# US 9,517,220 B2 · Bromfenac bioavailability

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- Number: US 9,517,220 B2
- Document ID: US9517220B2
- Status: Granted
- Kind: B2
- Application number: 13/649,271
- Filed: 2012-10-11
- Published: 2013-04-18
- Granted: 2016-12-13
- Earliest claimed: 2011-10-12
- Assignees: Bausch & Lomb Pharma Holdings Corp.
- Applicants: Angel Padilla; George Baklayan
- Inventors: Angel Padilla; George Baklayan
- Web page: https://patentgrep.com/patent/US9517220B2

## CPC

- A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/14: Quaternary ammonium compounds, e.g. edrophonium, choline (betaines A61K31/205)
- A61K 31/775: Phenolic resins
- A61K 31/79: Polymers of vinyl pyrrolidone
- A61K 33/04: Sulfur, selenium or tellurium; Compounds thereof
- A61K 47/02: Inorganic compounds
- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- 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: 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)

## Abstract

Formulations and methods that provided enhanced bromfenac penetration into ocular tissue when topically administered, compared to the currently available BROMDAY™ formulation and method when topically administered. The formulations and methods did so while retaining the patient convenience of a once-daily administration and advantageously lowered the bromfenac concentration dosed to the patient.

## Claims

### Claim 1

A method for treating an ocular condition in a patient in need thereof with bromfenac, the method comprising
administering bromfenac as the only active 0.07% w/v in a composition at a pH≧6.0 and pH<8.0 and containing 1.0% povidone, topically to the eye of the patient, enhancing bromfenac penetration into ocular tissue to provide the same or better therapy than a higher bromfenac concentration.

### Claim 2 (depends on 1)

The method of claim 1 wherein the bromfenac formulation is at pH≧7.0 and ≦7.8.

### Claim 3 (depends on 1)

The method of claim 1 wherein the bromfenac formulation contains 0.07% bromfenac and is at pH 7.0.

### Claim 4 (depends on 1)

The method of claim 1 wherein the bromfenac formulation contains 0.07% bromfenac and is at pH 7.1.

### Claim 5 (depends on 1)

The method of claim 1 wherein the bromfenac formulation contains 0.07% bromfenac and is at pH 7.2.

### Claim 6 (depends on 1)

The method of claim 1 wherein the bromfenac formulation contains 0.07% bromfenac and is at pH 7.3.

### Claim 7 (depends on 1)

The method of claim 1 wherein the bromfenac formulation contains 0.07% bromfenac and is at pH 7.4.

### Claim 8 (depends on 1)

The method of claim 1 wherein the bromfenac formulation contains 0.07% bromfenac and is at pH 7.5.

### Claim 9 (depends on 1)

The method of claim 1 wherein the bromfenac formulation further comprises at least one of tyloxapol, sodium sulfite, and benzalkonium chloride.

### Claim 10 (depends on 1)

The method of claim 1 wherein the bromfenac formulation further comprises at least one of tyloxapol at a concentration of 0.01% to 0.5%, sodium sulfite, or benzalkonium chloride at a concentration of ≦0.01%.

### Claim 11 (depends on 1)

The method of claim 1 wherein the ocular condition is selected from the group consisting of meibomianitis, blepharitis, uveitis, iritis, conjunctival hyperemia, eyelid hyperemia, keratitis, ocular rosacea, scleritis, wet age related macular degeneration, diabetic retinopathy, diabetic macular edema, central retinal vein occlusion, branch retinal vein occlusion, anterior chamber inflammation, allergic conjunctivitis, conjunctivitis, surgical trauma, dry eye, viral conjunctivitis, bacterial conjunctivitis, anterior uveitis, penetration from a foreign body, burns (chemical, radiation, or thermal), and combinations thereof.

### Claim 12 (depends on 1)

The method of claim 1 wherein administration is to a post-cataract surgery patient and treats post-cataract surgery pain, post-surgery inflammation, or both in the patient.

### Claim 13 (depends on 1)

The method of claim 1 wherein administration is once daily prior to surgery performed on the patient and continues once daily through day 14 after said surgery.

### Claim 14 (depends on 1)

The method of claim 1 wherein the ocular condition is an ocular inflammatory condition.

### Claim 15 (depends on 1)

The method of claim 1 wherein administration is as needed.

### Claim 16 (depends on 1)

The method of claim 1 resulting in enhanced bromfenac bioavailability in an ocular tissue in the anterior segment of the eye.

### Claim 17 (depends on 1)

The method of claim 1 resulting in enhanced bromfenac bioavailability in an ocular tissue in the back of the eye.

### Claim 18 (depends on 1)

The method of claim 1 wherein the concentration of bromfenac at 0.07% w/v is used without having to concurrently increase the frequency of dosing to achieve the same or better efficacy as a composition containing 0.09% w/v of bromfenac at pH 8.3.