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Details for Patent: 8,119,150

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Details for Patent: 8,119,150

Title:Non-flammable insecticide composition and uses thereof
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.
Inventor(s): Tamarkin; Dov (Ness Ziona, IL), Friedman; Doron (Karmei Yosef, IL), Eini; Meir (Ness Ziona, IL)
Assignee: Foamix Ltd. (Rehovot, IL)
Filing Date:Jul 06, 2006
Application Number:11/481,596
Claims:1. A foamable insecticide composition, including: an emulsion, comprising: i. a first insecticide; ii. at least one organic carrier selected from the group consisting of a hydrophobic organic carrier, an organic polar solvent, an emollient and mixtures thereof, at a concentration of about 2% to about 50% by weight; iii. surface active agent; iv. about 0.01% to about 5% by weight of at least one polymeric agent selected from the group consisting of bioadhesive agents, gelling agents, film forming agents and phase change agents; v. water; and vi. liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition; wherein the composition is released as a breakable foam that collapses upon application of shear force; and wherein the composition includes less than 5% or about 5% by weight of lower alcohols.

2. The insecticide composition of claim 1, wherein said organic carrier comprises at least one member selected from the group of (1) a second insecticide, and (2) a potent solvent.

3. The insecticide composition of claim 2, wherein said organic carrier comprises about 5% to about 50% by weight of said composition and said surface-active agent about 0.1% to about 5% by weight of said composition.

4. The insecticide composition of claim 1, wherein said organic carrier comprises (1) a plant derived insecticide, and (2) a potent solvent.

5. The composition of claim 1 or 2, wherein the emulsion is selected from the group consisting of an oil-in-water emulsion and a water-in-oil emulsion.

6. The composition of claim 1 or 2, wherein the foamable composition includes less than 2% or about 2% by weight of lower alcohols.

7. The composition of claim 1, further including about 0.1% to about 5% by weight of a therapeutically active 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 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 thereof.

8. The composition of claim 1 or 2, wherein the first 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 regulatora 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, such as isazofos and triazophos; 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 and a urea insecticide.

