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Bupe Suboxone's Intranasal Bioavailability - accurate figure?

I usually dose 130-175 micrograms a day because I'm using it for pain, so I'm just using it as a prodrug for norbupe (full agonist)
But read up on Norbupe, it has very little analgesia sadly. Sedation yes pain relief no. imhr (in my humble research)
 
You know this thread is two years old?

But I am also not a big believer in the norbupe theory of low dose buprenorphine, it may have some additive effects but it seems unlikely that norbupe is really reaching the brain, but as evidenced by loperamide and plenty of empirical data about peripheral antagonists effecting certain types of pain relief I wouldn't be surprised if its full agonist peripheral action was coming through somehow...but it doesn't pass the BBB.

Besides, if the norbupe theory really were accurate we should all be swallowing our bupe to get the best effects, even those who claim to believe in the norbupe theory don't do that.

Instead, I think it's motly high dose bupe causes much more tachyphylaxis and it's as simple as that. Take high doses of bupe, tachyphylaxis occurs; keep the dose low, keep tachyphylaxis low, bupe keeps working.
 
Take high doses of bupe, tachyphylaxis occurs; keep the dose low, keep tachyphylaxis low, bupe keeps working.
What do u consider high dose? because i take 4-6 mg daily. ------yes i know it is an old post...not anymore! ;)
 
Just wanted to add, naloxone has a very high Intrnasal BA. I sometimes get a wave of pwd, before the bupe kicks in, and I've been wondering if it is the naloxones BA and fast onset of action.
 
Through experimentation I've found that I get the most consistent effects from buprenorphine if I dissolve my pills in a minimum volume of vodka, I add ~0.2 mL of vodka per 2 mg of buprenorphine put in a very small container (just big enough to accomodate the pill and alcohol volume + some extra space; if you have a blister strip with tearable segments, such a segment is the best IME, has a very small surface and is easily washed to minimize any loses), after pill disintergration (it takes several minutes on its own but can be crushed wet) I mix it a bit to make the suspension homogenous, draw into a 1mL syringe and apply it under my tongue, then use another 0.2 mL for a quick wash of the container and apply it immediately. I use a generic, so the amount of vodka necessary to disintegrate the pill and make the suspension thin enough to draw into a syringe may be a bit different for different brands. I don't think alcohol does much in this method, it's rather just that by applying it in the form of a suspension, you have the maximum practical concentration of bupe under your tongue in the minimum volume of liquid, so more bupe is absorbed before salivation dilutes the concentration. The effects from a given dose are consistent in my experience and it's because every time one starts with a similar concentration of bupe, the effect of salivation rate is decreased and the factor of time needed for pill disintegration under one's tongue and buprenorphine dissolution is completely eliminated.

Considering that pill disintegration immersed in alcohol takes several minutes, the amount of saliva has a huge impact on the amount of buprenorphine absorbed IMO.
 
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Just wanted to add, naloxone has a very high Intrnasal BA. I sometimes get a wave of pwd, before the bupe kicks in, and I've been wondering if it is the naloxones BA and fast onset of action.
Really? I never felt any bad feeling from sniffing it.
Through experimentation I've found that I get the most consistent effects from buprenorphine if I dissolve my pills in a minimum volume of vodka, I add ~0.2 mL of vodka per 2 mg of buprenorphine put in a very small container (just big enough to accomodate the pill and alcohol volume + some extra space; if you have a blister strip with tearable segments, such a segment is the best IME, has a very small surface and is easily washed to minimize any loses), after pill disintergration (it takes several minutes on its own but can be crushed wet) I mix it a bit to make the suspension homogenous, draw into a 1mL syringe and apply it under my tongue, then use another 0.2 mL for a quick wash of the container and apply it immediately. I use a generic, so the amount of vodka necessary to disintegrate the pill and make the suspension thin enough to draw into a syringe may be a bit different for different brands. I don't think alcohol does much in this method, it's rather just that by applying it in the form of a suspension, you have the maximum practical concentration of bupe under your tongue in the minimum volume of liquid, so more bupe is absorbed before salivation dilutes the concentration. The effects from a given dose are consistent in my experience and it's because every time one starts with a similar concentration of bupe, the effect of salivation rate is decreased and the factor of time needed for pill disintegration under one's tongue and buprenorphine dissolution is completely eliminated.

Considering that pill disintegration immersed in alcohol takes several minutes, the amount of saliva has a huge impact on the amount of buprenorphine absorbed IMO.
Thanks!!! I'm nervous to buy vodka, but maybe I'll do this with my mouthwash? :) It's like 40 proof I think. Should work right?
 
if you have a blister strip with tearable segments, such a segment is the best IME
Here is what I tried. I mixed the sub powder with some high alcohol propolis sublingual stuff on a spoon. Once it was mixed up, I just licked the brown liquid with the bottom of my tongue. Does this sound like I pretty much did it right? :) Seems like it would be good enough this way, right? ---------- p.s. how long do I have to hold the alcohol/propolis/bupe solution under my tongue? Seems like they could have made a better way to do this. So hard to dose if you work in public.
 
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CfZrx said:
Thanks!!! I'm nervous to buy vodka, but maybe I'll do this with my mouthwash? It's like 40 proof I think. Should work right?

I'd minimize any extra compounds to a minimum, mouthwash may contain a lot of stuff including dyes, antiseptics, fluoride salts and whatnot, I'm not sure if there's anything that could slowly decompose bupe as it's quite labile under acidic and basic conditions, but I'd avoid holding mouthwash under my tongue so I don't get stuff meant for topical contact absorbed through mucosa in bigger quantities. IMO you don't need to use alcohol in this method at all, just use mineral water instead, I did it many times and I honestly did not notice any difference, I only use vodka out of habit, I guess.

