Foamable suspension gel

• US 20070237724A1
• Filed: 03/29/2007
• Published: 10/11/2007
• Est. Priority Date: 03/31/2006
• Status: Active Grant

• Current Assignee: Stiefel Research Australia Pty Limited (GSK plc)
• Original Assignee: Stiefel Research Australia Pty Limited (GSK plc)
• Inventors: Fuchshuber, Lilian, Abram, Albert
• Granted Patent: US 8,158,109 B2
• Time in Patent Office: Days
• US Class Current: 424/47
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• 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 31/203 Retinoic acids ; Salts thereof
• CPC Class Codes: A61K 31/327 Peroxy compounds, e.g. hydroperoxides, peroxides, peroxyacids
• CPC Class Codes: A61K 31/63 Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
• CPC Class Codes: A61K 31/7034 attached to a carbocyclic compound, e.g. phloridzin
• CPC Class Codes: A61K 31/7056 containing five-membered rings with nitrogen as a ring hetero atom
• 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 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 9/122 Foams; Dry foams edible foams A61K9/0056
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/10 Anti-acne agents
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/10 Antimycotics

Abstract

The present subject matter provides foamable suspension gels that foam after release from a container. The foamable suspension gels contain at least one pharmaceutically active agent that is sparingly soluble to insoluble in water, a second pharmaceutically active agent, and optionally a third active agent.

Claims

1. An aqueous foamable suspension gel, comprising:

up to 40% w/w of a first active agent that is sparingly soluble to insoluble in water, suspended in an aqueous phase;

up to 40% of a second active agent; and

from about 0.1% to about 2% of a thickening agent;

wherein the gel is aqueous and forms a homogenous foam.

2. The foamable suspension gel of claim 1, wherein the foamable suspension gel is in a container.

3. The foamable suspension gel of claim 2, wherein the container is a pressurized container.

4. The foamable suspension gel of claim 1, wherein the first active agent is selected from the group consisting of benzoyl peroxide, a retinoid, an azole antimicrobial agent, and mixtures thereof.

5. The foamable suspension gel of claim 1, wherein the second active agent is selected from the group consisting of an antibacterial, an antifungal, an antibiotic, an immunomodulator, a peptide, a vitamin, a vitamin derivative, an azole, an oxide, and mixtures thereof.

6. The foamable suspension gel of claim 5, wherein if the second active agent comprises an antibiotic, the second active agent must comprise an additional active agent.

7. The foamable suspension gel of claim 1, wherein the second active agent is selected from the group consisting of a lincomycin antibiotic, a retinoid, sodium sulfacetamide, and mixtures thereof.

8. The foamable suspension gel of claim 1, wherein the first active agent is selected from the group consisting of benzoyl peroxide, a retinoid, an azole antimicrobial agent, and mixtures thereof thereof and the second active agent is selected from the group consisting of an antibacterial, an antifungal, an antibiotic, an immunomodulator, a peptide, a vitamin, a vitamin derivative, an azole, an oxide, and mixtures thereof;

wherein if the second active agent comprises an antibiotic, the second active agent must comprise an additional active agent.

9. The foamable suspension gel of claim 1, wherein the first active agent is benzoyl peroxide and the second active agent is tretinoin.

10. The foamable suspension gel of claim 1, wherein the first active agent is metronidazole and the second active agent is sodium sulfacetamide.

11. The foamable suspension gel of claim 1, further comprising a third active agent.

12. The foamable suspension gel of claim 1, wherein the gel comprises at least about 30% water.

13. The foamable suspension gel of claim 1, wherein the gel is alcohol-free.

14. The foamable suspension gel of claim 1, wherein the gel is oil-free.

15. The foamable suspension gel of claim 1, further comprising a surfactant.

16. The foamable suspension gel of claim 1, further comprising a wetting agent.

17. The foamable suspension gel of claim 1, further comprising a sun filter.

18. The foamable suspension gel of claim 1, wherein the gel has a viscosity permitting it to be delivered through an actuator.

19. The foamable suspension gel of claim 1, wherein the gel has a viscosity of less than about 40,000 centipoise (cP) at 25°

C.

20. The foamable suspension gel of claim 1, wherein the gel has a viscosity of about 1,000 centipoise (cP) to about 20,000 cP at 25°

C.

21. The foamable suspension gel of claim 1, wherein the gel is a post-foaming gel that foams after release from a container.

22. The foamable suspension gel of claim 1, wherein the thickening agent is a hydrocolloid.

23. The foamable suspension gel of claim 22, wherein the thickening agent is selected from the group consisting of xanthan gum, a carbomer, salts or derivatives thereof, and mixtures thereof.

24. The foamable suspension gel of claim 3, wherein the pressure in the pressurized container is from about 5 psi to about 110 psi at 25°

C.

25. The foamable suspension gel of claim 1, further comprising a pH-adjusting agent.

26. The foamable suspension gel of claim 1, wherein the pH of the foam is about 4-9.

27. The foamable suspension gel of claim 1, wherein the first and second active agents are chemically and physically stable for about 24 months at about 5°

C.

28. The foamable suspension gel of claim 1, wherein the first and second active agents are chemically and physically stable for about 6 months at about 25°

C.

33. A method of treating a dermatological condition, comprising contacting the skin of an individual in need thereof with the foamable suspension gel of claim 1.

29. An aqueous foamable suspension gel, comprising:

from about 1% to about 8% w/w benzoyl peroxide suspended in an aqueous phase;

from about 0.025% to about 2% of a retinoid; and

from about 0.5% to about 2% xanthan gum;

wherein the gel is aqueous and forms a homogenous foam.

30. The foamable suspension gel of claim 29, wherein the foamable suspension gel is in a container.

31. The foamable suspension gel of claim 30, wherein the container is selected from the group consisting of a pressurized container, a pumpable container, and a combination thereof.

32. A method of treating acne, the method comprising contacting the skin of an individual in need thereof with the foamable suspension gel of claim 29.

34. A method of treating a dermatological condition, comprising contacting the skin of an individual in need thereof with the foamable suspension gel of claim 29.

35. An aqueous foamable suspension gel, comprising:

from about 1% to about 25% w/w benzoyl peroxide as the sole active agent present suspended in an aqueous phase; and

from about 0.5% to about 2% xanthan gum;

wherein the gel is aqueous and fonns a homogenous foam.

36. An aqueous foamable suspension gel, comprising:

from about 4% to about 8% w/w benzoyl peroxide as the sole active agent present suspended in an aqueous phase; and

from about 0.5% to about 2% xanthan gum;

wherein the gel is aqueous and forms a homogenous foam.

37. An aqueous foamable suspension gel, comprising:

from about 1% to about 8% w/w of a first active agent comprising benzoyl peroxide suspended in an aqueous phase;

from about 0.025% to about 4% of a second active agent comprising a retinoid in combination with clindamycin phosphate; and

from about 0.5% to about 2% xanthan gum;

wherein the gel is aqueous and forms a homogenous foam.

38. An aqueous foamable suspension gel, comprising:

from about 4% to about 8% w/w of a first active agent comprising benzoyl peroxide suspended in an aqueous phase;

from about 0.5% to about 4% of a second active agent comprising a retinoid in combination with clindamycin phosphate; and

from about 0.5% to about 2% xanthan gum;

wherein the gel is aqueous and forms a homogenous foam.