9. The composition of claim 8, wherein the first insecticide is selected from the group consisting of allosamidin, thuringiensin, spinosad, avermectin, abamectin, doramectin, emamectin, eprinomectin, ivermectin and selamectin, lepimectin, milbemectin, milbemycin oxime and moxidectin, anabasine, azadirachtin, d-limonene, nicotine, pyrethrins, cinerins, jasmolin, quassia, rotenone, ryania, sabadilla, bendiocarb, carbaryl, benfuracarb, carbofuran, carbosulfan, decarbofuran, furathiocarb, dimetan, dimetilan, hyquincarb, pirimicarb, alanycarb, aldicarb, aldoxycarb, butocarboxim, butoxycarboxim, methomyl, nitrilacarb, oxamyl, tazimcarb, thiocarboxime, thiodicarb, thiofanox, allyxycarb, aminocarb, bufencarb, butacarb, carbanolate, cloethocarb, dicresyl, dioxacarb, ethiofencarb, fenethacarb, fenobucarb, isoprocarb, methiocarb, metolcarb, mexacarbate, promacyl, promecarb, propoxur, trimethacarb, xylylcarb, dinex, dinoprop, dinosam, barium hexafluorosilicate, cryolite, sodium fluoride, sodium hexafluorosilicate, sulfluramid, amitraz, chlordimeform, formetanate, formparanate, bistrifluoron, buprofezin, chlorfluazuron, cyromazine, diflubenzuron, flucycloxuron, flufenoxuron, hexaflumuron, lufenuron, novaluron, noviflumuron, penfluoron, teflubenzuron, triflumuron, epofenonane, fenoxycarb, hydroprene, kinoprene, methoprene, pyriproxyfen, triprene, chromafenozide, halofenozide, methoxyfenozide, tebufenozide, .alpha.-ecdysone, ecdysterone, dicyclanil, bensultap, cartap, thiocyclam, thiosultap, flonicamid, clothianidin, dinotefuran, imidacloprid and thiamethoxam, nitenpyram, nithiazine, acetamiprid, imidacloprid, nitenpyram, thiacloprid, bromo-DDT, camphechlor, DDT, lindane, methoxychlor, pentachlorophenol, aldrin, bromocyclen, chlorbicyclen, chlordane, chlordecone, dieldrin, dilor, endosulfan, endrin, heptachlor, isobenzan, isodrin, kelevan, mirex, bromfenvinfos, chlorfenvinphos, crotoxyphos, dichlorvos, dicrotophos, dimethylvinphos, fospirate, heptenophos, methocrotophos, mevinphos, monocrotophos, naftalofos, phosphamidon, propaphos, tetrachlorvinphos, dioxabenzofos, fosmethilan, phenthoate, acethion, amiton, cadusafos, chlorethoxyfos, chlormephos, demephion, demephion, demeton, disulfoton, ethion, ethoprophos, isothioate, malathion, methacrifos, oxydemeton-methyl, oxydeprofos, oxydisulfoton, phorate, sulfotep, terbufos, thiometon, amidithion, cyanthoate, dimethoate, ethoate-methyl, formothion, mecarbam, omethoate, prothoate, sophamide, vamidothion, chlorphoxim, phoxim and phoxim-methyl, azamethiphos, coumaphos, coumithoate, dioxathion, endothion, menazon, morphothion, phosalone, pyraclofos, pyridaphenthion, quinothion, dithicrofos, thicrofos, azinphos-ethyl, azinphos-methyl, dialifos, phosmet, isoxathion, zolaprofos, chlorprazophos, pyrazophos, chlorpyrifos, chlorpyrifos-methyl, butathiofos, diazinon, etrimfos, lirimfos, pirimiphos-ethyl, pirimiphos-methyl, primidophos, pyrimitate, tebupirimfos, quinalphos, quinalphos-methyl, athidathion, lythidathion, methidathion, prothidathion, isazofos, triazophos, azothoate, bromophos, bromophos-ethyl, carbophenothion, chlorthiophos, cyanophos, cythioate, dicapthon, dichlofenthion, etaphos, famphur, fenchlorphos, fenitrothion, fensulfothion, fenthion, fenthion-ethyl, heterophos, jodfenphos, mesulfenfos, parathion, parathion-methyl, phenkapton, phosnichlor, profenofos, prothiofos, sulprofos, temephos, trichlormetaphos-3, trifenofos, butonate, trichlorfon, mecarphon, fonofos, trichloronat, cyanofenphos, EPN, leptophos, crufomate, fenamiphos, fosthietan, mephosfolan, phosfolan, pirimetaphos, acephate, isocarbophos, isofenphos, methamidophos, propetamphos, dimefox, mazidox, mipafox, schradan, indoxacarb, dialifos, phosmet, tetramethrin, acetoprole, ethiprole, fipronil, pyrafluprole, pyriprole, tebufenpyrad, tolfenpyrad, vaniliprole, acrinathrin, allethrin, bioallethrin, barthrin, bifenthrin, bioethanomethrin, cyclethrin, cycloprothrin, cyfluthrin, beta-cyfluthrin, cyhalothrin, cypermethrin, alpha-cypermethrin, beta-cypermethrin, theta-cypermethrin, zeta-cypermethrin, cyphenothrin, deltamethrin, dimefluthrin, dimethrin, empenthrin, fenfluthrin, fenpirithrin, fenpropathrin, fenvalerate, esfenvalerate, flucythrinate, fluvalinate, furethrin, imiprothrin, metofluthrin, permethrin, biopermethrin, transpermethrin, phenothrin, prallethrin, profluthrin, pyresmethrin, resmethrin, bioresmethrin, cismethrin, tefluthrin, terallethrin, tetramethrin, tralomethrin and transfluthrin, etofenprox, flufenprox, halfenprox, protrifenbute, silafluofen, flufenerim, pyrimidifen, chlorfenapyr, spiromesifen, spirotetramat, diafenthiuron, flucofuron, sulcofuron, closantel, crotamiton, fenazaflor, fenoxacrim, flubendiamide, hydramethylnon, isoprothiolane, malonoben, metaflumizone, metoxadiazone, nifluridide, pyridaben, pyridalyl, rafoxanide, triarathene and triazamate.

