Details for Patent: 8,114,385

Title:	Oleaginous pharmaceutical and cosmetic foam
Abstract:	The invention relates to stable oleaginous cosmetic or therapeutic foam compositions containing certain active agents, having unique therapeutic properties and methods of treatment using such compositions. The foamable composition includes a polyethylene glycol (PEG) or PEG derivative and mixtures thereof, wherein the PEG or PEG derivative is present at a concentration of about 70% to about 96.5% by weight of the total composition; a surface-active agent at a concentration of about 0.1% to less than about 10% by weight of the total composition; and a therapeutically effective amount of at least one active agent.
Inventor(s):	Tamarkin; Dov (Maccabim, IL), Friedman; Doron (Karmei Yosef, IL), Eini; Meir (Ness Ziona, IL), Besonov; Alex (Rehovot, IL)
Assignee:	Foamix Ltd. (Rehovot, IL)
Filing Date:	Dec 26, 2006
Application Number:	11/645,444
Claims:	1. An foamable pharmaceutical or cosmetic composition, comprising: a polyethylene glycol (PEG) or mixtures thereof, wherein the PEG is present at a concentration of about 70% to about 96.5% by weight of the total composition; at least one gelling agent at a concentration of about 0.1% to about 5% by weight of the total composition; a surface-active agent at a concentration of about 0.1% to about 10% by weight of the total composition; and a therapeutically effective amount of at least one active agent; wherein the composition has less than about 5% final concentration of lower alcohols having up to 5 carbon atoms in their carbon chain skeleton; and wherein if mixed with a propellant in a canister, the composition is capable of being released as a breakable foam which collapses on application of shear force and that does not readily collapse upon dispensing on the skin. 2. The composition of claim 1, wherein the at least one gelling agent is selected from the group consisting of natural polymeric materials, semi-synthetic polymeric materials, synthetic polymeric materials, inorganic gelling agents and mixtures thereof. 3. The composition of claim 1, further comprising: at least one liquefied or compressed gas propellant, at a concentration of about 3% to about 25% by weight of the total composition. 4. The composition of claim 1, wherein the polyethylene glycol (PEG) or mixtures thereof is liquid or is flowable at ambient temperature. 5. The composition of claim 1, wherein the polyethylene glycol (PEG) or mixtures thereof have an average Molecular Weight of about 190 kD to about 10,000 kD. 6. The composition of claim 1, wherein the polyethylene glycol (PEG) is selected from the group consisting of PEG200, PEG300, PEG400, PEG600, PEG 4000,PEG 6000 and PEG 10000and mixtures thereof. 7. The composition of claim 1, wherein the polyethylene glycol (PEG) comprises PEG400. 8. The composition of claim 1, wherein the surface-active agent is a non-ionic surface active agent. 9. The composition of claim 1, wherein surface-active agent is selected from the group consisting of sorbitan derivatives, alkoxylated alcohols, hydroxylated derivatives of polymeric silicones, alkylated derivatives of hydroxylated polymeric silicones, glyceryl esters, beeswax derivatives, lecithin, and mixtures thereof. 10. The composition of claim 1, wherein surface-active agent is selected from the group consisting of polysorbates, polyoxyethylene fatty acid esters, polyoxyethylene alkyl ethers, sucrose esters, partial esters of sorbitol and its anhydrides, mono and diglycerides, isoceteth-20, sodium methyl cocoyl taurate, sodium methyl oleoyl taurate, sodium lauryl sulfate, triethanolamine lauryl sulfate, betaines and mixtures thereof. 11. The composition of claim 10, wherein the surface-active agent comprises a polyoxyethylene alkyl ether. 12. The composition of claim 1, further comprising an emollient. 13. The composition of claim 12, wherein the emollient is selected from the group consisting of hexylene glycol, propylene glycol, isostearic acid derivatives, isopropyl palmitate, isopropyl isostearate, diisopropyl adipate, diisopropyl dimerate, maleated soybean oil, 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, propylene glycol ricinoleate, isopropyl lanolate, pentaerythrityl tetrastearate, neopentylglycol dicaprylate/dicaprate, isononyl isononanoate, isotridecyl isononanoate, myristyl myristate, triisocetyl citrate, octyl dodecanol, sucrose esters of fatty acids, octyl hydroxystearate and mixtures thereof. 