180 replies to this topic

[niner]

Given that it seems that most now feel that large doses of resveratrol are not required and may be harmful, why the continued focus on increasing absorption?

From the reports I've seen, the buccal/alcohol method is a qualitatively different experience from ordinary oral dosing. (i.e. I'm just in it for the buzz...)

[maxwatt]

Given that it seems that most now feel that large doses of resveratrol are not required and may be harmful, why the continued focus on increasing absorption?

How high is up?

I think the consensus is that such large doses are over two grams per day, and most long-term users seem to have settled on 500 mg or so per day. Even then, lager two gram doses may be useful on initial use, an attack dose to obtain desirable effects before tapering to a lower dose. If one can get the effect of a 500 mg dose from 250 mg, I suppose that would be more economical. As niner pointed out, the buccal-alcohol method seems to be used for psychotropic effects, and perhaps for boosted testosterone during workouts. Neither of these has much hard science behind it, the evidence is anecdotal so far.

[John Barleycorn]

A shot of tequila is a slightly impractical delivery method. I find I can handle about 2 mL comfortably for sublingual/buccal absorption; any more and it starts to become a case of ballooning cheeks. So the choice of solvent would seem to be fairly crucial (provided of course that dissolved reseveratrol is deemed to be important, which may well not be the case). A bit of digging around suggests that polysorbates are a popular emulsifier in the food industry, and have in fact been used experimentally to increase the bioavailability of polyphenols. These come in different molecular weights, and the idea seems to be to match that weight with the target molecule. This would presumably be a bit more selective than using a general-purpose emulsifier like lecithin.

[maxwatt]

A shot of tequila is a slightly impractical delivery method. I find I can handle about 2 mL comfortably for sublingual/buccal absorption; any more and it starts to become a case of ballooning cheeks. So the choice of solvent would seem to be fairly crucial (provided of course that dissolved reseveratrol is deemed to be important, which may well not be the case). A bit of digging around suggests that polysorbates are a popular emulsifier in the food industry, and have in fact been used experimentally to increase the bioavailability of polyphenols. These come in different molecular weights, and the idea seems to be to match that weight with the target molecule. This would presumably be a bit more selective than using a general-purpose emulsifier like lecithin.

This thought is exactly what occurred to the people at Sirtris in 2006 or so, when they formulated resveratrol as SRT501. They used HPMC as an emulsifier or dispersant and a small amount of DOSS, an edible detergent, to keep it in suspension. One of their papers showed they had also explored using polysorbate-80 (aka Tween 80) for that purpose, and that the peak blood level obtained was even higher than with HPMC. Tween 80 tastes awful, so I do not think you will want to use it for buccal delivery. HPMC is a powder, and tasteless. It takes perhaps half an hour of stirring to get resveratrol into liquid suspension with it; some of us experimented with ultrasonic "sonication" to do this. I think I still have some HPMC around if anyone is interested in experimenting with it.

FWIW, the advertizer and sponsor in the banner at the top of this page carries a gel capsule with resveratrol formulated in Tween80, and it is in stock.

The Wikipedia entry on buccal delivery is suspect(1). I have no doubt that the ratio of blood serum resveratrol to dose taken is higher for buccal delivery, but only to a limit, an upper bound of a small dose, at most tens of milligrams. Most of what one puts in one's cheek or under one's tongue is swallowed, but is effectively dispersed so it will be more easily absorbed further on in the gut. Overall, higher blood levels can be obtained by swallowing than by buccal delivery, but not as quickly. Perhaps it is the speed of onset that accounts for the effect people are noting. Resveratrol does cross the blood-brain barrier, but nothing in the scientific literature notes a psychotropic effect. But then no one has been looking for it. According to the paper referenced by the Wiki article, 1 mg buccal resveratrol yielded a blood serum level of 37ng/ml. Hedgehog posted some results when he measured blood serum levels with oral ingestion, and Boocock's paper is available on the web; they measured levels up to four times higher, but only with resveratrol doses of 500 mg up to 2 grams. Buccal is much more efficient, but the levels are not quite as high, and the area under the curve is probably less.

Not wanting to imbibe in the morning, I experimented with using resveratrol at night, using melatonin later in the evening to counteract the wakefulness caused by resveratrol (it does reset one's circadian rhythm caused by resveratrol activating CLK genes.) I mixed it with some Jack Daniels, and sipped it, swooshing it in my cheeks, but did not attempt to retain it in my mouth. It's definitely a fun way to take resveratrol. But the sense of well-being I felt could as well been due to the alcohol or to a placebo effect.