10. The composition of claim 1 or 2, wherein the concentration range of the first insecticide is selected from the group of (i) between about 0.005% and about 0.5%; (ii) between about 0.5% and about 2%; (iii) between about 2% and about 5%; and (iv) between about 5% and about 12%.

11. The composition of claim 1, wherein upon release from the container, a shear-sensitive foam, having a density range selected from (1) between about 0.02 gr/mL and about 0.1 gr/mL; and (2) between about 0.02 gr/mL and about 0.1 gr/mL, is produced.

12. The composition of claim 1, wherein the foamable composition further contains at least one additional therapeutic agent selected from the group consisting of an 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 thereof.

13. The composition of claim 1, wherein the concentration of the surface active agent is between about 0.1% and about 5%.

14. The composition of claim 1, wherein the emulsion is a water in oil emulsion and wherein the HLB range of the surface active agent is selected from (1) between about 2 and about 9; and (2) between about 9 and about 14.

15. The composition of claim 2, wherein the second insecticide is selected from the group consisting of: i. an oil, selected from anise oil, bergemot oil, canola oil, cassia oil, catnip oil, cedarwood oil, citronella oil, clove oil, eucalyptus oil, garlic oil, ginger oil, grapefruit oil, jojova oil, lavender oil, lavandin oil, lemon oil, lime oil, orange oil, peppermint oil, pine oil, rosemary oil, sage oil, spearmint oil, star anise oil, styrax oil, tea tree oil, tangerine oil, thyme oil and white clover oil; ii. an insect repellent; iv. diethyl toluamide; v. a terpenoid compound; and vi. a compound selected from the group consisting of perillyl alcohol, carveol, myrtenol, cis-verbenol, myrtanol, iso-pinocampheol, dihydrocarveol, isopulegol, terpineol, terpinen-4-ol, nerol, geraniol, linalool, menthol, beta-citronellol, and dihydro-myrcenol, an ester of a terpene-ol with an aliphatic carboxylic acid, carvyl acetate and carvyl propionate.

16. The composition of claim 2, wherein the potent solvent is selected from the group consisting of a polyol, propylene glycol, hexylene glycol, butanediol, diethylene glycol, benzyl alcohol, terpenes, di-terpenes, tri-terpenes, limonene, terpene-ol, dioxolane, dimethylformanide, dimethyl solfoxide (DMSO), 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, dimethyl isosorbide, glycofurol and ethoxydiglycol (transcutol) and mixtures thereof in any proportion.

17. The composition of claim 1, wherein the composition is housed in a pressurized container.

18. The composition of claim 1, wherein the composition is petrolatum-free.

19. The composition of claim 1, wherein the composition is non-occlusive.

20. The composition of claim 1, wherein the composition includes less than 1% or about 1% by weight of lower alcohols.

21. The composition of claim 1, wherein the insecticide is selected from the group consisting of hexachlorobenzene, carbamate, naturally occurring pyrethroids, permethrin, allethrin, bioalethrin, phenothrin, malathion and piperonyl butoxide.

22. The composition of claim 21, wherein the insecticide is permethrin in a concentration of between 0.1% and 10%.

23. The composition of claim 21, wherein the insecticide is malathion in a concentration of between 0.1% and 5%.

24. The composition of claim 21, wherein the insecticide is metronidazole.

25. The composition of claim 2 or 3, wherein the second insecticide is star anise oil.

26. The composition of claim 2 or 3, wherein the potent solvent is selected from the group consisting of propylene glycol, hexylene glycol, benzyl alcohol, terpene-ol and dimethyl isosorbide.

