Let?s talk Extended Release Medication

[quietcowgirl]

I tried searching the net but came up empty handed aside from a bunch of drug detox ads lol. I want to know more about extended release medications and how they work. I?m specifically wondering about Morphine ER 60mg tablets (Orange RD 72) but I?m curious in general as well. Here are my questions:

-Does breaking an extended release tablet really ruin its method of delivery?
-when do extended release tablets kick in and does it peak for the full 12 hours or does it go up and down?
-How exactly is the medication absorbed? Like does it completely dissolve and then your body slowly uses it up for 12 hours or is it like a layer situation where each layer has some of the drug and your body dissolves a layer at a time for 12 hours?
-how much of the drug is released at a time? Like for a 60mg ER tablet, does it release 5mg at a time to add up to 60mg at the end of 12 hours? Or does it release 60mg at a time?
-Lastly, If you were to get nauseous and puke like 6 hours after taking the medication; would it bring up what’s left of the pill (if that’s how it works) or would the liquid that you throw up have the rest of the medication in it, rendering you without further medication inside your stomach?

thank you!

 

[Automator]

Really weird that I want answers to all these questions. Googled to no avail.

 

[quietcowgirl]

Lol I even checked YouTube to see if there was some cheesy video explaining how extended release medication works but can’t find anything

 

[Jekyl Anhydride]

I tried searching the net but came up empty handed aside from a bunch of drug detox ads lol. I want to know more about extended release medications and how they work. I?m specifically wondering about Morphine ER 60mg tablets (Orange RD 72) but I?m curious in general as well. Here are my questions:

-Does breaking an extended release tablet really ruin its method of delivery?
-when do extended release tablets kick in and does it peak for the full 12 hours or does it go up and down?
-How exactly is the medication absorbed? Like does it completely dissolve and then your body slowly uses it up for 12 hours or is it like a layer situation where each layer has some of the drug and your body dissolves a layer at a time for 12 hours?
-how much of the drug is released at a time? Like for a 60mg ER tablet, does it release 5mg at a time to add up to 60mg at the end of 12 hours? Or does it release 60mg at a time?
-Lastly, If you were to get nauseous and puke like 6 hours after taking the medication; would it bring up what’s left of the pill (if that’s how it works) or would the liquid that you throw up have the rest of the medication in it, rendering you without further medication inside your stomach?

thank you!

The ER formulations are evolving these days into hard, plastic like pellets from Polyethylene Oxides, as in the "new & improved" extraction proof Oxycontin OP in the US. Before that Ammonio Methacrylate Copolymer was acceptable and even pre-gelatinized maize, yep as in cornstarch. The particular MS ER pill you're interested in uses hydroxyethyl cellulose, hydroxypropyl cellulose & hypromellose as it's "Goop".

Actually the Hypromellose and the Hydroxyethyl cellulose gels while the Hydroxypropyl cellulose binds and helps to form a union for proper Bi-Phasic release of API or active pharmaceutical ingredient (MS).

Regardless of the medium used, they are designed to diffuse the drug out in two stages. The stages occur at around 0.6 hours and 6.9 hours for an even effect of the Morphine sulfate being released. Breaking a tablet allows drug being saved for a later delivery to "leach" out quicker as more surface area is exposed changing the kinetics and the integrity of the pill. With a whole pill it dumps the first stage out quickly peaking at 0.6 hrs so it can take effect saving the next release for a peak at around 6.9 hrs so it wears off right at 12 hours or at least close to that. If it leached for the whole 12 hours then the pill would work for 16-17 hours.

Usually with short acting opioids, 40% is used for the first stage with a small amount continuing to diffuse up until the second peak when the last remaining amount is expelled. The Bi-Phasic release curve is shaped like a plateau that slants forward a little depending on the manufacturer. It's main goal is to avoid spikes and keep an even amount in circulation.

If you vomited after 6 hours, it would take some serious work to get that blob of time release excipients back up. Depending on the release medium, it can be like nacho cheese at the end and way down the waterslide of yer gullet.

 

[quietcowgirl]

The ER formulations are evolving these days into hard, plastic like pellets from Polyethylene Oxides, as in the "new & improved" extraction proof Oxycontin OP in the US. Before that Ammonio Methacrylate Copolymer was acceptable and even pre-gelatinized maize, yep as in cornstarch. The particular MS ER pill you're interested in uses hydroxyethyl cellulose, hydroxypropyl cellulose & hypromellose as it's "Goop".

Actually the Hypromellose and the Hydroxyethyl cellulose gels while the Hydroxypropyl cellulose binds and helps to form a union for proper Bi-Phasic release of API or active pharmaceutical ingredient (MS).

