IP Library Granted Patent US 8,802,736
Granted Patent B2
US 8,802,736 · App. 13/797,494 · Granted Aug 12, 2014

High concentration capsaicinoid pain relief composition

Inventors: Daniel Bucks (Millbrae, CA); Philip J. Birbara (West Hartford, CT)
Assignee: API Genesis, LLC
A61K31/513A61K9/08A61K31/165A61K31/125A61K45/06A61K47/10A61K31/05A61K31/351A61K31/352A61K9/0014A61K31/60A61K31/618A61K31/35A61K31/045
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Quick Facts
Patent No.
US 8,802,736
App. No.
13/797,494
Granted
Aug 12, 2014
Kind
B2
Abstract

The present invention relates to a composition useful for pain relief. The composition is high concentration capsaicinoid topical composition comprising an analgesic agent that eliminates or reduces the burning or stinging sensation or erythema of the capsaicinoid.

Claims (69)

1. 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) a TRPM8 agonist or a TRPV3 agonist,

wherein said topical salicylate solubilizes said capsaicinoid and said TRPM8 agonist or said TRPV3 agonist, and

wherein said composition comprises an amount of analgesic agent sufficient to eliminate or reduce the burning or stinging sensation or erythema created by the topical administration of the capsaicinoid to a mammal.

2. The composition as claimed in claim 1 , wherein said analgesic agent comprises a topical salicylate, a TRPM8 agonist, and a TRPV3 agonist.

3. The composition as claimed in claim 1 , wherein the composition is a non aqueous liquid solution.

4. The composition as claimed in claim 1 , wherein said capsaicinoid is capsaicin.

5. The composition as claimed in claim 1 , wherein said capsaicinoid is trans-capsaicin or nonivamide.

6. The composition as claimed in claim 1 , wherein said TRPM8 agonist is menthol, icilin or eucalyptol.

7. The composition as claimed in claim 1 , wherein the TRPV3 agonist is camphor.

8. The composition as claimed in claim 1 , wherein said analgesic agent comprises i) methyl salicylate and ii) at least one of menthol, camphor and phenol.

9. The composition as claimed in claim 1 , wherein said composition further comprises an alcohol.

10. The composition as claimed 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, and

1-20% by weight camphor,

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

11. The composition as claimed in claim 1 , wherein said composition comprises:

2-30% by weight of a capsaicinoid,

30-75% by weight methyl salicylate and ethanol,

1-20% by weight menthol, and

1-20% by weight camphor,

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

12. The composition as claimed 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.

13. The composition as claimed in claim 1 , wherein said composition comprises:

2-30% by weight of 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.

14. The composition as claimed in claim 11 , wherein said composition further comprises glycerol.

15. The composition as claimed in claim 14 , wherein said composition is a gel.

16. The composition as claimed in claim 1 , wherein said composition further comprises an anti-inflammatory agent.

17. The composition as claimed in claim 1 , wherein said composition further comprises a surfactant.

18. The composition as claimed in claim 1 , wherein said composition further comprises an NSAID.

19. The composition as claimed in claim 18 , wherein the NSAID is selected from the group consisting of aspirin, ibuprofen, naproxen, ketoprofen, and diclofenac.

20. The composition as claimed in claim 1 , wherein said composition further comprises an odor reducing agent.

21. The composition as claimed in claim 1 , wherein said composition further comprises phenol.

22. The composition as claimed in claim 11 , wherein said composition further comprises phenol.

23. A liquid composition comprising:

2-30% by weight of a capsaicinoid,

methyl salicylate and ethyl alcohol, and

phenol,

wherein said methyl salicylate and ethyl alcohol solubilize said capsaicinoid, and

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

24. The composition as claimed in claim 23 , wherein said composition comprises:

2-30% by weight of a capsaicinoid compound,

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

and

0.5-5% phenol.

25. A liquid composition comprising:

2-30% by weight of a capsaicinoid, and

70-95% by weight of an analgesic agent comprising a topical salicylate,

wherein said topical salicylate solubilizes said capsaicinoid, and

wherein said composition comprises an amount of analgesic agent sufficient to eliminate or reduce the burning or stinging sensation or erythema created by the topical administration of the capsaicinoid to a mammal, and wherein said composition does not include turpentine oil.

26. The composition as claimed in claim 25 , wherein said analgesic agent comprises a topical salicylate and a TRPM8 agonist.

27. The composition as claimed in claim 25 , wherein the composition is a non aqueous liquid solution.

28. The composition as claimed in claim 25 , wherein said analgesic agent is i) methyl salicylate and ii) at least one of menthol, camphor and phenol.

29. The composition as claimed in claim 25 , wherein said composition further comprises an alcohol.

30. The composition as claimed in claim 26 wherein said composition further comprises a TPRV3 agonist.

31. The composition as claimed in claim 27 , wherein said non aqueous liquid solution comprises capsaicin, methyl salicylate, camphor and menthol.

Assignments (5)
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 →
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 Mar 12, 2013
From: BUCKS, DANIEL; BIRBARA, PHILIP J.
To: API GENESIS, LLC
Reel/Frame 030006/0421 →
Continuity (4)
Continuation 13609100 · Sep 10, 2012
Provisional Application 61533120 · Sep 9, 2011
Provisional Application 61642942 · May 4, 2012
Related Publication 20130252925A1 · Sep 26, 2013