Extracting Methylphenidate from Generic Concerta to bypass Extended Release Mechanism

[BarcelonaBeijing]

So for some generic methylphenidate hydrochloride pills not using the osmotic pump release system (which is easily bypassed with cutting), it seems quite difficult to defeat the ER. After some research the last few days, I've discovered that this particular generic I'm taking (https://pdf.hres.ca/dpd_pm/00045600.PDF) and likely others, are likely using hydroxypropyl methylcellulose (acronym HPMC and listed in the ingredients) as well as magnesium stearate to slow down the dissipation of the drug. Crushing DOES NOT turn it into IR - I've tried high power blender and taken it and it still lasts 3 hours for me while splitting brand name concerta only lasts 1....

Turns out HPMC can be solvated using alcohol, and methylphenidate dissolves easily in alcohol as well. I tried dissolving the powder in vodka, as apparently some research mentioned you need at least 10% water for this to work, although I am not sure why. On this forum from years ago (https://bluelight.org/xf/threads/ex...g-preparations-such-as-concerta.440279/page-2) people discuss whether ethyl alcohol or methyl should be used. I went with vodka, since it's 40% ethyl, contains water, and is less harmful in theory... but I am a bit concerned as someone pointed out "If you dissolve methylphenidate in any alcohol it will react with the solvent. Methylphenidate + Ethanol -> Ethylphenidate + Methanol" so does that mean I didn't just drink vodka with methylphenidate like I wanted, but rather, methanol with ethylphenidate?
This is so convoluted, can anyone share some perspective here? Would I be better off dissolving the crushed generic methylphenidate in isopropyl alcohol, letting it evaporate, and then dissolving the remainder in water? Bypassing the "HPMC gel matrix" or whatever they've used, 3D printed microscopic particles of HPMC and magnesium stearate surrounding every particle of methylphenidate, seems to be VERY complicated and it seems nobody on earth has figured out a good way to do it.

Help?

 

[Fertile]

You won't get much trans-esterification at RT. It takes energy and the environment won't provide enough.

Ever tried just boiling them in water? HPMC is water soluble (10mg/mL at 20C) but if you JUST seek to make them IR, this is simple and safe. I cannot fond HPMCs solubility in boiling water - but safe to say it's a lot less.

Or just leave it in a glass of water on a radiator.

Yes - it might take a day or two to work, but if you are extracting to IV, I wouldn't be helping anyway. The 'needle barrier' is a big psychological step. Once someone is prepared to shoot 1 drug, they often go on to shoot just about everything. '

 

[BarcelonaBeijing]

Thanks for the reply. I have thought about boiling in water... but I have read that methylphenidate becomes unstable at higher temperatures, and I am not sure if that simply means it becomes a bit less effective (say, a 10% reduction in potency?) or worse, would the molecules potentially break down and become other compounds, not all of which may be safe?
I actually left some powder in water overnight and although it hardly dissolved at all from the looks of it... I drank what was in there a little while ago to see if I get any IR effect. Might be some effect, but still nothing like splitting a genuine concerta (and bypassing its ER mechanism). It really seems like whatever powder they've locked it all into is really at quite a granular level. I am starting to wonder if it is designed to be activated somehow by gut bacteria after it gets out of the stomach... (purely speculation)
I could try the boiling water thing, but do you see any potential problems there with what I mentioned?

 

[Fertile]

Hydroxypropyl Methylcellulose​

Hydroxypropyl methylcellulose (HPMC) belongs to the group of cellulose ethers in which hydroxyl groups have been substituted with one or more of the three hydroxyl groups present in the cellulose ring (Fig. 3.10). HPMC is hydrophilic (water soluble), a biodegradable, and biocompatible polymer having a wide range of applications in drug delivery, dyes and paints, cosmetics, adhesives, coatings, agriculture, and textiles [174–176]. HPMC is also soluble in polar organic solvents, making it possible to use both aqueous and nonaqueous solvents. It has unique solubility properties with solubility in both hot and cold organic solvents. HPMC possesses increased organo-solubility and thermo-plasticity compared to other methyl cellulose counterparts. It forms gel upon heating with gelation temperature of 75–90oC.

