Compositions and methods for treating presbyopia, mild hyperopia, and irregular astigmatism
The present invention is directed to compositions and methods for treating presbyopia, mild hyperopia, and irregular astigmatism. 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.
1. A composition for treatment of an ocular condition comprising presbyopia, comprising
a muscarinic acetylcholine receptor M 3 agonist comprising pilocarpine, and
an alpha-stimulant agonist having an imidazoline group comprising oxymetazoline,
wherein the composition is therapeutically effective in the treatment of the ocular condition for at least six hours.
2. The composition of claim 1 , wherein the composition comprises:
from about 0.01% to about 4% w/v pilocarpine; and
from about 0.01% to about 0.5% w/v oxymetazoline.
3. The composition of claim 1 , wherein the composition comprises:
from about 0.01% to about 2% w/v pilocarpine; and
from about 0.01% to about 0.2% w/v oxymetazoline.
4. The composition of claim 1 , wherein the composition comprises:
from about 0.5% to about 1.5% w/v pilocarpine; and
from about 0.02% to about 0.1% w/v oxymetazoline.
5. The composition of claim 1 , wherein the composition further comprises an ophthalmically acceptable carrier.
6. The composition of claim 1 , wherein the composition further comprises a cyclodextrin or derivative thereof to enhance ocular penetration of the composition.
7. The composition of claim 1 , wherein the composition is in the form of an eye drop, suspension, gel, ointment, injectable solution, or spray.
8. The composition of claim 1 , wherein the composition comprises from about 0.01% to about 10% w/v pilocarpine and from about 0.01% to about 0.5% w/v oxymetazoline.
9. The composition of claim 1 , wherein the composition comprises from about 0.5% to about 2% w/v pilocarpine and from about 0.02% to about 0.125% w/v oxymetazoline.
10. The composition of claim 1 , wherein the composition comprises from about 0.03% to about 1.8% w/v pilocarpine.
11. The composition of claim 1 , wherein the composition comprises from about 0.00625% to about 0.125% w/v oxymetazoline.