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Old 07-20-2003, 12:22 PM   #1
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Topical anti-inflamatory

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Old 07-20-2003, 04:10 PM   #2
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Old 07-20-2003, 04:29 PM   #3
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Old 07-20-2003, 05:59 PM   #4
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Just mixed up my first batch of a homebrew transdermal joint gel. The formula for the carrier is:

50% Aloe (99.3 % Pure)
20% Water
10% PG
10% Peppermint Oil
10% IPM
Carbomer 934 and Triethanolamine to desired consistency

The solutes comprise of:

44.4% MSM
16.6% Glucosamine Sulfate
16.6% N-Acetyl Glucosamine
22.2% Chondroitin Sulfate

Glucosamine Sulfate and Chondroitin sulfate have relatively poor bioavailability (26% and 13% respectively). I chose the ingredients in the carrier to provide a balance between delivering the solutes to the targeted deep joint tissue and increasing plasma blood solute concentrations by bypassing first pass metabolism. In addition to having poor bioavailability, glucosamine sulfate also has a very short half life in the bloodstream. In most of the clinical cases I found, blood concentrations (after oral administration) peaked between 1.1 and 2 hours after ingestion and then fell off quickly. While there is 50% less glucosamine in n-acetyl glucosamine as compared to glucosamine sulfate, the half life is much longer. Studies have shown that after oral administration of n-acetyl glucosamine, blood plasma levels remained high as long as 48 hours after ingestion. N-acetyl glucosamine has another unique benefit in that like chondroitin it can inhibit the release of the leukocyte-elastase enzyme, thus reducing cartilage degradation.

I chose to include MSM as a solute due to its natural anti-inflammatory properties. MSM is a derivative of DMSO. I found that my joints “ached” much less during my last couple homebrew cycles. I can only assume it was the addition of the DMSO that helped.

My goal was to create a carrier that would allow me to apply approximately 1000 mg’s of MSM, 750 mg’s of glucosamine and 500 mg’s of chondroitin a day. At a concentration of 50 mg’s/mL, this would equate to a volume of 45 mL/day. If applied twice per day, this volume was not practical. There simply is not enough skin around the joints I needed to target. Thus, I mixed the solutes in the carrier at 100 mg’s/mL. While this concentration may seem high, I found that MSM, glucosamine and chondroitin were all very soluble. In addition, after application, there is no sign of the solutes on the skin. They appear to have absorbed completely.

At 31 years old, my joints have been hacked. Between professional Kick-Boxing and Skiing, my shoulder, elbow and knees are always aching. I underwent ACL (Knee) replacement surgery in May and I have been unable to lift more than a 10 RM weight on bench due to my shoulder injuries. I am constantly looking for something that may help. I will report the results.

BTW, my sinuses are also very clear from the peppermint oil.





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12-16-2002 at 12:44 AM

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Sounds awesome bro. Im curious as to why you chose the msm over just straight dmso. I thought the dmso had equal anti-inflammatory action as its derivative msm. If this is so the questoin becomes does the msm have the skin penetrating power of dmso? Would like to know your throught process and reasoning....





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12-16-2002 at 06:03 AM

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Bow I remember you talking about this awhile back. Glad to see your finally going through with it. Please keep us updated on how it goes. The formular is great as well as the dosages for the active ingredients.

TMack: While DMSO is a great carrier/solvent to use to get hormones into the bloodstream. With this particular homebrew blood stream delivery is not what we are aiming for. MSM is a natural derivative of DMSO and just as DMSO it posses great joint pain relieving property just without the penetration properties. So it should work well.












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12-16-2002 at 06:35 PM

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I see what your saying diablo, but even with the ingredients listed its going to get absorbed by the blood stream no? Furthermore, wouldnt one want this to actually happen. Obviously the solvents arent going to be able to get to the joints any other way without going through the bloodstream. Site application would make it relevant as the joints closest to the application site would get first crack at the ingredients. (Kind of the like the principle behind site injections) So wouldnt you want to use dmso to make sure your gettin as much of the solvent in there as possible? I might be slightly confused, please elaborate on your former point if my arguments do not make sense. Thanks bro.





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12-16-2002 at 08:33 PM

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BDC, when you going to start selling this as a premixed product?





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12-16-2002 at 09:28 PM

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do we know how well it works yet?










