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Buccal delivery superior?


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#61 maxwatt

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Posted 27 March 2009 - 10:32 AM

So what about opening resv caps and sticking the stuff on your gums? Better or worse than just taking the caps orally?

More expensive in the long run.

You may not get pure resveratro. Capsules tend to contain flow-agents and excipients and such, to aid in packing. Things like silicon dioxide (sand) and magnesium stearate. Perfectly harmless take orally. they help prevent static electricity from interfering with encapsulation process, filling the capsule while keeping the amount of ingredient constant.

#62 2tender

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Posted 28 March 2009 - 10:49 PM

Its all about conveniance of dosing, for me I suppose if I were going to use it Buccal or sublingual I would just get the straight powder at 99% micronized, others have devised formulas for this. I would rather just use the tween80 and probably get the same or approximate absorbtion. Without individual scientific testing we can only go by the data that is presented to us and our own subjective experiences, albeit, some of those may be placebo.

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#63 Adistar

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Posted 30 March 2009 - 05:35 AM

Its all about conveniance of dosing, for me I suppose if I were going to use it Buccal or sublingual I would just get the straight powder at 99% micronized, others have devised formulas for this. I would rather just use the tween80 and probably get the same or approximate absorbtion. Without individual scientific testing we can only go by the data that is presented to us and our own subjective experiences, albeit, some of those may be placebo.



So, would it be even better to apply buccal delivery with Tween80?

#64 2tender

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Posted 30 March 2009 - 11:25 AM

No, I think that the same or approximate absorbtion can be acheived by simply swallowing the Resveratrol capsule that is already combined with the Tween 80, its a product called "Nitro 250" you can read about it by clicking the Revgenetics ad at the top of this page, click products, then click on micronized Resveratrol Nitro 250. I hope that helps you.

#65 JD Kalloco

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Posted 08 April 2009 - 07:31 PM

Erythritol doesn't have the extensive studies done on oral health as xylitol has. It's less sweet, so you need more. It's more expensive compared to xylitol. Most people do not react to the relative small amount of xylitol in a gum.


Xylitol alert! (below)*

I've been enjoying Xylitol since 1980 ... although today's product is sourced primarily from corn. Is anyone familiar with birch sourced xylitol?

Xylitol comes in handy ... the Kimberly Clark patent for bacterial vaginitis comes to mind. Shared the patent information with a client ... she reports success.

As for stevia ... I prefer a mixture of xylitol and stevia for optimal sweetening. The cool fruity flavor of xylitol masks the stevia after-taste. Fortunately today, we are blessed with highly improved stevia ... either the 99% "Reb-A" stevia, or enzyme treated stevia which can taste even better.

If resveratrol tastes anything like 95% OPC grapeseed extract, I'd imagine that anything over 25mg would be problematic for a x-buccal lozenge. Ever try 500mg of grape seed extract in capsule format? I'd liken it to drinking a concentrated green tea extract with no sweeteners or flavoring, on an empty stomach. The astringent action is likely to trigger a regurg' action.

As for the x-resveratrol lozenge ... stevia, xylitol, along with methylsulphonylmethane (MSM ... DMSO2) might prove to boost efficacy. I would also include additional micronutrient(s) along with another botanical extract.

* Xylitol alert! Apparently Xylitol is toxic to dogs ... deadly toxic! http://www.aspca.org...ople-foods.html

Best regards,

JD Kalloco

#66 maxwatt

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Posted 08 April 2009 - 07:34 PM

Erythritol doesn't have the extensive studies done on oral health as xylitol has. It's less sweet, so you need more. It's more expensive compared to xylitol. Most people do not react to the relative small amount of xylitol in a gum.


Xylitol alert! (below)*

I've been enjoying Xylitol since 1980 ... although today's product is sourced primarily from corn. Is anyone familiar with birch sourced xylitol?

Xylitol comes in handy ... the Kimberly Clark patent for bacterial vaginitis comes to mind. Shared the patent information with a client ... she reports success.

As for stevia ... I prefer a mixture of xylitol and stevia for optimal sweetening. The cool fruity flavor of xylitol masks the stevia after-taste. Fortunately today, we are blessed with highly improved stevia ... either the 99% "Reb-A" stevia, or enzyme treated stevia which can taste even better.

If resveratrol tastes anything like 95% OPC grapeseed extract, I'd imagine that anything over 25mg would be problematic for a x-buccal lozenge. Ever try 500mg of grape seed extract in capsule format? I'd liken it to drinking a concentrated green tea extract with no sweeteners or flavoring, on an empty stomach. The astringent action is likely to trigger a regurg' action.

