IP Library Granted Patent US 9,956,190
Granted Patent B2
US 9,956,190 · App. 14/687,566 · Granted May 1, 2018

Topical compositions for pain relief, manufacture and use

Inventors: Philip J. Birbara (West Hartford, CT); Daniel Bucks (Millbrae, CA)
Assignee: VIZURI HEALTH SCIENCES LLC
A61K31/165A61K9/0014A61K9/06A61K9/08A61K31/00A61K31/045A61K31/05A61K31/125A61K31/618A61K31/728A61K45/06A61K47/10A61K47/26A61K47/36A61K47/42A61K47/44
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Quick Facts
Patent No.
US 9,956,190
App. No.
14/687,566
Granted
May 1, 2018
Kind
B2
Abstract

The present invention relates to TRPV1 selective agonist compositions including a capsaicinoid, a surfactant and an extended release agent, and to methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions.

Claims (95)

1. A composition comprising:

i) 0.2-20% by weight of capsaicinoid,

ii) 0.1-0.5% by weight of hyaluronic acid, wherein said hyaluronic acid is a mixture of both low molecular weight hyaluronic acid and high molecular weight hyaluronic acid,

iii) 0.5-15% by weight nonionic surfactant,

wherein said composition reduces or eliminates burning and stinging created by said capsaicinoid upon topical administration.

2. A composition comprising:

i) 2-20% by weight of capsaicinoid,

ii) 0.2-0.5% by weight of hyaluronic acid, and

iii) 2-15% by weight nonionic surfactant,

wherein said composition reduces or eliminates burning and stinging created by said capsaicinoid upon topical administration.

3. A composition comprising:

i) 0.20-20% by weight of a capsaicinoid,

ii) 0.1-0.5% by weight hyaluronic acid,

iii) 2-15% by weight PS 80 or polyoxy 40 hydrogenated castor oil, and

iv) 1-40% by weight penetration enhancer,

wherein said composition reduces or eliminates burning and stinging created by said capsaicinoid upon topical administration.

4. A composition comprising:

i) 0.20-20% by weight of a capsaicinoid,

ii) 0.1-1.5% by weight hyaluronic acid,

iii) 2-15% by weight PS 80 or polyoxy 40 hydrogenated castor oil, and

iv) 1-40% by weight of one or more penetration enhancers selected from the group consisting of DGME and propylene glycol,

wherein said composition reduces or eliminates burning and stinging created by said capsaicinoid upon topical administration.

5. A composition as in claim 1 , wherein said capsaicinoid is capsaicin.

6. A composition as in claim 2 , wherein said capsaicinoid is capsaicin.

7. A composition as in claim 3 , wherein said capsaicinoid is capsaicin.

8. A composition as in claim 4 , wherein said capsaicinoid is capsaicin.

9. A composition as in claim 1 , wherein said capsaicinoid is trans-capsaicin or nonivamide.

10. A composition as in claim 2 , wherein said capsaicinoid is trans-capsaicin or nonivamide.

11. A composition as in claim 3 , wherein said capsaicinoid is trans-capsaicin or nonivamide.

12. A composition as in claim 4 , wherein said capsaicinoid is trans-capsaicin or nonivamide.

13. A composition as in claim 2 , wherein said hyaluronic acid is a mixture of both low molecular weight hyaluronic acid and high molecular weight hyaluronic acid.

14. A composition as in claim 3 , wherein said hyaluronic acid is a mixture of both low molecular weight hyaluronic acid and high molecular weight hyaluronic acid.

15. A composition as in claim 4 , wherein said hyaluronic acid is a mixture of both low molecular weight hyaluronic acid and high molecular weight hyaluronic acid.

16. A composition as in claim 1 , wherein said nonionic surfactant is PS 80.

17. A composition as in claim 2 , wherein said nonionic surfactant is PS 80.

18. A composition as in claim 3 , wherein the composition comprises 2-15% by weight PS 80.

19. A composition as in claim 4 , wherein the composition comprises 2-15% by weight PS 80.

20. A composition as in claim 1 , wherein said nonionic surfactant is polyoxy 40 hydrogenated castor oil.

21. A composition as in claim 2 , wherein said nonionic surfactant is polyoxy 40 hydrogenated castor oil.

22. A composition as in claim 3 , wherein the composition comprises 2-15% by weight polyoxy 40 hydrogenated castor oil.

23. A composition as in claim 4 , wherein the composition comprises 2-15% by weight polyoxy 40 hydrogenated castor oil.

24. A composition as in claim 1 further comprising a penetration enhancer.

25. A composition as in claim 2 further comprising a penetration enhancer.

26. A composition as in claim 24 , wherein said penetration enhancer is selected from the group consisting of DGME or propylene glycol.

27. A composition as in claim 25 , wherein said penetration enhancer is selected from the group consisting of DGME or propylene glycol.

