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Sublingual NR and NMN

sublingual

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#31 TMNMK

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Posted 08 April 2018 - 02:58 PM

I'd like to put this out there and see what others think:

 

https://pdfs.semanti...ba0ead808ed.pdf

 

"Permeability of water through the buccal mucosa was approximately 10 times higher, whilst in floor of the mouth the permeability was approximately 20 times higher than skin . Drugs can be transported across epithelial membranes by passive diffusion, carrier-mediated active transport or other specialized mechanisms. Most studies of buccal absorption indicate that the predominant mechanism is passive diffusion across lipid membranes via either the paracellular or transcellular pathways .although these may actually be the same pathway. The hydrophilic nature of the paracellular spaces and cytoplasm provides a permeability barrier to lipophilic drugs but can be favorable for hydrophilic drugs. In contrast, the transcellular pathway involves drugs penetrating through one cell and the next until entering the systemic circulation. The lipophilic cell membrane offers a preferable route for lipophilic drugs compared to hydrophilic compounds . Drugs can transverse both pathways simultaneously although one route could be predominant depending on the physicochemical properties of the drug .Although passive diffusion is the predominant mechanism of absorption from the oral mucosa, specialized transport mechanisms have also been reported for a few drugs and nutrients. "

 

If this is the case then I was completely wrong about the hydrophilicity of the molecule making it less efficient for for sublingual administration. And furthermore, a solubilized preparation may be effective for sublingual administration also, either in water or aqueous ethanol perhaps.

 

We still have the question Michael brought up: "absorbed intact into the circulation" but otherwise this seems positive.

 


Edited by TMNMK, 08 April 2018 - 03:07 PM.

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#32 LawrenceW

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Posted 17 May 2018 - 03:30 PM

This may have been discussed before but looking at the prices, Revgenetics is selling 30 days of NMN of just 50 mg for about $35 if you buy two. Alivebynature is $45 a bottle but 250 mg for 30 days. 

 

1) Any idea why RevGenetics's NMN is about 5 times as expensive as AliveByNature's NMN? 

 

2) I can get NR for $30 a bottle of 30 days worth of 250 mg so is there extra value in paying 1.5 times more for the cheapest NMN?

 

 

From:  https://innovareacad...Suppl2/1092.pdf

 

"The  main  mechanism  for  the  absorption  of  the  drug  in  to  oral  mucosa  is  via  passive  diffusion  into  the  lipoidal  membrane3.  The  absorption of the drug through the sublingual route is 3 to 10 times  greater  than  oral  route  and  is  only  surpassed  by  hypodermic  injection.  For  these  formulations,  the  small  volume  of  saliva  is  usually sufficient to result in tablet disintegration in the oral cavity."  

 

So buying Alive by Nature Pure NMN powder and taking it sublingually, you will get a minimum of 3 times as much NMN into the bloodstream than the equivalent NR oral dose, therefore you end up paying a minimum of twice as much for the NR.


Edited by LawrenceW, 17 May 2018 - 03:30 PM.

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#33 able

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Posted 17 May 2018 - 04:11 PM

From:  https://innovareacad...Suppl2/1092.pdf

 

"The  main  mechanism  for  the  absorption  of  the  drug  in  to  oral  mucosa  is  via  passive  diffusion  into  the  lipoidal  membrane3.  The  absorption of the drug through the sublingual route is 3 to 10 times  greater  than  oral  route  and  is  only  surpassed  by  hypodermic  injection.  For  these  formulations,  the  small  volume  of  saliva  is  usually sufficient to result in tablet disintegration in the oral cavity."  

 

So buying Alive by Nature Pure NMN powder and taking it sublingually, you will get a minimum of 3 times as much NMN into the bloodstream than the equivalent NR oral dose, therefore you end up paying a minimum of twice as much for the NR.

 

 

Liu shows that very little NMR and NR make it to the blood from oral supplements.  (Which conflicts with other studies)

 

We don't really know how well NMN is absorbed sublingual, but any direct uptake would seem to be a huge improvement.

 

I don't know if  the "3 to 10 times"  estimate applies, but from my personal experience the last 3 months,I do believe sublingual delivery is much more effective using NMN and some NR.



