Rapamycin enteric coating vs powder bioavailability

I’m an idiot. I didn’t think about that. I also don’t know if it’s even possible to purchase Acid Armor capsules. I haven’t found a way to do it yet. It’s possible to purchase several supplements in Acid Armor capsules, but may not be possible to purchase the empty capsules.

“Anything you’ve been dreaming of, but I just won’t do that.”

It’s Joseph’s fault for suggesting Acid Armor :laughing:

Yes it is…

After a brief Google search I found the pamflet of an oral Rapamune solution for organ transplant patients. The active ingredients of the drink are Sirolimus, Ethanol, Propylene Glycol and soy oil.The dose is adjusted based on the blood levels of Sirolimus the solution achieves - and who knows, perhaps patients do indeed need to take higher doses to achieve the required blood levels of Rapa. But this would certainly indicate Rapamycin without enteric coated capsule is also bioavailable. The life of organ transplant patients is basically dependent on these Rapamune drinks after all. As was suggested, and as MAC also mentioned; we’d need to get a blood test done to check blood levels of Rapamycin. For US members this shouldn’t be an issue as LEF for example offers Rapamycin blood tests.
I’ve been searching high and low and haven’t found such an option here in the private medical sector, unfortunately.

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People have often talked about the increased AUC of rapa when taken with a fatty meal as compared to an empty stomach. However, in light of the stomach acid issue, it’s quite important to distinguish between rapamune taken with a meal and generic, non-enteric coated, taken with a meal. As far as I understand it, taking a medicine with a meal will cause it to spend more time in the stomach and the meal itself stimulates stomach acid, so it seems on net would expose the substance to substantially more stomach acid degradation. While this might not be a big issue for Rapamune, it could be quite a big issue for generic Sirolimus. This could tilt the tables in favor of taking generic Sirolimus on an empty stomach.

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Even though acid is secreted in response to food, the overall pH of the stomach goes up after a meal because the stomach acid is diluted.

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Thanks, I didn’t know that, but it makes a lot of sense. I suspect a pill will spend a longer time in the stomach though when food immediately precedes it. So the question is: which effect matters more - the longer time or the lower PH?

I’ve also been wondering: What causes an enteric-coated pill to actually dissolve or release its contents in the intestines? Is it just that its there for so much longer than the stomach, and this eventually causes dissolution even at PHs closer to neutral, or is it some other property of the environment of the intestines?

" Turns out, pretty much all drug absorption occurs in the small intestine. This is because:

  • Drugs spend longer in the small intestine
  • The small intestine has a larger surface area"

https://derangedphysiology.com/main/cicm-primary-exam/required-reading/pharmacokinetics/Chapter%201.3.4/drug-absorption-small-intestine

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The idea is to get the drug quickly out of the stomach. The drug biaxin gives considerable GI gastric side effects and this isn’t alleviated by food. However, it’s very well tolerated when taken immediately with 8 oz. of water. I do the same with rapamycin to increase its transit.

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The enteric capsules (if they work properly) are pH-dependent. They resist breaking down in low-pH (acidic) conditions (stomach) and then open up in a higher-pH setting (small intestine). Taking w/small amount of water and no food would keep the stomach pH low and allow for rapid transit to the small intestine.

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If Rapamycin tablets are enteric coated and that delays absorption so it’s not affected by stomach acid, why is the suggested time for a blood test to see peak amount 30 to 60 minutes after ingestion? The peak is supposed to be very sharp and drop off rapidly. Seems that wouldn’t be the case if it was slowly absorbed in the intestine.

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If you have not seen, review this paper;

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Empty Acid Armor capsules are apparently not available to consumers. So I purchased a product, Syntol AMD(R), manufactured by Arthur Andrew Medical, that comes in Acid Armor capsules. I took a capsule apart and emptied it, and put a smaller capsule of 3 mg pure rapamycin plus cellulose into the Acid Armor capsule. I got the rapamycin from a compounding pharmacy; my physician was willing to prescribe it for me. This rapamycin product contains no dyes, no titanium dioxide, etc. I had my blood drawn by LabCorp about 2 hrs and 45 mins after consuming it on an empty stomach and had it analyzed for rapamycin content for about $65 from Marek Health. The results: the lab report says < 0.5 ng/mL, which I take it means no measurable rapamycin.
Does anybody know if rapamycin would be absorbed if taken via suppository?

Google is your friend… FYI: and perhaps this would at least make your prostate live a long time :wink:

Preparation and quality evaluation of rapamycin suppository

Objective: To prepare rapamycin suppository, and to evaluate its quality. Methods: Rapamycin was used as active ingredient, polyethylene glycol 2000 and polyethylene glycol 4000 were used as main substrates. The suppositories were made using hot melt process method, and the drug content, weight difference, melting time, drug release with time were evaluated. Results: Polyethylene glycol suppository with rapamycin appeared white and translucent. Good hardness could be maintained at room temperature. The drug content, weight variation and melting time limit matched the requirements for the suppository. More than 75% of the loaded drug in the suppositories was released at about 25 min in the medium. Conclusion: This preparation of rapamycin polyethylene glycol (PEG) suppository can reach the quality requirements of Chinese pharmacopoeia, and may be developed as a new formulation of rapamycin.

https://xb.wmu.edu.cn/EN/abstract/abstract91.shtml

and a patent on a rapamycin suppository:

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Thanks for posting what Mr. Google found! I wonder if it would work to not use PEG 2000 or PEG 4000 and just insert the cellulose capsule containing the rapamycin.

You might also use Transcutol to increase absorption… its great for that; I use it for rapamycin skin cream and toothpaste. You want something like PEG or Transcutol to improve absorption.

Transcutol has a number of different chemical names/identifiers. Here is a list:

  • 2-(2-Ethoxyethoxy)ethanol: Ethoxydiglycol, 3,6-dioxa-1-octanol,
  • DEGEE, diethylene glycol monoethyl ether,
  • Carbitol,
  • Carbitol Cellosolve,
  • Transcutol,
  • Dioxitol,
  • Polysolv DE,
  • Dowanal DE

Chemical Identifier: CAS Number 111-90-0

Examples of Where you can order / buy Transcutol from in the USA:
LotionCrafters: Transcutol / Ethoxydiglycol
Laballey.com : Transcutol / Diethylene Glycol Monoethyl Ether

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I tried the Purecaps product and got the same result that I got with Acid Armor: a blood test result of < 0.5 ng/mL Sirolimus (rapamycin). However, at that time I was taking a turmeric product (Meriva, turmeric phytosome), which might have skewed the result. Elsewhere on this site, I believe RapAdmin posted a paper showing that turmeric in the system causes the liver to detoxify or break down everolimus, which is similar to rapamycin. But I would have taken the Meriva at least 24 hours prior to taking rapamycin in a Purecaps capsule. The half-life of Meriva in the blood is reported on some websites as 7.5 hours. So I would have taken the rapamycin about 3.2 half-lives after taking Meriva, so the Meriva concentrations should have been only 11% as much as the peak concentration.

https://www.amazon.com/s?k=enteric+capsules+large&crid=JTPSRUWEQGI5&sprefix=enteric+capsules+larg%2Caps%2C111&ref=nb_sb_noss

Can siroboon fit inside any of these?