Based on this{30% improvement in bioavailability] I am serious considering using Pfizer’s Rapamune (sirolimus).
It appears to be well worth the additional cost.
Why not just take 30% more of the generic medications - much less expensive.
From the pricing numbers I’ve seen the brand name sirolimus (Pfizer rapamune) is typically 300% to 500% higher in price. So it doesn’t seem reasonable to pay 300% to 500% to get 30% improvement in bioavailability.
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One could also buy empty enteric-coated capsules and put the Tailor Made capsules inside (I also have the TM 3mg ones). Amazon sells the empty capsules. I wonder if there would be an advantage in doing this?
Elan is a very successful drug delivery technology company that is well known in biotech / pharma circles.
For the past decade or so, EDT has been working on, and perfecting, its NanoCrystal technology, which essentially is a milling technique that breaks down drug crystal sizes to less than 2,000 nanometers. This seemingly small, simple solution addresses a few major problems facing the pharmaceutical industry today. The first is poor solubility of drugs. Even the most successful drugs often have trouble dissolving, so drugmakers tack on compounds to make it more soluble.
Unfortunately, patients read about the side-effects of those soluble compounds in the often-mocked, ubiquitous “fine print” that drug companies are forced to include in their commercials. Nano-sizing the drug compound increase its surface area, making it much more soluble. This increases the likelihood of patient compliance, not to mention an inability of generic drugmakers to copy the complete drug, since the compound can be reproduced once it’s off patent, but not Elan’s proprietary NanoCrystal technology.
https://www.crunchbase.com/organization/elan-pharmaceuticals
I think this is probably an over-simplified approach to solving the bioavailability issue. Elan pharmaceuticals, which developed and owns the patented nanocrystal technology that is used in the Pfizer version of sirolimus (rapamune). I suspect that to get patents and be used in leading products, the nanocrystal technology is probably a lot better than just using enteric-coating capsules.
Probably easier, and cheaper just to take the rapamycin with sardines or other higher fat meal, or with a little grapefruit juice (if you have no complicating factors).
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Take note, the enteric coated capsules on amazon (1st item: Amazon.com : enteric coated capsules) indicate they don’t release until 120 mins after ingestion. So this would technically complicate any blood Sirolimus peak capture testing immediately after dosing.
Typically the peak Cmax is approx 1-2 hrs after ingestion of “Rapamycin”. I italicized Rapamycin to note that I believe branded/generic pharma type grade rapamycin tablets have “some” type of coating to help improve bioavailability (and perhaps nano tech inside?), likely delaying release until after stomach passage (this is me hypothesizing, I haven’t confirmed this). And/or the coating is for shelf stability.
If you don’t care about cmax, then perhaps Sirolimus blood trough is sufficient for your dosing titrating self-experimentation. Regardless, just add this variable to your experimentation.
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I bought some acid resistant capsules that are designed to break down in the more alkaline environment of the small intestine. I will insert the smaller plain capsules into the larger. I think that should solve the problem.
FWIW…
You will have two capsules to
dissolve as they are travelling through the intestinial track. Re pack content to the new capsules.
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Given the relatively inexpensive blood test for serum rapamycin levels, it should be more worthwhile to check your peak level after dosing, rather than experimenting with putting one capsule into an enteric-coating and hoping for better absorption (but possibly resulting in decreased absorption).
Peak levels occur on average a little over 2.5 hours (ballpark estimate) after dosing, according to this chart for sirolimus tablets:
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I’m on standard medicare & have supplemental insurance w a major carrier I won’t name for now. Talking to the rep for this carrier, he told me they covered sirolimus regardless of purpose as long as I had a prescription. Cost=$78 for 30 table at Walgreens. Wondering if there are major downsides to using such insurance here. My worry is that the insurance will at some later time say it was a mistake and that I owe them full cost.
There is also the issue of it being on your permanent medical record and someone in an insurance company in the future may misinterpret it to mean you have had cancer or organ transplant…
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So you’re thinking I shouldn’t use the insurance?
This shouldn’t be an issue for medical insurance, since they aren’t allowed to discriminate against people with pre-existing conditions. Maybe life insurance, though?
I don’t know your situation well enough to comment on that. Just trying to help you identify pros and cons of each approach.
I pay about $40 per month for the rapamycin i use. Even if i could get it covered by insurance i don’t think it would be worth it for me.
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Can I ask where you get it?
I just order from one of the online stores on our list. I try different store each order.
Here is some more breakdown kinetics data on the enteric coated capsules from this vendor. Appears they start breaking down right away, but they don’t fully dissolve (is this how we should interpret this graph, the full wall breakthrough and release of contents?) does not happen until 120 mins.
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I called them today to ask about their 6mg rapa caps. They said they are not enteric coated. 
Easy enough to open the caps and dump them into some inexpensive enteric coated caps (only 9 bucks for 100 enteric gel caps on amazon, for instance). That’s what I’m going to do with my dog’s rapamycin capsules.
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Ordered and paid for 100 1mg tablets, 10 stripes
Rapacam, Sirolimus on 24th May 2022.
RL PHARMA & NIBA Healthcare.
Cost : $78
Shopping : $36
Total: $114.
Paid vía wise.com
Arrived in London this morning 1st June 2022.
8 days un total!
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Sirolimus is a Tier 2 drug on my Medicare Advantage Formulary. I pay $3 for 30 tables of 2mg Sirolimus. I use the Costco Web Pharmacy. Costco sources the Sirolimus from Dr. Reddy, an Indian company. My insurance is
Wellcare No Premium Best (HMO)
(H5087-016-000)
Policy # CA065
RXBIN: 004336
RXPCN: MEDDADV
RXGRP: 788257
I asked my PCP for a prescription.
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