Carriers, formulations, methods for formulating unstable active agents for external application and uses thereof
US-9161916-B2 · Oct 20, 2015 · US
US10369102B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10369102-B2 |
| Application number | US-201715493807-A |
| Country | US |
| Kind code | B2 |
| Filing date | Apr 21, 2017 |
| Priority date | Aug 7, 2007 |
| Publication date | Aug 6, 2019 |
| Grant date | Aug 6, 2019 |
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Unique foamable vehicles or carriers comprising at least one wax, waxy substance, counterpart or derivative, a stabilizer, water, and a propellant are provided. In some embodiments, the wax is a liquid wax. In some embodiments, the wax includes a solid wax and a liquid wax. The compositions are substantially free of crystals. The components are selected to provide a composition that is substantially resistant to aging and to phase separation, and/or can substantially solubilize and or stabilize active ingredients. Pharmaceutical and cosmetic compositions with potentially enhanced skin delivery and their uses are also provided.
Opening claim text (preview).
What is claimed is: 1. A foamble composition comprising a carrier and a liquefied hydrocarbon gas propellant, wherein the carrier comprises: a) a liquid wax comprising at least one fatty acid and/or at least one fatty alcohol; b) a non-ionic surface active agent; and c) water; wherein the ratio of the carrier to the gas propellant is about 100:3 by weight to about 100:35 by weight; wherein, upon release from a pressurized container, the foamable composition produces a breakable foam; wherein the carrier does not comprise a polymeric agent selected from the group consisting of a bioadhesive agent, a gelling agent, a film forming agent, and a phase change agent. 2. The foamable composition of claim 1 , wherein the fatty acid has 12-22 carbon atoms in its carbon backbone. 3. The foamable composition of claim 1 , wherein the fatty alcohol has 12-22 carbon atoms in its carbon backbone. 4. The foamable composition of claim 1 , wherein the fatty acid has 16-22 carbon atoms in its carbon backbone. 5. The foamable composition of claim 1 , wherein the fatty alcohol has 16-22 carbon atoms in its carbon backbone. 6. The foamable composition of claim 1 , wherein the fatty alcohol is a branched and/or unsaturated fatty alcohol. 7. The foamable composition of claim 1 , wherein the fatty acid is a branched and/or unsaturated fatty acid. 8. The foamable composition of claim 1 , wherein the liquid wax is present at a concentration of at least about 7.5% to about 60% by weight and comprises isostearic acid, myristoleic acid, palmitoleic acid, oleic acid, linoleic acid, alpha linolenic acid, arachidonic acid, eicosapentaenoic acid, erucic acid, docosahexaenoic acid, isostearyl alcohol, oleyl alcohol, lauric acid, octyldodecanol, jojoba oil, or a mixture of two or more thereof. 9. The foamable composition of claim 1 , wherein the carrier comprises a fatty acid and a fatty alcohol, and wherein the ratio of the amount by weight of the carrier of the fatty alcohol to that of the fatty acid is between about 10:9 and about 8:1. 10. The foamable composition of claim 1 , wherein the surface active agent is present at between about 0.2% and about 8% by weight of the carrier. 11. The foamable composition of claim 10 , 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, a polyoxyethylene cetyl ether, polyoxyethylene (23) cetyl ether, polyoxyethylene (2) cetyl ether, polyoxyethylene (10) cetyl ether, a sucrose ester, a partial ester of sorbitol, sorbitan monolaurate, a monoglyceride, a diglyceride, isoceteth-20, steareth 2, glyceryl stearate, steareth-21, sorbitan stearate, laureth 4, sorbitan monooleate, ceteareth 20, steareth 20, ceteth 20, macrogol cetostearyl ether, PEG-30 di polyhydroxystearate, sucrose distearate, cetomacrogol ether, cetearyl glucoside, polysorbate 20; methyl glucose sesquistearate, a sucrose stearic acid ester, a phospholipid, and a mixture of two or more thereof. 12. The foamable composition of claim 1 , further comprising a solvent selected from the group consisting of an organic carrier, a hydrophilic solvent, a hydrophobic solvent, a potent solvent, a polar solvent, a silicone, an emollient, and a mixture of two or more thereof. 