# US 8,772,338 B2 · Enhanced bimatoprost ophthalmic solution

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- Number: US 8,772,338 B2
- Document ID: US8772338B2
- Status: Granted
- Kind: B2
- Application number: 13/827,774
- Filed: 2013-03-14
- Published: 2013-08-08
- Granted: 2014-07-08
- Earliest claimed: 2005-03-16
- Assignees: Allergan, Inc.
- Applicants: Allergan, Inc.
- Inventors: Chin-Ming Chang; James N. Chang; Rhett M. Schiffman; R. Scott Jordan; Joan-En Chang-Lin
- Web page: https://patentgrep.com/patent/US8772338B2

## CPC

- A61K 31/5575: having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
- A01N 33/12: Quaternary ammonium compounds
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/14: Quaternary ammonium compounds, e.g. edrophonium, choline (betaines A61K31/205)
- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K 31/557: Eicosanoids, e.g. leukotrienes {or prostaglandins}
- A61K 47/02: Inorganic compounds
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 27/14: Decongestants or antiallergics
- 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)
- A01N: PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF (preservation of food or foodstuff A23); BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES (preparations for medical, dental or toiletry purposes which kill or prevent the growth or proliferation of unwanted organisms A61K); PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. A method which is useful in treating glaucoma or ocular hypertension related thereto is also disclosed herein.

## Claims

### Claim 1

A method of lowering intraocular pressure in a person with glaucoma or ocular hypertension, the method comprising administering once daily to an eye of the person a first composition comprising about 0.01% w/v bimatoprost and about 0.02% w/v benzalkonium chloride.

### Claim 2 (depends on 1)

The method of claim 1, wherein the method lowers intraocular pressure as effectively and results in less hyperemia as compared to the once daily administration of a second composition comprising 0.03% w/v bimatoprost and 0.005% w/v benzalkonium chloride.

### Claim 3 (depends on 1, 2)

The method of claims 1 or 2, wherein the first composition comprises 0.01% w/v bimatoprost and 0.02% w/v benzalkonium chloride.

### Claim 4 (depends on 2)

The method of claim 2, wherein the first composition further comprises dibasic sodium phosphate.

### Claim 5 (depends on 4)

The method of claim 4, wherein the first composition further comprises citric acid monohydrate.

### Claim 6 (depends on 5)

The method of claim 5, wherein the first composition further comprises sodium chloride.

### Claim 7 (depends on 6)

The method of claim 6, wherein the first composition further comprises hydrochloric acid and sodium hydroxide to adjust the pH.

### Claim 8 (depends on 7)

The method of claim 7, wherein the first composition further comprises water.

### Claim 9 (depends on 1)

The method of claim 1, wherein the first composition has a pH of about 7.3.

### Claim 10

A method of lowering intraocular pressure in a person with glaucoma or elevated intraocular pressure, the method comprising administering at least once daily to an eye of the person a first composition comprising 0.01% w/v bimatoprost and 0.02% w/v benzalkonium chloride and having a pH of about 7.3, wherein the method lowers intraocular pressure and results in less hyperemia as compared to the once daily administration of a second composition comprising 0.03% w/v bimatoprost and 0.005% w/v benzalkonium chloride.

### Claim 11 (depends on 10)

The method of claim 10, wherein the first composition lowers intraocular pressure as effectively as the second composition.

### Claim 12 (depends on 10)

The method of claim 10, wherein the first composition further comprises dibasic sodium phosphate heptahydrate.

### Claim 13 (depends on 12)

The method of claim 12, wherein the first composition further comprises citric acid monohydrate.

### Claim 14 (depends on 13)

The method of claim 13, wherein the first composition further comprises sodium chloride.

### Claim 15 (depends on 14)

The method of claim 14, wherein the first composition further comprises hydrochloric acid and sodium hydroxide to adjust the pH.

### Claim 16 (depends on 15)

The method of claim 15, wherein the first composition further comprises water.

### Claim 17 (depends on 10)

The method of claim 10, wherein the first composition has a pH of 7.3.

### Claim 18 (depends on 10)

The method of claim 10, wherein the first composition is administered once daily.

### Claim 19 (depends on 10)

The method of claim 10, wherein the method is effective in controlling elevated intraocular pressure in patients and lowering elevated intraocular pressure to acceptable levels.

### Claim 20 (depends on 10)

The method of claim 10, wherein the method is effective in treating glaucoma.