• Log in with Facebook Log in with Twitter Log In with Google      Sign In    
  • Create Account
  LongeCity
              Advocacy & Research for Unlimited Lifespans

Photo
- - - - -

Resveratrol - Micronized?


  • Please log in to reply
64 replies to this topic

#1 Anthony_Loera

  • Life Member
  • 3,130 posts
  • 713
  • Location:Miami Florida

Posted 27 September 2007 - 03:26 PM


Hi Everyone,

Many folks here take resveratrol powder in 80 or 120 mesh particle size, some may even take tablets. At RevGenetics we are having an internal debate regarding micronized resveratrol, which no one offers at this time.

I wanted to ask about it to you all, as your opinion matters and maybe I am missing something obvious. The debate really centers around cost vs benefit. Most rsv capsule makers and suppliers will supply powder, but not micronized powder.

I believe first off, we need to understand some of the sizes for comparison here (please correct me if I am wrong):

"Mesh 80" is about 0.178mm particles
"Mesh 120" is about 0.12 mm particles (120um)
"Micronized" particles are about 1.0 um and in some cases lower.

The current SRT501 formulation uses micronized resveratrol, and likely anyone making a look-a-like formulation will eventually use micronized rsv as well.

the issue then is this...

When we compare 99% Resveratrol against the SRT501 formulation we have a 202% percent increase in SIRT1 activation (according to Sirtris). Does this percentage really benefit the consumer if the formulation is produced at a higher cost than buying non-micronized resveratrol? We are still gathering equipment pricing to consider a micronized rsv formulation, but what (other than marketing) benefit will micronizing the resveratrol produce for the average person if it costs more to buy 2 grams of micronized rsv than 4 grams of regular 99% rsv?


Other than a marketing benefit (Marketing is powerful, don't get me wrong)... I am not sure micronized rsv presents such a powerful benefit over non-micronized rsv to support a higher cost for the average person.

Am I missing something here?

Anthony

#2 dannov

  • Guest
  • 317 posts
  • -1

Posted 27 September 2007 - 05:44 PM

I'm glad you're looking into this, the problem is, it's probably too early to tell if micronized res really will make a difference or not until those human studies are released to the public and successfully replicated. It could and will most likely take years. From what I've seen though, micronized anything (ie. - creatine) gets much better absorption into the bloodstream.

Click HERE to rent this advertising spot to support LongeCity (this will replace the google ad above).

#3 malbecman

  • Guest
  • 728 posts
  • 151
  • Location:Sunny CA

Posted 27 September 2007 - 09:31 PM

Am I missing something here?

Anthony




I think you are on track here Anthony (more or less). The main question would be who are you selling to? For the "novice" resveratrol supplementer, you may be able to market the micronized res at a sufficient price point to make it worth your while. For the more experienced res-head people on these boards, I don't think it will fly, at least until we see if there is a clear benefit in a year or two.......

#4 niner

  • Guest
  • 16,276 posts
  • 2,001
  • Location:Philadelphia

Posted 28 September 2007 - 02:49 AM

I thought SRT501 was supposed to be more like an order of magnitude better blood levels rather than 200%... but I don't have the data in front of me. SRT501 is also wrapped up in cyclodextrin. Maybe another substance could be used, like lecithin or Miralax. We wouldn't really know how good such an approach would be, but it would have to be better than the suspensions of larger particles that a lot of us are drinking. I'd be very interested in a micronized product if the price was not too crazy.

#5 ilanso

  • Guest
  • 153 posts
  • 0

Posted 28 September 2007 - 03:17 AM

I would go for it if the premium did not exceed 50% of the regular 99% price.
This would open the door to different delivery vehicles, possibly ophthalmic (with cyclodextrin), intra-nasal, dermal or sub-cutaneous (via insulin pens). I remember having heard of chewing gum formulations. I don't think the sub-lingual / gingival / rectal (suppositories) transmucosal routes hold much promise.
Next thing you know, the new generation junkies (resv-heads) will do lines, smoke freebase and "slam" ;)

#6 galtsgulch

  • Guest
  • 51 posts
  • 7
  • Location:Varies

Posted 01 October 2007 - 11:10 PM

Life-Enhancement presently offers a PEGylated Liposomal (i.e. NanoSphere) Resveratrol. Here's what their online catalog says about it:

Resveratrol is a choice example of the antioxidant polyphenols prevalent in such foods as red wine, green tea, apples, berries, pomegranates, and dark chocolate.* Yet despite wide acclaim for its properties, when taken orally resveratrol has very low bioavailability, and even the small portion that enters the bloodstream is rapidly metabolized. Until now! This PEGylated liposomal formulation enters the bloodstream via transmucosal absorption, thus providing enhanced bioavailability. As well, it is designed to help sustain blood levels, achieve higher-potency responses, increase circulatory half-life, and enhance site-specific actions.* Also, PEGysomal Resveratrol can more readily cross the blood-brain barrier.*

They have an excellent article about the PEGylation process (which is short for coating the Liposomal NanoShere with polyethylene glycol so as to make it "stealth") at: http://www.life-enha...ate.asp?id=1106.

