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How to Make Your Own Extended Release Pills


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#1 devinthayer

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Posted 15 June 2011 - 04:54 AM


I tried looking up how to make your own time released supplements, and the best I found was some druggie forum talking about a few methods, some quite confusing. The topic starter eventually decided to try and make his own time release (caffeine) pills using candle wax. I though that was a bit crude and possibly unhealthy, but it was a druggie forum, ya know... This is LongeCity. You guys know what ain't going to kill me. Wax matrices are used in all sorts of formulas for TR/XR medicines such as Concerta and Oxycotin.

Is it possible to make my own crude time release tablets using edible paraffin wax and maybe some starch or oil?

I'm sick of taking my supplements 3x or 4x a day if I could take it 2x and be okay.

Has anyone seriously done this or something equally easy, safe, and effective?

Edited by devinthayer, 15 June 2011 - 04:57 AM.

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#2 jadamgo

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Posted 15 June 2011 - 07:38 PM

I think it would work, as long as you used food-grade or pharmaceutical-grade wax. You ought to combine an edible wax that is solid but soft at body temperature together with lecithin and perhaps a bit of edible oil such as olive oil, and of course, your desired supplement or medication.
Write down your recipes, and find the right proportions of wax to lecithin that will maintain solidity at room temp, and make it melt at around 100 degrees -- a degree or two higher than internal body temperature.

Acidic salts of lipophilic substances, e.g. methylphenidate neutralized into methylphenidate hydrochloride, might do better if re-basified back into lipophilic form.
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#3 Robert C

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Posted 15 June 2011 - 09:25 PM

My compounding pharmacy makes "slow release" meds and supps by mixing them with celulose. It is supposed to realease over 8 to 10 hours. It forms a sticky non digestable ball in you GI tract and the ball slowly disolves over time releasing the med.
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#4 devinthayer

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Posted 15 June 2011 - 09:26 PM

I think it would work, as long as you used food-grade or pharmaceutical-grade wax. You ought to combine an edible wax that is solid but soft at body temperature together with lecithin and perhaps a bit of edible oil such as olive oil, and of course, your desired supplement or medication.
Write down your recipes, and find the right proportions of wax to lecithin that will maintain solidity at room temp, and make it melt at around 100 degrees -- a degree or two higher than internal body temperature.

Acidic salts of lipophilic substances, e.g. methylphenidate neutralized into methylphenidate hydrochloride, might do better if re-basified back into lipophilic form.


Thanks for the input! Lecithin is a great emulsifier that I totally spaced. Just a couple questions...

How do I control heat to 100 degrees? It's not a setting on any oven that I own...lol.
Explain a little bit more about lipophilic forms and neutralization... what is it and what method is best? You got a guide you can link?
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#5 jadamgo

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Posted 15 June 2011 - 10:44 PM

The cellulose idea sounds good too, in fact, it would probably be way easier. Just mix the supplement with the powder, and stick it in a capsule. Part of it would release immediately, and part would be trapped in the sticky mass.

The lecithin/wax idea would be like a stomach-acid-proof coating, if you need to deliver something (like selegiline) that doesn't handle acid very well. If you want to do this, you could use a double-boiler to heat the wax and lecithin together. Now that I think of it, liquid lecithin would probably be a better idea, because you wouldn't have to complicate the proportions by also adding oil. I'd start with about 3/4 paraffin wax with 1/4 liquid lecithin, and see if that melts somewhere around or just above body temperature.

Really, what you want is for the wax/medicine/lecithin mixture to be very soft at body temperature, so the bile acids in the small intestine (which are like soap or detergent to dissolve fatty foods) can gradually dissolve it, but not so quickly that it behaves like an instant-release. That's why a final melting point of around 100-105 would be good, because if it was liquid at body temperature, the sustained release wouldn't be very sustained.

As for neutralization, I'm now thinking that this wouldn't really be necessary. It would create far more problems than it would solve. So forget about that, because it complicates things for no good reason.

