Dicarboxylic acid foamable vehicle and pharmaceutical compositions thereof

• US 10,322,085 B2
• Filed: 11/13/2018
• Issued: 06/18/2019
• Est. Priority Date: 10/25/2002
• Status: Expired due to Term

• Current Assignee: VYNE Therapeutics, Inc.
• Original Assignee: Foamix Pharmaceuticals, Ltd. (VYNE Therapeutics, Inc.)
• Inventors: Tamarkin, Dov, Friedman, Doron, Berman, Tal, Ziv, Enbal, Schuz, David
• Primary Examiner(s): Cabral, Robert S
• Application Number:
  US16/189,767
• Publication Number:
  US 20190076356A1
• Time in Patent Office: 217 Days
• CPC Class Codes: A01N 25/16 Foams
• CPC Class Codes: A61K 8/046 Aerosols; Foams
• CPC Class Codes: A61K 8/362 Polycarboxylic acids
• CPC Class Codes: A61K 8/37 Esters of carboxylic acids
• CPC Class Codes: A61K 8/4993 Derivatives containing from 2 to 10 oxyalkylene groups
• CPC Class Codes: A61K 8/86 Polyethers
• 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 9/122 Foams; Dry foams edible foams A61K9/0056
• CPC Class Codes: A61P 23/00 Anaesthetics
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin

Abstract

The present invention teaches a foamable pharmaceutical carrier comprising a benefit agent, selected from the group consisting of a dicarboxylic acid and a dicarboxylic acid ester; a stabilizer selected from the group consisting of at least one surface-active agent; at least one polymeric agent and mixtures thereof; a solvent selected from the group consisting of water, a hydrophilic solvent, a hydrophobic solvent, a potent solvent, a polar solvent, a silicone, an emollient, and mixtures thereof, wherein the benefit agent, stabilizer and solvent are selected to provide a composition that is substantially resistant to aging and to phase separation and or can substantially stabilize other active ingredients. The invention further relates to a foamable composition further containing a liquefied hydrocarbon gas propellant.

Claims

1. A foamable composition comprising a carrier and a liquefied or compressed gas propellant, wherein the carrier comprising:

(a) about 15% by weight of the carrier of azelaic acid;

(b) about 2% to about 50% by weight of the carrier of a hydrophobic solvent;

(c) a polar solvent;

(d) a surface-active agent;

(e) a polymeric agent; and

(f) water; and

wherein the surface-active agent comprises a combination of at least two surface-active agents and wherein there is a difference of about 4 or more units between the HLB values of the at least two surface-active agents;

wherein combined amount of the polymeric agent and the surface-active agent is about 0.05% to about 10% by weight of the carrier; and

wherein the liquefied or compressed gas propellant is present at about 3% to about 25% by weight of the composition.

2. The foamable composition of claim 1, wherein the hydrophobic solvent comprises caprylic/capric triglyceride.

3. The foamable composition of claim 2, wherein caprylic/capric triglyceride is present at about 11% by weight of the carrier.

4. The foamable composition of claim 1, wherein the polar solvent comprises dimethyl isosorbide.

5. The foamable composition of claim 4, wherein dimethyl isosorbide is present at about 5% by weight of the carrier.

6. The foamable composition of claim 4, wherein the polar solvent further comprises propylene glycol.

7. The foamable composition of claim 1, wherein the combination comprises at least one non-ionic surface-active agent having an HLB value of less than 9.

8. The foamable composition of claim 7, wherein the at least one non-ionic surface-active agent comprises glyceryl stearate.

9. The foamable composition of claim 1, wherein the combination comprises at least one non-ionic surface-active agent having an HLB value of more than 9.

10. The foamable composition of claim 9, wherein the at least one non-ionic surface-active agent having an HLB value of more than 9 comprises PEG-40 stearate and/or Polysorbate 80.

11. The foamable composition of claim 1, wherein the combination comprises at least one ionic surface-active agent.

12. The foamable composition of claim 1, wherein the polymeric agent is present at about 0.01% to about 5% by weight of the carrier.

13. The foamable composition of claim 1, wherein the polymeric agent comprises a naturally-occurring polymeric agent and/or a semi-synthetic polymeric agent.

14. The foamable composition of claim 13, wherein the naturally-occurring polymeric agent comprises xanthan gum.

15. The foamable composition of claim 13, wherein the semi-synthetic polymeric agent comprises methylcellulose.

16. The foamable composition of claim 11, wherein the foamable composition further comprises a foam adjuvant.

17. The foamable composition of claim 16, wherein the foam adjuvant comprises a fatty alcohol having 15 or more carbons in its carbon chain and/or a fatty acid having 16 or more carbons in its carbon chain.

18. The foamable composition of claim 17, wherein the fatty alcohol comprises cetostearyl alcohol.

19. The foamable composition of claim 1, wherein the foamable composition comprises less than about 5% by weight of the carrier of a short-chain alcohol.

20. The foamable composition of claim 1, wherein the foamble composition further comprises an anti-perspirant, an anti-static agent, a buffering agent, a bulking agent, a chelating agent, a cleanser, a colorant, a conditioner, a deodorant, a diluent, a dye, an emollient, a fragrant, a hair conditioner, a humectant, a pearlescent acid, a perfuming agent, a permeation enhancer, a pH-adjusting agent, a preservative, a protectant, a skin penetrating enhancer, a softener, a solubilizer, a sunscreen, a sun blocking agent, a sunless tanning agent, a viscosity modifier, and/or a vitamin.

21. The foamable composition of claim 1, the pH of the foamable composition is in the range from about 4.0 to about 6.0.

22. The foamable composition of claim 1, wherein the foamable composition has a shelf-life of at least one year at ambient temperature.