Heated Transdermals

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    Heated Transdermals


    I just stumbled across something interesting. I am having difficulty getting my carbomer to dissolve in the transdermal mix. Taking some advise from another post, I tried heating the mix. I didn’t work. The carbomer is still clumping. Pissed off, I dumped the mix back into my pump bottle and applied my morning dosage. It was very warm (I would guess about 150 deg F). It appeared that that my homebrew solution absorbed in about half the normal time! This based on typical drying time and the oiliness (from the PG) after applying the solution. After observing this, I did some research and found a number of studies (including one with testosterone) that supports the theory that heat dramatically increases the flux of topically applied drugs. Apparently heat increases the kinetic energy of the drug molecules and increases the solubility of the drug in formulation. Heat also dilates the skin pathways, increasing the movement of the drug though the skin.

    So, the question becomes how to conveniently heat our homebrew solutions prior to application. I have seen warmers for shaving cream, coffee cups, etc. I was thinking about some type of electrical warming container that could be plugged in just prior to showering. You get out of the shower and apply your warmed homebrew.

    What do you think?


    Here are some studies.
    ……………………………………………………………………………… ……………………
    A pilot study assessing the impact of heat on the transdermal delivery of testosterone.
    Shomaker TS, Zhang J, Ashburn MA.

    University of Hawaii, John A. Burns School of Medicine, 1960 East-West Road, Honolulu, HI 96822-2319, USA.

    This study evaluated the effect of locally applied heat on the transdermal delivery of testosterone. Six healthy adult volunteers were tested three times while receiving a 5 mg androgen patch, the same patch with a heat-generating patch, and no patch at all over 12 hours. Statistically significant differences in mean maximum serum testosterone concentration values were seen. Heat plus patch resulted in a mean maximum serum testosterone concentration of 939 ng/dl versus 635 ng/dl (patch only) and 425 ng/dl (no patch). (Heat + patch vs. no patch: p < 0.001; heat + patch vs. patch: p < 0.001; patch vs. no patch: p = 0.003.) The area under the curve of plasma testosterone concentration versus time values were means of 4114 ng/dl.h versus 1985 ng/dl.h for the patch-only group (p = 0.001). The use of heat improved absorption of transdermal testosterone and decreased time to peak serum testosterone concentrations, resulting in a statistically significant difference in mean maximum serum testosterone concentrations compared with the use of the patch without heat.

    ……………………………………………………………………………… …………………
    Heat-Enhanced Transdermal Drug Delivery: A Survey Paper
    Wade Hull, MS
    ….Heat is known to increase the kinetic energy of both the drug molecules and the proteins, lipids, and carbohydrates in the cell membrane. Heating prior to or during topical application of a drug will dilate penetration pathways in the skin, increase kinetic energy and the movement of particles in the treated area, and facilitate drug absorption….

    ….Heat is also expected to enhance transdermal drug penetration by enhancing solubility of the drug in formulation. As a general rule, the aqueous solubility of inorganic and organic solid drugs increases with increasing temperature….

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    That makes sense.. what you could use to heat it would be one of those baby bottle warmers... I don't remember them getting that hot and they are cheap I think
    Matt
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    An easy way would be to fill the sink with some hot tap water and place your homebrew in it before you get in the shower.
    •   
       

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    Originally posted by SteveDFW
    An easy way would be to fill the sink with some hot tap water and place your homebrew in it before you get in the shower.
    I don't think it would be hot enough. Tap water is 130 deg F.
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    True, but it would be better than room temperture, as well as FREE & EASY !!!
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    The study doesn't mention the temperature, but it does say "heat generating patch", which would lead me to believe the patch is using a chemical method of generating heat like handwarmers (which generate heat by oxidizing iron filings, IIRC).

    Keeping in mind that this stays in contact with the skin for long periods of time, it can't get that hot, but rather delivers sustained amounts of relatively low heat.

