Foamable vehicle and pharmaceutical compositions thereof

• US 8,362,091 B2
• Filed: 04/26/2010
• Issued: 01/29/2013
• Est. Priority Date: 08/04/2003
• Status: Active Grant

• Current Assignee: VYNE Therapeutics, Inc.
• Original Assignee: Foamix Ltd. (VYNE Therapeutics, Inc.)
• Inventors: Tamarkin, Dov, Friedman, Doron, Eini, Meir, Besonov, Alex
• Primary Examiner(s): ARNOLD, ERNST V
• Application Number:
  US12/767,511
• Publication Number:
  US 20100266510A1
• Time in Patent Office: 1,009 Days
• Field of Search: None
• US Class Current: 514/945
• CPC Class Codes: A01N 25/16 Foams
• CPC Class Codes: A01N 53/00 Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof
• 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 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 8/046 Aerosols; Foams
• 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 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• 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 17/02 for treating wounds, ulcers, burns, scars, keloids, or the like
• CPC Class Codes: A61P 17/04 Antipruritics
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 17/12 Keratolytics, e.g. wart or anti-corn preparations
• CPC Class Codes: A61P 23/02 Local anaesthetics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/10 Antimycotics
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 33/00 Antiparasitic agents
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61Q 19/00 : Preparations for care of the skin

Abstract

A hygroscopic pharmaceutical composition includes at least one hygroscopic substance at a concentration sufficient to provide an Aw value of at least 0.9 and an antiinfective agent. A foamble pharmaceutical carrier includes about 50% to about 98% of a polar solvent selected from the group consisting of a polyol and PEG; 0% to about 48% of a secondary polar solvent; about 0.2% to about 5% by weight of a surface-active agent; about 0.01% to about 5% by weight of at least one polymeric agent; and a liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition.

Claims

1. A foamable hygroscopic pharmaceutical composition in a pressurized container, the foamable hygroscopic pharmaceutical composition comprising:

i) a carrier composition comprising;

a. at least one hygroscopic substance selected from the group consisting of;

a polyethylene glycol (PEG) and a polyol at a sufficient concentration to provide an Aw value of the hygroscopic pharmaceutical composition of less than 0.9;

b. about 0.01% to about 5% by weight of the carrier composition of a gelling agent; and

c. 0% to about 25% by weight of the carrier composition of water; and

ii) a liquefied or compressed gas propellant;

wherein the foamable hygroscopic pharmaceutical composition forms a breakable foam upon release from the pressurized container;

wherein the breakable foam does not immediately collapse upon exposure to skin temperature; and

wherein the breakable foam breaks under shear force.

2. The hygroscopic pharmaceutical composition of claim 1, further comprising 0% to about 5% by weight of a surface-active agent;

and a therapeutically effective concentration of one or more active agents.

3. A foamable pharmaceutical carrier composition in a pressurized container comprising:

i) a carrier composition comprising;

a. about 50% to about 98% by weight of the carrier composition of a polar solvent selected from the group consisting of (1) a polyol and (2) a polyethylene glycol (PEG);

b. 0% to about 48% by weight of the carrier composition of a secondary polar solvent;

c. about 0.01% to about 5% by weight of the carrier composition of a gelling agent; and

d. 0% to about 25% by weight of the carrier composition of water; and

ii) a liquefied or compressed gas propellant;

wherein the foamable pharmaceutical carrier composition forms a breakable foam upon dispensing from the pressurized container;

wherein the breakable foam does not immediately collapse upon exposure to skin temperature; and

wherein the breakable foam breaks under shear force.

4. The pharmaceutical composition of claim 3, wherein the gelling agent comprises a cellulose polymer.

5. The pharmaceutical composition of claim 3, wherein the polar solvent is a PEG selected from the group consisting of PEG 200, PEG 300, PEG 400, PEG 600, PEG 1000, PEG 4000, PEG 6000 and PEG 8000.

6. The pharmaceutical composition of claim 3, wherein the composition does not contain a surface-active agent.

7. The pharmaceutical composition of claim 3, further comprising a therapeutically effective concentration of one or more active agents.

8. The pharmaceutical composition of claim 3, wherein the polyol comprises at least one of glycerin, butane-1,2,3-triol, butane-1,2,4-triol, hexane-1,2,6-triol, propylene glycol, butanediol, butenediol, butynediol, pentanediol, hexanediol, octanediol, neopentyl glycol, 2-methyl-1,3-propanediol, diethylene glycol, triethylene glycol, tetraethylene glycol, dipropylene glycol, and dibutylene glycol or a mixture of at least two polyols.

9. The pharmaceutical composition of claim 3, wherein the polar solvent comprises a mixture of at least one polyol and at least one PEG.

10. The pharmaceutical composition of claim 3, wherein the pharmaceutical composition is substantially non-aqueous.

11. The pharmaceutical composition of claim 3, wherein the pharmaceutical composition is substantially free of short-chain alcohols.

12. The pharmaceutical composition of claim 3, wherein the pharmaceutical composition forms a stable foam at normal skin temperature for at least about 240 seconds upon release from the pressurized container.

13. The pharmaceutical composition of claim 3, further comprising about 0.2% to about 5% by weight of a surface-active agent.

14. The pharmaceutical composition of claim 13, wherein the surface-active agent comprises a non-ionic surfactant.

15. The pharmaceutical composition of claim 13, wherein the surface-active agent comprises at least one non-ionic surfactant and at least one ionic surfactant.

16. The pharmaceutical composition of claim 15, wherein the ratio of non-ionic surfactant to ionic surfactant is in the range of about 100:

1 to about 6;

1.

17. The pharmaceutical composition of claim 13, further comprising a hygroscopic substance selected from the group consisting of monosaccharides, disaccharides, oligosaccharides, sugar alcohols, honey and a PEG containing surfactant, wherein the composition can provide an Aw value of less than 0.9.

18. The pharmaceutical composition of claim 17, further comprising a therapeutically effective concentration of one or more active agents.