Making topicals - reasons and methods

CCS

Senior Member
Reaction score
27
The point of topicals is to give your scalp first shot at the meds before your prostate hogs it all and your body gets side effects. While everything you put in your scalp eventually will probably get to the rest of your body, you can treat your hairs and make sure that DHT inhibitors take a few 5AR's with them when they go to your body, thereby reducing side effects.

1. Pores are the highways for topicals. Many topicals can penetrate skin, but entry through the pores is much faster. This is why rats absorb more than humans and the scalp absorbs more than your hands. (sorry guys with near shiny heads)
2. Liquids are almost always absorbed better than solids no matter how thin the solid is. And if the solid is thick, any part not touching the skin (like the second layer of solid and everything above it up to the surface of the solid) is not going to enter the skin. Pastes are very similar.
3. The contact time is also a factor. If the liquid dries up in 2 minutes, that means the active ingredient had only 2 minutes to penetrate the skin. I hope it all went in. The reason minoxidil should be left on for 4 hours is so it has more time to enter, though about 75% of the amound that will enter has entered after 2 hours.
4. The drug must be soluble in the carier vehicle (the liquide you are using). If it is not, you just won't get it on, or the active ingredients will be solid.
5. The higher the concentration and amount of drug you use, the more that will go in until the scalp is saturated, but also the lower the percentage of the total drug that will make it in. If you use 1mg/mL and 80% goes in, then perhaps if you use 30 mg/mL only half will go in, but you still get 15mg instead of 0.8 mg.
6. Mixtures of liquids evaporated faster than pure liquids, and solutions of dissolved solids evaporate slower than their pure liquids. The higher the boiling point of a liquid, the slower it evaporates. So isopropyl alcohol is slower than ethanol, and water is slower than isopropyl, and propylene glycol is slower than water, and glycerol is slower than propylene glycol, and a water/ethanol misture is slower than pure ethanol but faster than water, and (at 50%) is closer to the ethanol's rate than the water's.
7. If you put a think topical on your head, only the part in contact with yoru scalp will be absorbed, and this layer is thin. In order for the rest of the active ingredients to enter, they must diffuse through the past to the surface of your skin, and this is extremely slow if the past is thick or the active ingredient is not soluble in the paste. It is like trying to walk from new york to san fran before your next show. The only benifit is their is a little time release if you leave it on for 12+ hours, but it will probably dry by then and be useless. This is why I strongly recommend liquids.
8. The ingredients I listed are generally safe. Infact, the glycerol in dutasteride is safe enough to swallow that small amount. If you leave your arm in a vat of isopropyl alcohol for an hour, you'll absorb enough to make you sick. However, the amount used on your scalp is probably OK.
The alcohol in Rogaine is ethanol, the same stuff in beer. Because of my inability to know which liquids will go through the scalp, I recommend you stick to rogaine and 70% isopropyl alcohol. Do not use the kind of rubbing alcohol that is ethanol with some methanol. Not only will it evaporate faster, the methanol is more toxic than isopropyl alcohol, though is thought generally safe at this low dose.
9. I don't know why minoxidil is absorbed or how much is aborbed, and why propylene glycol does not go through the skin (at least in large amounts). Molecule size is not the only facter here. However, I do know that 4g of a 12g testosterone patch will go through the skin near a blood vessel in 23 hours. I also know that Dutasteride and Finasteride are similar to testosterone (this is how they fool 5AR to grab them instead of Testosterone. do a google image search to see the similaries), and that both do penetrate the skin. I do not know how much could make it through.
10. To make topical dutasteride, squirt a few capsules in Rogaine or 70% isopropyl alcohol. To make topical finasteride, thurough grind proscar, wet with rogaine, grind some more, mix in with rogaine or alcohol, shake well, let pill particles settle. If it is powder and there are no chucks, most of the finasteride should be disolved. Pour off the liquid into another rogaine bottle and try to leave the chucks behind, as they will interfer with absorption on your scalp. I recommend 0.5 - 6 pills per month, depending on what side effects you get.
 

Bryan

Senior Member
Staff member
Reaction score
42
collegechemistrystudent said:
7. If you put a think topical on your head, only the part in contact with yoru scalp will be absorbed, and this layer is thin. In order for the rest of the active ingredients to enter, they must diffuse through the past to the surface of your skin, and this is extremely slow if the past is thick or the active ingredient is not soluble in the paste. It is like trying to walk from new york to san fran before your next show. The only benifit is their is a little time release if you leave it on for 12+ hours, but it will probably dry by then and be useless. This is why I strongly recommend liquids.

