# US 5,703,122 A · Ascorbic acid compositions for reducing irritation of topically applied active ingredients

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- Number: US 5,703,122 A
- Document ID: US5703122A
- Status: Granted
- Kind: A
- Application number: 08/597,149
- Filed: 1996-02-06
- Granted: 1997-12-30
- Earliest claimed: 1993-04-26
- Assignees: Avon Products, Inc.
- Inventors: John A. Duffy
- Web page: https://patentgrep.com/patent/US5703122A

## CPC

- A61K 8/365: Hydroxycarboxylic acids; Ketocarboxylic acids
- A61K 8/676: {Ascorbic acid, i.e. vitamin C}
- A61K 31/375: Ascorbic acid, i.e. vitamin C; Salts thereof
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61Q 17/00: Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
- A61Q 19/00: Preparations for care of the skin
- A61K 2800/75: Anti-irritant
- A61Q 19/007: {Preparations for dry skin}
- 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)
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

The use of an effective amount of ascorbic acid (Vitamin C) or one or more of its derivatives, has been found to decrease skin irritation caused by the topical administration of an active ingredient for treating a skin condition. Examples of the active ingredient include .alpha.-hydroxy acids, .beta.-hydroxy acids, keto acids, benzoyl peroxide, retinol (Vitamin A), retinoic acid, retinal A.sub.2, Vitamin A epoxide, lactamides and quaternary ammonium lactates, C.sub.4-12 hydroxylated carboxylic acids, sulfur, resorcinol and salicylic acid, and various derivatives thereof. The ascorbic acid (or its derivatives) is present in effective amounts from about 0.5% to about 25% by weight. It is provided by topical application of a separate solution or by admixture with a cosmetically or pharmaceutically acceptable vehicle for the active ingredient.

## Claims

### Claim 1

A dermatological composition which comprises an active ingredient selected from the group consisting of retinoids, salicylic acid, benzoyl peroxide, .alpha.-hydroxy acids, keto acids, hydroquinone and compatible mixtures thereof, in an amount effective for treating a skin condition, and
an ascorbic acid component selected from the group consisting of ascorbic acid, alkali ascorbates, alkali earth ascorbates, ascorbate esters, ascorbyl-phosphoryl-cholesterol, ascorbate anhydrides and compatible mixtures thereof, in an amount effective for reducing irritation induced by said active ingredient, said active ingredient and said ascorbic acid component being admixed in a cosmetically or pharmaceutically acceptable vehicle.

### Claim 2 (depends on 1)

The dermatological composition as defined by claim 1, wherein said vehicle is selected from the group consisting of water, propylene glycol, ethanol, propanol, glycerin, polyvinyl alcohol, and mixtures thereof.

### Claim 3 (depends on 1)

The dermatological composition as defined by claim 1, further comprising at least one adjuvant selected from the group consisting of viscosity modifiers, preservatives, colorants, fragrances, humectants, demulcents, and compatible mixtures thereof.

### Claim 4 (depends on 1)

The dermatological composition as defined by claim 1, wherein the ascorbic acid is present in an effective amount of at least about 0.5% by weight of the dermatological composition.

### Claim 5 (depends on 4)

The dermatological composition as defined in claim 4, wherein the ascorbic acid is present in an effective amount of not more than about 25% by weight of the dermatological composition.

### Claim 6 (depends on 1)

The dermatological composition as defined by claim 1, wherein the ascorbic acid is present in an effective amount of at least about 5% by weight of the dermatological composition.

### Claim 7 (depends on 6)

The dermatological composition as defined in claim 6, wherein the ascorbic acid is present in an effective amount of not more than about 20% by weight of the dermatological composition.

### Claim 8 (depends on 1)

The dermatological composition as defined by claim 1, wherein the ascorbic acid is present in an effective amount of at least about 10% by weight of the dermatological composition.

### Claim 9 (depends on 8)

The dermatological composition as defined by claim 8, wherein the ascorbic acid is present in an effective amount of not more than about 15% by weight of the dermatological composition.

### Claim 10

A topical composition for use with a topically applied active ingredient selected from the group consisting of retinoids, salicylic acid, benzoyl peroxide, .alpha.-hydroxy acids, keto acids, hydroquinone and compatible mixtures thereof, said composition comprising an inert vehicle and an ascorbic acid component selected from the group consisting of ascorbic acid, alkali ascorbates, alkali earth ascorbates, ascorbate esters, ascorbyl-phosphoryl-cholesterol, ascorbate anhydrides and compatible mixtures thereof, in an amount effective to reduce irritation caused by said active ingredient.

### Claim 11 (depends on 10)

The composition as defined by claim 10, wherein said inert vehicle is selected from the group consisting of water, propylene glycol, ethanol, propanol, glycerin, polyvinyl alcohol, and compatible mixtures thereof.

### Claim 12 (depends on 10)

The composition as defined by claim 10, further comprising at least one adjuvant selected from the group consisting of viscosity modifiers, preservatives, colorants, fragrances, humectants, demulcents, and compatible mixtures thereof.
