Foamable carriers

• US 8,722,021 B2
• Filed: 03/06/2013
• Issued: 05/13/2014
• Est. Priority Date: 10/25/2002
• Status: Expired due to Term

• Current Assignee: VYNE Therapeutics, Inc.
• Original Assignee: Foamix Ltd. (VYNE Therapeutics, Inc.)
• Inventors: Friedman, Doron, Besonov, Alex, Tamarkin, Dov, Eini, Meir
• Primary Examiner(s): ZISKA, SUZANNE E
• Application Number:
  US13/786,902
• Publication Number:
  US 20130183250A1
• Time in Patent Office: 433 Days
• Field of Search: None
• US Class Current: 424/43
• CPC Class Codes: A01N 25/16 Foams
• CPC Class Codes: A61K 2800/24 Thermal properties
• CPC Class Codes: A61K 2800/242 Exothermic; Self-heating; Heating sensation
• CPC Class Codes: A61K 2800/244 Endothermic; Cooling; Cooling sensation
• CPC Class Codes: A61K 2800/30 Characterized by the absence of a particular group of ingredients
• CPC Class Codes: A61K 2800/75 Anti-irritant
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/351 not condensed with another ring
• CPC Class Codes: A61K 31/4164 1,3-Diazoles
• CPC Class Codes: A61K 31/4174 Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
• CPC Class Codes: A61K 31/522 having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• CPC Class Codes: A61K 31/535 having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
• CPC Class Codes: A61K 31/567 substituted in position 17 alpha, e.g. mestranol, norethandrolone
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 31/7036 having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
• CPC Class Codes: A61K 31/7048 having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin , digitoxin or digoxin
• CPC Class Codes: A61K 38/12 Cyclic peptides , e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C A61K38/043 - A61K38/046 take precedence
• CPC Class Codes: A61K 38/212 IFN-alpha
• CPC Class Codes: A61K 47/06 Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
• 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 47/20 : containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• CPC Class Codes: A61K 47/26 : Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/34 : Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61K 47/38 : Cellulose; Derivatives thereof
• CPC Class Codes: A61K 47/46 : Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
• CPC Class Codes: A61K 8/046 : Aerosols; Foams
• CPC Class Codes: A61K 8/34 : Alcohols
• CPC Class Codes: A61K 8/345 : containing more than one hydroxy group
• CPC Class Codes: A61K 8/362 : Polycarboxylic acids
• CPC Class Codes: A61K 8/37 : Esters of carboxylic acids
• CPC Class Codes: A61K 8/42 : Amides
• CPC Class Codes: A61K 8/4993 : Derivatives containing from 2 to 10 oxyalkylene groups
• CPC Class Codes: A61K 8/60 : Sugars; Derivatives thereof
• CPC Class Codes: A61K 8/731 : Cellulose; Quaternized cellulose derivatives
• CPC Class Codes: A61K 8/736 : Chitin; Chitosan; Derivatives thereof
• CPC Class Codes: A61K 8/8152 : Homopolymers or copolymers of esters, e.g. (meth)acrylic acid esters; Compositions of derivatives of such polymers
• CPC Class Codes: A61K 8/8158 : Homopolymers or copolymers of amides or imides, e.g. (meth) acrylamide; Compositions of derivatives of such polymers
• CPC Class Codes: A61K 8/86 : Polyethers
• CPC Class Codes: A61K 8/87 : Polyurethanes
• CPC Class Codes: A61K 8/922 : of vegetable origin
• CPC Class Codes: A61K 9/0007 : Effervescent A61K9/0065 takes precedence
• 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 9/107 : Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00
• 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 1/00 : Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 17/00 : Drugs for dermatological disorders
• CPC Class Codes: A61P 17/02 : for treating wounds, ulcers, burns, scars, keloids, or the like
• CPC Class Codes: A61P 17/14 : for baldness or alopecia
• CPC Class Codes: A61P 17/16 : Emollients or protectives, e.g. against radiation
• 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 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: A61P 37/06 : Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 37/08 : Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 5/00 : Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 9/00 : Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61Q 17/02 : containing insect repellants
• CPC Class Codes: A61Q 17/04 : Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• CPC Class Codes: A61Q 19/00 : Preparations for care of the skin
• CPC Class Codes: A61Q 19/007 : Preparations for dry skin
• CPC Class Codes: A61Q 19/02 : for chemically bleaching or whitening the skin
• CPC Class Codes: A61Q 19/04 : for chemically tanning the skin topical sun or radiation screening or tanning preparations A61Q17/04
• CPC Class Codes: A61Q 19/08 : Anti-ageing preparations
• CPC Class Codes: A61Q 7/00 : Preparations for affecting hair growth
• CPC Class Codes: A61Q 7/02 : Preparations for inhibiting or slowing hair growth

Abstract

The invention relates to an alcohol-free cosmetic or therapeutic foam carrier comprising water, a hydrophobic organic carrier, a foam adjuvant agent, a surface-active agent and a gelling agent. The cosmetic or therapeutic foam carrier does not contain aliphatic alcohols, making it non-irritating and non-drying. The alcohol-free foam carrier is suitable for inclusion of both water-soluble and oil soluble therapeutic and cosmetic agents.