My understanding is that they are going to come out with some higher strength PEGylated Resveratrols soon.

#7 maxwatt

  • Guest, Moderator LeadNavigator
  • 4,938 posts
  • 1,612
  • Location:New York

Posted 02 October 2007 - 12:20 AM

Life-Enhancement presently offers a PEGylated Liposomal (i.e. NanoSphere) Resveratrol.  Here's what their online catalog says about it:

Resveratrol is a choice example of the antioxidant polyphenols prevalent in such foods as red wine, green tea, apples, berries, pomegranates, and dark chocolate.* Yet despite wide acclaim for its properties, when taken orally resveratrol has very low bioavailability, and even the small portion that enters the bloodstream is rapidly metabolized. Until now! This PEGylated liposomal formulation enters the bloodstream via transmucosal absorption, thus providing enhanced bioavailability. As well, it is designed to help sustain blood levels, achieve higher-potency responses, increase circulatory half-life, and enhance site-specific actions.* Also, PEGysomal Resveratrol can more readily cross the blood-brain barrier.*

They have an excellent article about the PEGylation process (which is short for coating the Liposomal NanoShere with polyethylene glycol so as to make it "stealth") at: http://www.life-enha...ate.asp?id=1106.

My understanding is that they are going to come out with some higher strength PEGylated Resveratrols soon.


I would hope so. The amount of resveratrol per serving is so low I doubt the efficacy, no mater how efficient the delivery system. And there's no PEG listed in the ingredients.

Supplement Facts
 
Serving size: 1 ml
Servings per container: 60  Amount
Per Serving  % Daily
Value 
Resveratrol (polygonum cuspidactum root)  10 mg  * 
Lecithin  110 mg  * 

*Daily Value Not Established


Other Ingredients: Purified water, ethanol, phospholipids, polyethylene glycol, phosphatidylethanolamine, natural chocolate flavoring, and sweeteners.



#8 zoolander

  • Guest
  • 4,724 posts
  • 55
  • Location:Melbourne, Australia

Posted 02 October 2007 - 12:46 AM

Life-enhancement have a very bad reputation from what I have seen and heard. Have a look at their product over at consumerlabs

#9 galtsgulch

  • Guest
  • 51 posts
  • 7
  • Location:Varies

Posted 02 October 2007 - 03:08 AM

I would hope so.  The amount of resveratrol per serving is so low I doubt the efficacy, no mater how efficient the delivery system.  And there's no PEG listed in the ingredients. 

Supplement Facts
 
Serving size: 1 ml
Servings per container: 60  Amount
Per Serving  % Daily
Value 
Resveratrol (polygonum cuspidactum root)  10 mg  * 
Lecithin  110 mg  * 

*Daily Value Not Established


Other Ingredients: Purified water, ethanol, phospholipids, polyethylene glycol, phosphatidylethanolamine, natural chocolate flavoring, and sweeteners.


The PEG is listed in the "Other Ingredients" list as polyethylene glycol (that's that PEG stands for). I recommend reading the article that I linked.

#10 galtsgulch

  • Guest
  • 51 posts
  • 7
  • Location:Varies

Posted 13 October 2007 - 05:41 AM

Life-enhancement have a very bad reputation from what I have seen and heard. Have a look at their product over at consumerlabs


I asked Will Block, the founder of Life-Enhancement about those tests. He said that all Consumerlabs would tell him was the lot number, which was a four-year old bottle (L-E doesn't sell supplements that old) and they wouldn't tell him anything about the tests or the protocols they use.

I checked in with them and they say that they charge $3,750 to have a single product tested and "certified" by them. Seems like they have the potential for abuse, since if you're not a member they don't have to tell you anything and can basically slam you without any recourse.

That's just my opinion.

#11 galtsgulch

  • Guest
  • 51 posts
  • 7
  • Location:Varies

Posted 13 October 2007 - 06:21 AM

Dear James,

Thank you for your e-mail and interest in ConsumerLab.com. As the leading consumer-oriented testing service company, consumers, health practitioners, and retailers actively use our CL Approved Products Lists to select products. Our website,www.consumerlab.com, received over 3 million visits in the last 12 months and 80,000+ people have joined our e-newsletter. In addition to our individual subscribers, our institutional subscribers have included university libraries, public libraries, hospitals, healthcare centers, HMOs, medical practices and government agencies.

The media has embraced CL's work with extensive coverage in The New York Times, The Los Angeles Times, The Wall Street Journal, Health Magazine, Prevention Magazine, Money Magazine, Time Magazine, Better Homes & Gardens, O, The Oprah Magazine, Men’s Health, The Today Show, CNN, Good Morning America, and many other consumer/health related periodicals, and newsletters, radio programs and Web sites. Additionally in September 2003, CL released its first book, a Buyer's Guide, which includes a number of our Product Reviews. The book has received rave reviews and a second book was published in 2007.

