5α-DHP - Liquid 5α-Dihydroprogesterone For Lab/R&D

[Mauritio]

For people buying it (from suchlabs) and wanting to make their own solution:

I was wondering about the solubility of 5aDHP, since it's a progesterone metabolite and progesterone is very insoluble in water.

I contacted such labs and they said it should be soluble in water and ethanol, but I dont think this is true, at least the water part.

It is 5alpha reduced, but that doesn't mean it's more water soluble, DHT is also 5 alpha reduced and very hydrophobic.

Also this chemical website says it is insoluble in water and soluble in ethanol.

So once I'll get the powder I'll try to dilute it in Gin and make a 0.5mg/drop solution.

https://www.selleckchem.com/products/5a-pregnane-320-dione.html

 

[golder]

For people buying it (from suchlabs) and wanting to make their own solution:

I was wondering about the solubility of 5aDHP, since it's a progesterone metabolite and progesterone is very insoluble in water.

I contacted such labs and they said it should be soluble in water and ethanol, but I dont think this is true, at least the water part.

It is 5alpha reduced, but that doesn't mean it's more water soluble, DHT is also 5 alpha reduced and very hydrophobic.

Also this chemical website says it is insoluble in water and soluble in ethanol.

So once I'll get the powder I'll try to dilute it in Gin and make a 0.5mg/drop solution.

https://www.selleckchem.com/products/5a-pregnane-320-dione.html

Could you let us know how you get on with the dilution? Thanks man.

 

[Mauritio]

Could you let us know how you get on with the dilution? Thanks man.

What do you mean by that? If it works ?

 

[golder]

What do you mean by that? If it works ?

Yeah if you're succesful. I have a few grams coming and I'm looking to mix it, but don't want to have a failed practise run on my first attempt.

 

[Mauritio]

Yeah if you're succesful. I have a few grams coming and I'm looking to mix it, but don't want to have a failed practise run on my first attempt.

It should definitely dissolve in ethanol. These chemical sites are usually reliable with their data.
But I'll let you guys know if and how it works.

 

[brightside]

It should definitely dissolve in ethanol. These chemical sites are usually reliable with their data.
But I'll let you guys know if and how it works.

There’s a discrepancy here. The link you posted claims a maximum 3.5mg/mL concentration. While haidut’s product has a much higher ~ 20mg/mL assuming 20 drops in 1 mL. Haidut utilizes SFA esters in his steroid products. I have yet to figure out what they are. I have seen octanol used to increase solubulity of progesterone, but you can smell that right away. Ive also seen PEG 400 used, but I doubt he would use that. He could just be using something like IPM, or Stearyl alcohol, but that itself can barely dissolve in ethanol.

Regardless, you need to use high proof (190) everclear. Whatever the true concentration is, gin will cut it in half. It doesnt make sense to use it unless you simply cannot buy Everclear.

Either that site is wrong, or haidut is using some surfactants to increase the concentration. At 3.5mg/mL you will get something like 175 micrograms per drop. With gin, you can cut that in half.

 

[Mauritio]

There’s a discrepancy here. The link you posted claims a maximum 3.5mg/mL concentration. While haidut’s product has a much higher ~ 20mg/mL assuming 20 drops in 1 mL. Haidut utilizes SFA esters in his steroid products. I have yet to figure out what they are. I have seen octanol used to increase solubulity of progesterone, but you can smell that right away. Ive also seen PEG 400 used, but I doubt he would use that. He could just be using something like IPM, or Stearyl alcohol, but that itself can barely dissolve in ethanol.

Regardless, you need to use high proof (190) everclear. Whatever the true concentration is, gin will cut it in half. It doesnt make sense to use it unless you simply cannot buy Everclear.

Either that site is wrong, or haidut is using some surfactants to increase the concentration. At 3.5mg/mL you will get something like 175 micrograms per drop. With gin, you can cut that in half.

True, I forgot about 1ML beeing 20 drops. And even for someone like me taking low doses, that would be too low of a concentration per drop to really be usable...

And for haidut: he used large amounts of vitamin E to dissolve 5adhp in, as per the old peat method (dissolving steroids in vitamin E).
I do have vitamin E succinate powder at home ,but I'm not sure if that would work or what ratio of
vitamin E : 5adhp : MCT oil, should be used. Maybe I can dig up Peats old patent and see if he mentions that...

I think you might be referring to a newer version of the product that only contains SFAesters?!

I might try dissolving it in octacosanol/policosanol, that's actually a good idea since the long chain fatty acids are also taken up by the lymphatic system, similarly to the steroid in vitamin E solution by Peat.

