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Capsaicin vs. pain neurotransmitters - Calling all chile alchemists


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#1 DWB

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Posted 12 February 2017 - 10:44 PM

One of the reasons I keep a pepper buzz going is to keep my endorphins kicking to help control chronic pain. I think it may be a good idea to control it from the outside too and use the capsaicin topically. Although I've never been able to accomplish it with commercially available capsaicin pain relief products, the science says if you do it right, you can deplete the nerves in the target area of the type of slow moving neurotransmitter responsible for sending the chronic pain signals.  I've started  looking for a better way than use of the impotent commercial products that are available.

 

Here's what I've learned so far. I did skin testing with the hottest products I have in the house. First I used 1 million SHU Ghost Cap. That's pretty much imperceptible when painted on top of my forearm. I gave it a half hour before moving up the ladder. Next step was two drops of 1.5 million SHU Pure Evil capsaicin spread on the inside of my forearm. I did get a little tingle from that but nothing notable. After another half hour I moved up to the biggest gun I have and painted a 3x3" patch of custom built 5 million SHU Ghost Cap on my inner forearm. That indeed gave me a stronger tingle but was definitely a non-event. I washed after an hour and the tingle remained for another 15 minutes or so.

 

All this established is my skin can tolerate a whole lot of very hot stuff without the slightest bit of discomfort or blistering or peeling like flesh from a zombie. I guess it also establishes I can utilize just about anything I can make and anything I make will certainly be a whole lot stronger than the store-bought junk I've tried over the years.

 

The next thing I learned is I may be able to make me some stuff out of my scorpireaper powder but I wonder about the "transfer rate". I started cold soaking ½ tsp of my powder in 9 ml of 190 proof Everclear this afternoon. It didn't take long for it to turn a very pretty red color and then after a few hours, develop about a millimeter of oil that floats on the top. I didn't try the oil but I pulled a drop of the red alcohol from beneath the capsaicin layer and it was pretty spicy. About wallyworld habañero hot, I'd say.

 

My idea of a perfect product is a spray that evaporates quickly and doesn't leave me an oily mess to contaminate my surroundings with highly potent capsaicin residue. Another plus to a product like this is my wife could spritz me and be done. There would be no pepper accidents that would certainly occur if I asked her to rub a capsaicin cream or oil into my back every day.

 

Now to ask for the advice, experience and insight from any who know or have ideas. I need a carrier. I wonder about the  transferability of compounds like this ethanol tincture. I can certainly make it much, much more potent than the little bit I have brewing at the moment but will it be effective as a transdermal application? It would evaporate very quickly and wouldn't leave a mess but how well would it work at getting the active ingredient to the target?

 

What level of heat should I try to create in a brew like this?

 

Another carrier option is the opposite extreme of blending pepper extract into a phospholipid deficient oil like emu oil. This stuff pulls medications through the skin like grease through a goose but I wonder if it's really a good thing to do that with capsaicin.

 

Thanks for sharing any of the productive things you may know.



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#2 Hybrid Mode 01

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Posted 13 February 2017 - 09:30 AM

     I've had the best relief using capsaicin linament along with some other muscle rub like Ben Gay. I don't know if the salicylate or camphor/menthol in the muscle rub helps the capsaicin permeate the skin better, or makes nerves more sensitive to capsaicin or maybe it's just the extra massaging that helps get the capsaicin working. But I seem to get a better "burn" out of the capsaicin that way.

     If I were you and needed some serious capsaicin penetration, I would put on some nitrile gloves (or ask your wift to) and try mixing some extract with body lotion. Then massage it into the problem area until your skin is dry. That might help work the stuff through your skin better. See how that works and then experiment with other mixes like muscle rub or emu oil.

     I know that the methyl salicylate in muscle rub not only feels good on painful spots, but it's also basically topical aspirin. It soaks in and relieves inflammation and actually dulls pain. Maybe there's something synergistic going on between the capsaicin and salicylate that makes them work better.



