Improve Bioavailability of Rapamycin (2)

#78

Hi All, I may be unique with my rapa absorption problem, I can’t swallow pills. All pills need to be blended into a slurry in a bullet grinder. I blood test via the lifeextension.com via labcorp sirolimus blood test ($99). You have to call their support number then ask for blood testing, support and eventually they will find who can sell this test. Its not on their website.

First of all; any have a good guess at what blood concentration I should be shooting for? 20ng/ml? 40ng/ml? The blood test states a range of 3-20ng/ml. I’ve seen absorbtion studies in this threa mentioning 40 and up to 70ng/ml…

My highest test results so far is 7.2 ng/ml and this was after this dosing protocol;

  • each day, 2 days every 2 weeks; In the morning; (attempts to increase aborbtion) 1T dried GF powder, 1T GF extract, peperine 10mg, 2T olive oil. I’ve already been filled in re the value of frozen GF concentrate vs my attempts to be simplier with dried GF powders.

Then 2 hrs later, giving time for CYP34A to be suppressed.

2t olive oil + 10mg via 1mg indian sourced sirolimus pills, tossed in 6mg via diluted down pure chinese powder (just for good measure). IE kitchen sink approach.

One the 3rd day I had blood draw for the sirolimus blood test and got 7.2.

== Improvements I’ll add gleened from above (thanks all)

  • During the pre-dose dose I’ll add additional CYP3A4 suppressors:

  • 1/2 can of frozen GF concentrate. Yes giving in and just have this product flowing through the freezer.

  • 1g berberine

  • 1g fiesitin

  • 1g sodiumm caprate (an MCT/coconut oill derivative)

Then reblood test.

=== General comment to other DIY rapa experimentors.

Given my close inspection of my indian 1mg pills, I found them to be fragile, easily broken and crushed. I wonder if they are at all enteric? Disolve in the stomach much likee my grinding and drinking a slurry?

You guys may not be achieving the blood levels that are beneficial?? Given the risk to true benefit and variability of the sirolimus / rapa drug pill / supply chain. Do you really know what blood levels you are achieving?

Just a comment; I would suggest that everyone doing this protocol should do at least a few blood tests to verify for their (your) stomach, pills, protocol you are really getting the benefit you want.

I agree that canker sores and other symptoms are useful.

Rambling a bit; My opinion re canker sores to me says; your immune system is marginal to begin with and the initial function of rapa to (in theory temporarily knock down your immune system) causes the always present canker sore (like shingles like many lurking bugs). My question is why is your immune system marginal in the first place? Just questioning.

Not sure if my having no symptoms post rapa means much good or bad. Just plodding along, collecting data.

Not detailed; I do a 2day dosing of the classic D+Q+F (and kitchen sink add ons) scenolitic protocol on the alternating weeks.

Best to all, curt

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#79

You test on day 3? Max is 2 hours after you swallow the pills. It goes down pretty quick.

That could be why you get low numbers.

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#80

What do you think about putting the Sirolimus pills inside these? https://amzn.to/3qJ8deK

The generic Sirolimus I get from Amazon pharmacy are tiny and I’m now worried about stomach acid.

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#81

It seems like the thing to do, but I would say if you don’t test, you won’t know.

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#82

Has anyone done a test with the generic Zydus pills to see if there are any problems?

#83

Apparently this Rapamycin he’s referring to was Zydus:

Also for what it’s worth ive been taking 6mg of Zydus for the past few weeks (I just started Rapamycin) and have had a mouth ulcer and high postprandial glucose after my Rapa dose for 24-48 hrs (with higher carb foods). These seem to be common side effects of Rapamycin, so that’s something.

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#84

Yes, I got 3 canker sores after I took my 2 mg dose of Zydus + GFJ yesterday. Makes me wonder about my immune system. Although I have been exposed to COVID frequently and have never gotten it. So I am not sure how good my immune system is.

Although there is no euphoric or nauseous feeling like I had last week. That was probably due to dehydration due to cycling in very hot weather.

