Buprenorphone and vinegar

[Peckerwood23squeak]

I have what is maybe a stupid idea but in 1930 the health people outlawed acetyloxymorphone because of its increased potency linking it to heroin. So why couldnt you try using distilled white vinegar added to a little water to dissolve the pill. Does this effectively create acetylbuprenorphone? I tried it and it seems to have increased potency and i may be wrong but perhaps the Ph change has also affected the naloxone in a way that decreases its effects. Anyone with chemistry knowledge have any ideas if this idea is

 

[sekio]

Does this effectively create acetylbuprenorphone

No, white vinegar is usually only 5% acetic acid and 95% water so ester formation is not favored.

 

[Hodor]

I have what is maybe a stupid idea but in 1930 the health people outlawed acetyloxymorphone because of its increased potency linking it to heroin. So why couldnt you try using distilled white vinegar added to a little water to dissolve the pill. Does this effectively create acetylbuprenorphone?

Not really.

First of all: It is buprenorphine, not buprenorphone.

Anyway: You know how Mexican black tar heroin differs from "proper" heroin? Basically, "real" heroin (i.e. 3,6-diacetylmorphine, which has two acetyl groups) is made using a substance called acetic anhydride, which is *really* effective at attaching those acetyl groups. Mexican BTH, on the other hand, is made by boiling morphine with glacial (i.e. pure) acetic acid, yet it still mostly contains 6-monoacetylmorphine (as the 6-position is more readily acetylated), whereas the only position to acetylate in buprenorphine would be the 3-position.

As sekio said, white vinegar is only 5% acetic acid, and since you further diluted it with water, and you need to acetylate your bupe at the 3-position, there is basically no way that all but the tiniest trace amounts of acetylbuprenorphine were formed. *If* you were to create acetylbuprenorphine, the best you could hope for would be higher oral/sublingual bioavailability; I wouldn't expect it to make any difference when injected (while both a 3- and a 6-acetyl increase bioavailability, only the 3-acetyl-group also prevents the molecule from binding to the receptor before it is cleaved off).

Also, food for thought: IF successful, wouldn't you also be acetylating the naloxone, thus creating acetylnaloxone? One of the reasons naloxone works as an abuse deterrent in pills is because its oral bioavailability is so much lower than that of most opioids (whereas IV bioavailability for naloxone would be 100%, so you'd suffer precipitated withdrawal when injecting it); however, suboxone has been criticized for not containing enough naloxone to do that: Bupe itself has a pretty low oral bioavailability, and coupled with its strong receptor affinity that means that the relative increase in BA of naloxone over bupe isn't great enough for the naloxone to displace most of the bupe when injected; at best it blunts the initial rush.
Presumably, 3-acetylnaloxone would be a more effective pro-drug for naloxone, so your acetylated suboxone mix could actually be *inferior* (atleast orally/sublingually) to the original.

tl,dr: No, you're not going to be able to create acetylbupe like that, and even if you did, it might actually suck because you'd also have acetyl-naloxone in it.

Edit: Also, the one banned in 1930 was acetylmorphone (i.e. 3-acetyl-hydromorphone, not acetyloxymorphone).

 

[Peckerwood23squeak]

Thank you so much for the information I am very ignorant when it comes to chemistry I'm just another addict,happily may I add, that can only get Suboxone from the doctor instead of Subutex if you have any ideas of how I may be able to increase the bioavailability of the buprenorphine or decrease the effects of naloxone it would be greatly appreciated I realize the Bupes affinity to the receptors is much greater than that of the naloxone so the difference won't be much but I have long sought away to get that nasty naloxone out of the Suboxone because the buprenorphine on its own has a much better high a better rush and lacks the other nasty side-effects that seem to come along with naloxone. I'm also wondering if there are any other ingredientd that would help me create a naloxone free substance. I have tried removing the naloxone by dissolving the tablets in 91% isopropyl rubbing alcohol and then pulling it through a filter then putting it in front of heat allowing the alcohol to dissolve and then using hot water 2 extract the water-soluble bupe left in the spoon. it does still get me high but it doesn't seem to make much difference at all compared to the difference between doing a regular subutex vs. Suboxone. I'm also wondering if there is any other way to create acetylbuprenorphine if I had subutex to begin with? Would acetylbuprenorphines bioavailability be greater than bupe on its own?

 

[sekio]

I have tried removing the naloxone by dissolving the tablets in 91% isopropyl rubbing alcohol and then pulling it through a filter then putting it in front of heat allowing the alcohol to dissolve and then using hot water 2 extract the water-soluble bupe left in the spoon.

I don't think that will remove the naloxone, it's present as a water-soluble HCl salt in Subutex. And AFAIK it's soluble in alcohols just like bupe is.

I'm also wondering if there is any other way to create acetylbuprenorphine if I had subutex to begin with?

There isn't anything accessible to the home user that would allow you to do that.

Given that bupe outcompetes naloxone at the mu opioid receptor there shouldn't be any difference between Subutex and Suboxone anyway, the naloxone has crap BA and what is absobed is very rapidly metabolized.