Benefits of participating in CL’s Voluntary Certification Program for Approved Products include:
• Online listing as “Approved Quality” on the popular ConsumerLab.com website
• Listing in a future ConsumerLab.com book
Potential mention of your product as Approved in free media coverage
• Use of the CL Seal in:
On your web site
Business-to-business marketing/sales materials
Presentations
Trade Show displays
News releases
Internal Reports, including Annual Reports
• Other promotional opportunities through our licensing program -- including use of the CL Seal on labels, displays, and consumer-directed marketing materials (see attached)

The average testing fee for a single product is approximately $3,750. Volume discounts are available for both our testing and licensing programs.

CL's testing and Seal licensing programs are invaluable, additional marketing tools for a brand. In this competitive marketplace, independent, third-party testing makes a difference to consumers and helps a product standout on its quality claim. If you are interested in getting quotes for testing specific products, please send me a list. Also, if you would like to be added to my industry e-mail list so you will receiving notification as to when categories will be tested, let me know. I look forward to hearing from you.

#12 craigb527

  • Guest
  • 116 posts
  • -9

Posted 13 October 2007 - 05:42 PM

Life-Enhancement presently offers a PEGylated Liposomal (i.e. NanoSphere) Resveratrol.  Here's what their online catalog says about it:

Also, PEGysomal Resveratrol can more readily cross the blood-brain barrier.*

They have an excellent article about the PEGylation process (which is short for coating the Liposomal NanoShere with polyethylene glycol so as to make it "stealth") at: http://www.life-enha...ate.asp?id=1106.

My understanding is that they are going to come out with some higher strength PEGylated Resveratrols soon.

.
It is my understanding that the blood brain barrier is like the high end night clubs, very selective. Resveratrol is not on the guest list. I think them making the claim more readily cross the bbb is a sales pitch because more readily implies resveratrol was crossing the barrier before and that they are improving on this. I may be wrong, but from
what I have read, resveratrol was not crossing the bbb.

Edited by craigb527, 13 October 2007 - 05:53 PM.


#13 tintinet

  • Location:ME

Posted 13 October 2007 - 07:09 PM

1: Brain Res. 2002 Dec 27;958(2):439-47. Related Articles, Links
Click here to read
Resveratrol protects against global cerebral ischemic injury in gerbils.

Wang Q, Xu J, Rottinghaus GE, Simonyi A, Lubahn D, Sun GY, Sun AY.

Department of Pharmacology, School of Medicine, M526 Medical Science Bldg, 1 Hospital Drive, University of Missouri-Columbia, Columbia, MO 65212, USA.

Increased oxidative stress has been implicated in the mechanisms of delayed neuronal cell death (DND) following cerebral ischemic insult. In this study, we investigated whether resveratrol, a polyphenolic antioxidant enriched in grape, may ameliorate ischemia-induced neuron cell death. Mongolian gerbils were divided into three groups, namely, sham control, ischemia and ischemia treated with resveratrol. Transient global cerebral ischemia was induced by occlusion of both common carotid arteries (CCA) for 5 min. Resveratrol was injected i.p. (30 mg/kg body weight), either during or shortly after CCA occlusion, and again at 24 h after ischemia. Cerebral blood flow was monitored before and during CCA occlusion using a laser Doppler flowmeter. Brain sections were immuno-stained for neurons, astrocytes and microglial cells. A time course study was also carried out to assess the bioavailability of resveratrol in serum, liver and brain using high performance liquid chromatography (HPLC). Morphometric measurements indicated extensive DND in the hippocampal CA1 region 4 days after ischemia and that neuron cell death was marked by the increase in reactive astrocytes and microglial cells. Administration of resveratrol, either during or after CCA occlusion, significantly (P<0.05) decreased DND as well as glial cell activation. Analysis of resveratrol after i.p. injection indicated its presence in serum, liver and brain with peak activity at 1, 4 and 4 h, respectively. This study demonstrated for the first time that resveratrol, a polyphenolic antioxidant, can cross the blood-brain barrier and exert protective effects against cerebral ischemic injury.Copyright 2002 Elsevier Science B.V.

Publication Types:

* Research Support, Non-U.S. Gov't
* Research Support, U.S. Gov't, P.H.S.


MeSH Terms:

* Animals
* Brain Ischemia/metabolism
* Brain Ischemia/prevention & control*
* Cell Death/drug effects
* Cell Death/physiology
* Gerbillinae
* Hippocampus/drug effects
* Hippocampus/metabolism
* Male
* Neuroglia/drug effects
* Neuroglia/metabolism
* Neurons/drug effects
* Neurons/metabolism
* Reperfusion Injury/metabolism
* Reperfusion Injury/prevention & control
* Stilbenes/metabolism
* Stilbenes/pharmacology
* Stilbenes/therapeutic use*


Substances:

* Stilbenes
* resveratrol


Grant Support:

* 1 P01 ES10535/ES/NIEHS
* AA 06661/AA/NIAAA
* AG18357/AG/NIA


PMID: 12470882 [PubMed - indexed for MEDLINEB]
  • like x 1

#14 craigb527

  • Guest
  • 116 posts
  • -9

Posted 14 October 2007 - 02:21 AM

Hmm.... worked on gerbils when injected, seems resonable it would work on humans taken orally. Article kinda old, but study seems professionally done.

