# US 12,005,139 B2 · Ophthalmic formulations and related methods

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- Number: US 12,005,139 B2
- Document ID: US12005139B2
- Status: Granted
- Kind: B2
- Application number: 18/207,339
- Filed: 2023-06-08
- Published: 2023-10-05
- Granted: 2024-06-11
- Earliest claimed: 2022-03-08
- Assignees: Eternatear, Inc.
- Applicants: EternaTear, Inc.
- Inventors: Timothy R Willis; Ralph P. Stone
- Web page: https://patentgrep.com/patent/US12005139B2

## CPC

- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14)
- A61P 27/04: Artificial tears; Irrigation solutions
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

This disclosure is directed to ophthalmic suspensions for dry eye and other ocular indications that provide long-lasting on eye benefits. The disclosure provides methods of increasing lipid layer thickness and methods of lubricating an eye. The disclosure also provides methods of maintaining integrity of an eye's tear film layers which increases the eye's lipid layer thickness and methods of recreating or building one or more layers of an eye's tear film.

## Claims

### Claim 1

An ophthalmic suspension comprising
i) an aqueous phase comprising water and one or more components selected from the group consisting of at least one wax ester, at least one anionic polar surfactant, at least one nonionic surfactant, at least one salt, and at least one phosphate; and
ii) an oil phase comprising at least one mineral oil and, optionally, at least one wax ester,
wherein the ophthalmic suspension exhibits a Zeta potential of from about −60 mV to about −110 mV.

### Claim 2 (depends on 1)

The ophthalmic suspension of claim 1, wherein the ophthalmic suspension has an osmolality of from about 245 mOsmol/kg to about 315 mOsmol/kg.

### Claim 3 (depends on 1)

The ophthalmic suspension of claim 1, wherein the ophthalmic suspension is formulated as a free flowing emulsified suspension at about 30° C.

### Claim 4 (depends on 1)

The ophthalmic suspension of claim 1, wherein the ophthalmic suspension includes a total wax ester content of about 0.8 weight percent to about 1.2 weight percent.

### Claim 5 (depends on 1)

The ophthalmic suspension of claim 1, wherein the ophthalmic suspension exhibits an ionic mobility of from about −5.9 (μms)/(V/cm) to about −7.4 (μms)/(V/cm).

### Claim 6 (depends on 1)

The ophthalmic suspension of claim 1, wherein the oil s a mixture of a lightweight mineral oil and a heavy weight mineral oil.

### Claim 7 (depends on 6)

The ophthalmic suspension of claim 6, wherein the lightweight mineral oil exhibits a kinetic viscosity of from about 3.0 mm2s−1 to about 34.4 mm2s−1 at 40° C. and the heavy weight mineral oil exhibits a viscosity of kinetic viscosity of from about 34.5 mm2s−1 to about 150 mm2s−1 at 40° C.

### Claim 8 (depends on 1)

The ophthalmic suspension of claim 1, further comprising an anionic polar surfactant comprising a mixture of a polysorbate non-ionic surfactant at a concentration of about 0.35 to about 0.45 weight percent and an anionic polar dimyristoylphosphatidylglycerol at a concentration of about 0.35 to about 0.55 weight percent.

### Claim 9 (depends on 1)

The ophthalmic suspension of claim 1, packaged in a sterile multi-use or sterile single use container.

### Claim 10 (depends on 1)

The ophthalmic suspension of claim 1, packaged in a multi-dose non-preserved (MDNP) container or a container including at least one preservative.

### Claim 11 (depends on 1)

The ophthalmic suspension of claim 1, wherein the ophthalmic suspension increases lipid layer thickness by at least 20 nanometers at 60 minutes after administration.

### Claim 12 (depends on 1)

The ophthalmic suspension of claim 1, wherein the ophthalmic suspension increases lipid layer thickness by at least 20 nanometers at two hours after administration.