# US 7,744,860 B2 · Reduced bioirritant composition

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- Number: US 7,744,860 B2
- Document ID: US7744860B2
- Status: Granted
- Kind: B2
- Application number: 11/254,014
- Filed: 2005-10-19
- Published: 2006-03-16
- Granted: 2010-06-29
- Earliest claimed: 1999-06-28
- Assignees: Minu, L.L.C.
- Inventors: Gholam A. Peyman
- Web page: https://patentgrep.com/patent/US7744860B2

## CPC

- A61K 31/375: Ascorbic acid, i.e. vitamin C; Salts thereof
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals}
- A61K 9/0058: {Chewing gums (non-medicinal aspects, preparing chewing gum A23G4/00; chewing gum for care of the teeth or oral cavity, e.g. with breath freshener A61Q11/00)}
- A61K 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- 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

A method for reducing irritancy of ascorbic acid administered to a biological surface for anti-angiogenic, anti-oxidant, anti-inflammatory and other effects. It has been discovered that pH neutralized ascorbic acid retains the efficacy of non-pH neutralized ascorbic acid in reducing neovascularization, providing an anti-oxidant effect, etc. but is less irritating and thus enhances patient comfort and compliance. It may be administered into or on the eye, on skin, into a body cavity, etc. either alone or with other agents.

## Claims

### Claim 1

A method of reducing neovascularization comprising administering to an individual a composition comprising an effective concentration from about 250 μg/ml to about 100 mg/ml of ascorbic acid in a composition neutralized to a pH of about 7 under conditions sufficient to reduce neovascularization wherein the composition further comprises at least one of an anti-irritant sweetener, a non-steroidal anti-inflammatory drug (NSAID), or a steroid, and wherein if topically administered the composition further comprises an NSAID.

### Claim 2 (depends on 1)

The method of claim 1 wherein the concentration of ascorbic acid in the composition ranges from about 500 μg/ml up to about 100 mg/ml.

### Claim 3 (depends on 1)

The method of claim 1 wherein the composition is administered topically, by injection, or by instillation in a body cavity.

### Claim 4 (depends on 1)

The method of claim 1 wherein the composition is administered to at least one of skin, eye, or a mucous membrane.

### Claim 5 (depends on 1)

The method of claim 1 where the individual has at least one of diabetic retinopathy, age-related macular degeneration, uveitis, ischemic retinopathies, iritis, iritis, rubeosis, retinitis of prematurity, cyclitis, sickle cell retinopathy, corneal transplantation, ocular surgery, hypoxia, trauma, physical insult, or chemical inside.

### Claim 6 (depends on 1)

The method of claim 1 wherein the composition further comprises a metalloproteinase inhibitor, a non-steroidal anti-inflammatory drug, an antibiotic, an antiproliferative drug, or combinations thereof.

### Claim 7 (depends on 1)

The method of claim 1 wherein the composition further includes at least one non-steroidal anti-inflammatory drug and at least one metalloproteinase inhibitor to provide a synergistic effect in reducing ocular neovascularization.

### Claim 8

A method of reducing ocular neovascularization comprising administering to an individual a composition comprising an effective concentration of ascorbic acid from about 250 μg/ml to about 100 mg/ml ascorbic acid adjusted to a pH of about 7 in a biocompatible composition under conditions sufficient to reduce ocular neovascularization wherein the composition further comprises an anti-irritant sweetener, a non-steroidal anti-inflammatory drug (NSAID), or a steroid, and wherein a topically administered composition contains an NSAID.

### Claim 9 (depends on 1)

The method of claim 1 wherein the sweetener is a natural sweetener or non-nutritive sweetener.

### Claim 10 (depends on 8)

The method of claim 8 wherein the sweetener is a natural sweetener or non-nutritive sweetener.