Italian Hair Loss Lotion To Hit The Market In 2016

[MomoGee]

I'm in italy right now

does someone want me to throw a brick with a note through Brotzu's clinic window?

NO NO NO!!! We need you to make this a reality.

We need him to make the best lotion around, one that has 99.9% purity, blue in colour, and will bring terror to the eyes of Merck.

 

[plisk]

brotzu ends up dead in mysterious insulin overdose for man who was never known to be diabetic, guarantee it

Merck dont play around with that hair loss money game

 

[Royaume]

We need this lotion. The fkcing hairs are getting thinner and thinner and the adverts on this website getting stronger and stronger.
I need fkcing 20 seconds to scroll this page down.

 

[Trouse]

@MomoGee Actually in that picture, I'd be Walter, since I'm the pissed off bald guy

 

[d3nt3dsh0v3l]

You know, we could be making our own topicals instead of memes and trying it out...

We know r-equol and s-equol work just as well for binding DHT. We know that equolibrium may be a way to get our hands on the stuff, if research labs are not even considered (p.s., if they are considered, then lc labs, cayman chem, alfa-aesar all show up on fisher scientific - these are legitimate labs, i.e. not Chinese...no offense to Chinese).

We know Brotzu's example lotions use a 0.1% s-equol concentration, albeit higher concentrations are suggested also. The claim is that the 0.1% lotions he made did indeed have an effect.

We know that "the" equol patent had a human pilot study listed in an older version:

[Example 20
Human Pilot Study

In Men and Women, Serum 5α-DHT Levels Before and after Treatment with Non-Racemic Equol

[0245]In a pilot study involving 4 men (ages 50 to 59 years old) and 2 postmenopausal women (ages 60 to 62), baseline levels of serum 5α-dihydrotestosterone (5α-DHT) were determined by ELISA in triplicate. After 7 days of oral dosing with 3 mg of non-racemic equol per day, 5α-DHT levels were again determined.

TABLE-US-00013 TABLE 13 Baseline: 5α-DHT levels 5α-DHT levels on day 7 of before the 1st morning oral dosing (two to four dose on the 7th day of hours after the 1st morning MEN treatment dose) Subject A 692 + 10 pg/ml 600 + 13 pg/ml* Subject B 724 + 18 pg/ml 612 + 18 pg/ml* Subject C 658 + 23 pg/ml 534 + 16 pg/ml* Subject D 747 + 27 pg/ml 596 + 28 pg/ml* *= significant decrease compared to baseline values

TABLE-US-00014 TABLE 14 Baseline: 5α-DHT levels 5α-DHT levels on day 7 of before the 1st morning dose oral dosing (two to four hours WOMEN on the 7th day of treatment after the 1st morning dose) Subject E 221 + 5 pg/ml 170 + 6 pg/ml* Subject F 265 + 14 pg/ml 193 + 20 pg/ml* *= significant decrease compared to baseline values

[0246]This studies demonstrated that oral consumption of equol significantly decreased serum 5α-DHT levels in men (by approximately 17%) and in women (by approximately 26%) that provided androgen hormone modulation in dermal applications for preventing and treating skin disorders and chronological and intrinsic aging.

Read more: http://www.patentsencyclopedia.com/app/20100076071#ixzz4fZkdRuGt ]


"Long-Term Effects of Dihydrotestosterone Treatment on Prostate Growth in Healthy, Middle-Aged Men Without Prostate Disease
A Randomized, Placebo-Controlled Trial"
Amanda Idan, BSc, MHSc; Kaye A. Griffiths, AMS, DMU; D. Tim Harwood, PhD; Markus J. Seibel, MD, PhD; Leo Turner, MMed, RN;
Ann J. Conway, MBBS; and David J. Handelsman, MBBS, PhD

That paper there gave old men 70 mg DHT/day. The results were that the DHT-treated group had a 10-fold increase in serum DHT levels, well above the normal range of circulating DHT. Please see the attached picture for results. After a year of treatment, it was found that the average increase in serum DHT levels was 20 nmol/L.

What is the normal range? https://www.endocrinesciences.com/sites/endocrinesciences/files/imce/uploads/L5167.pdf
30-85 ng/dL (the linked pdf is kind enough to give the conversion factor for nmol/dL, because when I did the conversion by hand, I thought I fucked up lol). The normal range is then 0.69 nmol/L-3.1 nmol/L.