It seems oral use of the powder wouldn't be useless, but a lot less effective than the powder dissolved in Vitamin E.
And ethanol also doesn't seem to be the best solution:

Ray Peat:
"Progesterone is extremely insoluble in water, and, though it is vastly more soluble in vegetable oil than in water, it does not stay in solution at room temperature even at the low concentration of 1 part in 1000 parts of a typical vegetable oil."

"Other alcohols, including ethanol, have been used as solvents, but since they (ethanol even more than benzyl alcohol) have an affinity for water, the solution decomposes in contact with tissue water."

"According to a consultant for a major medical journal, the idea “…of dissolving progesterone, a fat soluble steroid hormone, in vitamin E which is then incorporated into chylomicrons absorbed via the lymphatics, and thus avoids the liver on the so called first pass… …is so simple it is amazing that the pharmaceutical companies have not jumped on it.” (A more sophisticated writer might have said “…stomped on it.”)
In the powder form, direct and intimate contact with a mucous membrane allows lipid phase to lipid phase transfer of progesterone molecules. Instead of by-passing the liver, much of the progesterone is picked up in the portal circulation, where a major part of it is glucuronidated, and made water soluble for prompt excretion.
Since this glucuronide form cross-reacts to some extent with the ordinary progesterone in the assay process, and since 50% of the ordinary free progesterone is carried inside the red blood cells (10,11), and 50% is associated with proteins in the plasma, while the glucuronide hardly enters the red blood cells at all, it is better to judge by clinical efficacy when comparing different oral forms. My comparisons show several times higher potency in the tocopherol composition than in powder form."

 

[Mauritio]

I found the patent and it answered almost all my questions of what and how much to use and how to prepare the solution:


"Suitable forms of tocopherol include d-alpha tocopherol, and mixed tocopherols of the dextro-rotatory form.
Suitable additives include coconut oil, palm kernel oil, jojoba oil, and olive lil, used in concentrations up to about 15% to lower the viscosity of the solution and to thus speed absorption; ascorbyl palmitate and/or glyceryl monophosphate in concentrations sufficient to emulsify the composition with water; biological or organic gels including aloe gel and extracts from marine algae to thicken the consistency and to stabilize the emulsion; and ethanol, in a concentration of up to about 7% by volume, to modify consistency and to increase absorption of progesterone.
The composition is prepared by mixing the ingredients to obtain a homogeneous product. Stirring at room temperature is adequate, but may require several days to reach complete homogeneity. An oxygen-free atmosphere is preferred but not essential. If higher temperatures are used for faster mixing, an oxygen-free atmosphere becomes more important to prevent oxidation of the materials.
Progesterone and tocopherol can be mixed in the proportions of from 1% to about 25% progesterone by weight, to about 75% to 99% of tocopherol, with a preferred concentration for most uses of from about 10% to 20% progesterone to about 80% to 90% tocopherol."

- US4439432A - Treatment of progesterone deficiency and related conditions with a stable composition of progesterone and tocopherols - Google Patents

 

[Mauritio]

I would go for the following mixture:

10g in total, of which:

0.25g 5adhp = 2.5%
8.25g alpha-tocpherol = 82.5%
1,5g olive/mct-oil = 15%

40 mg of the solution contains 1mg of 5aDHP, or 100mg equals 2.5mg of 5aDHP, which is relatively easy to measure with a mg-scale.

The only problem that I have is that all the vitamin E's (alpha tocopherol or mixed tocopherol) I can find are already premixed in olive oil.
And if I'm not mistaken the olive oil is the biggest part of that mixture. So if took my 8.25g of alpha tocopherol from that mixture, that would contain an amount of olive oil many times higher than the 1.5g I would need, throwing off the whole ratio of ingridients.
Anybody know how to circumvent this ?

 

[brightside]

And for haidut: he used large amounts of vitamin E to dissolve 5adhp in, as per the old peat method (dissolving steroids in vitamin E).
I do have vitamin E succinate powder at home ,but I'm not sure if that would work or what ratio of
vitamin E : 5adhp : MCT oil, should be used. Maybe I can dig up Peats old patent and see if he mentions that...

I think you might be referring to a newer version of the product that only contains SFAesters?!

Ohh, I assumed incorrectly. He has two versions, tocopherols, and ethanol/SFA esters. Since you were talking about dissolving in ethanol, I wrongly assumed that his was ethanol based as well, since I can't actually see what the ingredients were before. That makes sense now.

It seems oral use of the powder wouldn't be useless, but a lot less effective than the powder dissolved in Vitamin E.
And ethanol also doesn't seem to be the best solution:

Ray Peat:
"Progesterone is extremely insoluble in water, and, though it is vastly more soluble in vegetable oil than in water, it does not stay in solution at room temperature even at the low concentration of 1 part in 1000 parts of a typical vegetable oil."

