# US 8,569,273 B2 · Ophthalmic formulations of cetirizine and methods of use

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- Number: US 8,569,273 B2
- Document ID: US8569273B2
- Status: Granted
- Kind: B2
- Application number: 12/888,117
- Filed: 2010-09-22
- Published: 2011-10-20
- Granted: 2013-10-29
- Earliest claimed: 2009-03-17
- Assignees: Aciex Therapeutics, Inc.
- Applicants: Mark Barry Abelson; Matthew J. Chapin; Paul Gomes; George Minno; Jackie Nice
- Inventors: Mark Barry Abelson; Matthew J. Chapin; Paul Gomes; George Minno; Jackie Nice
- Web page: https://patentgrep.com/patent/US8569273B2

## CPC

- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)}
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 27/02: Ophthalmic agents
- A61P 27/14: Decongestants or antiallergics
- A61P 27/16: Otologicals
- 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

The present invention provides stable topical formulations of cetirizine that provide a comfortable formulation when instilled in the eye and is effective in the treatment of allergic conjunctivitis and/or allergic conjunctivitis. The invention further provides methods of treating allergic conjunctivitis rhinitis, and/or allergic rhinoconjunctivitis in a subject in need of such treatment by topical application of the cetirizine formulations of the invention directly to the eye.

## Claims

### Claim 1

A topical ophthalmic formulation comprising 0.1% to 0.25% cetirizine (w/v), 0.005% to 0.01% fluticasone (w/v), 1% Polyethylene Glycol 400, NF, 0.2% Dibasic Sodium Phosphate, Anhydrous, USP, 0.25% Hypromellose, USP, 0.1% Polysorbate 80, NF, 1.8% Glycerin, USP, 0.025% Edetate Disodium, USP and 0.01% Benzalkonium Chloride, NF.

### Claim 2 (depends on 1)

The formulation of claim 1, wherein the pH is about 5.0-8.0.

### Claim 3 (depends on 1)

The formulation of claim 1, wherein the pH is 7.0.

### Claim 4 (depends on 1)

A method of treating a sign or symptom of an ocular or nasal allergic disorder by topically administering to the eye of a subject in need of such treatment the ophthalmic formulation of claim 1.

### Claim 5 (depends on 4)

The method of claim 4, wherein the allergic disorder is against an airborne allergen.

### Claim 6 (depends on 4)

The method of claim 4, wherein the sign or symptom is selected from the group comprising, ocular itching, redness, lid swelling, chemosis, tearing rhinorrhea, sneezing, nasal congestion, nasal itching, itching of the palate, or itching of the ear itching, redness, lid swelling, chemosis, tearing rhinorrhea, sneezing, nasal congestion, nasal itching, itching of the palate, or itching of the ear.

### Claim 7 (depends on 4)

The method of claim 4, wherein the allergic disorder is allergic conjunctivitis, allergic rhinoconjuntivitis or rhinitis.

### Claim 8 (depends on 1)

A method for treating a sign or a symptom of allergic conjunctivitis by topically administering to the eye of a subject in need of such treatment the ophthalmic formulation of claim 1.

### Claim 9 (depends on 8)

The method of claim 8, wherein said sign and symptom is selected from the group consisting of ocular itching, redness, lid swelling, chemosis or tearing.

### Claim 10 (depends on 1)

A method for treating a sign or a symptom of allergic rhinoconjunctivitis by topically administering to the eye of a subject in need of such treatment the ophthalmic formulation of claim 1.

### Claim 11 (depends on 10)

The method of claim 10, wherein said sign and symptom is selected from the group consisting of ocular itching, redness, lid swelling, chemosis, tearing, rhinorrhea, sneezing, nasal congestion, nasal itching, itching of the palate, or itching of the ear.

### Claim 12 (depends on 1)

A method for treating a sign or a symptom of rhinitis by topically administering to the eye of a subject in need of such treatment the ophthalmic formulation of claim 1.

### Claim 13 (depends on 12)

The method of claim 12, wherein said sign and symptom is selected from the group consisting of rhinorrhea, sneezing, nasal congestion, nasal itching, itching of the palate, or itching of the ear.

### Claim 14 (depends on 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)

The method of claim of any one of claims 4 to 13, wherein the ophthalmic formulation is administered once daily.