of  claim 32 , wherein the composition further comprises an ophthalmically acceptable carrier. 
     
     
         34 . The composition of  claim 32 , wherein the composition further comprises a cyclodextrin or derivative thereof to enhance ocular penetration of the composition. 
     
     
         35 . The composition of  claim 32 , wherein the composition is in the form of an eye drop, suspension, gel, ointment, injectable solution, or spray. 
     
     
         36 . The composition of  claim 32 , wherein the NSAID is meloxicam. 
     
     
         37 . The composition of  claim 32 , wherein the NSAID is celecoxib. 
     
     
         38 . The composition of  claim 32 , wherein the NSAID is rofecoxib. 
     
     
         39 . The composition of  claim 32 , wherein the NSAID is valdecoxib. 
     
     
         40 . The composition of  claim 32 , wherein the NSAID is parecoxib. 
     
     
         41 . The composition of  claim 32 , wherein the NSAID is etoricoxib. 
     
     
         42 . The composition of  claim 32 , wherein the NSAID is nimesulide. 
     
     
         43 . The composition of  claim 32 , wherein the NSAID is etodolac. 
     
     
         44 . The composition of  claim 32 , wherein the NSAID is nabumetone. 
     
     
         45 . A method of treating an ocular condition in a subject, comprising administering to the subject a therapeutically effective amount of a composition comprising pilocarpine, oxymetazoline, and an NSAID selected from the group consisting of meloxicam, celecoxib, rofecoxib, valdecoxib, parecoxib, etoricoxib, nimesulide, etodolac, and nabumetone; wherein the ocular condition is selected from the group consisting of presbyopia, and wherein the composition is effective for at least six hours. 
     
     
         46 . The method of  claim 45 , wherein administering comprises administering the composition to an eye of the subject. 
     
     
         47 . The method of  claim 45 , wherein the composition is administered to only one eye of the subject. 
     
     
         48 . The method of  claim 45 , wherein the NSAID is meloxicam. 
     
     
         49 . The method of  claim 45  wherein the NSAID is celecoxib. 
     
     
         50 . The method of  claim 45 , wherein the NSAID is rofecoxib. 
     
     
         51 . The method of  claim 45 , wherein the NSAID is valdecoxib. 
     
     
         52 . The method of  claim 45 , wherein the NSAID is parecoxib. 
     
     
         53 . The method of  claim 45 , wherein the NSAID is etoricoxib. 
     
     
         54 . The method of  claim 45 , wherein the NSAID is nimesulide. 
     
     
         55 . The method of  claim 45 , wherein the NSAID is etodolac. 
     
     
         56 . The method of  claim 45 , wherein the NSAID is nabumetone.

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