"Other alcohols, including ethanol, have been used as solvents, but since they (ethanol even more than benzyl alcohol) have an affinity for water, the solution decomposes in contact with tissue water."

"According to a consultant for a major medical journal, the idea “…of dissolving progesterone, a fat soluble steroid hormone, in vitamin E which is then incorporated into chylomicrons absorbed via the lymphatics, and thus avoids the liver on the so called first pass… …is so simple it is amazing that the pharmaceutical companies have not jumped on it.” (A more sophisticated writer might have said “…stomped on it.”)
In the powder form, direct and intimate contact with a mucous membrane allows lipid phase to lipid phase transfer of progesterone molecules. Instead of by-passing the liver, much of the progesterone is picked up in the portal circulation, where a major part of it is glucuronidated, and made water soluble for prompt excretion.
Since this glucuronide form cross-reacts to some extent with the ordinary progesterone in the assay process, and since 50% of the ordinary free progesterone is carried inside the red blood cells (10,11), and 50% is associated with proteins in the plasma, while the glucuronide hardly enters the red blood cells at all, it is better to judge by clinical efficacy when comparing different oral forms. My comparisons show several times higher potency in the tocopherol composition than in powder form."

Yep. Ethanol is quite polar, so it doesn't make much sense as a solvent for steroids (it's polarity does make it a decent penetration enhancer, though). I think the only reason it works so well is because of it's size. Increasing the amount of carbons doesn't yield any benefit and actually reduces the ability to solubilize hormones despite the reduced polarity (so fats don't work, as Ray pointed out). It's clearly not only the polarity of the solvent, but also the shape. The proof seems to be in aromatic solvents. Benzyl alcohol, and phenoxyethanol are very potent solvents of T, and toluene is quite potent for progesterone. I assume that this is because of the aromatic base that matches closely to the general shape of the sterol core and therefore allows for better solubilization (as opposed to fatty acids). So it makes sense that tocopherols are decent solvents, however, they're obviously not penetration enhancers and don't make sense for use on skin. Perhaps the unsaturation might play a role too, but cyclohexane is used as a solvent, so who knows.

I kind of doubt that you will be able to dissolve much in the policosanols, but perhaps adding it to your mixture might be an idea. For example, Octanol (C8) and stearyl alcohol (C18) both hold insignificant amounts of T on their own. If you plan to use it topically, you could try using a bit of benzyl alcohol in a combination with ethanol to boost the concentration without using too much to make the toxicity an issue. I mean, at a few drops/day I doubt it would be an issue. If you could get away with 10% BA, you would have roughly 1-2mg of BA per drop which is pretty minor.

You can also buy mixed tocopherols up to 95% from places like lotioncrafter. Using this you can fix your problem by adding it to the other mixtures to bring the tocopherol content to what you want. It seems to be extracted from soy, just like ProgestE, and is probably pretty good. The only caveat, it's out of stock..

Mixed Tocopherols 95%, Natural Vitamin E is a transparent, brownish-red, viscous oil with a mild characteristic odor. It is a 95% active blend of natural mixed tocopherols isolated from the distillation of soybean oil and concentrated to contain naturally occurring d-alpha, d-beta, d-gamma and d-delta tocopherols.

They also have vitamin E acetate, which I have a bit of. I only tried dissolving DHEA into it, and just dumped like 200mg into 1mL. It didn't dissolve and I got bored and left it. Perhaps it would work well with lower quantities.

 

[Mauritio]

I kind of doubt that you will be able to dissolve much in the policosanols, but perhaps adding it to your mixture might be an idea. For example, Octanol (C8) and stearyl alcohol (C18) both hold insignificant amounts of T on their own. If you plan to use it topically, you could try using a bit of benzyl alcohol in a combination with ethanol to boost the concentration without using too much to make the toxicity an issue. I mean, at a few drops/day I doubt it would be an issue. If you could get away with 10% BA, you would have roughly 1-2mg of BA per drop which is pretty minor.

You can also buy mixed tocopherols up to 95% from places like lotioncrafter. Using this you can fix your problem by adding it to the other mixtures to bring the tocopherol content to what you want. It seems to be extracted from soy, just like ProgestE, and is probably pretty good. The only caveat, it's out of stock..

Yeah I discarded the policosanol possibility relatively quickly.
Thanks for the idea on the 95% vitamin E.
I found one that is in stock and sells the same/similar one. For me in Europe shipping will cost as much as the product itself but so be it, I couldn't find any similar products from Europe

I'm not the biggest fan of vitamin E acetate , vitamin E succinate has been shown superior in a few studies.
I ordered the mixed tocopherols but if they dont work or if they take too long to arrive I might try a mix of olive oil , 5adhp and vitamin E succinate.