Really, I think the cellulose idea is easier than the wax idea, and would work quite well for many substances. I'd try it first if I were you. It would be really simple -- mix powdered medication/supplement together with powdered cellulose, and stick it in capsules.

The only problem would be with substances that are very bulky, since you'll need to use way more cellulose powder than supplement powder to extend the release. If you wanted to make a sustained-release piracetam dose of 4 g, for example, you'd have to mix it with something like 10-20g cellulose powder. God only knows how many pills you'd have to take! But for something like caffeine or picamilon, with doses in the tens to low-hundreds of milligrams, you could fit a hefty dose into 1-3 medium/large capsules. (I forget whether those are the 0 or the 00 capsules... I'm thinking of the ones that usually fit about 800-1100mg piracetam per capsule... surely someone here knows which size that is?)
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#6 niner

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Posted 16 June 2011 - 02:53 AM

Which supplements do you want to make an extended release formulation for? The most frequently I take anything is twice a day, which isn't too tough.
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#7 devinthayer

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Posted 16 June 2011 - 03:25 AM

The cellulose idea sounds good too, in fact, it would probably be way easier. Just mix the supplement with the powder, and stick it in a capsule. Part of it would release immediately, and part would be trapped in the sticky mass.

The lecithin/wax idea would be like a stomach-acid-proof coating, if you need to deliver something (like selegiline) that doesn't handle acid very well. If you want to do this, you could use a double-boiler to heat the wax and lecithin together. Now that I think of it, liquid lecithin would probably be a better idea, because you wouldn't have to complicate the proportions by also adding oil. I'd start with about 3/4 paraffin wax with 1/4 liquid lecithin, and see if that melts somewhere around or just above body temperature.

Really, what you want is for the wax/medicine/lecithin mixture to be very soft at body temperature, so the bile acids in the small intestine (which are like soap or detergent to dissolve fatty foods) can gradually dissolve it, but not so quickly that it behaves like an instant-release. That's why a final melting point of around 100-105 would be good, because if it was liquid at body temperature, the sustained release wouldn't be very sustained.

As for neutralization, I'm now thinking that this wouldn't really be necessary. It would create far more problems than it would solve. So forget about that, because it complicates things for no good reason.

Really, I think the cellulose idea is easier than the wax idea, and would work quite well for many substances. I'd try it first if I were you. It would be really simple -- mix powdered medication/supplement together with powdered cellulose, and stick it in capsules.

The only problem would be with substances that are very bulky, since you'll need to use way more cellulose powder than supplement powder to extend the release. If you wanted to make a sustained-release piracetam dose of 4 g, for example, you'd have to mix it with something like 10-20g cellulose powder. God only knows how many pills you'd have to take! But for something like caffeine or picamilon, with doses in the tens to low-hundreds of milligrams, you could fit a hefty dose into 1-3 medium/large capsules. (I forget whether those are the 0 or the 00 capsules... I'm thinking of the ones that usually fit about 800-1100mg piracetam per capsule... surely someone here knows which size that is?)

You are a fricking genius. Cellulose sounds like a bad idea by itself because the mixture I want is about 660mg medicine currently in my ADHD stack: 350mg DMAE Tartrate, 200mg Pramiracetam, 50mg Picamilon, 25mg Hordenine, 25mg DMAA, and 10mg Huperzine 1%. A 000 capsule will hold about 1350mg. I was thinking that I could take two capsules at a time 2x a day.

The main reason for this is the sustained hordenine release is a crazy cheap NRI, especially when mixed with caffeine or DMAA due to it's MAO substrate qualities. The second reason is that the DMAE effects as a light circulatory stimulant diminish fairly quickly. I could eat that stuff all day. I think it goes right through me, so a sustained release would help keep it in my blood stream a bit longer, possibly providing better long-term benefits like lipofuscin removal, DNA repair, and antioxidation. Lastly, the Pramiracetam effects seem to only last 4 hours, and I'd like that to be more like 8.