Note on melatonin use: proper dose is a half gram or less. Either split a one mg tablet, or use the 300 mg tablets sold by LEF or Sundown sublingual tablets sold in many drugstores. Higher doses can lead to early waking after a few hours, and will leave one groggy the next day.

1) Niner pointed out that in the Pharmacology section of the Wikipedia article on Resveratrol, it says:

One way of administering resveratrol in humans appears to be buccal delivery, that is without swallowing, by direct absorption through the inside of the mouth. When one mg of resveratrol in 50 mL solution was retained in the mouth for one min before swallowing, 37 ng/ml of free resveratrol were measured in plasma two minutes later. This level of unchanged resveratrol in blood can only be achieved with 250 mg of resveratrol taken in a pill form.

12.5 mg of resveratrol will dissolve in 12 ounces of water (according to the solubility data in the Wikipedia article, and on Sigma-Aldrich's website). so one ounce of water should be adequate; it should be possible to obtain 1 mg of reseratrol in one ounce of water 30 ml., about a shot-glass full. This is practical with no dicey chemicals. I'm going into my kitchen to try to mix some up. I doubt it will dissolve quickly.

Edited by maxwatt, 04 March 2011 - 02:18 PM.

[JD.]

We are looking at Xylitol with possibly a little Stivia... as sweeteners.

Initial consideration was around 50mg-100mg a piece... I am not sure we can add more than this.
Time frame?... 2-3 months (The packaging appears to be the holdup on this...)

I am just not sure about the flavors... and of course, you heard it here first.

cheers!
A

Please make it grape!

It would be so appropriate

[Geoffrey]

Some time ago I accidentally bought the 500mg "time-release" (TR) tablets of 98% trans-resveratrol (sold by B******a). I thought I'd wasted my money because TR presumably provides a dose/time which the liver can dispose of too quickly to achieve useful blood concentrations. However, as far as I can tell, these tablets don't contain any fillers or other substance, and seem to be just very tightly packed/caked resveratrol (it's possible they have a caking agent, but this isn't indicated on the packaging). So I thought that they might work for buccal/sublingual delivery. As each tablet is scored, they can be easily split into two 250mg chunks, and each chunk placed either side under the tongue or between gum and cheek at the back. I find that under the tongue, the tablets take about 30 minutes to dissolve/disintegrate in the constant flow of saliva and friction from tongue movement. In the cheek, where there is less movement and saliva, they can stay easily for 2 hours or more. I prefer under the tongue, and because the pill dissolves relatively slowly, I don't get a mouthful of powder, or caked-up teeth and lips. Taking the tablet this way (rather than swallowing it whole), I can definitely feel the resveratrol in my system. It goes very quickly to my eyes, for starters (slight itchiness which I've noticed with high doses of standard micronized resv., like the beginning of allergy), and there is a slight irritation/burning sensation running down my throat. For several hours afterwards, I can feel a tension in my throat/sinus/nose area, and a certain zinginess bordering on irritation. I wouldn't call it an energy boost, rather a feeling of over-alertness with some tension/irritation. Hard to describe, but I don't get these feelings if I swallow the TR tablet whole.

Edited by Geoffrey, 07 March 2011 - 01:22 PM.

[niner]

Some time ago I accidentally bought the 500mg "time-release" (TR) tablets of 98% trans-resveratrol (sold by B******a). I thought I'd wasted my money because TR presumably provides a dose/time which the liver can dispose of too quickly to achieve useful blood concentrations. However, as far as I can tell, these tablets don't contain any fillers or other substance, and seem to be just very tightly packed/caked resveratrol (it's possible they have a caking agent, but this isn't indicated on the packaging). So I thought that they might work for buccal/sublingual delivery. As each tablet is scored, they can be easily split into two 250mg chunks, and each chunk placed either side under the tongue or between gum and cheek at the back. I find that under the tongue, the tablets take about 30 minutes to dissolve/disintegrate in the constant flow of saliva and friction from tongue movement. In the cheek, where there is less movement and saliva, they can stay easily for 2 hours or more. I prefer under the tongue, and because the pill dissolves relatively slowly, I don't get a mouthful of powder, or caked-up teeth and lips. Taking the tablet this way (rather than swallowing it whole), I can definitely feel the resveratrol in my system. It goes very quickly to my eyes, for starters (slight itchiness which I've noticed with high doses of standard micronized resv., like the beginning of allergy), and there is a slight irritation/burning sensation running down my throat. For several hours afterwards, I can feel a tension in my throat/sinus/nose area, and a certain zinginess bordering on irritation. I wouldn't call it an energy boost, rather a feeling of over-alertness with some tension/irritation. Hard to describe, but I don't get these feelings if I swallow the TR tablet whole.