13. The foamable composition of claim 12 , wherein the organic carrier is selected from the group consisting of mineral oil, triglyceride, medium chain triglyceride (MCT) oil, capric/caprylic triglyceride, alkyl esters of fatty acids isopropyl palmitate, isopropyl myristate, isopropyl isostearate, poly propylene glycol 15-stearly ether, octyl palmitate, cetyl lactate, cetyl ricinoleate, tocopheryl acetate, acetylated lanolin alcohol, cetyl acetate, phenyl trimethicone, glyceryl oleate, tocopheryl linoleate, wheat germ glycerides, arachidyl propionate, myristyl lactate, decyl oleate, ricinoleate, isopropyl lanolate, pentaerythrityl tetrastearate, neopentylglycol dicaprylate/dicaprate, isononyl isononanoate, isotridecyl isononanoate, myristyl myristate, triisocetyl citrate, octyl dodecanol, maleated soybean oil, unsaturated or polyunsaturated oils, olive oil, corn oil, soybean oil, canola oil, cottonseed oil, coconut oil, sesame oil, sunflower oil, borage seed oil, syzigium aromaticum oil, hempseed oil, herring oil, cod-liver oil, salmon oil, flaxseed oil, wheat germ oil, evening primrose oil, essential oil, silicone oil, dimethicone, cyclomethicone, polyalkyl siloxane, polyaryl siloxane, polyalkylaryl siloxane, a polyether siloxane copolymer, a poly(dimethylsiloxane)-(diphenyl-siloxane), and a mixture of two or more thereof. 14. The foamable composition of claim 12 , wherein the polar solvent is selected from the group consisting of dimethyl isosorbide, glycerol, propylene glycol, hexylene glycol, diethylene glycol, propylene glycol n-alkanols, terpenes, di-terpenes, tri-terpenes, limonene, terpene-ol, 1-menthol, dioxolane, ethylene glycol, oleyl alcohol, alpha-hydroxy acids, lactic acid, glycolic acid, sulfoxides, dimethylsulfoxide (DMSO), dimethylformanide, methyl dodecyl sulfoxide, dimethylacetamide, azone (1-dodecylazacycloheptan-2-one), 2-(n-nonyl)-1,3-dioxolane, alkanols, dialkylamino acetates, and a mixture of two or more thereof. 15. The foamable composition of claim 1 , further comprising a modulating agent, an anti-perspirant, an anti-static agent, a buffering agent, a bulking agent, a chelating agent, a colorant, a conditioner, a deodorant, a diluent, a dye, an emollient, fragrance, a humectant, an occlusive agent, a penetration enhancer, a perfuming agent, a permeation enhancer, a pH-adjusting agent, a preservative, a skin penetration enhancer, a sunscreen, a sun blocking agent, a sunless tanning agent, a vitamin, or a mixture of two or more thereof. 16. The foamable composition of claim 1 , further comprising an active agent. 17. The foamable composition of claim 16 , wherein the active agent is selected from the group consisting of an active herbal extract, an acaricide, an age spot and keratose removing agent, an allergen, an analgesic, a local anesthetic, an antiacne agent, an antiallergic agent, an antiaging agent, an antibacterial, an antibiotic, an antiburn agent, an anticancer agent, an antidandruff agent, an antidepressant, an antidermatitis agent, an antiedemic, an antihistamine, an antihelminth, an antihyperkeratolyte agent, an antiinflammatory agent, an antiirritant, an antilipemic, an antimicrobial, an antimycotic, an antiproliferative agent, an antioxidant, an anti-wrinkle agent, an antipruritic, an antipsoriatic agent, an antirosacea agent, an antiseborrheic agent, an antiseptic agent, an antiswelling agent, an antiviral agent, an antiyeast agent, an astringent, a topical cardiovascular agent, a chemotherapeutic agent, a corticosteroid, a dicarboxylic acid, a disinfectant, a fungicide, a hair growth regulator, a hormone, a hydroxy acid, an immunosuppressant, an immunoregulating agent, an immunomodulatory, an insecticide, an insect repellent, a keratolytic agent, a lactam, a metal oxide, a mitocide, a neuropeptide, a steroid, a non-steroidal anti-inflammatory agent, an oxidizing agent, a pediculicide, a photodynamic therapy agent, a retinoid, a sanative, a scabicide, a vasoconstrictor, a vasodilator, a vitamin, a vitamin D derivative, niacinamide, a wound healing agent, a wart remover; an agent having activity against superficial basal cell
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Ear · CPC title
characterised by the propellant · CPC title
Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title
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 title
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