Mixed Tocopherols 95% Vitamin E Oil - Skincare Essentials • Non-GMO • All Natural

Discover Mixed Tocopherols Vitamin E Oil. Shield your skin from harmful UV rays, find it in sunscreens, moisturizers, makeup, and hair products.

www.bulknaturalswholesale.com

 

[brightside]

Yeah I discarded the policosanol possibility relatively quickly.
Thanks for the idea on the 95% vitamin E.
I found one that is in stock and sells the same/similar one. For me in Europe shipping will cost as much as the product itself but so be it, I couldn't find any similar products from Europe

I'm not the biggest fan of vitamin E acetate , vitamin E succinate has been shown superior in a few studies.
I ordered the mixed tocopherols but if they dont work or if they take too long to arrive I might try a mix of olive oil , 5adhp and vitamin E succinate.

Mixed Tocopherols 95% Vitamin E Oil - Skincare Essentials • Non-GMO • All Natural

Discover Mixed Tocopherols Vitamin E Oil. Shield your skin from harmful UV rays, find it in sunscreens, moisturizers, makeup, and hair products.

www.bulknaturalswholesale.com

Yeah, VE succinate is pretty interesting stuff. I really like Travis's comments on it.

Have you yet to try this combination?

 

[Mauritio]

Yeah, VE succinate is pretty interesting stuff. I really like Travis's comments on it.

Have you yet to try this combination?

Yes, Peat didnt like it in his last years even when I send him studies on it. Although he did say it the succinate functions in a detoxing way. ...

You mean vitamin E+ 5aDHP?
I had to order both from the US and both haven't arrived. Let's hope the steroid makes it through customs

 

[TTorque]

Has anyone been successful at supplementing Suchlabs verison? Either by their own mixture, or straight MCT + x amount of mg?
I miss haidut's drops - I'm trying to get a rough idea how much powder is equal to 3-4 drops orally.

 

[dukesbobby777]

Has anyone been successful at supplementing Suchlabs verison? Either by their own mixture, or straight MCT + x amount of mg?
I miss haidut's drops - I'm trying to get a rough idea how much powder is equal to 3-4 drops orally.

Is just taking the powder, as is, not an option? You can buy the 10mg scoop spoons and just dose?

 

[Mauritio]

Has anyone been successful at supplementing Suchlabs verison? Either by their own mixture, or straight MCT + x amount of mg?
I miss haidut's drops - I'm trying to get a rough idea how much powder is equal to 3-4 drops orally.

My powder is still stuck in customs unfortunetly. But it should be here soon.
It better be , because I only have a couple droos of idealabs 5adhp left.

 

[Mauritio]

Is just taking the powder, as is, not an option? You can buy the 10mg scoop spoons and just dose?

You could try that , I don't think it's useless . Because of the high quantity such labs sell 5adhp ,the amount "wasted" doesn't really matter.
Actually now that I've reread peats comment on that , I think you might just take a dose that is several times higher then your idealabs dose. That's at least how I interpret the following, and given you can substitute 5adhp for progesterone in this paragraph.

"In the powder form, direct and intimate contact with a mucous membrane allows lipid phase to lipid phase transfer of progesterone molecules. Instead of by-passing the liver, much of the progesterone is picked up in the portal circulation, where a major part of it is glucuronidated, and made water soluble for prompt excretion.
Since this glucuronide form cross-reacts to some extent with the ordinary progesterone in the assay process, and since 50% of the ordinary free progesterone is carried inside the red blood cells (10,11), and 50% is associated with proteins in the plasma, while the glucuronide hardly enters the red blood cells at all, it is better to judge by clinical efficacy when comparing different oral forms. My comparisons show several times higher potency in the tocopherol composition than in powder form."

 

[BRMarshall]

Maybe Haidut will open source the recipe of his now discontinued formula.
@haidut

I am not a chemist but such discussions are interesting.

 

[Mauritio]

Maybe Haidut will open source the recipe of his now discontinued formula.
@haidut

I am not a chemist but such discussions are interesting.

I'm pretty sure he used one variation of peats formula that I posted in this thread, but yeah Id like to see his formula too.

 

[TTorque]

I'm pretty sure he used one variation of peats formula that I posted in this thread, but yeah Id like to see his formula too.

Rat just received theirs today. 5g
Still have no idea on dosage. But based on peats comment you quoted, the powder form does NOT bypass the liver? And let's estimate 50% is "wasted" ? So 4mg of drops, might be equal to ~100mg of powder? Tried ~10mg + plain water to no avail. (compared to the drops, anyways)