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Devising our own method for slow release... (Read 11884 times)
comedydood
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Devising our own method for slow release...
07/04/11 at 07:20:09
 
Okay, so in my opinion, the reason why it takes us 50mg of melanotan-1 to get results, whereas the implant is only 16mg, is due to one thing: stable blood levels. If you inject 1 or 2 times per day, the Melanotan is in your system for 1-2 hours each time... that's it. Whereas, the implant, while a much lower dose, is a stable release over 5 days. So the receptors are slowly and constantly being stimulated. Hence the great results from the implant compared to daily injections.
 
So, how do we attain slow release of this peptide?  
 
1. Modified delivery is a possibility. There are certain slow-release gel formulations that are used for steroid injections. If we could procure some of these gels, add Melanotan to them, and inject... we could make one injection dissolve over a few days, rather than all at once.  
 
Unfortunately, I'm not sure what these gels are made of, nor where to procure them. I think most are patented, and most come already prepared with the medication in them.
 
2. Different injection site. I was reading about subcutaneous injections and B-12 shots. Apparently, injections into most sites yielded quick results the same day, whereas B-12 shots into the buttocks took 3 days to fully absorb.  The guy even advocated injection just below the skin on the buttocks, to maximize the time it would take to absorb.
 
I'm going to try switching to injections on the butt. I think this could be the easiest way to slow absorption and get better results.
 
Anyone have any additional ideas?
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paradiso
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Re: Devising our own method for slow release...
Reply #1 - 07/30/11 at 14:24:59
 
Quote from comedydood on 07/04/11 at 07:20:09:
Okay, so in my opinion, the reason why it takes us 50mg of melanotan-1 to get results, whereas the implant is only 16mg, is due to one thing: stable blood levels. If you inject 1 or 2 times per day, the Melanotan is in your system for 1-2 hours each time... that's it. Whereas, the implant, while a much lower dose, is a stable release over 5 days. So the receptors are slowly and constantly being stimulated. Hence the great results from the implant compared to daily injections.

So, how do we attain slow release of this peptide?

1. Modified delivery is a possibility. There are certain slow-release gel formulations that are used for steroid injections. If we could procure some of these gels, add Melanotan to them, and inject... we could make one injection dissolve over a few days, rather than all at once.

Unfortunately, I'm not sure what these gels are made of, nor where to procure them. I think most are patented, and most come already prepared with the medication in them.

2. Different injection site. I was reading about subcutaneous injections and B-12 shots. Apparently, injections into most sites yielded quick results the same day, whereas B-12 shots into the buttocks took 3 days to fully absorb.  The guy even advocated injection just below the skin on the buttocks, to maximize the time it would take to absorb.

I'm going to try switching to injections on the butt. I think this could be the easiest way to slow absorption and get better results.

Anyone have any additional ideas?

 
B12 injections are actually given intramuscularly, I don't think injecting subcut over the buttocks will make any difference.
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darkhorse
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Re: Devising our own method for slow release...
Reply #2 - 07/31/11 at 09:36:01
 
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paradiso
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Re: Devising our own method for slow release...
Reply #3 - 07/31/11 at 13:26:21
 
Well there you go, can be done both ways.
 
The ones I give are always intramuscular, as is the recommendation in Australia.
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Re: Devising our own method for slow release...
Reply #4 - 08/13/11 at 12:42:48
 
I love B12.
One of the best supps i have ever used.
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Re: Devising our own method for slow release...
Reply #5 - 08/13/11 at 21:41:25
 
intersesting i might try this, it may give a better outcome because of a slower absorbion rate, although it sounds like a pain in the ass!  (sorry  Smiley)
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RIURAO
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Re: Devising our own method for slow release...
Reply #6 - 08/31/11 at 14:05:26
 
There should be any Gel that could release the product slowly,  
Only with a 24 hours delivery would be enought !!!  
I am asking to medical personal but no one knows how it could be possible, any suggestion ?
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sirler84
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Re: Devising our own method for slow release...
Reply #7 - 09/01/11 at 12:15:51
 
RIURAO, Scenesse just consists of a biodegradable polymer PLGA (a mixture of lactic acid and glycolic acid) and melanotan-1. U can control the release (or half life of PLGA) by using different percentage of glycolic or lactic acid in PLGA. Clinuvel only mixes the peptide with the PLGA and presses it into a solid rice-grain like formulation.
 
