IP Library Granted Patent US 10,583,100
Granted Patent B2
US 10,583,100 · App. 16/243,317 · Granted Mar 10, 2020

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 10,583,100
App. No.
16/243,317
Granted
Mar 10, 2020
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 (105)

1. A composition comprising:

i) 0.2-30% by weight of a capsaicinoid,

ii) 0.1-1.5% by weight of hyaluronic acid, wherein said hyaluronic acid comprises a mixture of low molecular weight hyaluronic acid and high molecular weight hyaluronic acid,

iii) 0.5-15% by weight nonionic surfactant, and

iv) lidocaine.

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

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

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

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

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

7. A composition as in claim 6 , wherein said penetration enhancer is selected from the group consisting of DGME or propylene glycol.

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

9. A composition as in claim 8 , wherein said alcohol is ethanol.

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

11. A composition as in claim 10 , wherein said analgesic agent or anesthetic agent is selected from the group consisting of methyl salicylate, camphor, menthol, icilin, eucalyptol and phenol.

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

13. A composition as in claim 12 , wherein said anti-inflammatory agent is selected from the group consisting of a flavonoid, a steroid, and an NSAID.

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

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

16. A kit comprising:

i) a composition as in claim 1 , and

ii) a non occlusive applicator device.

17. A kit as in claim 16 further comprising a cleaning solution for removal of residual capsaicinoid.

18. A composition as in claim 1 comprising 1-20% by weight of capsaicinoid.

19. A composition as in claim 1 , wherein the low molecular weight hyaluronic acid has a molecular weight less than 200 Daltons, and the high molecular weight hyaluronic acid has a molecular weight greater than 800 kDaltons.

20. A composition as in claim 1 , wherein the molecular weight of hyaluronic acid ranges from 3 Daltons to 1,000 kDaltons.

21. A composition comprising:

i) 0.2-30% by weight of capsaicinoid,

ii) 0.1-1.5% by weight of hyaluronic acid,

iii) 0.5-15% by weight nonionic surfactant, and

iv) lidocaine.

22. A composition as in claim 21 , wherein said capsaicinoid is capsaicin.

23. A composition as in claim 21 , wherein said capsaicinoid is trans-capsaicin or nonivamide.

24. A composition as in claim 21 , wherein said nonionic surfactant is PS 80.

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

26. A composition as in claim 21 further comprising a penetration enhancer.

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

28. A composition as in claim 21 further comprising an alcohol.

29. A composition as in claim 28 , wherein said alcohol is ethanol.

30. A composition as in claim 21 further comprising an analgesic or anesthetic agent.

31. A composition as in claim 30 , wherein said analgesic agent or anesthetic agent is selected from the group consisting of methyl salicylate, camphor, menthol, icilin, eucalyptol and phenol.

32. A composition as in claim 21 further comprising an anti-inflammatory agent.

33. A composition as in claim 32 , wherein said anti-inflammatory agent is selected from the group consisting of a flavonoid, a steroid, and an NSAID.

34. A composition as in claim 21 , wherein the composition is a liquid solution.

35. A composition as in claim 21 further comprising phenol.

36. A kit comprising:

i) a composition as in claim 21 , and

ii) a non occlusive applicator device.

37. A kit as in claim 36 further comprising a cleaning solution for removal of residual capsaicinoid.

38. A composition as in claim 21 comprising 1-20% by weight of capsaicinoid.

39. A composition as in claim 21 , wherein the molecular weight of hyaluronic acid ranges from 3 kDaltons to 1,000 kDaltons.

40. A composition comprising:

i) 0.2-30% 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,

iv) 1-40% by weight penetration enhancer, and

v) lidocaine.

41. A composition as in claim 40 , wherein said capsaicinoid is capsaicin.

42. A composition as in claim 40 , wherein said capsaicinoid is trans-capsaicin or nonivamide.

43. A composition as in claim 40 , wherein said hyaluronic acid comprises a mixture of low molecular weight hyaluronic acid and high molecular weight hyaluronic acid.