This does sound like an allergic response, at least partly, but some of what you describe (the zingy part) sounds like something I might have felt a touch of the other day when I tried buccal resveratrol in tequila. I was almost going to post and say "nothing happened", but I'm not entirely sure it was nothing. I think I need to run another experiment. At this point, I can say that it didn't knock my socks off, but I'm not sure I gave it a proper test. I was in a pretty glum mood when I tried it, but that's largely cleared now, so maybe I'll try again tomorrow. BTW, if that Time-Release tablet is for real, then it almost surely contains something other than resveratrol. Considering the pharmacokinetics of resveratrol, that has to be in the running for the most useless formulation of the year.

[maxwatt]

...
BTW, if that Time-Release tablet is for real, then it almost surely contains something other than resveratrol. Considering the pharmacokinetics of resveratrol, that has to be in the running for the most useless formulation of the year.

Sublingual or time release tablets are often made by loosely compressing a mixture containg the substance and water soluble binder, such as cornstarch, and a enough moisture to make the mixture bind together. Was is sometimes used, to slow the release. I think I could make my own sublingual tabs with such a mix, and use a paper hole punch for the compression. But I've never seen a time-release resveratrol pill from B****a or anyone else. Maybe it didn't last long as a product?

A sublingual tablet containing one mg of resveratrol would have a tremendous profit margin.

[platypus]

Hasn't anyone measured concentrations in the blood after various delivery methods?

[maxwatt]

Hasn't anyone measured concentrations in the blood after various delivery methods?

See Boocock's paper referenced often in theis forum, hedgehog's measurements that he published here, and the paper referenced above from the wikipedia quote.

Edited by maxwatt, 10 March 2011 - 03:00 AM.

[John Barleycorn]

Resveratrol does cross the blood-brain barrier, but nothing in the scientific literature notes a psychotropic effect. But then no one has been looking for it.

A number of the currently trendy polyphenols like resveratrol, curcumin and quercetin impact BDNF and neurogenesis, a feature also shared by antidepressants. They have also been shown to reduce development of morphine tolerance, to guard against NMDA excitotoxicity, and to be analgesic (although admittedly it is unclear whether this is a central or peripheral effect). There is an emerging view that certain anti-inflammatories may be psychotropic. Speculating a bit here, the NMDA system has been shown to be fairly intimately involved with endocrine signalling, and that can be mood-altering.

For the sake of a reference, there's this:

1. Eur Neuropsychopharmacol. 2010 Jun;20(6):405-13. Epub 2010 Mar 30.Antidepressant-like effect of trans-resveratrol: Involvement of serotonin andnoradrenaline system.Xu Y, Wang Z, You W, Zhang X, Li S, Barish PA, Vernon MM, Du X, Li G, Pan J, OgleWO.J. Crayton Pruitt Family Department of Biomedical Engineering and Evelyn F. &William L. Mcknight Brain Institute, University of Florida, Gainesville, FL32611, USA.The antidepressant-like effect of trans-resveratrol, a phenolic compound present in polygonum cuspidatum, was evaluated through behavioral and neurochemicalmethods. trans-Resveratrol (20, 40 and 80 mg/kg, via gavage) significantlydecreased the immobility time in mouse models of despair tests, but did notinfluence locomotor activity. Two behavioral models and neurochemical assayssuggested that trans-resveratrol produced a significant increase in serotonin andnoradrenaline levels at 40 or 80 mg/kg in brain regions. In addition,trans-resveratrol dose dependently inhibited MAO-A activity. These findingsindicate that the antidepressant-like effect of trans-resveratrol might berelated to serotonergic and noradrenergic activation.PMID: 20353885 [PubMed - indexed for MEDLINE]

All of this suggests chronic administration may be psychotropic, but that doesn't necessarily account for the acute effects. It could potentially be an anti-inflammatory rather than an allergic thing, although it doesn't sound like it.

