MODIFIED RELEASE EMULSIONS FOR APPLICATION TO SKIN OR VAGINAL MUCOSA

• US 20110195944A1
• Filed: 09/21/2009
• Published: 08/11/2011
• Est. Priority Date: 10/08/2008
• Status: Abandoned Application

• Current Assignee: Polichem, SA (Grupo Corporativo Landon SL)
• Original Assignee: Polichem, SA (Grupo Corporativo Landon SL)
• Inventors: Mailland, Federico, Ceriani, Daniela, Mura, Emanuela
• Application Number:
  US12/998,331
• Publication Number:
  US 20110195944A1
• Time in Patent Office: Days
• US Class Current: 514/182
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61K 9/107 Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00
• CPC Class Codes: A61P 15/02 for disorders of the vagina
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/10 Antimycotics
• CPC Class Codes: A61P 33/02 Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis

Abstract

Modified release oil in water emulsions that delivers drugs to a target tissue. The emulsions according to the present invention contain the lipophilic active ingredient completely dissolved into the hydrophobic internal phase stabilised by a polymeric surfactant. The presence of this polymer around the hydrophobic droplets avoids the migration of the active ingredient into the external hydrophilic phase and, consequently, its re-crystallization.

Claims

1-19. -19. (canceled)

20. ) An oil in water emulsion comprising (i) an internal hydrophobic phase in an amount from 1 to 40% by weight, (ii) an external hydrophilic phase in an amount from 60 to 99% by weight, (iii) at least a polymeric surfactant in an amount from 0.50 to 2.50% by weight and (iv) at least a water insoluble active principle in an amount from 0.01 to 25% by weight, and wherein the polymeric surfactant is selected from acrylates/C₁₀-C₃₀ alkyl acrilate crosspolymers and cellulose ethers.

21. ) The oil in water emulsion of claim 20, wherein the internal hydrophobic phase is present in an amount from 5 to 30% by weight.

22. ) The oil in water emulsion of claim 21, wherein the internal hydrophobic phase is present in an amount from 10 to 25% by weight.

23. ) The oil in water emulsion of claim 20, wherein the internal hydrophobic phase comprises benzyl alcohol and 2-octyldodecanol.

24. ) The oil in water emulsion of claim 23, wherein the weight ratio of benzyl alcohol:

2-octyldodecanol ranges from 1;

3 to 1;

13.

25. ) The oil in water emulsion of claim 24, wherein the weight ratio of benzyl alcohol:

2-octyldodecanol ranges from 1;

5 to 1;

11.

26. ) The oil in water emulsion of claim 20, wherein the external hydrophilic phase is present in an amount from 70 to 95% by weight.

27. ) The oil in water emulsion of claim 26, wherein the external hydrophilic phase is present in an amount from 75 to 90% by weight.

28. ) The oil in water emulsion of claim 20, wherein the external hydrophilic phase comprises water in an amount up to 80% by weight.

29. ) The oil in water emulsion of claim 20, wherein the external hydrophilic phase comprises water in an amount up to 60% by weight.

30. ) The oil in water emulsion of claim 20, wherein the external hydrophilic phase comprises lower alkanols, polyhydric alcohols, polyethylene glycols, polypropylene glycols or mixtures thereof.

31. ) The oil in water emulsion of claim 20, wherein the polymeric surfactant is present in an amount from 1.00 to 2.00% by weight.

32. ) The oil in water emulsion of claim 20, wherein the cellulose ether is selected from alkylcellulose, methylcellulose, hydroxyalkylcellulose, and hydroxypropylmethylcellulose.

33. ) The oil in water emulsion of claim 20 which does not comprise neutralizing agents.

34. ) The oil in water emulsion of claim 20, further comprising a bio/mucoadhesive ingredient in an amount from 0.5 to 1.5% by weight.

35. ) The oil in water emulsion of claim 34, wherein the bio/mucoadhesive ingredient is a Carbomer.

36. ) The oil in water emulsion of claim 20, wherein the water insoluble active principle is present in an amount from 0.5 to 15% by weight.

37. ) The oil in water emulsion of claim 36, wherein the water insoluble active principle is present in an amount from 1.0 to 10% by weight.

38. ) The oil in water emulsion of claim 20, wherein the water insoluble active principle is selected from anti-bacterial drugs, anti-fungal drugs, anti-protozoal drugs, anti-inflammatory drugs and hormones.

39. ) The oil in water emulsion of claim 20, wherein the water insoluble active principle is selected from Ciclopirox, Nifuratel, Estradiol, Imiquimod, Acyclovir, Metronidazole and Clotrimazole.

40. ) The oil in water emulsion of claim 20 which is in the form of a lotion, cream or gel.

41. ) The oil in water emulsion of claim 20 which is in a topical form for application to the skin or into the vaginal cavity.

42. ) A method for the treatment of vaginal infections and/or vaginal inflammations comprising administering the oil in water emulsion of claim 20 into the vaginal cavity of a human or animal subject exhibiting vaginal infections and/or vaginal inflammations.

43. ) The method of claim 42, wherein the vaginal infections are of bacterial, fungal or protozoal origin.