14. The composition of claim 1, wherein the composition is contained within a pressurized container. 15. The composition of claim 1, further comprising an antioxidant. 16. The composition of claim 15, wherein the antioxidant is one or more antioxidants selected from the group consisting of ascorbic acid (vitamin C) and its salts, ascorbyl esters of fatty acids, ascorbic acid derivatives, tocopherol (vitamin E), tocopherol sorbate, tocopherol acetate, other esters of tocopherol, butylated hydroxy benzoic acids and their salts, 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid, gallic acid and its alkyl esters, propyl gallate, uric acid and its salts and alkyl esters, sorbic acid and its salts, lipoic acid, amines, sulfhydryl compounds, dihydroxy fumaric acid and its salts, lycine pidolate, arginine pilolate, nordihydroguaiaretic acid, bioflavonoids, curcumin, lysine, methionine, proline, superoxide dismutase, silymarin, tea extracts, grape skin/seed extracts, melanin, and rosemary extracts. 17. An foamable pharmaceutical or cosmetic composition, comprising: a polyethylene glycol (PEG) or mixtures thereof, wherein the PEG is present at a concentration of about 70% to about 96.5% by weight of the total composition; at least one gelling agent at a concentration of about 0.1% to about 5% by weight of the total composition; a surface-active agent at a concentration of about 0.1% to about 10% by weight of the total composition; and a therapeutically effective amount of an antiproliferative agent, wherein the composition has less than about 5% final concentration of lower alcohols having up to 5 carbon atoms in their carbon chain skeleton; and wherein if mixed with a propellant in a canister, the composition is capable of being released as a breakable foam which collapses on application of shear force and that does not readily collapse upon dispensing on the skin. 18. The composition of claim 17, wherein the at least one gelling agent is selected from the group consisting of natural polymeric materials, semi-synthetic polymeric materials, synthetic polymeric materials, inorganic gelling agents and mixtures thereof. 19. The foamable therapeutic composition of claim 17, further comprising: at least one liquefied or compressed gas propellant, at a concentration of about 3% to about 25% by weight of the total composition. 20. The composition of claim 17, wherein the polyethylene glycol (PEG) or mixtures thereof is liquid or flowable at ambient temperature. 21. The composition of claim 17, wherein the polyethylene glycol (PEG) is selected from the group consisting of PEG200, PEG300, PEG400, PEG600, PEG 4000,PEG 6000 and PEG 10000and mixtures thereof. 22. The composition of claim 17, wherein the polyethylene glycol (PEG) or mixtures thereof have an average Molecular Weight of about 190 kD to about 10,000 kD. 23. The composition of claim 17, wherein the polyethylene glycol (PEG) comprises PEG400. 24. The composition of claim 17, wherein the surface-active agent is a non-ionic surface active agent. 25. The composition of claim 17, wherein surface-active agent is selected from the group consisting of sorbitan derivatives, alkoxylated alcohols, hydroxylated derivatives of polymeric silicones, alkylated derivatives of hydroxylated polymeric silicones, glyceryl esters, beeswax derivatives, lecithin, and mixtures thereof. 26. The composition of claim 17, wherein surface-active agent is selected from the group consisting of polysorbates, polyoxyethylene fatty acid esters, polyoxyethylene alkyl ethers, sucrose esters, partial esters of sorbitol and its anhydrides, mono and diglycerides, isoceteth-20, sodium methyl cocoyl taurate, sodium methyl oleoyl taurate, sodium lauryl sulfate, triethanolamine lauryl sulfate, betaines and mixtures thereof. 27. The composition of claim 26, wherein the surface-active agent comprises a polyoxyethylene alkyl ether. 28. The composition of claim 17, further comprising an emollient. 29. The composition of claim 28, wherein the emollient is selected from the group consisting of hexylene glycol, propylene glycol, isostearic acid derivatives, isopropyl palmitate, isopropyl isostearate, diisopropyl adipate, diisopropyl dimerate, maleated soybean oil, 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, propylene glycol ricinoleate, isopropyl lanolate, pentaerythrityl tetrastearate, neopentylglycol dicaprylate/dicaprate, isononyl isononanoate, isotridecyl isononanoate, myristyl myristate, triisocetyl citrate, octyl dodecanol, sucrose esters of fatty acids, octyl hydroxystearate and mixtures thereof. 