As for the x-resveratrol lozenge ... stevia, xylitol, along with methylsulphonylmethane (MSM ... DMSO2) might prove to boost efficacy. I would also include additional micronutrient(s) along with another botanical extract.

* Xylitol alert! Apparently Xylitol is toxic to dogs ... deadly toxic! http://www.aspca.org...ople-foods.html

Best regards,

JD Kalloco


That might be a solvent residue you are tasting. 98% resveratrol should be tasteless.

#67 thoughtworm

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Posted 14 July 2009 - 11:48 PM

"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]"


So what if I open one of my 100 mg. resveratrol capsules and empty the powder into a big bottle of listerine? That would result in >1mg per 50 mg of listerine. I would then just use the listerine as intended, swishing it in my mouth for 1 minute and spitting it out.

Why wouldn't this work to effect the buccal delivery seen in the study, and all at negligible cost?

#68 niner

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Posted 15 July 2009 - 12:32 AM

"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]"


So what if I open one of my 100 mg. resveratrol capsules and empty the powder into a big bottle of listerine? That would result in >1mg per 50 mg of listerine. I would then just use the listerine as intended, swishing it in my mouth for 1 minute and spitting it out.

Why wouldn't this work to effect the buccal delivery seen in the study, and all at negligible cost?

Would you happen to have the bibliographic data for reference [21] above? Some of us would be interested in checking it out. Considering that they only used 1mg total resveratrol, getting 37ng/ml = 0.16 microM is pretty good. You could try the listerine trick. I think it would be hard to get much resveratrol to dissolve, but if you're only shooting for 1mg/50ml, it ought to be feasible. You really only need to get 20mg to go into a liter in order to hit this concentration. Of course, the solubility of resveratrol in water is only about 30mg/liter, and that would probably require warming. Does listerine have alcohol in it? That would help a little. Finally, if you get the solution at a high enough concentration, and hold it in your mouth for one minute, it sounds like you will get a small bolus of free resveratrol. It won't last long though. It's a little bit like taking a hit off a cigarette; the nicotine doesn't stick around for long. Likewise, the resveratrol will be quickly metabolized. You might have better luck if you could prepare some sort of resveratrol lozenge that you could suck on for a long time. BTW, it occurs to me that 50ml is a pretty big mouthful.

#69 immortali457

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Posted 15 July 2009 - 02:03 AM

http://www.myresvera...a-delivery.html

#70 Anthony_Loera

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Posted 15 July 2009 - 02:24 AM

Listerine?

Please.. give me pure ethanol instead!! Anything but listerine for a full minute...

#71 maxwatt

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Posted 15 July 2009 - 03:04 AM

I used Listerine with a 50% resveratrol extrct to spray in my garden. It killed aphids and eliminated the fungus on my plants.

Bucal deliver results in a higher percentage of free resveratrol being delivered into the blood, bypassing 1st pass liver metabolism, but there is an upper limit on how much you can absorb that way. So it's more efficient up to a point, beyond which swallwing it is necessary to absorb more.

#72 2tender

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Posted 15 July 2009 - 03:30 AM

In my opinion, based on the conclusions of previous reads and experiences, adequate, comparable absorbtion can be acheived through regular oral dosing of the existing pre-emulsified product mentioned elsewhere here. To get the exact effect obtained in the buccal study you would have to follow their protocol of preparation and administration, even if a person were ill it would be much less work to just swallow a capsule daily and eventually get the same results. I think that if a buccal product were viable it would have been produced by now. Listerine and some left over Resveratrol powder? Probably wouldnt hurt to try that, but I wouldnt go out of my way to do so.

#73 bluemoon

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Posted 15 July 2009 - 08:13 AM

the Tween 80, its a product called "Nitro 250" you can read about it by clicking the Revgenetics ad at the top of this page, click products, then click on micronized Resveratrol Nitro 250. I hope that helps you.


Gee, no bias here. where is maxwatt or niner pouncing on 2tender for pointing to an add at the top of the page for the 100th time , or why dont they rewrite it as something like revgeriatrics?

I think it is perfectly fine for 2pretneder to constantly promote a brand run by a dude
who hasnt learn how to spell "a lot" and twist people's words into a pretzel here, since I think it is likely a quality brand.

But for the love of God, give us thinking humans a break.

#74 2tender

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Posted 15 July 2009 - 12:01 PM

It seems my posts regarding this helpful information have been misconstrued as covert advertising. Holmes, I want you to know that I will refrain from posting this elsewhere, it seems to have ruffled your feathers. I did receive a pm advising me that mentioning specific products was a no-no, fear not, dear thinker here is your "break".