I know it's probably starting to seem like I'm playing "Devil's Advocate" with a lot of your posts ( :) ), but for an interesting study that seems to disagree with your claims above, read the following:

http://www.geocities.com/bryan50001/spironolactone.txt
(spironolactone creams versus spironolactone solutions)

I quote extensively from a study on topical spironolactone by a famous hair researcher (Dr. Roger Rittmaster), who did some testing that found that a cream vehicle was more effective than an alcoholic vehicle. Check it out!

Bryan
 

Old Baldy

Senior Member
Reaction score
1
Bryan said:
collegechemistrystudent said:
7. If you put a think topical on your head, only the part in contact with yoru scalp will be absorbed, and this layer is thin. In order for the rest of the active ingredients to enter, they must diffuse through the past to the surface of your skin, and this is extremely slow if the past is thick or the active ingredient is not soluble in the paste. It is like trying to walk from new york to san fran before your next show. The only benifit is their is a little time release if you leave it on for 12+ hours, but it will probably dry by then and be useless. This is why I strongly recommend liquids.

I know it's probably starting to seem like I'm playing "Devil's Advocate" with a lot of your posts ( :) ), but for an interesting study that seems to disagree with your claims above, read the following:

http://www.geocities.com/bryan50001/spironolactone.txt
(spironolactone creams versus spironolactone solutions)

I quote extensively from a study on topical spironolactone by a famous hair researcher (Dr. Roger Rittmaster), who did some testing that found that a cream vehicle was more effective than an alcoholic vehicle. Check it out!

Bryan

Also:

From: Peter H. Proctor - view profile
Date: Sun, Sep 24 2000 12:00 am
Email: pproc...@proctorgamble.com (Peter H. Proctor)
Groups: alt.baldspot
Not yet ratedRating:
show options


Reply | Reply to Author | Forward | Print | Individual Message | Show original | Report Abuse | Find messages by this author



In article <8qkg5o$3i...@nnrp1.deja.com> needmoreh...@my-deja.com writes:
>From: needmoreh...@my-deja.com
>Subject: Liquid Retin-A helps more than cream? Dr P?
>Date: Sun, 24 Sep 2000 09:06:05 GMT
>I started using liquid retin-A 2 months ago. And now I am starting to
>see fine vellus hair on temples (I can't really tell if this is good or
>just that my hair line might actually be moving back so what was once
>thick hair is now vellus?!?!!?) but it seems good to me.
>I had been using liquid retin-A for about 2 years over a year or two
>ago. Then I stopped and used the cream form. Is it possible at all that
>liquid retin-A helps me more than cream?!?! Maybe cause of the solvent?


It is possible that you are loking at some sort of vehicle affect.


>Any thoughts at all? Am I just absorbing more with this liquid form
>than cream? Since my hair still have full coverage, Cream is REALLY
>hard to be worked into all my scalp area. Liquid on the other hand goes
>to all scalp area better.


Skin penetration of drugs is generally significantly better from cream
vehicles than from liquid ones. This is an important reason most skin
drugs come in cream vehicles.



>So is it the solvent? Is it the liquid ability to reach more area? Is
>it my imagination? Is it something else?[


Don't know.


>Dr. P, any experience with patients who respond to liquid retin-A
>better than cream? Should it make a difference?


Don't know. Retin-A alone seems to be a hair-growth -stimulator, at
least in moderate amounts. But I never use it by itself, so I cannot
comment on it.

Peter H. Proctor, PhD, MD
http://www.drproctor.com
 

CCS

Senior Member
Reaction score
27
I'll look this over in more detail in a second. But my first guess at what is going on here is that the cream works better because it has a lot more active ingredient than the liquid. I did not say that testosterone patch delivers less testosterone than a minoxidil dropper delivers DHT. I just said that the ratio of the amount absorbed to the amount on the skin is higher with the liquid, and then used the 1/3 absorption of the scream patch as a lower estimate for the ratio, not the amount.

Now that that is said, I'll read the links and the posts and see if equal amounts of active ingredients are being compared. Thanks for pulling up those older posts for me oldbaldie.

And one more quick comment: 25 proscar pills have only 0.125g of active ingredient that is maybe 1% of the mass. I doubt this is nearly true of a 12g testosterone patch.

