Degradation of Cetirizine in alcohol vehicles!

[jgray201]

Anyone interested see linked study https://www.google.co.uk/url?sa=t&s...FjACegQIBBAB&usg=AOvVaw0Jna0x-Fc3olecR_MZUlvD
Im the first to admit that i often dont understand a lot of the stuff in these studies but surely this puts to bed the idea that Cet cant be used in some way with alcohols. Not only do they mix it with PG, PEG and ethanol. But youll see at the end that there was very little change in the presence of the drug after 3 months. There are other studies similar to this that can be found too.

The studies that show degradation of Cetirizine in ethanol tend to be in the presence of a low PH/acid or some kind of stress testing.

 

[ElTioLaBota]

I never said I was a good responder. I said I saw positive signs which are less burning sensation, sebum control, . and thats a good sign isnt it?I don’t have the regrowth(yet?) some experienced. Maybe few sparse terminals .I use ceti for 68days exactly. so I can’t say yet if it works or not should I see result already? dunno. that said even if I don’t see miracle in coming month that does not mean it won’t work for others. I’ll keep you up to date though. I just apply ceti once a day (1ml) mixed In water after the shower(clean scalp / acid salycilic shampoo for sebum) It makes hair damp obviously and I apply minoxidil on top of it.

If you had to try this or castor oil, which one would you pick first? I have some vellis hairs on the hairline and temples that i want to thicken up, so i'll be starting 1mm dermastamp + one castor oil or ceti.

 

[kiwipilu]

If you had to try this or castor oil, which one would you pick first? I have some vellis hairs on the hairline and temples that i want to thicken up, so i'll be starting 1mm dermastamp + one castor oil or ceti.

I have already tried castor oil oral + topical (dmso vehicle) during months and I never noticed something spectacular. I dunno why because I always have a strict routine and I think some people had success with it....
Anyway I will come to a conclusion with ceti pretty soon. Now it's too early to tell but I might consider another vehicle other concentration, or other anti histamine later.
All in all ceti(antihistamine) approach looks better on paper because you adress the pgd2/pge2 angle while castor oil=pge2. but it's theorical. it's also way easier to apply than castor oil that's always a bonus ; )

 

[ElTioLaBota]

I have already tried castor oil oral + topical (dmso vehicle) during months and I never noticed something spectacular. I dunno why because I always have a strict routine and I think some people had success with it....
Anyway I will come to a conclusion with ceti pretty soon. Now it's too early to tell but I might consider another vehicle other concentration, or other anti histamine later.
All in all ceti(antihistamine) approach looks better on paper because you adress the pgd2/pge2 angle while castor oil=pge2. but it's theorical. it's also way easier to apply than castor oil that's always a bonus ; )

I forgot to mention im also using finasteride.
So castor oil showed no improvement for you?

 

[Jk1]

i have been useing 1pcnt cetrizine oral drops for 1 month.. it stops any itch instantly. hard to tell any effect on hair growth yet?

does it need a pentration enhancer ? would it mix well with stemoxidine ? or should i apply after dermarolling ? or not needed?

if i put too much on i notice i get runny then dry eyes ? so it is getting into the scalp !

 

[jgray201]

i have been useing 1pcnt cetrizine oral drops for 1 month.. it stops any itch instantly. hard to tell any effect on hair growth yet?

does it need a pentration enhancer ? would it mix well with stemoxidine ? or should i apply after dermarolling ? or not needed?

if i put too much on i notice i get runny then dry eyes ? so it is getting into the scalp !

Where do you get your drops from? I think the drops typically have PG and other things in which should help with penetration to the scalp. So it should be fine.

 

[jamesbooker1975]

Where do you get your drops from? I think the drops typically have PG and other things in which should help with penetration to the scalp. So it should be fine.

Yes, It contain PG and Glycerine, both use it on topical lotions .

 

[Jk1]

Where do you get your drops from? I think the drops typically have PG and other things in which should help with penetration to the scalp. So it should be fine.

in australia its sold as zyrtek kids oral drop 10mg per ml i.e 1pcnt over the counter so easy to get... how long before i should see results ? i do think frontal hair is growing faster but no new regrowth yet ??

 

[Maave]

In the very same Patent from Pfizer there's actually an example on how NOT to do it, i.e. mixing Cetirizine and Alcohol and measuring what happens after some time ("Example 1"). They created a tablet which consisted of:

* Tablet Core 450mg (processed with 90mg Alcohol: Ethanol and Isopropyl Alcohol)
+ Membrane Coating yielding 585 mg (processed with 723mg Alcohol: mostly Ethanol and Isopropyl Alcohol, 45mg Glycerin)
+ Cetirizine/Pseudoephedrine Coating yielding 710mg (containing 10mg CET)
+ Taste Mask Coating yielding a total of 730mg for the whole tablet

Note that the alcohols have been marked as "volatile" and do (should?) not exist in the final product. Then they stored those tablets under different conditions and after three weeks they determinded CET degradation into "Cetirizine ester of glycerol" (CEG) relative to the CET peak amount.