Edited by John Barleycorn, 10 March 2011 - 02:29 AM.

[longevitynow]

1/4th of a cap under my tongue and I felt different. 1 or more caps orally, never noticed anything. But I do a lot of things sublingually (dhea, melatonin, selegiline) and one question is, are you really absorbing more or is it just getting into your system quickly so you notice it.

[maxwatt]

1/4th of a cap under my tongue and I felt different. 1 or more caps orally, never noticed anything. But I do a lot of things sublingually (dhea, melatonin, selegiline) and one question is, are you really absorbing more or is it just getting into your system quickly so you notice it.

The amount absorbed sublingually or bucally in a minute (assuming there is some liquid to serve as a carrier, even water will work here) one achieves a high blood serum level. The actual amount absorbed this way is low, as the liver quickly removes it from circulation. It does pass the blood-brain barrier, and probably raises cAMP levels, which could possibly have a noticeable effect. Or it could be placebo. I've never noticed any such effect myself.

Edited by maxwatt, 08 April 2011 - 01:43 AM.

[Mr. Pink]

Has someone posted about this yet?

http://en.wikipedia....iki/Resveratrol

"The most efficient way of administering resveratrol in humans appears to be buccal delivery, that is without swallowing, by direct absorption through the inside of the mouth. When 1 mg of resveratrol in 50 mL solution was retained in the mouth for 1 min before swallowing, 37 ng/ml of free resveratrol were measured in plasma 2 minutes later. This level of unchanged resveratrol in blood can only be achieved with 250 mg of resveratrol taken in a pill form.[21]"

what do you guys make of the next couple sentenses that follow the above statement in the current incarnation of the wiki article:

"However, the effectiveness via buccal delivery is called into question because this represents only a transient advantage in blood levels. All resveratrol that enters the blood circulation will eventually be conjugated (attached) to detox molecules (glucuronate, sulfate) as it passes through the liver. Without liver metabolism, resveratrol has a relatively short half life (14 minutes) versus 9 hours when glucuronidated."

[Young Paul]

taking flavonoids may help: The present results show that resveratrol is glucuronated in the human liver. Glucuronidation may reduce the bioavailability of this compound however, flavonoids inhibit resveratrol glucuronidation and such an inhibition might improve the bioavailability of resveratrol.

and here's another interesting article

http://dmd.aspetjour...t/36/2/322.fullMy link

[maxwatt]

Has someone posted about this yet?

http://en.wikipedia....iki/Resveratrol

"The most efficient way of administering resveratrol in humans appears to be buccal delivery, that is without swallowing, by direct absorption through the inside of the mouth. When 1 mg of resveratrol in 50 mL solution was retained in the mouth for 1 min before swallowing, 37 ng/ml of free resveratrol were measured in plasma 2 minutes later. This level of unchanged resveratrol in blood can only be achieved with 250 mg of resveratrol taken in a pill form.[21]"

what do you guys make of the next couple sentenses that follow the above statement in the current incarnation of the wiki article:

"However, the effectiveness via buccal delivery is called into question because this represents only a transient advantage in blood levels. All resveratrol that enters the blood circulation will eventually be conjugated (attached) to detox molecules (glucuronate, sulfate) as it passes through the liver. Without liver metabolism, resveratrol has a relatively short half life (14 minutes) versus 9 hours when glucuronidated."

It is a complex issue. Buccal does achieve very high levels quickly but briefly. If some effects of resveratrol require high serum levels, higher than can be obtained by swallowing a pill, then is helpful. If the total area under the curve is important for other effects, then swallowing is the way to go. I've been hedging my bets, and doing both.

The glucoronidated form of resveratrol is also thought to be bioactive and responsible for some of its effects. Resveratrol is well absorbed in the intestines. I am concerned that some pill forms do not disperse, and much of the resveratrol may clump together in a bolus that passes unchanged through the digestive tract, without contacting the intestinal walls to be absorbed. This may be a baseless worry, but I've not seen it disproved. I know that Sinclair's human studies used a dispersant which avoids this possibility, and the rodents received it mixed in chow, which also spreads it around.