Claims

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

i) about 0.1% to about 5% by weight of the carrier of a surface-active agent;

ii) about 2% to about 75% by weight of the carrier of an organic solvent selected from the group consisting of an emollient, a polar solvent, an oil, and mixtures thereof;

iii) about 0.01% to about 5% by weight of the carrier of at least one polymeric agent selected from the group consisting of a bioadhesive agent, a gelling agent, a film forming agent, and a phase change agent; and

iv) water;

wherein upon release from a foam dispenser, a foam is produced; and

wherein the foam remains stable as a foam for at least 60 seconds at 37°

C.

2. The foamable composition of claim 1, wherein the carrier further comprises an active agent.

3. The foamable composition of claim 1, wherein the liquefied or compressed gas propellant is present at about 3% to about 25% by weight of the carrier.

4. The foamable composition of claim 1, wherein the organic solvent is selected from the group consisting of an emollient, a polar solvent, an essential oil, and mixtures of any two or more thereof.

5. The foamable composition of claim 1, wherein the carrier comprises a micro-emulsion.

6. The foamable composition of claim 1, wherein the carrier comprises nanoparticles.

7. The foamable composition of claim 1, wherein the surface-active agent is present at less than about 2% by weight of the carrier.

8. The foamable composition of claim 1, wherein the polymeric agent is present at less than about 1% by weight of the carrier.

9. The foamable composition of claim 1, wherein the carrier does not include petrolatum.

10. The foamable composition of claim 2, wherein the active agent is selected from the group consisting of an antibacterial agent, an antibiotic, an anti-parasitic agent, an antifungal agent, an antiviral agent, a corticosteroid, a steroidal anti-inflammatory agent, a non-steroidal immunomodulating agent, an immunosuppressant, an anti-allergic agent, an antihistamine, an anticancer agent, a hormone, an androgen, an estrogen, a progesterone, a contraceptive agent, a retinoid, vitamin A, vitamin B, vitamin D, an anesthetic, a lubricating agent, an immunizing agent, a cytotoxic drug, an antiproliferative drug, an anti-oxidant, a radical scavenger, and mixtures of any two or more thereof.

11. The foamable composition of claim 1, wherein the carrier comprises less than about 2% by weight of the carrier of one or more lower alcohols having up to 5 carbon atoms in their carbon chain skeleton.

12. The foamable composition of claim 1, wherein the polymeric agent is selected from the group consisting of a locust bean gum, sodium alginate, sodium caseinate, egg albumin, a gelatin agar, a carrageenin gum, a xanthan gum, a quince seed extract, a tragacanth gum, a guar gum, a starch, a chemically modified starch, cellulose ethers, a hydroxyethyl cellulose, a methyl cellulose, a carboxymethyl cellulose, a hydroxy propylmethyl cellulose, a hydroxypropyl guar gum, a soluble starch, cationic celluloses, cationic guars, carboxyvinyl polymers, a polyvinylpyrrolidone, a polyvinyl alcohol, polyacrylic acid polymers, polymethacrylic acid polymers, polyvinyl acetate polymers, polyvinyl chloride polymers, polyvinylidene chloride polymers, acrylic acid/ethyl acrylate copolymers, crosslinked copolymers of acrylic acid and C10-C30 alkyl acrylate (pemulen), carboxyvinyl polymers, a carbopol, and mixtures of any two or more thereof.

13. The foamable composition of claim 1, wherein the foamable composition further comprises about 0.1% to about 5% by weight of the carrier of a foam adjuvant selected from the group consisting of a fatty alcohol having 15 or more carbons in its carbon chain;

a fatty acid having 16 or more carbons in its carbon chain;

fatty alcohols, derived from beeswax and including a mixture of alcohols, a majority of which has at least 20 carbon atoms in their carbon chain;

a fatty alcohol having at least one double bond;

a fatty acid having at least one double bond;

a branched fatty alcohol;

a branched fatty acid;

a fatty acid substituted with a hydroxyl group;

cetyl alcohol;

stearyl alcohol;

arachidyl alcohol;

behenyl alcohol;

1-triacontanol;

hexadecanoic acid;

stearic acid;

arachidic acid;

behenic acid;

octacosanoic acid;

12-hydroxy stearic acid; and

mixtures of any two or more thereof.