#15 malbecman

  • Guest
  • 728 posts
  • 151
  • Location:Sunny CA

Posted 15 October 2007 - 11:29 PM

Hmm.... worked on gerbils when injected, seems resonable it would work on humans taken orally.  Article kinda old, but study seems professionally done.




Don't forget this study on rats, ip admin., showed effects on antiox. enzymes in the brain.....
(my emphasis added)



Neurochem Res. 2007 Jun;32(6):981-7. Epub 2007 Mar 31.
Effect of resveratrol on antioxidant enzyme activities in the brain of healthy rat.
Mokni M, Elkahoui S, Limam F, Amri M, Aouani E.
Laboratoire de Physiologie de la Nutrition, Faculté des Sciences de Tunis, Campus Universitaire El Manar II, Tunis, Tunisia.

We have studied the effect of resveratrol on lipoperoxidation and antioxidant enzyme activity level in the brain of healthy rats. When intraperitoneally administered, resveratrol significantly and dose dependently decreased brain malondialdehyde level. Resveratrol also increased in a dose-dependent way brain superoxide dismutase, catalase and peroxidase activities. Optimal effect on antioxidant enzyme and lipoperoxidation products were obtained with resveratrol concentration of 12.5 mg/kg body wt. Native polyacrylamide gel electrophoresis analysis of antioxidant isoenzymes revealed that resveratrol up regulated at least two acidic superoxide dismutase isoforms called A(1) and A(2), two basic isoforms called B(1) and B(2). Resveratrol also up regulated two catalase isoforms and a broad peroxidase band corresponding to several isoforms. All these findings suggest that resveratrol is able to cross the blood brain barrier and exerts potent antioxidant features. Resveratrol also exerts neuroprotective properties by up regulating several detoxifying enzymes, most of which are iron proteins.

#16 stephen_b

  • Guest
  • 1,661 posts
  • 196

Posted 16 October 2007 - 01:17 AM

Resveratrol also exerts neuroprotective properties by up regulating several detoxifying enzymes, most of which are iron proteins.[/b]

Makes me wonder if my high blood iron can be related to 2g/day resveratrol intake?

Stephen

#17 Anthony_Loera

  • Topic Starter
  • Life Member
  • 3,130 posts
  • 713
  • Location:Miami Florida

Posted 17 October 2007 - 08:31 PM

Am I missing something here?

Anthony




I think you are on track here Anthony (more or less). The main question would be who are you selling to? For the "novice" resveratrol supplementer, you may be able to market the micronized res at a sufficient price point to make it worth your while. For the more experienced res-head people on these boards, I don't think it will fly, at least until we see if there is a clear benefit in a year or two.......


[lol]
Just an FYI:

We have scheduled a chat with a chemist that specializes in nano particles in November.
We will be combining rsv & lecithin into a micronized (or better) gelatin like sludge, that should be able to mix well with almost anything including creams, sprays, drops, and be injectable for those serious enough to consider it.

Because of the previous 'Sample Dosage' thread I think there may be a market for this, but we will not know until we get a sample batch produced and tested in a California university lab.

[thumb]
We are shooting to have something interesting 1st quarter 2008 (If things stay on schedule).

Anthony Loera

#18 stephen_b

  • Guest
  • 1,661 posts
  • 196

Posted 17 October 2007 - 10:04 PM

Sounds very innovative; I haven't heard of anyone else going that route. I'll stay tuned.

Stephen

#19 malbecman

  • Guest
  • 728 posts
  • 151
  • Location:Sunny CA

Posted 18 October 2007 - 04:20 PM

Very interesting, indeed. We'll all stay tuned, I'm sure. Same bat-time, same bat-channel (an old reference to the Batman TV show....)


[lol]
Just an FYI:

We have scheduled a chat with a chemist that specializes in nano particles in November.
We will be combining rsv & lecithin into a micronized (or better) gelatin like sludge, that should be able to mix well with almost anything including creams, sprays, drops, and be injectable for those serious enough to consider it.

Because of the previous 'Sample Dosage' thread I think there may be a market for this, but we will not know until we get a sample batch produced and tested in a California university lab.

[thumb]
We are shooting to have something interesting 1st quarter 2008 (If things stay on schedule).

Anthony Loera



#20 Hedgehog

  • Guest
  • 462 posts
  • 1

Posted 08 January 2008 - 12:16 AM

Hi Everyone,

Many folks here take resveratrol powder in 80 or 120 mesh particle size, some may even take tablets. At RevGenetics we are having an internal debate regarding micronized resveratrol, which no one offers at this time.