    You could get good results by heating your bottle in the sink or microwave, then applying and rubbing vigorously to generate frictional heat (as recommended by others).
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    Ok.... With the patch raising temp is a good thing. It is proven that skin temp increases absorption. The patch is constantly releasing hormone slowly so to elivate the skin temp would be benifficial. But not to us.. I always say to rub the solution in hard because it raises the skin temp but only until the solution is rubber on. You don't not want it to rub in in 30 secs that is not benificial.. The longeer the skin stays "wet" the easier it is for the ph to go through. That is the purpose of the pg is to keep the skin wet to alow for penetration... SO it is not a good idea to heat the homebrew becasue the longer the wet th better. Maybe try cooliing it...NO thats just dumb..hehehe. Hope that helps.. Talk to ya
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    Curt2go,

    Regarding keeping the application site wet. It is recommended to spread the transdermal over a large area for better absorption. Obviously, if we place a large amount in a small area it will remain wet longer, but yet absorption will suffer. But yet on the flip side, if the solution dries too quickly it will leave the (pro)hormone on the surface of the skin (I experienced this recently. After applying my 4ad transdermal I went outside in the heat and sun. I later noticed white powder covering the application area - unabsorbed 4ad).

    It may be necessary when applying heated transdermal mixtures to apply it to a somewhat smaller area, resulting in a "thicker" application in order to prevent the PE's from evaporating before the hormone has had time to absorb.
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    And/Or following up with an application of the carrier only gel after the initial application to keep the applied area saturated. I still like the heating idea based on the theory of increasing the kinetic energy of the drug and opening up the skin passageways.
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    Good point skazzel. i just like to rub the area hard to increase skin temp. The pg will not absorb too welll even when you rub to hard. It will still take about 2-5min to absorb but the skinn will feel oily for about 1 hr. For me anyways. What recipe do you guys use. If you are doing this heating the soluion you may want to increase the Pg to 15% to kepp the area "wet".. What do you think??? Talk to ya..
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    Ok, just heated up some 4aderm that I have here in the microwave for about 20sec and applied it as usual. One thing I noticed is it was completely clear when it was hot. Anyone who has used 4aderm will tell you it is usually quite opaque from the high amount of 4ad dissolved in it. Correct me if I'm wrong, but shouldn't it being clear be taken as a sign that the 4ad was more completely dissolved? And shouldn't this boost absorption?

    It soaked in quite rapidly (about 1-2min instead of the usual 5-10), but my skin still has the moist feeling it usually has after the 4ad soaks in. No signs of any 4ad powder on the skin surface.
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    It will absorb better beacsue the ph is completely disolved. Keep an eye on it and let us know how i pans out.... Talk to ya... Youguys may be on to something to increase just that little bit more.. But every little bit counts right!!!! Talk to ya.

    PS Hey skazz did the ph come back out of solution when it cooled down. This is the whole reason I use clear bottles . you can see everything.. Talk to ya..
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    Propylene Glycol also changes viscosity dramatically with temperature. PG is used as an antifreeze in hydronic heating and cooling systems to prevent freezing water. As the viscosity of the solution decreases (with increasing temperature), the solute will dissolve more readily. As the viscosity increases (with decreasing temperature), the solute will begin to precipitate.
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    Curt,

    As the 4aderm is cooling, it is becoming cloudy again, signifying the 4ad coming out of solution and forming more of a suspension.
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    I'm not sure that heating like this will increase overall absorption by much as the solution cools very quickly once you spread it on your skin (unlike the patches in the study which remained warm for quite some time). It would be useful however when you don't have as much time to wait on your solution to soak in. If you only have 2-3 min, just put the bottle in the microwave for 20sec, apply, wait 1-2min and you are good to go.
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    Microwave?
    I didn't know alcohol + microwave mixed too well.
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    Just thinking here, but I'm not too sure heating, cooling and heating again would be such a good idea. Why? I don't know. Just doesn't sound like it would be good for the PH. Would it break down over continuous heating and cooling?
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    Originally posted by dg806
    Just thinking here, but I'm not too sure heating, cooling and heating again would be such a good idea. Why? I don't know. Just doesn't sound like it would be good for the PH. Would it break down over continuous heating and cooling?
    Maybe one could heat only the amount one is to apply immediately after?
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    Yeh I would think the diff in absorption is miniscule... But to each his own. If you want better absorption go with more dmso.... Talk to ya...
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    More DMSO? Didn't someone say that the difference in absorption percentages hardly changed when there was more than 24ml (10%) of DMSO in a brew?