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12-18-2002 at 04:12 PM

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quote:
Originally posted by TMack40
I see what your saying diablo, but even with the ingredients listed its going to get absorbed by the blood stream no? Furthermore, wouldnt one want this to actually happen. Obviously the solvents arent going to be able to get to the joints any other way without going through the bloodstream. Site application would make it relevant as the joints closest to the application site would get first crack at the ingredients. (Kind of the like the principle behind site injections) So wouldnt you want to use dmso to make sure your gettin as much of the solvent in there as possible? I might be slightly confused, please elaborate on your former point if my arguments do not make sense. Thanks bro.


I want the ingredients to be absorbed in the bloodstream, but slowly and gradually. My rationale for this is twofold. First, I want a time released formula. Second, glucosamine has a very short half life in the blood. If we can deliver the glucosamine in a time released fashion, we will extend the steady state flux of glucosamine in your circulatory system. Hence the addition of the 10% IPM. However, first I want to deliver the actives to the deep tissue I am trying to target. IPM is not nearly as strong of a penetration enhancer as DMSO. We know that a combination of aloe and menthol is effective at penetrating and holding solutes in deep tissue. The IPM should then slowly deliver the solutes from the deep tissue to the circulatory system. DMSO would speed the solutes directly past the targeted joint tissue. This is the compromise between delivering to deep tissue and delivering to blood that I spoke of when designing the carrier.


quote:
Originally posted by BigBenn
do we know how well it works yet?


In terms of short term joint pain, it works great. I noticed that if I apply to problematic joints immediately before working out, the typical discomfort is reduced significantly. I can not yet speculate regarding the long term effects as I have only been applying the gel for a couple of days now.





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12-18-2002 at 06:48 PM

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That def makes a lot of sense. Youve really done your reasearch on this bro, good job! Ive had an achy shoulder for years; i may just have to brew up a batch. Keep us posted on results. Thanks and good luck!





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12-18-2002 at 06:52 PM

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This is a great thread. Please post results ASAP and let us know. I too would like to give this a go.





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12-18-2002 at 08:57 PM

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my hat off to you bow. great and informative thread. i also would like to hear the results, and possibly make me a bottle for my pains and joints.





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04-20-2003 at 03:41 PM

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It’s been a few months now since I started this experiment, so I figured I would post the results.

I have continued with the protocol described above since December with one exception. I tapered back the dosage to about 15 ml/day (just a matter of convenience).

My shoulder feels great. The range of motion is back to 100%. There are still some movements that are bothersome, but nowhere near the discomfort I had prior to December. The best part is that I can actually perform a 1RM max on bench again without screaming like a banshee. My knee also feels very good, although I don’t consider it that great of a metric being that it has been cut on.

I have not taken any other OTC or prescription meds since beginning the experiment. I truly believe that this transdermal does work very well for damaged joints. I went from barely being able to perform a 10RM bench to a 1RM bench without pain in less than four months. Considering that I dealt with severe joint discomfort for over a year, this was a dramatic improvement.

I’d be curious to see if anyone else with joint pain experiences the same results.





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06-26-2003 at 01:31 AM

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I was thinking of making a homebrew transdermal for joints but I want to incorporate emu oil and menthol in the gel. Any ideas?????










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06-26-2003 at 02:30 AM

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quote:
Originally posted by he_hate_me
I was thinking of making a homebrew transdermal for joints but I want to incorporate emu oil and menthol in the gel. Any ideas?????



Peppermint oil contains 50-78% methanol. The active ingredient in emu oil is oleic acid. Oleic acid is known as being effective at disrupting the stratum corneum lipid membrane. Thus, oleic acid should also work well as a shallow tissue penetration enhancer. This should work well. Keep us posted on your results.





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06-26-2003 at 03:37 AM

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quote:
Originally posted by bow



Peppermint oil contains 50-78% methanol. The active ingredient in emu oil is oleic acid. Oleic acid is known as being effective at disrupting the stratum corneum lipid membrane. Thus, oleic acid should also work well as a shallow tissue penetration enhancer. This should work well. Keep us posted on your results.


The reason I was thinking of using menthol insetead of peppermint oil was cuz I want menthol to be atleast 12-13% of the gel and emu oil to be about 7%. So how would you suggest I should tweak the other ingredients to get the desired homebrew.