28. A composition as in claim 3 , wherein said penetration enhancer is selected from the group consisting of DGME or propylene glycol.

29. A composition as in claim 4 , wherein said penetration enhancer is selected from the group consisting of DGME or propylene glycol.

30. A composition as in claim 1 further comprising an alcohol.

31. A composition as in claim 2 further comprising an alcohol.

32. A composition as in claim 3 further comprising an alcohol.

33. A composition as in claim 4 further comprising an alcohol.

34. A composition as in claim 30 , wherein said alcohol is ethanol.

35. A composition as in claim 31 , wherein said alcohol is ethanol.

36. A composition as in claim 32 , wherein said alcohol is ethanol.

37. A composition as in claim 33 , wherein said alcohol is ethanol.

38. A composition as in claim 1 further comprising an analgesic or anesthetic agent.

39. A composition as in claim 2 further comprising an analgesic or anesthetic agent.

40. A composition as in claim 3 further comprising an analgesic or anesthetic agent.

41. A composition as in claim 4 further comprising an analgesic or anesthetic agent.

42. A composition as in claim 38 , wherein said analgesic agent or anesthetic agent is selected from the group consisting of methyl salicylate, camphor, menthol, icilin, eucalyptol and phenol.

43. A composition as in claim 39 , wherein said analgesic agent or anesthetic agent is selected from the group consisting of methyl salicylate, camphor, menthol, icilin, eucalyptol and phenol.

44. A composition as in claim 40 , wherein said analgesic agent or anesthetic agent is selected from the group consisting of methyl salicylate, camphor, menthol, icilin, eucalyptol and phenol.

45. A composition as in claim 41 , wherein said analgesic agent or anesthetic agent is selected from the group consisting of methyl salicylate, camphor, menthol, icilin, eucalyptol and phenol.

46. A composition as in claim 1 further comprising an anti-inflammatory agent.

47. A composition as in claim 2 further comprising an anti-inflammatory agent.

48. A composition as in claim 3 further comprising an anti-inflammatory agent.

49. A composition as in claim 4 further comprising an anti-inflammatory agent.

50. A composition as in claim 46 , wherein said anti-inflammatory agent is selected from the group consisting of a flavonoid, a steroid, and an NSAID.

51. A composition as in claim 47 , wherein said anti-inflammatory agent is selected from the group consisting of a flavonoid, a steroid, and an NSAID.

52. A composition as in claim 48 , wherein said anti-inflammatory agent is selected from the group consisting of a flavonoid, a steroid, and an NSAID.

53. A composition as in claim 49 , wherein said anti-inflammatory agent is selected from the group consisting of a flavonoid, a steroid, and an NSAID.

54. A composition as in claim 1 , wherein the composition is a liquid solution.

55. A composition as in claim 2 , wherein the composition is a liquid solution.

56. A composition as in claim 3 , wherein the composition is a liquid solution.

57. A composition as in claim 4 , wherein the composition is a liquid solution.

58. A composition as in claim 1 further comprising phenol.

59. A composition as in claim 2 further comprising phenol.

60. A composition as in claim 3 further comprising phenol.

61. A composition as in claim 4 further comprising phenol.

62. A kit comprising:

i) a composition as in claim 1 , and

ii) a non occlusive applicator device.

63. A kit comprising:

i) a composition as in claim 2 , and

ii) a non occlusive applicator device.

64. A kit comprising:

i) a composition as in claim 3 , and

ii) a non occlusive applicator device.

65. A kit comprising:

i) a composition as in claim 4 , and

ii) a non occlusive applicator device.

66. A kit as in claim 62 further comprising a cleaning solution for removal of residual capsaicinoid.

67. A kit as in claim 63 further comprising a cleaning solution for removal of residual capsaicinoid.

68. A kit as in claim 64 further comprising a cleaning solution for removal of residual capsaicinoid.

69. A kit as in claim 65 further comprising a cleaning solution for removal of residual capsaicinoid.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 25, 2025
From: ASTELLAS US LLC
To: JIANGSU AOSAIKANG PHARMACEUTICAL CO., LTD.
Reel/Frame 072378/0590 →
MERGER Recorded Nov 15, 2024
From: PROPELLA THERAPEUTICS, INC.
To: ASTELLAS US LLC
Reel/Frame 069281/0486 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 15, 2020
From: VIZURI HEALTH SCIENCES LLC
To: PROPELLA THERAPEUTICS, INC.
Reel/Frame 052939/0276 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 3, 2017
From: BIRBARA, CAROL; BUCKS, DANIEL
To: VIZURI HEALTH SCIENCES LLC
Reel/Frame 040823/0385 →
Continuity (2)
Provisional Application 61979905 · Apr 15, 2014
Related Publication 20150290151A1 · Oct 15, 2015