Result:

* 50 Degree Celsius / 20% Humidity: 57% CEG
* 40 Degree Celsius / 75% Humidity: 43% CEG
* 5 Degree Celsius: 17% CEG

Thank you for posting this info and the patent number. (US6171618B1) It repeatedly says to use alcohols with over 100 molecular weight

A few seconds of searching gives us our answers

ethanol: 46.07 g/mol
isopropyl alcohol: 60.1 g/mol
propylene glycol (PG): 76.09 g/mol
glycerine: 92.09 g/mol
polyethylene glycol (PEG): betweem 300 g/mol and 10,000 g/mol

So there we go, use PEG. Polyethylene glycol is available in a variety of molecular weights. The weight is usually in the product name like " polyethylene glycol 3350". 3350 is a popular one for whatever reason.

Also the temperature makes a difference. 5C is your fridge temp. So even if you make a mix with ethanol just put it in the fridge and it'll be fine for a week. Heck, save it for all 3 weeks and just use slightly more to compensate.


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There is also some conflicting information about stabilizers.

I found WO2007087344A2, also on google patents. The original PDF with tables is not available unfortunately so some of the data is missing, but it provides excellent hints. Please post if you know where to get the original texts with tables.

Surprisingly, we have discovered a spill resistant cetirizine formulation, containing high levels of low molecular weight polyhydric alcohol that does not form the most common cetirizine formulation degradative products, has a high degree of purity and increased storage time
...
Consequently, one embodiment of the invention allows for antihistamine solutions that have a storage stability of up to 24 months. Another embodiment would allow for a storage stability of up to 36 months
...
The vehicle carrier component comprises propylene glycol up to about 20%, or from about 3 to about 10%. Glycerin up to about 50% may be present. Additionally, sorbitol, up to 10%, may be added as a vehicle and stabilizer. Purified water comprises the bulk of the carrier component comprising from about 29% to about 64% of the formulation.

Yes sorbitol the sweetener. That is the polyhydric alcohol aka sugar alcohol.

Oddly this conflicts with some previous information, PubMed PMID: 20627436 which says

It was found that the carboxylic acid cetirizine readily reacts with sorbitol and glycerol to form monoesters. At a temperature as low as 40 degrees C, more than 1% of the cetirizine content was transformed into a monoester within 1 week using concentrations similar to those used in marketed preparations.

Lemme know what you guys think about the stabilizers.

 

[jgray201]

Thank you for posting this info and the patent number. (US6171618B1) It repeatedly says to use alcohols with over 100 molecular weight

A few seconds of searching gives us our answers

ethanol: 46.07 g/mol
isopropyl alcohol: 60.1 g/mol
propylene glycol (PG): 76.09 g/mol
glycerine: 92.09 g/mol
polyethylene glycol (PEG): betweem 300 g/mol and 10,000 g/mol

So there we go, use PEG. Polyethylene glycol is available in a variety of molecular weights. The weight is usually in the product name like " polyethylene glycol 3350". 3350 is a popular one for whatever reason.

Also the temperature makes a difference. 5C is your fridge temp. So even if you make a mix with ethanol just put it in the fridge and it'll be fine for a week. Heck, save it for all 3 weeks and just use slightly more to compensate.


-------------

There is also some conflicting information about stabilizers.

I found WO2007087344A2, also on google patents. The original PDF with tables is not available unfortunately so some of the data is missing, but it provides excellent hints. Please post if you know where to get the original texts with tables.

Yes sorbitol the sweetener. That is the polyhydric alcohol aka sugar alcohol.

Oddly this conflicts with some previous information, PubMed PMID: 20627436 which says


Lemme know what you guys think about the stabilizers.

This is really interesting and shows it is not as simple as cetirizine cannot be mixed with ethanol/PG etc. Many formulations contain PG and sorbitol and they claim to be stable for years.

I am using a solution which i think is similar to the study with 20% of a cyclo silicone solution and the rest 96% ethyl alcohol. I will start keeping it in the fridge from now. However, i mix every 4 to 5 days so hoping that will help too. Could consider adding sorbitol or some kind of stabiliser but i dont know much about them.

 

[Maave]

I found another patent for a stabilized solution, this time with good measurements. CN102133179A. This one is originally Chinese. The text has been translated but there's a table that is still in Chinese, so you have to make some educated guesses. Table 1 is the various solutions and their ingredients. Table 2 is the stability at 0 months (time of production) and at 6 months.

