# US 6,120,779 A · Use of partial and complete salts of choline and carboxylic acids for the treatment of skin disorders

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- Number: US 6,120,779 A
- Document ID: US6120779A
- Status: Granted
- Kind: A
- Application number: 09/015,239
- Filed: 1998-01-29
- Granted: 2000-09-19
- Earliest claimed: 1998-01-29
- Assignees: Soma Technologies
- Inventors: Smita Nayak; Vinayak Nayak
- Web page: https://patentgrep.com/patent/US6120779A

## CPC

- A61K 8/362: Polycarboxylic acids
- A61K 8/416: {Quaternary ammonium compounds (A61K8/35 takes precedence)}
- A61K 31/205: Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
- A61Q 3/00: Manicure or pedicure preparations
- A61Q 5/00: Preparations for care of the hair
- A61Q 5/006: {Antidandruff preparations}
- 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 17/04: Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
- A61Q 19/00: Preparations for care of the skin
- A61Q 19/001: {Preparations for care of the lips}
- A61Q 19/007: {Preparations for dry skin}
- A61Q 19/06: for countering cellulitis
- A61Q 19/08: Anti-ageing preparations
- A61K 2800/75: Anti-irritant
- 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

Novel skin care, hair care, nail care, lip care and related external formulations based on partial and complete choline salts of mono, di, tri and polyvalent carboxylic acids of food, cosmetic and pharmaceutical acids are described. These salts have better moisturizing and treating properties compared to the original acids. They tend to form highly elegant cosmetic treatment products when incorporated into lotions, creams, gels, liquids, bars, sticks, sprays and foam products. The mono choline salts of di and polyvalent carboxylic acids are also described in the invention. These mono choline salts tend to retain or enhance the biological properties of the parent molecule with enhanced solubility and bio-availability. These mono choline salts can be formulated as simple solutions and lotions eliminating need of complicated solubilizing systems. The partial and mono choline salts tend to reduce irritation, burning and stinging sensation common to these carboxylic acids.

## Claims

### Claim 1

A method of alleviating dry and irritated skin by topically applying to the skin, a cosmetic composition comprising complete or partial choline salts of pharmaceutically acceptable carboxylic acids.

### Claim 2 (depends on 1)

The method of claim 1, wherein the said choline salt in the cosmetic composition is prepared in situ, by
A) neutralization of the said carboxylic acid or their combinations with free choline base
B) neutralization of the said carboxylic acids with basic choline salts
C) neutralization of the said carboxylic acids to a pH range of 1.0 to 9.0 by the choline or its basic salts
D) partial neutralization of the single carboxylic group from a multi carboxylic acid to get mono or di choline salts or incorporation of the pure choline salts in different ratios to get the desired concentrations.

### Claim 3 (depends on 1)

The method of claim 1, wherein the said carboxylic acid in the composition, is either a single ingredient or a combination selected from the group consisting of alpha hydroxy acids, alpha keto acids, beta hydroxy acids, dicarboxylic acids, mono carboxylic acids, amino acids found in nature, polymeric carboxylic acids, and aromatic acids.

### Claim 4 (depends on 1)

The method of claim 1, wherein the composition is formulated in the form of skin moisturizing, antiacne, anti dandruff, anticellulite, nail softening, cleansing, dry-scalp moisturizing/conditioning, ear moisturizing/conditioning, hair-care, lip-treatment, sun-screening lotions, creams, gels or liquids.

### Claim 5 (depends on 4)

Skin moisturizing compositions, cleansing compositions and dry-scalp moisturizing and conditioning compositions of claim 4, comprising partial or complete choline salts of nontoxic mono, di, tri, and poly carboxylic acids in 0.001 to 50% of the weight of composition.

### Claim 6 (depends on 4)

Lip treatment products, hair care products and ear moisturizers and cleansers of claim 4, wherein partial or complete choline salts of mono, di, tri and poly carboxylic acids are in the range of in 0.001 to 20% of the weight of the composition.

### Claim 7 (depends on 4)

Acne treatment products of claim 4 comprising partial or complete choline salts of alpha hydroxy acids, salicylic acid, mandelic acid, C-7 to C-20 dicarboxylic acids or boswalic acid in 0.001 to 50% concentration.

### Claim 8 (depends on 4)

Nail softening treatment complexes of claim 4 containing partial and complete choline salts of mono, di, tri and poly carboxylic acids in 0.001 to 70% of the weight of the composition.

### Claim 9 (depends on 2)

Method of manufacturing the partial salts as described in claim 2 which results in the formation of odor free, color free and stable choline complexes.

### Claim 10 (depends on 2)

The method described in claim 2, wherein substantial reduction in local irritation, inflammation, burning and stinging is attained by formation of partial choline salts compared to the free acid formulations.

### Claim 11 (depends on 1)

The cosmetic composition according to claim 1, wherein different combinations of aromatic, aliphatic, alpha and beta hydroxy acids along with C-4 to C-36 dicarboxylic acid mono choline salts are used in a pH range of 2 to 8 for the treatment of sun-damaged skin, wrinkles and age spots.

### Claim 12 (depends on 4)

Anti-cellulite compositions of claim 4 containing mixed acid salts of choline in 0.01 to 50% concentration in combination with nicotinic acid, inositol hexanicotinate, caffeine, DHEA, and guggulsterone.

### Claim 13 (depends on 3)

Mixed or mono choline salts of long chain carboxylic acids and polymeric carboxylic acids of claim 3 in 0.001 to 50% range used with dual intend as an emulsifier/stabilizer or solubilizer while imparting moisturizing properties to skin care products.

### Claim 14 (depends on 2)

Partial neutralization of carboxylic acids of claim 2 with choline base to pH range of 2.0 to 8.0 to have better color stability and alleviate odor problems compared to the completely neutralized carboxylic acid salts.

### Claim 15 (depends on 2)

Partially neutralized choline salts of carboxylic acids of claim 2 in 0.005 to 50% concentration in an anhydrous base to be molded in different cosmetic solid or semisolid dosage formulations.