# US 9,750,684 B2 · Ophthalmic formulations of cetirizine and methods of use

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- Number: US 9,750,684 B2
- Document ID: US9750684B2
- Status: Granted
- Kind: B2
- Application number: 14/982,258
- Filed: 2015-12-29
- Published: 2016-04-21
- Granted: 2017-09-05
- Earliest claimed: 2009-03-17
- Assignees: Nicox Ophthalmics, Inc.
- Applicants: Aciex Therapeutics, Inc.
- Inventors: Mark Barry Abelson; Matthew J. Chapin; Paul Gomes; George Minno; Jackie Nice
- Web page: https://patentgrep.com/patent/US9750684B2

## CPC

- 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})
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/4174: Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
- A61K 31/4965: Non-condensed pyrazines
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 31/569: substituted in position 17 alpha, e.g. ethisterone
- A61K 47/02: Inorganic compounds
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/26: 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 11/02: Nasal agents, e.g. decongestants
- A61P 27/02: Ophthalmic agents
- A61P 27/14: Decongestants or antiallergics
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

## 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 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% (w/v) cetirizine hydrochloride or dihydrochloride, wherein cetirizine is the only active agent in the formulation and is formulated in a vehicle comprising 1% polyethylene glycol 400, NF, 0.2% dibasic sodium phosphate, anhydrous, USP, 0.25% hypromellose, USP, 0.1% Polysorbate 80, NF, 1.2% to 1.8% glycerin, USP, 0.025% edetate disodium, USP; 0.01% benzalkonium chloride, NF, and purified water, USP, and wherein the formulation has a pH 7 and does not contain a cyclodextrin or other solubilizing compound.

### Claim 2 (depends on 1)

The topical ophthalmic formulation of claim 1, wherein the concentration of cetirizine is 0.1%.

### Claim 3

A topical ophthalmic formulation consisting essentially of 0.1% (w/v) cetirizine, 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; 0.01% Benzalkonium Chloride, NF, and Purified Water, USP, wherein the formulation has a pH 7 and does not contain a cyclodextrin or other solubilizing compound.

### Claim 4 (depends on 3)

The topical ophthalmic formulation according to claim 3, wherein the cetirizine is present as cetirizine hydrochloride or dihydrochloride.