Revisiting Oral Testosterone
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Hello all!
There is a TL;DR summary at the bottom.
When it comes to "supplementing" testosterone, I know the TRT and bodybuilding bros insist that injections are the best and anything other than injections is stupid. But I tend to agree with the sentiment previously and extensively shared over at the "other" forum that injecting those ester formulas aren't very healthy and you can get raw, micronized powder pretty easily and DIY. The overall consensus from people like @Santosh and others settled on transdermal application.
I wanted to understand why every hormone on the planet can be taken orally except testosterone -- DHEA, pregnenolone, progesterone, estrogen, BC pill, etc. From what I read, although the bioavailability of T is high, it's rapidly metabolized in the first pass through the liver. Since I don't know what "metabolized" means in this sense, I learned some more and apparently a large portion of the T is converted to DHT in the intestinal tract and the liver, and then most of the rest into the other T metabolites, and so not much of the actual T hits the bloodstream. I guess there isn't a similar problem for the other hormones.
So I came across an older (2005) study [1] that tried to mix T powder with sesame oil (yeah, I know) and they got pretty decent results. They also added dutasteride (not sure how I feel about that) to suppress DHT conversion and got even better results. This was a heterogeneous mixture (so no dissolving of course) of micronized T suspended in sesame oil at a concentration of 100 mg/ml. (For reference, a ml is a little less than a quarter teaspoon, so this is a rather thick concentration.) This was "mixed thoroughly on a magnetic stir plate to create a homogenous T/sesame oil emulsion". I'm not sure if that's an important detail or just means that the powder was evenly distributed amongst the oil. The mixture was then "vigorously mixed (by shaking) with milk and administered to the subject".
The idea was to coat the T particles in oil so that they would be taken up by the lymphatic digestive system and bypass the liver, in a similar manner to how the fat-soluble vitamins A, D, E and K are taken up. It seems like the results showed some feasibility.
Here are the max results, which were achieved between 3-4 hours after administration. The subjects were chemically castrated down to almost zero T before hand, so the numbers indicate how much effect the oral T caused. In theory, for a normal person, these numbers would be added on top of one's baseline T.
T 200 mg (+ Dutasteride): 357 ng/dL (644 ng/dL)
T 400 mg (+ Dutasteride): 757 ng/dL (1459 ng/dL)
T 800 mg (+ Dutasteride): 1172 ng/dL (3541 ng/dL)It took about 10-12 hours for things to return to baseline, so I wonder if this could be worked to not interfere with natural overnight production?
They also tested with Testosterone Enanthate, which showed similar time to achieve max and similar return to baseline times, but in some cases higher maxes. (Not sure that I'm a fan of using an ester like this, but if clearance is quick maybe it's ok?)
TE 200 mg (+ Dutasteride): 424 ng/dL (586 ng/dL)
TE 400 mg (+ Dutasteride): 1502 ng/dL (2146 ng/dL)
TE 800 mg (+ Dutasteride): 4663 ng/dL (6641 ng/dL)Now 800 mg of T would cost about $1 per day at PPL prices, plus whatever for dutasteride. But I'm not convinced of the value of having such high T values? Wouldn't that be over and above what could be handled by the androgen receptors?
Regarding DHT, the only combination where it was kept below the upper reference range was 200 mg T + D, 400 mg T + D, and 200 mg TE + D. I know DHT is somewhat controversial; some in the looksmax community think it's a trash hormone, others say it's the most important for male characteristics; maybe the truth is somewhere in between.
E2 and SHBG were mid-range for all combinations. Probably the relatively short half-life kept the T from aromatizing. One subject did develop some small gyno however, which completely resolved within a couple days of the study. No liver or kidney toxicity was found.
"These data contradict the prevailing wisdom in the field, which states that the oral route for T delivery is impractical due to near-complete hepatic first-pass metabolism of orally administered T. Although it is true that the bioavailability of orally administered T is very low, probably around 1%, our work demonstrates that if sufficient T is administered orally in oil, potentially therapeutic levels of serum T can be achieved after oral dosing."
Building on this, I found a much more recent (2021) study [2] that took the same idea of powdered T in sesame oil but also added two solvents (benzyl alcohol and ethanol) and a surfactant (?) (propylene glycol monolaurate) and, in brief, was able to get about the same results as above with half of the dose (800 ng/dL with 200 mg T) but still struggled to keep DHT down (dutasteride was not used).
TL;DR Summary
- Micronized powdered T mixed in sesame oil, taken orally, does boost serum testosterone levels.
- The potential issues are: a) you need a decent dose (400 - 800mg) to get the bigger numbers; and b) you risk raising DHT too high.
- Both issues in #2 can be mitigated somewhat by supplementing with dutasteride.
