Foamable composition and uses thereof

• US 8,900,554 B2
• Filed: 02/20/2012
• Issued: 12/02/2014
• 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, Eini, Meir
• Primary Examiner(s): Arnold, Ernst V
• Assistant Examiner(s): Song, Jianfeng
• Application Number:
  US13/400,330
• Publication Number:
  US 20120148503A1
• Time in Patent Office: 1,016 Days
• Field of Search: None
• US Class Current: 424/43
• CPC Class Codes: A01N 2300/00 Combinations or mixtures of active ingredients covered by classes A01N27/00 - A01N65/48 with other active or formulation relevant ingredients, e.g. specific carrier materials or surfactants, covered by classes A01N25/00 - A01N65/48
• CPC Class Codes: A01N 25/02 containing liquids as carriers, diluents or solvents
• CPC Class Codes: A01N 25/04 Dispersions, emulsions, suspoemulsions, suspension concentrates or gels foams A01N25/16
• CPC Class Codes: A01N 25/06 Aerosols
• CPC Class Codes: A01N 25/16 Foams
• CPC Class Codes: A01N 25/30 characterised by the surfactants
• CPC Class Codes: A01N 43/30 with two oxygen atoms in positions 1,3, condensed with a carbocyclic ring
• 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: A01N 57/12 containing acyclic or cycloaliphatic radicals
• CPC Class Codes: A01N 65/00 Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof containing compounds of determined constitution A01N27/00 - A01N59/00
• CPC Class Codes: A01N 65/08 Magnoliopsida [dicotyledons]
• CPC Class Codes: A01N 65/12 Asteraceae or Compositae [Aster or Sunflower family], e.g. daisy, pyrethrum, artichoke, lettuce, sunflower, wormwood or tarragon
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 8/046 Aerosols; Foams
• CPC Class Codes: A61K 8/31 Hydrocarbons
• CPC Class Codes: A61K 8/37 Esters of carboxylic acids
• CPC Class Codes: A61K 8/375 the alcohol moiety containing more than one hydroxy group
• CPC Class Codes: A61K 8/4973 with oxygen as the only hetero atom
• CPC Class Codes: A61K 8/73 Polysaccharides
• CPC Class Codes: A61K 8/731 Cellulose; Quaternized cellulose derivatives
• CPC Class Codes: A61K 8/86 : Polyethers
• 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: A61P 29/00 : Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• 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 37/02 : Immunomodulators
• CPC Class Codes: A61P 37/08 : Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61Q 17/00 : Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
• CPC Class Codes: A61Q 17/02 : containing insect repellants
• CPC Class Codes: A61Q 19/02 : for chemically bleaching or whitening the skin
• CPC Class Codes: A61Q 19/08 : Anti-ageing preparations
• CPC Class Codes: Y02A 50/30 : Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The present invention provides a safe and effective insecticide composition suitable for treating a subject infested with a parasitic anthropode or to prevent infestation by an arthropod. The insecticide composition is a foamable composition, including a first insecticide; at least one organic carrier selected from a hydrophobic organic carrier, a polar solvent, an emollient and mixtures thereof, at a concentration of about 2% to about 5%, or about 5% to about 10%; or about 10% to about 20%; or about 20% to about 50% by weight; about 0.1% to about 5% by weight of a surface-active agent; about 0.01% to about 5% by weight of at least one polymeric agent selected from a bioadhesive agent, a gelling agent, a film forming agent and a phase change agent; and (5) a liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition.

Claims

1. A composition comprising a foamable composition and a propellant, the foamable composition comprising:

i. an active agent;

ii. at least one organic carrier selected from the group consisting of a hydrophobic organic carrier, an organic polar solvent, an emollient, and mixtures of any two or more thereof, at a concentration of about 2% to about 50% by weight of the foamable composition;

iii. a surface active agent; and

iv. water;

wherein the propellant is a liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the foamable composition;

wherein the composition is stored in a container and upon release form a breakable foam that collapses upon application of shear force; and

wherein the foamable composition comprises less than 5% or about 5% by weight of the foamable composition of lower alcohols.

