Thread: Did I just find a new way to brew gear ?!?

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.



So it can only go to about 50mg/ml but its still gotta be less painful and easier to push through a small gauge needle for daily injections. I realize the second post is referring to nasal and sublingual delivery, but it apparently does work for injectable as well. Any thoughts on this? Anyone ever tried it, or even heard of it?

From what I'm reading it sounds like TNE would be a perfect candidate for this stuff, it supposedly releases much faster than any other delivery method, it could even be used to make sublingual tablets of Test no ester. Also orals can be made into injectables, and for most 25-50mg/ml will be enough, saves you from using nasty solvents like guaiacol and EO... Sounds like good stuff but I hear its pricy..

HPBCD Basics
By David Tolson


One of the primary issues concerning steroids and prohormones is that of optimal delivery. While most drugs and supplements are taken orally, there are a number of reasons why this method is largely ineffective with most prohormones. When taken orally, these compounds are extensively metabolized in the liver, making the dose used much larger than the amount that gets through. This may also place undue stress on the liver, especially with certain substances. Because of this, other delivery methods, such as transdermal, sublingual, and intranasal, have all become popularized, and each has advantages and disadvantages. This article discusses the compound hydroxypropyl-beta cyclodextrin (HPBCD), which can be used to facilitate prohormone delivery in a number of ways.

Cyclodextrins are a group of compounds that are commonly used in medicine to increase the aqueous solubility of drug substances by complexation [1]. Cyclodextrins are cyclic oligosaccarides, or sugars, which contain alpha-1,4 linked glucopyranose units (in the case of beta-cyclodextrins, seven of these units) in a truncated cone shape [2]. This results in a molecule that has an internal cavity that is hydrophobic and easily forms a complex with a steroid/prohormone molecule, while the outer surface of the cyclodextrin is hydrophilic, and this makes the complex easily dissolvable in water [2-4]. This renders prohormones much more bioavailable, and cyclodextrins are capable of enhancing nasal, sublingual, and transdermal delivery [5-6], among others. Moreover, cyclodextrins will cause much less irritation than other methods [3, 7].

The cyclodextrin of choice for prohormone delivery is HPBCD. When compared to other testosterone beta-cyclodextrin complexes, HPBCD was 1,533 percent more soluble in water, while another study found that HPBCD-steroid complexes were effective while beta-cyclodextrin-steroid complexes were not [4]. HPBCD also has an excellent safety profile.

Sublingual delivery

Sublingual delivery (administered under the tongue) presents an attractive alternative to traditional oral administration. Because of the limited surface area, the amount of prohormone that can be absorbed at one time appears to be 25 milligrams or less. However, when compared to oral delivery, even this amount is advantageous. One study found that a cyclodextrin complex containing 10 mg of testosterone delivered sublingually raised testosterone levels by 900% over baseline, with a 485% elevation at the two hour point. In contrast, even 200 mg of oral testosterone only raises levels by around 500% at the peak. A study comparing oral and cyclodextrin complexed 4-androstenediol also found that the sublingual version lead to a 261% greater increase in testosterone with one quarter of the dose, with the peak levels at 40 as opposed to 90 minutes. [4]

All in all, sublingual delivery is much more effective than oral for the amount used, but it does require more frequent dosing. Sublingual prohormones are usually taken 3-5 times daily.

Intranasal delivery

Intranasal delivery takes the trend of sublingual delivery even further. It is doubtful that more than 20 mg at a time will be absorbed using this method, and blood levels quickly spike 15 minutes after delivery and then dissipate to baseline by 90 minutes. Running a cycle using this method is impractical, as one has to dose up to 10 times daily. However, bioavailability is further increased ? intranasal delivery has the highest bioavailability of all prohormone delivery methods, short of injection [7]. Additionally, intranasal delivery provides the most direct route to the brain [6, 7]. For these reasons, this method has become popular for pre-workout stimulant purposes. Many people report increased workout intensity from intranasal prohormones. DHT precursors are best suited to this purpose, although some other prohormones may make effective pre-workout stimulants as well.

Conclusion

HPBCD complexes can allow for a number of novel effective prohormone delivery methods. Each one has unique advantages and disadvantages.

It takes 9x as much cyclodextrin as hormone to make the "complex", and this stuff is like $1-3 per gram. So for a 100g batch you'd need 900g cyclo and it would cost an extra $900-2700 per batch lol.... nevermind then thats probably why people don't use it. Too bad, I wanted to give it a try

Pretty expensive