Personally I use it for healthy gums and to prevent age related gum recession. I only use it with an electric toothbrush to massage my gums. I use baking soda for my teeth.
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Has anyone else tried to make the repigment concoction? I now realize that ordering small sizes of tacrolimus and cyclosporin was a probably a mistake: opening them proved extremely difficult because the capsules were so tiny - like one eighth of an inch.
I am about to order my medications for this formulation. Was planning on similar to what @Radiata ordered:
Cyclosporine 25 mg, 7 strips
Tacrolimus 0.5 mg, 7 strips
Minoxidil 10 mg, 300 total pills
But - what size tacrolimus and cyclosporin did you buy? I’m going to order in the next day or two. What would you recommend?
I see cyclosporin typically comes in 25mg, 50mg or 100mg capsules.
And Tacrolimus comes in .5mg, 1mg and 2mg capsules.
It sounds like you would suggest the largest capsules available - is that correct?
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I had the most trouble with 1 mg tacrolimus. They are tiny -presumably to ease swallowing. I couldn’t pry the capsules apart with my fingers. I finally settled on holding the larger side with a small forceps and cutting the smaller side with a scalpel. But the powder went everywhere. I would order very large next time and hope they are easier to pull apart. Then there is the added problem of measuring the correct amount - you’ll need a fairly accurate scale down to .5 gm.The cyclosporine is a liquid also in a sealed capsule, also teeny tiny. I cut the ends off in a beaker so the liquid would stay contained. I think larger would be better for holding and extracting the liquid but you’ll also have to measure quantities. The minoxidil is no problem -it’s a tablet easily crushed by hand or with a grinder.
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I went with 25 mg capsules for Cyclosporine, 0.5 mg for tacrolimus, and 10 mg for minoxidil. My thinking was that for a single bottle of 100 ml solution of 2% minoxidil, you’d need:
Cyclosporine: 125 mg (5 capsules)
Tacrolumus: 2.5 mg (5 capsules)
Minoxidil: 200 mg (20 capsules) (500 mg for a 5% solution)
This was the closest way I could get close to the paper quantities, which for a 100 ml solution would be:
Cyclosporine: 120 mg
Tacrolumus: 2.4 mg
Minoxidil: 500 mg (5% minoxidil solution)
This way, you would not need to accurately do partial pills, like if you had bought 2 mg tacrolumus capsules, or larger cyclosporine. A lot of minoxidil is needed, so I went with the biggest pills possible.
I ordered mine at the end of October and it still hasn’t arrived, though Kachhela definitely sent it. Tracking shows that it’s stuck in NY and hasn’t moved in nearly a month, so it’s either been lost or confiscated, though I haven’t received a notice of confiscation. I’m wondering if 300 minoxidil pills was too many. Overall it wasn’t expensive, so I figured ordering a year’s worth of pills for solution would be the way to go. It might be better to order a smaller quantity and just accept more frequent shipping costs. The other possibility is that I just got unlucky and was in the 3% of confiscations mentioned in the “how to order” post.
I’m debating reordering the same quantity or ordering a reduced quantity. I suppose not many people have tried ordering large quantities of minoxidil from India like they have rapamycin. Do you think I was unlucky, or they didn’t like the quantity of minoxidil?
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To have a better formula of RiverTown topical solution, recently I searched some papers on how to make topical drugs, but I think I lack the general knowledge, I am going to read the following 2 books to enhance my knowledge on it.
-
Cosmetic formulation: principles and practice 2006
Heather A.E. Benson (Editor), Michael S. Roberts (Editor), Vania Rodrigues Leite-Silva (Editor), Kenneth Walters (Editor) -
Cosmetic Formulation of Skin Care Products 2021
Zoe Diana Draelos(Editor), Lauren Thaman-Hodges (Editor)
I don’t know if these 2 book are good or not, I also afraid if 2006 is out of date, if anyone has read any of them, it would be great to hear your book review, and if anyone can give recommend book lists, I will appreciate it.
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A robust preview of the full-text of the first title is available on GoogleBooks.
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For people doing the deep research into chemical formulation, biology, cosmetic dermatology, etc. and want to get a look at the good academic textbooks … the woman who created the website that hosts all the world’s research papers (https://sci-hub.wf ), well, she’s also created a similar site for science textbooks like the one mentioned above.