#34 bluemoon

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Posted 17 May 2018 - 04:31 PM

 

 

So buying Alive by Nature Pure NMN powder and taking it sublingually, you will get a minimum of 3 times as much NMN into the bloodstream than the equivalent NR oral dose, therefore you end up paying a minimum of twice as much for the NR.

 

But then is there a reason to take NMN sublingualy when I can take NR sublingually and for quite a bit less money?


Edited by bluemoon, 17 May 2018 - 04:31 PM.

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#35 Heisok

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Posted 17 May 2018 - 04:41 PM

Hi LawrenceW,

 

If you look at the doses in your link they are 10 mg or less. There is only so much that can be absorbed sublingually. Of course, contact time in the mouth would effect it, but there seems to be a saturation point which once reached, slows the process as the drug is transferred into the system . This would not limit the total dose as some would be absorbed in other parts of the mouth, throat and gastrointestinal system. You are also comparing oral NR to sublingual NMN for your price comparison. All 3 NR sellers capsules which I have taken poured in the mouth dissolved rapidly. Tested one with rice bran this morning, and my memory is correct. As far as effect, it is quickly noticeable.

 

Beyond the possibility of better absorption compared to sublingual, I believe that there is a good reason that TNMNK is having good results with the nasal method. They are taking many small doses spread throughout the day. This allows the system to absorb the amount, and be ready so-to-speak for another dose. It might be recreated taking NMN/NR in very small doses, maybe 20 mg ,sublingually spread out through the day.

 

Conclusion:

 

"The observed Tmax of ~1 h following sublingual administration of asenapine is shown to be consistent with the reported range of Tmax values following sublingual administration of other compounds found in the literature. It is also in line with a proposed model in which drug rapidly partitions into the mucosal membranes, where it is stored for extended periods and then slowly partitions out of this lipid tissue and into the systemic circulation. The bioavailability of a sublingually administered drug at doses below the saturation solubility in the mouth is constant and controlled primarily by a mass transport equilibrium. At doses above the saturation solubility, the bioavailability becomes more dependent not only on the distribution equilibrium but also on contact time in the mouth because additional variables need to be accounted for (e.g., dissolution of excess drug and re-establishing the distribution equilibrium). These explanations were shown to be consistent with oral cavity absorption models from the literature as well as the current clinical data for asenapine."

 

"The bioavailability of a 5-mg sublingually administered dose is around 35%. The bioavailability values of other doses were calculated from clinical data (Fig. 3). The bioavailability is more or less constant at low doses and goes down when the doses exceed around 5 mg. In the non-simulated state around 1 ml saliva is present in the oral cavity (16,17). So, the dose to reach saliva saturation is about 5.4 mg. The observation that higher bioavailability is not observed at doses below the saturation solubility and that bioavailability is constant across this dose range is consistent with a rapid mass transport equilibrium being established between drug in solution in the mouth and drug in the mucosal membranes (Fig. 1). Once the mass transport equilibrium has been reached, no further drug absorption into the sublingual membranes is expected unless a shift occurs in the mass balance (e.g., sufficient drug is transported from the mucosal membranes and into the systemic circulation in the relatively short time the drug is in contact with the oral cavity). At this equilibrium point, the remaining dose, which cannot be absorbed into the mucosal tissues, will simply be swallowed over time."

 

https://www.ncbi.nlm...MC3513449/#CR11
 

 

 

 

 

 


Edited by Heisok, 17 May 2018 - 05:07 PM.

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#36 orion22

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Posted 01 July 2018 - 06:12 PM

safe to take true niagen brand sublingual it contains Microcrystalline cellulose?


safe to take true niagen brand sublingual it contains Microcrystalline cellulose?



#37 male_1978

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Posted 02 July 2018 - 06:32 AM

I have a stupid question about taking NR sublingually. If you take it that way, how long are you waiting before swallowing again? How long do you think will it take for 100 mg of NR powder to get absorbed in the mouth?



#38 AliceTu

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Posted 03 July 2018 - 08:44 PM

I have a stupid question about taking NR sublingually. If you take it that way, how long are you waiting before swallowing again? How long do you think will it take for 100 mg of NR powder to get absorbed in the mouth?