2. The composition of claim 1, wherein the active agent is an insecticide.

3. The composition of claim 1, wherein the organic carrier is present at about 5% to about 50% by weight of the foamable composition and the surface-active agent is present at about 0.1% to about 5% by weight of the foamable composition.

4. The composition of claim 1, wherein the foamable composition is an emulsion.

5. The composition of claim 1, further including about 0.1% to about 5% by weight of the foamable composition of a foam adjuvant.

6. The composition of claim 2, wherein the insecticide is selected from the group consisting of an antibiotic insecticide, a botanical insecticide, a carbamate insecticide, a dinitrophenol insecticide, a fluorine insecticide, an insect growth regulator, a chitin synthesis inhibitor, a juvenile hormone mimics, a moulting hormone agonist, a moulting inhibitor, a nereistoxin analogue insecticide, a nicotinoid insecticide, a pyridylmethylamine insecticide, an organochlorine insecticide, a cyclodiene insecticide, an organophosphorus insecticide, an organophosphate insecticide, an organothiophosphate insecticides, an aliphatic amide organothiophosphate insecticide, an oxime organothiophosphate insecticide, a heterocyclic organothiophosphate insecticide, a benzothiopyran organothiophosphate insecticide, a benzotriazine organothiophosphate insecticide, an isoindole organothiophosphate insecticide, an isoxazole organothiophosphate insecticide, a pyrazolopyrimidine organothiophosphate insecticide, a pyridine organothiophosphate insecticide, a pyrimidine organothiophosphate insecticide, a quinoxaline organothiophosphate insecticide, a thiadiazole organothiophosphate insecticide, a triazole organothiophosphate insecticide;

a phenyl organothiophosphate insecticides, a phosphonothioate insecticide, a phenyl ethylphosphonothioate insecticide, a phenyl phenylphosphonothioate insecticide, a phosphoramidate insecticide, a phosphoramidothioate insecticide, a phosphorodiamide insecticide, an oxadiazine insecticide, a phthalimide insecticide, a pyrazole insecticide, a pyrethroid insecticide, a pyrethroid ester insecticide, a pyrethroid ether insecticide, a pyrimidinamine insecticide, a pyrrole insecticide, a tetronic acid insecticide, a thiourea insecticide, a urea insecticide, and mixtures of any two or more thereof.

7. The composition of claim 1, wherein the at least one active agent is selected from the group consisting of a steroidal antiinflammatory agent, an immunosuppressive agent, an immunomodulator, an immunoregulating agent, a hormonal agent, an antibiotic agent, an antifungal agent, an antiviral agent, an antiparasitic agent, vitamin A, a vitamin A derivative, vitamin B, a vitamin B derivative, vitamin C, a vitamin C derivative, vitamin D, a vitamin D derivative, vitamin E, a vitamin E derivative, vitamin F, a vitamin F derivative, vitamin K, a vitamin K derivative, a wound healing agent, a disinfectant, an anesthetic, an antiallergic agent, an alpha hydroxyl acid, lactic acid, glycolic acid, a beta-hydroxy acid, a protein, a peptide, a neuropeptide, a allergen, an immunogenic substance, a haptene, an oxidizing agent, an antioxidant, a dicarboxylic acid, azelaic acid, sebacic acid, adipic acid, fumaric acid, a retinoid, an antiproliferative agent, an anticancer agent, a photodynamic therapy agent, benzoyl chloride, calcium hypochlorite, magnesium hypochlorite, an anti-wrinkle agent, a radical scavenger, a metal, silver, a metal oxide, titanium dioxide, zinc oxide, zirconium oxide, iron oxide, silicone oxide, talc, carbon, an anti wrinkle agent, a skin whitening agent, a skin protective agent, a masking agent, an anti-wart agent, a refatting agent, a lubricating agent, and mixtures of any two or more thereof.