CfZrx said:
Here is what I tried. I mixed the sub powder with some high alcohol propolis sublingual stuff on a spoon. Once it was mixed up, I just licked the brown liquid with the bottom of my tongue. Does this sound like I pretty much did it right? Seems like it would be good enough this way, right? ---------- p.s. how long do I have to hold the alcohol/propolis/bupe solution under my tongue? Seems like they could have made a better way to do this. So hard to dose if you work in public.

I know what you mean, it's not really convenient, I have a very specific order of doing things in the morning so that I can have 20-30 minutes to dose bupe and not lose that precious time, it's problematic at times if I oversleep or something unpredicted happens out of the blue but I got used to it. More often it's more of a problem to dose it in the afternoon as I split my dose, sometimes I can't dose it until very late evening when I get home. I used to take my second dose while at work or during classes at the uni occasionally but it was very uncomfortable and I often had to swallow it after 5 min. when someone asked me something.

I normally hold the solution under my tongue until the characteristic bitter, slightly numbing taste dissipates which takes 20-30 minutes IME but it's also highly dependent on the rate of saliva volume increase, the minimum time I try to hold it is 30 min., if I don't have to talk to anyone, I usually hold it until there's too much saliva to contain it under my tongue. I also brush my teeth and rinse my mouth with tap water thoroughly so there are no small chunks of food or anything that makes saliva thicker. The slower the volume of saliva increases, the better, sometimes I notice dramatically stronger effect if I barely salivate and have like 2mL of liquid under my tongue after an hour, hence I believe for optimal absorption these 20-30 min. are necessary as opposed to what we're told at the program that the pill should be held until it dissolves, that's nonsense IMO and probably often the reason why people end up at very high doses.

I immerse the pill in alcohol instead of crushing it to minimize any loses in the powder stuck to a tool used for crushing, for the same reason I use a small syringe so I can wash it with little alcohol, although I'm sure such loses from crushing are insignificant overall. Like I wrote, I minimize extra stuff in the pill slurry, but if an alcoholic propolis extract works for you, it's fine.
 
I'd minimize any extra compounds to a minimum, mouthwash may contain a lot of stuff including dyes, antiseptics, fluoride salts and whatnot, I'm not sure if there's anything that could slowly decompose bupe as it's quite labile under acidic and basic conditions, but I'd avoid holding mouthwash under my tongue so I don't get stuff meant for topical contact absorbed through mucosa in bigger quantities. IMO you don't need to use alcohol in this method at all, just use mineral water instead, I did it many times and I honestly did not notice any difference, I only use vodka out of habit, I guess.
Mineral water!? Lol, thanks, that sounds easier.


I know what you mean, it's not really convenient, I have a very specific order of doing things in the morning so that I can have 20-30 minutes to dose bupe and not lose that precious time, it's problematic at times if I oversleep or something unpredicted happens out of the blue but I got used to it. More often it's more of a problem to dose it in the afternoon as I split my dose, sometimes I can't dose it until very late evening when I get home. I used to take my second dose while at work or during classes at the uni occasionally but it was very uncomfortable and I often had to swallow it after 5 min. when someone asked me something.

I normally hold the solution under my tongue until the characteristic bitter, slightly numbing taste dissipates which takes 20-30 minutes IME but it's also highly dependent on the rate of saliva volume increase, the minimum time I try to hold it is 30 min., if I don't have to talk to anyone, I usually hold it until there's too much saliva to contain it under my tongue. I also brush my teeth and rinse my mouth with tap water thoroughly so there are no small chunks of food or anything that makes saliva thicker. The slower the volume of saliva increases, the better, sometimes I notice dramatically stronger effect if I barely salivate and have like 2mL of liquid under my tongue after an hour, hence I believe for optimal absorption these 20-30 min. are necessary as opposed to what we're told at the program that the pill should be held until it dissolves, that's nonsense IMO and probably often the reason why people end up at very high doses.

I immerse the pill in alcohol instead of crushing it to minimize any loses in the powder stuck to a tool used for crushing, for the same reason I use a small syringe so I can wash it with little alcohol, although I'm sure such loses from crushing are insignificant overall. Like I wrote, I minimize extra stuff in the pill slurry, but if an alcoholic propolis extract works for you, it's fine.
I'm very surprised you are able to fall asleep after a very late dose! ---Now we need to find a way to make the mouth extremely dry! --------- So the propolis idea went to hell today. It didn't seem to work as strong as I'd hoped AT ALL, and then I accidentally dumped the whole bottle all over the kitchen floor! Honestly, tomorrow I'm just gonna take it as prescribed, with as little saliva as possible. I'm tired of maybe wasting my doses, and I don't want to snort them, as that doesn't seem like a long term solution. Frankly, the bupe holds my pain at bay when I spread 5 or 6 1mg doses throughout the day, even just plain old sublingual :)
 
Let me say this Again...I
YIU DO NOT NEED ETHANOL TO IMPROVE SL BA%, dissolving in, say, 0.7ml of water (or up to to 1 or 1.2ml, depending on brand and amount) shall enchance absorption, and increase BA% (possibly, improve Tmax?)


50%, roughly, is intranasal figure
 
Check out the Suboxone mega thread...
Yea usually people don?t do this because they want an answer to a specific question and not every comment ever on suboxone.

That being said does anyone know if it?s soluable in water like other opiates and if iv would be the way to go?
 
I dont agree a solution works just as good under your tongue, Ive tried every way possible because Im sick of damaging my nose and it never works for me. I could put an entire 8mg pill under my tongue, hold all the spit there for an hour without swallowing it and its less effective than snorting 2mgs.
 
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