Non surface active agent non polymeric agent hydro-alcoholic foamable compositions, breakable foams and their uses

• US 10,350,166 B2
• Filed: 06/08/2015
• Issued: 07/16/2019
• Est. Priority Date: 07/29/2009
• Status: Active Grant

• Current Assignee: VYNE Therapeutics, Inc.
• Original Assignee: Foamix Pharmaceuticals, Ltd. (VYNE Therapeutics, Inc.)
• Inventors: Tamarkin, Dov, Ziv, Enbal, Hazot, Yohan, Schuz, David
• Primary Examiner(s): Browe, David
• Application Number:
  US14/733,418
• Publication Number:
  US 20150374625A1
• Time in Patent Office: 1,499 Days
• Field of Search: None
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• 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 47/12 Carboxylic acids; Salts or anhydrides thereof
• 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 8/046 Aerosols; Foams
• CPC Class Codes: A61K 8/34 Alcohols
• CPC Class Codes: A61K 8/342 Alcohols having more than seven atoms in an unbroken chain
• CPC Class Codes: A61K 9/12 Aerosols; Foams A61K9/0043, A61K9/0056, A61K9/006, A61K9/0073 take precedence; spray-films A61K9/7015
• 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: A61Q 19/00 Preparations for care of the skin

Abstract

A substantially surface active agent-free and substantially polymeric agent-free foamable composition is disclosed, which includes short-chain alcohol, water, fatty alcohol or fatty acid or a combination of fatty alcohol and fatty acid and propellant. Also disclosed is a method of treatment by applying the substantially surface active agent-free and substantially polymeric agent-free foamable composition.

Claims

1. A foamable composition comprising a liquefied or compressed gas propellant and a carrier composition;

wherein the carrier composition comprises;

a) at least 15% by weight of a short chain alcohol having up to six carbon atoms in its carbon chain,

b) a humectant,

c) water, and

d) two fatty alcohols at a ratio of between 1.35;

1 and 1;

1.35;

wherein the liquefied or compressed gas propellant is at a concentration of 3% to 30% by weight of the carrier composition;

wherein the foamable composition comprises 0% by weight of a surfactant; and

wherein upon dispensing, a foam is formed that is thermally stable at a temperature of 36°

C. and has a collapse time of 60 seconds or more.

2. The foamable composition of claim 1, wherein the carrier composition comprises at least one active agent.

3. The foamable composition of claim 2, wherein the active agent is selected from the group consisting of an active herbal extract, an acaricide, an age spot and keratose removing agent, an allergen, an alpha hydroxyl acid, an analgesic agent, an anesthetic, an immunogenic substance, an antiacne agent, an antiallergic agent, an antiaging agent, an antibacterial agent, an antibiotic, an antiburn agent, an anticancer agent, an antidandruff agent, an antidepressant, an antidermatitis agent, an antiedemic agent, an antifungal agent, an antihistamine, an antihelminth agent, an antihyperkeratolyte agent, an anti-infective agent, an anti-inflammatory agent, an antiirritant, an antilipemic agent, an antimicrobial agent, an antimycotic agent, an antioxidant, an antiparasitic agent, an anti-pigmentation agent, an antiproliferative agent, an antipruritic agent, an antipsoriatic agent, an antirosacea agent, an antiseborrheic agent, an antiseptic agent, an antiswelling agent, an antiviral agent, an anti-wart agent, an anti-wrinkle agent, an antiyeast agent, an astringent, a beta-hydroxy acid, benzoyl peroxide, a topical cardiovascular agent, a chemotherapeutic agent, a corticosteroid, an immunogenic substance, a dicarboxylic acid, a disinfectant, a fungicide, a hair growth regulator, a haptene, a hormone, a hydroxy acid, an immunosuppressant, an immunoregulating agent, an immunomodulator, an insecticide, an insect repellent, a keratolytic agent, a lactam, a local anesthetic agent, a lubricating agent, a masking agent, a metal, a metal oxide, a mitocide, a neuropeptide, a non-steroidal anti-inflammatory agent, an oxidizing agent, a pediculicide, a peptide, a protein, a photodynamic therapy agent, a radical scavenger, a refatting agent, a retinoid, a sanative, a scabicide, a self-tanning agent, silicone talc, a skin protective agent, a skin whitening agent, a steroid, a steroid hormone, a steroidal anti-inflammatory agent, a vasoconstrictor, a vasodilator, a vitamin, a vitamin A, a vitamin A derivative, a vitamin B, a vitamin B derivative, a vitamin C, a vitamin C derivative, a vitamin D, a vitamin D derivative, a vitamin D analog, a vitamin F, a vitamin F derivative, a vitamin K, a vitamin K derivative, a wound healing agent, a wart remover, and mixtures of any two or more thereof.