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07-01-2003 at 07:09 PM

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I would run 60% aloe and 20% water for the remainder of the solvent solution. Mix your solutes at 100 mg’s/ml. Go for approx 1000 mg’s of MSM, 750 mg’s of glucosamine and 500 mg’s of chondroitin a day.





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07-01-2003 at 07:43 PM

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quote:
Originally posted by bow
I would run 60% aloe and 20% water for the remainder of the solvent solution. Mix your solutes at 100 mg’s/ml. Go for approx 1000 mg’s of MSM, 750 mg’s of glucosamine and 500 mg’s of chondroitin a day.


So no IPM or PG?










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07-01-2003 at 07:51 PM

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quote:
Originally posted by he_hate_me


So no IPM or PG?


Not with the emu oil. The purpose of the IPM is to disrupt the stratum corneum and provide slow but stead absorption to the circulatory system. Too high of a concentration of penetration enhancers and you are going to speed the solutes right past the target tissue. The emu oil (via the oleic acid) should be ample. I might increase the concentration of the emu oil by 5-10% and decrease the aloe %.





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07-01-2003 at 08:18 PM

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Originally posted by bow


Not with the emu oil. The purpose of the IPM is to disrupt the stratum corneum and provide slow but stead absorption to the circulatory system. Too high of a concentration of penetration enhancers and you are going to speed the solutes right past the target tissue. The emu oil (via the oleic acid) should be ample. I might increase the concentration of the emu oil by 5-10% and decrease the aloe %.


ok sounds good, but how about PG as it will used for consistency.










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07-05-2003 at 07:04 AM

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This is what I came up with for a glucosamine sterile solution, but I may have to try a transdermal without the menthol ( can't tolerate it), but anyway no responses to my post as of yet. This is what I came up with posted below, but the emu oil may be an option if no replies to my post. I just wish I could get some comments in reference to my post.


Ok, This is the best I can figure a recipe in development for a sterile glucosamine solution.

Step 1
Use Cottonseed Oil, Peg 400, BA 3%, likely BB, and powder.

First boil water in sauce pan to use at 212 F degrees for 10 minutes. Empty water out of pan, and add 52 ml oil to sauce pan. At slow heat, bring oil to 212 F degrees, maintain for 5 minutes. Perhaps use syringe and transfer oil to pre-sterilized vial using sterial filter on the syringe and set aside. This should be sterile oil in the vial if I understand correctly.

Step 2
In a open 100 ml vial, put in 15 grams of glucosamine powder, and add 2 ml or 200 cc of BA to the powder, add 6 ml of Peg 400, and likely some BB. Transfer some warm oil if need be. Close the vial with a lid, and roll/ shake vial to attempt to dissolve the powder. If powder dissolves, filter through a coffee filter once or twice, and place inside a new open vial.

Step 3
Take the dissolved powder mix, and draw up into a syringe, and sterial filter the powder solution into the 100 ml vial containing the oil using a syringe and a sterile filter on the syringe.


Now if I understand all that I have read, I should have a sterile solution of 60ml inside a pre-sterilized 100 ml vial.
=============================================


For those that know how to do this process, did I end up with a sterile soultion? If not, what did i do wrong, or what do you think may be a potential problem with the solution?


Regards,
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07-07-2003 at 03:31 PM

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Sorry CNN. Wish I could help, but my conversion to injectible knowledge is limited. You might try Dazed.





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Re: homebrew transdermal joint gel multiple post quote:

07-10-2003 at 08:39 AM

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[quote]Originally posted by bow
[b]Just mixed up my first batch of a homebrew transdermal joint gel. The formula for the carrier is:

50% Aloe (99.3 % Pure)
20% Water
10% PG
10% Peppermint Oil
10% IPM
Carbomer 934 and Triethanolamine to desired consistency

The solutes comprise of:
44.4% MSM
16.6% Glucosamine Sulfate
16.6% N-Acetyl Glucosamine
22.2% Chondroitin Sulfate
==================================================
==========================================

HI Bow,


I found your recipe for a transdermal joint gel to peek my interest
I too suffer from joint pains, and have tried Glucosamine, Chrondroiton, and MSM orally, and I believe there is some extra relief. However, they don't seem to set with my intestines very well, so I have been looking for an alternative way to get the ingrediants in my system hopefully without intestinal disturbance.