I wanted to ask about it to you all, as your opinion matters and maybe I am missing something obvious. The debate really centers around cost vs benefit. Most rsv capsule makers and suppliers will supply powder, but not micronized powder.

I believe first off, we need to understand some of the sizes for comparison here (please correct me if I am wrong):

"Mesh 80" is about 0.178mm particles
"Mesh 120" is about 0.12 mm particles (120um)
"Micronized" particles are about 1.0 um and in some cases lower.

The current SRT501 formulation uses micronized resveratrol, and likely anyone making a look-a-like formulation will eventually use micronized rsv as well.

the issue then is this...

When we compare 99% Resveratrol against the SRT501 formulation we have a 202% percent increase in SIRT1 activation (according to Sirtris). Does this percentage really benefit the consumer if the formulation is produced at a higher cost than buying non-micronized resveratrol? We are still gathering equipment pricing to consider a micronized rsv formulation, but what (other than marketing) benefit will micronizing the resveratrol produce for the average person if it costs more to buy 2 grams of micronized rsv than 4 grams of regular 99% rsv?


Other than a marketing benefit (Marketing is powerful, don't get me wrong)... I am not sure micronized rsv presents such a powerful benefit over non-micronized rsv to support a higher cost for the average person.

Am I missing something here?

Anthony


I knew to the SRT501 being a micronized sample? Did you find this in a patent? I guess if you are taking it in a pill form micronized would be the best. However, most of the literature seems to think that the low bioavailability comes from the rapid breakdown. However, Micronizing a sample probably won't hurt it and might help but probably not all that much.


"HIGH ABSORPTION BUT VERY LOW BIOAVAILABILITY OF ORAL RESVERATROL IN HUMANS"


Micronization: A method of improving the bioavailability of poorly soluble drugs
Chaumeil, J.C. Posted Image Posted Image

For poorly soluble drugs, the digestive absorption depends on their rate of dissolution. Decreasing the particle size of these drugs improves their rate of dissolution. Fine grinding mills are use to micronize powders: either jar mills or fluid energy mills. These processes were applied to griseofulvin, progesterone, spironolactone and diosmin. For each drug, micronization improved their digestive absorption, and consequently their bioavailability and clinical efficacy.

#21 maxwatt

  • Guest, Moderator LeadNavigator
  • 4,938 posts
  • 1,612
  • Location:New York

Posted 08 January 2008 - 12:43 AM

Hi Everyone,

Many folks here take resveratrol powder in 80 or 120 mesh particle size, some may even take tablets. At RevGenetics we are having an internal debate regarding micronized resveratrol, which no one offers at this time.

I wanted to ask about it to you all, as your opinion matters and maybe I am missing something obvious. The debate really centers around cost vs benefit. Most rsv capsule makers and suppliers will supply powder, but not micronized powder.

I believe first off, we need to understand some of the sizes for comparison here (please correct me if I am wrong):

"Mesh 80" is about 0.178mm particles
"Mesh 120" is about 0.12 mm particles (120um)
"Micronized" particles are about 1.0 um and in some cases lower.

The current SRT501 formulation uses micronized resveratrol, and likely anyone making a look-a-like formulation will eventually use micronized rsv as well.

the issue then is this...

When we compare 99% Resveratrol against the SRT501 formulation we have a 202% percent increase in SIRT1 activation (according to Sirtris). Does this percentage really benefit the consumer if the formulation is produced at a higher cost than buying non-micronized resveratrol? We are still gathering equipment pricing to consider a micronized rsv formulation, but what (other than marketing) benefit will micronizing the resveratrol produce for the average person if it costs more to buy 2 grams of micronized rsv than 4 grams of regular 99% rsv?


Other than a marketing benefit (Marketing is powerful, don't get me wrong)... I am not sure micronized rsv presents such a powerful benefit over non-micronized rsv to support a higher cost for the average person.

Am I missing something here?

Anthony


I knew to the SRT501 being a micronized sample? Did you find this in a patent? I guess if you are taking it in a pill form micronized would be the best. However, most of the literature seems to think that the low bioavailability comes from the rapid breakdown. However, Micronizing a sample probably won't hurt it and might help but probably not all that much.


"HIGH ABSORPTION BUT VERY LOW BIOAVAILABILITY OF ORAL RESVERATROL IN HUMANS"


Micronization: A method of improving the bioavailability of poorly soluble drugs
Chaumeil, J.C. Posted Image Posted Image

For poorly soluble drugs, the digestive absorption depends on their rate of dissolution. Decreasing the particle size of these drugs improves their rate of dissolution. Fine grinding mills are use to micronize powders: either jar mills or fluid energy mills. These processes were applied to griseofulvin, progesterone, spironolactone and diosmin. For each drug, micronization improved their digestive absorption, and consequently their bioavailability and clinical efficacy.


Some background information, since reading all the resveratrol threads, especially the 500 mg one, is tedious.

The patent was referenced in the 500 mg thread last winter. It was posted by Paragon, I think, and vetted by Proteomist, neither of whom have been around for months. It claims a 5 to 10 times greater availability with this method than with oral consumption of a powder.

