US2021100759A1PendingUtilityA1

Pain relief compositions, manufacture and uses

71
Assignee: PROPELLA THERAPEUTICS INCPriority: Sep 9, 2011Filed: Oct 12, 2020Published: Apr 8, 2021
Est. expirySep 9, 2031(~5.1 yrs left)· nominal 20-yr term from priority
Inventors:Daniel BucksPhilip J. Birbara
A61K 31/352A61K 31/05A61K 47/10A61K 31/35A61K 31/513A61K 9/0014A61K 31/045A61K 45/06A61P 19/02A61P 11/02A61P 17/00A61K 31/618A61K 31/125A61P 43/00A61P 17/04A61K 31/351A61K 9/08A61P 25/06A61P 13/10A61K 9/06A61P 15/00A61K 31/60A61P 1/02A61K 31/165A61P 17/06A61P 31/22A61K 31/196A61P 29/00A61P 25/04
71
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Claims

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

exact text as granted — not AI-modified
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 or a TRPV3 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, and   wherein the composition is in a form selected the group consisting of sprays, gels, emulsions, and mixtures thereof.   
     
     
         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 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 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 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,   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, 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, 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.

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