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What number of are making their very own options from powder? – newbie


Are you getting the rapamycin powder analyzed for purity and and customary contaminants? @Mac wrote a superb submit on his course of for doing this, and his outcomes: Sirolimus Powder – third celebration evaluation

Additionally, FYI: I Do Not Advocate shopping for rapamycin powder from this Chinese language vendor (Zhejiang Multinpharma)




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No, I’m not getting the powder examined regardless of being conscious of the dangers.
Seems I purchased from the identical provider as MAC. Individuals have shared purity reviews of different compounds which were provided by them and so far as I can inform they’re pretty constant.
Simply had capsules delivered immediately – didn’t realise dimension 000 can be fairly that giant!



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Are you conscious how small an quantity of 100mg of purified rapamycin is?

See hooked up photograph;

100mg of purified rapamycin;



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I discovered a video about find out how to make liposomes, for folks wish to make their very own home made liposomal ingredient, the process appears to be like very straightforward.

The supplies and instruments required:

  • Lecithin powder
  • Lively elements (rapamycin, trehalose, ect.)
  • Excessive velocity blender (as @bizgoz talked about)
  • Ultrasonic cleaner

I plan to make liposomal trehalose, liposomal rapamycin cream, liposomal dasatinib face cream and liposomal RiverTown Hair Repigmentation formulation Reverse Grey Hair, Hair Repigmentation

Thanks for sharing this cool method.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6801558/



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Can verify Rapamycin is soluble in Peg400. I added 300mg to 30ml PEG 400. Heated in microwave 20 seconds and it dissolved and has been secure in answer for @ 10mg/ml.
Observe: I added .2ml benzyl alcohol to keep up sterility



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This will likely be an extended submit… however please learn in its entirety!

Biochemist right here, remember that there are a number of components you must think about when utilizing an injectable answer. It was my job for years to formulate injections for mice, and whereas I don’t suggest you homebrew medication, I’ve a sense you’re gonna do it in any case, so may as nicely give a information.

  1. First, think about equal dose. For example, think about an oral drug that’s just one% bioavailable. Meaning out of a hypothetical dose of 1 mg, you can be getting 0.01 mg circulating in your bloodstream. That is why oral doses are fairly excessive, as it’s principally to compensate for poor absorption and efficient dose. Most often, an injected drug is 100% bioavailable. That is particularly so for a lipophilic drug similar to rapamycin and its analogues when suspended in a lipophilic provider similar to PEG 400 or oil. You bypass first-pass metabolism, or unmetabolized drug that merely passes via you in stool or urine. Due to this fact, it might be necessary to reference what a 6-7 mg dose of oral rapamycin interprets to in regard to bloodstream circulation, and goal to imitate that ballpark in your injected dose.

  2. Second, lipophilic injections are usually sustained doses. With an oral dose of a typical drug, peak ranges are reached normally inside a pair hours, after which peters off quickly. Rapamycin is exclusive in that its oral half life is already lengthy, about 3 days for elimination. An injected answer, whether it is intramuscular or subcutaneous, will possible final for much longer than that, and should attain an excellent larger peak as a result of elevated bioavailability.

  3. Injection automobile properties have an effect on launch profile. Choosing the injection automobile can delay the discharge profile of a drug. For example, a extremely lipophilic drug suspended in a barely lipophilic automobile may have a faster launch time than in a extremely lipophilic automobile. Rapamycin is very lipophilic, in order that’s already a given. Moreover, the viscosity may also have an effect on launch time, with the extra viscous answer being the extra sluggish to launch. The perfect instance of that is evaluating suspensions in MCT oil versus castor oil; castor oil prolongs the discharge of an injection significantly, nevertheless it additionally flows like glue.