30. The composition of claim 17, wherein the composition is contained within a pressurized container. 31. The composition of claim 17, further comprising an antioxidant. 32. The composition of claim 31, wherein the antioxidant is one or more antioxidant selected from the group consisting of ascorbic acid (vitamin C) and its salts, ascorbyl esters of fatty acids, ascorbic acid derivatives, tocopherol (vitamin E), tocopherol sorbate, tocopherol acetate, other esters of tocopherol, butylated hydroxy benzoic acids and their salts, 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid, gallic acid and its alkyl esters, propyl gallate, uric acid and its salts and alkyl esters, sorbic acid and its salts, lipoic acid, amines, sulfhydryl compounds, dihydroxy fumaric acid and its salts, lycine pidolate, arginine pilolate, nordihydroguaiaretic acid, bioflavonoids, curcumin, lysine, methionine, proline, superoxide dismutase, silymarin, tea extracts, grape skin/seed extracts, melanin, and rosemary extracts. 33. A foamable composition, comprising: a polyethylene glycol (PEG) or mixtures thereof, wherein the PEG is present at a concentration of about 70% to about 96.5% by weight of the total composition; at least one gelling agent at a concentration of about 0.1% to about 5% by weight of the total composition; a surface-active agent at a concentration of about 0.1% to about 10% by weight of the total composition; and a therapeutically effective amount of a vitamin or a derivative thereof; wherein the composition has less than about 5% final concentration of lower alcohols having up to 5 carbon atoms in their carbon chain skeleton; and wherein if mixed with a propellant in a canister, the composition is capable of being released as a breakable foam which collapses on application of shear force and that does not readily collapse upon dispensing on the skin. 34. The composition of claim 33, wherein the at least one gelling agent is selected from the group consisting of natural polymeric materials, semi-synthetic polymeric materials, synthetic polymeric materials, inorganic gelling agents and mixtures thereof. 35. The composition of claim 33, further comprising: at least one liquefied or compressed gas propellant, at a concentration of about 3% to about 25% by weight of the total composition. 36. The composition of claim 33, wherein the polyethylene glycol (PEG) or mixtures thereof is liquid or flowable at ambient temperature. 37. The composition of claim 33, wherein the polyethylene glycol (PEG) is selected from the group consisting of PEG200, PEG300, PEG400, PEG600, PEG 4000,PEG 6000 and PEG 10000and mixtures thereof. 38. The composition of claim 33, wherein the polyethylene glycol (PEG) or mixtures thereof have an average Molecular Weight of about 190 kD to about 10,000 kD. 39. The composition of claim 33, wherein the polyethylene glycol (PEG) comprises PEG400. 40. The composition of claim 33, wherein the surface-active agent is a non-ionic surface active agent. 41. The composition of claim 33, wherein the surface-active agent is selected from the group consisting of sorbitan derivatives, alkoxylated alcohols, hydroxylated derivatives of polymeric silicones, alkylated derivatives of hydroxylated polymeric silicones, glyceryl esters, beeswax derivatives, lecithin, and mixtures thereof. 42. The composition of claim 33, wherein the surface-active agent is selected from the group consisting of polysorbates, polyoxyethylene fatty acid esters, polyoxyethylene alkyl ethers, sucrose esters, partial esters of sorbitol and its anhydrides, mono and diglycerides, isoceteth-20, sodium methyl cocoyl taurate, sodium methyl oleoyl taurate, sodium lauryl sulfate, triethanolamine lauryl sulfate, betaines and mixtures thereof. 43. The composition of claim 42, wherein the surface-active agent comprises a polyoxyethylene alkyl ether. 44. The composition of claim 33, further comprising an emollient. 