Orally disintegrating performation enhancing agents Delivery

Performation enhancing agents are metabolic precursors to male hormones such as testosterone, which is known to make men stronger, more energetic and more virile. This is why they have obvious applications within Bodybuilding because they can increase testosterone levels and/or combat low testosterone. This is also why they are among one of the most popular categories of Bodybuilding supplements since higher testosterone levels can lead to increased muscle mass.

Popularity not withstanding, the present technology of drug delivery systems as they pertain to testosterone and/or performation enhancing agents are behind the curve. performation enhancing agents taken orally via standard capsules are ingested and digested so they have to make their way through the stomach, small intestine and liver respectively. In the liver, these compounds are broken down and for the most part, deactivated. Therefore, the majority of the compound will not be utilized and will put a bit of a non-toxic burden on the liver.

This is where orally disintegrating delivery comes in. orally disintegrating simply means ‘under the tongue’. It allows the compound or drug to enter the bloodstream through the tissue under the tongue. As it applies to steroid hormones, the technology has been patented and has been studied exhaustively. Its first applications were for active steroid hormones as a drug delivery, but it is also particularly applicable to prohormone supplements. These orally disintegrating supplements solve the poor bioavailability, first pass liver problem posed by oral capsules. The most effective way to utilize orally disintegrating delivery for these supplements is by combining the prohormone with a cyclodextrin compound, a carbohydrate like molecule that allows the prohormone to be absorbed by the oral mucosa. The orally disintegrating delivery (orally disintegrating tablets) of the cyclodextrin compound with small doses of testosterone/prohormone can produce from a five to tenfold increase over oral capsules. The specific type of cyclodextrin used should be Hydroxyproply-beta cyclodextrin which is many times more water soluble than beta cyclodextrin and therefore is superior for mucosal delivery. The cyclodextrin complex acts as a ‘molecular condom’ for the prohormone. This causes a normally fat soluble compound such as performation enhancing agents to become water soluble [1].

Joseph Pitha of the United States Department of Health and Human Services has been the pioneer of this type of orally disintegrating research. Pitha published a study in which he used a cyclodextrin/testosterone complex on men. Pitha found that this complex containing just 10 milligrams of testosterone raised testosterone levels 900% (from normal baseline level) in one hour. On the other hand, oral testosterone at 20 times this dose (200 mgs), raised testosterone just 500% at the peak. Another study comparing a 100 mg. oral vs. a 25 mg. cyclodextrin complexed orally disintegrating 4-androstenediol, found the orally disintegrating version led to nearly a threefold (261% to be exact) greater increase in testosterone with one quarter of the dose (25 mgs), with the peak levels at 40 as opposed to 90 minutes [2].

According to two other studies, 20 to 21.4 mgs Cyclodextrin androstenediol taken orally disintegratingly increases serum testosterone levels in healthy young men from their original baseline levels. The findings suggest that this orally disintegrating concoction is “superior to oral ingestion for the delivery of androstenediol to the peripheral tissues and subsequent conversion to testosterone”. These studies further demonstrate that orally disintegrating, mucosal delivery of small doses of testosterone precursors produces a much better hormonal response than does oral ingestion of large doses [3, 4].

Finally, an Eastern Michigan study, again done with oral
4-Androstenediol and a 4-AD/cyclodextrin orally disintegrating compound concludes that the orally disintegrating delivery wins again. A 25 mg orally disintegrating dose outperformed a 100 mg oral dose by a 261% greater testosterone increase! Again that is at 25 mgs, one quarter the dosage! It should be noted however, that orally disintegrating absorption does have its limits. This same study was also done with a 50 mg orally disintegrating dose and was shown to me no more effective than a 25 mg dose. This may be due to a somewhat limited capacity for absorption through the orally disintegrating tissues. There is a limited surface area under the tongue, which probably means there is a finite amount of material that can be absorbed orally disintegratingly [1].

In conclusion, orally disintegrating prohormone products raise testosterone much more effectively than oral capsules. These increases in testosterone are rapid and last for about three hours in healthy men. For the best way to achieve desired gains, orally disintegrating products should be administered in three doses per day for the length of a cycle. The increased efficacy of orally disintegrating vs. oral is about tenfold. Therefore, they are unquestionably the most effective and safest way to use performation enhancing agents.

References

1. IronMan Magazine. December 1999. Super Andro: Cyclodextrin Technology Shatters the Absorption Barrier by Patrick Arnold and David Garrett.
2. Pitha, J. J Pharm Sci. 75(2):165-167.
3. Eur J Appl Physiol. 2006 97: 404-412. Acute Resistance exercise does not change the hormonal response to orally disintegrating androstenediol intake. Brown GA, McKenzie D.
4. J Appl Physiol. 2002 92: 142-146. Acute hormonal response to orally disintegrating androstenediol intake in young men.