# US 2019/0167625 A1 · Methods and compositions for reducing ocular discomfort

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- Number: US 2019/0167625 A1
- Document ID: US20190167625A1
- Status: Published application
- Kind: A1
- Application number: 16/114,902
- Filed: 2018-08-28
- Published: 2019-06-06
- Earliest claimed: 2012-03-30
- Assignees: Brien Holden Vision Institute Limited
- Applicants: Brien Holden Vision Institute
- Inventors: Qian Garrett
- Web page: https://patentgrep.com/patent/US20190167625A1

## 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}
- A61P 27/02: Ophthalmic agents
- G02C 7/04: Contact lenses for the eyes (disinfection or sterilisation of contact lenses A61L12/00)
- 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
- G02C: SPECTACLES; SUNGLASSES OR GOGGLES INSOFAR AS THEY HAVE THE SAME FEATURES AS SPECTACLES; CONTACT LENSES (trial frames for testing the eyes A61B3/04; goggles or eyeshields not having the same features as spectacles A61F9/00)

## Abstract

The invention relates to compositions and devices which include an osmolytic agent, in particular a betaine or carnitine compound, for reducing ocular discomfort associated with various diseases or conditions, in particular diseases or conditions associated with high tear film tonicity. The invention also relates to methods of treating or preventing various diseases or conditions using compositions and devices of the invention.

## Claims

### Claim 1

An ophthalmic device including a physiologically acceptable osmolytic agent, wherein the device permits a therapeutically effective amount of the agent to be desorbed from the device into the eye during wear.

### Claim 2 (depends on 1)

An ophthalmic device according to claim 1, wherein the osmolytic agent is one or more betaine compounds.

### Claim 3 (depends on 1)

An ophthalmic device according to claim 1, wherein the osmolytic agent is one or more carnitine compounds.

### Claim 4 (depends on 1)

An ophthalmic device according to claim 1, wherein the osmolytic agent includes one or more betaine compounds and one or more carnitine compounds.

### Claim 5 (depends on 2)

An ophthalmic device according to claim 2, wherein the betaine compound has a molecular weight of about 600 Da or less.

### Claim 6 (depends on 5)

An ophthalmic device according to claim 5, wherein the betaine compound has a molecular weight of about 250 Da less.

### Claim 7 (depends on 2)

An ophthalmic device according to claim 2, wherein the betaine compound is selected from the group consisting of trimethylglycine, proline betaine, betaine hydrochloride, beta-alanine betaine, hydroxyproline betaine, cocamidopropyl betaine, carbethoxymethyltrimethylammonium hydroxide and analogs thereof.

### Claim 8 (depends on 2)

An ophthalmic device according to claim 2, wherein the betaine compound is selected from the group consisting of trimethylglycine, proline betaine, betaine hydrochloride, beta-alanine betaine and hydroxyproline betaine.

### Claim 9 (depends on 3)

An ophthalmic device according to claim 3, wherein the carnitine compound is selected from the group consisting of L-carnitine, alkanoyl L-carnitines including those selected from the group consisting of acetyl, propionyl, isovaleryl, butyryl, and isobutyryl L-carnitine and their pharmaceutically acceptable salts.

### Claim 10 (depends on 9)

An ophthalmic device according to claim 9, wherein the carntine compound is L-carnitine.

### Claim 11 (depends on 1)

An ophthalmic device according to claim 1, wherein the device is a contact lens.

### Claim 12 (depends on 11)

An ophthalmic device according to claim 11, wherein the contact lens is a single use contact lens.

### Claim 13 (depends on 1)

An ophthalmic device according to claim 1, wherein the device permits a therapeutically effective amount of the osmolytic agent to be desorbed over about a 12 hour period.

### Claim 14 (depends on 1)

An ophthalmic device according to of claim 1, further including a diffusion attenuator.

### Claim 15 (depends on 1)

An ophthalmic device according to claim 1, wherein the diffusion attenuator is vitamin E.

### Claim 16 (depends on 1)

A method for inhibiting, reducing or ameliorating ocular discomfort associated with high tear film tonicity in a subject including applying an ophthalmic device according to claim 1 to the subject.

### Claim 17 (depends on 16)

A method according to claim 16, wherein the method includes a step of determining whether a subject has or is at risk of developing tear film with high tonicity prior to applying the ophthalmic device.

### Claim 18 (depends on 16)

A method according to claim 16, wherein the subject has Dry Eye Syndrome.

### Claim 19

Use of a betaine and/or a carnitine compound in the preparation of an medicament for inhibiting, reducing or ameliorating ocular discomfort associated with high tear film tonicity.

### Claim 20 (depends on 19)

Use according to claim 19, wherein the medicament is an ophthalmic device.

### Claim 21 (depends on 20)

Use according to claim 20, wherein the ophthalmic device is a contact lens.

### Claim 22 (depends on 19)

Use according to claim 19, wherein the medicament does not include erythritol.

### Claim 23

A solution for adding a therapeutically effective amount of one or more betaine compounds and/or one or more carnitine compounds to an ophthalmic device, the solution including a betaine and/or a carntine compound and a physiologically acceptable carrier, dliuent or excipient.

### Claim 24 (depends on 23)

A solution according to claim 23, wherein the carrier, dliuent or excipient facilitates the addition of one or more betaine compounds and/or one or more carnitine compounds to the ophthalmic device.
