Comment · Fri, June 10, 2016 · Ceretropic & Nootropics Depot
Sublingual noopept with tablets?
Original post in this thread
FaxFromKorea · 0 points
I received a free set of Noopept tablets from Smartnootropics, to which I've been taking 10-20mg doses of orally, with no effects.
I've been reading a bit and read that sublingual noopept is absorbed better than oral noopept. I tried putting the capsule sublingually, however the capsule clumped up and the taste of the capsule itself was disgusting.
Has anyone got any suggestions to take noopept tablets sublingually?
What they were answering
112358134 · 3 points
:/ This is what happens when people decide to ignore the valid information and instead read many times anecdotal references of those who for well-known reasons decided to believe that noopept does not have a sufficient bioavailability and therefore should either be snorted or put under the tongue.
u/MisterYouAreSoDumb · Ceretropic & Nootropics Depot
I get that you really just want to defer to Russians companies without evidence, but to say there is no evidence that the oral bioavailability of Noopept is low, is ridiculous. The Russian studies themselves are where I first found that data. Noopept is a dipeptide with a phenylacetyl group. It will be broken down by enzymes in the GI tract. That is a fact.
I'll copy what I wrote someone else about it over 2 years ago:
A lot of people quote a Russian study as saying that it's oral bioavailability is 97%, but that is incorrect. The study showing that is in Russian and was done on rats and chinchilla rabbits. Their finding was actually 98.67% bioaccessibility of oral tablets in comparison to the oral parent compound via a feeding tube. The actual finding of peroral in comparison to IV was 9.33%. That means that only roughly 10% of the oral dose makes it to your bloodstream. Those quoting the 97% number have not read the actual study. I'll link the full text for you below.
The absolute bioaccessibility was on the average AUC p.o./ AUC i.v. = 9.33 +-1.30%, which is evidence of a pronounced effect of the “first passage” via the gastrointestinal tract and the liver. In comparison with rats, rabbits are characterized by slower absorption of the parent substance, which is manifested by an almost twofold increase in MRT and by decrease in the C max AUC 0 ratio in the latter case.
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Peptides are easily ripped apart by digestive enzymes, and noopept is not immune to these effects. It's only saving grace is that it is a very small dipeptide. This means that it has a higher likelihood of being absorbed before being ripped apart than larger peptides that are almost 0% bioavailable. The longer it takes to get to your bloodstream, the more it will be broken apart. It will be ripped into it's 3 parts, the glycine, proline, and phenylacetyl esters. If this happens peripherally, the molecules are useless to the brain. They must pass the BBB before being metabolized. This is much less likely if you allow it to undergo first pass metabolism. The only thing noopept has going for it is size, which as you can see from the study doesn't help much.
Noopept is active orally, but much less than sublingual. Even the Russian pharmaceutical instructions state that it should be taken sublingually. The study I linked used 10mg/kg IV, and 50mg/kg peroral, and still the oral was unable to get close to the Cmax of IV.
Thus, the results of our investigation showed that the absolute (peroral) bioaccessibility of noopept is 7.09% in rats and 9.33% +-1.30% in rabbits.
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Here is another Russian study on the matter:
Similar plasma level of GVS- 111 was observed after 5 mg/kg parenteral and 50 mg/kg oral administration.
So it took 50mg/kg peroral to reach the plasma concentration of 5mg/kg paenteral. A very substantial difference.
Considerable differences related to the administration route were revealed in GVS-111 metabolism. After parenteral administration, apart from the unchanged GVS-111 molecule, the plasma contained 2 phenylacetyl metabolites phenylacetylproline and phenylacetic acid, which were not detected after oral administration. At the same time, plasma chromatograms after oral administration showed a peak which was eluted before GVS-111 and differed from the known phenylacetyl-derivatives by the elution time. It could be either hydroxylated or methylated GVS-111 metabolite. This difference in GVS-111 metabolism in different administration routes seems to be due to the fact that parenterally administered peptide is hydrolyzed preferentially by plasma peptidases, while metabolic transformations after oral administration occur during its first passage through the liver.
Given the evidence, noopept should be taken sublingually or nasally to be most effective. There is scientific evidence for the first pass metabolism of Noopept after oral administration causing it to have low bioavailability, and changing its effects. This is not just anecdotal reviews (which are extensive, by the way). This is scientific data that backs up the countless anecdotes out there.