Bottom line: ~70 mg DHT/day gives an increase of ~5-10x physiological levels of DHT.

Rough back-of-the-envelope calculations:
One might expect that to just double normal DHT levels, one would only dose on the order of ~7 mg DHT/day. (Just an order of magnitude less).
Assuming equol binds to DHT 1:1 to render it inactive, we would need on the order of ~7 mg/day to get high DHT suppression (equol and DHT have pretty similar molar masses). Looking at that old pilot study in that patent, we see that 3 mg/day supposedly resulted in ~20% decrease in unbound serum DHT. I think this means we are in the correct order of magnitude.

Now for the last bit of hand-waving that I will just pull out of my ***: an equol topical is supposed to only lower DHT on the scalp and leave DHT elsewhere alone. For simplicity, I assumed that 10% of the body's total DHT resides in the scalp. So the dose might be something like 0.7 mg/day.

So an equol topical would have a concentration of 0.07-0.7%, let's just call it 0.01-0.1%. (1-10 mg/ml, assuming 1 ml applied daily).

Inb4 my analysis is retarded. It's just an order of magnitude check for sanity bro, chill. I'm not claiming anything is exact.

Moral of the story -
1) ~1-10 mg/ml solutions can have an effect.
2) R,S Equol, 99% is available at 100-200 mg/$100 through research labs and you get, what, 30 pills at 6 mg/pill supposedly with that Equolibrium supplement (but you have to extract the equol out, ew).
3) That patent I linked has several examples where they just use DMSO as a vehicle. It's gonna absorb into your skin if you resort to DMSO, lol. Some here might be waiting on liposomes because they don't want to fart around with an ethanol vehicle and absorption, etc. Just sayin'
4) Half life of s-equol is 7-8 hours. Unless metabolizing equol is like...sensitive to chirality, probably r-equol has a similar half life. This is a pretty solid half life for daily application. If you want to get off, you should just be able to.
"Equol: Pharmacokinetics and Biological Actions"
Kenneth D. R. Setchell3* and Carlo Clerici
5) Here's the shitty thing. The mechanism of action is similar to that of finasteride - stopping DHT's actions on the follicles. So....the timeline for improvement will be similar. This means you can't necessarily assess progress until 9 months or so. Brotzu's patent also says the treatment must be continued for many months for a significant effect. But he talks about hair fall stopping, etc. Wouldn't be out of the question if instead the reverse happened and you started shedding lol.
5.1) I'm just a scared doge on the internet... I haven't jumped on any of this other than fleshing out a plan. I figured I'd share it...

Love you guys, hang in there
But for those willing to stray from the off beaten path... the starting point awaits...

Finally, I leave you with this:

https://google2.fda.gov/search?q=equol&client=FDAgov&site=FDAgov&lr=&proxystylesheet=FDAgov&requiredfields=-archive:Yes&output=xml_no_dtd&getfields=*

The first four items on that list provide arguments and counter arguments to the FDA for the use for soy isoflavones and thus equol. Equol is specifically referenced in some of the documents. Bear in mind that soy isoflavones are part of the GRAS (generally recognized as safe) substances list. If you read the document arguing why, you see the mention of alleviating hot flashes and improving prostate health. These things are likely due to the production of equol, not the isoflavones themselves.
And the petition against soy isoflavones is by the Weston Price Foundation...I'll just leave it at that...

https://clinicaltrials.gov/ct2/results?term=equol&Search=Search
I also invite you to peruse through the few phase II trial studies that exist to evaluate the safety of s-equol. Bear in mind that doses up to 150-300 mg were used orally.

And finally, for those so inclined, here is a quick reference compounding guide.
http://pharmasy.weebly.com/uploads/...ompounding_and_dispensing__second_edition.pdf

 

[ironix]

You know, we could be making our own topicals instead of memes and trying it out...

I appreciate your effort but at this point it's faster to wait for fidia and their trails and bypass the time with memes.

