Embeda efficiency and understanding its website info.

[Tommyboy]

The Embeda website has information on the drug that seems to contradict itself every other paragraph. I copied and pasted text from the website, as you see below.

EMBEDA® contains pellets of an extended-release oral formulation of morphine sulfate, an opioid receptor agonist, surrounding an inner core of naltrexone hydrochloride, an opioid receptor antagonist indicated for the management of moderate to severe pain when a continuous, around-the-clock opioid analgesic is needed for an extended period of time.
I have heard two different things about the pellets in the capsules. All of the pellets looks the same, but some say that some of them are morphine, and the others are the naltrexone. The naltrexone is said to be coated in wax, therefore would not be released unless it is crushed.

The website here says that the naltrexone is within the morphine pellets, so how would that prevent them from being absorbed, unless the outer part of the pellet is morphine, then a layer of wax, then the naltrexone?

EMBEDA® 100 mg/4 mg IS FOR USE IN OPIOID-TOLERANT PATIENTS ONLY. Ingestion of these capsules or the pellets within the capsules may cause fatal respiratory depression when administered to patients not already tolerant to high doses of opioids.

Patients should not consume alcoholic beverages while on EMBEDA® therapy. Additionally, patients must not use prescription or non-prescription medications containing alcohol while on EMBEDA® therapy. The co-ingestion of alcohol with EMBEDA® may result in an increase of plasma levels and potentially fatal overdose of morphine. EMBEDA® is to be swallowed whole or the contents of the capsules sprinkled on apple sauce. The pellets in the capsules are not to be crushed, dissolved, or chewed due to the risk of rapid release and absorption of a potentially fatal dose of morphine.

^I don't get how it says that crushing it may increase the risk of overdosing, yet it also says that crushing it will cause the naltrexone to be released, putting you in withdrawls. I understand the concept of the naltrexone having a higher affinity to the opiate receptors than the morphine, which would cause precipitated withdrawals when activated, but I don't understand how crushing it could cause overdose. Also, whats the deal with sprinkling the contents onto apple sauce, couldnt that end up in you chewing it?

Crushing, chewing, or dissolving EMBEDA® will also result in the release of naltrexone which may precipitate withdrawal in opioid-tolerant individuals.

^ Has anybody tried this "dissolving" method? I don't get how dissolving the pill in water, and then ingesting it would be any different than it dissolving in your stomach, in terms of the release of the naltrexone. Idk, this stuff doesn't make sense to me, and a family memeber just got it prescribed. I don't crush regular morphine when I take it, and I usually take between 100-200mgs for relief. I took 300mgs of embeda, and it did not relieve my pain much at all. I should also add that this was my third time using any opiated since august, so my tolerance is down.

Thank you for any help understanding this new medication.

Link

 

[23536]

The website here says that the naltrexone is within the morphine pellets, so how would that prevent them from being absorbed, unless the outer part of the pellet is morphine, then a layer of wax, then the naltrexone?

yes that's correct. Imagine an inner sphere (Si) surrounded by a crust (Ci) surrounded by a thick outer shell (So) surrounded by an outer crust (Co):

Co is very soluble at low pH
So is slightly soluble at low pH and soluble at neutral to alkaline pH
Ci is insoluble at low pH and soluble at alkaline pH
Si is very soluble at low pH but insoluble at alkaline pH

the morphine is in So. The naltrexone is in Si.

 

[Kurt_Cobain]

Thank you for the info Tommy, and for starting this thread. Quick question though; how many embedas would it take to feel actual reduction of pain you've had chronically for nearly 4 years?
(Keep in mind, I'm also on percocets so my opiate tolerance is rather large when I have to take 4-6 10mg to block it out and have a buzz.)

 

[Pharma Kologee]

yes that's correct. Imagine an inner sphere (Si) surrounded by a crust (Ci) surrounded by a thick outer shell (So) surrounded by an outer crust (Co):

Co is very soluble at low pH
So is slightly soluble at low pH and soluble at neutral to alkaline pH
Ci is insoluble at low pH and soluble at alkaline pH
Si is very soluble at low pH but insoluble at alkaline pH

the morphine is in So. The naltrexone is in Si.

So is this to imply that if the pellets were disolved in a low pH solution that the morphine could be dissolved into the solution and leave the wax coated naltrexone in a solid, easily separated form?

 

[23536]

oh shit I should've stated that I was merely solving the riddle the OP put up. I don't know if it is descriptive of Embeda's composition. I glanced at the patents in the prescribing info and it seems that what I wrote is more or less the design.

So is this to imply that if the pellets were disolved in a low pH solution that the morphine could be dissolved into the solution and leave the wax coated naltrexone in a solid, easily separated form?

I would think that the morphine layer is only slightly soluble at low pH, and raising the pH to increase yield would free the coating on the naltrexone. Does this make sense?