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#3 DWB

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Posted 13 February 2017 - 02:41 PM

Wow! Word of the day... "linament". Thanks for that! I searched on capsaicin linament and found an organic family farm product made of grain-free alcohol, distilled water and habañero peppers and seeds. No percentages or strength info offered and no idea if it's worth a hoot but it appears somebody preceded my thinking on a basic recipe if not method. Their stuff is served up with an eyedropper rather than a spray.

 

This has been going on for 13 years so I've tried many different bengay, biofreeze, aspercream types of products. I've also tried numerous capsaicin products. None of them do much at all.

 

I don't know the "strength" of all the capsaicin creams, gels and roll-ons I've tried but a good friend suggested the commercial stuff may be too weak to suit my needs. The way my mind works with a suggestion like this is "go nuclear".  Indeed, the only capsaicin product I can find in the junk bin now is a 0.025% roll-on. I don't know how that translates into SHU but a tongue test produces a very unremarkable result.

 

If capsaicin is the magic ingredient, it seems like more is better and I'm thinking due to my skin tests, I'll have a very difficult time going too high.



#4 b3rnd

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Posted 13 February 2017 - 03:52 PM

I don't know what kind of chronic pain you are experiencing. But if it is joint pain for example, it depends on which part of the point is sending the pain signals. Nociceptors in joints are located in 'the joint capsule, ligaments and proximal tendons, bone, periosteum, articular fat pad and around blood vessels', so which receptors you want to desensitize, and how deep the capsaicin needs to penetrate to work is dependant on where exactly your pain comes from.

 

Capsaicin binds to the the TRPV1-receptor, or capsaicin receptor. This receptor signals the body about scalding hot temperatures (above 42 degrees C). By overstimulating these receptors with prolonged exposure to capsaicin, nerve desensitization occurs. Capsaicin is lipophilic, which means that it is very soluble in fat. This also means that it is hydrophobic, and doesn't mix with water very well. The protective layer of your skin is called the epidermis, and to maximize the effect of any topically applied substance, it needs to be able to penetrate this layer. Edited to add: The epidermis secretes sebum, a fatty substance that waterproofs and lubricates the skin. This stuff is why oil-based substances are absorbed better then water-based ones.

 

Alcohol evaporates too fast to be of use for you, I think. I like the emu oil idea actually, because oil penetrates the skin better. That's why practically all skin creams are fatty. And because capsaicin is hydrophobic, and blood is water-based , you don't have to worry about it entering your blood stream (that would probably hurt....) The method that gave the best results according to studies was an skin patch (à la nicotine patch) with '8% capsaicin', called Qutenza. You can find that study here. I couldn't find exactly what that percentage refers to, but I'm guessing they are using pure capsaicin.

 

I would go as hot and oily as can be. Maybe mix some in with a face or body cream to test it out (those are already made to be easily absorbed). I would leave the pure cap for what it is, that stuff is nasty. The body will still react with various level of inflammations to high amounts of capsaicin, even though there was nothing really there.


Edited by b3rnd, 13 February 2017 - 04:43 PM.

It's a little chilly.


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Posted 13 February 2017 - 04:09 PM

     DWB, I think the .025% roll on product you mentioned is the same one I use. Cura-Heat is the name. I agree that it's pretty weak, but repeated application seems to do the trick with me. I have hand and wrist pain and find that covering the linament with gloves (that I wear for work) also boosts the effect.

     I think b3rnd is definitely on the right track as far as finding ways to get the capsaicin to penetrate to the deeper tissues where the problem originates.

     My hand pain is a result of pinched nerves in my upper back. Since the pain doesn't originate deep inside a joint or other hard to access area, maybe that's why I see a better response to topical capsaicin. Maybe the warmth and counterirritant burning of the capsaicin doesn't necessarily stop the nerves from firing, it just makes it feel better overall.