    And as for the heating itself - my wife just thought of this - wouldn't it just have been the alcohol evaporating a little faster than usual from the heat?
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    Ah it was just chemo. He knows nothing...hehehe. I would not put more dmso in becasue we have found out that 10% is the threashold for it. IMO the formula is very good. Trying to gain .5 or 1% more is futile when you probably won't notice the difference.But thats just me. With the dmso in there it will be hard to gain any points on the %.But on the other hand nothing is perfect it can always be improved.SO keep trying to increase it I guess if you add up 5 differernt things at 1% increase thats 5% increase. I just don't think the heating is worth it(unless the ph is not in solution) Well Talk to ya..
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    I would be interested in knowing from one of the chemists if dg's instincts are correct and heating and cooling the solvent/solute would damage the solute (1-test and/or 4-ad). I am not worried about heating the solvent.

    I tried the microwave method this moring. It worked great. Sh*t the stuff absorbs fast. I want to continue with heating my homebrew so long as it is not destroying the 1-test (or 4-ad).
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    Chemically I don't think it would affect the 1-test or 4AD. Usually organic compounds like this are pretty tough.
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    Maybe in hot water but in the microwave i think would be different.It disrupts molecules. It is low frequency radiation in a sence? But i am no chemist... Talk to ya
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    Okay you got me there Curt.. I think I would do the warm water bath on it.. but not the microwave.. something about high powered radiation
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    I tried the hot water bath this morning. I ran the tap water until it was at its hottest and then filled the bathroom sink. Laid the bottle in it for about 15 mins (the time it took me to shower and shave). The solution was luke warm but not hot upon application. Only seemed to make a small difference in dry time but then I used 10% PG, 10% Glyc and 5% OS this batch. I usually get dressed about 8-10 min after applying since that is how long it takes me to prepare and drink my morning protein shake.
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    Okay I guess I am going to have to try using a baby bottle warmer when I go back on cycle.. those don't get that hot but hotter than normal tap water. I have one sitting around here from my youngest and he isn't using it now.
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    Hey Chemo whats your opinion on this!!!! talk to ya
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    Carbomer 934


    I'm not trying to change the subject but I have been having a hard time geting my carbomer to dissolve too even after heating the soulution. I heated it with hot tap water since I did not want the iso-alc to get too hot.
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    Yea. There's got to be a way. Maybe the carbomer should be added to the Iso Alchohol before any of the penetration enhancers are added? If you figure it out, please post on the "Carbomer and Clumping" thread.
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    You have to get the ph right are you using the triwhatever it is to get the ph more neutral?? Talk to ya...
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    I would personally think that the microwave radiation would, in a way, denature the molecules of the 1-test/4-ad.

    same thing happens to proteins when exposed to electricity, radiation or extreme heat.

    JMO
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    Watcha think? Would it work? I wonder how much it dispenses per pump?

    http://www.shoplifestyle.com/store/p...67&********goto
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    I don't thinl thats lotion.hahahahahahahahaha..

    Talk to ya..
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    Am I the only guy that likes spray bottles. The are the best way.. Man I love them. give them a try .. Talk to ya..
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    Originally posted by bow
    Watcha think? Would it work? I wonder how much it dispenses per pump?

    http://www.shoplifestyle.com/store/p...67&********goto

    That ****'s tight!! I want one.
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    Originally posted by Lifeguard



    That ****'s tight!! I want one.
    I'm going to order it and give it a try.
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    Originally posted by curt2go
    Am I the only guy that likes spray bottles. The are the best way.. Man I love them. give them a try .. Talk to ya..
    I am using a Oral Syringe to apply mine, that way you know EXACTLY how much you are getting.



    Curt

    you're green, I'm yellow...hehehaha

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    Originally posted by curt2go
    Am I the only guy that likes spray bottles. The are the best way.. Man I love them. give them a try .. Talk to ya..
    Yes. You damn Canadians are always trying to swim upstream.....

    I actually started transdermals back with Biotests Androsol (hey, it was all there was at the time). I didn't like it because I felt that I was spraying half of the compound to the atmosphere. So, I switched to a pump bottle and a gel.
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    The solution without the carbomer is very thick. It does not spray everywhere at all anymore. It works very good... Talk to ya.

    Also could be the cold weather acctually keeps it thicker...huh.. Talk to ya...

    Lifeguard thats a big chainsaw..hehehe. Talk to ya
  

  
 

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