4. The foamable composition of claim 1, wherein the foamable composition is transparent upon pressurization by the gas propellant.

5. The foamable composition of claim 1, wherein the humectant is selected from the group consisting of polyethylene glycol (PEG) 400, propylene glycol, and glycerin.

6. The foamable composition of claim 1, wherein the composition contains less than 0.2% by weight of the carrier composition of a polymeric agent.

7. The foamable composition of claim 1, wherein at least one of the fatty alcohols has 14 to 18 carbon atoms in its carbon chain.

8. The foamable composition of claim 1, wherein the composition comprises a combination of two fatty alcohols selected from the group consisting of:

(i) stearyl alcohol and cetyl alcohol and (ii) cetyl alcohol and myristyl alcohol; and

the ratio of the two fatty alcohols is 1;

1.

9. The foamable composition of claim 1, wherein the short chain alcohol is present in an amount between 20% and 60% by weight of the carrier composition.

10. The foamable composition of claim 1, wherein upon dispensing, the foam formed is thermally stable at a temperature of 36°

C. and has a collapse time of 120 seconds or more.

11. The foamable composition of claim 1, wherein the foam is a breakable foam that breaks upon application of shear force.

20. The foamable composition of claim 3, wherein the active agent is selected from the group consisting of an antibacterial agent, an antibiotic, an antifungal agent, an antiviral agent, and mixtures of any two or more thereof.

26. The foamable composition of claim 2, wherein the short chain alcohol comprises ethanol;

wherein at least one of the fatty alcohols comprises cetyl alcohol or stearyl alcohol;

wherein the humectant comprises propylene glycol; and

wherein the at least one active agent comprises an antifungal agent.

27. The foamable composition of claim 2, wherein the composition comprises:

15% to 65% by weight of the short chain alcohol;

1% to 10% by weight of the two fatty alcohols; and

2% to 50% by weight of the humectant.

34. The foamable composition of claim 1, wherein the carrier composition further comprises one or more hydrophobic solvents.

36. The foamable composition of claim 1, wherein the carrier composition further comprises a chelating agent.

38. The foamable composition of claim 1, wherein the carrier composition further comprises a pH modifying agent.

40. The foamable composition of claim 1, wherein the short chain alcohol is present in an amount between 30% and 60% by weight of the carrier composition.

41. The foamable composition of claim 1, wherein the short chain alcohol is present in an amount between 40% and 60% by weight of the carrier composition.

42. The foamable composition of claim 1, wherein the short chain alcohol is present in an amount of at least 50% by weight of the carrier composition.

44. The foamable composition of claim 1, wherein the ratio between the two fatty alcohols is between 1.20:

1 and 1;

1.20.

45. The foamable composition of claim 1, wherein the ratio between the two fatty alcohols is between 1.10:

1 and 1;

1.10.

12. A foamable composition comprising a liquefied or compressed gas propellant and a carrier composition;

wherein the carrier composition comprises;

a) 15% to 65% by weight of a short chain alcohol having up to six carbon atoms in its carbon chain,

b) a humectant,

c) water, and

d) two fatty alcohols at a ratio of between 1.35;

1 and 1;

1.35;

wherein the liquefied or compressed gas propellant is at a concentration of 3% to 30% by weight of the carrier composition;

wherein the foamable composition comprises 0% by weight of a surfactant; and

wherein upon dispensing, a foam is formed that is thermally stable at a temperature of 36°

C. and has a collapse time of 60 seconds or more.

13. The foamable composition of claim 12, wherein the carrier composition comprises an active agent.

14. The foamable composition of claim 12, wherein the carrier composition contains less than 0.2% by weight of the carrier composition of a polymeric agent.

21. The foamable composition of claim 13, wherein the active agent is selected from the group consisting of an antibacterial agent, an antibiotic, an antifungal agent, an antiviral agent, and mixtures of any two or more thereof.

24. The foamable composition of claim 12, wherein at least one of the two fatty alcohols has 14 to 18 carbons in its carbon chain.

28. The foamable composition of claim 13, wherein the short chain alcohol comprises ethanol;

wherein the two fatty alcohols comprise cetyl alcohol and stearyl alcohol;

wherein the humectant comprises propylene glycol; and

wherein the at least one active agent comprises an antifungal agent.

