USE OF PROTOBERBERINES AS AN ACTIVE SUBSTANCE REGULATING THE PILOSEBACEOUS UNIT

• US 20090269395A1
• Filed: 09/06/2006
• Published: 10/29/2009
• Est. Priority Date: 09/06/2005
• Status: Active Grant

• Current Assignee: Sederma, Co.
• Original Assignee: Sederma, Co.
• Inventors: Lintner, Karl, Mas Chamberlin, Claire
• Granted Patent: US 8,846,019 B2
• Time in Patent Office: Days
• US Class Current: 424/450
• CPC Class Codes: A61K 8/361 Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
• CPC Class Codes: A61K 8/416 Quaternary ammonium compounds A61K8/35 takes precedence
• CPC Class Codes: A61K 8/9789 Magnoliopsida [dicotyledons]
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/08 Antiseborrheics
• CPC Class Codes: A61P 17/10 Anti-acne agents
• CPC Class Codes: A61P 17/14 for baldness or alopecia
• CPC Class Codes: A61Q 7/02 Preparations for inhibiting or slowing hair growth

Abstract

The present invention relates to cosmetic use, by topic application on the skin of at least one protoberberine, with exception of berberine, or a vegetable extract containing it, as an active substance reducing activity of the pilosebaceous unit, preferably inhibiting activity of the pilosebaceous unit. In particular, the invention relates to cosmetic use of at least one protoberberine, with exception of berberine, or a vegetable extract containing it, as an agent reducing, preferably inhibiting the growth of hairs of the face and/or the body, and/or seborrheic activity of the sebaceous glands. The invention also relates to a cosmetic composition comprising in a dermatologically acceptable carrier, at least one protoberberine, with exception of berberine, or a vegetable extract containing protoberberines, as an active substance, which reduces, preferably inhibits the skin'"'"'s pilosebaceous unit activity.

Claims

1. A method for reducing activity of the pilosebaceous unit comprising topically applying a composition comprising an effective amount of at least one protoberberine or at least a vegetable extract containing said at least one protoberberine, and a dermatologically acceptable carrier, wherein said protoberberine is not berberine.

2. The method of claim 1, wherein said protoberberine or said vegetable extract is present in an amount sufficient to reduce activity of growth of hair of hair follicle and/or seborrheic activity of sebaceous glands.

5. The method of claim 1, wherein said protoberberine is obtained by chemical synthesis, or vegetable extraction.

7. The method of claim 1, wherein said protoberberine or said vegetable extract is used as an agent to prevent and/or inhibit seborrheic activity of sebaceous glands.

8. The method of claim 7, wherein said protoberberine is selected from the group consisting of columbamine, pseudocolumbamine, jatrorrhizine and palmatine and their salts and derivatives.

9. The method of claim 7, wherein said protoberberine is obtained by chemical synthesis, or vegetable extraction.

10. The method of claim 7, wherein said vegetable extract is an extract of Eenanthia chloranta.

37. The method of claim 1, wherein said protoberberine is present in an amount from about 0.00001% w/w to about 10% w/w with respect to total weight of the composition.

38. The method of claim 37, wherein said protoberberine is present in an amount from about 0.0001% w/w to about 1% w/w with respect to total weight of the composition.

39. The method of claim 1, wherein said vegetable extract is present in an amount from about 0.0001% w/w to about 20% w/w, with respect to total weight of the composition.

40. The method of claim 39, wherein said vegetable extract is present in an amount from about 0.001% w/w to 5% w/w with respect to total weight of the composition.

3. The method of 1, wherein said protoberberine, or said vegetable extract is used as an agent slowing down and/or inhibiting the growth of hairs of the face and/or the body.

4. The method of claim 3, wherein said protoberberine is selected from the group consisting of chelidonine, palmatine and their salts and derivatives.

6. The method of claim 3, wherein said vegetable extract is selected from the group consisting of an extract of Fibraurea recisa and an extract of Chelidonium majus.

11. A composition comprising, an effective amount of at least one protoberberine or a vegetable extract containing said at least one protoberberine, and a dermatologically acceptable carrier, wherein said protoberberine is not berberine.

12. The composition of claim 11, wherein said protoberberine or said vegetable extract is used as an agent to slow down and/or inhibit growth of hair of the face and/or the body.

13. The composition of claim 12, wherein said protoberberine is selected from the group consisting of chelidonine, palmatine and their salts and derivatives.

14. The composition of claim 11, wherein said protoberberine is obtained by chemical synthesis, or vegetable extraction.

15. The composition of claim 11, wherein said vegetable extract is selected from the group consisting of an extract of Fibraurea recisa and an extract of Chelidonium majus.

16. The composition of claim 12, further comprising microspheres.

18. The composition of claim 11, wherein said protoberberine or a said vegetable extract is used as an agent to prevent and/or inhibit seborrheic activity of sebaceous glands.

19. The composition of claim 18, wherein said vegetable extract is an extract of Enanthia chloranta.

20. The composition of claim 18, further comprising oleanolic acid.

21. The composition of claim 20, wherein said oleanolic acid is present in an amount from about 0.0001% w/w to about 1% w/w with respect to total weight of the composition.

22. The composition of claim 18, further comprising an anti-seborrheic agent.

23. The composition of claim 11, wherein said protoberberine is present in an amount from about 0.00001% w/w to about 10% w/w with respect to total weight of the composition.