If u mix PLGA with water it builds a gel. Then u would need to add the melanotan and then inject it. However, u need to be sure that no bacteria are present in ur mixture. So u need to incorporate an antibacterial agent.  
 
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darkhorse
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Re: Devising our own method for slow release...
Reply #8 - 09/01/11 at 19:24:58
 
How easy is it to obtain pharmaceutical grade PLGA?
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RIURAO
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Re: Devising our own method for slow release...
Reply #9 - 09/02/11 at 11:59:47
 
For me it is could be easy to get it , are you interested darkhorse ?
 
I probably will give it a try, any suggestion for the antibacterial agent ?  
Does it results in a very dense gel, or could it be injected  with with a insulin syringe?
I also guess that it has to be injected in fat parts ?
Could it be possible to manage the density of the finished product ?
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Scott Stevenson
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Re: Devising our own method for slow release...
Reply #10 - 09/02/11 at 12:13:44
 
Quote from RIURAO on 09/02/11 at 11:59:47:
For me it is could be easy to get it , are you interested darkhorse ?

I probably will give it a try, any suggestion for the antibacterial agent ?
Does it results in a very dense gel, or could it be injected  with with a insulin syringe?
I also guess that it has to be injected in fat parts ?
Could it be possible to manage the density of the finished product ?

 
Clinuvel's implants are irradiated to kill any living organisms in them. Irradiation for sterilization is probably going to be the most effective way to overcome active biological contamination issues.
 
-Scott
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sirler84
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Re: Devising our own method for slow release...
Reply #11 - 09/02/11 at 12:30:55
 
Quote from Scott Stevenson on 09/02/11 at 12:13:44:


Clinuvel's implants are irradiated to kill any living organisms in them. Irradiation for sterilization is probably going to be the most effective way to overcome biological contamination issues.

-Scott

 
Yes, u are right, Scott. Clinuvel produces its implant in an aseptic facility to ensure a bacteria free formulation. However, if u want to make this implant at home i strongly advise to add some antibacterial agents. The most effective way would be to incorporate an broad spectrum antibiotic, e.g. norfloxacin etc into ur mixture.  
 
Clinuvels uses an extrusion machine, that presses the mixture through a small hole resulting in long sausage-like product. Finally, it is cut into smaller pieces that give a small implant.
 
Extrusion machines are often used in meat preparations. I guess, u can find similar machines in the housewares section in ur supermarket.  
 
 
 
Literature:
 
1.  D. Chitkara et al., Biodegradable injectable in situ depot-forming drug delivery systems,
     Macromol. Biosci. 6(2006). pp. 977-990.  
2. M. van de Weert et al., Semisolid, Self-catalyzed Poly(Ortho Ester)s as Controlled-Release  
    Systemes: Protein Release and Protein Stability Issues, J. Pharm. Sci. 91(2002b). pp. 1065-
    1074.  
3. A. Hatefi, B. Amsden, Biodegradable injectable in situ forming drug delivery systems, J.  
   Control. Release 80(2002). pp. 9-28.  
4. S.J. de Jong et al., Physically crosslinked dextran hydrogels by stereocomplex formation of  
   lactic acid oligomers: degradation and protein release behavior, J. Control. Release  
   71(2001). pp. 261-275.  
5. C.B. Packhaeuser et al., In situ forming parenteral drug delivery systems: an overview, Eur.  
    J. Pharm. Biopharm. 58(2004). pp. 445-455.  
6. M. Luck et al., Plasma protein adsorption on biodegradable microspheres consisting of  
    poly(D,L-lactide-co-glycolide), poly(L-lactide) or ABA triblock copolymers containing  
    poly(oxyethylene). Influence of production method and polymer composition, Journal of  
    Controlled Release. 55(2-3), (1998). pp. 107-20.  
7. K.J. Brodbeck et al., Phase inversion dynamics of PLGA solutions related to drug delivery  
   Part II. The role of solution thermodynamics and bath-side mass transfer, J. Control.  
   Release 62(1999). pp. 333-344.  
8. H. Kranz, R. Bodmeier, A novel in situ forming drug delivery system for controlled  
    parenteral drug delivery, Int. J. Pharm. 332(2007). pp. 107-114.  
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RIURAO
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Re: Devising our own method for slow release...
Reply #12 - 09/02/11 at 15:49:13
 