 

[Hodor]

Thank you so much for the information I am very ignorant when it comes to chemistry I'm just another addict,happily may I add, that can only get Suboxone from the doctor instead of Subutex if you have any ideas of how I may be able to increase the bioavailability of the buprenorphine or decrease the effects of naloxone it would be greatly appreciated I realize the Bupes affinity to the receptors is much greater than that of the naloxone so the difference won't be much but I have long sought away to get that nasty naloxone out of the Suboxone because the buprenorphine on its own has a much better high a better rush and lacks the other nasty side-effects that seem to come along with naloxone. I'm also wondering if there are any other ingredientd that would help me create a naloxone free substance. I have tried removing the naloxone by dissolving the tablets in 91% isopropyl rubbing alcohol and then pulling it through a filter then putting it in front of heat allowing the alcohol to dissolve and then using hot water 2 extract the water-soluble bupe left in the spoon. it does still get me high but it doesn't seem to make much difference at all compared to the difference between doing a regular subutex vs. Suboxone.

Here's the thing: This isn't like a CWE of a codeine/acetaminophen product where the two ingredients have radically different solubility. Suboxone is a mix of two thebaine-derived semi-synthetic opioids, both in their HCl forms, so assuming you'll be able to just separate the two based on solubility alone is a pretty optimistic prospect. Likewise, they may be expected to react with acetylating agents in a similar fashion, so any reaction that would give you 3-acetyl-buprenorphine would likely also give you 3-acetyl-naloxone.

Basically, if you want to minimize the relative effect of the naloxone, then just take the pill sublingually as intended. Virtually all the naloxone will be destroyed as it goes through the liver, and what little manages to survive/bypass the liver won't put a dent in the buprenorphine's effects.
If you're going to inject it, both buprenorphine and naloxone will be 100% bioavailable, which is a much greater relative increase for naloxone than it is for bupe.

I'm also wondering if there is any other way to create acetylbuprenorphine if I had subutex to begin with? Would acetylbuprenorphines bioavailability be greater than bupe on its own?

If you're injecting it, bioavailability for buprenorphine is already at 100%. Even if you had an acetylating agent to make acetylbuprenorphine, it would at best slightly increase blood-brain-barrier penetration for an extremely short amount of time before being converted back to buprenorphine. So no point in doing that, especially if you have to deal with very aggressive chemicals for it.

 

[Weltmeister]

From what ive found Naloxone and Buprenorphine have a melting point of 205?C and 262?C. This means theoretically its possible to remove the Naloxone by fractional distillation. Unless of course the Buprenorphine decomposes at the required temperature or the pills have some kind of built in mechanism to prevent this.

 

[sekio]

This means theoretically its possible to remove the Naloxone by fractional distillation.

Melt points are not the same as boiling points, there's no way you'd be able to distill the two apart.

 

[Prescottdave]

I don't think that will remove the naloxone, it's present as a water-soluble HCl salt in Subutex. And AFAIK it's soluble in alcohols just like bupe is.



There isn't anything accessible to the home user that would allow you to do that.

Given that bupe outcompetes naloxone at the mu opioid receptor there shouldn't be any difference between Subutex and Suboxone anyway, the naloxone has crap BA and what is absobed is very rapidly metabolized.

This is partly what I tell people when they claim to know how to separate the naloxone from the bupe. There is no point in the first place.

I prefer the suboxone strips over subutex as they seem to work a bit better due to the formulation of the medication.

 

[Weltmeister]

Melt points are not the same as boiling points, there's no way you'd be able to distill the two apart.

Thanks for the reality check

 

[Iknowmorethanmost]

Best and only noticeable way to brand new naloxone from your Suboxone pill is by using isopropyl alcohol. 70% to 90% and accepted . Me and Jackie for over half my life I learned that there's three main ways fixing up a shot . Water, heat, and sometimes alcohol. in this page me to crush the Suboxone pill up to powder and then add anywhere from 75 units of alcohol. You will filter that act normal and then work that Lincoln onto a clean spoon. From there you can either allow the alcohol to slowly evaporate or you can add little heat to it to speed up process.then when all the alcohol has evaporated there will be a film on the spoon. Add a little bit of water and refilter and it will make a milky liquid. I think you'll agree it's close as you can get to Subutex but starting from a Suboxone pill.

 

[Captain.Heroin]

I created a “how to IV suboxone” for dummies guide, and I still see posts like that.

 

[Hodor]

Best and only noticeable way to brand new naloxone from your Suboxone pill is by using isopropyl alcohol. 70% to 90% and accepted . Me and Jackie for over half my life I learned that there's three main ways fixing up a shot . Water, heat, and sometimes alcohol. in this page me to crush the Suboxone pill up to powder and then add anywhere from 75 units of alcohol. You will filter that act normal and then work that Lincoln onto a clean spoon. From there you can either allow the alcohol to slowly evaporate or you can add little heat to it to speed up process.then when all the alcohol has evaporated there will be a film on the spoon. Add a little bit of water and refilter and it will make a milky liquid. I think you'll agree it's close as you can get to Subutex but starting from a Suboxone pill.

Except that at no point during the process did you actually remove any of the naloxone. Where is it supposed to have gone? Evaporated with the isopropyl alcohol? It doesn't work like that.
You can't use isopropyl alcohol to separate bupe from naloxone in the first place, because their solubilities are pretty much the same.