Hey folks
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Hey folks
Bit of an odd practical biochemistry question in relation to the absorption speed of any meds.
Hypothetically-speaking, is it possible to turn an instant release (IR) med into an extended-release¹ (ER) version via non-commercial means?
Examples of IR meds might include:
- A capsule (designed to dissolve in the stomach) containing an easily-absorbed powder.
- A tablet without any coating and a structure that dissolves very easily.
Examples of ER meds we've seen include:
- Capsules containing tiny pellets, coated with something to slow absorption.
- Tablets with a coating designed to slow absorption.
Could you, for example:
- Encase the capsule in a larger, acid-resistant / enteric capsule?
- e.g., like the ones described here
- Coat the tablet in some kind of food-safe coating?
Genuinely asking here, as we neither have the spoons nor time to go down an AuDHD rabbit hole investigating this
#biochemistry #AskFedi #GenuinelyAsking #NoReplyGuysPlease
¹ aka prolonged, sustained, modified, or controlled release
@SleepyCatten It depends, but it can be tricky. Quite a bit of the complexity of coating for oral medicines involves arranging the coating to dissolve in an appropriate (variable) part of tthe digestive tract. Your options are limited if you're trying to restrict yourself to only adding coatings, not replacing any.
A typical mechanism for these capsules-filled-with-pellets is, the pellets have different coatings, some designed to dissolve slower, some designed to dissolve faster. You really can't replicate this by adding something around a pre-assembled capsule. You might be able to do something like that if you were willing to take the capsule apart and add coating to some of the pellets.
And, well, then there's the issue that sometimes, you don't care just about slowing the relese, but that the release curve be adequately shaped, such as 'mostly flat' or, alternatively, 'three bumps, equally spaced', or maybe 'initial release followed by compensating for power law excretion, to keep the blood level flat'. And ensuring those requires calibration that is hard to do right with just kitchen and/or garage tools.
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@SleepyCatten It depends, but it can be tricky. Quite a bit of the complexity of coating for oral medicines involves arranging the coating to dissolve in an appropriate (variable) part of tthe digestive tract. Your options are limited if you're trying to restrict yourself to only adding coatings, not replacing any.
A typical mechanism for these capsules-filled-with-pellets is, the pellets have different coatings, some designed to dissolve slower, some designed to dissolve faster. You really can't replicate this by adding something around a pre-assembled capsule. You might be able to do something like that if you were willing to take the capsule apart and add coating to some of the pellets.
And, well, then there's the issue that sometimes, you don't care just about slowing the relese, but that the release curve be adequately shaped, such as 'mostly flat' or, alternatively, 'three bumps, equally spaced', or maybe 'initial release followed by compensating for power law excretion, to keep the blood level flat'. And ensuring those requires calibration that is hard to do right with just kitchen and/or garage tools.
@SleepyCatten If you don't mind me asking, do you have a particular medicine in mind?
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@SleepyCatten Sadly it's not that easy!
- In fact you need some really professional gear if you want a slow, prolonged release and not merely a delayed release post-stomach, because that requires layering with specific carrier media and really is challenging.
- Even for material scientists and pharmacologists unless they know exactly the kind of medication they have to target and where it should be released, it's really hard for anything gastrointernally consumed.
The most efficient and slow release I know is transdermal, tho that does come with issues of it's own.
- I mean, #Gynokadin and other #Estrogen gels are alcohol-soluble and gel'd with glycerin to enshure proper application.
- And just like with transdermal Fentanyl patches, unless the applicant is also the patient, it's basically necessary to use latex or nitrile gloves.
@kkarhan That was kinda our feeling on the matter from the limited amount of info we absorbed before catching ourselves falling into a deeper AuDHD into rabbit hole, but we thought it best to ask.
We're mostly asking where it's possible to acquire IR versions of meds but not the ER/PR/SR/CR versions.
We suppose delayed-release (DR) would still be helpful though where the meds are more sensitive to stomach acid, but we'd imagine any further delay would require some kind of complex matryoshka encapsulation or coating
- In fact you need some really professional gear if you want a slow, prolonged release and not merely a delayed release post-stomach, because that requires layering with specific carrier media and really is challenging.
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afaik, ER is often made of some kind of nanostructure. but i don't know if that's true, i just heard that from someone else a bunch of years ago.
@burnitdown Oftentimes, it's just marketing talk justified by "we looked into our old fancy thing in an electron microscope, and noticed that there's nano-sized things in there! Now, it's a cool new nano-thing! We're already writing the patents!"
But there's exceptions, mostly having to deal with cases where the precise shape of either the release curve or the blood level curve really matters. Some enzymes can also cause trouble in some contexts, and some countermeasures against those can be legitimately described as "nanotech".
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@SleepyCatten When I was on ER Adderall, I asked my doctor about the differently colored pellets inside the capsule, and apparently it was, in fact, basically a cocktail of various delayed-release flavors of the drug mixed together. My IR of the same drug, on the other hand (my rx was to take the IR if I still needed to focus after the 8 hours were up) was a solid tablet of Adderall and a binder.
In theory, if you can figure out a way do make those little delayed-release micro-pellets, you could convert one to the other, but that would probably require a chemistry lab, and almost certainly you'd need one to separate the drug from the binder.
@SymTrkl Adderall is a special case, though: it doesn't just do different coatings, it starts from different salts. A part of the reason why it does it so weirdly is, this is really old tech for an old medicine.
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@kkarhan That was kinda our feeling on the matter from the limited amount of info we absorbed before catching ourselves falling into a deeper AuDHD into rabbit hole, but we thought it best to ask.
We're mostly asking where it's possible to acquire IR versions of meds but not the ER/PR/SR/CR versions.