A stabilized cetirizine oral solutions, characterized by: comprising an 1g cetirizine, propylene glycol 80~100g, sorbitol 360~400g in 1000ml solution.

Composition 7 was by far the most stable and appears to be 1g cetirizine, 80g PG, 370g sorbitol, and the rest is distilled water. Google translate is a little rough:

7 composition, Example 1, when put to Example 6 months, and the content of related substances were no significant changes in the second embodiment.

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The studies that show degradation of Cetirizine in ethanol tend to be in the presence of a low PH/acid or some kind of stress testing.

Yeah the pH of the mixture seems to make a big difference. Study PMC3813251 on NCBI shows this. I wonder if some of the oral solutions fail to neutralize the acidity of their flavorings.

 

[FOLLICLOLZ]

I found another patent for a stabilized solution, this time with good measurements. CN102133179A. This one is originally Chinese. The text has been translated but there's a table that is still in Chinese, so you have to make some educated guesses. Table 1 is the various solutions and their ingredients. Table 2 is the stability at 0 months (time of production) and at 6 months.

Composition 7 was by far the most stable and appears to be 1g cetirizine, 80g PG, 370g sorbitol, and the rest is distilled water. Google translate is a little rough...

I'll see if one of my fluent Chinese colleagues at work can translate.

 

[pizzadriver1933]

It's relatively quite about this topic overall, are the chances for this method to do something so small?

I just ordered the liquid drops. Besides Castor-Oil it's the only thing i'm taking right now then. Will see.

 

[Murkey Thumb]

I would like to see some real proof that this works so far nobody has posted any supporting evidence in the way of pictures.

 

[Maave]

I'll be trying it for about 3 months before getting on anti-androgens (Doctor appt is scheduled 3mo out). I'll take pics. After that the results will be invalidated by the anti-androgens. It would be better if we could see results from someone not on fina/duta.

 

[pizzadriver1933]

Well there is this one guy in this thread claiming to have had results. I wish he would come out again and post some pics or giving a small statusreport on this.

I applied the liquid drops today on my scalp..about 7 or 8 drops and massaged it in... and slowly after i felt super tired and dizzy and had really short breath. The manual says 20 drops for adults a day is alright, and in regards to systemic absoprtion through the skin it's hard to believe it is related.. so this is unlikely a side-effect, but it felt weird and i think i'm just going easy on it now lol.

 

[Nostro100]

I just made a theoretical 2.85~mg/ml batch (20pills, 70ml). Even tho cetirizine is very solvable with water, I think I may lose a bit when let the filler sit in the bottom and transfer the liquid to another bottle. In the past , 1mg/ml worked best at halting my shedding with dermarolling. (then I stopped using it because I got lazy, *because I forgot I had hairlos* because my hair was actually better* )
What I havent figured out yet is the "easiest" part, that is, how to keep the dermaroller in a sterilised environment (and how to sterilise it after each usage). Until now I just have dipped it in a bit of alcohol but I think that's not nearly enough to be acceptably sterilised... I'm thinking about burning it lightly with a lighter. Is that too crazy?

 

[FOLLICLOLZ]

@Maave The only bit of info I've been able to extract from my fluent translator through brief online communication thus far is that mixture 7 was the most stable within 6 months with byproducts generation occurrence at 0.048%... which is about in line with the rough google translation.

I'll be visiting this colleague in person early next week for as much info as I can gather regarding composition, preparation notes, etc.

 

[Maave]

What I havent figured out yet is the "easiest" part, that is, how to keep the dermaroller in a sterilised environment (and how to sterilise it after each usage). Until now I just have dipped it in a bit of alcohol but I think that's not nearly enough to be acceptably sterilised... I'm thinking about burning it lightly with a lighter. Is that too crazy?

Don't use a lighter, it'll deposit soot into the roller which you'll have to clean off. A cleaner flame like a gas stove might work as long as the heat doesn't damage the rest of the roller. I'd just dip it in alcohol and store it in a clean container after. You could get a UV sterilizing lamp but I think that's overkill

 

[Nostro100]

Don't use a lighter, it'll deposit soot into the roller which you'll have to clean off. A cleaner flame like a gas stove might work as long as the heat doesn't damage the rest of the roller. I'd just dip it in alcohol and store it in a clean container after. You could get a UV sterilizing lamp but I think that's overkill

But you keep it in alcohol or just really a alcohol bath? I know or a fact that alcohol alone doesnt kill every single thing. Maybe mix alcohol with salt. Salt kills bad organisms doesnt it?