For more info see the patents cited in the prescribing info

 

[Pharma Kologee]

I have done about as much research as possible on Embeda with particular interest in defeating the time release mechanism with limited success. Suppose the morphine does disolve slowly at low pH. Rather than increase the pH to disolve the morphine more rapidly, couldn't the time spent diluting be increased theoretically indefinitely without risk of diluting the naltrexone as well? SWIM had a few Embeda and experimented to an extent, but not in the manner I am proposing now, but I am still quite curious if the method is viable.
Let's get some of the chemists in here to verify/disprove the possibility!

 

[23536]

the "SWIM" gambit is taboo here

I have done about as much research as possible on Embeda with particular interest in defeating the time release mechanism with limited success. Suppose the morphine does disolve slowly at low pH. Rather than increase the pH to disolve the morphine more rapidly, couldn't the time spent diluting be increased theoretically indefinitely without risk of diluting the naltrexone as well?

if (if) it is slightly soluble at low pH, time is not exactly a variable. The key variable is concentration. Once the solution is saturated, you can let it sit there indefinitely but no more solute will go into solution.

maybe the plausible way to do this is to dissolve the whole formulation and only then separate the morphine from the naltrexone

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5378474

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The FDA's Big & Dandy EMBEDA Page (hundreds of printed pages of scientific literature)

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a 2-phase extraction can also be tried: the first under highly acidic conditions and the second under relatively alkaline (intestine-like) conditions. Methinks you'd want to keep the precipitate of the first and the filtrate of the second.

also, is there a published tek for removing the naloxone from Talwins?

 

[Pharma Kologee]

the "SWIM" gambit is taboo here

First point noted. Been lurking quite some time, made the jump to active contributor recently. Proably a good time to read the rules

if (if) it is slightly soluble at low pH, time is not exactly a variable. The key variable is concentration. Once the solution is saturated, you can let it sit there indefinitely but no more solute will go into solution.

maybe the plausible way to do this is to dissolve the whole formulation and only then separate the morphine from the naltrexone

Consider adding more solvent or utilizing a multiple extraction type method. Could then one end up with a pure(er) morphine solution with exactly 0% naltrexone concentration (considering it is still totally encapsulated in the wax, Ci in your descriptive model)?

oh shit I should've stated that I was merely solving the riddle the OP put up. I don't know if it is descriptive of Embeda's composition. I glanced at the patents in the prescribing info and it seems that what I wrote is more or less the design.

I do tend to agree with you that it seems like a similar design.

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5330766

5378474

5202128

The above patents describe the time release mechanism, as far as I can tell, for the release of the morphine. If it covers the addition of the naltrexone (basically a time release inside a time release) I missed that part. Three patents is an awful lot of information to soak up though, so I may have missed it

The FDA's Big & Dandy EMBEDA Page (hundreds of printed pages of scientific literature)

---

a 2-phase extraction can also be tried: the first under highly acidic conditions and the second under relatively alkaline (intestine-like) conditions. Methinks you'd want to keep the precipitate of the first and the filtrate of the second.

Your suggested alternative extraction methods are intriguing and i'll look into them now, but I feel dissolving at low pH may yield a higher degree of assurance that there is absolutely no naltrexone dissolved into the end product, and potentially much easier to accomplish. Maybe that is covered in one of the above methods.

also, is there a published tek for removing the naloxone from Talwins?

Wasn't aware of the similarities or the processes hence my interest in this experiment!

 

[Pharma Kologee]

Thank you for the info Tommy, and for starting this thread. Quick question though; how many embedas would it take to feel actual reduction of pain you've had chronically for nearly 4 years?
(Keep in mind, I'm also on percocets so my opiate tolerance is rather large when I have to take 4-6 10mg to block it out and have a buzz.)

If being used for alagesic qualities for pain relief, depending on your body's reactions/tolerance to morphine it is quite effective at mainitaining levels of morphine in the body for extended periods of time if used as prescribed. It is not effective at relieving symptoms on an as needed basis. Taking it 1 - 2 times daily would build significant dosages in your body and keep it that way, but would never give you any kind of buzz due to the time release mechanism of the morphine, and can not be (traditionally) bypassed due to the presence of the naltrexone.

 

[Tommyboy]

If being used for alagesic qualities for pain relief, depending on your body's reactions/tolerance to morphine it is quite effective at mainitaining levels of morphine in the body for extended periods of time if used as prescribed. It is not effective at relieving symptoms on an as needed basis. Taking it 1 - 2 times daily would build significant dosages in your body and keep it that way, but would never give you any kind of buzz due to the time release mechanism of the morphine, and can not be (traditionally) bypassed due to the presence of the naltrexone.

I agree. It took very long to peak in me, over 12 hours after ingestion. It lasted a nice amount of time after that, which is when I realized that it would be effective if taken daily.

 

[humanguineapig]

Hi guys, I signed up for a recreational drug abuser study with Lifetree clinical research center. I go in tomorrow and they are going to be giving us crush embeda 120mg.

I have a history of opioid abuse but its been more than 4 months since I've taken any opioids of any kind..

In addition, I've never taken morphine...

I've been doing a far amount of research over the past couple of days and it seems like 120mg of embeda is quite a lot... Should I be concerned?