On a side note, Picamilon seems to be a great supplement to take the edge off stimulants... haven't found this quality in many other things besides plain old B Vitamins and a good meal. 100mg was almost knocking me out, so I cut back and saw a huge increase in energy and mental capacity. It's like a balancing act with GABAergic supplements. To get these all released at the same time would be saweeet, so that I can have that synergy all the time and not have everything bell curve at different times.

Anyhow, I can't wait to try the lecithin/wax combo. Would adding a little cellulose to the outside harden it up for a timed release? What about tapioca dextrose?

Edited by devinthayer, 16 June 2011 - 03:35 AM.

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#8 Robert C

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Posted 16 June 2011 - 04:22 AM

As a way to check your time release you could could make a few up and mix in a stout dose of vitamin b2 and see how long your urine is bright yellow.
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#9 devinthayer

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Posted 16 June 2011 - 04:32 AM

As a way to check your time release you could could make a few up and mix in a stout dose of vitamin b2 and see how long your urine is bright yellow.

Haha that's awesome! B2 is the yellow one? I knew at least one of them was. I have a B/C complex tablet I can crush into a powder at 660mg. That's an ingenious idea.
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#10 jadamgo

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Posted 16 June 2011 - 04:39 AM

I don't know anything about tapioca, and I'm not sure what effects you'd get from adding cellulose to the outside of a lecithin/wax capsule. The best way to extend the release further would be to make the ingredients more solid, by increasing the ratio of wax to lecithin. If you're using about 350mg supplement per capsule, you might combine that with 800mg wax and 200mg lecithin. Or even 850mg wax and 150mg lecithin. This would mean proportions of 17 parts wax to 7 parts supplement to 3 parts liquid lecithin.

Your plan for 2x 000 capsules twice a day would probably work well. As a fellow ADHDer, I understand the problem of remembering to take the pills that help you remember things. Sustained release is your friend. (What would I do without Concerta? No other MPH formulation works quite like it.)

If you want to smooth out the effects of these things, you could add some aniracetam. A sustained release of aniracetam could be a beautiful thing, acting as a mild tranquilizer to counteract stimulant side effects (just like picamilon, but aniracetam causes a different subjective feeling) and yet also becoming a gentle stimulant and memory enhancer itself, starting around 2-3 hours after you take it.

Subjectively, I find that frequent microdoses of aniracetam cause similar effects to a strong cup of chinese black or green tea. Good chinese teas have high levels of both theanine and caffeine that provide a combined stimulant and anti-stress effect, almost like meditation-in-a-cup. 75-100mg of aniracetam per capsule (so 150-200mg per dose) would be great, if you're interested.
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#11 Robert C

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Posted 16 June 2011 - 01:03 PM

Yes vitamin B2 is the B that makes your urine bright yellow. I think you can also buy it as a single vitamin at various vitamin relailers if you wanted to keep the amount of things in your mix to a minimum.
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#12 MrSpud

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Posted 17 June 2011 - 04:08 AM

It's actually very complex to get timed release formulations to work properly. It is easier to get delayed release or enteric release where you tend to not get anything right away then an hour or 2 later you get the dose all at once. Waxy matrixes are unpredictable and it might go right through you without releasing some or all of the actives. Parrafin wax also isn't the best thing to ingest. Beeswax/soybean oil/lecithin would be a better choice but would still be unpredictable in terms of releasing the actives in a controlled release manner. This is actually what is used in immediate release softgel suspension formulations but would become more of a delayed/extended release as the amount of beeswax is increased. The cellulose polymers are the easiest way to get a reproducable time release matrix. Here's how it's done if you want to know. http://www.colorcon....atrix_broch.pdf If the link doesn't work just poke around in https://www.colorcon...ease/Literature til you find the one called Using METHOCEL™ Cellulose Ethers for Controlled Release of Drugs in Hydrophilic Matrix Systems


You can also browse through some of these articles to get more ideas on how to do it properly https://www.colorcon...ease/Literature

The controlled release polymers were invented by DOW but now Colorcon sells them.

