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Last Updated: March 28, 2024

Details for Patent: 7,700,076


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Title:Penetrating pharmaceutical foam
Abstract: The invention relates to an alcohol-free cosmetic or pharmaceutical foam composition comprising water, a hydrophobic solvent, a surface-active agent, a gelling agent, an active component selected from the group of urea, hydroxy acid and a therapeutic enhancer and a propellant. The foam further comprises active agents and excipients with therapeutic properties having enhanced skin penetration.
Inventor(s): Tamarkin; Dov (Maccabim, IL), Friedman; Doron (Karmei Yosef, IL), Eini; Meir (Ness Ziona, IL)
Assignee: Foamix, Ltd. (Ness Ziona, IT)
Filing Date:Aug 20, 2004
Application Number:10/922,358
Claims:1. A foamable composition comprising: (i) about 0.1 to 5% by weight of a surface-active agent selected from the group consisting of a polysorbate, a polyoxyethylene fatty acid ester, a polyoxyethylene alkyl ether, a sucrose ester, a partial ester of sorbitol, a partial ester of sorbitol anhydride, sodium methyl cocoyl taurate, sodium methyl oleoyl taurate, sodium lauryl sulfate, triethanolamine lauryl sulfate, a betaine, a mono-, di- or tri-ester of sucrose with food fatty acids (sucrose esters), a monoglyceride, a diglyceride, polyoxyethylene (20) sorbitan monostearate, polyoxyethylene (20) sorbitan monooleate, Myrj 45 (Polyoxyethylene (8) Stearate), Myrj 49 (polyoxyethylene (20) stearate), Myrj 59 (polyoxyethylene (100) stearate), a polyoxyethylene cetyl ether, a polyoxyethylene palmityl ether, a polyethylene oxide hexadecyl ether, Brij 52 (polyoxyethylene (2) cetyl ether), Brij 56 (polyoxyethylene (10) cetyl ether), sorbitan monolaurate, isoceteth-20, cocamidopropyl betaine, and Myrj 52 (polyoxyethylene 40 stearate); (ii) about 0.1 to 5% by weight of a gelling agent; (iii) an active component selected from the group consisting of one or more of urea and a hydroxy acid; (iv) water; and (v) a liquefied or a compressed gas propellant at a concentration of about 3% to about 18% by weight of the total composition; wherein the composition contains no more than 7.5% of methyl alcohol, ethyl alcohol, isopropyl alcohol, butyl alcohol, or mixtures thereof; and wherein the composition forms a breakable foam upon dispensing.

2. The foamable composition of claim 1, further comprising about 5 to about 50% by weight of composition of a liquid, non-volatile hydrophobic solvent, wherein said composition is an oil in water emulsion.

3. The foamable emulsion of claim 2, wherein said emulsion is stable in its pre-dispensed state.

4. The foamable composition of claim 1, wherein said active component consists of about 1% to about 50% urea.

5. The foamable composition of claim 4, wherein said active component consists of about 10% to about 20% urea.

6. The foamable composition of claim 4, wherein said active component consists of about 20% to about 50% urea.

7. The foamable composition of claim 1, wherein said active component consists of about 1% to about 30% hydroxy acid.

8. The foamable composition of claim 7, wherein said active component consists of about 1% to about 10% hydroxy acid.

9. The foamable composition of claim 7, wherein said active component consists of about 10% to about 30% hydroxy acid.

10. The foamable composition of claim 1, wherein said active component consists of a combination of about 1% to about 50% urea and about 1% to about 30% hydroxy acid.