You can follow the italian guys who made such an experiment and in my opinion it leads to nothing. The chances that you get an exact copy of the fidia lotion are non-existent and even if you get a similar lotion your results are most likely not representative. Look at the results from samumed for example. They tested 2 differend types of their drug with only a slight change on the main ingredient and the differences are clearly evident. The Brotzu lotion has 2-3 main ingredients and lipsomeds as a vehicle which are basically one of the most complex vehicles which you can us. Also you need a very potent stabilizer and it's not quite clear which stabilizer they use and if their stabilizer does work at all. So you would have to consider a lot of different things and only a slight change in the reciept could change a lot. I think it would be funny if you will make a test lotion which end up giving better results than the actual lotion from fidia but let's keep it real if you try to bake the same delicious cake as the one from your grandmother you always fail.

All in all I don't wanna be pessimistic or anything about such a project but I like to be realistic and if someone is willing to spend their time and money in such a project i would like to see the result but like I said we will probabely have some major news from fidia before you even apply the first drop of your test lotion on your head

 

[d3nt3dsh0v3l]

I appreciate your effort but at this point it's faster to wait for fidia and their trails and bypass the time with memes.

You can follow the italian guys who made such an experiment and in my opinion it leads to nothing. The chances that you get an exact copy of the fidia lotion are non-existent and even if you get a similar lotion your results are most likely not representative. Look at the results from samumed for example. They tested 2 differend types of their drug with only a slight change on the main ingredient and the differences are clearly evident. The Brotzu lotion has 2-3 main ingredients and lipsomeds as a vehicle which are basically one of the most complex vehicles which you can us. Also you need a very potent stabilizer and it's not quite clear which stabilizer they use and if their stabilizer does work at all. So you would have to consider a lot of different things and only a slight change in the reciept could change a lot. I think it would be funny if you will make a test lotion which end up giving better results than the actual lotion from fidia but let's keep it real if you try to bake the same delicious cake as the one from your grandmother you always fail.

All in all I don't wanna be pessimistic or anything about such a project but I like to be realistic and if someone is willing to spend their time and money in such a project i would like to see the result but like I said we will probabely have some major news from fidia before you even apply the first drop of your test lotion on your head

You know, I will have to respectfully disagree with almost everything you said.

I understand the inherent instability of liposomes and the magnitude of the problem of finding a formulation for a product expected to sit on store shelves for on the order of months at room temperature or perhaps warmer conditions without degrading. But in my post, I actually never discussed making any type of liposomal formulation, let alone reproducing Fidia's lotion. In fact, the very reason that I specifically restricted the discussion to simple vehicles only is that I agree with you. I too think it is too difficult of a problem to formulate stable liposomes at home. Unsaturated lipids will hydrolyze. SUVs will not remain small for extended periods of time. So to me, the majority of your rebuttal doesn't really seem germane.

Firstly, the basis of liposomes is to improve the uptake of a topical drug. Brotzu has not discussed or shown that the use of liposomes prevents systemic absorption of the drugs within his formulation. Secondly, I am well aware of the efforts on Ieson to reproduce the lotion. If you read through the posts, some users report some degree of improvement or change that occurs within the first few weeks before the lotion no longer appears to function. Again, it wouldn't be surprising if that homebrew solution was unstable. If you look at Brotzu's lotion, the primary solvent is water. If the liposomes fail, you effectively have NO vehicle because neither equol nor DGLA will be very water soluble. A failure of the liposomes doesn't just reduce the lotion's efficacy - it is catastrophic. Considering the first and second points, I therefore discuss the potential use of DMSO as a vehicle to get the job done because it is well known for enabling transdermal delivery. Ethanol is an option too as always.

Next, I understand that you are not pessimistic and that you are hopeful about Fidia, but as a reminder, Fidia themselves made an announcement that we cannot expect a viable product for at least another year. That is not as short of a period of time as you make it out to be.

I was just trying to provide information to those who are interested in dosing themselves with equol now. We know from experience that addressing the DHT issue is paramount to stopping hairloss. Otherwise the majority of people who do not want to use finasteride would just use a vasodialator like minoxidil and expect lasting results. So in the current situation, other than Merck's 5ARIs, equol is one of the few alternatives. This was the basis for my post.

I just want to end by saying that I appreciate the time you took to respond to my post and that my intent wasn't to suggest that people stop making memes and "be productive." I only meant that lightly. I like the memes and if you want to meme and wait, more power to you! I completely understand. You know, there are those online who have made their own finasteride topicals as well as RU58841. Compounding something simple at home is neither unreasonable nor destined to fail - people have shown results with the two aforementioned substances with a simple ethanol vehicle.

