Ocular formulations for drug-delivery to the posterior segment of the eye
The present invention relates to topical formulations comprising a compound of the following formula: for treating ocular neovascularization. The Compound-I is present in a solution or a suspension in about 0.005% to about 5.0% w/v, such that the solution or suspension delivers the compound at the posterior segment of the eye for inhibiting VEGF in the retina and/or the choroid.
1. A topical ocular formulation, comprising:
an active agent of Formula II:
or a pharmaceutically acceptable salt thereof,
wherein the active agent or the pharmaceutically acceptable salt is present in about 0.1% to about 2.0% w/v,
about 0.2% to about 1% tromethamine,
about 1% to about 2% glycerin, and
hydroxy ethyl cellulose (HEC) or hydroxy propyl methyl cellulose (HPMC), such that the formulation forms a suspension.
2. The formulation of claim 1 , further comprising a solubilizing agent.
3. The formulation of claim 1 , wherein the pharmaceutically acceptable salt is a hydrochloride salt of the formula:
4. The formulation of claim 1 , comprising about 0.1% to about 1.0% w/v of the active agent or a pharmaceutically acceptable salt thereof.
5. The formulation of claim 1 , comprising one or more of benzalkonium chloride (BAK), sodium chloride, and a pH adjusting agent.
6. The formulation of claim 1 , comprising about 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1.0%, or 2.0% w/v of the active agent or a pharmaceutically acceptable salt thereof, and about 0.6% w/v tromethamine.
7. The formulation of claim 1 , comprising about 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1.0%, or 2.0% w/v of the active agent or a pharmaceutically acceptable salt thereof, about 0.6% w/v tromethamine, and about 2% glycerin.
8. The formulation of claim 1 , having a pH value of about 4.5 to 7.5 at or under about 40° C.
9. The formulation of claim 1 , having a pH value of about 6.0 at or under about 40° C.
10. The formulation of claim 1 , having a pH value of about 5.0 to 7.0 at or under about 40° C.
11. The formulation of claim 1 , wherein the formulation is suitable for treating ocular neovascularization.