Dermatological compositions comprising at least one naphthoic acid compound and at least one film-forming agent and treatment of keratinization disorders therewith

• US 8,937,098 B2
• Filed: 11/24/2008
• Issued: 01/20/2015
• Est. Priority Date: 05/31/2006
• Status: Active Grant

• Current Assignee: Galderma Research And Development Snc (Nestle SA)
• Original Assignee: Galderma Research And Development Snc (Nestle SA)
• Inventors: Mallard, Claire, Ferrara, Eve
• Primary Examiner(s): Heyer, Dennis
• Application Number:
  US12/276,584
• Publication Number:
  US 20090247630A1
• Time in Patent Office: 2,248 Days
• Field of Search: None
• US Class Current: 514/557
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 8/04 Dispersions; Emulsions
• CPC Class Codes: A61K 8/06 Emulsions
• CPC Class Codes: A61K 8/368 with carboxyl groups directly bound to carbon atoms of aromatic rings
• CPC Class Codes: A61K 8/735 Mucopolysaccharides, e.g. hyaluronic acid; Derivatives thereof
• CPC Class Codes: A61K 8/8182 Copolymers of vinyl-pyrrolidones. Compositions of derivatives of such polymers
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/10 Anti-acne agents
• CPC Class Codes: A61Q 17/04 Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• CPC Class Codes: A61Q 19/008 Preparations for oily skin
• CPC Class Codes: A61Q 19/08 Anti-ageing preparations
• CPC Class Codes: A61Q 5/00 Preparations for care of the hair

Abstract

Topically applicable, reduced-irritant dermatological/cosmetic compositions useful for the treatment of a variety of keratinization disorders, for example acne vulgaris, contain at least one naphthoic acid compound essentially uniformly distributed therethrough and an amount of at least one hydrophilic film-forming agent, formulated into a topically applicable, physiologically acceptable medium.

Claims

1. A topically applicable, dermatological/cosmetic gel composition useful for the treatment of acne, comprising at least one naphthoic acid compound essentially uniformly distributed therethrough, said at least one naphthoic acid compound having the formula (I):

2. The dermatological/cosmetic gel composition as defined by claim 1, wherein the concentration of the at least one naphthoic acid compound ranges from 0.001% to 10%, by weight relative to the total weight thereof.

3. The dermatological/cosmetic gel composition as defined by claim 1, said at least one naphthoic acid compound being selected from the group consisting of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, 6-[3-(1-adamantyl)-4-hydroxyphenyl]-2-naphthoic acid, 6-[3-(1-adamantyl)-4-decyloxyphenyl]-2-naphthoic acid and 6-[3-(1-adamantyl)-4-hexyloxyphenyl]-2-naphthoic acid.

4. The dermatological/cosmetic gel composition as defined by claim 3, said at least one naphthoic acid compound comprising 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid.

5. The dermatological/cosmetic gel composition as defined by claim 4, wherein the concentration of said 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid is about 0.1% by weight relative to the total weight thereof.

6. The dermatological/cosmetic gel composition as defined by claim 4, wherein the concentration of said 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid is about 0.3% by weight relative to the total weight thereof.

7. The dermatological/cosmetic gel composition as defined by claim 1, wherein the concentration of said at least one film-forming agent ranges from 0.5% to 20% by weight relative to the total weight thereof.

8. The dermatological/cosmetic gel composition as defined by claim 7, wherein the concentration of said at least one film-forming agent is 2%, 4% or 6% by weight relative to the total weight thereof.

9. The dermatological/cosmetic gel composition as defined by claim 1, which comprises, in water:

from 0.1% to 0.3% of at least one naphthoic acid compound;

from 1% to 10% of at least one film-forming agent;

from 0.1% to 3% of gelling agents;

from 0.01% to 1.5% of chelating agents;

from 0.1% to 10% of a wetting agent; and

from 0.01% to 3% of preservatives.

10. The dermatological/cosmetic gel composition as defined by claim 1, which comprises, in water:

from 0.1% to 0.3% of at least one naphthoic acid compound;

from 1% to 10% of at least one film-forming agent;

from 0.1% to 3% of gelling agents;

from 0.01% to 1.5% of chelating agents;

from 0.1% to 10% of a wetting agent; and

from 0.1% to 20% of an emollient;

from 0.01% to 3% of preservatives.

11. A process for preparing a dermatological/cosmetic gel composition as defined by claim 1, comprising mixing a physiologically acceptable vehicle which comprises said at least one naphthoic acid compound with said at least one film-forming agent, and neutralizing, if necessary, to provide a gel composition in which said at least one naphthoic acid compound is in a form dispersed therein.

12. The process as defined by claim 11, which comprises the following steps:

a) mixing said at least one naphthoic acid compound with at least one wetting agent, and at least one chelating agent in water, until said at least one naphthoic acid compound is fully dispersed, to provide an aqueous active phase;

b) mixing said at least one film-forming agent with water to provide a film-forming phase;

c) introducing said at least one film-forming agent obtained in b) into the aqueous active phase obtained in a), or vice versa, and neutralizing, if necessary.

13. A method for the treatment of acne, comprising topically applying onto the affected skin area of an individual in need of such treatment, a thus effective amount of the dermatological/cosmetic gel composition as defined by claim 1.

14. A method for treating common acne, comedonal acne, papulopustular acne, papulocomedonal acne, nodulocystic acne, acne conglobata, acne keloid of the nape of the neck, recurrent military acne, acne necrotica, acne neonatorum, occupational acne, acne rosacea, senile acne, solar acne or acne medicamentosa, comprising topically applying onto the affected skin area of an individual in need of such treatment, a thus effective amount of the dermatological/cosmetic gel composition as defined by claim 1.

15. A method for the treatment of common acne, comprising topically applying onto the affected skin area of an individual in need of such treatment, a thus effective amount of the dermatological/cosmetic gel composition as defined by claim 1.