IP Library Granted Patent US 8,889,659
Granted Patent B2
US 8,889,659 · App. 13/609,100 · Granted Nov 18, 2014

Pain relief compositions, manufacture and uses

Inventors: Daniel Bucks (Millbrae, CA); Philip J. Birbara (West Hartford, CT)
Assignee: API Genesis, LLC
A61K31/513A61K31/05A61K47/10A61K9/0014A61K31/35A61K31/045A61K31/618A61K31/60A61K31/125A61K9/08A61K45/06A61K31/165A61K31/352A61K31/351
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Quick Facts
Patent No.
US 8,889,659
App. No.
13/609,100
Granted
Nov 18, 2014
Kind
B2
Abstract

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

Claims (81)

1. A method of treating pain in a mammal suffering from pain comprising topically administering to said mammal a therapeutically effective amount of a liquid composition comprising:

i) 2-30% by weight of a capsaicinoid and

ii) 50-95% by weight of an analgesic agent comprising a) a topical salicylate and b) TRPM8 agonist or a TRPV3 agonist;

wherein said topical salicylate solubilizes said capsaicinoid, and said TRPM8 agonist or said TRPV3 agonist, and reduce the burning and/or stinging sensation or erythema created by the topical administration of the capsaicinoid.

2. The method as in claim 1 wherein said mammal is a human.

3. The method as in claim 1 further comprising administering a nonsteroidal anti-inflammatory agent (NSAID).

4. The method as in claim 3 , wherein the NSAID is administered by a different route than the capsaicinoid composition.

5. The method as in claim 3 , wherein the NSAID is administered orally or parentally.

6. The method as in claim 1 wherein said pain is arthritis pain.

7. The method as in claim 6 wherein said arthritis pain is osteoarthritis or rheumatoid arthritis pain.

8. The method as in claim 1 wherein said pain is nociceptive pain.

9. The method as in claim 1 wherein said pain is neuropathic pain.

10. The method as in claim 1 wherein said pain is selected from the group consisting of post-operative pain, headaches, dental pain, surgical pain, and pain associated with sports injuries.

11. The method as in claim 1 wherein said pain is pain from inflammatory hyperalgesia, vulvodynia, interstitial cystitis, rhinitis, burning mouth syndrome, oral mucositis, herpes, dermatitis, pruritus, tinnitus, or psoriasis.

12. The method as in claim 1 wherein said topically administering comprises administering said composition topically 1-4 times daily.

13. The method as in claim 1 wherein said topically administering comprises administering said composition topically 1-4 times daily for 1-7 days.

14. The method as in claim 1 wherein said topically administering comprises administering said composition with a roller bottle.

15. The method as in claim 1 wherein the composition is a non aqueous liquid.

16. The method as in claim 1 wherein said capsaicinoid is capsaicin.

17. The method as in claim 1 wherein said capsaicinoid is trans-capsaicin.

18. The method as in claim 1 wherein said capsaicinoid is nonivamide.

19. The method as in claim 1 wherein said TRPM8 agonist is menthol, icilin or eucalyptol.

20. The method as in claim 1 wherein the TRPV3 agonist is camphor.

21. The method as in claim 1 wherein said analgesic agent is a topical salicylate, a TRPM8 agonist, and a TRPV3 agonist.

22. The method as in claim 1 wherein said analgesic agent is i) methyl salicylate and ii) menthol or camphor.

23. The method as in claim 1 wherein said analgesic agent is i) methyl salicylate, ii) menthol, and iii) camphor.

24. The method as in claim 1 wherein said analgesic agent is methyl salicylate, menthol and phenol.

25. The method as in claim 1 wherein said analgesic agent is methyl salicylate, camphor, and phenol.

26. The method as in claim 1 wherein said composition further comprises an alcohol.

27. The method as in claim 1 wherein said composition further comprises phenol.

28. The method as in claim 1 wherein said composition further comprises a flavonoid.

29. The method as in claim 1 wherein said composition further comprises an anti-inflammatory agent.

30. The method as in claim 1 wherein said composition further comprises a surfactant.

31. The method as in claim 1 wherein said composition further comprises glycerol.

32. The method as in claim 1 wherein said composition is a gel.

33. The method as in claim 1 wherein said composition comprises:

2-30% by weight of a capsaicinoid,

30-70% by weight methyl salicylate,

1-20% by weight menthol,

1-20% by weight camphor,

wherein the percentage by weight of methyl salicylate, menthol, and camphor is greater than 50% of the composition.

34. The method as in claim 1 wherein said composition comprises:

2-30% by weight of a capsaicin,

30-75% by weight methyl salicylate and ethanol

1-20% by weight menthol,

1-20% by weight camphor,

wherein the percentage by weight of methyl salicylate, menthol, and camphor is greater than 50% of the composition.

35. The method as in claim 33 or 34 wherein said composition further comprises phenol.

36. The method as in claim 1 wherein said composition comprises:

2-30% by weight of a capsaicinoid,

40-75% by weight methyl salicylate

10-25% ethanol,

10-20% by weight menthol, and

10-20% by weight camphor.

37. The method as in claim 1 wherein said composition comprises:

2-30% by weight of a capsaicin,

40-75% by weight methyl salicylate

10-25% ethanol,

10-20% by weight menthol,

10-20% by weight camphor, and

0.5-5% phenol.

38. A method of treating pain in a mammal suffering from pain comprising topically administering to said mammal a liquid composition comprising:

2-30% by weight of a capsaicinoid,

methyl salicylate, and

phenol,

wherein the percentage by weight of the methyl salicylate and phenol is greater than 50% of the composition.

39. The method as in claim 38 wherein said composition comprises:

2-30% by weight of a capsaicinoid,

30-75% by weight methyl salicylate and ethyl alcohol,

and

0.5-5% phenol.

40. A method of treating pain in a mammal suffering from pain comprising topically administering to said mammal a liquid composition comprising:

2-30% by weight of a capsaicinoid, and

70-95% by weight of an analgesic agent comprising a topical salicylate, and wherein said composition does not include turpentine oil.

41. The method as in claim 38 or 40 wherein the capsaicinoid is trans-capsaicin or nonivamide.

42. The method as in claim 38 or 40 wherein the liquid composition is a non-aqueous liquid.

43. The method as in claim 40 , wherein the liquid composition is a non-aqueous liquid solution comprising capsaicin, methyl salicylate, camphor and menthol.

44. The method as claimed in claim 40 , wherein said analgesic agent is a topical salicylate, and a TRPM8 agonist.

45. The method as claimed in claim 44 , wherein said composition further comprises a TRPV3 agonist.

46. The method as claimed in claim 40 , wherein said analgesic agent is i) methyl salicylate and ii) at least one of menthol, camphor and phenol.

47. The method as claimed in claim 38 or 40 , wherein said composition further comprises an alcohol.

Assignments (4)
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 →
CHANGE OF NAME Recorded Jan 20, 2017
From: API GENESIS, LLC
To: VIZURI HEALTH SCIENCES LLC
Reel/Frame 041451/0290 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 25, 2013
From: BUCKS, DANIEL; BIRBARA, PHILIP J.
To: API GENESIS, LLC
Reel/Frame 029873/0347 →
Continuity (3)
Provisional Application 61533120 · Sep 9, 2011
Provisional Application 61642942 · May 4, 2012
Related Publication 20130157985A1 · Jun 20, 2013