I am a little bit confused about something, any help will be wellcome:
 
It is suppused that the first alpha-Msh experiment performed by humans in the forum prior to melanotan.org, wich i don´t actually remember the name but surely Scott does, well this alpha-Msh was extracted from pig´s  pituitary glands ?? , and it could be extracted by heating it, becouse alpha-msh is stable at high temperatures while any other components not ? .
 
If all related above is right, the easyest way to kill 95% of the bacterial at home would be at the microwave then?.
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RIURAO
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Re: Devising our own method for slow release...
Reply #13 - 09/02/11 at 15:56:54
 
I also understand that an anti bacterial component is needed for an implant wich will stay in your body at 36,5ºC during 14 days, it is perfect culture medium for any bacterial, but what if the gel or implant has a self life of let say 24-48 hours, probably an amount of 1 mg in daily injections ( Gel) could be enought and mimic the scen3sse implant as close as possible, we could have a constant release during 24 hours, aprox.
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darkhorse
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Re: Devising our own method for slow release...
Reply #14 - 09/07/11 at 17:36:45
 
Why would you need a different anti-bacterial agent? You could simply mix the melanotan-1 with bacteriostatic water, like usual, then add some PLGA to the mix to form a sustained release Gel. The only problem is getting hold of pharmaceutical grade PLGA. So who can do that?
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RIURAO
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Re: Devising our own method for slow release...
Reply #15 - 09/07/11 at 17:59:56
 
I can.
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Scott Stevenson
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Re: Devising our own method for slow release...
Reply #16 - 09/07/11 at 19:17:12
 
If you folks make this happen (I see it being very much in reach) please ensure that the implant(s) are irradiated to kill off any potential biologically active contamination agents (viruses, bacteria) prior to administration.
 
-Scott
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darkhorse
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Re: Devising our own method for slow release...
Reply #17 - 09/08/11 at 19:26:35
 
Maybe I'm misunderstanding here. This method would not result in an 'implant'. It would be an injectable gel. The method will involve mixing melanotan-1 with bacteriostatic water (as usual). Next adding bacteriostatic water to PLGA and then adding the two solutions together to 'thicken up' the mixture an a single, injectable gel.  
 
Important questions: How is the PLGA packaged? Is it in a sterile container/vial? Is it a dry powder? Would it mix with bac water to form a solution. And finallly, would said solution pull into a syringe when mixed with bacteriostatic water?
 
If the answer is yes to all of the above then I see no reason why this could not be acheived.
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Re: Devising our own method for slow release...
Reply #18 - 09/08/11 at 22:55:55
 
I would strongly advise against trying this..
 
For non-professionals in a non-lab setting, there's simply too much guesswork and too much that could go wrong. I might have misinterpreted the implant talk as well, but even if your were able to produce one you cannot insert it.
 
As mentioned, sterilisation is a big issue and the fact that you think it's ok to "kill 95% of the bacteria at home in the microwave" is quite alarming.
 
Sorry to rain on your parade, but again I would not recommend this.
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comedydood
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Re: Devising our own method for slow release...
Reply #19 - 09/13/11 at 19:49:04
 
This company produces pharmaceutical grade PLGA: http://www.wako-chem.co.jp/specialty/plga/index.htm
 
I'm interested in trying this. RIURAO - where are you with this? Contact me via PM and we can talk about specifics.
 
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