Controlled-release ophthalmic vehicles
View Patent ↗An ophthalmically acceptable vehicle includes an aqueous suspension having a first viscosity. The suspension includes about 0.1% to about 6.5% by weight of a carboxyl-containing polymer prepared by polymerizing one or more carboxyl-containing monoethylenically unsaturated monomers and less than about 5% by weight of a cross-linking agent. The polymer has average particle size of not more than about 50 μm in equivalent spherical diameter. The vehicle includes a second polymer that allows the carboxyl-containing polymer to remain suspended. Upon contact with tear fluid, the vehicle gels to a second viscosity which is greater than the first viscosity. A method of administering a medicament to the eye of a subject includes applying a composition that includes this ophthalmically acceptable vehicle and a medicament contained for treatment of a disease or disorder for which ophthalmic delivery is indicated. The medicament is released from the vehicle in a sustained release manner.
1. An ophthalmically acceptable drug delivery vehicle, comprising:
an aqueous suspension having a first viscosity, said suspension comprising from about 0.1% to about 6.5% by weight, based on the total weight of the suspension, of a polycarbophil prepared by polymerizing one or more carboxyl-containing monoethylenically unsaturated monomers and less than about 5% by weight of a cross-linking agent, said weight percentages of monomers being based on the total weight of monomers polymerized, said polycarbophil having average particle size of not more than about 50 μm in equivalent spherical diameter, and no more than 5% of said polycarbophil has a particle size below 1 μm, and;
a sufficient amount of chitosan to allow said polycarbophil to remain suspended,
wherein upon contact with tear fluid, said vehicle gels to a second viscosity which is greater than the first viscosity.
2. The vehicle of claim 1 , wherein the chitosan has a molecular weight in the range of from about 1000 to 3000 kDa and is present in a range from between about 0.01% to about 0.15% by weight.
3. The vehicle of claim 1 , wherein the chitosan has a molecular weight of from about 50 to 100 kDa and is present in a range from between about 0.01% and about 0.4% by weight.
4. A composition comprising the ophthalmically acceptable vehicle of claim 1 and a medicament for treatment of a disease or disorder, wherein ocular delivery of said medicament is indicated for the treatment of said disease or disorder.
5. The composition of claim 4 , wherein the composition further comprises an ophthalmically acceptable salt in an amount of from about 0.01% to about 1% by weight, based on the total weight of the composition.
6. The composition of claim 4 , wherein said medicament is present in an amount of from about 0.005% to about 10% by weight, based on the total weight of the composition.
7. The composition of claim 4 , wherein said medicament is selected from the group consisting of an antibacterial antibiotic agent, an antibacterial agent, an antifungal antibiotic agent, an antifungal agent, an antineoplastic agent, a steroidal anti-inflammatory agents, a nonsteroidal anti-inflammatory agent, an anti-allergic agent, a glaucoma-treating agent, an antiviral agent, an anti-mycotic agent, an anti-infective agent, an anti-allergic agent, an antiviral agent, an anti-glaucoma agent, an anesthetic agent, a retinal like anti-angiogenesis agent, an agent to treat AMD, an agent to treat diabetic retinopathy, an agent to treat macular edema, and combinations thereof.
8. The composition of claim 7 , wherein the composition comprises at least two medicaments.
9. The composition of claim 8 , wherein said at least two medicaments are different nonsteroidal anti-inflammatory agents.
10. The composition of claim 8 , wherein said at least two medicaments are a non-steroidal anti-inflammatory agent and a steroidal anti-inflammatory agent.
11. The composition of claim 4 further comprising a preservative.
12. The composition of claim 4 further comprising a thickener.
13. The composition of claim 4 further comprising a wetting agent.
14. A method of administering a medicament to the eye of a subject comprising applying to the eye of a subject a composition comprising the ophthalmically acceptable vehicle of claim 1 and a medicament contained therein for treatment of a disease or disorder for which ophthalmic delivery is indicated;
wherein said medicament is released from the vehicle in a sustained release manner.
15. The vehicle of claim 4 wherein the medicament is ketorolac.
16. The vehicle of claim 15 wherein the ketorolac is present in the composition in an amount of about 0.4% by weight based on the total weight of the composition.
17. The vehicle of claim 15 wherein the ketorolac is present in the composition in an amount of about 0.2% by weight based on the total weight of the composition.