Like the site for research papers, this is a pirate website, and it has all the same issues around it - the books are being shared for free, the authors are not being compensated for their hard word in writing the books, so lots of ethical considerations to think about. I support authors and I do buy books when I need them. But I also tend to think that if you would never buy the book because you can’t afford it, or if you just want to see if it has any helpful information (e.g. for formulation of this type of topical formula), them maybe its use is justified. I’ll let you make your own decision. The site is: https://libgen.rs
As an example, the “Cosmetic Formulation” book is available there:
More info:
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Based on this info, magnesium stearate is soluble in hot ethanol. The boiling point of ethanol is about 78 C, and the melting point of tacrolimus is 126 C. If dissolving the crushed tacrolimus pills ends up being an issue when mixing the formula, then it stands to reason that we should be able to heat the ethanol to near boiling, mix the tacrolimus (and magnesium stearate) in to dissolve, and not risk harming the tacrolimus. The tacrolimus should dissolve in the ethanol.
@Radiata Just found your post, my tacrolimus pills can’t dissolve in the minoxidil solution, thanks for the information, I will heat it to see if tacrolimus can dissolve in it.
Update:
I am not familiar with drug industry, I think there are 2 cases when we put the tacrolimus pills in the cold ethanol:
- tacrolimus dissolves in the ethanol, but magnesium stearate remains insoluble in the ethanol.
- tacrolimus is firmly compressed with magnesium stearate, because magnesium stearate can’t dissolve in the cold ethanol, both can’t dissolve in the cold ethanol.
Which one is correct?
Here is a formula for 0.1% Tacrolimus, but it didn’t mention the heating process, I am curious if dissolving those magnesium stearate necessary or not?
https://www.uspharmacist.com/article/tacrolimus-01-topical-microemulsion-43011
Method of Preparation: Calculate the quantity of each ingredient for the amount to be prepared. Accurately weigh or measure each ingredient. Mix together the propylene glycol (PG), polysorbate 80, Brij 30, isopropyl myristate, and tartaric acid solutions. Add the tacrolimus and purified water; mix well. Package and label.
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I still have not been able to try this because I still haven’t received my shipment so I’m basing all my assumptions on the data sheets I read.
Did you first crush up the pills? This would increase the surface area and probably help it dissolve. Otherwise it might take a long time to dissolve or just not dissolve at all.
Since the melting point of tacrolimus is 126 C, I’d assume that once the magnesium is dissolved, the actual tacrolimus would be undamaged but in the solution. Remember, the actual amount of tacrolimus in each pill is only about 0.5 mg, whereas the entire pill is probably something like 10-20 mg, so what you’re seeing is mostly magnesium stearate.
What I would do would be to heat only the ethanol portion of the solution to near boiling (78 C), and try to dissolve the crushed up tacrolimus pills. Then you can add the ethanol solution to the water + glycol and mix in the crushed minoxidil and cyclosporine.
The tacrolimus 0.1% formula is likely referring to an ointment that was made by a legitimate lab, so they probably would be starting with pure tacrolimus in a power form rather than crushing up pills, as well as having several processing steps.
The paper seems to indicate that both the minoxidil and cyclosporine are needed for this to work, so I wouldn’t expect one of the tacrolimus ointments alone to do anything.
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I expect the cyclosporin to be superfluous as both it and tacrolimus are both calcineurin inhibitors…
I dissolved tablets into DMSO slowly and then decanted the solution to get rid of the titanium dioxide, but it took perhaps a couple of weeks to finish off.
Why would they include both in the formulation (and patent) if you don’t need both of them? It would seem unusual to do this.
It may make the patent stronger.
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That seems unlikely. Here is an example from this year of a very successful patented product using two generic compounds:
Amylyx’s drug is a combination of generic compounds sodium phenylbutyrate and taurursodiol that work together to prevent nerve cells in the brain and spinal cord from dying prematurely.
Amylyx - Went public this year, current market cap is $2.4 Billion. It is based on the unique combination of two generic / supplement compounds being combined and packaged together for treatment of ALS.
Heating ethanol to dissolve stearate won’t help. Once solution cools down, magnesium stearate would undissolve again and come out of ethanol. Isn’t that so ?
I thought I would provide a copy of a photo which shows that increasing gene expression provides pigmented facial hair where no facial hair has grown previously. This is with a default phenotype that otherwise generates white hair.
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That is encouraging. I have plenty of hair but its nearly all gray.
It appears that only when old follicles have regenerated does this color change occur, and that there is no pigmentation change in already functional hair follicles. Is that how you see it?
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I think that’s essentially the case. Follicles generating strong white hair stay white. Those with pigmented hair stay pigmented. The point is that the local biochemistry of follicles varies. Those with the stronger environment start strong pigmented hair, the weakest produce frail white hair.
My belief is that gradually the local environment will improve for the bad areas and they will switch to pigmented, but to speed that up requires risks I am unwilling to take.
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So has everything that supposedly changes pigmentation been included in your mix?
One thing probably not included was bimatoprost. Expensive, and I havent seen any reports from users. I might try on my eyebrows.
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