hOW ABOUT SOME LINKS TOT HAT RECIPE ... I DID A SEARCH AND DIDNT COME UP WITH ANYTHING. I'LL TRY AGAIN. THANKS ...
Alternative Steroid Delivery Systems
by Dazed
In the premiere issue of Mind and Muscle (“Big Motherf*cker�, at the time), there was an article with a formula making your own trenbolone nasal spray. While this formula “works�, it is not the most elegant way to use steroids intranasally. Unfortunately, the feedback often contained complaints of serious irritation to the nasal cavities, which as you can imagine is no fun. So in the spirit of improving upon what we already know, I will show you how to make some better steroid delivery systems.
First, a little background on this subject -- the reason why steroids, including prohormones, need these delivery systems is because, when taken orally, a very high percentage of the steroid is deactivated by the liver, via first pass metabolism. This deactivation can be reduced many ways, including 17-alpha alkylation of the steroid, addition of esters and ethers to the 17beta hydroxyl group, using steroids that are unsaturated at the 1 position, or a combination thereof.(1)
Another strategy is to avoid the digestive tract all together. There are many ways to do this, but the most common delivery systems are transdermal, intranasal, and sublingual, and parenternal (injectable). The transdermal route is very well covered by the supplement industry, and from what I have seen and heard, some of these systems vastly surpass topical steroids compounded by pharmacists for hormone replacement therapy.
Injectable steroids are obviously a great choice of delivery system, and these are also well covered and come commercially in both oil solutions and water-based suspension, as well as in some, um, original unknown forms from certain bootleggers. This leaves us with nasal and sublingual forms to explore for our alternative steroid delivery systems.
Don’t underestimate the utility of nasal and sublingual delivery systems. The nasal cavity of an adult has a large surface area of about 180 cm^2 and has about a 20ml capacity.(2)) The microvilli present along the pseudostratified columnar epithelial cells in the nasal mucosa provide this large surface area.(2) These microvilli are highly vascularized as well, allowing direct access of a drug to the bloodstream.(2) As far as the mouth goes, well, some of us have bigger ones than others. All kidding aside, there is a significant surface area of highly vascularized tissues located under your tongue as well. Now we just need to find a nonirritating way to get the steroid to and through these tissues.
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.
Where to get Steroids
You can obtain your steroid as described in the original trenbolone nasal spray article, or from one of the various sources for steroid powders out there. Prohormones can be used as well, any steroid will work. The products here can be administered as described in the trenbolone nasal spray article. The following formulas will work for nasal and sublingual administration.
Complexation:
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.
Intranasal and sublingual delivery systems can be very useful. Not only do they work well, but the needle phobic and the human pincushion now have a way to add more steroids to their body. Those who want to get a boost in blood levels before a workout are now free to do so. As an added benefit, I can’t say I have ever heard of someone having their nasal inhaler confiscated to be tested for anabolic steroids. Enjoy!
Reference:
1. Vida, J. (1955), Androgens and Anabolic Agents: Chemistry and Pharmacology. publisher
2. Ansel, H., Allen, L., & Popvich, N. (1999), Pharmaceutical Dosage Forms and Drug Delivery Systems Seventh Edition. Maryland: Lippincott, Williams, and Wilkins.
3. Loftsson, T. (1998) Increasing the cyclodextin complexation of drugs and drug bioavailability through addition of water soluble polymers. Pharmazie, 53, 733-740.
4. Cyclodextrins in Pharmacy
Carlito
Can I Inject?
I performed a little experiment with 4-androstenediol and HPBCD. I complexed some 4-Adiol with HPBCD as in example 1. I evaporated off some water until there was a 50mg/ml solution. This was sterile filtered this into a sterile vial and injected. These were the most painfree injections I have ever had with 4-Androstenediol. The cool thing about this formula is that it can be shot subcutaneously or intermuscularly, since it cannot crystallize and dissipates quickly because it is so water-soluble. Although I never tried, multiple daily shots would be needed to impart any kind of muscle building effect, and although you will never be limping because of a painful muscular injection, it would just be too much of a hassle. Another reason not to do this is because most HPBCD available is not endotoxin free, so you could be setting yourself up for a nice fever or illness, or possibly a very bad reaction that could cause death. That is always a good reason to avoid something.
Carlito says he does this with bases, you can PM him or find him on this board.