  4. Blood ranges should be carefully monitored to be throughout the therapeutic window. That is a very powerful issue. The dose is the poison. Sometimes, blood ranges of a specific drug are carefully monitored in a affected person to make sure that circulating ranges don’t exceed a sure threshold, referred to as the therapeutic window. Going exterior that window can both imply ineffectiveness if you happen to dose too weakly, or severe hurt if you happen to dose too strongly. Happily, rapamycin blood testing is on the market! Normally we monitor blood ranges for a peak and trough stage, primarily based on the half life. So, if one had been to inject rapamycin, which has a half-life of about 3 days, I might hazard a guess that an IM peak can be reached someplace between 1-3 days after injection. So, I suppose one may take a blood check at 2 days after injection and one other proper earlier than the following injection for a trough stage to make sure you aren’t exceeding the secure baseline. Additionally remember that consecutive doses will accumulate increase your baseline over time till a steady-state is reached, so after 3-5 doses it might be good to do one other trough test.

Contemplating that rapamycin is most well-liked to be dosed and eradicated rapidly, I wouldn’t suggest injections in any respect. However! This can be a discussion board of mad scientists, so if you happen to’re gonna do it, simply please think about these factors. The entire level of weekly dosing is that every day or fixed dosing provides you fairly detrimental uncomfortable side effects (we aren’t organ transplant sufferers, in any case).

So, if I had been to hypothetically do it (despite the fact that I don’t condone it), I might droop in MCT oil or comparable (viscosity ~27 mPa.s in comparison with PEG 400 between 90-110 mPa.s), lowball the dose at round 1 mg, and monitor the height and trough stage through blood check after 2 days of preliminary dose and proper earlier than the following dose. If the dose appears to be like too low, I might attempt to regulate the dose and do one other peak/trough check till it appears to be like good. Then, after a couple of month and a half, I might re-check the trough to see what the steady-state stage is, and cut back if obligatory.

EDIT: Apparently some madman did it already… see right here.
Granted, it’s nonetheless n=1, however apparently the man tolerated a 15 mg injection. Completely insane.

Thanks a lot for posting some good in depth info. @MAC has really been dosing this repeatedly for previous six months or so and appears to be doing fairly nicely. We don’t suggest it, however persons are attempting new issues and reporting their outcomes.

What are your opinions on utilizing DMSO as the primary reagent for the formulation?

That @MAC man is wild! I noticed his submit after I had replied. Very impressed by how thorough he’s about monitoring his therapy, although he does quite a lot of different issues I’ve issues about.

Concerning DMSO, it’s not a super automobile because of its cytotoxicity. Most pharmaceutical formulations solely use DMSO to assist in solubility, and usually round 10% v/v. He appears to be injecting it in 100% DMSO, and I’m shocked he’s tolerating it thus far.

Most have injection web site reactions from that a lot DMSO, and I imagine somebody additionally mentions that to him. What I think is that @MAC could have used degraded DMSO over time. 100% DMSO may be very light-sensitive, and degrades quickly. I have no idea if he shops his answer in an amber or opaque bottle, however certainly one of his photos reveals an everyday glass jar. The freeze/thaw cycles may need additionally contributed to degradation, and I imagine he additionally states he makes use of a “glass vial” of types. For a multi-dose container, this isn’t supreme as publicity to humidity/oxygen/contamination from the air can hasten the “spoilage” of the answer, which is why sealed vials with septa mats are used.

He mentions that he had such intense ache when he started injecting that he may barely stroll, which progressively diminished over time. That’s not regular, and certain as a result of near-pure DMSO he was injecting. He could have broken his injection web site tissues to the purpose the place he could have constructed up a “tolerance” solely as a result of he has change into much less delicate to the ache. The rapamycin may also be irritating him, however I’d think about altering his components.

Maybe he may check out a distinct formulation with out DMSO to see if it makes a distinction. I’d personally attempt to solubilize in MCT oil first, and solely add a most of 10% v/v DMSO if solubility is a matter. Sometimes, benzyl benzoate between 10-40% can also be added as a preservative and would assist stabilize rapamycin.

I’m additionally very involved as as to whether or not he’s utilizing aseptic/sterile method in his preparations. I get the impression he’s simply mixing it and injecting it… which is terrifying to me.

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