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#85

It has been suggested that such capsules are not truly enteric coated. It appears the capsules are not ‘airtight’ where the two halves meet and liquid will still be able to get in and out of the capsule. (I believe it was Mac who suggested this, and he may very well be right about that).

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#86

@curt504
Thanks a lot for your comments above. Could you please report your next test when using the Grapefruit juice and also the exact brand of your generic rapamycin.
Many thanks.

#87

Not all statins. Crestor is fine with grapefruit

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#88

I really don’t worry too much about the bioavailability of the major producers of generic rapamycin (e.g. Zydus, Dr. Reddy’s and Biocon) because these drugs are used for organ transplant patients. These drugs are used by hundreds of thousands, (if not millions) of organ transplant patients. If there was a significant bioavailability issue with these drugs, so much so that they were not doing their intended job, the negative press would be huge and the number of dying patients would be obvious to anyone.

The bioavailability issues that we’ve seen in the compounded pharmacy capsules are a tiny slice of the market, and thats why its been noticed and reported quite a bit around here and others. Just avoid the compounded pharmacy capsules and you’ll likely be fine.

Just my opinion on this issue.

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#89

Just saw this today, confirming what I said earlier - that generic and brand name rapamycin / sirolimus are both good from a bioavailability standpoint:

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#90

Berberine also blocks CaKG according to the CEO of Rejuvant. Rejuvant is a time release CaKG that their web page claims reverses biological age by 8 years…

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#91

That’s good to know because I take generic Crestor 3 days a week. I have been taking rapamycin with grapefruit juice on one of my off days from Crestor.

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#92

Biocon works, I feel it when I workout. It takes about a week after I take it to get back to normal strength. IIt seems to hit hardest mid week (I take it on saturdays) That’s one of the reasons I take it semi-monthly. I like a week off to feel normal

1 Like
#93

@RapAdmin
I really don’t worry too much about the bioavailability of the major producers of generic rapamycin (e.g. Zydus, Dr. Reddy’s and Biocon) because these drugs are used for organ transplant patients. These drugs are used by hundreds of thousands, (if not millions) of organ transplant patients. If there was a significant bioavailability issue with these drugs, so much so that they were not doing their intended job, the negative press would be huge and the number of dying patients would be obvious to anyone.

Have you tested yourself? I’ve asked in a Lab here in Perth, Australia, and I need a prescription for the test. So it is going to take me a while till I find a doctor to give a prescription. Therefore, my tests will have to wait.

But what about you? You expressed interest on testing yourself, it would be nice if you could test Pfizer, and some generics, with and without Grapefruit, with and without Fat. I know I’m asking a lot, but even just a piece of comparison between two cases would be great. For example just the plane Pfizer vs Generic.

Many thanks.

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#94

I agree with his point about the major producers of generic rapamycin tablets. It seems a waste to personally pay out of pocket for a bunch of personal “n of 1” bioavailability comparison lab tests given that so many organ transplant patients take these generics and have their trough levels tested without apparent problems.

I think most of us are interested in the serum rapamycin tests because we’d want to know peak levels with/without grapefruit juice and at any particular dose and we want to look at trough levels to make sure we have an effective washout period between doses.

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#95

In what way / direction does it work?

#96

I did a little test today where I filled the delayed release capsule with oil and placed it in vinegar. I swirled the glass once every 15 minutes. It took 3:15 until the capsule started to break down to the point where any oil was released. @MAC you might be interested as well.

I’m considering loading up 6mg of my Glenmark Sirolimus tabs into the capsule. I do wonder how they prevent it from breaking down otherwise. I wish it were easier to get a serum level!

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#97

I go to the same fitness classes 4x week. Days 2-5 after taking my semi monthly dose I can feel a lot more struggle doing my fitness routine. My stamina and strength is negatively impacted. I feel weaker and run down.

About 7 days after my dose I’m back to feeling my normal strength and energy levels along with no body aches or pains.

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