IP Library Granted Patent US 10,821,088
Granted Patent B2
US 10,821,088 · App. 14/482,930 · Granted Nov 3, 2020

Pain relief compositions, manufacture and uses

Inventors: Daniel Bucks (Millbrae, CA); Philip J. Birbara (West Hartford, CT)
Assignee: PROPELLA THERAPEUTICS, INC.
A61K31/165A61K9/0014A61K9/06A61K9/08A61K31/045A61K31/05A61K31/125A61K31/196A61K31/35A61K31/351A61K31/352A61K31/513A61K31/60A61K31/618A61K45/06A61K47/10
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Quick Facts
Patent No.
US 10,821,088
App. No.
14/482,930
Granted
Nov 3, 2020
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 (74)

1. A 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, capable of solubilizing said capsaicinoid,

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,

wherein the composition is in a form selected the group consisting of sprays, gels, emulsions, and mixtures thereof, and

wherein said TRPM8 agonist is icilin or eucalyptol.

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

3. The composition as claimed in claim 1 , wherein said composition is a gel.

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 eucalyptol.

7. The composition as claimed in claim 2 , 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 composition comprising:

2-30% by weight of a capsaicinoid,

icilin or eucalyptol,

methyl salicylate and ethyl alcohol, and

phenol,

wherein said methyl salicylate and ethyl alcohol solubilize said capsaicinoid,

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

wherein the composition is in a form selected the group consisting of sprays, gels, emulsions, and mixtures thereof.

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 composition comprising:

2-30% by weight of a capsaicinoid,

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

icilin or eucalyptol,

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, wherein said composition does not include turpentine oil, and

wherein the composition is in a form selected the group consisting of sprays, gels, emulsions, and mixtures thereof.

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 gel.

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 gel 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 Jun 27, 2016
From: BUCKS, DANIEL; BIRBARA, PHILIP J.
To: API GENESIS, LLC
Reel/Frame 039011/0474 →
Continuity (4)
Division 13609100 · Sep 10, 2012
Provisional Application 61533120 · Sep 9, 2011
Provisional Application 61642942 · May 4, 2012
Related Publication 20160106690A1 · Apr 21, 2016