Your recipe was interesting, but for me menthol does not set well with my skin even at low concentrations, so I picked up on the other person's suggestion of Emu oil, and came up with the following after reading all the posts, and was curious as to what your opinion was of the following recipe.

52% Aloe
25% Water
20& Emu oil
3% DSMO
Carbomer 934 and Triethanolamine to desired consistency

USE MSM, Glucosamine & Chondroitin at a desired range similar to yours.

Although I would like some local effect, I have multiple joint trouble, and would like the ingrediants to get absorbed into the blood stream as well, and take on a systemic effect. However, something that might concern me would be too much absorbtion of some ingrediants into the blood stream, mainly the Carbomer 934 and Triethanolamine.

What are your thoughts, or suggestions you might have regarding this recipe? Might I be better off trying to do it as a liquid rather than a gel and drop the Carbomer 934 and Triethanolamine? Thanks for any suggestions.


Regards,
On1Mission










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07-10-2003 at 06:44 PM

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I am personally skeptical of using DMSO as a penetration enhancer for a local delivery. DMSO it not only effective at disrupting the lipid membrane (like Oleic Acid and IPM) but it also interacts with the intercellular proteins. My concern is that any amount of DMSO is going to speed the actives past the target tissue. Will it still work effectively for systematic delivery, probably. But I would skip it. You will get the desired systematic effect and local delivery without the addition of DMSO. Otherwise, your choice of solvents and ratios look good.

Don’t worry about the carbomer or triethanolamine. They are both non-toxic. However, I have read studies on pubmed showing that they may hinder absorption slightly. This would follow being that absorption is a function of viscosity, and the purpose of those two ingredients is to increase viscosity. So, if you don’t mind the inconvenience of a liquid, it may actually be more effective.

Good luck.





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07-12-2003 at 04:58 AM

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Bow,

Thanks for the comments. I appreciate it.


Reagrds,
On1Mission










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07-15-2003 at 10:46 AM

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Say Bow,

Would you mind sharing what brand(s) of the following products you used, and perhaps where you bought them? There are so many brands out there claiming to have the best. I finally settled on Cardinal Nutrition for the MSM. You can PM if you wish. By the way, how many days does your transdermal gel last?


MSM
Glucosamine Sulfate
N-Acetyl Glucosamine
Chondroitin Sulfate
Aloe vera


Regards,
On1Mission










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07-15-2003 at 01:31 PM

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quote:
Originally posted by bow
It’s been a few months now since I started this experiment, so I figured I would post the results.

I have continued with the protocol described above since December with one exception. I tapered back the dosage to about 15 ml/day (just a matter of convenience).

My shoulder feels great. The range of motion is back to 100%. There are still some movements that are bothersome, but nowhere near the discomfort I had prior to December. The best part is that I can actually perform a 1RM max on bench again without screaming like a banshee. My knee also feels very good, although I don’t consider it that great of a metric being that it has been cut on.

I have not taken any other OTC or prescription meds since beginning the experiment. I truly believe that this transdermal does work very well for damaged joints. I went from barely being able to perform a 10RM bench to a 1RM bench without pain in less than four months. Considering that I dealt with severe joint discomfort for over a year, this was a dramatic improvement.

I’d be curious to see if anyone else with joint pain experiences the same results.


Awesome! I'm glad your pain has subsided. I'm definitely going to have to try this formula. Thanks alot for the info man, it's appreciated...










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07-19-2003 at 10:42 PM

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quote:
Originally posted by On1Mission
Say Bow,

Would you mind sharing what brand(s) of the following products you used, and perhaps where you bought them? There are so many brands out there claiming to have the best. I finally settled on Cardinal Nutrition for the MSM. You can PM if you wish. By the way, how many days does your transdermal gel last?


MSM
Glucosamine Sulfate
N-Acetyl Glucosamine
Chondroitin Sulfate
Aloe vera




The Glucosamine Sulfate, MSM, N-Acetyl Glucosamine and Chondroitin are all from Beyond A Century. I got the Aloe Vera Gell at a local health food store, its is manufactured by Herbal Authority.

A 240 mL batch lasts about 10-15 days.





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