OK. Now I will read the link.
 

CCS

Senior Member
Reaction score
27
they are both 1%. That cream looks pretty liquidy from the ingredients, but maybe that is normal. The dissolved petroleum jelly and mineral oil slow evaporation for longer exposer times, but are dissolved enough for mobility. This is not a paste, which I still say would work worse.

Clearly the cream did better, from the results.

As for the liquid, does "41.5% ethyl acohol, water" mean 41.5% of each? Ethyl alcohol does evaporate fast. A problem I see in Eucapil is the pure isopropyl alcohol evaporates in 2 minutes, so I question the absorption rate.

Minoxidil has propylene glycol in it primarily to make the skin more permeable (causing irritation is some people), though its high boiling point also slows evaporation. the alcohol base solution did not have any propylene glycol, whereas the creme had 13%. I think that played a factor. Minoxidil has 50% propylene glycol.

I think that cream was much closer to an ideal liquid than a paste. I don't know what is going on at the microscopic level when they rub it in. Interesting.
 

Bryan

Senior Member
Staff member
Reaction score
42
collegechemistrystudent said:
I'll look this over in more detail in a second. But my first guess at what is going on here is that the cream works better because it has a lot more active ingredient than the liquid.

Nope. Sorry. They were the same concentration in both the cream and the solution.

Bryan
 

Bryan

Senior Member
Staff member
Reaction score
42
Oops! You beat me to it!
 

Bryan

Senior Member
Staff member
Reaction score
42
collegechemistrystudent said:
Minoxidil has propylene glycol in it primarily to make the skin more permeable (causing irritation is some people)...

Well, you wouldn't even be able to HAVE a 5% minoxidil solution, without the propylene glycol. The maximum solubility of minoxidil in pure ethanol is only about 2.9%, while it dissolves to about 7.5% in pure propylene glycol. So its role as a solvent in Rogaine is critical, for all those users out there who play the minoxidil "Numbers Game"! :)

Bryan
 
G

Guest

Guest
collegechemistrystudent wrote:
Minoxidil has propylene glycol in it primarily to make the skin more permeable (causing irritation is some people)...


Well, you wouldn't even be able to HAVE a 5% minoxidil solution, without the propylene glycol. The maximum solubility of minoxidil in pure ethanol is only about 2.9%, while it dissolves to about 7.5% in pure propylene glycol. So its role as a solvent in Rogaine is critical, for all those users out there who play the minoxidil "Numbers Game"! Smile

Bryan does that mean 92.5% of minoxidil is waisted in pure propylene glycol. I probably did not understand it correctly, but when you write minoxidil dissolving about 7.5%, what about the other 92.5%?

Music23
 

hairwegoagain

Senior Member
Reaction score
6
Music23 said:
Bryan does that mean 92.5% of minoxidil is waisted in pure propylene glycol. I probably did not understand it correctly, but when you write minoxidil dissolving about 7.5%, what about the other 92.5%?
Music23

No. It means that only 7.5 parts of minoxidil can be dissolved in 100 parts of total solution, i.e. 7.5 parts minoxidil to 92.5 parts propylene glycol. Any further minoxidil will not go into solution, and will exist in its solid crystalline state.

An analogy is table salt in water. Past a certain amount, the solution becomes saturated and will not dissolve further salt. Salt added over this saturation point simply sinks to the the bottom of the container.
 
G

Guest

Guest
Music23 said:
Quote:

Bryan does that mean 92.5% of minoxidil is waisted in pure propylene glycol. I probably did not understand it correctly, but when you write minoxidil dissolving about 7.5%, what about the other 92.5%?
Music23


No. It means that only 7.5 parts of minoxidil can be dissolved in 100 parts of total solution, i.e. 7.5 parts minoxidil to 92.5 parts propylene glycol. Any further minoxidil will not go into solution, and will exist in its solid crystalline state.

An analogy is table salt in water. Past a certain amount, the solution becomes saturated and will not dissolve further salt. Salt added over this saturation point simply sinks to the the bottom of the container.

Thnx for the explanation!
 

Bryan

Senior Member
Staff member
Reaction score
42
hairwegoagain said:
Music23 said:
Bryan does that mean 92.5% of minoxidil is waisted in pure propylene glycol. I probably did not understand it correctly, but when you write minoxidil dissolving about 7.5%, what about the other 92.5%?
Music23

No. It means that only 7.5 parts of minoxidil can be dissolved in 100 parts of total solution, i.e. 7.5 parts minoxidil to 92.5 parts propylene glycol. Any further minoxidil will not go into solution, and will exist in its solid crystalline state.

