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Comment · Wed, October 20, 2021 · ND Owner

Reddit AMA | In-House Lab Edition

Original post in this thread

NootropicsDepotGuru · 77 points

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We are very excited to announce that Nootropics Depot will be conducting its first-ever Reddit AMA (Ask Me Anything), which is a semi-live Q&A session, about our In-House Analytical Laboratory and we would love for you to join us! See below for full details and get your question(s) ready. We hope to see you there!

WHEN

STARTS: October 20th | 9am AZ MST

ENDS: October 22nd | 9am AZ M…

What they were answering

JohnTorque · 1 points

What is the product that took the most effort from your team to develop? Why?

u/MisterYouAreSoDumb · ND Owner

The second one I would say has been difficult is adrafinil. This is one we have been selling since 2013. However, it's a very complex one for a number of reasons. Going all the way back to the Ceretropic days, some batches we would get in would be dark pink/orange. Other batches we would get in would be white or very light pink. We were stumped as to what the color difference were, as all the batches were matching each other on FTIR, NMR, and assay. We thought maybe it was iron content, so we tested tons of batches from over the years to see if we could correlate the color to the iron content. Nope, no correlation. There was no correlation to anything we could see on the analytical techniques we were using. I poured through the research that I could find, but nothing was conclusive. I did find some interesting references to crystal structures and polymorphs in some Cephalon papers. However, a lot of that info is kept as trade secrets in the pharma world, so I only had speculation. We worked with some labs to synthesize adrafinil different ways, and we discovered that the color differences were arising from the recrystallization step. If you crystallized it one way it came out dark pink. If you crystallized it another way it came out white. They were the same chemically. They just differed by the shape/size of the crystal structure. However, we were still limited in what the labs would share with us. Most contract labs don't want to give away too many secrets, so they keep things tight to the chest. Then something happened that nobody expected: China banned adrafinil.

After China announced the ban on adrafinil, we had to scramble to figure out what we were going to do. First steps were securing as much as we could before the ban went into effect. This is easier said than done, as labs only wanted to do the work if we agreed to buy the entire batch. These were half a million dollar batches each time, but we had to do it. Then we had to figure out what our long-term solution was. We spoke to suppliers and labs all over the world, from India to Germany. Nobody wanted to take the project on, and the ones that did wanted 5X the normal price, which would not be economically workable. So we decide to jump into building our own synthesis lab in the EU. This has turned into one of the most expensive and difficult undertakings we have done for a product. We had to go through the synthetic pathways to pick the most efficient syntheses, then we had to ensure we could get the precursors. Then we had to do lab scale batches. This took a long time to work through all the problems and get good yields, but also get a pure final product. During that process we connected all the dots with the polymorph/crystal structure thing, so now we fully understand how the color can shift based on the crystal structure created during the recrystallization process, and we can control that process to make it exactly how we want it to be. Then we had to scale the batch sizes up. This is what has taken the most time.

When you do lab scale batches of a synthesis, things can act very differently than when you scale them up to production size. You have larger reaction vessels that can cause weird effects you didn't see in the lab scale. You need larger vacuum ovens and drying processes that affect the final product. You also have reactions with the materials use for the vessels and drying containers. Scaling adrafinil synths up to production scale has been a massive pain in the ass, and has cost roughly 3 times what I expected it would. We are getting very close to having full capacity batches running through the large production line, so that is exciting. We have learned a lot, and are going to be able to control every step in the process in more detail than anyone else in the world, which is pretty cool. However, this whole process is one reason I consider adrafinil one of the most difficult products to deal with in recent times.

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