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Nootropic transdermal spray?


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7 replies to this topic

#1 Pike

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Posted 05 February 2009 - 05:17 AM


So, after perusing the forums of some body-building websites, it seems that transdermals are quite an effective route for delivery of agents that have relatively low bioavailability or low half-lives. Apparently, it's reported that with transdermals, the active agent of something can last as long as 12 hours!

When I hear 12 hours of an active agent, I think of substances like CX-516 or Noopept and wonder if we could extend their bioavailability/acting times.

Apparently, bulknutrition sells something called the transport matrix where it essentially is a make-it-yourself transdermal bottle.

Has anyone else ever delved into this?

#2 hamishm00

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Posted 05 February 2009 - 08:58 AM

Yeah, I've looked into all this and I think it's all 100% nonsense most of the time, particularly when they go the homeopathic route.

Honestly I think the future is in sublingual applications.

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#3 skinniest200

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Posted 08 February 2009 - 11:07 AM

When I hear 12 hours of an active agent, I think of substances like CX-516 or Noopept and wonder if we could extend their bioavailability/acting times.


Could you give some more info and references for Noopept's acting time in humans? I've seen some studies showing it's metabolism in rats and some saying it's metabolized differently for rats and humans, and I think one showing it had like 98% oral bioavailability in humans, but none mentioning it's duration of action.

#4 Pike

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Posted 08 February 2009 - 02:45 PM

The present study was conducted with the purpose to examine experimental and clinical pharmacokinetics of a new dipeptide drug noopept (N-phenylacetyl-L-prolyl&shy;glycine ethyl ester) possessing nootropic, anxiolytic and neuroprotective activities [1]. The experiments have been performed using high performance liquid chromatography technique. The results obtained from experimental pharmacokinetic studies showed noopept to be more resistant to the action of metabolizing enzyme systems as compared to naturally occurring neuropeptides. Noopept was determined in rat blood plasma independently of the route of administration for 25 min. Noopept was subjected to an intense biotransformation thus demonstrating rather low bioavailability. Pharmacokinetic investigation was carried out with two formulations for peroral usage: tablets (Technological Department of Zakusov State Institute of Pharmacology RAMS) and capsules (DVD Pharma Inc., USA). This study showed that capsules have no advantage over tablets neither in rate nor in extent of absorption. Pharmacokinetics studies in animals of different species and humans revealed significant interspecies differences: half-life time of noopept increased in the following order: rat < rabbit < human. These peculiarities could be attributed to different activity of biotransformation by enzymic systems. In view of obtained data, for the clinical trials the noopept dose of 10 mg was selected as the test dose, while the dose for course therapy was scheduled as 15 mg per day (5 mg x 3 times daily) throughout 28 days. The results of clinical pharmacokinetic investigation in patients with cognitive disorders of traumatic and vascular genesis showed that noopept was rapidly absorbed from the gastrointestinal tract, its concentration reached maximal level in the majority of patients 15 min after the test dose. Noopept was detected in patients' blood plasma throughout 45 min. Half elimination time was 22.05±14.37 min. In patients with vascular disorders this period was longer than that in subjects with craniocerebral trauma, and this should be taken into account in case of course therapy. Our previous experiments demonstrated that the metabolism of noopept has as a consequence the formation of cyclo-L-prolyl&shy;glycine - cPG [2]. This cyclic dipeptide, possessing pronounced antiamnestic activity, was determined in blood plasma of rats up to 5-6 hours after noopept administration. It possible to suppose that not only the parent molecule of noopept, but its metabolite also contribute to clinical effects of this systemically active dipeptide.

http://ex2.excerptam...tartRowDetail=1

I was mentioning noopept more along the lines that it's a model candidate for trandermal delivery systems because it's theraputic dosage range was effective at doses as low as .01mg/kg (and that was for patients with AD too!). Seeing as the only vendor we have for noopept is TLR, and it goes for like $95 for 500mg, I thought that thinking of new ways to increase its length of efficacy wouldn't be a bad idea (you can get up to about 80% absorption even with commercially available trandermal delivery systems).

