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Pharmacology - The coating on Oxy or any other pill

Discussion in 'Oxycodone' started by Wehr, Feb 17, 2009.

  1. Wehr

    Wehr Silver Member

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    It is a common misconception that the coating on Oxy Contin or other pills is responsible for the time release of the medication. I believe that the time release takes place at a molecular level and not by a mere coating on the pill. The coating is just a color coding and also helps the pill to be swallowed easily so it doesn't get stuck in your throat. Correct me if I am wrong but it makes sense to me. Care to elaborate?:)

    Swim was just reading some posts where the op said SWIthey licked off the time release and just want to put in SWIme's 2 cents!
     
  2. Oneiros

    Oneiros Titanium Member

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    The time release coating of OC is a matrix of water insoluble fibers. The drug encapsulated within this matrix slowly diffuses outwards as small quantities of water penetrate the fibers and dissolve it bit by bit.

    This is true for OxyContin. Some drugs, however, do have molecular time release mechanisms, as you suggested. Vyvanse, for example, is amphetamine that has been bonded to the amino acid lysine. Once that compound gets into your body, your enzymes get to work on that peptide bond, metabolizing the inactive prodrug into the active amphetamine and inactive lysine. This whole process takes a bit of time, resulting in an extended duration of effect. Codeine works in a similar fashion, being inactive in the body itself until being broken down into morphine.

    Licking the pill won't really do anything except maybe remove the dye. Acetone, on the other hand might work well for removing the coat itself.
     
  3. Songcycle67

    Songcycle67 Newbie

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    SWIM removes the coating by just dampening a paper towel, getting the coating a bit wet and scraping it off. It comes off quite easily once wet and one suffers no detectable loss of the oxycontin tablet beneath as long as the coating is just lightly moistened.

    SWIM believes the coating also serves as a deterrent for insufflation (snorting) as many other methods could be used to make it time-release that wouldn't involve such a coating.
     
  4. Phentasies

    Phentasies Newbie

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    There are generally 2 types of controlled/sustained/time release mechanisms.

    1) Mechanical technologies;
    This is when there is a phsyical barrier that restricts exposure of the ingredients. The most common way of this involves the use of insoluble "balls" of a given material encapsulating the active ingredients. Theyre basically a visible or microscopic ball that has holes in its shell, and encased inside the ball is the active ingredients. The limited exposure to digestive fluids of the active ingredients inside the "ball" controls their release. The faster someone wants the ingredients to release, the more holes the "ball" will have.


    2) Molecular technologies;
    This is when the drug molecule itself is modified in any number of ways to increase impede its digestion or to impede its pharmacokinetics once digested. For example, molecular modifications that limit the digested molecules ability to be metabolized over a certain period of time into the active metabolite that exerts the pharmacologic effects.

    A great example of molecular technologies are steroid esters. Testosterone freebase lasts just minutes in the body. Whereas the Propionate ester of testosterone lasts a couple days. The enanthate ester, reffered to as Testosterone Depot, lasts about 2 weeks.

    There are many different methods for molecular modifications for the purpose of controlled release, and these vary on the molecule in question.



    When a molecular technology is used, trying to bypass that can be extremely hard if not entirely impossible depending on the particular way its been modified. If its been modified in a way that is rate-limiting through metabolic mechanisms, there may be things you can take to counteract that. In otherways, there may be chemistry procedures that can be done to the molecule to bypass the technology.

    Mechanical (or physical) technologies are usually easier to bypass. In the event that the ingredients encased in insoluble balls with holes, these balls could be crushed and broken apart by pounding the powder. In the event of a coating, it could be scraped off.


    In order to know how to bypass a controlled-release technology, if its even possible, is to first know the exact mechanism being used to control the release, and this will vary from product to product!
     
  5. hamsterdam

    hamsterdam Silver Member

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    So if SWIY were to let the (crushed) OC tablet sit in water for a few days (maybe with a magnetic stirrer) then drink the water, that'll bypass the extended release?
     
  6. Pickpoke

    Pickpoke Silver Member

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    snort the beotch, then youll feel it in the matter of minutes :p
     
  7. Songcycle67

    Songcycle67 Newbie

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    SWIM says:

    It could, but as phentasies pointed out it ultimately depends on the type of time-release that was used. It could take a shitload of esoteric reagents or it may be just as simple as dissolving it in distilled water. SWIY would have to either do it on a trail and error basis (which would take for ever -- especially if SWIY doesn't know what the immediate effects are supposed to feel like as opposed to the effects experienced with time release) or perform chemical studies on the tablets to discern the method of release. Either way it's going to be a huge undertaking (i.e. more time than it's worth).

    One possible solution, hypothetically speaking of course, would be to confer with a chemist who is familiar with the particular product being used. More than likely any organic chemist worth their salt will be able to quickly answer that question with a bit of research and give SWIY an idea as to how to remove it.

    Either way it's going to be very hard. I'm sure some time-release solutions would require watched reagents to get rid of the necessary mechanisms.


    Insufflation is always an option, but that in itself is very addictive and the side-effects are terribly unpleasant for most people. But I suppose if a thing's worth doing...
     
  8. hamsterdam

    hamsterdam Silver Member

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    One easy way to see if it works is let the OC tablet sit in water for a few days, then drink that and compare it to drinking a CWE of percocet for an equal amount of oxycodone.

    SWIM doesn't have OC or percocet, so he can't try this.
     
