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jstanziale
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The best tool available to make nasal and sublingual steroids are derivatives of beta cyclodextrins. The one that is most readily available is hydroxypropyl-beta cyclodextrin (HPBCD). (Note: Plain beta-cyclodextrin is of little use) In case you have not heard of these, cyclodextrins are cyclic oligosaccarides (sugars) that have a hydrophilic outer surface and a hydrophobic inner surface.(3) They can be thought of as a doughnut, with the center capable of having a steroid molecule stuck inside it. The hydrophilic outer surface makes the cyclodextrin soluble in water, and when it is combined with a steroid, it can make the poorly water soluble steroid soluble as well.(3) In addition to making steroids soluble, cyclodextrins have very other important properties that make them ideal for our purpose. Cyclodextrins are known to enhance steroid delivery through biological membranes.(3) The large CDs themselves are very bad at permeating biological membranes, but they deliver the steroid to the membrane, where it partitions into the membrane, leaving the CD on the outside of the membrane.(3) The conventional penetration enhancers like alcohols or polyethylene glycol act by disrupting the lipid layers of membranes.(3) That is a big source of irritation from the old formula, and this irritation can thus be avoided by the use of CD’s. Another advantage is, once administered, the steroid is rapidly absorbed. Nearly 95% of the steroid will be absorbed within 20 minutes. This also causes the need for multiple doses throughout the day.
It seems that hardly anyone out there knows how to complex a steroid with a cyclodextrin. One procedure I saw on a different company’s steroid column was laughable. It was pretty obvious that whoever wrote that procedure knew very little about cyclodextrins. It is really fairly easy to do. There are multiple ways to do it, but I will tell you three methods to try, depending on what resources you have available. In all instances, you need a ratio of 9g of HPBCD to 1g of steroid. Complexation occurs because the steroid is more energetically stable inside the CD than outside of it. It is an equilibrium process, but the equilibrium lies much more on the side of complexation.(3) Water is essential for complexation to occur. It is removed from the inner cavity to allow for the steroid to enter, but even normal room humidity is sufficient for complexation if the mix is given sufficient time.(4)
Method1
For the first method we will formulate it for a total of 2g of steroid.
Dissolve 18g of HPBCD in 80ml saline in a beaker on a stir plate. Once this is dissolved, slowly add the 2g of steroid over about 5 minutes. Let this stir overnight. Filter out any insoluble particles. This provides a 25mg/ml solution.
Method 2
For the second method, we will formulate it for 1g of steroid.
Triturate (mix in a mortar with a pestle) 9g HPBCD with 1g steroid. Place this in a high humidity environment for 2-4 days. I have used a covered fish tank with water in the bottom, but anything that can create a humid environment will work. A syrup will form, and this is dissolved in 40ml saline and you have a 25mg/ml solution.
Method 3
For the third method, we will formulate for 4g of steroid.
Triturate 36g of HPBCD with 4g steroid. Let this sit at normal room temperature and humidity for a week. Complexation will occur, but takes time with this process Dissolve the powder in 160ml saline. This again makes a 25mg/ml solution.
These solutions can be made stronger by adding less saline, but the closer you get to 50mg/ml, the thicker the solution becomes. At 75mg/ml, the solution is too viscous to do anything with.
Editors Note: I am assuming he is talking about mg of actual androgen, not mg of androgen/cyclodextrin complex, because cyclos will dissolve just fine at 300mg/ml, which I think is ample, anyway.
If prohormones are used, you will probably want to filter the solution, since there are a lot of insoluble impurities in most of the prohormone powders out there.
i am not sure if this article is bullshit but it sounds interesting i was wondering if anyone has tried this i was thinking of trying this with fina
It seems that hardly anyone out there knows how to complex a steroid with a cyclodextrin. One procedure I saw on a different company’s steroid column was laughable. It was pretty obvious that whoever wrote that procedure knew very little about cyclodextrins. It is really fairly easy to do. There are multiple ways to do it, but I will tell you three methods to try, depending on what resources you have available. In all instances, you need a ratio of 9g of HPBCD to 1g of steroid. Complexation occurs because the steroid is more energetically stable inside the CD than outside of it. It is an equilibrium process, but the equilibrium lies much more on the side of complexation.(3) Water is essential for complexation to occur. It is removed from the inner cavity to allow for the steroid to enter, but even normal room humidity is sufficient for complexation if the mix is given sufficient time.(4)
Method1
For the first method we will formulate it for a total of 2g of steroid.
Dissolve 18g of HPBCD in 80ml saline in a beaker on a stir plate. Once this is dissolved, slowly add the 2g of steroid over about 5 minutes. Let this stir overnight. Filter out any insoluble particles. This provides a 25mg/ml solution.
Method 2
For the second method, we will formulate it for 1g of steroid.
Triturate (mix in a mortar with a pestle) 9g HPBCD with 1g steroid. Place this in a high humidity environment for 2-4 days. I have used a covered fish tank with water in the bottom, but anything that can create a humid environment will work. A syrup will form, and this is dissolved in 40ml saline and you have a 25mg/ml solution.
Method 3
For the third method, we will formulate for 4g of steroid.
Triturate 36g of HPBCD with 4g steroid. Let this sit at normal room temperature and humidity for a week. Complexation will occur, but takes time with this process Dissolve the powder in 160ml saline. This again makes a 25mg/ml solution.
These solutions can be made stronger by adding less saline, but the closer you get to 50mg/ml, the thicker the solution becomes. At 75mg/ml, the solution is too viscous to do anything with.
Editors Note: I am assuming he is talking about mg of actual androgen, not mg of androgen/cyclodextrin complex, because cyclos will dissolve just fine at 300mg/ml, which I think is ample, anyway.
If prohormones are used, you will probably want to filter the solution, since there are a lot of insoluble impurities in most of the prohormone powders out there.
i am not sure if this article is bullshit but it sounds interesting i was wondering if anyone has tried this i was thinking of trying this with fina
