COMPOSITIONS AND METHODS FOR THE TREATMENT OF PRESBYOPIA
The invention provides compositions and methods for the treatment of presbyopia. The compositions preferably comprise aceclidine, oxymetazoline, a cryoprotectant and a non-ionic surfactant. The compositions optionally contain a viscosity enhancer.
1 . An ophthalmological composition for the treatment of presbyopia comprising aceclidine, oxymetazoline, a cryoprotectant, and a nonionic surfactant.
2 . The composition of claim 1 , wherein the cryoprotectant is selected from the group consisting of a polyol, a sugar, an alcohol, a lower alkanol, a lipophilic solvent, a hydrophilic solvent, a bulking agent, a solubilizer, an antioxidant, a cyclodextrin, a maltodextrin, colloidal silicon dioxide, polyvinyl alcohol, glycine, 2-methyl-2,4-pentanediol, cellobiose, gelatin, polyethylene glycol (PEG), dimethyl sulfoxide (DMSO), formamide and antifreeze protein 752.
3 . The composition of claim 1 , wherein the aceclidine is at a concentration from about 0.25% to about 2.5% w/v, wherein w/v denotes weight by total volume of the composition.
4 . The composition of claim 1 , wherein the cryoprotectant is at a concentration from about 1% to about 10% w/v, wherein w/v denotes weight by total volume of the composition.
5 . The composition of claim 2 , wherein the cryoprotectant is a polyol.
6 . The composition of claim 5 , wherein the polyol is selected from the group consisting of glycerin, pentaerythritol, ethylene glycol, sucrose, mannitol, glycerol, erythritol, lactitol, xylitol, sorbitol, isosorbide, ethylene glycol, propylene glycol, maltitol, threitol, arabitol and ribitol.
7 . The composition of claim 6 , wherein the polyol is mannitol.
8 . The composition of claim 1 , wherein the nonionic surfactant is at a concentration from about 1.0% to about 6.0% w/v, wherein w/v denotes weight by total volume of the composition.
9 . The composition of claim 1 , wherein the nonionic surfactant is selected from the group consisting of a polysorbate, tyloxapol, a poloxamer, a cyclodextrin, vitamin E TPGS and a polyoxyl.
10 . The composition of claim 1 , wherein the nonionic surfactant is polysorbate 80.
11 . The composition of claim 1 , wherein the oxymetazoline is at a concentration from about 0.01% to about 2.0% w/v, wherein w/v denotes weight by total volume of the composition.
12 . An ophthalmological composition for the treatment of presbyopia comprising:
from about 0.25% to about 2.5% w/v aceclidine;
from about 0.01% to about 2.0% w/v oxymetazoline;
from about 1% to about 10% w/v mannitol; and
from about 1% to about 5% w/v polysorbate 80,
wherein w/v denotes weight by total volume of the composition.
13 . The composition of claim 12 , further comprising from about 0.1% to about 2.25% w/v hydroxypropylmethyl cellulose.
14 . An ophthalmological composition for the treatment of presbyopia comprising:
about 1.75% w/v aceclidine;
about 0.125% w/v oxymetazoline;
about 2.5% w/v mannitol;
about 4.0% w/v polysorbate 80; and
about 1.25% w/v hydroxypropylmethyl cellulose,
wherein w/v denotes weight by total volume of the composition
15 . A method of treating presbyopia comprising administering to a subject in need thereof the ophthalmological composition of claim 1 .
16 . The method of claim 15 , wherein the treatment of presbyopia occurs for more than 4 hours.
17 . A method of reducing side effects of ophthalmic aceclidine administration selected from the group consisting of ciliary spasm, ciliary induced brow ache, ciliary induced headache, eye redness a combination thereof comprising administering to a subject in need thereof the ophthalmological composition of claim 1 .