I've been doing sublinguals (b12s) for years, and NR/NMN sublingual as powders for a month and change, so I'll take a stab at answering this.

It's not about whether you swallow or not. It's about how much time the substance has to interact with your oral mucosa, ideally the musoca that has the best blood flow, which is why we typically put it under the tongue (though some swear by upper-gums-and-cheek). The point is not to avoid swallowing, but to keep the stuff against the mucosa for as long as you can. You can do both. Well, I can, anyway. :)

Regardless, it's not going to be long. Especially in the case of loose powder, I find that a 1-2 minutes is about as long as the low dose I tuck under my tongue stays before saliva and dissolving make it just another thing that finds it way to my stomach. 

 

I don't know that there is an objective answer to your question about how long for 100mg NR to get absorbed in the mouth. The musoca can only absorb so much, so fast. I don't have data on that for NR (or b12 for that matter; it depends on brand and quality as well), and I haven't run across any data that isn't highly subjective. Mouths and absorption capability varies between individuals, whether stomach or mucosa. Even nasal absorption will vary, depending on the body in question.

 

Some people on these forums feel that any amount of sublingual time is useful. I tend to agree, so I accept whatever sublingual absorption my mouth happens to allow and I don't worry about the rest, because it's going to my stomach, where I would have put it anyway.

If you're using NR sublingual tabs instead of powder, time-to-dissolve also depends on the filler in the tab that makes it dissolve more slowly, which is the point of sublingual tabs, and how slowly that dissolves in your mouth in particular (try not to chew it, for example, which defeats the purpose), but the answer is essentially the same:

As long as possible, but don't make yourself crazy by trying not to swallow. Just try not to swallow what's under your tongue (or your tongue, for that matter) for as long as it is comfortable for you to do so.
 


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#39 able

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Posted 03 July 2018 - 10:41 PM

Nice explanation AliceTu.

 

You mention the dissolve time depends on the fillers, which is key.  

 

Most use a capsule size that fits around 500 mg (depending on density), so is a lot of filler that is unpleasant (to me) sitting in the mouth.  And it depends what they use for filler.

 

Some use a smaller capsule size  which has much less filler and works better.  Sorry, I can't recall now which brands of NR were the smaller capsule, and many are no longer around now. 

 

I do know the Maac10 NMN uses the small capsule, with very little filler, so is ok to use sublingual when Alivebynature powder is out of stock.  

 

The ABN powder  is hands down the best choice imo, as it is just pure NMN, and dissolves within seconds.

 

I am curious to try their new sublingual tablets, but still waiting on delivery.

 


Edited by able, 03 July 2018 - 10:43 PM.

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#40 Oakman

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Posted 08 July 2018 - 07:54 PM

Got my 'New Sublingual' NMN tabs last week, and have taken some. I use it with other NAD+ boosters, in something like the original ABN formula , that is,  Niacin, Tryptophan, NR, Nicotinamide. I think it works, but really, I can't tell.

 

However, I have some concerns about their new formulation:

 

1) each tablet is approximately the size of a dime, and three times as thick. It weighs almost a gram. This shape and size is not easily kept under the tongue as they suggest to do. It's not comfortable. It would be better formed into a capsule shape that would fit under the tongue. And/or make the cap half size by simply cutting out half the non-NMN ingredients. Or cut the dose in half per tab.

 

2) It takes more than a while to dissolve. I've kept in there for up to 20 minutes waiting. And they say don't swallow, so you end up with a mouth full of saliva (and the remains of the tablet) for the whole time. Not particularly pleasant.

 

3) It's way, way too 'sweet'. Artificial sweeteners should not be overpowering and obvious.  This is, and apparently made to satisfy folks who crave a strong fake-sugar-like taste. It's like artificial flavored and sweetened candy. Not good.

 

I was hoping for a small tablet that easily would fit under the tongue, with a nominal taste, delivering NMN. This isn't that.


