# US 10,864,208 B2 · Ophthalmic composition

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- Number: US 10,864,208 B2
- Document ID: US10864208B2
- Status: Granted
- Kind: B2
- Application number: 16/224,286
- Filed: 2018-12-18
- Published: 2019-10-03
- Granted: 2020-12-15
- 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/US10864208B2

## 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

An ophthalmic composition comprising about 0.01% w/v of atropine or its pharmaceutically acceptable salt and deuterated water, at a pD of from about 5 to about 7.

### Claim 2 (depends on 1)

The ophthalmic composition of claim 1, wherein the pharmaceutically acceptable salt of atropine is atropine sulfate.

### Claim 3 (depends on 1)

The ophthalmic composition of claim 1, wherein the ophthalmic composition further comprises sodium chloride.

### Claim 4 (depends on 3)

The ophthalmic composition of claim 3, wherein the ophthalmic composition comprises about 0.9% w/v of sodium chloride.

### Claim 5 (depends on 1)

The ophthalmic composition of claim 1, wherein the ophthalmic composition further comprises benzalkonium chloride (BAK).

### Claim 6 (depends on 5)

The ophthalmic composition of claim 5, wherein the ophthalmic composition comprises from about 0.002% w/v of BAK to about 0.01% w/v of BAK.

### Claim 7 (depends on 5)

The ophthalmic composition of claim 5, wherein the ophthalmic composition comprises about 0.01% w/v of BAK.

### Claim 8 (depends on 1)

The ophthalmic composition of claim 1, wherein the ophthalmic composition further comprises citric acid.

### Claim 9 (depends on 8)

The ophthalmic composition of claim 8, wherein the ophthalmic composition comprises about 0.04% w/v of citric acid.

### Claim 10 (depends on 1)

The ophthalmic composition of claim 1, wherein the pD is about 6.

### Claim 11 (depends on 1)

The ophthalmic composition of claim 1, wherein the ophthalmic composition comprises one of: at least about 80%, at least about 85%, at least about 90%, at least about 93%, at least about 95%, at least about 97%, at least about 98%, or at least about 99% of atropine or its pharmaceutically acceptable salt based on initial concentration after extended period of time under storage condition.

### Claim 12 (depends on 11)

The ophthalmic composition of claim 11, wherein the extended period of time is one of: about 1 week, about 2 weeks, about 3 weeks, about 1 month, about 2 months, about 3 months, about 4 months, about 5 months, about 6 months, about 8 months, about 10 months, about 12 months, about 18 months, about 24 months, about 36 months, about 4 years, or about 5 years.

### Claim 13 (depends on 11)

The ophthalmic composition of claim 11, wherein the storage condition has a storage temperature of from about 2° C. to about 10° C. or from about 16° C. to about 26° C.

### Claim 14 (depends on 1)

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

### Claim 15 (depends on 14)

The ophthalmic composition of claim 14, wherein the pD adjusting agent comprises deuterated hydrochloric acid, deuterated sodium hydroxide, deuterated acetic acid, or deuterated citric acid.

### Claim 16 (depends on 14)

The ophthalmic composition of claim 14, wherein the pD adjusting agent comprises hydrochloric acid, sodium hydroxide, acetic acid, or citric acid.

### Claim 17

An ophthalmic composition comprising about 0.03% w/v of atropine or its pharmaceutically acceptable salt and deuterated water, at a pD of from about 5 to about 7.

### Claim 18 (depends on 17)

The ophthalmic composition of claim 17, wherein the pharmaceutically acceptable salt of atropine is atropine sulfate.

### Claim 19 (depends on 17)

The ophthalmic composition of claim 17, wherein the ophthalmic composition further comprises sodium chloride.

### Claim 20 (depends on 19)

The ophthalmic composition of claim 19, wherein the ophthalmic composition comprises about 0.9% w/v of sodium chloride.

### Claim 21 (depends on 17)

The ophthalmic composition of claim 17, wherein the ophthalmic composition further comprises benzalkonium chloride (BAK).

### Claim 22 (depends on 21)

The ophthalmic composition of claim 21, wherein the ophthalmic composition comprises from about 0.002% w/v of BAK to about 0.01% w/v of BAK.

### Claim 23 (depends on 21)

The ophthalmic composition of claim 21, wherein the ophthalmic composition comprises about 0.01% w/v of BAK.

### Claim 24 (depends on 17)

The ophthalmic composition of claim 17, wherein the ophthalmic composition further comprises citric acid.

### Claim 25 (depends on 24)

The ophthalmic composition of claim 24, wherein the ophthalmic composition comprises about 0.04% w/v of citric acid.

### Claim 26 (depends on 17)

The ophthalmic composition of claim 17, wherein the pD is about 6.

### Claim 27 (depends on 17)

The ophthalmic composition of claim 17, wherein the ophthalmic composition comprises one of: at least about 80%, at least about 85%, at least about 90%, at least about 93%, at least about 95%, at least about 97%, at least about 98%, or at least about 99% of atropine or atropine sulfate based on initial concentration after extended period of time under storage condition.

### Claim 28 (depends on 27)

The ophthalmic composition of claim 27, wherein the extended period of time is one of: about 1 week, about 2 weeks, about 3 weeks, about 1 month, about 2 months, about 3 months, about 4 months, about 5 months, about 6 months, about 8 months, about 10 months, about 12 months, about 18 months, about 24 months, about 36 months, about 4 years, or about 5 years.

### Claim 29 (depends on 27)

The ophthalmic composition of claim 27, wherein the storage condition has a storage temperature of from about 2° C. to about 10° C. or from about 16° C. to about 26° C.

### Claim 30 (depends on 17)

The ophthalmic composition of claim 17, wherein the ophthalmic composition further comprises a pD adjusting agent.

### Claim 31 (depends on 30)

The ophthalmic composition of claim 30, wherein the pD adjusting agent comprises deuterated hydrochloric acid, deuterated sodium hydroxide, deuterated acetic acid, or deuterated citric acid.

### Claim 32 (depends on 30)

The ophthalmic composition of claim 30, wherein the pD adjusting agent comprises hydrochloric acid, sodium hydroxide, acetic acid, or citric acid.