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#6 DWB

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Posted 13 February 2017 - 06:41 PM

Oh my goodness. Some interesting stuff here. I've not seen this concept of "Defunctionalization" before. This merits some serious study while I continue preparing my stuff.  The first quick scan of the prescribing info for Qutenza hasn't yet revealed the carrier used in the patch. Maybe there isn't one.  Thanks for the links b3rnd. Great stuff that gives me a lot to consider.

 

The capsaicin product I have here now is Arth-Rx. Basically a little bit of cap with a vasodilator. HM01, I'm glad treating the hand and wrist helps the pain.  Funny how that works even though the source of the pain is more than an arm's length away. The source of my pain is 5 crushed vertebrae. T1 through T5 right between my shoulder blades. There's no question about the epicenter of my pain. I imagine the source of that pain is deep and I'm sure the deeper I can drive the capsaicin, the better it will work.

 

The emu oil is one of the few things that passes right through all skin layers and carries everything with it. Bad juju to put it on something like a fresh case of poison ivy. It can drive the poison systemic. I think another one that can go through all skin layers is DMSO but I have no experience with that. Emu oil I keep on hand.

 

I do wish to start out with a simple spray but will undoubtedly quickly progress from here. I'm liking this new thing  about defunctionalization treatment. If treatment with high strength capsaicin can last for 12 weeks, I'm all on board for learning all about it.  Although the patch prescribing info discusses concurrent treatment with opioids to treat pain during and after the treatment, I'm thinking that's a little over the top. I don't know what 8% capsaicin consists of (other than 179 mg of capsaicin per patch) but it can't be more brutal than painting 5 million SHU hot sauce on sensitive skin and leaving it there for an hour. As I said, that was a non-event. I just looked a little funny with a huge red and oily patch painted on my arm.

 

Regardless,  I reckon I can mix something up and lay still for an hour.  That will work well for my wife too. She doesn't mind helping me with any of this but I don't want her to get burned which is more likely with daily hands-on treatments. When I first spoke to her about this new project, she jumped right in and suggested making a poultice and painting it on. My friend suggested something similar about putting on a bunch of superhot and covering it or taping plastic wrap over it for a while.

 

It's damn good to have smart people around me. Thanks y'all.



#7 salsalady

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Posted 13 February 2017 - 08:27 PM

If that one product is 8% capsaicin by volume, that would equate to about 1,280,000 SHU.  Capsaicinoids are basically a PPM type equation.

 

I'd discourage using a spray, as that will put capsaicin airborn and could be really irritating to you and your Lovely.  It would also have the potential to get on surrounding surfaces and come back to bite'cha later.

 

If you want, I can mix up an oil based solution for you.  Sounds like emu oil would be a good place to start.  I've mixed some with coconut oil for someone else to use in some kind of topical lotion.  Never heard back how it worked.  I can make a 2mil or 3mil SHU concentration level. 

 

The Pure Evil you have is alcohol and water based.  From the discussion above, it sounds like an oil based product would work better.  I also have some oil based extracts....I wonder how that would work when mixed with a carrier oil like emu?  Small side effect would be that your skin would be bright orange-red for a while.  :lol:

 

Let me know if it's something you are interested in.

 

SL

 


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#8 SmokenFire

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Posted 13 February 2017 - 08:49 PM

Wow.  This is such an awesome community.  So very proud to be a small piece in this puzzle.  :D


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#9 DWB

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Posted 13 February 2017 - 09:03 PM

Thanks for jumping in salsalady. I had a feeling you know quite a bit about this topic. Here are the specs for the patch. I haven't done the math but it doesn't seem like much of a stretch to duplicate and even improve. As far as I've learned so far, there is no carrier for the (synthetic) capsaicin other than the silicon adhesive. Certainly no emu oil to drive it home..