The micronization is to enable the resveratrol to bind to the surfactant, specified preferentially as tween80, but also PEG or other embodiments known to those skilled in the art. The patent implies the surfactant acts as a carrier in the body to get it to the cells where it is needed. Our skilled chemists determined lecithin is one such embodiment. We tried Miralax which is PEG350, as a surfactant. Some people have problems with a cumulative laxative effect from Miralax and prefer lecithin. Much of the powdered resveratrol we use is specified at 80 or 120 mesh, but a lot of it is a fine dust, a high percentage of which is under 10 microns. Also some of the literature specifies micronized particle size of between 5 and 10 microns. I spoke to my contact in China, who said they could supply micronized trans-resveratrol if I wanted, but the purity would only be guaranteed to 95%, since heat from the grinding process causes some of the material to decompose.

Malbecman and others have dissolved resveratrol in Everclear (95% alcohol) then added water with lecithin. This precipitates the resveratol out of solution whence it binds with the lecithin or miralax surfactant.
  • like x 1

#22 Anthony_Loera

  • Topic Starter
  • Life Member
  • 3,130 posts
  • 713
  • Location:Miami Florida

Posted 08 January 2008 - 08:19 PM

I believe the micronization the Chinese folks you mentioned will be doing is through grinding, and leave a very fine powder.

The end product for us will not be dry powder, and grinding is not used so the issue of t-res loss is minimized. We do have other issues though, so we continue to push through these.

A

#23 Hedgehog

  • Guest
  • 462 posts
  • 1

Posted 08 January 2008 - 09:33 PM

Hi Everyone,

Many folks here take resveratrol powder in 80 or 120 mesh particle size, some may even take tablets. At RevGenetics we are having an internal debate regarding micronized resveratrol, which no one offers at this time.

I wanted to ask about it to you all, as your opinion matters and maybe I am missing something obvious. The debate really centers around cost vs benefit. Most rsv capsule makers and suppliers will supply powder, but not micronized powder.

I believe first off, we need to understand some of the sizes for comparison here (please correct me if I am wrong):

"Mesh 80" is about 0.178mm particles
"Mesh 120" is about 0.12 mm particles (120um)
"Micronized" particles are about 1.0 um and in some cases lower.

The current SRT501 formulation uses micronized resveratrol, and likely anyone making a look-a-like formulation will eventually use micronized rsv as well.

the issue then is this...

When we compare 99% Resveratrol against the SRT501 formulation we have a 202% percent increase in SIRT1 activation (according to Sirtris). Does this percentage really benefit the consumer if the formulation is produced at a higher cost than buying non-micronized resveratrol? We are still gathering equipment pricing to consider a micronized rsv formulation, but what (other than marketing) benefit will micronizing the resveratrol produce for the average person if it costs more to buy 2 grams of micronized rsv than 4 grams of regular 99% rsv?


Other than a marketing benefit (Marketing is powerful, don't get me wrong)... I am not sure micronized rsv presents such a powerful benefit over non-micronized rsv to support a higher cost for the average person.

Am I missing something here?

Anthony


I knew to the SRT501 being a micronized sample? Did you find this in a patent? I guess if you are taking it in a pill form micronized would be the best. However, most of the literature seems to think that the low bioavailability comes from the rapid breakdown. However, Micronizing a sample probably won't hurt it and might help but probably not all that much.


"HIGH ABSORPTION BUT VERY LOW BIOAVAILABILITY OF ORAL RESVERATROL IN HUMANS"


Micronization: A method of improving the bioavailability of poorly soluble drugs
Chaumeil, J.C. Posted Image Posted Image

For poorly soluble drugs, the digestive absorption depends on their rate of dissolution. Decreasing the particle size of these drugs improves their rate of dissolution. Fine grinding mills are use to micronize powders: either jar mills or fluid energy mills. These processes were applied to griseofulvin, progesterone, spironolactone and diosmin. For each drug, micronization improved their digestive absorption, and consequently their bioavailability and clinical efficacy.


Some background information, since reading all the resveratrol threads, especially the 500 mg one, is tedious.

The patent was referenced in the 500 mg thread last winter. It was posted by Paragon, I think, and vetted by Proteomist, neither of whom have been around for months. It claims a 5 to 10 times greater availability with this method than with oral consumption of a powder.

The micronization is to enable the resveratrol to bind to the surfactant, specified preferentially as tween80, but also PEG or other embodiments known to those skilled in the art. The patent implies the surfactant acts as a carrier in the body to get it to the cells where it is needed. Our skilled chemists determined lecithin is one such embodiment. We tried Miralax which is PEG350, as a surfactant. Some people have problems with a cumulative laxative effect from Miralax and prefer lecithin. Much of the powdered resveratrol we use is specified at 80 or 120 mesh, but a lot of it is a fine dust, a high percentage of which is under 10 microns. Also some of the literature specifies micronized particle size of between 5 and 10 microns. I spoke to my contact in China, who said they could supply micronized trans-resveratrol if I wanted, but the purity would only be guaranteed to 95%, since heat from the grinding process causes some of the material to decompose.