  9. Issmortor

    Issmortor Silver Member

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    There-in lies the problem, after hours of searching, there doesnt seem to be any public information on the mechanism of Oxycontin's time-release. I even asked a few pharmacists and got a few different "made-up-on-the-spot" answers that were quite funny...

    why would purdue be witholding the mechanism of action? is it really that special of a trade production secret?

    some generic ER oxycodone seem to work off a slowly disolving gelly-goo that the entire pill - coating to core - is made of, therefor also making it very difficult to snort...
     
  10. Phentasies

    Phentasies Newbie

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    The idea that you can just wet the OC tablet and rub off the enteric coating and that will bypass the time release mechanism is very flawed.

    Think about it, if simple saliva and a little mechanical force could remove the time-release mechanism in seconds, then the acids of the stomach would destroy the time-release mechanism in an instant and it wouldnt be a controlled release product.

    Alls the coating on OC tablet is-is an enteric coating. Done for no reason other than to add color-coding to the tablets.

    In SWIMs experience with OC tablets, there is no discernable coating on the tablet beyond a simple enteric coating.

    This leads SWIM to beleive the time release mechanism is probably little insoluble balls that contain active ingredient inside them.

    If one crushed the tablet and pounded it until it was a fluffy powder, this would almost certainly bypass the insoluble ball form of time release. This is the most common time-release method used, its cheap, relatively easy to manufacture, and effective.


    One way someone could see if this is how OC's are time-released would be to remove the enteric coating, crush and pound the tablet until its a perfectly uniform granule size and a very fine fluffy powder. THEN place into a small amount of water (say 2ml), and leave for several hours. IF the product uses insoluble balls, there should be some insoluble particulate matter that will collect on the bottom of the container, whereas all the active ingredients and possibly the filler ingredients (depending what they are, usually starch), will dissolve into solution.

    If there was particulate matter in the bottom of the container, it could be the broken shell of the insoluble balls thus indicating this method, however it could also be insoluble filler/binding ingredients used in the tablet production as well.

    It would be interesting experiment to do. One could then filter the solution and drink the filtered liquid (or just drink the particulate matter to).
     
  11. Songcycle67

    Songcycle67 Newbie

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    If you're referring to my statements, SWIM was talking about rubbing the coating off to make them snortable. Some people in SWIM's area were convinced that if you snorted the coating it would make your nose bleed or give you terrible nasal pain, not to mention the inconvenience of snorting rigid flakes of coating.

    As SWIM understands it, snorting the pill would make it release automatically no matter what kind of time-release is used, and he was just talking about removing the coating so that it could be insufflated.
     
  12. samuraigecko

    samuraigecko Newbie

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    The time release in Oxycontin is just an edible wax throughout the pill. As the wax dissolves it releases the Oxycodone from the wax. It is supposed to work over a 4 hour period so 20mg would release 5mg an hour, 40's would release 10mg an hour, etc etc.

    Peace :)

    BTW to test if this is correct, use a pill crusher (screw type) and crush the pill down. One will be left with wax marks on the sides and have to scrape the powder from the bottom (which is also waxy). One can also burn the wax and get that same "burned wax smell" if one is to spin the crusher quick enough.

    Peace :)
     
  13. Politicalchalk

    Politicalchalk Titanium Member

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    It APPEARS to swim that MS CONTIN (morphine -er) uses a similar matrix, any thoughts?

    Swim once heard that the ER formulation w/ OCs had to do nothing with the coating, but she (a drug rep) laughed and said that it had something to do with the way the salts were pressed. he can't supply anything factual here though.

    What's swiy's most difficult time barrier to break?

    1 ion-exchange matric (such as in tussionex, hydrocodone/chlorpheniramine er)
    2 oxycodone er (oxycontin)/ms-contin, oxymorphone er, etc
    3 time release capsules

    *lysine....couldn't this be metabolizes faster just with supplements that metabolize amino acids faster?
     
  14. LinusMundane

    LinusMundane Silver Member

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    SO if SWIM were to obtain say a Tylenol rapid release capsule, empty it out, crush up his generic OC 40 and put the powder in the empty casing then ingest this concoction, would SWIM theoretically have an IR OC 40?
     
  15. jon-q

    jon-q Gold Member

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    There are some Oxycodone ER tablets that do still use wax based release systems Teva pharmaceuticals are possibly one of them, but Oxycontin produced by or under agreement with Penwest pharmaceuticals use the TIMERx release system.

    The TIMERx® technology is based on a customized, agglomerated hydrophilic complex that forms a controlled-release matrix upon compression. The matrix consists of two polysaccharides, xanthan and locust bean gum. Interactions between these components in an aqueous environment form a tight gel with a slowly eroding core.
    The following mechanistic illustration shows how the interactions between the polysaccharides form a matrix with the active compound. This system controls the rate of water ingress into the matrix and subsequent diffusion and release of the drug.
    [​IMG]


    Oxycontin with TIMERx profiles release Oxycodone at a steady, constant rate for about 12hrs. Oxycodone starts entering the blood stream between 1-2 hrs this peaks at about 3-4hrs and then remains fairly constant up to the 11-12hr mark, the levels then slowly subside for another 3-4hrs. When you factor in for the half life of Oxycodone peak plasma levels are reached after about 2-3 days.

    The patent held by Penwest pharmaceuticals was due to expire in 2009; I’m not too sure whether or not this has been renewed.
    Q
     
    Last edited by a moderator: Apr 30, 2017
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