29. The foamable composition of claim 13, wherein the composition comprises:

15% to 65% by weight of the short chain alcohol;

1% to 10% by weight of the two fatty alcohols; and

2% to 50% by weight of the humectant.

35. The foamable composition of claim 12, wherein the carrier composition further comprises one or more hydrophobic solvents.

37. The foamable composition of claim 12, wherein the carrier composition further comprises a chelating agent.

39. The foamable composition of claim 12, wherein the carrier composition further comprises a pH modifying agent.

43. The foamable composition of claim 12, wherein the short chain alcohol is present in an amount of at least 50% by weight of the carrier composition.

46. The foamable composition of claim 12, wherein the ratio between the two fatty alcohols is between 1.20:

1 and 1;

1.20.

47. The foamable composition of claim 12, wherein the ratio between the two fatty alcohols is between 1.10:

1 and 1;

1.10.

15. A method of ameliorating or eliminating or treating or alleviating a dermatological or a mucosal disorder, the method comprising:

applying a foam composition to a surface having the dermatological or mucosal disorder in need of treatment, wherein the foam is formed from a foamable composition comprising a liquefied or compressed gas propellant and a carrier composition;

wherein the carrier composition comprises;

a) at least 15% by weight of a short chain alcohol having up to six carbon atoms in its carbon chain,

b) a humectant,

c) water,

d) two fatty alcohols at a ratio of between 1.35;

1 and 1;

1.35, and

e) at least one active agent;

wherein the liquefied or compressed gas propellant is at a concentration of 3% to 30% by weight of the carrier composition;

wherein the foamable composition comprises 0% by weight of a surfactant; and

wherein upon dispensing, the foam formed is thermally stable at a temperature of 36°

C. and has a collapse time of 60 seconds or more.

16. The method of claim 15, wherein the disorder is selected from the group consisting of a bacterial infection, a fungal infection, and a viral infection.

17. The method of claim 15, wherein the carrier composition is free of a polymeric agent or contains less than 0.2% by weight of the carrier composition of a polymeric agent.

22. The method of claim 15, wherein the active agent is selected from the group consisting of an antibacterial agent, an antibiotic, an antifungal agent, an antiviral agent, and mixtures of any two or more thereof.

30. The method of claim 15, wherein the short chain alcohol comprises ethanol;

wherein at least one of the two fatty alcohols comprises at least one of cetyl alcohol and stearyl alcohol;

wherein the humectant comprises propylene glycol; and

wherein the at least one active agent comprises an antifungal agent.

31. The method of claim 15, wherein the composition comprises:

15% to 65% by weight short chain alcohol;

1% to 10% by weight of the two fatty alcohols; and

2% to 50% by weight humectant.

18. A method of ameliorating or eliminating or treating or alleviating a dermatological or a mucosal disorder, the method comprising:

applying a foam composition to a surface having the dermatological or mucosal disorder in need of treatment, wherein the foam is formed from a foamable composition comprising a liquefied or compressed gas propellant and a carrier composition;

wherein the carrier composition comprises;

a) 15% to 65% by weight of a short chain alcohol having up to six carbon atoms in its carbon chain,

b) a humectant,

c) water,

d) two fatty alcohols at a ratio of between 1.35;

1 and 1;

1.35, and

e) at least one active agent;

wherein the liquefied or compressed gas propellant is at a concentration of 3% to 30% by weight of the carrier composition;

wherein the foamable composition comprises 0% by weight of a surfactant;

wherein the disorder is selected from the group consisting of a bacterial infection, a fungal infection, and a viral infection; and

wherein upon dispensing, the foam formed is thermally stable at a temperature of 36°

C. and has a collapse time of 60 seconds or more.

19. The method of claim 18, wherein the carrier composition is free of polymeric agent or contains less than 0.2% by weight of the carrier composition of a polymeric agent.

23. The method of claim 18, wherein the active agent is selected from the group consisting of an antibacterial agent, an antibiotic, an antifungal agent, an antiviral agent, and mixtures of any two or more thereof.

25. The method of claim 18, wherein at least one of the two fatty alcohols has 14 to 18 carbons in their carbon chain.

32. The method of claim 18, wherein the short chain alcohol comprises ethanol;

wherein the two fatty alcohols comprise cetyl alcohol and stearyl alcohol;

wherein the humectant comprises propylene glycol; and

wherein the at least one active agent comprises an antifungal agent.

33. The method of claim 18, wherein the composition comprises:

15% to 65% by weight of the short chain alcohol;

1% to 10% by weight of the two fatty alcohols; and

2% to 50% by weight of the humectant.