So body temperature water is best (top of radiator). The length of the chain gives it all of these different properties but I do not see pH affecting it so at body heat, it should dissolve and get a bit gloopy.

https://ibb.co/SPcCTjC

 

[BarcelonaBeijing]

Interesting. Thank you. It's still a bit over my head, but I am glad I'm getting some kind of insight. Are you a chemist by profession?

 

[Fertile]

I did study medicinal chemistry for 7 years, but that was in the 1980s-1990s so mostly forgotten.

I just follow the obvious fact hat if one can estimate the conditions within the body, it will break down just the same.

I wondered if the pH might need to be altered but it does not seem to be the case, Let me know how you get on.

But never forget that for every injecting opioid user their are 3 injecting speed users. That is a hidden disaster. But since it's quite cheap, these people do not end up arrested and so it isn't seem as a 'social problem' or at least not the way meth was in the 1980s and 1990s.

I've seen a few speed labs and trust me - it's the BEST way to be put off their use. They have got creative. Glass breaks & large (pilot scale) plants are suspicious. So their are a lot of welders getting good at making complete 'sets' from stainless steel. I don't like steel. I KNOW you need it at scale but that's the job of a chemical engineer, a whole different profession and some REAL talent. The BEST P2P ---> methamphetamine with a yield of >97% at RT using only methanol as solvent is from a patent on sertraline synthesis. It truly is an amazing piece of work.

They even use naproxen ($329/Kg) to resolve the active isomers. Then they can concentrate the inactive isomer, use some radical producers to produce a 50-50 mix of the 2 isomers and repeat.

They even use solvent management to deal with the naproxen (not being) waste and don't even throw away much methanol. It's RT so no smell, much safer, highest yield, lowest costs.

 

[Foerock]

Cutting, peeling, crushing and snorting KINDA works. You absorb some, but sadly not all as it slowly gels in your nose. Kinda wasteful and not worth it IMO.

Adding the powder into a glass of soda and drinking also KINDA works. It will result in a kind of limbo state between XR and IR.

Adding water and straight plugging DOES NOT WORK. You will barely feel anything then go directly into a horrible, gittery, anxious comedown.

I can confirm that lemon/lime COMPLETELY DESTROYS (or prevents absorption of) MPH. After you add water to the lemon MPH and drink or plug it, you will feel NOTHING. No effect and no comedown; nothing.

I suspect temperature of solvent affects how it gels, but cannot confirm this.

Many people report successful extraction using 96%+ isopropyl, but I personally could never for the life of me get it to work. No matter how much care I took to having the stuff totally dry, once I add isopropyl, it still gels and the syringe cannot draw anything through the cotton filter. And whatever little I could draw would become chalky/plastic-like after evaporation, never got crystals.

I would've tried the microwave method that people used to do on generic Oxy's, but I don't own a microwave.

Seriously though... fuck Concerta. It is inferior to Ritalin in every way possible. Doesn't matter if you intend to take therapeutically or recreationally; Concerta is far inferior for both purposes (and everything in between).

And if Adderall then fuck Ritalin too, lol. I miss Adderall.

 

[grus]

Cutting, peeling, crushing and snorting KINDA works. You absorb some, but sadly not all as it slowly gels in your nose. Kinda wasteful and not worth it IMO.

Adding the powder into a glass of soda and drinking also KINDA works. It will result in a kind of limbo state between XR and IR.

Adding water and straight plugging DOES NOT WORK. You will barely feel anything then go directly into a horrible, gittery, anxious comedown.

I can confirm that lemon/lime COMPLETELY DESTROYS (or prevents absorption of) MPH. After you add water to the lemon MPH and drink or plug it, you will feel NOTHING. No effect and no comedown; nothing.

I suspect temperature of solvent affects how it gels, but cannot confirm this.