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#41 able

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Posted 08 July 2018 - 08:31 PM

Got my 'New Sublingual' NMN tabs last week, and have taken some. I use it with other NAD+ boosters, in something like the original ABN formula , that is,  Niacin, Tryptophan, NR, Nicotinamide. I think it works, but really, I can't tell.

 

However, I have some concerns about their new formulation:

 

1) each tablet is approximately the size of a dime, and three times as thick. It weighs almost a gram. This shape and size is not easily kept under the tongue as they suggest to do. It's not comfortable. It would be better formed into a capsule shape that would fit under the tongue. And/or make the cap half size by simply cutting out half the non-NMN ingredients. Or cut the dose in half per tab.

 

2) It takes more than a while to dissolve. I've kept in there for up to 20 minutes waiting. And they say don't swallow, so you end up with a mouth full of saliva (and the remains of the tablet) for the whole time. Not particularly pleasant.

 

3) It's way, way too 'sweet'. Artificial sweeteners should not be overpowering and obvious.  This is, and apparently made to satisfy folks who crave a strong fake-sugar-like taste. It's like artificial flavored and sweetened candy. Not good.

 

I was hoping for a small tablet that easily would fit under the tongue, with a nominal taste, delivering NMN. This isn't that.

 

Interesting.  I wonder if we got the same product.  

 

The ones I got last week sound like the same size, but is 750 mg.  

 

It takes 4 minutes to dissolve if I didn't move them around.  I mostly though didn't have that much patience, and found myself chewing them a few times and then letting it dissolve.  I admire your patience !

 

I didn't find it sweet at all myself - actually like the little hint of lemon taste.  

 

I do still prefer the powder, but find it convenient to carry these with me during the day.


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#42 Phoebus

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Posted 12 July 2018 - 11:57 PM

will someone PLEEEEEAAASSEE make some pure NR powder so I can take it sublingual?

 

geeze 

 

these niagen caps are like 70% mag stearate I bet. I do take them SL but I can only imagine how much mg stearate is getting into my blood stream

 

anyone know which brand of NR has the least amount of filler? 

 

thanks 



#43 Phoebus

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Posted 13 July 2018 - 12:03 AM

 

 

I was hoping for a small tablet that easily would fit under the tongue, with a nominal taste, delivering NMN. This isn't that.

 

IF thats the case, then forget sublingual, get yourself the pure NMN powder, mix with DMSO, water, and hyaluronic acid. 

 

makes an incredible transdermal NMN serum 

 

I have done it and it works, unfortunately I prefer NR to NMN 


Edited by Phoebus, 13 July 2018 - 12:03 AM.


#44 able

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Posted 13 July 2018 - 12:10 AM

will someone PLEEEEEAAASSEE make some pure NR powder so I can take it sublingual?

 

geeze 

 

these niagen caps are like 70% mag stearate I bet. I do take them SL but I can only imagine how much mg stearate is getting into my blood stream

 

anyone know which brand of NR has the least amount of filler? 

 

thanks 

 

I hear ya. It seems a simple problem.  Just buy the brand that uses the smallest capsule, so has least filler.

 

Unfortunately, there is no such thing as Nicotinamide Riboside on the market.  They all us NR + C (chloride) to make it stable.

 

Revgenetics was selling a jar of pure NR powder that I used for 3-4 months.

 

The chloride in the Revgenetics product made it quite nasty.   Capsules with 75% filler actually taste better.

 

I don't think they use a lot of magnesium stearate, but all use different filler in different quantities. Which have you tried so far? 

 

I would recommend trying all of the brands and seeing which you personally find most palatable.

 



#45 able

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Posted 13 July 2018 - 12:14 AM

IF thats the case, then forget sublingual, get yourself the pure NMN powder, mix with DMSO, water, and hyaluronic acid. 

 

makes an incredible transdermal NMN serum 

 

I have done it and it works, unfortunately I prefer NR to NMN 

 

 

That sounds very interesting.  

 

I remember reading about your (or someones) dmso transdermal patch approach.  

 

How much can you dissolve into a patch?  

 

Any idea what % of the liquid/powder is absorbed and how much is lost?



#46 able

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Posted 13 July 2018 - 12:17 AM

IF thats the case, then forget sublingual, get yourself the pure NMN powder, mix with DMSO, water, and hyaluronic acid. 