#75 maxwatt

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Posted 15 July 2009 - 12:01 PM

Gee, no bias here. where is maxwatt or niner pouncing on 2tender for pointing to an add at the top of the page for the 100th time , or why dont they rewrite it as something like revgeriatrics?

I think it is perfectly fine for 2pretneder to constantly promote a brand run by a dude
who hasnt learn how to spell "a lot" and twist people's words into a pretzel here, since I think it is likely a quality brand.

But for the love of God, give us thinking humans a break.


It is acceptable to occasionally mention a product name for the sake of clarity, but you are abusing that.

It's erotic to use a feather. It is kinky when you use the whole chicken.

There are two reasons we do not want you spelling out L___________X: one, the owner googles the net looking for his product's name, and threatens to sue when he doesn't like what he sees. We have little control over what people post, really. It is a pain to deal with, so we'd rather avoid it.

The second point is google add words. It has been proposed that you are an intentional troll working for that company, attempting to influence google addwords to display L_______x ads here when people look for resveratrol. Indeed, I can find no other rational explanation for your behavior other than puerility.

It is a pain to edit out the product name every time you post, so be warned: I will make any further posts of Holmes or anyone else spelling out the name L____x invisible. Only because it is easier for me.

#76 faustus

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Posted 17 July 2009 - 06:21 AM

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

Anthony,
I would be very interested in buying a gum product. Get one out the door and the money is on the way.

PS, not a big mint fan, but any flavors are ok.

#77 immortali457

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Posted 26 July 2009 - 09:31 PM

So anymore thoughts at the moment on taking such a small amount ot trans-resveratrol via Buccal delivery?
Man that would be like an unbelievable savings of money compared to 250-500 mg orally.

#78 kilgoretrout

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Posted 12 August 2009 - 03:58 PM

RE: Increasing buccal absorption...

I recall reading somewhere that "Listerine" style mouthwashes just prior to buccal delivery of stuff works really well to boost uptake.

It said that all 3 primary elements: the alcohol, the menthol, and the eucalyptol ALL increase the permeability and rate of absorption of mouth tissues by a large degree.

(Plus I would think in addition to this, it would also help in a simple mechanical fashion via removal of food residue, saliva, mucus film, etc)

Oh, to the non-mint fan above... actually I would be willing to bet that a strong amount of mint oil/flavor would additionally boost the permeability of mouth tissues in similar fashion to menthol/eucalyptol. I think it shares a class of aromatic compounds called, if I am not mistaken. "phenols"?, that is mainly responsible for this effect? So a good stiff mint flavor would probably be a good one to make the gum more effective. And your girl/boy friend will probably appreciate it, too!

Edited by kilgoretrout, 12 August 2009 - 04:03 PM.


#79 stephen_b

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Posted 14 August 2009 - 04:35 PM

Critical evaluation of permeation enhancers for oral mucosal drug delivery (PMID 19663558):

Background: Drug delivery via oral mucosa is an alternative method of systemic administration for various classes of therapeutic agents. Among the oral mucosae, buccal and sublingual mucosae are the primary focus for drug delivery. Buccal delivery offers a clear advantage over the peroral route by avoidance of intestinal and hepatic first-pass metabolism. However, despite offering the possibility of improved systemic drug delivery, buccal administration has been utilized for relatively few pharmaceutical products so far. One of the major limitations associated with buccal delivery is low permeation of therapeutic agents across the mucosa. Various substances have been explored as permeation enhancers to increase the flux/absorption of drugs through the mucosa, but irritation, membrane damage, and toxicity are always associated with them and limit their use. ...


This might be an interesting paper, dated this month.

StephenB

#80 niner

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Posted 15 August 2009 - 04:43 AM

This is an impressive therapeutic agent used exclusively via the buccal route:

Attached File  skoal_long_cut_straight_smokeless_tobacco.jpg   35.11KB   41 downloads

#81 kilgoretrout

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Posted 17 August 2009 - 08:50 PM

This is an impressive therapeutic agent used exclusively via the buccal route:


Even better is "Snus", which does not undergo the same heating processes that produce the carcinogenic nitrosamines in tobacco, including the above, yet still delivers the fix of nic.

Apparently there is published medical research showing lack of cancer in users compared to significant mouth & throat cancer in users of traditional "chewing" tobacco.

#82 2tender

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Posted 18 August 2009 - 01:49 AM

Please post on topic, a little levity is okay but pertinent Resveratrol information is what this forum is all about. Im not convinced that buccal is anymore advantageous than combining the current state-of-the-art product(s) ie TD, pre-emulsified, and micronized powder. JMO

#83 immortali457

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Posted 20 September 2009 - 02:56 PM

Bump.......so is Buccal delivery not something most here believe in?