45. The composition of claim 44, wherein the emollient is selected from the group consisting of hexylene glycol, propylene glycol, isostearic acid derivatives, isopropyl palmitate, isopropyl isostearate, diisopropyl adipate, diisopropyl dimerate, maleated soybean oil, 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, propylene glycol ricinoleate, isopropyl lanolate, pentaerythrityl tetrastearate, neopentylglycol dicaprylate/dicaprate, isononyl isononanoate, isotridecyl isononanoate, myristyl myristate, triisocetyl citrate, octyl dodecanol, sucrose esters of fatty acids, octyl hydroxystearate and mixtures thereof. 46. The composition of claim 33, wherein the composition is contained within a pressurized container. 47. The composition of claim 33, further comprising an antioxidant. 48. The composition of claim 47, wherein the antioxidant is one or more antioxidant selected from the group consisting of ascorbic acid (vitamin C) and its salts, ascorbyl esters of fatty acids, ascorbic acid derivatives, tocopherol (vitamin E), tocopherol sorbate, tocopherol acetate, other esters of tocopherol, butylated hydroxy benzoic acids and their salts, 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid, gallic acid and its alkyl esters, propyl gallate, uric acid and its salts and alkyl esters, sorbic acid and its salts, lipoic acid, amines, sulfhydryl compounds, dihydroxy fumaric acid and its salts, lycine pidolate, arginine pilolate, nordihydroguaiaretic acid, bioflavonoids, curcumin, lysine, methionine, proline, superoxide dismutase, silymarin, tea extracts, grape skin/seed extracts, melanin, and rosemary extracts. 49. The composition of claim 33, wherein the vitamin comprises a vitamin B3 compound. 50. The composition of claim 49, wherein the composition additionally comprises another vitamin or vitamin derivative. 51. A method of treating or alleviating a hyper proliferative dermal disease, comprising administering topically to a subject having said disorder, a therapeutically effective amount of a foam composition according to claim 17. 52. An foamable pharmaceutical or cosmetic carrier composition, comprising: a polyethylene glycol (PEG) or mixtures thereof, wherein the PEG is present at a concentration of about 70% to about 96.5% by weight of the total composition; at least one gelling agent at a concentration of about 0.1% to about 5% by weight of the total composition; and a surface-active agent at a concentration of about 0.1% to about 10% by weight of the total composition; wherein the composition has less than about 5% final concentration of lower alcohols having up to 5 carbon atoms in their carbon chain skeleton; and wherein if mixed with a propellant in a canister, the composition is capable of being released as a breakable foam which collapses on application of shear force and that does not readily collapse upon dispensing on the skin. 53. The composition of claim 52, wherein the at least one gelling agent is selected from the group consisting of natural polymeric materials, semi-synthetic polymeric materials, synthetic polymeric materials, inorganic gelling agents and mixtures thereof. 54. The composition of claim 52, further comprising: at least one liquefied or compressed gas propellant, at a concentration of about 3% to about 25% by weight of the total composition. 55. The composition of claim 52, wherein the polyethylene glycol (PEG) or mixtures thereof is liquid or is flowable at ambient temperature. 56. The composition of claim 52, wherein the polyethylene glycol (PEG) or mixtures thereof have an average Molecular Weight of about 190 kD to about 10,000 kD. 57. The composition of claim 52, wherein the polyethylene glycol (PEG) is selected from the group consisting of PEG200, PEG300, PEG400, PEG600, PEG 4000,PEG 6000 and PEG 10000and mixtures thereof. 58. The composition of claim 52, wherein the polyethylene glycol (PEG) comprises PEG400. 59. The composition of claim 52, wherein the surface-active agent is a non-ionic surface active agent. 60. The therapeutic composition of claim 52, wherein surface-active agent is selected from the group consisting of sorbitan derivatives, alkoxylated alcohols, hydroxylated derivatives of polymeric silicones, alkylated derivatives of hydroxylated polymeric silicones, glyceryl esters, beeswax derivatives, lecithin, and mixtures thereof. 61. The composition of claim 52, wherein the surface-active agent is selected from the group consisting of polysorbates, polyoxyethylene fatty acid esters, polyoxyethylene alkyl ethers, sucrose esters, partial esters of sorbitol and its anhydrides, mono and diglycerides, isoceteth-20, sodium methyl cocoyl taurate, sodium methyl oleoyl taurate, sodium lauryl sulfate, triethanolamine lauryl sulfate, betaines and mixtures thereof. 