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

28. A foamable insecticide composition, including: an emulsion comprising: i. about 0.5% to about 10% permethrin; ii. at least one organic carrier selected from the group consisting of a hydrophobic organic carrier, an organic polar solvent, an emollient and mixtures thereof, at a concentration of about the total amount of hydrophobic carrier is in the range between 20% and 40% by weight; iii. about 0.1% to about 5% of a non-ionic surface active agent by weight; iv. about 0.01% to about 5% by weight of at least one polymeric agent; v. water; and vi. liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition, wherein the composition is released as a breakable foam that collapses upon application of shear force; and wherein the composition includes less than 5% or about 5% by weight of lower alcohols.

29. The insecticide composition of claim 28, wherein the surface active agent is non-ionic or a combination of non-ionic and ionic surface active agent, wherein the ratio of non-ionic surface active agent to ionic surface active agent is about 6:1 or greater than 6:1.

30. A method of treating, alleviating or preventing a disorder, wherein the disorder involves a parasitic anthropod infestation as one of its etiological factors, including: administering topically to a surface having the disorder, a foamed composition comprising: an emulsion comprising: i. a first insecticide; ii. at least one organic carrier selected from the group consisting of a hydrophobic organic carrier, an organic polar solvent, an emollient and mixtures thereof, at a concentration of about 2% to about 50% by weight; iii. surface active agent; iv. 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; v. water; and vi. liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition, wherein the composition is released as a breakable foam that collapses upon application of shear force; and wherein the composition includes less than 5% or about 5% by weight of lower alcohols.

31. The method claim 30, wherein said organic carrier comprises at least one member, selected from the group consisting of (1) a second insecticide, and (2) a potent solvent.

32. The method of claim 30, wherein said organic carrier contains both a plant derived insecticide and a potent solvent.

33. The method of claim 30 or 31, wherein the composition includes less than 2% or about 2% by weight of lower alcohols.

34. The method of claim 31, wherein the second insecticide is selected from the group consisting of: i. an oil, selected from anise oil, bergemot oil, canola oil, cassia oil, catnip oil, cedarwood oil, citronella oil, clove oil, eucalyptus oil, garlic oil, ginger oil, grapefruit oil, jojova oil, lavender oil, lavandin oil, lemon oil, lime oil, orange oil, peppermint oil, pine oil, rosemary oil, sage oil, spearmint oil, star anise oil, styrax oil, tea tree oil, tangerine oil, thyme oil and white clover oil; ii. an insect repellent; iv. diethyl toluamide; v. a terpenoid compound; and vi. a compound selected from the group consisting of perillyl alcohol, carveol, myrtenol, cis-verbenol, myrtanol, iso-pinocampheol, dihydrocarveol, isopulegol, terpineol, terpinen-4-ol, nerol, geraniol, linalool, menthol, beta-citronellol, and dihydro-myrcenol, an ester of a terpene-ol with an aliphatic carboxylic acid, carvyl acetate and carvyl propionate.

35. The method of claim 31, wherein the potent solvent is selected from the group consisting of a polyol, propylene glycol, hexylene glycol, butanediol, diethylene glycol, benzyl alcohol, terpenes, di-terpenes, tri-terpenes, limonene, terpene-ol, dioxolane, dimethylformanide, dimethyl solfoxide (DMSO), 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, an isosorbide derivative, dimethyl isosorbide, glycofurol and ethoxydiglycol (transcutol) and mixtures thereof in any proportion.

36. The method of claim 30 or 31, wherein the disorder is pediculosis.

37. The method of claim 30 or 31, wherein the first insecticide is selected from the group of include hexachlorobenzene, carbamate, a naturally occurring pyrethroid, permethrin, allethrin, bioalethrin, phenothrin, malathion and piperonyl butoxide.

38. The method of claim 30, wherein the surface active agent is non-ionic or a combination of non-ionic and ionic surface active agent, wherein the ratio of non-ionic surface active agent to ionic surface active agent is about 6:1 or greater than 6:1.
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