 

[inmyhead]

You know, I will have to respectfully disagree with almost everything you said.

I understand the inherent instability of liposomes and the magnitude of the problem of finding a formulation for a product expected to sit on store shelves for on the order of months at room temperature or perhaps warmer conditions without degrading. But in my post, I actually never discussed making any type of liposomal formulation, let alone reproducing Fidia's lotion. In fact, the very reason that I specifically restricted the discussion to simple vehicles only is that I agree with you. I too think it is too difficult of a problem to formulate stable liposomes at home. Unsaturated lipids will hydrolyze. SUVs will not remain small for extended periods of time. So to me, the majority of your rebuttal doesn't really seem germane.

Firstly, the basis of liposomes is to improve the uptake of a topical drug. Brotzu has not discussed or shown that the use of liposomes prevents systemic absorption of the drugs within his formulation. Secondly, I am well aware of the efforts on Ieson to reproduce the lotion. If you read through the posts, some users report some degree of improvement or change that occurs within the first few weeks before the lotion no longer appears to function. Again, it wouldn't be surprising if that homebrew solution was unstable. If you look at Brotzu's lotion, the primary solvent is water. If the liposomes fail, you effectively have NO vehicle because neither equol nor DGLA will be very water soluble. A failure of the liposomes doesn't just reduce the lotion's efficacy - it is catastrophic. Considering the first and second points, I therefore discuss the potential use of DMSO as a vehicle to get the job done because it is well known for enabling transdermal delivery. Ethanol is an option too as always.

Secondly, I understand that you are not pessimistic and that you are hopeful about Fidia, but as a reminder, Fidia themselves made an announcement that we cannot expect a viable product for at least another year. That is not as short of a period of time as you make it out to be.

I was just trying to provide information to those who are interested in dosing themselves with equol now. We know from experience that addressing the DHT issue is paramount to stopping hairloss. Otherwise the majority of people who do not want to use finasteride would just use a vasodialator like minoxidil and expect lasting results. So in the current situation, other than Merck's 5ARIs, equol is one of the few alternatives. This was the basis for my post.

I just want to end by saying that I appreciate the time you took to respond to my post and that my intent wasn't to suggest that people stop making memes and "be productive." I only meant that lightly. I like the memes and if you want to meme and wait, more power to you! I completely understand. You know, there are those online who have made their own finasteride topicals as well as RU58841. Compounding something simple at home is neither unreasonable nor destined to fail - people have shown results with the two aforementioned substances with a simple ethanol vehicle.

yes equal is really quite interesting, but it's quite hard to make it work for us

 

[MomoGee]

I am just here for sh*t posting

 

[ironix]

Did the memes broke this site? I literally tried to scroll for 2 minutes to reach the last post.

You know, I will have to respectfully disagree with almost everything you said. [...] Compounding something simple at home is neither unreasonable nor destined to fail - people have shown results with the two aforementioned substances with a simple ethanol vehicle.

Like I said, i appreciate the effort you took to provide those informations and if anyone wants to test the lotion for themself and do some experiments you had some good and useful ideas. I just think that you made it look a bit too "easy" which could also lead to false hope and I wanted to add a few points to keep expections at a realistic level. Also the idea about making our own lotion at home was already discussed a few times here and nobody really made his own lotion. Probabely because it would need a lot of time and money and has a good chance to fail.

Considering the first and second points, I therefore discuss the potential use of DMSO as a vehicle to get the job done because it is well known for enabling transdermal delivery. Ethanol is an option too as always.

They had to use lipsomes to penetrate the skin and reach the hair follicle. I remember that I read somewhere that ethanol alonen wasn't capable to work as a vehicle for equol and/or dgla because they were not able to penetrate the skin. I don't know anything about DMSO so maybe this is a new option.

As a reminder, Fidia themselves made an announcement that we cannot expect a viable product for at least another year. That is not as short of a period of time as you make it out to be.

Unfortunately I'm aware of this news but this does not mean that we don't get some news about the functionality of this lotion from fidia this year. I think a lot of people really wanna know if the lotion works and if it is a potential replacement for fina/minoxidil.