What HE said! :)

Bryan
 

CCS

Senior Member
Reaction score
27
Finasteride extraction steps, dose. Topical Dutasteride

My homemade topical finasteride (not the pastes that don't work) is good for people who get side effects from Propecia but might tolerate very small doses or just want a higher concentration to their follicles. Shedmaster wanted more detailed directions, and I think this thread is more on this topic than my original post.

Since 5% minoxidil is close to the saturation point (7.5%), I would not want to risk precipitating more by putting some pill powder in it. Maybe some sugar would dissolve and compete with the minoxidil. The 2% minoxidil should be fine, though.

Step 1:
Cut desired number of pills (see bottom of post) up as many times as is convenient with a pill cutter in 30 seconds or a minute without making a powdery mess or having difficulty. Just make small chunks with the closed top pill cutter so they don't get all over the place.

Step 2:
Dump the chunks in a shot glass or somthing with a small diameter for holding a small amount of fluid. It must be strong enough for grinding.

Step 3:
Add a few drops of 70% isopropyle rubbing alcohol to the chunks. This helps them break and keeps chunks from flying.

Step 4:
Use the handle of fat handled fork (one of those with plastic handles you can get at a 99 cent store) or some other medium hard, non-porous, rounded rodlike object that fits in the vial or shot glass but is not hard enough to scratch the glass. Very important if you don't want to get cut. Plastic is better.

Step 5:
Use that handle to grind the chunks up very good. Make a fine powder paste. Any chunks that are not fully crushed contain finasteride that will not get dissolved in the next step.

Step 6a:
If you have a shot glass:
Fill the shot glass half or 2/3 the way with 2% minoxidil or 70% isopropyl rubbing alcohol. (5% might not dissolve it fast or you might loose minoxidil as a powder.) Hold it with one hand and seal the top with the other. Shake vigorously for 10-20 seconds. Put it down and let it settle for however long it takes while you rinse off your hand.
Step 6b:
If you just have a minoxidil bottle and ground the stuff on something else:
Use some 2% minoxidil or 70% isopropyl alcohol to rince the paste into a minoxidil bottle. Wipe and stir up the paste as needed so that you can rinse it off the grinding surface without using more than 1/3 a rogaine bottle volume of 70% alcohol or 2/3 a rogaine bottle of 2% minoxidil to rinse the paste into the bottle.

Step 7: Once it has settled enough that you see powder on the bottom and most of the volume is transparent liquid above it (it helps if used a clear vial or shot glass instead of a rogaine bottel), pour most of the liquid into anther rogaine bottle while being careful not to shake up the powder. You need to leave the behind, though a small amount is OK. If it shakes up, let it settle again, and next time use your rogaine dropper to suck the top off one mL at a time without agitating the powder on the bottom.

Step 8:
Rince the remaining powder down the drain. Probably 90% of the finasteride is now in your bottle.

Step 9:
Add minoxidil 5% or 2% to your new solution, to increase the minoxidil concentration. If you can't handle the 5%, use 2%. If 2% is too strong for you, then you should have just used the 70% isopropyl alcohol. The propylene glycol in rogaine is what irritates your scalp, but it also is what makes absorption go so well. This is a trade off that you will have to decide on. Your bottle now probably has 4.5mg finasteride depending on how well you ground it and shook it. You can dilute this with your other minoxidil or isopropyl alcohol to the amount you can tolerate without side effects.

Dosing:
To probably give your scalp the same finasteride concentation that 1mg/day orally would give, and give your body the same concentration that 0.05mg/day orally would have, the solution you would make from full proscar pill or 5 propecia pill should last you 50 days. Round it to 60 if you want and just dilute the bottle with a fresh minoxidil bottle.
This means you grind proscar or propecia pills per month. Proscar has more finasteride and less filler and will give you better solutions because less will be stuck to the filler.

To probably give your scalp the same finasteride concentration that 20 mg/day orally would give, and give your body the same concentration that 1 mg/day orally would give, whatever solution you made from one full Proscar pill or 5 propecia pills should last you 2.5 days. You need 12 Proscar pills or 4 finasteride pill for one month. It is hard to make less than a bottle, so the topical better not break down in a month. I use 4mL 2x a day, so I can use 3 pills and one bottle for 1 week if I want.

