Compositions and methods for treating presbyopia

Abstract

Compositions for treating presbyopia may include active pharmaceutical ingredients of pilocarpine HCl, phenylephrine HCl, pheniramine maleate, and ketorolac tromethamine. Other ingredients may include boric acid, polyethylene glycol, propylene glycol, and BAK (benzalkonium chloride). The pilocarpine HCl may be in a range of 0.1% to 2%. The phenylephrine HCl may be in a range of 0.1% to 1.5%. The pheniramine maleate may be in a range of 0.07% to 0.35%. The ketorolac tromethamine may be in a range of 0.01% to 0.6%. The boric acid may be in a range of 0.5% to 1.5%. The polyethylene glycol may be in a range of 0.1% to 1%. The propylene glycol may be in a range of 0.1% to 1%. The BAK may be in a range of 0.005% to 0.01%. The solvent may be mostly water.

1 .- 16 . (canceled) 
     
     
         17 . A method of providing a therapeutic effect to an eye of a human, wherein the therapeutic effect changes a refractive power in the human eye up to +4.00 diopters, wherein the method comprises administering to the eye of the human an aqueous ophthalmic composition comprising pilocarpine hydrochloride, phenylephrine hydrochloride, pheniramine maleate, and ketorolac tromethamine as active pharmaceutical ingredients. 
     
     
         18 . The method according to  claim 17 , wherein the human has hyperopia. 
     
     
         19 . The method according to  claim 17 , wherein the aqueous ophthalmic composition has a pH in range of 6.39 to 6.51. 
     
     
         20 . The method according to  claim 17 , wherein the aqueous ophthalmic composition has a pH in range of 5.50 to 7.50. 
     
     
         21 . The method according to  claim 17 , wherein the aqueous ophthalmic composition comprises:
 pilocarpine hydrochloride at a concentration in the range of 0.10% w/v to 2.00% w/v;   (ii) phenylephrine hydrochloride at a concentration in the range of 0.10% w/v to 1.50% w/v;   (iii) pheniramine maleate at a concentration in the range of 0.07% w/v to 0.35% w/v; and   (iv) ketorolac tromethamine at a concentration in the range of 0.01% w/v to 0.60% w/v.   
     
     
         22 . The method according to  claim 17 , wherein the aqueous ophthalmic composition further comprises boric acid, polyethylene glycol, propylene glycol, and benzalkonium chloride. 
     
     
         23 . The method according to  claim 22 , wherein the aqueous ophthalmic composition comprises:
 (i) boric acid at a concentration in the range of 0.50% w/v to 1.50% w/v;   (ii) polyethylene glycol at a concentration in the range of 0.10% w/v to 1.00% w/v;   (iii) propylene glycol at a concentration in the range of 0.10% w/v to 1.00% w/v; and   (iv) benzalkonium chloride at a concentration in the range of 0.005% w/v to 0.010% w/v.   
     
     
         24 . The method according to  claim 23 , wherein the aqueous ophthalmic composition comprises:
 (i) pilocarpine hydrochloride at a concentration in the range of 0.10% w/v to 2.00% w/v;   (ii) phenylephrine hydrochloride at a concentration in the range of 0.10% w/v to   
     
     
       1. 50% w/v;
 (iii) pheniramine maleate at a concentration in the range of 0.07% w/v to 0.35% w/v; and 
 (iv) ketorolac tromethamine at a concentration in the range of 0.01% w/v to 0.60% w/v. 
 
     
     
         25 . An ophthalmic dropper bottle comprising an aqueous ophthalmic composition comprising pilocarpine hydrochloride, phenylephrine hydrochloride, pheniramine maleate, and ketorolac tromethamine. 
     
     
         26 . The ophthalmic dropper bottle according to  claim 25 , wherein the aqueous ophthalmic composition has a pH in range of 6.39 to 6.51. 
     
     
         27 . The ophthalmic dropper bottle according to  claim 25 , wherein the aqueous ophthalmic composition has a pH in range of 5.50 to 7.50. 
     
     
         28 . The ophthalmic dropper bottle according to  claim 25 , wherein the aqueous ophthalmic composition comprises:
 pilocarpine hydrochloride at a concentration in the range of 0.10% w/v to 2.00% w/v;   (ii) phenylephrine hydrochloride at a concentration in the range of 0.10% w/v to 1.50% w/v;   (iii) pheniramine maleate at a concentration in the range of 0.07% w/v to 0.35% w/v; and   (iv) ketorolac tromethamine at a concentration in the range of 0.01% w/v to 0.60% w/v.   
     
     
         29 . The ophthalmic dropper bottle according to  claim 25 , wherein the aqueous ophthalmic composition further comprises boric acid, polyethylene glycol, propylene glycol, and benzalkonium chloride. 
     
     
         30 . The ophthalmic dropper bottle according to  claim 29 , wherein the aqueous ophthalmic composition comprises:
 boric acid at a concentration in the range of 0.50% w/v to 1.50% w/v;   (ii) polyethylene glycol at a concentration in the range of 0.10% w/v to 1.00% w/v;   (iii) propylene glycol at a concentration in the range of 0.10% w/v to 1.00% w/v; and   (iv) benzalkonium chloride at a concentration in the range of 0.005% w/v to 0.010% w/v.   
     
     
         31 . The ophthalmic dropper bottle according to  claim 30 , wherein the aqueous ophthalmic composition comprises:
 pilocarpine hydrochloride at a concentration in the range of 0.10% w/v to 2.00% w/v;   (ii) phenylephrine hydrochloride at a concentration in the range of 0.10% w/v to 1.50% w/v;   (iii) pheniramine maleate at a concentration in the range of 0.07% w/v to 0.35% w/v; and   (iv) ketorolac tromethamine at a concentration in the range of 0.01% w/v to 0.60% w/v.   
     
     
         32 . The ophthalmic dropper bottle according to  claim 25 , wherein the aqueous ophthalmic composition provides a therapeutic effect to an eye of a human, wherein the therapeutic effect changes a refractive power in the human eye up to +4.00 diopters.