 

This is a newborn idea for me but I'm thinking I'd do a lot better to get the a.i. from you rather than try to make it myself. This will offer much better control of the project. I can handle a red, oily patch. Not much difference between  a 3" x 3" patch on my arm and a patch on my back that probably shoutd be about 6" x 8". to adequately cover my damage. That should be pretty close to the size of the Qutenza patch at 14 cm x 20 cm

 
Qutenza (capsaicin) 8% patch contains capsaicin in a localized dermal delivery system. The capsaicin in Qutenza is a synthetic equivalent of the naturally occurring compound found in chili peppers. Capsaicin is soluble in alcohol, acetone, and ethyl acetate and very slightly soluble in water.
Qutenza is a single-use patch stored in a foil pouch. Each Qutenza patch is 14 cm x 20 cm
(280 cm²) and consists of a polyester backing film coated with a drug containing silicone adhesive mixture, and covered with a removable polyester release liner.
The backing film is imprinted with “capsaicin 8%”. Each Qutenza patch contains a total of 179 mg of capsaicin (8% in adhesive, 80 mg per gram of adhesive) or 640 micrograms (mcg) of capsaicin per square cm of patch. The empirical formula is C18 H27 NO3, with a molecular weight of 305.42. The chemical compound capsaicin [(E)-8-methyl-N-vanillyl-6-nonenamide] is an activating
ligand for transient receptor potential vanilloid 1 receptor (TRPV1) and it has the following structure:


#10 JUR-Z-Devil

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Posted 13 February 2017 - 09:58 PM

nice conversation started... ill read through when i get over this flu... all sounds very intriguing... hope ya find relief in all this knowledge... plenty of smart people in this thread to bounce ideas off of... looking forward to catching up... ttys brother..

 

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#11 DWB

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Posted 13 February 2017 - 10:45 PM

Hey SL, how many milligrams of capsaicin in a milliliter of say 6 million SHU extract? Half the milligrams per milliliter for 3 million SHU?

 

How does the viscosity of 6 million SHU extract compare to that of drops? Is the capsaicin itself identical between the oleoresin and the drops?



#12 salsalady

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Posted 14 February 2017 - 12:50 AM

Think of it as a PPM (parts per million) equation.  As I understand it, Wilbur Scoville realized that sugar water lessened the sensation of heat from hot chiles and devised the sugar dilution method of determining the heat (or Pungency) of peppers.  Correlated that to the 0-16,000,000 scale that we know to be the Scoville Scale.  HPLC testing reads all the capsaicinoid compounds in (whatever) the sample is and correlates that back to the Scoville scale.

 

 

http://thehotpepper....d-other-things/

 

 

What is capsaicin?

"Capsaicin" is one of many capsaicinoid compounds found in chilies.  There are over 20 different capsaicinoid compounds in most chiles.  The different capsaicinoids react differently in the mouth and body causing the mouth burn and the body endorphin rush.  Different chiles have different amounts of these different compounds, which is why some chiles will hit hard and fast in the mouth, others will hit the gut, others will have the slow creeping burn.

 

All these different capsaicinoids have been erroneously lumped together under the general heading of 'capsaicin' because that one capsaicinoid is the most prominent one in most chiles.  Google is your friend for more information on capsaicinoids.

 

______________________

 

The viscosity of the extracts are 2-3x thicker than Pure Evil drops of comparable SHUs.  The room temp 12mil extract is very thick, thicker than peanut butter, maybe like automotive grease consistency.  The 13 mil Pure Evil drops are like a thick cooking oil at medium to cool room temps, and when at warm room temp or heated under a bit of hot water, they are a thin oil consistency. 

 

 

 

From there, you have to look at what the capsaicin is mixed with.  Same thing for hot sauces.  You could put 1 Reaper Pepper in 2 gallons of sauce, and technically you could sell it as a "REAPER SAUCE".  The creams and WhatNot have all been commercially developed for ....yea...you guessed it....the GenPop....who have a tolerance of, like 0.003 out of 16mil.  Since most people (like 90% of the population) think that jalapenos are hot, the same would apply to commercially prepared lotions.  Manufacturers are producing for the 95% of consumers. 

 

Just my thoughts and opinions, Take it with a big grain of Himalayan Pink Salt.  :)

SL
 

 

edit- and yes, capsaicinoids are capsaicinoids.  The chemical compounds are what they are, it's the carrier that makes all the difference.  12 mil extract will have the same amount of capsacinoid compounds as a 12mil Pure Evil.  The taste, viscosity and smell are completely different, but at the end of the day, they both have the same pungency.   