[Mr. Pink]

Has someone posted about this yet?

http://en.wikipedia....iki/Resveratrol

"The most efficient way of administering resveratrol in humans appears to be buccal delivery, that is without swallowing, by direct absorption through the inside of the mouth. When 1 mg of resveratrol in 50 mL solution was retained in the mouth for 1 min before swallowing, 37 ng/ml of free resveratrol were measured in plasma 2 minutes later. This level of unchanged resveratrol in blood can only be achieved with 250 mg of resveratrol taken in a pill form.[21]"

what do you guys make of the next couple sentenses that follow the above statement in the current incarnation of the wiki article:

"However, the effectiveness via buccal delivery is called into question because this represents only a transient advantage in blood levels. All resveratrol that enters the blood circulation will eventually be conjugated (attached) to detox molecules (glucuronate, sulfate) as it passes through the liver. Without liver metabolism, resveratrol has a relatively short half life (14 minutes) versus 9 hours when glucuronidated."

It is a complex issue. Buccal does achieve very high levels quickly but briefly. If some effects of resveratrol require high serum levels, higher than can be obtained by swallowing a pill, then is helpful. If the total area under the curve is important for other effects, then swallowing is the way to go. I've been hedging my bets, and doing both.

The glucoronidated form of resveratrol is also thought to be bioactive and responsible for some of its effects. Resveratrol is well absorbed in the intestines. I am concerned that some pill forms do not disperse, and much of the resveratrol may clump together in a bolus that passes unchanged through the digestive tract, without contacting the intestinal walls to be absorbed. This may be a baseless worry, but I've not seen it disproved. I know that Sinclair's human studies used a dispersant which avoids this possibility, and the rodents received it mixed in chow, which also spreads it around.

can you elaborate on how you do both. do you do buccal absorption and then swallow it? do you buccal one day and swallow the next day? Also, does sublingual work as well as in the cheek?

[maxwatt]

...

can you elaborate on how you do both. do you do buccal absorption and then swallow it? do you buccal one day and swallow the next day? Also, does sublingual work as well as in the cheek?

I put about 350 mg on a spoon, and place the contents under my tongue, or in my cheek. If my mouth is dry, I sip a little water and swish it around, otherwise I let my saliva do the job. I hold it in my mouth for about a minute. The liquid in one's mouth will be saturated in that the max4imal amount of resveratrol that can dissolve in aqueous solution will do so, and be aborbed by the oral mucosa, both buccal and sublingual. One can repeat sipping thus maintaining a relatively high blood serum level until the resveratrol has disappeared. Most of it will have been swallowed, but one will have had a high blood level for several minutes. Most though will have been swallowed, and enter the bloodstream in about half an hour, leading to a second peak in serum level, one lasting longer, if not so high.

Perhaps a slowly dissolving lozenge, held in the mouth, would deliver a prolonged high blood level. It's worth experimenting with,

FWIW, I am alternating resveratrol with luteolin as self-experimentation.

[Cephalon]

Has anyone tried to make the bubble gum yet?
http://www.ehow.com/...bubble-gum.html

[longevitynow]

...

can you elaborate on how you do both. do you do buccal absorption and then swallow it? do you buccal one day and swallow the next day? Also, does sublingual work as well as in the cheek?

I put about 350 mg on a spoon, and place the contents under my tongue, or in my cheek. If my mouth is dry, I sip a little water and swish it around, otherwise I let my saliva do the job. I hold it in my mouth for about a minute. The liquid in one's mouth will be saturated in that the max4imal amount of resveratrol that can dissolve in aqueous solution will do so, and be aborbed by the oral mucosa, both buccal and sublingual. One can repeat sipping thus maintaining a relatively high blood serum level until the resveratrol has disappeared. Most of it will have been swallowed, but one will have had a high blood level for several minutes. Most though will have been swallowed, and enter the bloodstream in about half an hour, leading to a second peak in serum level, one lasting longer, if not so high.

Perhaps a slowly dissolving lozenge, held in the mouth, would deliver a prolonged high blood level. It's worth experimenting with,

FWIW, I am alternating resveratrol with luteolin as self-experimentation.

Most sublinguals don't absorb that well sublingually, I'd guess 25% absorption at best. Then you swallow the rest, say 75%, but that absorption may be very mediocre also (probably depends a lot on the substance, as well as GI contents). But I will agree that with a sublingual you will have a substantial amount of both oral and GI absorption.

[maxwatt]

...

can you elaborate on how you do both. do you do buccal absorption and then swallow it? do you buccal one day and swallow the next day? Also, does sublingual work as well as in the cheek?

