DERMATOLOGICAL FOAMS OBTAINED FROM A GEL OR SUSPENSION CONTAINING ADAPALENE

• US 20130338230A1
• Filed: 12/22/2011
• Published: 12/19/2013
• Est. Priority Date: 12/23/2010
• Status: Active Grant

• Current Assignee: Galderma Research And Development Snc (Galderma Holding SA)
• Original Assignee: Galderma Research And Development Snc (Galderma Holding SA)
• Inventors: At, Emmanuelle
• Granted Patent: US 9,271,930 B2
• Time in Patent Office: Days
• US Class Current: 514/569
• 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 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• 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 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 8/042 Gels
• CPC Class Codes: A61K 8/044 Suspensions
• CPC Class Codes: A61K 8/046 Aerosols; Foams
• CPC Class Codes: A61K 8/368 with carboxyl groups directly bound to carbon atoms of aromatic rings
• 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: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61K 9/10 Dispersions; Emulsions A61K9/06 takes precedence; composition of dispersions, emulsions A61K47/00
• CPC Class Codes: A61K 9/122 Foams; Dry foams edible foams A61K9/0056
• CPC Class Codes: A61P 17/10 Anti-acne agents
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin
• CPC Class Codes: A61Q 19/10 Washing or bathing preparations

Abstract

Intermediate compositions and in particular gels and suspensions for a foam composition comprising adapalene are described. Also described, is the dermatological use of such compositions.

Claims

1. A composition comprising adapalene, wherein the composition is in the form of a foam and is obtained from an intermediate composition in the form of a gel or a suspension.

2. The composition as defined by claim 1, wherein the composition has a viscosity of greater than 8,000 cps.

3. The composition as defined by claim 1, wherein the composition has a viscosity of between 8,000 cps and 32,000 cps.

4. The composition as defined by claim 1, wherein the composition comprises:

between 60% and 98% of an intermediate gel composition, and

between 2% and 40% of at least one propellant gas.

5. The composition as defined by claim 1, wherein the composition comprises:

between 60% and 98% of an intermediate suspension composition, and

between 2% and 40% of at least one propellant gas.

10. A method for treating a keratinization disorder, the method comprising administering to a subject in need thereof the composition as defined by claim 1.

14. The composition as defined by claim 4, wherein the intermediate gel composition is present in an amount between 80% and 96%.

15. The composition as defined by claim 4, wherein the at least one propellant gas is present in an amount from 4% and 20%.

16. The composition as defined by claim 5, wherein the intermediate suspension composition is present in an amount between 80% and 96%.

17. The composition as defined by claim 5, wherein the at least one propellant gas is present in an amount between 4% and 20%.

22. The method as defined by claim 10, wherein the keratinization disorder is acne.

6. An intermediate composition in gel form, wherein the intermediate composition comprises, in a physiologically acceptable medium:

adapalene,

water,

at least one gelling agent and/or pH-independent gelling agent,

at least one surfactant,

at least one wetting agent,

optionally, a chelating agent,

optionally, at least one humectant and/or emollient, and

optionally, one or more additives.

8. The intermediate composition as defined by claim 6, wherein the composition comprises, as a weight percentage relative to the total weight of the intermediate composition, from 0.1% to 10% of at least one gelling agent and/or pH-independent gelling agent for the aqueous phase.

9. The intermediate composition as defined by claim 6, wherein the adapalene is in dispersed form in the composition.

11. The intermediate composition in gel form as defined by claim 6, wherein the intermediate composition comprises on a weight basis relative to the total weight of the gel or suspension:

(a) 0.01% to 5% of adapalene;

(b) 65% to 85% of water;

(c) 0.2% to 5% of at least one gelling agent and/or pH-independent gelling agent for the aqueous phase;

(d) 0% to 5% of at least one suspension agent and/or viscosity enhancer;

(e) 0.5% to 10% of at least one surfactant;

(f) 0.1% to 8% of at least one wetting agent;

(g) 0% to 1% of a chelating agent;

(h) 0% to 15% of at least one humectant and/or emollient; and

(i) 0% to 15% of one or more additives.

12. The intermediate composition suspension form, as defined by claim 11, wherein the content of surfactant (e) is between 2% and 10% by weight relative to the total weight of the intermediate composition.

21. The intermediate composition of claim 8, wherein the at least one gelling agent and/or pH-independent gelling agent is present in an amount from 0.2% to 5%.

23. The intermediate composition in gel form as defined by claim 11, wherein the content of surfactant (e) is between 2% and 10% by weight relative to the total weight of the intermediate composition.

7. An intermediate composition in suspension form, wherein the suspension comprises, in a physiologically acceptable medium:

adapalene,

water,

at least one gelling agent and/or pH-independent gelling agent,

optionally, one or more suspension agents,

at least one surfactant,

at least one wetting agent,

optionally, a chelating agent,

optionally, at least one humectant and/or emollient, and

optionally, one or more additives.

13. A process for obtaining an intermediate composition as defined by claim 7, the process comprising combining adapalene;

water;

gelling agent and/or pH-independent gelling agent;

suspension agent;

surfactant;

wetting agent;

a chelating agent;

humectant and/or emollient, and optionally, one or more additives in a physiologically acceptable medium.

18. The intermediate composition as defined by claim 7, wherein the composition comprises as a weight percentage relative to the total weight of the intermediate composition, 0.1% to 10% of at least one gelling agent and/or pH-independent gelling agent for the aqueous phase.

19. The intermediate composition as defined by claim 18, wherein the at least one gelling agent and/or pH-independent gelling agent is present in an amount of from 0.2% to 5%.

20. The intermediate composition as defined by claim 7, wherein the adapalene is in dispersed form in the composition.

24. The intermediate composition in suspension form as defined by claim 7, wherein the intermediate composition comprises on a weight basis relative to the total weight of the gel or suspension:

(a) 0.01% to 5% of adapalene;

(b) 65% to 85% of water;

(c) 0.2% to 5% of at least one gelling agent and/or pH-independent gelling agent for the aqueous phase;

(d) 0% to 5% of at least one suspension agent and/or viscosity enhancer;

(e) 0.5% to 10% of at least one surfactant;

(f) 0.1% to 8% of at least one wetting agent;

(g) 0% to 1% of a chelating agent;

(h) 0% to 15% of at least one humectant and/or emollient; and

(i) 0% to 15% of one or more additives.