Comment · Tue, August 23, 2022 · ND Owner
why isn't ecdysterone complexed with cyclodextrin?
Original post in this thread
samuelx23 · 10 points
So the literature seems to indicate that ecdysterone has low water solubility and thus low abortion orally. When conplexed with beta cyclodextrin it seems to have much high solubility and theoretically higher bioavailability. Because of this I wonder why ND doesn't sell a complexed version? Although I know guerilla minds turkesterone is controversial there product is supposedly complexed this way. Anecdotally I found this to give massive benefit. Are you guys taking higher doses of 20E to account for this? Am I missing something?
Poor bioavailability
https://www.google.com/url?sa=t&source=web&rct=j&url=https://www.mdpi.com/2227-9059/9/5/492/pdf&ved=2ahUKEwjlusOj2tr5AhXrk4kEHcn6BFMQFnoECAcQAQ&usg=AOvVaw1UaFF8k25MHizLT2OvG1yA
Compmexex cyclodextrin and 20E has better water solubility
https://pubmed.ncbi.nlm.nih.gov/30458190/
In vitro simulation of stomach environment increased absorption
https://pubmed.ncbi.nlm.nih.gov/35311602/
What they were answering
samuelx23 · 2 points
yeah, I combed through his comments and couldn't find anything. u/misteryouaresodumb any chance you could elucidate this for me?
u/MisterYouAreSoDumb · ND Owner
Beta-ecdysterone is currently in multiple human trials, and none of those trials are using cyclodextrins. Moreover, those studies talking about cyclodextrin complexes make no sense. Beta-ecdysterone's LogP is right smack dab in the ideal range for bioavailability. One of the studies above claims it is poorly water soluble, and that you can only dissolve 0.084mg/ml in water, but that's horseshit. Just dump some of our powder in water and you will immediately see that's BS. Even ADME software shows it is water soluble, and in the ideal range for oral bioavailability. I really have no fucking clue what those Kazakh and and Chinese studies are on about. The French study you linked is actually from Biophytis, and they are running human trials right now at 175mg and 350mg 2X per day of just 97% pure beta-ecdysterone. They study you linked even talks about it.
>Biophytis has recently undertaken the first in-human, randomized, double-blind, single-centre study to determine the safety of 20E and its major metabolites in healthy young (18–55 years) and elderly (>65 years) adult subjects [136,137]. The study comprised two parts: a single ascending dose component (SAD; 16 subjects) and a multiple ascending dose component (MAD; 30 subjects). **20E showed a good safety and pharmacokinetic
profile**, which allowed the doses for a Phase 2 Sarcopenia clinical trial to be defined. Pharmacokinetics in subjects treated with increasing amounts of orally delivered 20E (Table 4) showed that the level found in the plasma is dose-related and also apparently saturable. The kinetics of plasma 20E was similar between young and older subjects (Figure 9).
Where it has been investigated, the effects are brought about by low µM concentrations of 20E, but to achieve maintained concentrations of this level in the plasma it is necessary that 20E should be supplied orally in large amounts (100–1000 mg) at least twice a day, because the bioavailability of 20E is poor and the half-life in the plasma is short.
Pharmaceutical companies often have a different definition of what constitutes a large dose compared to what we are used to in supplements. You can see they overcome the bioavailability issues by taking a dose in the 100mg to 1g range. Our capsules are 250mg of beta-ecdysterone each. That's solidly in the range needed. Moreover, other studies have used lower doses and found positive effects. It's in the table in the study.
Improvement in kidney function from 15mg/day. Improvement in libido in 75% of patients at 7.5-10mg/day. Improved sperm quality from 5mg 2X and 3X per day. Reduction in body fat and improvement in lipid profile from 50mg twice a day. Improvement in metabolic syndrome and as a proposed alternative for hormone replacement therapy at 100mg or 200mg per day. So you can see it works perfectly fine orally. Also, the Chinese study you linked shows that the cyclodextrin complex was only 2.97 times more bioavailable. That sounds nice on the surface, but you have to take double the dose because of the 1:1 molar ratio. This means you would need to use pure beta-ecdysterone, which is more expensive, then make that into a cyclodextrin complex, adding even more cost. Then you need to take double the dose to get the same amount you were shooting for. There is a reason the pharmaceutical company decided to just go with a higher dose of normal beta-ecdysterone.
Also, everyone on the market is just buying shit from China claiming to be a cyclodextrin complex. However, these Chinese suppliers are usually just mixing maltodextrin into it in a 1:1 ratio and calling them cyclodextrin complexes. Have you seen any of the brands claiming to be selling a beta-ecdysterone cyclodextrin complex showing NMR, SEM, and XRD data proving it? I mean, just ask them for the lab data and be prepared to laugh. Deep down you already know what the answers will be. Nobody out there is testing shit. They are just selling BS from Chinese suppliers that are telling people what they want to hear. Could a properly made beta-ecdysterone cyclodextrin complex be a bit more bioavailable than normal beta-ecdysterone? Yeah, possibly. Would it justify the cost, and does it actually exist on the market right now? Doubtful.