 

 

re-edit- I have not played around very much with using the 16mil cap powder in oil based solutions as there has not been a need/request for it. 

 


Edited by salsalady, 14 February 2017 - 01:04 AM.

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#13 DWB

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Posted 14 February 2017 - 01:48 AM

I need to quantify the statement below. Without knowing how many milligrams of capsaicin(oids) exist in a certain volume at a certain certain SHU level, I have no way to begin.

 

"Each Qutenza patch contains a total of 179 mg of capsaicin (8% in adhesive, 80 mg per gram of adhesive) or 640 micrograms (mcg) of capsaicin per square cm of patch."

 

 



#14 JUR-Z-Devil

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Posted 14 February 2017 - 01:54 AM

i think what he is asking is how do you measure the dilution... as in, equal parts 16 million shu crystals (say 1 gram) mixed with equal parts alcohol (would you weigh the alcohol to 1 gram or would it be by volume to cut the 16 mill to 8 mill)

 

because1 mil of oil will weigh more than one mil of everclear... so the dilutions wouldnt be equal if done by weight but crystals also contain airspace between them so volume isnt very accurate... i think he means how do you compare one ingredient to the next to accurately predict the shu outcome...


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#15 DWB

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Posted 14 February 2017 - 11:25 AM

Here's a good example of what I need to know for the purpose of making comparative calculations. How many milligrams of capsaicin(oids) would there be in one milliliter of the 3 million SHU oil based solution you can mix up for me?

 

Here's why I need to know. if I dissolve 100 mg of pure capsaicin crystals in a milliliter of solvent, the concentration will be 100 milligrams per milliliter. If I want to duplicate the dosing of the pharmaceutical patch,  I simply need to dissolve 179 mg of capsaicin crystals into enough solution to allow thin coverage of a 280² cm area. Since capsaicin is soluble in oil and the ideal carrier may be emu oil, all I have to do is weigh the amount of emu oil required to paint a thin layer on the area of my back that I want to treat and mix accordingly. SHU is pretty much irrelevant but is a point of reference.

 

Hmmm, I think maybe the path of least resistance may be using pure capsaicin crystals.



#16 DWB

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Posted 14 February 2017 - 02:26 PM

Patch math. Depending on which of their figures you give priority, it looks they blend 179.2 mg of synthetic capsaicin into 2240 mg of adhesive.



#17 salsalady

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Posted 14 February 2017 - 08:30 PM

I need to quantify the statement below. Without knowing how many milligrams of capsaicin(oids) exist in a certain volume at a certain certain SHU level, I have no way to begin.
 
"Each Qutenza patch contains a total of 179 mg of capsaicin (8% in adhesive, 80 mg per gram of adhesive) or 640 micrograms (mcg) of capsaicin per square cm of patch."
 
 


I guess you could look at the above like- they make a mixture using 1790 mg of capsaicin which is enough for ten patches, so each patch gets 179 mg. I am not totally undersdtanding what they are saying. That might be a place to start.
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#18 salsalady

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Posted 14 February 2017 - 08:34 PM

Fwiw, synthetic capsaicin is about 20% the price of real capsaicin at 95% purity. What I use is 100% pure and about 3-4x the price of 95%.
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#19 DWB

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Posted 14 February 2017 - 09:28 PM


If you want, I can mix up an oil based solution for you.  Sounds like emu oil would be a good place to start.  I've mixed some with coconut oil for someone else to use in some kind of topical lotion.  Never heard back how it worked.  I can make a 2mil or 3mil SHU concentration level. 

 

I think the 3 mil SHU oil based solution you can mix up for me will work nicely. If I mix it 50-50 with emu oil or coconut oil it will be 1.5 million SHU or 9.375% yes?



#20 salsalady

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Posted 14 February 2017 - 09:51 PM

Yes. Where do I get emu oil?
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