#84 maxwatt

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Posted 20 September 2009 - 03:01 PM

Bump.......so is Buccal delivery not something most here believe in?

It exists, and is more efficient in that a higher amount gets into the blood and avoids first pass liver metabolism so the levels are higher for longer, but only up to a point. Only a ceretain amount can be absorbed this way, as the mucosal surface area is limited. If oe wants to take amounts greatere than perhaps 50 mg, one would still hve to swallow, and simply taking higher doses obviates the effect of buccal delivery.

#85 immortali457

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Posted 20 September 2009 - 03:49 PM

I guess what I'm getting at is the tittle of this thread. If true...why not just take a few miligrams via buccal delivery and be done with it. Of course this thought, if true, would dig deep into the pockets of manufacturers.

Edited by immortali457, 20 September 2009 - 03:50 PM.


#86 2tender

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Posted 20 September 2009 - 05:03 PM

It is rumoured that someone is coming out with a liquid product containing 100mgs Resveratrol per dose that can theoretically be used for buccal admin, but it is not straight Res. its compounded with other things.

#87 niner

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Posted 21 September 2009 - 03:22 AM

It is rumoured that someone is coming out with a liquid product containing 100mgs Resveratrol per dose that can theoretically be used for buccal admin, but it is not straight Res. its compounded with other things.

I suspect that they will not demonstrate that it works, for example by performing a series of blood draws on humans using the formulation, then analyzing them for resveratrol level. They will likely cite the Wikipedia article that claims 1 mg resveratrol in solution in 50 ml water when held in the mouth resulted in 37ng/ml in blood 2 minutes later. They will extrapolate that their product will result in 3700 ng/ml = 16 uM, two minutes later... They will not say anything about what the level will be two minutes after that, or ten minutes after that, but it won't be 16 uM, that's for sure. The important number in my view is not the maximum plasma concentration, or Cmax, which is only reached for a brief time. I am more interested in the Area Under the concentration-time Curve, or AUC. I think the AUC is going to be higher with an oral dose of a good formulation rather than a buccal dose. The reason I prefer to consider the AUC is because tissue levels of the drug depend on both the concentration they are exposed to and the time they are exposed to it. If they could show that their method led to a higher AUC than an oral dose of a similarly priced formulation, then I would be truly impressed. They will not need to go to that trouble, however, as there will be plenty of customers who will buy it based on an extrapolation from the Wikipedia claim.

#88 2tender

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Posted 21 September 2009 - 10:32 PM

I doubt the R and D will be that extensive, The Resveratrol combo product has already been proven to their target marketing group in another form, so yes you're right they probably wont. Whether this formulation will be as popular as the other remains to be seen. I think most people will just swish it around for a few seconds then swallow. It will be interesting to say the least.

#89 health_nutty

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Posted 20 October 2009 - 05:19 AM

Quick update. At some point I was frustrated with the increasing amount of resveratrol that was seemingly needed to obtain "rat like" plasma levels. This was maybe a year ago. Then I recently read about the buccal method and I decided to give it a try again.

Method (one in the morning and once in the evening):
1) Prep with Listerine for 30sec. Spit out then...
2) 100-150mg scoop of 98% resvertrol under the tongue.
3) One cap of vodka (less than a tablespoon).
4) Swish in mouth for 10 minutes
5) Swallow.

There probably isn't nearly enough alcohol to fully dissolve the resveratrol, but i'm hoping it keeps the pores in my mouth open during the the swishing (keeping the mouthwash prep effective for longer).

Using this method I have experienced *significant* anti-inflammatory effects. Like maxwatt's toe, I have a indicator as well: my midback stiffness. The vertebre in my back are significantly more "free" 30 minutes after ingestion. The anti-inflammatory effect is stronger than 600mg of ibuprophen (advil). The anti-inflammatory is also much much greater than the even 800mg of resveratrol (1.6g of 50%) resveratrol I was taking in the past.

I'm a pretty active person (lift, run, play ultimate frisbee). I will keep you guys updated on any performance effects (I should at least get a nice placebo boost).

Edited by health_nutty, 20 October 2009 - 05:24 AM.


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#90 health_nutty

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Posted 20 October 2009 - 10:13 PM

Holy placebo effect Batman! I've been doing this method for 3 weeks. 2 weeks with 50% res and 1 week with 99%.

I had unbelievable stamina during my Ultimate game. Simply the best I've ever had hands down. In case you don't know in Ultimate frisbee you basically do repeated all out sprints with some jogging/walking in between.

My weight lifting does not seem to have benefited.

Edited by health_nutty, 20 October 2009 - 10:16 PM.





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