8. The composition of claim 1, wherein the organic carrier comprises a potent solvent selected from the group consisting of propylene glycol, hexylene glycol, benzyl alcohol, terpene-ol, dimethyl isosorbide, a polyol, butanediol, diethylene glycol, terpenes, di-terpenes, tri-terpenes, limonene, dioxolane, dimethylformamide, dimethyl solfoxide, methyl dodecyl sulfoxide, ethyl oleate, ethyl caprylate, diisopropyl adipate, dimethylacetamide, N-methylpyrrolidone, N-hydroxyethylpyrrolidone, polyvinylpyrrolidone, dimethylacetamide, azone (1-dodecylazacycloheptan-2-one), 2-(n-nonyl)-1,3-dioxolane, isosorbide derivatives, glycofurol, ethoxydiglycol, and mixtures of any two or more thereof.

9. The composition of claim 1, wherein the surface active agent is non-ionic or a combination of non-ionic and ionic surface active agents, wherein the ratio of non-ionic surface active agent to ionic surface active agent is about 6:

1 or greater than 6;

1.

10. The composition of claim 1, wherein the organic carrier is a hydrophobic solvent and wherein the surface active agent is present at a concentration of about 0.1% to about 5% by weight of the foamable composition.

11. The composition of claim 1, wherein the foamable composition further comprises at least one polymeric agent selected from the group consisting of bioadhesive agents, gelling agents, film forming agents, phase change agents, and mixtures thereof.

12. The composition of claim 1, wherein the organic carrier is an organic polar solvent.

13. The composition of claim 5, wherein the foam adjuvant is selected from the group consisting of a fatty alcohol having 15 or more carbons in their carbon chain, a fatty acid having 16 or more carbons in their carbon chain, fatty alcohols derived from beeswax, 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 composition of claim 11, wherein the at least one polymeric agent selected from the group consisting of naturally-occurring polymeric materials, a locust bean gum, sodium alginate, sodium caseinate, an egg albumin, a gelatin agar, a carrageenin gum, an xanthan gum, a quince seed extract, a tragacanth gum, a guar gum, a starch, chemically modified starches, semi-synthetic polymeric materials, cellulose ethers, a hydroxyethyl cellulose, a hydroxypropyl cellulose, a methyl cellulose, a carboxymethyl cellulose, a methylhydroxyethylcellulose, hydroxypropyl methylcellulose, a hydroxyethyl carboxymethylcellulose, a carboxymethylcellulose, a hydroxypropyl guar gum, a soluble starch, cationic celluloses, cationic guars, synthetic polymeric materials, 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, carboxyvinyl polymers, a colloidal water-soluble polyalkenyl polyether crosslinked polymer of acrylic acid crosslinked with polyallyl sucrose or polyallyl pentaerythritol, carbomer 934, carbomer 940, carbomer 950, carbomer 980, carbomer 951, carbomer 981, silicon dioxide, a poloxamer, and mixtures of any two or more thereof.

15. The composition of claim 1, wherein the active agent is selected from the group consisting of niacinamide, tazarotene, azelaic acid, permethrin, and mixtures of any two or more thereof.

16. The composition of claim 1, further comprising an excipient selected from the group consisting of a stabilizing agent, an antioxidant, a humectant, a preservative, a colorant, an odorant, and mixtures of any two or more thereof.

17. The composition of claim 2, wherein the insecticide is capable of treating or alleviating a disorder involving an anthropod or parasite.

18. The composition of claim 1, wherein the active agent is water soluble, oil soluble, or both.

19. The composition of claim 1, wherein the composition does not form an impermeable occlusive barrier.

20. The composition of claim 18, wherein the at least one organic carrier is selected from the group consisting of caprylic/capric triglyceride, isopropyl myristate, cyclomethicone, dimethicone, castor oil, oleyl alcohol, diisopropyl adipate, mineral oil, and mixtures of any two or more thereof.