I put about 350 mg on a spoon, and place the contents under my tongue, or in my cheek. If my mouth is dry, I sip a little water and swish it around, otherwise I let my saliva do the job. I hold it in my mouth for about a minute. The liquid in one's mouth will be saturated in that the max4imal amount of resveratrol that can dissolve in aqueous solution will do so, and be aborbed by the oral mucosa, both buccal and sublingual. One can repeat sipping thus maintaining a relatively high blood serum level until the resveratrol has disappeared. Most of it will have been swallowed, but one will have had a high blood level for several minutes. Most though will have been swallowed, and enter the bloodstream in about half an hour, leading to a second peak in serum level, one lasting longer, if not so high.

Perhaps a slowly dissolving lozenge, held in the mouth, would deliver a prolonged high blood level. It's worth experimenting with,

FWIW, I am alternating resveratrol with luteolin as self-experimentation.

Most sublinguals don't absorb that well sublingually, I'd guess 25% absorption at best. Then you swallow the rest, say 75%, but that absorption may be very mediocre also (probably depends a lot on the substance, as well as GI contents). But I will agree that with a sublingual you will have a substantial amount of both oral and GI absorption.

Look at the reference a couple of pages earlier in this thread: they dissolved 1 mg of resveratrol in 50 cc of water, and subjects held it in their mouths for one minute. Subjects blood levels were then as high or higher than the peak you can get by oral administration of a quarter of a gram of resveratrol.

So you are swallowing more than 75%, but it doesn't matter. You get a peak from what bucal absorption does occur, and a secondary peak about half an hour later from what is swallowed. And if one retains some under the tongue for five to ten minutes, I believe the initial peak will remain high, as blood levels should be continuously replenished - though I have no test data for this, it's a reasonable assumption.

I'd like to see some kind of sublingual dissolving lozenge or tablet. Cephalon's chewing gum (two posts ago) might be a good idea too.

Edited by maxwatt, 11 June 2011 - 01:50 PM.

[unglued]

Without browsing the entire resveratrol forum, I'm curious, has anyone tried dissolving it in wine?

I've been doing this every night for a year or so, in addition to a pill in the morning. As the earlier replies mention, wine doesn't have enough alcohol to dissolve much resveratrol. What I do is to spoon around 250mg into a bottle partially filled with vodka, more than will dissolve even in the vodka, keep it wrapped in aluminum foil to protect it from light, and every night I shake it up pour a couple of ml into the wine. I happen to prefer white wine, taste-wise. It also makes it easy to see that a little more of the suspended resveratrol dissolves in the extra volume alcohol, but not much; it makes the wine a bit cloudy. Of course, the vodka is also completely saturated with as much resveratrol as it can hold in solution. There's usually some powder left at the bottom of the wine glass when it's empty, so I fill it with water and drink that, and then sometimes repeat, so essentially all of it gets into me.

I may not be getting as much resveratrol into the wine as I get from the pill, but I figure I'm getting a couple of mg, a lot more than those snobby French red wine drinkers. That's assuming of course that it's really resveratrol alone responsible for the French paradox, and not the other wine skin components I'm missing out on as a white wine drinker.

[Geoffrey]

Sublingual or time release tablets are often made by loosely compressing a mixture containg the substance and water soluble binder, such as cornstarch, and a enough moisture to make the mixture bind together. Was is sometimes used, to slow the release. I think I could make my own sublingual tabs with such a mix, and use a paper hole punch for the compression. But I've never seen a time-release resveratrol pill from B****a or anyone else. Maybe it didn't last long as a product?
A sublingual tablet containing one mg of resveratrol would have a tremendous profit margin.

You didn’t look very hard! The product is called Transmax Time Release, and it's very much available and advertised on the front page of the B******a website. I'm sure it does have a binder, because I sometimes chew these tablets up, and you can feel something a bit chewy in them. So you’re probably right that it’s cornstarch being used to hold the resveratrol together.

I'd like to see some kind of sublingual dissolving lozenge or tablet. Cephalon's chewing gum (two posts ago) might be a good idea too.

As I said, it’s not formulated as sublingual, but I use it as such. Because it’s a compact tablet, it dissolves slowly, and can be split in two along the score to put on both sides of the tongue. Takes about 30mins to dissolve completely, and no mess of powder floating around your mouth. However, I don’t really like the hassle of taking resveratrol this way. I prefer a powdered form which I mix into yoghurt and have first thing in the morning when I wake up. I can’t help feeling that our guts are far more efficient absorption engines than our mouths!