Malbecman and others have dissolved resveratrol in Everclear (95% alcohol) then added water with lecithin. This precipitates the resveratol out of solution whence it binds with the lecithin or miralax surfactant.


has there been any published papers saying that the glycosylation and sulfonation moieties to Resveratrol don't get cleaved once inside the destination cell? I have read in a few papers that the reason for added moieties is not only elimination but also to direct it to a certain type of cell(s). This would be another important experiment. Maybe somebody should ask Sirtris? Seems like a fundamental experiment they should have run.

With regards to micronization. Typically there is a machine that blows the stuff around, once it gets to a certain size it can blow out of the container into holding bag. (a simplistic way of explaining it) The bag should be analyzed by a number of test including SEM and Laser Light Scattering. If only one of these tests are done it can be very misleading! So I guess Anthony if you do want to validate you are getting the certain size particle you want you should at least have these two tests done if not more. It takes a lot of work to get it down to your specifications.

Adding a Salt Typical greatly enhances absorbation. Anthony, do you know if your resveratrol is free base or is it salt form? My guess is that it is a free base? Anyways, another experiment would be to dissolve resveratrol in EtOH add different salts such as (K,Na,Citrate...ect), might also work like surfactant.

#24 Anthony_Loera

  • Topic Starter
  • Life Member
  • 3,130 posts
  • 713
  • Location:Miami Florida

Posted 08 January 2008 - 09:51 PM

hedgehog_info,

at this point no one is doing micronized resveratrol for supplements.
Having said that, we have this process:

1- Particle Size Testing (before)
2- <ejem> Processing
3- Particle Size Testing (after)
4- Microscopic Imaging (before & after)

But don't have a finalized version of the end product. We have some delays and are taking baby steps at this point...

A

Edited by Anthony_Loera, 08 January 2008 - 09:56 PM.


#25 Hedgehog

  • Guest
  • 462 posts
  • 1

Posted 08 January 2008 - 10:39 PM

1- Particle Size Testing (before)
2- <ejem> Processing
3- Particle Size Testing (after)
4- Microscopic Imaging (before & after)


Thanks, with regards to the microscope imaging I have seen our drug crystals grow over time! This has happened in as little as a month. Thats why you sometimes need a salt form of your API which might help.

What is ejem processing?

#26 niner

  • Guest
  • 16,276 posts
  • 2,001
  • Location:Philadelphia

Posted 09 January 2008 - 04:21 AM

has there been any published papers saying that the glycosylation and sulfonation moieties to Resveratrol don't get cleaved once inside the destination cell? I have read in a few papers that the reason for added moieties is not only elimination but also to direct it to a certain type of cell(s). This would be another important experiment. Maybe somebody should ask Sirtris? Seems like a fundamental experiment they should have run.

Yeah, this is an important question. Glucuronidates have been used in prodrug approaches; I don't know what the nature of the drug is in these cases. Generally speaking, conjugation targets the compound mainly for elimination, by virtue of the enhanced water solubility that it confers. It does seem like if anyone would know if resveratrol has active metabolites, it would be Sirtris. I'd be kind of surprised if they'd be willing to talk details, but you never know.

Adding a Salt Typical greatly enhances absorbation. Anthony, do you know if your resveratrol is free base or is it salt form? My guess is that it is a free base? Anyways, another experiment would be to dissolve resveratrol in EtOH add different salts such as (K,Na,Citrate...ect), might also work like surfactant.

The only ionizable groups on resveratrol are the phenolic OH's. They have pretty high pKa's and are essentially not ionized in the body, so it's just a neutral molecule for all intents and purposes.

#27 Anthony_Loera

  • Topic Starter
  • Life Member
  • 3,130 posts
  • 713
  • Location:Miami Florida

Posted 18 April 2010 - 08:07 PM

At this point in time, only one company is micronizing resveratrol down to the 1.5-1.8 micron particle size.
I remind folks to check if a product is micronized, as it will state the particle size on the label.

Be aware of marketing:

1- One competitor that went from stating that micronized resveratrol does not work, to coming out and selling a 2.5+ micron size micronized resveratrol product. Apparently folks are finally coming around to understand it's absorption benefits. I believe this is a good thing for everyone.

2- A second competitor states they use "micronized resveratrol matrix" in their product, however when asked, they have not provided any particle size on the product label or in any documentation.

3- Be aware that folks that use the term "Micronized Resveratrol" without stating the particle size, are strictly doing so for marketing and should be avoided until they label the product correctly or provide documentation about the particle size used in their product. Please ask to be told the particle size so that you can make quality comparisons between micronized products.

Be informed, and you will not go wrong. Here is the price list of many products that is provided by this forum:
http://www.imminst.o...ers-t36436.html


It is certainly possible to dissolve high purity 98% - 99% resveratrol in ethanol and make your own small particle resveratrol. However for folks that don't drink alcohol, it may be better to purchase micronized powder or capsules. Be smart when looking at labels, and check the particle size if this is something you are considering.