 

makes an incredible transdermal NMN serum 

 

I have done it and it works, unfortunately I prefer NR to NMN 

 

 

If you use NR with a lot of fillers, do those get absorbed  along with the NR?  I would think it depends on what filler they use?



#47 Phoebus

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Posted 13 July 2018 - 12:18 AM

That sounds very interesting.  

 

I remember reading about your (or someones) dmso transdermal patch approach.  

 

How much can you dissolve into a patch?  

 

Any idea what % of the liquid/powder is absorbed and how much is lost?

 

Look at my thread "How to make an awesome transdermal NMN serum"



#48 able

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Posted 13 July 2018 - 12:30 AM

Look at my thread "How to make an awesome transdermal NMN serum"

 

Ah, found it. thanks


Edited by able, 13 July 2018 - 12:32 AM.


#49 Harkijn

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Posted 13 July 2018 - 06:17 AM

Got my 'New Sublingual' NMN tabs last week, and have taken some. I use it with other NAD+ boosters, in something like the original ABN formula , that is,  Niacin, Tryptophan, NR, Nicotinamide. I think it works, but really, I can't tell.

 

However, I have some concerns about their new formulation:

 

1) each tablet is approximately the size of a dime, and three times as thick. It weighs almost a gram. This shape and size is not easily kept under the tongue as they suggest to do. It's not comfortable. It would be better formed into a capsule shape that would fit under the tongue. And/or make the cap half size by simply cutting out half the non-NMN ingredients. Or cut the dose in half per tab.

 

2) It takes more than a while to dissolve. I've kept in there for up to 20 minutes waiting. And they say don't swallow, so you end up with a mouth full of saliva (and the remains of the tablet) for the whole time. Not particularly pleasant.

 

3) It's way, way too 'sweet'. Artificial sweeteners should not be overpowering and obvious.  This is, and apparently made to satisfy folks who crave a strong fake-sugar-like taste. It's like artificial flavored and sweetened candy. Not good.

 

I was hoping for a small tablet that easily would fit under the tongue, with a nominal taste, delivering NMN. This isn't that.

I am using this product now too. 125mg NMN and 6.5mg stevia. I agree that the size but also the stevia stimulate saliva too much.

 

My 'solution ' : With nail scissors I cut the tablet into three or four parts. I take one or two fragments at a time .It's easier to keep under the tongue this way and  perhaps more effective because there is only so much NMN the tissues can absorb at a given time. During the day I take the other fragments whenever I am sure I won't eat or drink anything during the coming hour.

 

BTW: while cutting up the tablets I happened to notice that the tablets partly turn into a very fine powder. This powder easily dissolves in aloe vera gel.  So far when applying this topically it seems to be absorbed by the skin.


Edited by Harkijn, 13 July 2018 - 06:17 AM.

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#50 Phoebus

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Posted 13 July 2018 - 12:54 PM

what I am wondering is if you could get the pure NMN powder and add something to it that increase penetration across the skin then use that as sublingual. 

 

in other words DIY your own sublingual method. 

 

You could use dmso but it tastes AWFUL, truly terrible. Not sure what other product you could use. Food grade Emu oil? 



#51 orion22

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Posted 13 July 2018 - 02:50 PM

true niagen brand safe to take sublingual?



#52 Phoebus

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Posted 13 July 2018 - 03:05 PM

true niagen brand safe to take sublingual?

 

 

sure if you want to absorb a bunch of mag stearate (realistically thats probably not going to hurt you but it will get in the way of absorbing NR)

 

but since there is no pure NR powder available...what can you do? 



#53 orion22

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Posted 13 July 2018 - 03:09 PM

sure if you want to absorb a bunch of mag stearate (realistically thats probably not going to hurt you but it will get in the way of absorbing NR)

 

but since there is no pure NR powder available...what can you do? 

so thats a yes ?

also the they only list cellulose as other ingredients



#54 able

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Posted 13 July 2018 - 03:52 PM

so thats a yes ?

also the they only list cellulose as other ingredients

 

Yes, you can.  But its not a pleasant experience. 