Edited by MrSpud, 17 June 2011 - 04:51 AM.

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#13 devinthayer

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Posted 25 June 2011 - 02:00 AM

It's actually very complex to get timed release formulations to work properly. It is easier to get delayed release or enteric release where you tend to not get anything right away then an hour or 2 later you get the dose all at once. Waxy matrixes are unpredictable and it might go right through you without releasing some or all of the actives. Parrafin wax also isn't the best thing to ingest. Beeswax/soybean oil/lecithin would be a better choice but would still be unpredictable in terms of releasing the actives in a controlled release manner. This is actually what is used in immediate release softgel suspension formulations but would become more of a delayed/extended release as the amount of beeswax is increased. The cellulose polymers are the easiest way to get a reproducable time release matrix. Here's how it's done if you want to know. http://www.colorcon....atrix_broch.pdf If the link doesn't work just poke around in https://www.colorcon...ease/Literature til you find the one called Using METHOCEL™ Cellulose Ethers for Controlled Release of Drugs in Hydrophilic Matrix Systems


You can also browse through some of these articles to get more ideas on how to do it properly https://www.colorcon...ease/Literature

The controlled release polymers were invented by DOW but now Colorcon sells them.

Cool! Found methylcellulose for $31/pound. Not sure about the colorcon (hydroxypropyl methylcellulose)... PM me (or post it) if you find out where to buy that.
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#14 devinthayer

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Posted 25 June 2011 - 02:24 AM

Did the lecithin/paraffin combo... but I sucked at it. I only have the granules (local GNC didn't have powder or liquid), so I threw 15g in some water and a tsp of oil and boiled it. When the water was looking low and gravy-like, I added 14g of paraffin and stirred it up until it reached consistency. I let it cool in a glass as I stirred it into a gummy-goo that was oozing water as it cooled. I drained what I could.

Realizing that there was still a lot of water in the mix, I boiled it out. When the last few water bubbles popped out, it started turning brown, so I lifted it off the burner as quickly as I could, but it was burned. If anyone has made ghee (butterfat), this is common. I put it in a glass and swirled it until it was cool. The resulting substance was just like play-dough in the warmth of my hands.

This morning I added 60mg of DMAA into about a gram of the stuff and mushed it together and kneaded it. The reason why I did this is because DMAA will have a stimulating effect at 30mg or less and a reverse effect after 50mg. If I felt stimulated afterwards, then the time release worked. If I felt tired, the time release failed.

Guess what? I ruined the experiment by drinking coffee and eating two energy chews. Damnit, didn't engineering school teach me anything? I didn't feel tired, but that doesn't mean anything other than 60mg of DMAA doesn't inhibit caffeine stimulation at 200mg. I could have guessed that...

Anyhow, should I still experiment with this batch or try something else?
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#15 niner

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Posted 25 June 2011 - 03:14 AM

I don't see the point of the water.. Why not just dissolve the lecithin in wax? (assuming it would go in...) MrSpud is The Man on this stuff; I'd go with what he says.
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#16 MrSpud

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Posted 25 June 2011 - 07:41 AM

I really don't think it will work that great without lots of trial and error with the amount of wax, but if I was going to try this, I'd add the beeswax to vegetable oil (canola oil woild work fine) in something made of stainless steel (a metal beaker or a small cooking pot). Then I would heat this until the wax melts. When the last of the wax is melted, take it off of the heat source and immediately add the lecithin (add enough lecithin to equal 2% of the oil not counting the weight of the wax). then gently stir it occasionally with a steel spatula or a spoon as it starts to cool. When the wax/oil/lecithin mix starts to become hazy then you would add the powder and stir it vigorously until it is room temperature. I'd start with about 10% beeswax (10% of the oil and lecithin not including the powder) and then work my way up a couple % at a time until you get the resulting suspension to be a semisolid after it sets up for 24 hours. You would want to use at least a 50:50 ratio of oil/wax/lecithin to powder (you can use more of the oil/wax/lecithin than 50% but if you use less than 50% you'll end up with a powdery mess. This is actually how you would make a suspension to fill into a softgel capsule, but for a softgel you would only add enough wax to make a permanent suspension but it would still be a flowably liquid and the wax wouldn't be at a high enough level to slow down the disintegration. If you increase the level of wax until it is a semisolid it's disintegration would be slowed down at least somewhat.