Many people report successful extraction using 96%+ isopropyl, but I personally could never for the life of me get it to work. No matter how much care I took to having the stuff totally dry, once I add isopropyl, it still gels and the syringe cannot draw anything through the cotton filter. And whatever little I could draw would become chalky/plastic-like after evaporation, never got crystals.

I would've tried the microwave method that people used to do on generic Oxy's, but I don't own a microwave.

Seriously though... fuck Concerta. It is inferior to Ritalin in every way possible. Doesn't matter if you intend to take therapeutically or recreationally; Concerta is far inferior for both purposes (and everything in between).

And if Adderall then fuck Ritalin too, lol. I miss Adderall.

If you boil the ground up powder in a few ml water it is not gel and works perfect!

 

[ColdNorth]

I've been doing the following to extract the MPH into somewhat pure crystal form for the last decade or so. Before that, I must have injected thousands of Concerta pills (only the working parts though) in their rather slimy form which is the inevitable result when simply just dissolving in water.
Oddly enough, I never encountered any health problems resulting from flooding my veins with that crap, which often included even the worst possible parts - the coloring agent used on the outermost layer, which isn't water soluble and still to this day I occasionally shudder to think of the amounts that I have shoved into my circulation and where all that shit has ended up (my guess would be that it's hanging around the alvioli in my lungs).


..just to be clear, I am saying that I have personally somehow managed to avoid any damage to my health; not that it's objectively safe to do any of that even once. The only rational approach to injecting pills in any shape or form is to NEVER INJECT PILLS IN ANY SHAPE OR FORM - it is always a risk to one's health.


100% isopropyl alcohol (IPA) is the only thing you need, and once I started routinely doing this, it honestly doesn't take that much longer to do the extraction compared to just dissolving in water.

Here's a quick guide. I'll check back later and post a proper one if need be. I don't think I'm breaking any rules here but if I'm mistaken, my apologies and remove this post if needed.


Take your Concerta(s) apart. Toss out the transparent layer that is right after the colored layer, and the brown part of the inside. For original Concerta, the outer layer with the color contains 22% of the MPH and the non-brown inside parts contain the other 78%. If you have Sandoz generics, toss out the red and transparent parts instead. If you have Mylan generics, don't use this method at all.

Grind up the inside parts in a mortar & pestle or something similar into as fine a powder as you can manage. The outer part doesn't really crush, I find it easiest to cut into tiny pieces with scissors.

Put the active parts in a dish and add some 100% IPA. You don't really need much, easily less than 1ml for a single 54mg pill, but experiment at will. The idea is to let the MPH dissolve into the alcohol, and you'll immediately notice why pure IPA is so great as none of the visible bits dissolve in it, only the active ingredient.

You could just let it sit for 5-20 minutes. It seems to dissolve faster in a cold environment for some reason, like a fridge. Or, if using a metal or other durable dish you can find a tool with a flat surface and mash the stuff against the bottom with some force (like mortar & pestle), this is far quicker.

Then, draw the alcohol from the cup through a filter and into another dish and evaporate the alcohol. I prefer a metallic container with a wide bottom as it's the fastest way but you can also just let it sit in a well ventilated space until it's all gone.

If you want to speed it up though, the most optimal method I have found is to use a water bath and a fan. You'll need a dish that can safely float on water without falling over or taking in water.
If you want to do that, boil some water in a kettle and take it off the heat for a few minutes. Now, put your dish with the IPA in it on top of the hot water. The heat of the water bath will make the IPA evaporate very quickly. To accelerate the evaporation even further, you can use a fan, anything from a hair dryer to a simple USB fan or even a MacGyvered computer fan to circulate air towards the evaporating alcohol. Just don't overdo the heat (hair dryers blow hot air).

In either case, once the alcohol is all gone, you should be left with white crystal stuff which is relatively pure MPH. The effects are a little different, presumably because it is now freebase MPH (though I am no chemist, so that is just a guess). Personally, I love the end product both for the subjective effects and for being so much friendlier on my veins.

