# US 8,569,370 B2 · Ophthalmic compositions and methods for treating eyes

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- Number: US 8,569,370 B2
- Document ID: US8569370B2
- Status: Granted
- Kind: B2
- Application number: 13/842,555
- Filed: 2013-03-15
- Published: 2013-07-25
- Granted: 2013-10-29
- Earliest claimed: 2004-11-16
- Assignees: Allergan, Inc.
- Applicants: Allergan, Inc.
- Inventors: Joseph G. Vehige; Peter A. Simmons; Joan-En Chang-Lin
- Web page: https://patentgrep.com/patent/US8569370B2

## CPC

- A61K 31/205: Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/047: having two or more hydroxy groups, e.g. sorbitol
- A61K 31/14: Quaternary ammonium compounds, e.g. edrophonium, choline (betaines A61K31/205)
- A61K 31/70: Carbohydrates; Sugars; Derivatives thereof (sorbitol A61K31/047)
- A61K 31/717: Celluloses
- A61K 31/728: Hyaluronic acid
- A61K 38/1732: {Lectins}
- A61K 47/02: Inorganic compounds
- 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 47/38: Cellulose; Derivatives thereof
- A61P 27/02: Ophthalmic agents
- 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

Ophthalmic compositions including compatible solute components and/or polyanionic components are useful in treating eyes, for example, to relieve dry eye syndrome, to protect the eyes against hypertonic insult and/or the adverse effects of cationic species on the ocular surfaces of eyes and/or to facilitate recovery from eye surgery.

## Claims

### Claim 1

A method of treating dry eye, wherein the method comprises administering a topical ophthalmic composition comprising a therapeutically effective amount of each of:
an aqueous carrier;
erythritol, and its isomers thereof;
carnitine, its isomers or suitable salts thereof;
glycerin; and
an ionically charged polymeric material selected from the group consisting of carboxymethyl cellulose and mixtures of carboxymethyl cellulose compounds.

### Claim 2 (depends on 1)

The method of claim 1, wherein the composition has an osmolality in a range of 300 to 600 mOsmols/kg.

### Claim 3 (depends on 1)

The method of claim 1, wherein the ionically charged polymeric material is a polyanionic carboxymethyl cellulose present in an amount in a range of 0.1% (w/v) to 2.5% (w/v) of the composition.

### Claim 4 (depends on 1)

The method of claim 1, wherein the polyanionic polymeric material is sodium carboxymethyl cellulose.

### Claim 5 (depends on 1)

The method of claim 1, wherein the composition further comprises stabilized chlorine dioxide, boric acid and sodium citrate.

### Claim 6

A method for treating dry eye, wherein the method comprises dispensing to the ocular surface a composition comprising a therapeutically effective amount of each of:
erythritol, and its isomers thereof;
carnitine, its isomers or suitable salts thereof;
glycerin;
carboxymethylcellulose; and
water.

### Claim 7 (depends on 6)

The method of claim 6, wherein the composition comprises erythritol in an amount between 0.01% (w/v) and 3% (w/v), carnitine in an amount between 0.01% (w/v) and 3% (w/v), and carboxymethylcellulose in an amount between 0.1% (w/v) and 2.5% (w/v).

### Claim 8 (depends on 6)

The method of claim 6, wherein the erythritol is present in an amount between 0.25% (w/v) and 0.75% (w/v), the carnitine is present in an amount between 0.25% (w/v) and 0.75% (w/v), and the carboxymethylcellulose is present in an amount of about 0.5% (w/v).

### Claim 9 (depends on 6)

The method of claim 6, wherein the composition further comprises boric acid, sodium borate, sodium citrate, potassium chloride, calcium chloride, and magnesium chloride.

### Claim 10

A method for the treatment of dry eye, the method comprising administering to an eye needing treatment a composition comprising a therapeutically effective amount of each of:
carnitine, or a stereoisomer or a salt thereof;
erythritol, or a stereoisomer thereof;
glycerin, or a stereoisomer thereof;
at least one anionic cellulose derivative;
a tonicity adjusting component that is not erythritol; and
water.

### Claim 11 (depends on 10)

The method of claim 10, wherein the composition has a tonicity of about 310 Osmols/kg to about 600 Osmols/kg.

### Claim 12 (depends on 10)

The method of claim 10, wherein the composition has a viscosity of about 10 cps to about 70 cps.

### Claim 13 (depends on 10)

The method of claim 10, wherein the anionic cellulose derivative is carboxymethylcellulose at a concentration of about 0.5% w/v.

### Claim 14 (depends on 10)

The method of claim 10, wherein the composition comprises carnitine at a concentration of about 0.25% w/v to about 0.5% w/v.

### Claim 15 (depends on 10)

The method of claim 10, wherein the composition comprises erythritol at a concentration of about 0.25% w/v to about 0.5% w/v.

### Claim 16 (depends on 10)

The method of claim 10, wherein the composition comprises carnitine at a concentration of about 0.1% w/v to about 0.25% w/v.