Another old fashioned way to make a prolonged release tablet is to just load it up with stearic acid. It is waxy and waterproofs the tablet. About 2% or less of stearic acid is used as a tablet lubricant and doesn't make the tablet disintegrate slow, but as you increase the level of stearic acid above those levels it slows down the disintegration. You can still find a number of prolonged release supplements that are made this way.

Neither of these waxy techniques will give you a true timed release, but you can get a delayed or prolonged release that sort of works. The colorcon type cellulose polymers are better at making a very predictable true timed release. You shouldn't use regular cellulose polymers, you need the fancy high molecular weight ones. The regular hydroxypropyl methylcellulose acts as a binder for tablets and a filler for capsules but actually absorbs water and swells up quickly and makes an instant release. The higher molecular weight ones make the thick gel plug that slowly releases the actives over time. I don't know if colocon gould give you any or not if you asked them for a sample, but they might. They also might tell you where you could buy a small amount if you wanted to experiment.

Edited by MrSpud, 25 June 2011 - 07:50 AM.

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#17 devinthayer

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Posted 28 June 2011 - 06:06 PM

To sum up, the ingredient in pills that I am looking for is a pharmaceutical disintegrant to mix with an emulsifier to consistency and then to add powder of whatever.

If I can find an at-home wax matrix formula using house-hold ingredients, that would be awesome. There are so many ideas here, I am actually having trouble deciding where to start again. The paraffin/lecithin combo wasn't really all that. To be honest, it didn't hold the power very well and kept coming out as I mixed it at much less than 50% powder. Probably more around 20%.

I would like to try cellulose polymers as suggested. However, I don't have a company right now, so I wouldn't feel comfortable ordering manufacturer direct. I'd rather buy from Ebay, Amazon, Buy, iHerb, etc. if you know what I mean. Are there any other disintegrant products available at wholesale/online prices?

Perhaps adding beeswax and oil will help it hold better... and possibly stearic acid and starch to harden up the matrix...

PS: I added water to the Lecithin granules because they weren't dissolving. GNC added some type of phosphate or something. I don't know if that mattered, but I do know that the granules were getting harder rather than softer after sitting in the melted wax.
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#18 MrSpud

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Posted 28 June 2011 - 09:11 PM

If you are going to try the beeswax/vegetable oil/lecithin then you should use liquid lecithin instead of granules. Just poke a pin into a lecithin 1200mg softgel and use the liquid that is inside.

You wouldn't need a disintegrant, you would just use less wax. If you wanted it more solid or to take longer to disintegrate you'd just go up in the beeswax. A disintegrant, if needed, for an oil based system would be something ethoxylated, like tween 80 (polysorbate 80) or one of the gelucires.

For solid formulations a good disintegrant would be crospovidone or crosscarmellose or even some types of starch, but for a prolonged release formula it would be counterintuitive and would be better to just go down in the amount of stearic acid or whatever you are using to delay the release until you get just the right amount.

Go to www.pformulate.com and poke around for more info if needed on these ingredients. I think they have some supplier info available too. I'm not sure if you can get these kinds of ingredients on e-bay, but the beeswax, lecithin, vegetable oil is easy to obtain.

Of course, none of these will produce a real timed release, just some typre of delayed release or prolonged release. For example, one kind of prolonged release tablet (one that uses stearic acid) that I know of has a spec that not more than 50% of the actives are released after 1 hour and not less than 50% of the actives are released after 6 hours in a dissolution test. A true timed release tablet would release at a steady rate the entire time, like 20% released every hour for 5 hours for example.

