Topical analgesic pain relief formulations, manufacture and methods of use thereof

Abstract

This disclosure relates to natural topical and analgesic pain relief and anti-inflammation compositions and methods to reduce pain and inflammation. This disclosure also relates to the use of cannabinoid compounds in hydrophilic compositions comprised of synthetic and natural plant extract compounds that are multifunctional TRPM8 ion channel agonists, TRPA1 and TRPV1 ion channel antagonists, CGRP antagonists, COX-2 inhibitors and CB1 and CB2 antagonists. In particular, this disclosure relates to a topical analgesic composition comprising at least one synthetic or natural plant extract TRPM8 agonist, at least one synthetic or natural plant extract is a TRPA1 antagonist, and fixed plant seed oil containing Omega-3 fatty acids TRPV1 antagonists and a carrier.

1 . An analgesic composition comprising at least one TRPM8 agonist, TRPA1 antagonist, one or more natural or synthetically derived cannabinoid compounds, optionally at least one fixed plant seed oil TRPV1 antagonist containing Omega-3 fatty acids, optionally methyl salicylate, and optionally a carrier. 
     
     
         2 . The analgesic composition of  claim 1  in which the cannabinoid compound is selected from one or more of the group consisting of cannabidiol, cannabidivarin and delta9-tetrahydrocannabinbol. 
     
     
         3 . The analgesic composition of  claim 1  in which the cannabinoid compounds are extracted from  Cannabis saliva, Cannabis indica , and  Cannabis ruderalis  plants materials using one or more extraction processes including solvent and supercritical carbon dioxide extraction. 
     
     
         4 . The analgesic composition of  claim 1  where the TRPM8 agonist is a synthetic compound and/or the TRPA1 antagonist is a synthetic compound. 
     
     
         5 . The analgesic composition of  claim 1  in which the TRPM8 agonist is 1-menthol. 
     
     
         6 . The analgesic composition of  claim 1  in which 1-menthol is from a synthetic source or derived from one or more essential oils selected from the group consisting of:  Mentha  spp., including  Mentha piperita ; and  Mentha  arvensis. 
     
     
         7 . The analgesic composition of  claim 6  in which the TRPM8 agonist is menthone, 1,8-cineole, borneol, linalool, geraniol, or isopulegol. 
     
     
         8 . A method of relieving pains in mammals by administering an analgesic composition comprising at least one TRPM8 agonist, at least one TRPA1 antagonist, at least one natural or synthetically derived cannabinoid compound, optionally at least one fixed plant seed oil TRPV1 antagonist containing Omega-3 fatty acids, optionally methyl salicylate, and optionally a carrier. 
     
     
         9 . The method of  claim 8  in which the cannabinoid compound is selected from the group consisting of cannabidiol, cannabidivarin and delta9-tetrahydrocannabinbol. 
     
     
         10 . The method of  claim 8  in which the cannabinoid compounds are extracted from  Cannabis saliva, Cannabis indica , and  Cannabis ruderalis  plants materials using one or more extraction processes including solvent and supercritical carbon dioxide extraction. 
     
     
         11 . The method of  claim 8  in which the TRPM8 agonist is 1-menthol. 
     
     
         12 . The method of  claim 11  in which the source of 1-menthol is from a synthetic source or selected from one or more essential oils selected from the group consisting of:  Mentha  spp., including  Mentha piperita ; and  Mentha  arvensis. 
     
     
         13 . The method of  claim 8  in which the TRPM8 agonist is menthone, 1,8-cineole, borneol, linalool, geraniol, or isopulegol. 
     
     
         14 . The method of  claim 8  where the TRPM8 agonist is a synthetic compound and/or the TRPA1 antagonist is a synthetic compound. 
     
     
         15 . The method of  claim 8  in which the TRPA1 antagonist is 1,8-cineole from a synthetic source or derived from natural sources comprising one or more essential oils selected from the group consisting of:  Eucalyptus  spp., including  Eucalyptus polybractea; Eucalyptus globulus, Eucalyptus radiate, Eucalyptus camaldulensis, Eucalyptus smithii , and  Eucalyptus globulus; Rosmarinus  spp. including  Rosmarinus officinalis ; and  Salvia lavandulifolia ; or the TRPA1 antagonist is borneol from a synthetic source or derived from one or more of the essential oils selected from the group consisting of:  Thymus satureioides  and  Cinnamomum burmanni.    
     
     
         16 . The analgesic composition of  claim 1  in which the TRPA1 antagonist is 1,8-cineole from a synthetic source or derived from natural sources comprising one or more essential oils selected from the group consisting of:  Eucalyptus  spp., including  Eucalyptus polybractea; Eucalyptus globulus, Eucalyptus radiate, Eucalyptus camaldulensis, Eucalyptus smithii , and  Eucalyptus globulus; Rosmarinus  spp., including  Rosmarinus officinalis ; and  Salvia lavandulifolia.    
     
     
         17 . The analgesic composition of  claim 1  in which the TRPA1 antagonist is borneol from a synthetic source or derived from one or more of the essential oils selected from the group consisting of:  Thymus satureioides  and  Cinnamomum burmanni.    
     
     
         18 . The analgesic composition of  claim 1  in which the carrier is selected from the group consisting of a paste, a liquid, a gel, a wax, a cream, a suspension, a film, a stick, a patch, a solid, a powder, nanoparticles, and granules; and in which the carrier comprises one or more additives or excipients selected from the group consisting of odorants, deodorants, diluents, fillers, binders, adhesives, disintegrants, lubricants, anti-adhesives glidents, coloring agents, sweeteners, coating agents, plasticizers, wetting agents, and buffers. 
     
     
         19 . The method of  claim 8  in which the carrier is selected from the group consisting of a paste, a liquid, a gel, a wax, a cream, a suspension, a film, a stick, a patch, a solid, a powder, nanoparticles, and granules; and in which the carrier comprises one or more additives and excipients selected from the group consisting of odorants, deodorants, diluents, fillers, binders, adhesives, disintegrants, lubricants, anti-adhesives, glidents, coloring agents, sweeteners, coating agents, plasticizers, wetting agents and buffers. 
     
     
         20 . The method of  claim 8  wherein the composition is administered orally or topically.