Minoxidil 2% and 5% are available at walmart in the equate brand for $17 for a 3-month supply. Proscar is $85-110 for 30 tablets.

Topical dutasteride is easier. Just squirt 4 capsules into month supply of minoxidil or 1 capsule into a week supply. This amount won't should be very therapudic and is the maximum dose guaranteed not to touch the 5AR1 in your brain. Higher doses are probably safe too.
---------
While 1/3 of testosterone in patches is absorbed, and testosterone is very similar molecularly to finasteride, only 2/3 of finasteride is absorbed in the intestine, and is diluted in the body for systemic effects and used by the prostate, while the hair problem is in the follicle's own DHT production.
-------
Disclaimer/validator
Bryan agrees with me that both topicals are safe, but doubts I have any proof that finasteride or dutasteride are stable in Rogaine or will be absorbed or will not be swept away by the blood before entering the follicles if they are absorbed. I plan to use both topicals in case one is not absorbed, and use them in 1 week batches to reduce the chances of break down, even though I doubt it will occur with the dutasteride.
 

Goingat20

Senior Member
Reaction score
1
Re: Finasteride extraction steps, dose. Topical Dutasteride

collegechemistrystudent said:
Topical dutasteride is easier. Just squirt 4 capsules into month supply of minoxidil or 1 capsule into a week supply. This amount won't should be very therapudic and is the maximum dose guaranteed not to touch the 5AR1 in your brain. Higher doses are probably safe too.

Can you skirt these into Dr Lee's quick drying minoxidil?
Thanks
 

CCS

Senior Member
Reaction score
27
is dutasteride ok in dr lees quick drying minoxidil?

Let me look up the ingredients and I'll tell you. I'm skeptical about anything that is quick drying having significant absorption because of the small amount of time for liquid state transfer. But I am not an expert at all. Fluridil dries in 2 minutes and supposedly is absorbed.

inactive ingredients
PROSCAR (finasteride) tablets for oral administration are film-coated tablets that contain 5 mg of finasteride and the following inactive ingredients: hydrous lactose, microcrystalline cellulose, pregelatinized starch, sodium starch glycolate, hydroxypropyl cellulose LF, hydroxypropylmethyl cellulose, titanium dioxide, magnesium stearate, talc, docusate sodium, FD&C Blue 2 aluminum lake and yellow iron oxide.
The first ingredient, hydrous lactose, can compete with finsteride and minoxidil for dissolution in Rogaine. That is why I don't recommend putting the powder in the 5%, which only can hold 7.5% according to Bryan. Once it is extracted, it can be added.

Anyway, back to your question. could you give me the web site? All I'm getting are forums, not sales sites, on google.
 

CCS

Senior Member
Reaction score
27
i don't see "dr lees" anywhere

This is the same stuff I use, except for three times the price. #500 should work. Like I said, I don't see "quick drying" or "dr lee's" anywhere on the site. The only reason I asked was I wanted to see if there was anything that might react. I still don't know how good it for it to be in water a whole month, but there is water in our bodies and I have not heard it reacts with water. The tablet information just says "keep away from moisture". Maybe that is so the tablet does not fall apart or mold, not for the protection of the active ingredient.
 

CCS

Senior Member
Reaction score
27
my dosing problem

my main issue is if I apply fluridil, will the water in minoxidil 12 hours later destroy the fluridil in my scalp, and will sweating do this too during work outs. And if I order Spectra DNC and use it once a day with minoxidil, do I have to skip one of my topical dutasteride doses that day, or can I put in on after my minoxidil dries and will this cause heavy drying?

I would also like to sprinkle some of my grapeseed extract powder into my minoxidil, but I don't know if it will react with dutasteride or finasteride or min. I know it is stable in ethanol because that is how it gets into wine, so it is also stable in water.
 

Goingat20

Senior Member
Reaction score
1
Ive got a year supply of dr Lee;s, im going to start using four dutasteride capsules in each and see how things go, thanks for your help, youve been very helpful to everyone!
 

CCS

Senior Member
Reaction score
27
stability precautioin

OK, but save one of your empty containers. Fill it one fourth the way with your minoxidil (dr lee's in your case) and squirt one dutasteride in it and use that in one week and repeat each week. This is the same as 4 per month, but it is more cautious. dutasteride should be stable in your rogaine, but just in case something happens over a month, the one week preperations will be fresher.
 
Top