62. The composition of claim 61, wherein the surface-active agent comprises a polyoxyethylene alkyl ether. 63. The composition of claim 52, further comprising an emollient. 64. The composition of claim 63, wherein the emollient is selected from the group consisting of hexylene glycol, propylene glycol, isostearic acid derivatives, isopropyl palmitate, isopropyl isostearate, diisopropyl adipate, diisopropyl dimerate, maleated soybean oil, 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, propylene glycol ricinoleate, isopropyl lanolate, pentaerythrityl tetrastearate, neopentylglycol dicaprylate/dicaprate, isononyl isononanoate, isotridecyl isononanoate, myristyl myristate, triisocetyl citrate, octyl dodecanol, sucrose esters of fatty acids, octyl hydroxystearate and mixtures thereof. 65. The composition of claim 52, wherein the composition is contained within a pressurized container. 66. An pharmaceutical or cosmetic foam carrier, comprising: a polyethylene glycol (PEG) or mixtures thereof, wherein the PEG is present at a concentration of about 70% to about 96.5% by weight of the total composition; at least one gelling agent at a concentration of about 0.1% to about 5% by weight of the total composition; a surface-active agent at a concentration of about 0.1% to about 10% by weight of the total composition, at least one liquefied or compressed gas propellant, at a concentration of about 3% to about 25% by weight of the total composition, wherein the composition has less than about 5% final concentration of lower alcohols having up to 5 carbon atoms in their carbon chain skeleton; and wherein the foam breaks on application of shear force. 67. The composition of claim 66, further comprising a therapeutically effective amount of an active agent. 68. The composition of claim 67, wherein the at least one gelling agent is selected from the group consisting of locust bean gum, sodium alginate, sodium caseinate, egg albumin, gelatin agar, carrageenin gum sodium alginate, xanthan gum, quince seed extract, tragacanth gum, starch, chemically modified starches, cellulose ethers, hydroxyethyl cellulose, methyl cellulose, carboxymethyl cellulose, hydroxy propylmethyl cellulose, polyvinylpyrrolidone, polyvinylalcohol, guar gum, hydroxypropyl guar gum, soluble starch, cationic celluloses, cationic guars, carboxyvinyl polymers, polyvinylpyrrolidone, polyvinyl alcohol polyacrylic acid polymers, polymethacrylic acid polymers, polyvinyl acetate polymers, polyvinyl chloride polymers, polyvinylidene chloride polymers and mixtures thereof. 69. An foamable pharmaceutical or cosmetic composition, comprising: a polyethylene glycol (PEG) or mixtures thereof, wherein the PEG is present at a concentration of about 70% to about 96.5% by weight of the total composition; at least one gelling agent at a concentration of about 0.1% to about 5% by weight of the total composition; a surface-active agent at a concentration of about 0.1% to about 10% by weight of the total composition; and a therapeutically effective amount of at least one active agent; wherein the at least one gelling agent is selected from the group consisting of locust bean gum, sodium alginate, sodium caseinate, egg albumin, gelatin agar, carrageenin gum sodium alginate, xanthan gum, quince seed extract, tragacanth gum, starch, chemically modified starches, cellulose ethers, hydroxyethyl cellulose, methyl cellulose, carboxymethyl cellulose, hydroxy propylmethyl cellulose, polyvinylpyrrolidone, polyvinylalcohol, guar gum, hydroxypropyl guar gum, soluble starch, cationic celluloses, cationic guars, carboxyvinyl polymers, polyvinylpyrrolidone, polyvinyl alcohol polyacrylic acid polymers, polymethacrylic acid polymers, polyvinyl acetate polymers, polyvinyl chloride polymers, polyvinylidene chloride polymers and mixtures thereof; wherein the composition has less than about 5% final concentration of lower alcohols having up to 5 carbon atoms in their carbon chain skeleton; and wherein if mixed with a propellant in a canister, the composition is capable of being released as a breakable foam that does not readily collapse upon dispensing on the skin. 70. The foamable pharmaceutical or cosmetic composition of claim 1, further comprising a fatty acid or a fatty alcohol. 71. The foamable pharmaceutical or cosmetic composition of claim 52, further comprising a fatty acid or a fatty alcohol.