11. An oil in water foamable composition comprising: (i) about 5 to about 50% by weight of composition of a liquid, non-volatile hydrophobic solvent; (ii) about 0.1 to 5% by weight of a surface-active agent selected from the group consisting of a polysorbate, a polyoxyethylene fatty acid ester, a polyoxyethylene alkyl ether, a sucrose ester, a partial ester of sorbitol, a partial ester of sorbitol anhydride, sodium methyl cocoyl taurate, sodium methyl oleoyl taurate, sodium lauryl sulfate, triethanolamine lauryl sulfate, a betaine, a mono-, di- or tri-ester of sucrose with food fatty acids (sucrose esters), a monoglyceride, a diglyceride, polyoxyethylene (20) sorbitan monostearate, polyoxyethylene (20) sorbitan monooleate, Myrj 45 (Polyoxyethylene (8) Stearate), Myrj 49 (polyoxyethylene (20) stearate), Myrj 59 (polyoxyethylene (100) stearate), a polyoxyethylene cetyl ether, a polyoxyethylene palmityl ether, a polyethylene oxide hexadecyl ether, Brij 52 (polyoxyethylene (2) cetyl ether), Brij 56 (polyoxyethylene (10) cetyl ether), sorbitan monolaurate, isoceteth-20, cocamidopropyl betaine, and Myri 52 (polyoxyethylene 40 stearate); (iii) about 0.1 to 5% by weight of a gelling agent; (iv) a therapeutic enhancer selected from the group consisting of propylene glycol, butylene glycols, glycerol, pentaerythritol, sorbitol, mannitol, oligosaccharides, dimethyl isosorbide, monooleate of ethoxylated glycerides having about 8 to 10 ethylene oxide units, polyethylene glycol 200-600, transcutol, glycofurol and cyclodextrins; and a liquefied or compressed gas propellant at a concentration of about 3% to about 18% by weight of the total composition; wherein the composition contains no more than 7.5% of methyl alcohol, ethyl alcohol, isopropyl alcohol, butyl alcohol, or mixtures thereof; and wherein said composition is a stable emulsion in its pre-dispensed state and forms a breakable foam upon dispensing.

12. The foamable composition of claim 11, wherein the composition comprises about 1% to about 10% of the therapeutic enhancer.

13. The foamable composition of claim 11, wherein the composition comprises about 10% to about 30% of the therapeutic enhancer.

14. The foamable composition of claim 1, 2, 4, 7 or 11, further comprising a therapeutically effective concentration of at least one active agent.

15. The foamable composition of claim 2 or 11, wherein said hydrophobic solvent comprises about 5-10% by weight of the composition.

16. The foamable composition of claim 2 or 11, wherein said hydrophobic solvent comprises about 10-20% by weight of the composition.

17. The foamable composition of claim 2 or 11, wherein said hydrophobic solvent comprises about 20-50% by weight of the composition.

18. The foamable composition of claim 2 or 11, wherein said hydrophobic solvent comprises a mixture of mineral oil and an emollient in a ratio between 2:8 and 8:2 on a weight basis.

19. The foamable composition of claim 1 or 11, wherein said 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 and a zwitterionic surface active agent.

20. The foamable composition of claim 1 or 11, wherein said surface-active agent is a mixture of a non ionic surface active agent and an ionic surface active agent in a 1:1 to 20:1 ratio.

21. The foamable composition of claim 1 or 11, wherein said surface-active agent is a non ionic surface-active agent.

22. The foamable composition of claim 1 or 11, wherein the surface-active agent has HLB value of more than 9.

23. The foamable composition of claim 1 or 11, wherein the gelling agent comprises an amphiphilic copolymer.

24. The foamable composition of claim 2 or 11, wherein the hydrophobic solvent is selected from the group consisting of vegetable oil, marine oil, mineral oil, emollient, silicone oil, plant-derived therapeutic oil and mixture thereof at any proportion.

25. The foamable composition of claim 2 or 11, wherein the ratio between the surface active agent and the hydrophobic solvent is between about 1:8 and about 1:16.

26. The foamable composition of claim 2 or 11, wherein the ratio between the surface active agent and the hydrophobic solvent is between about 1:16 and about 1:32.

27. The foamable composition of claim 14, wherein said active agent is antibacterial.

28. The foamable composition of claim 27, wherein said active agent is selected from the group consisting of chloramphenicol, tetracyclines, synthetic and semi-synthetic penicillins, beta-lactams, quinolones, fluoroquinolnes, macrolide antibiotics, peptide antibiotics, cyclosporines, Metronidazole, free radical generating agents, iodine, chlorohexidine, benzoyl peroxide, hydrogen peroxide and any combination thereof at a therapeutically effective concentration.

29. The foamable composition of claim 14, wherein said active agent is antifungal.

30. The foamable composition of claim 29, wherein said active agent is selected from the group of azoles, diazoles, triazoles, miconazole, fluconazole, ketoconazole, clotrimazole, itraconazole griseofulvin, ciclopirox, amorolfine, terbinafine, amphotericin B, potassium iodide, flucytosine (5FC) and any combination thereof at a therapeutically effective concentration.

31. The foamable composition of claim 14, wherein said active agent is antiviral.

32. The foamable composition of claim 31, wherein said active agent is selected from the group consisting of vidarabine, acyclovir, gancyclovir, nucleoside-analog reverse transcriptase inhibitors, AZT (zidovudine), ddI (didanosine), ddC (zalcitabine), d4T (stavudine), 3TC (lamivudine), non-nucleoside reverse transcriptase inhibitors, nevirapine, delavirdine, protease Inhibitors, saquinavir, ritonavir, indinavir, nelfinavir, ribavirin, amantadine, rimantadine and interferon.