Just make sure your IPA is 100% pure and contains no water. If you do not have access to 100% IPA, I think you can remove water from it, first using table salt which can take you up to 91% purity or so, and then sodium hydroxide for the rest. Google it. At least in Finland it's easily available at hardware stores, it's great for cleaning electronics etc.

Right, about the Mylan generics. Those use a different ER, if you crush then gently at first you will see that there are tiny round pellets mixed in with the really fine powder. Simply separate those two and toss out the fine powder, all it does is turn into gel and expand, it contains no MPH. The tiny round pellets are similar to what is contained in many instant release MPH capsules so you'll know what to do with it. The outer colored layer..I would just eat it normally, it's IR anyway.

 

[sekio]

I think you can remove water from it, first using table salt which can take you up to 91% purity or so, and then sodium hydroxide for the rest. Google it.

Do not use sodium hydroxide to dry isopropanol: it will dissolve in the isopropanol and form a dangerously corrosive alkaline solution of sodium isopropoxide.
Instead, go buy some Epsom salts (magnesium sulfate heptahydrate), grind about 100-200g in a mortar and pestle or coffee grinder, and place it on a clean baking sheet, atop some parchment paper preferably. Bake at high heat (450F is good) and the water will sweat off and evaporate until it is white and crispy. Then grind it in your grinding utensil (careful: forms an irritating dust) and store it in a well sealed container. This is anhydrous magnesium sulfate and it is the best drying agent because it is mostly insoluble in almost every solvent except water, and most important, is pH neutral.
Or just, y'know, find some 99% isopropanol - it's not that uncommon. (99% isopropanol will work just as well as 100% - in fact you will find it's hard to find a vendor selling anything labeled 100% isopropanol. 99% is, for all intents and purposes, 100% pure. Source: the pure isopropanol we bought in 20L pails at my lab was labeled... 99%.)

SWGDRUG confirms that methylphenidate HCl is soluble in ethyl and methyl alcohol, so isopropanol should work as well too.

It seems to dissolve faster in a cold environment for some reason, like a fridge.

This is backwards. Substances dissolve faster as temperature increases. For instance, when I was extracting codeine from Tylenol 1's I would use boiling water to dissolve as much as possible initially. You could even literally boil the crushed pills in isopropanol (the methylphenidate will not be hurt), but that would be excessive.

Using mechanical agitation to improve extraction is a classic trick though.

presumably because it is now freebase MPH

No, it's still the salt form. You've just dissolved it selectively and then evaporated the solvent.


Also I personally had no problem with using Concerta "as labeled" - I found it was a reasonable enough XR of methylphenidate even if you do take the BA hit from oral usage.

All the addicts here are prescribed with generic 10mg IR methylphenidates anyway that flooded the local market - it's only the kids with ADD now with Concerta.

 

[ColdNorth]

Do not use sodium hydroxide to dry isopropanol: it will dissolve in the isopropanol and form a dangerously corrosive alkaline solution of sodium isopropoxide.
Instead, go buy some Epsom salts (magnesium sulfate heptahydrate), grind about 100-200g in a mortar and pestle or coffee grinder, and place it on a clean baking sheet, atop some parchment paper preferably. Bake at high heat (450F is good) and the water will sweat off and evaporate until it is white and crispy. Then grind it in your grinding utensil (careful: forms an irritating dust) and store it in a well sealed container. This is anhydrous magnesium sulfate and it is the best drying agent because it is mostly insoluble in almost every solvent except water, and most important, is pH neutral.
Or just, y'know, find some 99% isopropanol - it's not that uncommon. (99% isopropanol will work just as well as 100% - in fact you will find it's hard to find a vendor selling anything labeled 100% isopropanol. 99% is, for all intents and purposes, 100% pure. Source: the pure isopropanol we bought in 20L pails at my lab was labeled... 99%.)

SWGDRUG confirms that methylphenidate HCl is soluble in ethyl and methyl alcohol, so isopropanol should work as well too.