- Some companies are goofing around with adding solvents to make the bioavailability even better.
- Not sure if this can practically be applied without interfering with natural production; e.g., to produce 2-3 "peaks" of high testosterone throughout the day (rather than just the natural single early morning one).
I am experimenting, but nothing to report so far.
Anybody have any thoughts? Anybody care about this stuff?
[1] Oral Testosterone in Oil Plus Dutasteride in Men: A Pharmacokinetic Study
[2] An oral lipidic native testosterone formulation that is absorbed independent of food -
@Crypt-Keeper I think some people even tried oral testosterone in vit e. Similar to progest e.
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To my understanding, I thought oral testosterone worked but it wasn't used because its just less efficient and you need to take it daily similar to using testosterone topically which was more efficient than oral route.
Also why and how would raising DHT be bad? What are the issues with raising DHT to high?
I would likely never take dutasteride under most circumstances, and especially not to lower DHT lol
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@Crypt-Keeper said in Revisiting Oral Testosterone:
Hello all!
There is a TL;DR summary at the bottom.
When it comes to "supplementing" testosterone, I know the TRT and bodybuilding bros insist that injections are the best and anything other than injections is stupid. But I tend to agree with the sentiment previously and extensively shared over at the "other" forum that injecting those ester formulas aren't very healthy and you can get raw, micronized powder pretty easily and DIY. The overall consensus from people like @Santosh and others settled on transdermal application.
I wanted to understand why every hormone on the planet can be taken orally except testosterone -- DHEA, pregnenolone, progesterone, estrogen, BC pill, etc. From what I read, although the bioavailability of T is high, it's rapidly metabolized in the first pass through the liver. Since I don't know what "metabolized" means in this sense, I learned some more and apparently a large portion of the T is converted to DHT in the intestinal tract and the liver, and then most of the rest into the other T metabolites, and so not much of the actual T hits the bloodstream. I guess there isn't a similar problem for the other hormones.
So I came across an older (2005) study [1] that tried to mix T powder with sesame oil (yeah, I know) and they got pretty decent results. They also added dutasteride (not sure how I feel about that) to suppress DHT conversion and got even better results. This was a heterogeneous mixture (so no dissolving of course) of micronized T suspended in sesame oil at a concentration of 100 mg/ml. (For reference, a ml is a little less than a quarter teaspoon, so this is a rather thick concentration.) This was "mixed thoroughly on a magnetic stir plate to create a homogenous T/sesame oil emulsion". I'm not sure if that's an important detail or just means that the powder was evenly distributed amongst the oil. The mixture was then "vigorously mixed (by shaking) with milk and administered to the subject".
The idea was to coat the T particles in oil so that they would be taken up by the lymphatic digestive system and bypass the liver, in a similar manner to how the fat-soluble vitamins A, D, E and K are taken up. It seems like the results showed some feasibility.
Here are the max results, which were achieved between 3-4 hours after administration. The subjects were chemically castrated down to almost zero T before hand, so the numbers indicate how much effect the oral T caused. In theory, for a normal person, these numbers would be added on top of one's baseline T.
T 200 mg (+ Dutasteride): 357 ng/dL (644 ng/dL)
T 400 mg (+ Dutasteride): 757 ng/dL (1459 ng/dL)
T 800 mg (+ Dutasteride): 1172 ng/dL (3541 ng/dL)It took about 10-12 hours for things to return to baseline, so I wonder if this could be worked to not interfere with natural overnight production?
They also tested with Testosterone Enanthate, which showed similar time to achieve max and similar return to baseline times, but in some cases higher maxes. (Not sure that I'm a fan of using an ester like this, but if clearance is quick maybe it's ok?)
TE 200 mg (+ Dutasteride): 424 ng/dL (586 ng/dL)
TE 400 mg (+ Dutasteride): 1502 ng/dL (2146 ng/dL)
TE 800 mg (+ Dutasteride): 4663 ng/dL (6641 ng/dL)Now 800 mg of T would cost about $1 per day at PPL prices, plus whatever for dutasteride. But I'm not convinced of the value of having such high T values? Wouldn't that be over and above what could be handled by the androgen receptors?
Regarding DHT, the only combination where it was kept below the upper reference range was 200 mg T + D, 400 mg T + D, and 200 mg TE + D. I know DHT is somewhat controversial; some in the looksmax community think it's a trash hormone, others say it's the most important for male characteristics; maybe the truth is somewhere in between.
E2 and SHBG were mid-range for all combinations. Probably the relatively short half-life kept the T from aromatizing. One subject did develop some small gyno however, which completely resolved within a couple days of the study. No liver or kidney toxicity was found.