24. The composition of claim 11, wherein said vegetable extract is present in an amount from about 0.0001% w/w to about 20% w/w, with respect to total weight of the composition.

25. The composition of claim 11, further comprising at least one additional ingredient.

26. The composition of claim 11, wherein said dermatologically acceptable carrier is an aqueous or hydroalcoholic solution, a water in oil emulsion, an oil in water emulsion, a microemulsion, an aqueous gel, an anhydrous gel, a serum or a vesicle dispersion.

27. The composition of claim 11, wherein said at least one protoberberine or a vegetable extract containing said at least one protoberberine is in the form of solution, dispersion, emulsion, paste, or powder, individually or as a premix, or in vehicles such as macrocapsules, microcapsules, or nanocapsules, macrospheres, microspheres or nanospheres, liposomes, oleosomes or chylomicrons, macroparticles, microparticles, or nanoparticles or macrosponges, microsponges or nanosponges, or adsorbed on organic polymer powders, talcs, bentonites, or other inorganic or organic supports.

28. The composition of claim 11, wherein said composition is formulated in the form of creams, lotions, ointments, milks, gels, emulsions, dispersions, solutions, suspensions, cleansers, foundations, anhydrous preparations (sticks, in particular lipsticks, body and bath oils), shower and bath gels, shampoos and scalp treatment lotions, cream or lotion for care of the skin or hair, sun-screen lotions, milks or creams, artificial suntan lotions, creams or milks, shaving creams or foams, aftershave lotions, make-up, mascaras or nail varnishes, lipsticks, skin “

essences,”

serums, adhesive or absorbent materials, transdermal patches, powders, emollient lotion, emollient milk, emollient cream, sprays, oils for the body and the bath, foundation tint bases, pomade, emulsion, colloid, compact or solid suspension, pencil, sprayable formulation, or brossable.

41. The composition of claim 11 wherein said protoberberine or said vegetable extract is present in an amount sufficient to reduce activity of the pilosebaceous unit of skin.

42. The composition of claim 21, wherein said oleanolic acid is present in an amount from about 0.001% w/w to 0.1% w/w with respect to total weight of the composition.

43. The composition of claim 23, wherein said protoberberine is present in an amount from about 0.0001% w/w to about 1% w/w with respect to total weight of the composition.

44. The composition of claim 24, wherein said vegetable extract is present in an amount from about 0.001% w/w to 5% w/w with respect to total weight of the composition.

17. The composition of 12, further comprising products already known to slow down and/or inhibit growth of hair.

29. (canceled)

30. (canceled)

31. (canceled)

32. A method for reducing the frequency of shaving and/or depilation comprising, applying a composition comprising an active agent selected from the group consisting of palmatine, chelidonine, a vegetable extract of Fibraurea recisa, and a vegetable extract of Chelidonium majus, and a dermatologically acceptable carrier to facial and/or body skin.

33. A method for treating cutaneous disorders associated to a hyperseborrhoea such as brilliant aspect, glossy aspect, the size and the number of pores of oily skins or skins with an oily tendency, comprising applying a composition comprising, at least one extract of Enanthia chloranta and a dermatologically acceptable carrier to facial and/or body skin.

34. (canceled)

35. (canceled)

36. (canceled)

45. A method for reducing activity of the pilosebaceous unit comprising topically applying a composition consisting essentially of an effective amount of at least one protoberberine selected from the group consisting of palmatine, chelidonine, columbamine, psudocolumbamine, jatrorrhizine, stylophorine, diphylline, epichelidonine, oxychelidonine, norchelidonine, berbericinine, hindarine, gindarine, neprotine, yatrorizine, jateorhizine, palmatrubine, dehydrocorydalmine, demethyleneberberine, dehydroscoulerine, stepharine, dehydrodicretamine, calystigine, stylopine, coptisine, epiberberine, canadine, berberrubine and their salts and their derivatives, and a dermatologically acceptable carrier.

46. The method of claim 45, wherein said composition further comprises at least one additional ingredient.

47. A composition consisting essentially of an effective amount of at least one protoberberine selected from the group consisting of palmatine, chelidonine, columbamine, psudocolumbamine, jatrorrhizine, stylophorine, diphylline, epichelidonine, oxychelidonine, norchelidonine, berbericinine, hindarine, gindarine, neprotine, yatrorizine, jateorhizine, palmatrubine, dehydrocorydalmine, demethyleneberberine, dehydroscoulerine, stepharine, dehydrodicretamine, calystigine, stylopine, coptisine, epiberberine, canadine, berberrubine and their salts and their derivatives, and a dermatologically acceptable carrier.

48. The composition of claim 47, further comprising at least one additional ingredient.

49. A method for reducing activity of the pilosebaceous unit comprising topically applying a composition comprising an effective amount of at least one protoberberine selected from the group consisting of palmatine, chelidonine, columbamine, psudocolumbamine, jatrorrhizine, stylophorine, diphylline, epichelidonine, oxychelidonine, norchelidonine, berbericinine, hindarine, gindarine, neprotine, yatrorizine, jateorhizine, palmatrubine, dehydrocorydalmine, demethyleneberberine, dehydroscoulerine, stepharine, dehydrodicretamine, calystigine, stylopine, coptisine, epiberberine, canadine, berberrubine and their salts and their derivatives, and a dermatologically acceptable carrier.