# US 11,896,588 B2 · Ophthalmic composition

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- Number: US 11,896,588 B2
- Document ID: US11896588B2
- Status: Granted
- Kind: B2
- Application number: 18/055,945
- Filed: 2022-11-16
- Published: 2023-03-23
- Granted: 2024-02-13
- Earliest claimed: 2014-06-24
- Assignees: Sydnexis, Inc.
- Applicants: Sydnexis, Inc.
- Inventors: Gregory I. Ostrow; Kenneth J. Widder; David S. Baker
- Web page: https://patentgrep.com/patent/US11896588B2

## CPC

- A61K 31/46: 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 47/02: Inorganic compounds
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- 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
- A61P 27/02: Ophthalmic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

Provided herein is an ophthalmic composition. In some embodiments, the ophthalmic composition includes a low concentration of an ophthalmic agent for treatment of an ophthalmic disorder or condition; and an ophthalmically acceptable carrier, Wherein the ophthalmic agent is distributed with substantial uniformity throughout the ophthalmically acceptable carrier. Further disclosed herein include an ophthalmic composition including a low concentration of an ophthalmic agent and deuterated water. Also disclosed herein are methods of arresting or preventing myopia development by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.

## Claims

### Claim 1

A stabilized ophthalmic composition for treating pre-myopia, myopia, or progression of myopia, comprising from about 0,001 wt % to about 0.05 wt % of atropine or atropine sulfate and deuterated water, wherein the stabilized ophthalmic composition further comprises a buffering agent at a pD from about 4.2 to about 7.9, wherein the buffering agent comprises a citrate buffering agent, an acetate buffering agent, or a combination thereof.

### Claim 2 (depends on 1)

The stabilized ophthalmic composition of claim 1, wherein the buffering agent has a pD from about 4.2 to about 6.8.

### Claim 3 (depends on 1)

The stabilized ophthalmic composition of claim 1, further comprising noratropine, atropine-N-oxide, tropine, tropic acid, hyoscine, scopolamine, tropicamide, cyclopentolate, pirenzepine, homatropine, or a combination thereof.

### Claim 4 (depends on 1)

The stabilized ophthalmic composition of claim 1, wherein the atropine or atropine sulfate is present in the composition at a concentration of from about 0.001 wt % to about 0.03 wt %.

### Claim 5 (depends on 1)

The stabilized ophthalmic composition of claim 1, wherein the atropine or atropine sulfate is present in the composition at a concentration of from about 0.001 wt % to about 0.02 wt %.

### Claim 6 (depends on 1)

The stabilized ophthalmic composition of claim 1, wherein the atropine or atropine sulfate is present in the composition at a concentration of from about 0,001 wt % to about 0.01 wt %.

### Claim 7 (depends on 1)

The stabilized ophthalmic composition of claim 1, wherein the buffering agent further comprises a carbonate buffering agent, an organic buffering agent, an amino acid buffering agent, or a combination thereof.

### Claim 8 (depends on 1)

The stabilized ophthalmic composition of claim 1, wherein the stabilized ophthalmic composition further comprises a tonicity adjusting agent.

### Claim 9 (depends on 8)

The stabilized ophthalmic composition of claim 8, wherein the tonicity adjusting agent comprises a halide salt of a monovalent cation.

### Claim 10 (depends on 1)

The stabilized ophthalmic composition of claim 1, further comprising an ophthalmically acceptable viscosity agent.

### Claim 11 (depends on 10)

The stabilized ophthalmic composition of claim 10, wherein the ophthalmically acceptable viscosity agent comprises hydroxyethyl cellulose, hydroxypropyl cellulose, or hydroxypropylmethyl-cellulose (HPMC).

### Claim 12 (depends on 1)

The stabilized ophthalmic composition of claim 1, further comprising a preservative.

### Claim 13 (depends on 12)

The stabilized ophthalmic composition of claim 12, wherein a concentration of the preservative is from about 0.0001% to about 1%.

### Claim 14 (depends on 12)

The stabilized ophthalmic composition of claim 12, wherein the preservative is selected from benzalkonium chloride, certrimonium, sodium perborate, stabilized oxychloro complex, polyquaternium-1, chlorobutanol, edetate di sodium, polydexamethylene biguanide, or combinations thereof.

### Claim 15 (depends on 1)

The stabilized ophthalmic composition of claim 1, wherein the stabilized ophthalmic composition is essentially free of procaine and benactyzine, and pharmaceutically acceptable salts thereof.

### Claim 16 (depends on 1)

A method of treating the pre-myopia, myopia or progression of myopia in an individual in need thereof, comprising administering to an eye of the individual an effective amount of the stabilized ophthalmic composition of claim 1.

### Claim 17 (depends on 16)

The method of claim 16, wherein the stabilized ophthalmic composition is administered topically.

### Claim 18 (depends on 16)

The method of claim 16, wherein the stabilized ophthalmic composition is administered by instillation.

### Claim 19 (depends on 16)

The method of claim 16, wherein the stabilized ophthalmic composition is administered through an eye drop bottle containing the stabilized ophthalmic composition.

### Claim 20

A stabilized ophthalmic composition for treating pre-myopia, myopia, or progression of myopia, comprising from about 0,001 wt % to about 0.05 wt % of atropine or atropine sulfate and deuterated water, wherein the stabilized ophthalmic composition further comprises a buffering agent at a pD from about 4.2 to about 7.9, wherein the buffering agent consists essentially of citrate buffering agent, an acetate buffering agent, or a combination thereof.