I was just trying to provide information to those who are interested in dosing themselves with equol now. We know from experience that addressing the DHT issue is paramount to stopping hairloss. Otherwise the majority of people who do not want to use finasteride would just use a vasodialator like minoxidil and expect lasting results. So in the current situation, other than Merck's 5ARIs, equol is one of the few alternatives. This was the basis for my post.

Equol does really seem to be an option for adressing the dht problem but Brotzu also mentioned in his patent that equol or dgla alone are "useless" for hairloss and they only work in combination with eachother. Just to add equol in combination with a vehicle does probabely not work.

 

[shookones]

One more alleged year before it comes out!

 

[supersaiyannorwood6+]

duuuuude, I can't freaking wait, all hail Brotzu!!

 

[abcdefg]

Why would equol alone be worthless? So if equol alone is worthless does that mean this lotion if it worked would still need everyone to continue taking finasteride? If this lotion doesnt stop DHT or doesnt do it well enough your always going to have better results keeping finasteride on top of this.

"Equol does really seem to be an option for adressing the dht problem but Brotzu also mentioned in his patent that equol or dgla alone are "useless" for hairloss and they only work in combination with eachother. Just to add equol in combination with a vehicle does probabely not work."

 

[Afro_Vacancy]

Equol does really seem to be an option for adressing the dht problem but Brotzu also mentioned in his patent that equol or dgla alone are "useless" for hairloss and they only work in combination with eachother. Just to add equol in combination with a vehicle does probabely not work.

What I recall reading was that removing equol from the lotion reduces effectiveness by ~40%, not by 100%.

So PGE1+L-Carinitine would by itself be very useful.

 

[d3nt3dsh0v3l]

What I recall reading was that removing equol from the lotion reduces effectiveness by ~40%, not by 100%.

So PGE1+L-Carinitine would by itself be very useful.

See I interpreted that differently. Brotzu hasn't done long term studies from what I can tell. Even minoxidil should show an improvement in hair within a year, right? But we know from experience that a vasodialator alone will not halt the rate of progress of hairloss - it may only give you a buffer. So when he mentioned a 40% change in efficacy, I interpreted that as change in how quickly the hair improves, or how thick the shaft diameters get, not necessarily the effectiveness of halting the actual male pattern baldness process. Basically, we know that finasteride+min>finasteride alone. That's how I read it.

 

[d3nt3dsh0v3l]

Like I said, i appreciate the effort you took to provide those informations and if anyone wants to test the lotion for themself and do some experiments you had some good and useful ideas. I just think that you made it look a bit too "easy" which could also lead to false hope and I wanted to add a few points to keep expections at a realistic level. Also the idea about making our own lotion at home was already discussed a few times here and nobody really made his own lotion. Probabely because it would need a lot of time and money and has a good chance to fail.

This is true. I will have to agree that the approach I chose is really simple. It's the cheapest/easiest thing I could think of that "may" work, given that others have used ethanol to make topicals and that equol is readily soluble in ethanol. Very true that it may not work. As far as time and money go, I think actually that the ingredients are not that cheap but I mean they're within reach (~$70/month-ish). But yeah as I mentioned, you'd have to do it for 9 months before you even know for sure that it isn't doing anything and that's pretty annoying. I just figured that if there are people taking RU58841, they may be interested in trying equol too.

They had to use lipsomes to penetrate the skin and reach the hair follicle. I remember that I read somewhere that ethanol alonen wasn't capable to work as a vehicle for equol and/or dgla because they were not able to penetrate the skin. I don't know anything about DMSO so maybe this is a new option.

It's true that liposomes improve delivery. I haven't read anything about ethanol not working or not being able to penetrate the skin though. I know other drugs like estradiol can be delivered with an ethanol vehicle because they are lipophilic so they can go in. Now if you check out Brotzu's patent on the other hand, he mentions difficulty with PGE1 because it is really unstable.

"Such compositions are delivered in the form of liposomes, which had already demonstrated to be valuable carriers for PGE1 for systemic or local treatment of vascular diseases and their cutaneous outbreaks (ulcers). For example, WO 2011/095938 discloses unilamellar liposomes, encapsulating PGE1 and/or PGEl- -cyclodextrin in association with L-propionyl-carnitine for the treatment of vascular diseases in diabetic subjects.