14. The foamable composition of claim 1, wherein the surface-active agent is selected from the group consisting of a non ionic surface-active agent, a cationic surface-active agent, an amphoteric surface-active agent, an ionic surface-active agent, and mixtures of any two or more thereof.

15. The foamable composition of claim 1, wherein the surface-active agent is a non ionic surface-active agent.

16. The foamable composition of claim 13, wherein the combined amount of foam adjuvant, surface active agent, and gelling agent is less than about 8% by weight of the carrier.

17. The foamable composition of claim 14, wherein the surface-active agent is selected from the group consisting of a polysorbate, polyoxyethylene (20) sorbitan monostearate, polyoxyethylene (20) sorbitan monooleate, a polyoxyethylene fatty acid ester, polyoxyethylene (8) stearate, polyoxyethylene (20) stearate, polyoxyethylene (40) stearate, polyoxyethylene (100) stearate, a polyoxyethylene alkyl ether, polyoxyethylene cetyl ether, polyoxyethylene (23) cetyl ether, polyoxyethylene (2) cetyl ether, polyoxyethylene (10) cetyl ether, isoceteth-20, a sucrose ester, a partial ester of sorbitol, an anhydride of a partial ester of sorbitol, sorbitan monolaurate, sorbitan stearate, a monoglyceride, glyceryl monostearate, a diglyceride, lecithin, sodium methyl cocoyl taurate, sodium methyl oleoyl taurate, sodium lauryl sulfate, triethanolamine lauryl sulfate, a betaine, cocamidopropyl betaine, and mixtures of any two or more thereof.

18. The foamable composition of claim 1, wherein the carrier comprises more than about 50% by weight of the carrier of a potent solvent.

19. The foamable composition of claim 18, wherein the potent solvent is selected from the group consisting of polyethylene glycol, propylene glycol, hexylene glycol, butane-diol and isomers thereof, glycerol, benzyl alcohol, dimethyl sulfoxide, ethyl oleate, ethyl caprylate, dimethylacetamide, N-methylpyrrolidone, N-hydroxyethylpyrrolidone, polyvinylpyrrolidone, isosorbide derivatives, dimethyl isosorbide, glycofurol, ethoxydiglycol, and mixtures of any two or more thereof.

20. The foamable composition of claim 10, wherein the active agent is suitable for the treatment of a disorder of a body cavity or a mucosal surface, wherein the disorder is selected from the group consisting of a bacterial infection, a fungal infection, a viral infection, vaginal dryness, dyspareunia, HIV, a sexually transmitted disease, post-surgical adhesions, a hormonal deficiency, and a combination of any two or more thereof.

23. The foamable composition of claim 1, wherein the foam remains stable as a foam for at least 2 or 3 minutes at 37°

C.

25. The foamable composition of claim 2, wherein the active agent is an azole.

26. The foamable composition of claim 25, wherein the azole is selected from the group consisting of azoles, diazoles, triazoles, pyrazoles, and mixtures of any two or more thereof.

27. The foamable composition of claim 26, wherein the azole is selected from the group consisting of clotrimazole, econazole, fluconazole, ketoconazole, itraconazole, metronidazole, miconazole, phenylbutazone, oxyphenbutazone, feprazone, azapropazone, trimethazone, and mixtures of any two or more thereof.

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

i) about 0.1% to about 5% by weight of the carrier of a surface-active agent;

ii) about 70% to about 99% by weight of the carrier of a hydrophobic organic solvent;

iii) a stabilizer selected from the group consisting of about 0.01% to about 5% by weight of the carrier of a polymeric agent and about 0.1% to about 5% by weight of the carrier of foam adjuvant;

wherein upon release from a foam dispenser, a foam is produced; and

wherein the foam remains stable as a foam for at least 60 seconds at 37°

C.

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

i) about 0.2% to about 15% by weight of the carrier of a surface-active agent;

ii) about 70% to about 99% by weight of the carrier of a hydrophobic organic solvent;

iii) a stabilizer selected from the group consisting of about 0.01% to about 5% by weight of the carrier of a polymeric agent and about 0.1% to about 5% by weight of the carrier of foam adjuvant;

wherein upon release from a foam dispenser, a foam is produced; and

wherein the foam remains stable as a foam for at least 60 seconds at 37°

C.

24. The foamable composition of claim 22, wherein the foam remains stable as a foam for at least 2 or 3 minutes at 37°

C.