Dicarboxylic acid foamable vehicle and pharmaceutical compositions thereof

• US 9,265,725 B2
• Filed: 07/05/2007
• Issued: 02/23/2016
• Est. Priority Date: 10/25/2002
• Status: Active Grant

• 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): Hartley, Michael G
• Assistant Examiner(s): CABRAL, ROBERT S
• Application Number:
  US11/825,406
• Publication Number:
  US 20080044444A1
• Time in Patent Office: 3,155 Days
• US Class Current: 1/1
• 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 formable carrier and a propellant, the foamable carrier comprising:

a) about 15% by weight of an azelaic acid;

b) about 11% by weight of medium-chain triglycerides;

c) about 11% by weight of propylene glycol;

d) about 5% by weight of dimethyl isosorbide;

e) about 3% by weight of PEG-40 stearate;

f) about 1% by weight of a cetostearyl alcohol;

g) about 1% by weight of polysorbate 80;

h) about 0.5% by weight of a monoglyceride, a diglyceride, or a combination;

i) about 0.3% by weight of a xanthan gum;

j) about 0.1% by weight of methylcellulose;

k) about 0.1% by weight of a benzoic acid;

l) water;

m) sodium hydroxide; and

wherein the pH of said foamable carrier is about 4.5-5.3; and

wherein the propellant is at a concentration of about 3% to about 25% by weight of the total composition.

2. The foamable composition of claim 1, wherein the medium-chain triglycerides are caprylic/capric triglycerides.

3. The foamable composition of claim 1, wherein the monoglyceride is glyceryl stearate.

4. The foamable composition of claim 1, wherein the medium-chain triglycerides are caprylic/capric triglycerides and the monoglyceride is glyceryl stearate.

5. A foamable carrier comprising:

a) about 15% by weight of an azelaic acid;

b) about 11% by weight of medium-chain triglycerides;

c) about 11% by weight of propylene glycol;

d) about 5% by weight of dimethyl isosorbide;

c) about 3% by weight of PEG-40 stearate;

f) about 1% by weight of a cetostearyl alcohol;

g) about 1% by weight of polysorbate 80;

h) about 0.5% by weight of a monoglyceride, a diglyceride, or a combination thereof;

i) about 0.3% by weight of a xanthan gum;

j) about 0.1% by weight of methylcellulose;

k) about 0.1% by weight of a benzoic acid;

l) water;

m) sodium hydroxide; and

wherein the pH of said foamable carrier is about 4.5-5.3.

6. The foamable carrier of claim 5, wherein the medium-chain triglycerides are caprylic/capric triglycerides.

7. The foamable carrier of claim 5, wherein the monoglyceride is glyceryl stearate.

8. The foamable carrier of claim 5, wherein the medium-chain triglycerides are caprylic/capric triglycerides and the monoglyceride is glyceryl stearate.