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buprenorphine seperation...

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wesley90

Bluelighter
Joined
Mar 2, 2006
Messages
62
"Buprenorphine hydrochloride is a white powder, weakly acidic with limited solubility in
water (17mg/mL). Chemically, buprenorphine is 17-(cyclopropylmethyl)-α -(1,1-
dimethylethyl)-4, 5-epoxy-18, 19-dihydro-3-hydroxy-6-methoxy- α -methyl-6, 14-
ethenomorphinan-7-methanol, hydrochloride [5α, 7α(S)]-. Buprenorphine hydrochloride has
the molecular formula C29 H41 NO4 HCl and the molecular weight is 504.10."

"Naloxone hydrochloride is a white to slightly off-white powder and is soluble in water, in
dilute acids and in strong alkali. Chemically, naloxone is 17-Allyl-4,5 α -epoxy-3, 14-
dihydroxymorphinan-6-one hydrochloride. Naloxone hydrochloride has the molecular
formula C19 H21 NO4 HCl .2H2 O and the molecular weight is 399.87."

Source: http://www.opioids.com/buprenorphine/subutex-suboxone.pdf


Now, the only way I see to isolate the buprenorphine is by it's weight or use about 17mgs of buprenorphine in 1 mL of water and somehow seperate the naloxone...but I dont see how to isolate the buprenorphine if naloxone is so water soluble....

Any help would be greatly appreciated.
 
Merck does not provide solubility data for Buprenorphine, but does say the following:

Naloxone (freebase): Soluble in chloroform, insoluble in petroleum ether
Naloxone HCl: Soluble in water, alcohol, practically insoluble in diethyl ether

You should try and find out if:
- Buprenorphine HCl is soluble in diethyl ether; if so, you could selectively extract it, leaving the Naloxone behind
- Is Buprenorphine (freebase) poorly soluble in solutions of strong alkali? If so, you could probably wash away the Naloxone from crushed pills using an ice chilled sodium hydroxide solution.

Or, you could just use your pills as directed.

wesley90 said:
"Buprenorphine hydrochloride is a white powder, weakly acidic with limited solubility in
water (17mg/mL). Chemically, buprenorphine is 17-(cyclopropylmethyl)-α -(1,1-
dimethylethyl)-4, 5-epoxy-18, 19-dihydro-3-hydroxy-6-methoxy- α -methyl-6, 14-
ethenomorphinan-7-methanol, hydrochloride [5α, 7α(S)]-. Buprenorphine hydrochloride has
the molecular formula C29 H41 NO4 HCl and the molecular weight is 504.10."

"Naloxone hydrochloride is a white to slightly off-white powder and is soluble in water, in
dilute acids and in strong alkali. Chemically, naloxone is 17-Allyl-4,5 α -epoxy-3, 14-
dihydroxymorphinan-6-one hydrochloride. Naloxone hydrochloride has the molecular
formula C19 H21 NO4 HCl .2H2 O and the molecular weight is 399.87."

Source: http://www.opioids.com/buprenorphine/subutex-suboxone.pdf


Now, the only way I see to isolate the buprenorphine is by it's weight or use about 17mgs of buprenorphine in 1 mL of water and somehow seperate the naloxone...but I dont see how to isolate the buprenorphine if naloxone is so water soluble....

Any help would be greatly appreciated.
Click to expand...
 
Hang on, naloxone has a ketone group whereas buprenorphine does not. Therefore will naloxone not form a complex with bisulfite (or NaI)? I realize that it's not a lot of use unless your dealing with a reasonable amount, but wouldn't that be pretty efficient?
 
extraction based on the differential solubilies is not going to work very well unless you find a solvent in which one really has really poor solubility.
you also will have great fun with fillers absorbing product.

perhaps a better approach get a column, and do some chromatography, on a small scale this practially guarantees separation.
 
vecktor's idea is facile-just blend up some toilet paper/water into a gel. EN/bulk adjacent to carbonyl in that antagonist would hinder bisulphite adduct, nichts wahr? Why not just hydrolyze the relatively labile allyl to form an agonist allay!
 
sixstringsamurai11 said:
is it safe to inject buprenorphine? But i want to inject it without naloxone cause i'l be shooting heroin.:)
Click to expand...

Why do you want to waste heroin?

There's no difference doing it with or without naloxone. You get the same effects. Including but not limited to: heroin not working on you.
 
im afraid cause in the prescp it said that ppl died after injecting bupro n naloxone
Click to expand...

That's bullshit. The naloxone doesn't do shit.

I've injected bupre + naloxone hundreds of times. I'm still alive.
 
that's hardly a reason to go ahead and do the same. The pills are full of garbage that I sure as hell don't want ending up in my lungs.
 
Hammilton said:
that's hardly a reason to go ahead and do the same. The pills are full of garbage that I sure as hell don't want ending up in my lungs.
Click to expand...

I know, I'm just commenting on the ridiculousity of the notion of separating naloxone from bupe.

Besides, proper filtering can do away with most of the garbage.
 
http://www.bluelight.ru/vb/showthread.php?t=445570

Just wanted to point out that thread.. some pretty nasty stuff from injecting subs, and pills in general.

That's bullshit. The naloxone doesn't do shit.
Click to expand...

Wrong. The naloxone sends you into rapid withdrawal if youve been using heroin.
I know this first hand. The first time i did it, I didnt know what the hell was happening at first because straight after injecting I felt incredibly horrible.

However - I went back for more. Did it another time but after a second 'rapid withdrawal' decided that it was not worth it..

To be noted though - the withdrawals only lasted around 30 mins until the buprenorphine bonds to the opiate receptors and basically take over, but that 30 minutes was intense and very very uncomfortable.

Addicts know what WD's are like, and being thrown headfirst into the deep end of it isnt nice at all. No lead in at all, just immediately into the throes of WD.

Based on that and the fact you can lose an arm if youre not careful (pill filter etc), as much as I love the IV rush, I'd be going sublingual or plugging at most (not sure about BA% for that?)
 
Wrong. The naloxone sends you into rapid withdrawal if youve been using heroin.
I know this first hand. The first time i did it, I didnt know what the hell was happening at first because straight after injecting I felt incredibly horrible.
Click to expand...

It's the buprenorphine that is doing that. Bupre being a partial agonist, it will only partially activate the mu-receptor while your brain is used to full agonism from the H and you will go into withdrawal.

Naloxone being in the formulation doesn't mean anything, since buprenorphine overrides the naloxone with it's higher binding affinity.
 
Thats a load of crap, I've shot buprenorphine extracted from a Norspan patch LOADS of times and although very rarely would have some withdrawal symptoms, they were NOTHING compared to shooting Suboxone.

Why the hell would they put it in there?? It's not inert at all. And where's the facts that say bupe has a higher binding affinity than naloxone??

The reason they put it in there is so that people on sub maintenance are less likely to abuse it.
 
Actually, now that i think about it.. it's probably right that bupe binds better than naloxone BUT the naloxone must cross the BBB quicker. Ive shot a decent load of bupe (just bupe only)only hours after cessation of heroin use for several weeks and there was basically never WD's..

I only ever did the same thing with suboxone twice.. and both times it was incredibly horrible
 
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