IP Library Granted Patent US 12,268,779
Granted Patent B2
US 12,268,779 · App. 18/319,794 · Granted Apr 8, 2025

Ophthalmic emulsion

Inventors: Howard Allen Ketelson (Dallas, TX); David L. Meadows (Colleyville, TX)
Assignee: Alcon Inc.
A61K9/107A61K9/0048C09K23/017C09K23/14C09K23/34
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Quick Facts
Patent No.
US 12,268,779
App. No.
18/319,794
Granted
Apr 8, 2025
Kind
B2
Abstract

The present invention is directed to an ophthalmic emulsion. The emulsion has a unique combination of ingredients that promotes the stability of small oil droplets within the emulsion. The emulsion also includes a mucoadhesive polymer that aid in delivering a lipid to the ocular surface.

Claims (28)

1. An ophthalmic emulsion, the emulsion comprising:

water forming an aqueous phase;

oil forming an oil phase, wherein the oil is a hydrocarbon selected from mineral oil, paraffin oil and petrolatum, wherein the oil is at least 0.1 w/v % and no greater than 5 w/v %;

a hydrophilic surfactant having an HLB value of at least 8;

a hydrophobic surfactant having an HLB value of below 8;

an anionic phospholipid, wherein the anionic phospholipid is present in the emulsion in a concentration from 0.05 to 7.0 percent by weight;

borate;

a mucoadhesive galactomannan polymer, wherein the mucoadhesive galactomannan polymer is present in the emulsion in a concentration of at least 0.01 w/v %, but no greater than 1.0 w/v %;

an ophthalmic therapeutic agent for the treatment of ophthalmic diseases;

wherein the emulsion is free of a benzalkonium chloride,

wherein:

i. the oil phase is in droplets within the aqueous phase and the droplets have an average diameter that is no greater than about 1000 nm, but is at least 10 nm, wherein the average diameter is corresponding to 90% of the cumulative undersize distribution by volume measured using a Microtrac S3500 Particle Size Analyzer (Software Version 10.3.1); and

ii. the borate and galactomannan polymer cooperatively act to form a gel upon instillation of the emulsion in an eye of an individual.

2. The emulsion according to claim 1 , wherein the hydrophilic surfactant is present in the emulsion in an amount that is at least 0.08 w/v % and is present in the emulsion in an amount that is no greater than 0.8 w/v %.

3. The emulsion according to claim 1 , wherein the hydrophilic surfactant is polyoxyethylene-40-stearate.

4. The emulsion according to claim 1 , wherein the hydrophobic surfactant is present in the emulsion in an amount that is at least 0.11 w/v % and is present in the emulsion in an amount that is no greater than 2.0 w/v %.

5. The emulsion according to claim 1 , wherein the hydrophobic surfactant is a sorbitan tristearate.

6. The emulsion according to claim 1 , wherein the mucoadhesive galactomannan polymer is selected from the group consisting of guar and hydroxypropyl guar.

7. The emulsion according to claim 1 , wherein the anionic phospholipid is dimyristoyl phosphatidylglycerol.

8. The ophthalmic composition according to claim 1 , wherein the ophthalmic therapeutic agent is selected from a group consisting of anti-glaucoma agent, anti-angiogenesis agent; anti-infective agent; anti-inflammatory agent; growth factor; immunosuppressant agent; and anti-allergic agent.

9. The ophthalmic composition according to claim 8 , wherein the anti-glaucoma agent is betaxolol, levobetaxolol, brinzolamide, dorzolamide, travoprost, bimatoprost, or latanoprost.

10. The ophthalmic composition according to claim 8 , wherein the anti-angiogenesis agent is anecortave acetate or receptor tyrosine kinase inhibitors.

11. The ophthalmic composition according to claim 8 , wherein the anti-infective agent is triamcinolone actinide, suprofen, diclofenac, ketorolac, nepafenac, rimexolone, or tetrahydrocortisol.

12. The ophthalmic composition according to claim 8 , wherein the growth factor is EGF or VEGF.

13. The ophthalmic composition according to claim 8 , wherein the anti-allergic agent is olopatadine or epinastine.

14. The ophthalmic composition according to claim 8 , wherein the dry eye relieve agent is cilomilast, cyclosporins, or combinations thereof.

15. The ophthalmic composition according to claim 8 , wherein the ophthalmic therapeutic agent is present in the emulsion at a concentration of at least 0.005 w/v % and no greater than 10 w/v %.

16. The ophthalmic composition according to claim 15 , wherein the ophthalmic therapeutic agent is present in the emulsion at a concentration of at least 0.01 w/v % and no greater than 4.0 w/v %.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 18, 2023
From: KETELSON, HOWARD ALLEN; MEADOWS, DAVID L.
To: ALCON RESEARCH, LTD.
Reel/Frame 063685/0830 →
MERGER AND CHANGE OF NAME Recorded May 18, 2023
From: ALCON RESEARCH, LTD.; ALCON RESEARCH, LLC
To: ALCON RESEARCH, LLC
Reel/Frame 063685/0900 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 18, 2023
From: ALCON RESEARCH, LLC
To: NOVARTIS AG
Reel/Frame 063685/0965 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 18, 2023
From: NOVARTIS AG
To: ALCON INC.
Reel/Frame 063686/0035 →
Continuity (8)
Continuation 17200043 · Mar 12, 2021
Continuation 16811461 · Mar 6, 2020
Continuation 16405180 · May 7, 2019
Continuation 15989383 · May 25, 2018
Continuation 15228589 · Aug 4, 2016
Continuation 12958763 · Dec 2, 2010
Provisional Application 61266207 · Dec 3, 2009
Related Publication 20230285289A1 · Sep 14, 2023
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