Also, just so you know, I wouldn't recommend ingesting parrafin wax when beeswax is just as available because parrafin is basically solid mineral oil and is a laxative is large amounts and also is a suspected carcinogen (actually a co-carcinogen that can build up in your system and concentrates oil soluble carcinogens). Beeswax is considered safe and is very common in softgel supplements.

Edited by MrSpud, 28 June 2011 - 09:25 PM.

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#19 nootrop newbie

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Posted 26 January 2013 - 03:21 AM

Is this topic still open?
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#20 niner

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Posted 26 January 2013 - 03:47 AM

Is this topic still open?


All topics are open unless they're closed, which is rare. Closed topics show up with a padlock icon.
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#21 nootrop newbie

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Posted 26 January 2013 - 05:23 AM

Ok thanks!
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#22 nootrop newbie

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Posted 02 February 2013 - 01:45 AM

I just noticed nobody has spoken on this topic for awhile.
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#23 Matt79

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Posted 22 February 2013 - 02:02 AM

Has anyone tried this? I'm interested in slow release caffeine. There are some options, but not any I've found using a quality process and organic source extract.
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#24 astupidperson

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Posted 14 May 2013 - 11:58 AM

This is more of a delayed release idea, but I signed up to share this so hopefully it helps.

I take melatonin to asist with sleepiness, I also like the fact that it helps me with occasional lucid dreams. I heard from a friend it's even better when there's a sustained-release or slow-release.

So I gathered a small 3mg melatonin pill, an empty 00 cap, and a bit of whey protein powder. Then mixed the protein powder with a small amount of water to create a thick paste. After coating the small melatonin cap, I place it in the larger cap.

When I take the melatonin, I'll take 1 regular pill for immediate release and also the delayed release cap.

I'm literally trying this for the first time tonight, so I'm not sure how delayed the release of the cap but I'm sure the protein powder could be replaced with celulose or something different to arrive at the desired delay.

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#25 noot_in_the_sky

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Posted 22 May 2013 - 01:42 PM

So I gathered a small 3mg melatonin pill, an empty 00 cap, and a bit of whey protein powder. Then mixed the protein powder with a small amount of water to create a thick paste. After coating the small melatonin cap, I place it in the larger cap.

When I take the melatonin, I'll take 1 regular pill for immediate release and also the delayed release cap.

I'm literally trying this for the first time tonight, so I'm not sure how delayed the release of the cap but I'm sure the protein powder could be replaced with celulose or something different to arrive at the desired delay.


How was your expirement? Did it went well?

Will it not be better to mix the powder melatonin with the whey protein. It seems if you just cover the pill it will delay the release, rather then extended(ie slowly release melatonin).

Have you try it with casein protein? Some bodybuilders use it during the night to have a source of protein, it may to be a slower release.

Has anyone tried this? I'm interested in slow release caffeine. There are some options, but not any I've found using a quality process and organic source extract.


Hydroxypropyl methylcellulose, is a vegetarian ingredient use for slow release formulas.
Or
You can also use organic soy protein or whey protein.

Edited by noot_in_the_sky, 22 May 2013 - 01:45 PM.

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#26 robosapiens

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Posted 14 August 2013 - 11:28 PM

I'm interested in creating a slow release nootropic blend of noopept, low dose pramiracetam, and aniracetam.

I'll experiment with Niacin at first to detect the timing of skin reddening.

I think one capsule >>some material with beeswax and lecithin or polysorbate 80 >> within a capsule >>more material with beeswax and lecithin might work OK?
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#27 hephaestus

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Posted 05 October 2013 - 01:01 AM

Way late to the party, but I got this book from the library last year and found it very interesting:

http://www.amazon.co...lled release in

I didn't actually try making anything but it has a lot of details on various substrates and designs that can be used for controlled release.
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