Regardless of the medium used, they are designed to diffuse the drug out in two stages. The stages occur at around 0.6 hours and 6.9 hours for an even effect of the Morphine sulfate being released. Breaking a tablet allows drug being saved for a later delivery to "leach" out quicker as more surface area is exposed changing the kinetics and the integrity of the pill. With a whole pill it dumps the first stage out quickly peaking at 0.6 hrs so it can take effect saving the next release for a peak at around 6.9 hrs so it wears off right at 12 hours or at least close to that. If it leached for the whole 12 hours then the pill would work for 16-17 hours.

Usually with short acting opioids, 40% is used for the first stage with a small amount continuing to diffuse up until the second peak when the last remaining amount is expelled. The Bi-Phasic release curve is shaped like a plateau that slants forward a little depending on the manufacturer. It's main goal is to avoid spikes and keep an even amount in circulation.

If you vomited after 6 hours, it would take some serious work to get that blob of time release excipients back up. Depending on the release medium, it can be like nacho cheese at the end and way down the waterslide of yer gullet.

Thank you! This is exactly the type of information I was looking for!
So the pill turns into a hell in your stomach? How much is released at the first peak? Is it a full 60mg or is it 30 and then another 30?g

 

[Automator]

Thank you! This is exactly the type of information I was looking for!
So the pill turns into a hell in your stomach? How much is released at the first peak? Is it a full 60mg or is it 30 and then another 30?g

Looks like 30 then 30 after 6.9 hours.

 

[Jekyl Anhydride]

The release curves differ depending on the excipients and time release formulation, but for the most part the peaks aren't very steep aside from the initial release. Some of the brand names only have an actual peak at 4 hours an then just descend from there. 0.6 & 6.9h are more specific to the MS-contin/ oxycontin release formulations with the Ammonio Methacrylate Copolymer formulation. Kadian's 24 hour release is the flattest regarding peaks but for the most part you can expect 20mg within 90 mins, another 10 over the next 200mins with a final small bump 130 mins after that followed by an ever steepening curve. It def varies with the generics but a right slanting plateau or two small bumps (vs peaks) about 5 hours apart is the norm.

 

[quietcowgirl]

So I ended up trying half, which didn?t do much at all so yesterday I tried a whole one. It was...weird. At first I just noticed a weird head rush about an hour after taking it, then felt this odd.. calm feeling. I wasn?t tired or dopey but I was real mellow? It was comparable to smoking pot without high thc in it. I was also rather emotional and short tempered and I couldn?t seem to warm up throughout the day. It was weird, and not at all like the energetic feeling I get from oxy or norco. I don?t think I?ll try it again, it was rather unemployable. But the odd thing happened when I tried my normal dose of oxy this morning; that same calm feeling happened! Wtf? Did I ruin my receptors or something?

 

[Keif' Richards]

Cowgirls can't be quiet. We're starting off from a point of suspicion my friend. There are a lot more unclassy jokes to unpackage here, but sadly, got no time You've got several questions and I've got an article to write. So, in the immortal words of Barbara Bush, "Let's fuck this motherfucking shit up bitches".

- You must be more specific. Controlled-Release technology has evolved significantly over the past decade, from what was once a wholly inelegant and elementary system like that of Oxycontin (that will indeed be beaten by crushing, the OP's are different, more resilient), to mechanisms like that of Lisdexamphetamine (Vyvanse) which are only made active by specific processes in the body that are not so easy to replicate in vitro.

Morphine in the form of MSContin, which I believe is similar to what you have, is mostly beaten through crushing.

- Essentially, there are layers to this medication. It's my belief that this preparation is meant to be continually-released, not like, in two separate bolus doses.

- That's a very complicated question. If someone can answer it accurately, great, but I feel that's a bit of work. You would do best to consult the manufacturer on this one. While many of us are pretty well-versed in this sort of thing, we still speak in relatively vague terms and you're looking for an answer than can be taken to the bank.

- Again, without getting too specific, when one vomit's they typically are only expelling the contents of the stomach itself, not those of the entire GI tract. The small intestine is the much more permeable and better for drug absorption than the stomach, so many drugs are absorbed in the intestines, not the stomach, as is commonly thought. For this reason at the 6 hour mark, I believe any extended-release aspect of your pills should be long gone and your Morphine should be, at the most still sitting in your intestinal area waiting for absorption, hence, vomiting would probably not be so detrimental.

You can vomit up content, really, all the way to feces, but it's uncommon for a healthy individual to vomit anything other than their stomach contents and maybe just the beginning contents of the intestine. Hope that helps.

 

[Lelo]

Anyone know if I have taken 160mg of vyvanse at 5pm how much klonipin would I have to take to get sleep or will I be just wasting my benzoids and not get sleep at all