Encapsulation in liposomes is not able to increase the very poor stability of PGE1, though; the findings of WO2013171668 in fact, must be freeze-dried or, if in suspension, stored at low temperature (about -20°C) up to the time of use, if one intends to prevent the almost complete oxidation of PGE1."

Brotzu spent the majority of his time trying to make a PGE1 topical for diabetic patients. My interpretation of this is that because PGE1 is easily oxidized, he HAD to try to use liposomes to deliver it. And in his DGLA patent, he says even that didn't work. It's very possible that liposomes deliver equol better than ethanol. But I am saying it is also possible that Brotzu chose to even mess around with liposomes to begin with not because of efficacy issues with equol (he wasn't even using equol in the beginning), but because PGE1 is really hard to deliver and he was trying to figure out how to do it. Only recently did he figure out he can swap PGE1 for DGLA and that equol offers additional benefits (his PGE1 patent never mentions equol).

Also regarding DMSO...I don't know... some suggest that long term use can be bad because it has some toxicity so tentatively I say just rule it out as an option since this would be a long term treatment anyway. Nobody should risk getting hurt. But people on amazon buying DMSO seem to be addicted to it, lol.

Unfortunately I'm aware of this news but this does not mean that we don't get some news about the functionality of this lotion from fidia this year. I think a lot of people really wanna know if the lotion works and if it is a potential replacement for fina/minoxidil.

Fair enough. You're right - it would be really, really useful to see some goddamn efficacy data.

Equol does really seem to be an option for adressing the dht problem but Brotzu also mentioned in his patent that equol or dgla alone are "useless" for hairloss and they only work in combination with eachother. Just to add equol in combination with a vehicle does probabely not work.

Actually I just read through the patent again now and it does not say anything about equol being useless alone - he never made a lotion with equol alone. Here is the summary:

Lotion A: Has DGLA, L-propionylcarnitine, and equol. This is "the" main formulation in the patent
Lotion B: Has PGE1, L-propionylcarnitine, and equol. This is an "old" formulation.
Lotion C: Only PGE1.
Lotion D: Only DGLA.

Conclusion: Lotion A shows the best performance, lotion B is second place, lotion C and D show minimal improvement.

So again, it sounds actually like equol is doing a bunch of the work. There is synergy I'm sure, but I don't see how one can expect results without addressing the DHT problem, in this case by using equol. The results seem to agree with that logic. That was sort of the rationale for me post about maybe using a homemade equol topical. If people have a few hundred to burn and time...it might be possible. I know the ethanol vehicle isn't the best. But it might not be that bad either. I would be surprised if it just delivers 0, but I'm also open to being surprised as I don't know the real answer.

 

[MrJolly16]

The answer I want right now is: will beps come back again?

I think this radio silence has lasted long enough and we still need information.

 

[mr_robot]

S-Equol has a similar atomic weight to Minoxidil and considering it has easily soluble (200mg/ml) in ethanol I don't think penetration is an issue. What is an issue is cost, S-Equol is not cheap and if you can increase absorption by encasing in a liposome then that is what you will do. Same with DGLA, both of these ingredients are very expensive before you take into account stability factors.

 

[d3nt3dsh0v3l]

S-Equol has a similar atomic weight to Minoxidil and considering it has easily soluble (200mg/ml) in ethanol I don't think penetration is an issue. What is an issue is cost, S-Equol is not cheap and if you can increase absorption by encasing in a liposome then that is what you will do. Same with DGLA, both of these ingredients are very expensive before you take into account stability factors.

But Mr. Robot you're already using equol from equelle, right?

The dosage for a topical will likely be in the ballpark of 10mg/ml.
At $60 for 112 caps at 2.5 mg/cap = 280 mg potentially extractable from a month's supply of Equelle.

 

[Follisket]

Just how expensive are we talking about here?

I mean regardless of how the Brotzu lotion pans out (a million other things besides efficacy could go wrong), the s-equol angle alone deserves to be explored properly. So how have we still not found an affordable source for it? It's not like it needs to be cheap enough for everyone to use from the get-go - just about affordable enough for a handful of us to try it.

You know, if it works, it might generate enough interest to organize group buys and get some large scale production going.

But obviously, we'd need to make sure we're doing it under optimal conditions and for that we'd need to mobilize the science-savvy posters around here.

It would be crazy to just pass up on this when a safe maintenance treatment could be right under our nose.