Edited by Geoffrey, 17 September 2011 - 07:53 AM.

[Anthony_Loera]

Sorry but any resveratrol that is 'Time released' is a farce in my book, because of a humans metabolism.

In my book you need a high amount of res in plasma, and 'time released' product will not achieve this to the degree that a fast release product would do (micronized or not).


A

[Cephalon]

Resveratrol does cross the blood-brain barrier, but nothing in the scientific literature notes a psychotropic effect. But then no one has been looking for it.

A number of the currently trendy polyphenols like resveratrol, curcumin and quercetin impact BDNF and neurogenesis, a feature also shared by antidepressants. They have also been shown to reduce development of morphine tolerance, to guard against NMDA excitotoxicity, and to be analgesic (although admittedly it is unclear whether this is a central or peripheral effect). There is an emerging view that certain anti-inflammatories may be psychotropic. Speculating a bit here, the NMDA system has been shown to be fairly intimately involved with endocrine signalling, and that can be mood-altering.

For the sake of a reference, there's this:

1. Eur Neuropsychopharmacol. 2010 Jun;20(6):405-13. Epub 2010 Mar 30.Antidepressant-like effect of trans-resveratrol: Involvement of serotonin andnoradrenaline system.Xu Y, Wang Z, You W, Zhang X, Li S, Barish PA, Vernon MM, Du X, Li G, Pan J, OgleWO.J. Crayton Pruitt Family Department of Biomedical Engineering and Evelyn F. &William L. Mcknight Brain Institute, University of Florida, Gainesville, FL32611, USA.The antidepressant-like effect of trans-resveratrol, a phenolic compound present in polygonum cuspidatum, was evaluated through behavioral and neurochemicalmethods. trans-Resveratrol (20, 40 and 80 mg/kg, via gavage) significantlydecreased the immobility time in mouse models of despair tests, but did notinfluence locomotor activity. Two behavioral models and neurochemical assayssuggested that trans-resveratrol produced a significant increase in serotonin andnoradrenaline levels at 40 or 80 mg/kg in brain regions. In addition,trans-resveratrol dose dependently inhibited MAO-A activity. These findingsindicate that the antidepressant-like effect of trans-resveratrol might berelated to serotonergic and noradrenergic activation.PMID: 20353885 [PubMed - indexed for MEDLINE]

All of this suggests chronic administration may be psychotropic, but that doesn't necessarily account for the acute effects. It could potentially be an anti-inflammatory rather than an allergic thing, although it doesn't sound like it.

Hi John,

Thank you for sharing!

Do you also have references for the morphine tolerance counteracting properties of resveratrol?

[Young Paul]

thanks for posting Cephalon, I dont think the bubble gum will be as good as vodka, because without a carrier how will the res be absorbed buccaly? The swallowing of the res will give a slow absorption and thus not very high blood peak levels. I've tried mixing with wine and Baileys but vodka or rum seems the best for the speedy buzz, and amazing concentration for a few hours. Mixing with water doesn't do anything for me. I've never tried micronized with vodka, that seems an excellent method, have to order some now.

[O.N.]

So what is the result fo everything we know about resveratrol know? hold it in the mouth or just swallow the capsules?

[bixbyte]

 

 

Cool, ¹⁴C dosing of humans.......


I wonder how a 250mg or 500mg buccal dose would look instead of just 25mgs......

 

A.M., wife and I,I mix 3,000 mg of 99% RES and ultrasonicate with filtered H2O and HPMC make 2 X 3 oz liquid per doses. Supplementing with this dose for years.I leave the mixture in my mouth for a couple minutes before swallowing.Would be nice if I could see my RES blood plasma levels.

[Psychonaut]

Curious on peoples thoughts of using a suppository or injectable for resveratrol absorption? I noticed on another forum people were using resveratrol and curcumin as injectable's or taking the res/curc lipo/water solution, putting it into a capsule and taking it as a suppository.

Edited by Psychonaut, 27 August 2012 - 03:25 AM.

[Hebbeh]

Curious on peoples thoughts of using a suppository or injectable for resveratrol absorption? I noticed on another forum people were using resveratrol and curcumin as injectable's or taking the res/curc lipo/water solution, putting it into a capsule and taking it as a suppository.

How did they prepare the injectable and assure sterility? Daily injections? Intriguing idea...but a lot of sticking...and eventual scar tissue buildup.