This is backwards. Substances dissolve faster as temperature increases. For instance, when I was extracting codeine from Tylenol 1's I would use boiling water to dissolve as much as possible initially. You could even literally boil the crushed pills in isopropanol (the methylphenidate will not be hurt), but that would be excessive.

Using mechanical agitation to improve extraction is a classic trick though.


No, it's still the salt form. You've just dissolved it selectively and then evaporated the solvent.


Also I personally had no problem with using Concerta "as labeled" - I found it was a reasonable enough XR of methylphenidate even if you do take the BA hit from oral usage.

All the addicts here are prescribed with generic 10mg IR methylphenidates anyway that flooded the local market - it's only the kids with ADD now with Concerta.

Thanks for the corrections. I've always wondered why the extracted form feels so different compared to just dissolving in water (when taken IV), guess that still remains a mystery. I am aware that solubility tends to increase with temperature, but with this there really is a big difference when put in the cold for a bit. Although that might have nothing to do with MPH solubility, it's just an increase in the amount of white crystalline stuff left after evaporation and might be due to some unknown factor, like perhaps one of the binders/fillers being soluble at a lower temperature, or even something more mechanical in nature. Sometimes it even ends up a bit cloudy when dissolved in water where as it's completely clear if done at room temperature, so that would make sense. Better avoid the cold after all.

You seem knowledgeable about chemistry, do you have any idea why the end product can have a brownish color to it if the IPA is evaporated at a high enough temperature where it boils slightly? Also produces a distinct sweetish chemical odour.

Without going into too much detail, for someone like myself this approach has worked out best in the long term compared to the IR formulations. But I should just bite the bullet and get my prescription back anyway. Even though I insist on IV, it is generally for self-medication purposes. It's just a huge hassle here if you also happen to be in opioid replacement therapy, but since the arrival of Buvidal that seems to be finally changing.

 

[sekio]

> I've always wondered why the extracted form feels so different compared to just dissolving in water
Well, there should be no difference in the chemical at all.

> do you have any idea why the end product can have a brownish color to it if the IPA is evaporated at a high enough temperature where it boils slightly? Also produces a distinct sweetish chemical odour.
The odour I have no idea about, and going by your description could be anything. It's not likely to be a decomposition product of the MPH though.
As for the browning, it could be the typical light oxidation seen from drying out various compounds over high heat - they tend to go voloured from small amounts of oxidation.

 

[Serhat]

I must emphasize that tampering with medication, especially in ways that alter its intended release profile, can pose significant risks to health and safety. Taking medications in ways that are inconsistent with their labeling can lead to overdose, unintended side effects, and other serious health complications.

That said, I can provide some information about the compounds and processes you've described:

1. Ethylphenidate: The reaction between methylphenidate and ethanol to produce ethylphenidate and methanol is possible in theory. However, the extent to which this reaction would occur in a simple mixture of methylphenidate and vodka is uncertain. Even if it did occur, the amount of methanol produced would be negligible compared to the amount in commercial alcoholic beverages. That being said, it's essential to note that ethylphenidate is a psychoactive compound in its own right, with effects that can differ from methylphenidate.
2. HPMC solubility: It's true that hydroxypropyl methylcellulose (HPMC) can be solvated using certain alcohols. This solvation can be influenced by the molecular weight and substitution pattern of the HPMC, as well as the specific alcohol used. Ethanol is indeed one solvent in which HPMC can dissolve, especially if the ethanol is diluted with some water.
3. Isopropyl Alcohol: Using isopropyl alcohol (IPA) might solvate some of the excipients in the tablet. However, IPA is not meant for consumption, and even if you allow it to evaporate, there's always a risk of some residual solvent remaining.
4. Extended Release Mechanism: Many extended-release formulations are designed to be particularly resilient against tampering. They can utilize multiple mechanisms, from gelling agents like HPMC to waxy binders and beyond, to ensure a steady release of the active compound over time.

I cannot stress enough that attempting to alter the release profile of a medication, especially without a comprehensive understanding of its formulation and the potential reactions that can occur, can be dangerous. Additionally, using or distributing tampered medication can be illegal in many jurisdictions.