"These data contradict the prevailing wisdom in the field, which states that the oral route for T delivery is impractical due to near-complete hepatic first-pass metabolism of orally administered T. Although it is true that the bioavailability of orally administered T is very low, probably around 1%, our work demonstrates that if sufficient T is administered orally in oil, potentially therapeutic levels of serum T can be achieved after oral dosing."
Building on this, I found a much more recent (2021) study [2] that took the same idea of powdered T in sesame oil but also added two solvents (benzyl alcohol and ethanol) and a surfactant (?) (propylene glycol monolaurate) and, in brief, was able to get about the same results as above with half of the dose (800 ng/dL with 200 mg T) but still struggled to keep DHT down (dutasteride was not used).
TL;DR Summary
- Micronized powdered T mixed in sesame oil, taken orally, does boost serum testosterone levels.
- The potential issues are: a) you need a decent dose (400 - 800mg) to get the bigger numbers; and b) you risk raising DHT too high.
- Both issues in #2 can be mitigated somewhat by supplementing with dutasteride.
- Some companies are goofing around with adding solvents to make the bioavailability even better.
- Not sure if this can practically be applied without interfering with natural production; e.g., to produce 2-3 "peaks" of high testosterone throughout the day (rather than just the natural single early morning one).
I am experimenting, but nothing to report so far.
Anybody have any thoughts? Anybody care about this stuff?
[1] Oral Testosterone in Oil Plus Dutasteride in Men: A Pharmacokinetic Study
[2] An oral lipidic native testosterone formulation that is absorbed independent of foodEither swallow the raw powder or apply it transdermally.
Do you really see yourself swallowing 8ml of pure oil every day ? -
@Crypt-Keeper
There is an excellent article about it https://testonation.com/2023/01/15/oral-testosterone-hows-the-best-way-to-take-it/BTW, some basics:
- sesame oil is full of PUFA ie poisonous in the long term...
- dutasteride is a poison too, having enough DHT is highly important for health and wellbeing
You may want to research/learn more - for example by googling videos by:
- haidut oral testosterone or haidut DHT
- ray peat finasteride
And just google: "post finasteride syndrome reddit"
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Well I think I'm done experimenting with that. I did do up to 800mg in EVOO and a few hours after that I got that sensitive / inflamed / pink scalp issue that I remember getting back from the old days when I took Epistane, so I think DHT went way high as expected.
Otherwise, I think my face and skin looked better, but nothing else interesting to report, and overall I still felt like crap. Mood and energy were neither improved nor worsened. Allergies seem to have flared up a bit but that could be just a coincidence with it being spring and the trees blooming now. (Or DHT might have suppressed cortisol all the more.)
I want to try to experiment the opposite way now. I know I have way too low E2 and horribly out of balance TT:E2 ratio (something like 60:1) with long-standing low E2 symptoms that I can't seem to correct. I thought maybe I had low DHT but I was likely reading the bloodwork wrong and probably have borderline high DHT.
I suppose DHT is an anxiolytic and when it's too high there is too much of a sedative effect. And an anti-estrogenic effect. Plus, in a sense, it can be anti-androgenic if it's occupying too many androgen receptors and preventing T from doing the functions it wants to do.
I'm going to look into raising E2 which seems like a tough nut to crack. Then maybe find some mild, natural 5ar inhibitors to bring DHT down just a bit. I don't want to affect any other 5ar neurosteroids, but probably won't have a choice. I'm not touching fin or dutasteride either.
I may try the transdermal some day but I think too much of that will go to DHT and it will probably blow out my TT:E2 ratio even worse. Not sure why I have so little aromatase activity.
In conclusion, the much-lauded "low estrogen, high DHT" phenotype is probably not for me.
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dissolving it Vitamin E would increase half life enormously
In peat's book, he says progesterone dissolved in vitamin E lasts 10 times longer than just taking progesterone normally
I think the same applies to testosterone - the vitamin E makes it attached to chylomicrons that survive the liver
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@wester130 Any suggestions of where to source the vitamin E? Do you think that idealabs tocovit would suffice?
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@jamezb46 yes, tocovit can work, maybe with 5ml of Food grade Ethanol
https://www.toxinless.com/vitamin-e
Uniqe grace e vitamin E also works
healthantura also make a good vitamin E
maybe Now Foods Vitamin E,
https://raypeatforum.com/community/threads/transdermal-testosterone-solvent.52479/
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@wester130 Thank you. Any idea as to the solubility of T or DHT in tocopherols? For example, in Tocovit? Will be interesting to see how oral with tocopherols vs transdermal with DMSO + Ethanol or IPM + MCT + Ethanol will work.
