Originally Posted by Lozgod
I am about to begin my Sublingual Steroid experiment. This may one day have those too deathy afraid of the needle doing year long cycles one day.
Why? You may be asking yourself.
1. I do hate the needle with a passion, I use it, but I hate it.
2. Just to see if it works. Research and curiousity go good together.
3. If it were to work it is very very cost effective. Base hormones are very very inexpensive.
The proposed cycle will be 6-8 weeks long. The hormones will be Testosterone and Boldenone Base (suspension). Dosed 4 times daily at 25mg for test and 20mg for EQ. This will make for a total daily dose of 100mg of Test and 80mg of EQ, corresponding to 700mg and 560mg respectively per week.
The solution will be 25mg/ml of Test and 20mg/ml of EQ.
The dosage will be administered like so:
One ml of each hormone individually placed under the tongue for 3 minutes each. Then swallowed. After research it seems that 25mg is the limit to be absorbed under the tongue at one time.
This is not an investment so I can't justify paying for routine blood tests so my gains or lack there of will be the measuring factor of successful absorbtion. I may pay for one or two tests during the cycle.
Yes I did consider there will be 8 hours I will be asleep and not dosing. In spite of sleep orals are still effective. We will take Dbol for instance. It has a half-life of about 4 hours, so if taken close to bed time it is effective in your sleep, however I am estimating the suspensions half-life to be about an hour with the clock starting to tick down 20 minutes after taking dose. However I cant take it in my sleep so I wont lose any sleep worrying about this. :lol: Get it. It was a pun. Anyway...........
Here are a couple of my sources of info on this. Thank you AM for pointing me in the direction of the Avant Labs article.
Introduction
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. For further information, as well as information on creating your own cyclodextrin complexed prohormones, I recommend the following article:
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.
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.
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
