# US 10,307,368 B2 · Compositions containing alpha-2-adrenergic agonist components

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- Number: US 10,307,368 B2
- Document ID: US10307368B2
- Status: Granted
- Kind: B2
- Application number: 15/481,169
- Filed: 2017-04-06
- Published: 2018-01-25
- Granted: 2019-06-04
- Earliest claimed: 2000-07-14
- Assignees: Allergan, Inc.
- Applicants: Allergan, Inc.
- Inventors: Richard Graham; Peter Bakhit; Orest Olejnik
- Web page: https://patentgrep.com/patent/US10307368B2

## CPC

- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/498: Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
- A61K 31/715: Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K 31/716: Glucans
- A61K 31/734: Alginic acid
- A61K 31/78: of acrylic acid or derivatives thereof
- A61K 47/02: Inorganic compounds
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 27/02: Ophthalmic agents
- 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

Compositions useful for improving effectiveness of alpha-2-adrenergic agonist components include carrier components, alpha-2-adrenergic agonist components, solubility enhancing components which aid in solubilizing the alpha-2-adrenergic agonist components. In one embodiment, the alpha-2-adrenergic agonist components include alpha-2-adrenergic agonists. In another embodiment, the solubility enhancing components include carboxymethylcellulose.

## Claims

### Claim 1

A therapeutically effective aqueous ophthalmic composition for use in reduction of elevated intraocular pressure in patients with open-angle glaucoma and ocular hypertension comprising:
a solution containing 0.1% (w/v) of a compound selected from the group consisting of brimonidine, a salt of brimonidine, and an ester of brimonidine,
wherein the solution further comprises an oxy-chloro preservative and carboxymethyl cellulose,
wherein the composition has a pH between 7.0-8.0.

### Claim 2 (depends on 1)

The composition of claim 1 which comprises about 0.1% (w/v) of brimonidine tartrate.

### Claim 3 (depends on 1)

The composition of claim 1 which comprises 0.1% (w/v) of brimonidine tartrate.

### Claim 4 (depends on 3)

The composition of claim 3 wherein the carboxymethyl cellulose enhances the solubility of brimonidine tartrate in solution.

### Claim 5 (depends on 3)

The composition of claim 3 further comprising boric acid.

### Claim 6 (depends on 3)

The composition of claim 3 further comprising sodium borate.

### Claim 7 (depends on 3)

The composition of claim 3 further comprising hydrochloric acid.

### Claim 8 (depends on 7)

The composition of claim 7 wherein the composition has a pH of 7.4-8.0.