Cheers
A

Edited by Anthony_Loera, 18 April 2010 - 08:19 PM.


#28 zorba990

  • Guest
  • 1,381 posts
  • 207

Posted 19 April 2010 - 03:19 AM

Why does the micronized version cost so much to produce? Is it the machinery that does it, or is it labor intensive? The micronized powder is so much more expensive (and seems to be the only powder you currently carry, that I had to go looking elsewhere for the powder. Kings Herbs
is where I got my current batch but I'd still be buying from you guys if the regular powder was available.
99% seems to be fine in lecithin even without sonification.

I tried dissolving in a bit of vodka for a while but my lady said no to the early morning drinking
(and she asks for little in my crazy ways so I'm not gonna argue LOL).

BTW HMB, acidophilus, or anything that maintains intestinal butyrate levels keeps the loose stools away with
high dose TRES use. If I let it slide for a while then slide it does.

At this point in time, only one company is micronizing resveratrol down to the 1.5-1.8 micron particle size.
I remind folks to check if a product is micronized, as it will state the particle size on the label.

Be aware of marketing:

1- One competitor that went from stating that micronized resveratrol does not work, to coming out and selling a 2.5+ micron size micronized resveratrol product. Apparently folks are finally coming around to understand it's absorption benefits. I believe this is a good thing for everyone.

2- A second competitor states they use "micronized resveratrol matrix" in their product, however when asked, they have not provided any particle size on the product label or in any documentation.

3- Be aware that folks that use the term "Micronized Resveratrol" without stating the particle size, are strictly doing so for marketing and should be avoided until they label the product correctly or provide documentation about the particle size used in their product. Please ask to be told the particle size so that you can make quality comparisons between micronized products.

Be informed, and you will not go wrong. Here is the price list of many products that is provided by this forum:
http://www.imminst.o...ers-t36436.html


It is certainly possible to dissolve high purity 98% - 99% resveratrol in ethanol and make your own small particle resveratrol. However for folks that don't drink alcohol, it may be better to purchase micronized powder or capsules. Be smart when looking at labels, and check the particle size if this is something you are considering.

Cheers
A


Edited by zorba990, 19 April 2010 - 03:23 AM.


#29 browser

  • Validating
  • 319 posts
  • 1
  • Location:Austin, TX

Posted 19 April 2010 - 04:19 PM

Why does the micronized version cost so much to produce? Is it the machinery that does it, or is it labor intensive? The micronized powder is so much more expensive (and seems to be the only powder you currently carry, that I had to go looking elsewhere for the powder. Kings Herbs
is where I got my current batch but I'd still be buying from you guys if the regular powder was available.
99% seems to be fine in lecithin even without sonification.

I tried dissolving in a bit of vodka for a while but my lady said no to the early morning drinking
(and she asks for little in my crazy ways so I'm not gonna argue LOL).

BTW HMB, acidophilus, or anything that maintains intestinal butyrate levels keeps the loose stools away with
high dose TRES use. If I let it slide for a while then slide it does.


It's interesting, this game of supplier promotion. Sardi released something new a few days ago, saying that because of all the hype by the 350+ suppliers of Resveratrol on the 'Net, his company now only sells its product to the medical community. Interesting that his capsules are still available on his website for anyone with valid credit card credentials. Perhaps he means his product in bulk is only available to medical professionals. That can't be right. His product includes the titanium capsule. And here we have a blatant advert in the form of a public service announcement, which the moderators do nothing about. Sardi issues public service announcements as well. Gotta tell my friends that if they want to promote their wares, ImmInst.org is the place to do it.

I dropped Curcumin from my regimen temporarily. I am amazed that suddenly I've gotten my sh*t together. No more ghastly cramps, no more 14 trips+ a day to the lu. And I'm taking 20 grams of 98% Resveratrol in the morning and sucking on these really great NatriHill 20 mg. Resveratrol lozenges all day and evening.

Click HERE to rent this advertising spot to support LongeCity (this will replace the google ad above).

#30 Anthony_Loera

  • Topic Starter
  • Life Member
  • 3,130 posts
  • 713
  • Location:Miami Florida

Posted 19 April 2010 - 04:30 PM

Hi Zorba,

Micronization down to 1.5 microns is expensive, reducing the particle size to say... 5-8 microns is not quite as expensive, but we do not consider that particle size as "micronized" since it does not match closely the particle size used at Sirtris, when they compared micronized resveratrol absorption vs non-micronized resveratrol.

We are actually waiting on a new high purity shipment, to begin offering regular non-micronized resveratrol again in bulk form just for folks like yourself and browser who prefer the larger particle (or lower price) of high purity regular bulk resveratrol.

Cheers
A

Edited by Anthony_Loera, 19 April 2010 - 04:33 PM.





0 user(s) are reading this topic

0 members, 0 guests, 0 anonymous users