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@jamezb46 I think someone worked out testosterone should be identical to Progesterone in terms of solubility - and each bottle of 30ml progesterone usually has about 3 grams of progesterone in it
not totally sure about DHT - andractim can be bought at 10% solution - so 10% of 50ml apprixmately but not exactly 5 gram
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does anyone know the % value of Vitamin E to olive oil in this product?
it's not a great product but it has potential
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Thanks
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W wester130 referenced this topic on
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Where did you get the micronized testosterone from?
800 mg is a lot, was that in oil? My understanding is if it's in oil to bypass the lymphatic system you need to have fat with it to see a good increase in levels. This is why the Maximus protocol of trt+ has you taking in fat, they also use micronized testosterone with oil to bypass the lymphatic system.
interestingly they use small doses of enclomiphene to fight against suppression, not sure how needed that is though.
I recently did sublingual testosterone, great results, my energy and mood had huge increase, my allergies went crazy though so I assume I'm allergic to the carrier and had to stop.
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@RFC32 PPL sell micronised T
that study did 800mg in peanut oil
to bypass the liver/digestion/lymphatic system it needs to be in vitamin E
I have never seen a study where someone used T base in vitamin E, only things like peanut oil, corn oil and safflower oil or coconut oil and benzyl alcohol.
the same applies to testosterone
"The only solvent for progesterone which isn't toxic
and which will dissolve an effective quantity. is vitamin E.
In this form, it can be absorbed through the skin or other
membranes, or can be taken orally. Taken orally. it is
absorbed as chylomicrons. going into the general circulation
(as vitamin E does), instead of to the liver where it would be
prepared for excretion. In this form, therefore, it is fully
and quickly available to all tissues. It is approximately 20
times more powerful in its action than other preparations, so
it is important to use it in physiological quantities. rather
than in the huge doses commonly given rectally or by
injection. Ten or 20 mg. is often an effective dose, though
people with low thyroid or high estrogen sometimes use 50
to 100 mg . per day. In the customary 10% solution. one
drop contains about 3 mg . progesterone. and 1 011. (114 tsp.)
contains 100 mg . The first dose should never be more than
15 mg." -
So theoretically we could take much lower dosages.
There are studies with straight micronized T no carriers that show decent success with two dosages of 200mg per day, including showing how they solve many sex drive issues of people with T issues. If I recall it didn’t work for all participants to hit super high level. Haidt has it in his write up.
To me this says for those of us with decent levels it’s probably a very good solution. I can first hand say that suppression from sublingual was very manageable.
Maximus reports extremely good results doing a lymphatic bypass and micronized T with 6 mg of Enclomiphene a day to stop you from suppression. I don’t like Enclomiphene but the results are interesting. They do 500 mg micronized T once a day. My guess is with a protest e style formula we could get similar results with much lower dosage and less reliance on something like Enclomiphene.
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the problem is the ester, longer esters being worse
-Longer esters cause higher levels of estrogen
- Longer esters cause more water retention
- Longer esters cause more suppression of the HPTA
- Longer esters cause higher levels of nitrogen retention (muscle gain)in other words are more anabolic
-Shorter esters cause higher peak plasma levels -
I read a study where they gave 400 mg per day in 4 divided doses of 100mg to Eunuchs. There were no detrimental effects on the liver.
Given that Peat recommended 10-20 mg P4 when dissolved in vit E and taken orally, I cannot think of any reason why a low dose of 10mg T orally dissolved in vitamin E would not be massively effective at “supplementing” testosterone levels in healthy men.
I myself am going to get to the bottom of this. T powder is on the way, vitamin E is on hand. Hopefully I can get the T to dissolve in the tocopherols and I can present some solid results after a few weeks of use and we can all get on the same page about the exciting idea of homebrewing the “male version” of progest-e.
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@jamezb46 I’ve been thinking more about this and didn’t realize how similar the idea with this is to what I’ve already taken.
The other formula I’ve used is sublingual but with a different formula that unfortunately I am allergic to. My eyes get so dry after a few days of use I can barely see, it reverses when I drop the supplement.
Aside from that here’s my experiences with sublingual test:
- hits after about 15 minutes when I suddenly feel an increase in mood and energy.
- peaks around an hour, my sex drive suddenly goes way up and general drive goes up.
- desire to exercise goes up too
- aggression increases as well
- my weight decreased after using it for three weeks straight, I stopped because my vision got so bad I couldn’t drive.
- I started dreaming again, I haven’t had dreams in a long time.
I was doing 6 mg in the mornings, than 3 more doses of 4 mg later in the day.
I really want to try with another formulation that I’m not allergic to. I did get some suppression after a few days but I definitely was not shut down.
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@RFC32 Your reaction sounds more like enclomiphene which is known to damage eyesight, especially in DMSO
