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Resveratrol lozenge formulation shows promise

resveratrol ribose lozenge bioavailability

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#1 blood

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Posted 08 March 2014 - 04:20 AM


Summary of the research from nutra-ingredients:

Link: http://www.nutraingr...ry-system-Study

In order to test the potential of delivering trans-resveratrol via a lozenge, the researchers tested the solubility of the ingredient in the presence of dextrose, fructose, ribose, sucrose, and xylitol. Results showed that the resveratrol was,“significantly more soluble in the ribose solution than in the other four solutions”, they said, and ribose was subsequently used for the proof of concept test with two healthy human participants.

The volunteers consumed one lozenge containing 146 mg of trans-resveratrol (purchased from Biotivia Longevity Pharmaceuticals) per 2000 mg of lozenge mass.

Data showed that the peak plasma concentrations (Cmax) for resveratrol alone (and not its metabolites) were achieved after only 15 minutes, which is“considerably quicker than the 60–120 minutes reported using traditional free resveratrol tablets,” they said...

“Future research must be conducted to determine if the high plasma levels attained from the optimized resveratrol lozenge hold true across multiple individuals and whether the metabolite profile differs considerably from that obtained from an oral supplement,” they concluded.



Likelihood of seeing a resveratrol lozenge product on the market, soon:

Link: http://www.nutraingr...ry-system-Study

The study was funded by Wilmore Labs, LLC from San Antonio, TX, a start-up company which aims to develop novel formulations for nutraceutical delivery, and the company’s president and CTO, Otis Blanchard, is first author of the paper. The study was performed in collaboration with researchers from the University of Texas Health Science Center at San Antonio, High Point University in North Carolina.

The resveratrol-ribose lozenge is the subject of a pending patent application (2011/0130,469) by Blanchard, who told NutraIngredients-USA that he has been working on the resveratrol lozenge for four years, and the company is actively engaged in pursing commercialization of the product. The bottleneck for further development is investment, he said, and the company is exploring various options to move forward, including crowd-funding.



Full text:

Link: http://www.plosone.o...al.pone.0090131

Development of a Lozenge for Oral Transmucosal Delivery of Trans-Resveratrol in Humans: Proof of Concept

Resveratrol provides multiple physiologic benefits which promote healthspan in various model species and clinical trials support continued exploration of resveratrol treatment in humans. However, there remains concern regarding low bioavailability and wide inter-individual differences in absorption and metabolism in humans, which suggests a great need to develop novel methods for resveratrol delivery. We hypothesized that oral transmucosal delivery, using a lozenge composed of a resveratrol-excipient matrix, would allow resveratrol to be absorbed rapidly into the bloodstream. We pursued proof of concept through two experiments. In the first experiment, the solubility of trans-resveratrol (tRES) in water and 2.0 M solutions of dextrose, fructose, ribose, sucrose, and xylitol was determined using HPLC. Independent t-tests with a Bonferroni correction were used to compare the solubility of tRES in each of the solutions to that in water.tRES was significantly more soluble in the ribose solution (p = 0.0013) than in the other four solutions. Given the enhanced solubility of tRES in a ribose solution, a resveratrol-ribose matrix was developed into a lozenge suitable for human consumption. Lozenges were prepared, each containing 146±5.5 mg tRES per 2000 mg of lozenge mass. Two healthy human participants consumed one of the prepared lozenges following an overnight fast. Venipuncture was performed immediately before and 15, 30, 45, and 60 minutes following lozenge administration. Maximal plasma concentrations (Cmax) for tRES alone (i.e., resveratrol metabolites not included) were 325 and 332 ng⋅mL−1 for the two participants at 15 minute post-administration for both individuals. These results suggest a resveratrol-ribose matrix lozenge can achieve greater Cmax and enter the bloodstream faster than previously reported dosage forms for gastrointestinal absorption. While this study is limited by small sample size and only one method of resveratrol delivery, it does provide proof of concept to support further exploration of novel delivery methods for resveratrol administration.


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#2 APBT

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Posted 09 March 2014 - 08:35 PM

Would mixing ~ 1.5 grams of d-ribose powder, with resveratrol powder and emptying under the tongue with a bit of water to dissolve over several minutes, (potentially) achieve the same result?
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#3 niner

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Posted 10 March 2014 - 12:56 AM

Would mixing ~ 1.5 grams of d-ribose powder, with resveratrol powder and emptying under the tongue with a bit of water to dissolve over several minutes, (potentially) achieve the same result?


My guess would be that it would not. In the lozenge, the resveratrol is (presumably) dissolved in the ribose matrix. When you mix the two powders, you have separate crystals that are very large, compared to molecular dimensions. I think it would act about the same as resveratrol alone; maybe a little better, but not a lot.

#4 Wilmore Labs

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Posted 16 April 2014 - 11:40 PM

Thanks for the support!


Edited by Wilmore Labs, 16 April 2014 - 11:45 PM.


#5 bixbyte

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Posted 09 May 2014 - 11:45 PM

Dissolve Resveratrol with Ribose to make a lozenge does the melting point of Ribose have any negative impacts on the molecular Trans-Res?

I was under a belief that at a certain temp Trans-Res goes Cis?

 



#6 Wilmore Labs

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Posted 10 May 2014 - 04:51 PM

It's not temperature, but UV light can change it to cis-resveratrol.  Just leaving it out in the dark in liquid it'll change back to trans, and their are other tricks and conditions for cis/trans.  It's just a molecule with a hinge. That's all cis/trans is. "Cis" is on the same side, or closed up.  Trans is opened up/ straightened out.  In normal water in the dark at pretty much any temperature you'll have 99/1 trans/cis ratio.  

 

A few hours in the dark and it'll go back to trans because the OH groups do get kinda close with cis-resveratrol.  The negative charges of the OH groups do push against one another to open it up again.  


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#7 LexLux

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Posted 04 June 2014 - 09:11 AM

Anyone have an update?







Also tagged with one or more of these keywords: resveratrol, ribose, lozenge, bioavailability

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