We suppose delayed-release (DR) would still be helpful though where the meds are more sensitive to stomach acid, but we'd imagine any further delay would require some kind of complex matryoshka encapsulation or coating
@SleepyCatten anything but direct release requires either chemical encapsulation and/or layering into slowly dissolving material.
- If it was as easy as advertised then the Oxycontin - co-created #OpioidCrisis would not have grown that much and that quickly.
I mean, I know a [fmr.] material scientist who worked on encapsulation techniques but getting a slow release effectively and reproduceably done is a challenge in and of itself, as also absorbtion rate and dissolvement rate rapidly fluctuates between individuals and for it to work it needs to be rather consistent.
- Kinda like how any fizzy tablet is dissolving differently fast whether one has water, isotonic salt solution and whether the PH is 1 or 15.
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@SleepyCatten Sadly it's not that easy!
- In fact you need some really professional gear if you want a slow, prolonged release and not merely a delayed release post-stomach, because that requires layering with specific carrier media and really is challenging.
- Even for material scientists and pharmacologists unless they know exactly the kind of medication they have to target and where it should be released, it's really hard for anything gastrointernally consumed.
The most efficient and slow release I know is transdermal, tho that does come with issues of it's own.
- I mean, #Gynokadin and other #Estrogen gels are alcohol-soluble and gel'd with glycerin to enshure proper application.
- And just like with transdermal Fentanyl patches, unless the applicant is also the patient, it's basically necessary to use latex or nitrile gloves.
@kkarhan The OROS capsule is a really neat cheap way to actually do well-controlled slow releases. In theory, once the patent will be gone, you should be able to buy the empty capsules, put your own drugs in them, and get very flat release profiles for whatever you want that can be taken orally.
- In fact you need some really professional gear if you want a slow, prolonged release and not merely a delayed release post-stomach, because that requires layering with specific carrier media and really is challenging.
-
@kkarhan The OROS capsule is a really neat cheap way to actually do well-controlled slow releases. In theory, once the patent will be gone, you should be able to buy the empty capsules, put your own drugs in them, and get very flat release profiles for whatever you want that can be taken orally.
@riley @SleepyCatten Granted, those are microcapsules?
Cuz like stomach-acid resistant retard capsules ain't the problem, but slow and prolonged release is and that usually requires microcapsules and a delaying binder to slowly release those...
The problem isn't a patent but getting it assembled.
Kevin Karhan :verified: (@kkarhan@infosec.space)
@SleepyCatten@cultofshiv.wtf anything but direct release requires either chemical encapsulation and/or layering into slowly dissolving material. - If it was as easy as advertised then the Oxycontin - co-created #OpioidCrisis would not have grown that much and that quickly. I mean, I know a [fmr.] material scientist who worked on encapsulation techniques but getting a slow release effectively and reproduceably done is a challenge in and of itself, as also absorbtion rate and dissolvement rate rapidly fluctuates between individuals and for it to work it needs to be rather consistent. - Kinda like how any fizzy tablet is dissolving differently fast whether one has water, isotonic salt solution and whether the PH is 1 or 15.
Infosec.Space (infosec.space)
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@kkarhan The OROS capsule is a really neat cheap way to actually do well-controlled slow releases. In theory, once the patent will be gone, you should be able to buy the empty capsules, put your own drugs in them, and get very flat release profiles for whatever you want that can be taken orally.
@kkarhan On a related note, there's this thing, which can be electronically controlled: https://www.science.org/doi/10.1126/sciadv.adj3003. If you don't want flat release profile, but something complicated or maybe even feedback-controlled, you could hack a tiny swallowable release pump upon this sort of thing.
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@riley @SleepyCatten Granted, those are microcapsules?
Cuz like stomach-acid resistant retard capsules ain't the problem, but slow and prolonged release is and that usually requires microcapsules and a delaying binder to slowly release those...
The problem isn't a patent but getting it assembled.
Kevin Karhan :verified: (@kkarhan@infosec.space)
@SleepyCatten@cultofshiv.wtf anything but direct release requires either chemical encapsulation and/or layering into slowly dissolving material. - If it was as easy as advertised then the Oxycontin - co-created #OpioidCrisis would not have grown that much and that quickly. I mean, I know a [fmr.] material scientist who worked on encapsulation techniques but getting a slow release effectively and reproduceably done is a challenge in and of itself, as also absorbtion rate and dissolvement rate rapidly fluctuates between individuals and for it to work it needs to be rather consistent. - Kinda like how any fizzy tablet is dissolving differently fast whether one has water, isotonic salt solution and whether the PH is 1 or 15.
Infosec.Space (infosec.space)
@kkarhan These are effectively tiny swallowable syringes that get slowly pushed as they absorb, at a nearly constant rate, water from the digestive tract. This is a video that explains how the osmotic control works. https://www.youtube.com/watch?v=zaUaVsbACoY
Concerta, for ADHD, seems to have been the first one that did it this way, but as can be seen from the attached pictures, there's now other medicines that come out of factory with OROS delivery systems.
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@kkarhan On a related note, there's this thing, which can be electronically controlled: https://www.science.org/doi/10.1126/sciadv.adj3003. If you don't want flat release profile, but something complicated or maybe even feedback-controlled, you could hack a tiny swallowable release pump upon this sort of thing.
@kkarhan ADHD medicines are often seen as being particularly needful of flat relese profiles, so, naturally, somebody also did transdermal methylphenidate patches. But it was never approved in Europe, and from what I hear, might have been stopped being marketed in USA, as well. (As far as I can tell, for market reasons, with a wee bit of involvement from the War On Drugs, not because it was a bad way to deliver the medicine.)
SleepyCatten@cultofshiv.wtf
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