44. A composition as in claim 43 , wherein the low molecular weight hyaluronic acid has a molecular weight less than 200 kDaltons, and the high molecular weight hyaluronic acid has a molecular weight greater than 800 kDaltons.

45. A composition as in claim 40 , wherein the composition comprises 2-15% by weight PS 80.

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

47. A composition as in claim 40 , wherein said penetration enhancer is selected from the group consisting of DGME or propylene glycol.

48. A composition as in claim 40 further comprising an alcohol.

49. A composition as in claim 48 , wherein said alcohol is ethanol.

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

51. A composition as in claim 50 , wherein said analgesic agent or anesthetic agent is selected from the group consisting of methyl salicylate, camphor, menthol, icilin, eucalyptol and phenol.

52. A composition as in claim 40 further comprising an anti-inflammatory agent.

53. A composition as in claim 52 , 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 40 , wherein the composition is a liquid solution.

55. A composition as in claim 40 further comprising phenol.

56. A kit comprising:

i) a composition as in claim 40 , and

ii) a non occlusive applicator device.

57. A kit as in claim 56 further comprising a cleaning solution for removal of residual capsaicinoid.

58. A composition as in claim 40 comprising 1-20% by weight of capsaicinoid.

59. A composition as in claim 40 , wherein the molecular weight of hyaluronic acid ranges from 3 kDaltons to 1,000 kDaltons.

60. A composition comprising:

i) 0.2-30% 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,

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

v) lidocaine.

61. A composition as in claim 60 , wherein said capsaicinoid is capsaicin.

62. A composition as in claim 60 , wherein said capsaicinoid is trans-capsaicin or nonivamide.

63. A composition as in claim 60 , wherein said hyaluronic acid comprises a mixture of low molecular weight hyaluronic acid and high molecular weight hyaluronic acid.

64. A composition as in claim 63 , wherein the low molecular weight hyaluronic acid has a molecular weight less than 200 kDaltons, and the high molecular weight hyaluronic acid has a molecular weight greater than 800 kDaltons.

65. A composition as in claim 60 , wherein the composition comprises 2-15% by weight PS 80.

66. A composition as in claim 60 , wherein the composition comprises 2-15% by weight polyoxy 40 hydrogenated castor oil.

67. A composition as in claim 60 , wherein said penetration enhancer is selected from the group consisting of DGME or propylene glycol.

68. A composition as in claim 60 further comprising an alcohol.

69. A composition as in claim 68 , wherein said alcohol is ethanol.

70. A composition as in claim 60 further comprising an analgesic or anesthetic agent.

71. A composition as in claim 70 , wherein said analgesic agent or anesthetic agent is selected from the group consisting of methyl salicylate, camphor, menthol, icilin, eucalyptol and phenol.

72. A composition as in claim 60 further comprising an anti-inflammatory agent.

73. A composition as in claim 72 , wherein said anti-inflammatory agent is selected from the group consisting of a flavonoid, a steroid, and an MAID.

74. A composition as in claim 60 , wherein the composition is a liquid solution.

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

76. A kit comprising:

i) a composition as in claim 60 , and

ii) a non occlusive applicator device.

77. A kit as in claim 76 further comprising a cleaning solution for removal of residual capsaicinoid.

78. A composition as in claim 60 comprising 1-20% by weight of capsaicinoid.

79. A composition as in claim 60 , wherein the molecular weight of hyaluronic acid ranges from 3 kDaltons to 1,000 kDaltons.

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 9, 2019
From: BIRBARA, CAROL; BUCKS, DANIEL
To: VIZURI HEALTH SCIENCES LLC
Reel/Frame 047940/0437 →
Continuity (4)
Continuation 15939445 · Mar 29, 2018
Division 14687566 · Apr 15, 2015
Provisional Application 61979905 · Apr 15, 2014
Related Publication 20190247337A1 · Aug 15, 2019