33. The foamable composition of claim 14, wherein said active agent is selected from the group consisting of an anti-inflammatory agent and an anti-allergic agent.

34. The foamable composition of claim 33, wherein said active agent is selected from the group comprising corticosteroids, non-steroidal antiinflammatory drugs, anti- histamines, immunomodulating agents, immunosuppressants and any combination thereof at a therapeutically effective concentration.

35. The foamable composition of claim 33 wherein the anti-inflammatory agent is selected from the group comprising clobetasol proprionate, halobetasol proprionate, betamethasone diproprionate, betamethasone valerate, fluocinolone acetonide, halcinonide, betamethasone valerate, fluocinolone acetonide, hydrocortisone valerate, triamcinolone acetonide, hydrocortisone, oxicams, piroxicam, isoxicam, tenoxicam, sudoxicam, salicylates, aspirin, disalcid, benorylate, trilisate, safapryn, solprin, diflunisal, fendosal, diclofenac, fenclofenac, indomethacin, sulindac, tolmetin, isoxepac, furofenac, tiopinac, zidometacin, acematacin, fentiazac, zomepirac, clindanac, oxepinac, felbinac, ketorolac, fenamates, mefenamic, meclofenamic, flufenamic, niflumic, tolfenamic acids, propionic acid derivatives, ibuprofen, naproxen, benoxaprofen, flurbiprofen, ketoprofen, fenoprofen, fenbufen, indopropfen, pirprofen, carprofen, oxaprozin, pranoprofen, miroprofen, tioxaprofen, suprofen, alminoprofen, tiaprofenic, pyrazoles, phenylbutazone, oxyphenbutazone, feprazone, azapropazone and trimethazone, and any combinations thereof.

36. The foamable composition of claim 33 wherein the antiallergic agent is selected from the group comprising diphenhydramine, doxepin, phrilamine maleate, chlorpheniramine and tripelennamine, phenothiazines, promethazine hydrochloride, dimethindene maleate and any combination thereof at a therapeutically effective concentration.

37. The foamable composition of claim 14, wherein said active agent is an anticancer agent.

38. The foamable composition of claim 14, wherein the active agent is a photodynamic therapy agent.

39. The foamable composition of claim 14, wherein said active agent is a local anesthetic.

40. The foamable composition of claim 39, wherein said local anesthetic is selected from the group comprising benzocaine, lidocaine, bupivacaine, chlorprocaine, dibucaine, etidocaine, mepivacaine, tetracaine, dyclonine, hexylcaine, procaine, cocaine, ketamine, pramoxine, phenol

41. The foamable composition of claim 14, wherein the active agent is a retinoid.

42. The foamable composition of claim 41, wherein said retinoid is selected from the group comprising retinol, retinal, all trans retinoic acid, etretinate, actiretin, isotretinoin, adapalene and tazarotene.

43. The foamable composition of claim 14, wherein said active agent is an anti-wrinkle agent.

44. The foamable composition of claim 14, wherein said active agent is selected from the group comprising ascorbic acid and its salts, ascorbyl esters of fatty acids, magnesium ascorbyl phosphate, sodium ascorbyl phosphate, ascorbyl sorbate, tocopherol, 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, N,N-diethylhydroxylamine, amino-guanidine, sulfhydryl compounds, glutathione, dihydroxy fumaric acid and its salts, lycine pidolate, arginine pilolate, nordihydroguaiaretic acid, bioflavonoids, curcumin, lysine, methionine, proline, superoxide dismutase, silymarin, tea extract, grape skin/seed extract, melanin, and rosemary extract.

45. The foamable composition of claim 14, wherein said active agent is a self-tanning agent.

46. The foamable composition of claim 14, wherein said active agent is an anti-acne active agent.

47. The foamable composition of claim 46, wherein said active agent is selected from the group comprising resorcinol, sulfur, salicylic acid, salicylate salts, benzoyl peroxide, retinoic acid, isotretinoin, adapalene, tazarotene, azelaic acid and azelaic acid derivatives, antibiotic agents, erythromycin and clindamycin and zinc salts and complexes.

48. The foamable composition of claim 14, wherein said active agent is a skin whitening agents.

49. The foamable composition of claim 14, wherein said active agent is intended for transdermal delivery.

50. The foamable composition of claim 1 or 11, further comprising a foam adjuvant.

51. The foamable composition of claim 14, wherein, upon foaming of the foamable composition, an alcohol-free foam is obtained having a specific gravity of between about 0.01 g/mL and about 0.1 g/mL.

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