#5 skinniest200

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Posted 08 February 2009 - 08:04 PM

Half elimination time was 22.05±14.37 min


That would be the half-life of noopept, but I'm not sure the actual drug half-life corresponds to the duration of effects in this case. It looks more like noopept is a pro-drug for cyclo-L-prolylglycine.

This cyclic dipeptide, possessing pronounced antiamnestic activity, was determined in blood plasma of rats up to 5-6 hours after noopept administration. It possible to suppose that not only the parent molecule of noopept, but its metabolite also contribute to clinical effects of this systemically active dipeptide.


Eur J Drug Metab Pharmacokinet. 1997 Jul-Sep;22(3):245-52.
The major metabolite of dipeptide piracetam analogue GVS-111 in rat brain and its similarity to endogenous neuropeptide cyclo-L-prolylglycine.

Gudasheva TA, Boyko SS, Ostrovskaya RU, Voronina TA, Akparov VK, Trofimov SS, Rozantsev GG, Skoldinov AP, Zherdev VP, Seredenin SB.
Institute of Pharmacology, Russian Academy of Medical Science, Moscow, Russia.

The metabolism of a new piracetam analogue, the dipeptide cognitive enhancer N-phenylacetyl-L-prolylglycine ethyl ester (GVS-111) was studied in vivo. GVS-111 itself was not found in rat brain 1 h after 5 mg/kg i.p. administration up to limit of detection (LOD) under high performance liquid chromatography (HPLC) conditions. Three substances corresponding to the three possible GVS-111 metabolites, namely phenylacetic acid, prolylglycine and cyclo-prolylglycine, were found in experimental rat brain samples as well as in controls using HPLC, gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) methods. Only cyclo-prolylglycine concentration increased (2.5-fold) 1 h after GVS-111 administration. Cyclo-prolylglycine formation from GVS-111 in the presence of plasma and brain enzymes was shown in vitro. These data could be considered as evidence that GVS-111 is prodrug which converts in the body to cyclo-prolylglycine, and which is identical to the endogenous cyclopeptide that produces the nootropic activity.

PMID: 9358206 [PubMed - indexed for MEDLINE]


GVS-111 is another name for noopept. From these studies, and the fact that a drug that works for less than an hour would be rather useless and not worth persuing into clinical trials, I'm thinking the half-life of cyclo-L-prolylglycine would be closer to matching the actual duration of effects.

theraputic dosage range was effective at doses as low as .01mg/kg (and that was for patients with AD too!)


Would you have a link to that study? I think I've seen .1mg/kg listed in some studies, but they weren't even on humans.

I thought that thinking of new ways to increase its length of efficacy wouldn't be a bad idea (you can get up to about 80% absorption even with commercially available trandermal delivery systems).


You wouldn't actually be getting longer duration per amount used unless the ceiling for effects was reached well below the standard 5-10mg and the extra was being wasted. Even then it would probably be cheaper and easier to just make some more noopept than to mess with the transdermal route.

From http://translate.goo...l=e...l=en&sa=G

Sintez PBS-111 is not only easy because of the lack of chiral center in the glycine and low proline residue danger of racemization, but also inexpensive because low cost of starting compounds - proline, glycine, and phenylacetic acid, especially the last two.

So who know's how to cook? Let's mix us up a batch :p!

I have some noopept on order from TLR so we'll figure out the actual duration of action in a few days. I've only seen one experience report on the stuff and they said 10-15mg twice a day was effective, and I'm assuming they mean for all day effects. I'll post a link or copy if anybody's interested.

#6 Mikael Llerena

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Posted 01 November 2011 - 05:52 PM

Speaking of sublingual methods of transporting these substances, has anyone on here had experiences with taking any of the racetams sublingually?

#7 Mikael Llerena

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Posted 01 November 2011 - 06:59 PM

Sorry about the above post. Looked it up. Apparently the oral bioavailability of piracetam is nearly 100 percent so there doesn't seem to be a need (for anyone else who was wondering)

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#8 Mikael Llerena

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Posted 01 November 2011 - 07:01 PM

Sorry about the above post. Looked it up. Apparently the oral bioavailability of piracetam is nearly 100 percent so there doesn't seem to be a need (for anyone else who was wondering)




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