 

Tru Niagen is not Nicotinamide Riboside.  It is Nicotinamide Riboside Chloride.  

 

The Chloride makes it taste quite nasty.  

 

Adding Cellulose does dilute it, so Tru Niagen doesn't taste as "salty" as the pure powder Revgenetics used to sell, but cellulose doesn't absorb and just sits there in a soggy pile while you wait for the niagen to absorb.


Edited by able, 13 July 2018 - 04:42 PM.


#55 stefan_001

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Posted 13 July 2018 - 08:13 PM

sure if you want to absorb a bunch of mag stearate (realistically thats probably not going to hurt you but it will get in the way of absorbing NR)

 

but since there is no pure NR powder available...what can you do? 

 

TNMNK's filtering method to remove the filler may help.



#56 Phoebus

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Posted 13 July 2018 - 09:29 PM

TNMNK's filtering method to remove the filler may help.

 

 

??

 

whats this now? 



#57 Heisok

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Posted 14 July 2018 - 04:28 PM

Hi,

 

I started "sublingual" NMN yesterday. I took 3 doses of around 100 mgs between 2 pm and 8 pm. It did not hurt my sleep. My plan is to take smaller doses of 50 to 60 mgs spread out during the day for approximately 500 mgs total dose. My first dose will be around 5 minutes before my coffee in the morning.

 

I have read all the threads over time, but a lot of dosing information is buried in other threads.  Able and others, would you share how late you take your final dose whether sublingually or orally?



#58 able

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Posted 14 July 2018 - 04:47 PM

Hi,

 

I started "sublingual" NMN yesterday. I took 3 doses of around 100 mgs between 2 pm and 8 pm. It did not hurt my sleep. My plan is to take smaller doses of 50 to 60 mgs spread out during the day for approximately 500 mgs total dose. My first dose will be around 5 minutes before my coffee in the morning.

 

I have read all the threads over time, but a lot of dosing information is buried in other threads.  Able and others, would you share how late you take your final dose whether sublingually or orally?

 

 

I take it sublingual throughout the day and night.  

 

As we naturally have 2 peaks of NAD+  - one around noon and one at night (no idea what time?) , I think it's likely useful to keep NAD+ elevated during sleep if possible.  I take a scoop before bed, and most nights when I wake to visit the bathroom, take another.

 

I'm getting great results for strength, stamina, endurance, joint pain and less prostate issues.

 

I've never found NR or NMN to interfere with my sleep personally.  

 

I do find many smaller sublingual doses more effective for me, but I am taking a lot more than you.  Usually a  100-200 mg scoop, 10 or more times a day, for an average of 1,500 mg a day.

 

I have tried higher amounts.  At 3 grams a day or more, I actually feel a bit groggy, which is the opposite from the normal result I get. 


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#59 Qrazy

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Posted 14 July 2018 - 05:34 PM

I take it sublingual throughout the day and night.  

 

As we naturally have 2 peaks of NAD+  - one around noon and one at night (no idea what time?) , I think it's likely useful to keep NAD+ elevated during sleep if possible.  I take a scoop before bed, and most nights when I wake to visit the bathroom, take another.

 

I'm getting great results for strength, stamina, endurance, joint pain and less prostate issues.

 

I've never found NR or NMN to interfere with my sleep personally.  

 

I do find many smaller sublingual doses more effective for me, but I am taking a lot more than you.  Usually a  100-200 mg scoop, 10 or more times a day, for an average of 1,500 mg a day.

 

I have tried higher amounts.  At 3 grams a day or more, I actually feel a bit groggy, which is the opposite from the normal result I get. 

 

Able, how much $ does it cost at 1,500 mg a day?

 

Thanks.



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#60 able

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Posted 14 July 2018 - 06:10 PM

The powder is $60 for 12 grams.

 

If my math is correct, that last 8 days at 1.5 grams a day.

 

So about $7.50 a day.

 

Less than I spend at Peets, to feel 20 years younger  is worth it for me.

 

It is a hassle to carry the jar around and take a scoop every hour or so. Really want to try the transdermal patch.


Edited by able, 14 July 2018 - 06:13 PM.






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