Optimizing Absorption of Buprenorphine

I wrote this a couple years ago, and still get questions about the topic today.  Studies show that a small fraction of the amount of buprenorphine in a tablet or film strip actually gets absorbed through mucous membranes;  the rest is swallowed.  The 15%-30% amount of absorption is referred to as the ‘bio-availability’  of the drug.

People who feel like they are not getting enough buprenorphine to remove cravings can review the principles below, to see if there are ways they can easily improve the absorption of buprenorphine.  NOTE:  improving absorption is NOT an ‘addictive’ behavior, for a couple reasons…. first, because of the ceiling effect, increasing the amount absorbed will NOT cause a ‘buzz’ or high, but will only make the medication last the full 24 hours without wearing off.  Second, crushing a tablet will NOT cause a ‘rush’ or ‘high’ for two reasons– first, because of the ceiling effect as I just described, and second, because the rate-limiting step for absorption is the passage through tissue— NOT the dissolution of the tablet.  This is why, by the way, the film does not cause a ‘rush’, even though it dissolves more quickly.

Read on:

I often answer questions about Suboxone that require the qualification ‘if it is being absorbed properly’. If a person asks how long it takes for Suboxone to wear off, or at what dose does the ceiling effect occur, I need to be sure that the person is taking it in a way that maximizes absorption; otherwise all bets are off. If a person simply swallows the tablet, for example, the level of buprenorphine in the bloodstream will be much lower than if it is taken correctly.

The usual instructions for taking Suboxone are to place a tablet under the tongue and let it dissolve.  It is important that Suboxone be taken once per day, in the morning; this instruction is included in the course for physicians but is too often ignored.  I will talk another time about the philosophy for dosing once per day; the basic reason is to extinguish the behavior that has been conditioned as part of the addiction.  But the point of this post is the absorption of buprenorphine from the tablet into the bloodstream, and how to maximize that absorption.  It is important to maximize absorption, particularly if one is trying to save money by reducing the daily dose of Suboxone.

From my experiences as an anesthesiologist, as an addict**, and as a PhD chemist, I recognize that three factors will maximize absorption.  The first is the concentration of buprenorphine in the saliva, as the drug diffuses into tissue down a concentration gradient.  This gradient is maximized by having a small volume of saliva.  I recommend that a person start with a dry mouth, place the tablet in the mouth, and crush the tablet between the teeth until it is dissolved in a small volume of a concentrated solution.

The second factor that affects absorption is the amount of surface area.  Buprenorphine is absorbed through all mucous membranes (the tissue lining the inside of the mouth), passing through the surfaces and entering capillaries, the route into the bloodstream.  So the concentrated solution should be ‘painted’ repeatedly over all of the surfaces inside the oral cavity;  the inside surface of the cheeks, the tongue, the roof of the mouth, under the tongue, the back of the throat…  swished around in the mouth over and over, repeatedly bringing the concentrate into contact with new areas of mucous membranes.

The third factor is time– the longer period of time, the longer for the buprenorphine to make contact with the mucous membranes, attach to the surface, get absorbed into the tissue, and enter the capillaries.  The initial process will be the saturation of the surfaces of the mucous membranes, and the slower process will be the passage into the tissue;  that is why the amount of surface area has such an important effect on absorption.  Fifteen minutes is probablysufficient for most of the absorption to occur;  there may be drug remaining that is attached to the surface but not yet fully absorbed, and so I recommend avoiding eating or drinking within another fifteen minutes or so after swallowing the left-over saliva.

If you pay attention to these principles you will maximize absorption of the drug.  The ceiling effect will occur under these conditions at a dose of about 2-4 mg;  the long half-life of the drug will guarantee that if you take over 4 mg or so each morning, you won’t have any significant withdrawal for over 24 hours– allowing once-per-day dosing.  Yes, early in treatment patients will feel as if they need to dose more frequently– but that is not because of too little buprenorphine, but rather because of conditioned behavior.  A person early in Suboxone treatment will have feelings or minor withdrawal in the late afternoon or evening after dosing in the morning;  those minor withdrawal sensations will go away in about 15 minutes if the person takes more Suboxone, and will also go away in 15 minutes if the person doesn’t take Suboxone.  If the person takes more Suboxone, it will reinforce the sensations and the person will get stuck on dosing twice per day.  If, on the other hand, the person uses distraction and avoids dosing, those minor withdrawal sensations will completely disappear in a week or two, as the conditioned behavior is extinguished.

**I mentioned my experience ‘as an addict';  for a period of time my preferred route of administration of lipid-soluble opioids was ‘trans-mucosal’ or ‘trans-buccal’.  Since the amount of substance available was finite (albeit a fairly large finite amount!) I did all that I could to optimize absorption, including reading about diffusion of lipid-soluble molecules through mucous membranes.

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2 thoughts on “Optimizing Absorption of Buprenorphine”

  1. re subox film has better absorption apparently.the film has been just released in oz.
    i take my subx sublingually.
    in oz alot of idiots divert it/i.v causing big probs if pple want to travel o/s with subx.
    i went to Bali& last year could only go for 10 days.
    ( that was max dose by law my chemist could give me due to pple abusing it.)
    i love been on the film- i have been trying to get off tabs for years,but got stuck at 2mg due to finding chopping,cutting the pills messy,darn impossible to work with They just crumbles.so hard for correct dosage.
    Also made me paranoid at work having bits of powder in foil.( i work in d&a field)
    Reckitt shldve been sued for making suboxone tablets so crumbly-is not necessary.
    Im reducing off after 5+years on 6mg & have been looking at what im gunna be dealing with chemically.
    2mg subx(taking only approx 20% absorption into account) is equivalent
    (in my lay opinion)roughly to about 20mg morphine tablet.thats a serious amount of opiate.
    The 2mg sounds small and makes pple think its nothimg-mistake Beckitt.
    In Beckitts defense i LOVE THE FILMS re can cut up easy.
    -I WILL BE FREE SOON.YEEHAH.
    Due to raeding about the increased absorption film,i smartly reduced my dosage by 50% -from 5mg-3mg in the first week swapping.

    Re the ingredients ,the inactive ingredients could cause a few people allergies perhaps.white ink dosent sound the best!Mind u they would be similar inactives to the listerine film strips i suppose.

    Me On Storing the Film:
    People must remember if cutting up FILM dose. film is very light/air sensitive.
    also n.b pple to store below25c.
    Best storage method ive found–any tips much appreciated.
    Put the other piece film not using back in original foil slip & seal with sticky tape or any adhesive label.(One guy folds over tightly &uses a paper clip to secure foil slip!Another puts dose in a small baggie-can buy frm bead-jewelery shops)
    I store my unopened filmstrips at home in a small slim cigarette case.
    i dont smoke but perfect size for the films.(we dont get given the whole external cardboard box in oz.have to pick up twice a week frm chemist)
    good luck all.

  2. Doc,
    I find it difficult to crush and paint my mouth w/ the new Hi-Tech 8mg. generic subutex. They are so small, that I seem to get better results by just warming my mouth, keeping the pill under my tongue, and moving it around that way. It is hard for me to keep my mouth dry and I end up losing,(down my throat)…
    I had no problem w/ the larger pills, but I would just as soon take the smaller Hi-Techs, knowing that there is most likely less filler and excepients, which I have no use for…..
    just my opine,
    Scott…..