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Cyclo Diol™ and Cyclo NorDiol™

When a prohormone is taken orally, it is subject to First Pass (the body breaks it down which is not good because it leaves very little active hormone life). The hormone is in and out of the system very quickly. Cyclodextrin is a molecule with a water compatible exterior and a water incompatible interior. The ANDRODIOL™ or NORANDRODIOL™ molecule is placed inside the Cyclodextrin. The water compatible exterior of the Cyclodextrin will camouflage the water incompatible molecule, the pro-hormone. Your bloodstream will allow it to enter immediately, and the pro-hormone will be released into your body. It is taken by placing in the lining of the cheek or under the tongue. It goes directly into the blood stream.

In summary, cyclodextrin complexes taken sublingually (under the tongue) get pro-hormones into the bloodstream much better than orally taken capsules since over 90% of orally taken pro-hormones are never utilized by the body.

LPJ Research Cyclo Diol™ and Cyclo NorDiol™
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Sublingual Cyclodextrin Complexes

By Patrick Arnold

A clinical study was undertaken recently at Eastern Michigan University. Mind you, this study has yet to be published, so I have to be very careful about how I report on the results here (I can't give absolute numbers at this time, only percent increases). Otherwise, the researcher may run into problems getting the study published. Once it's published, however, the details can and will be released in their entirety.

This particular study examined the acute responses to 25 mg and 50 mg doses of Cyclo-Diol, a 4-androstenediol Sublingual Cyclodextrin Complex (SCC), in healthy males. These males (the same seven that took part in the original EMU 4-androstenediol study recently presented in Finland) had average baseline testosterone concentrations in the high-normal range. The results, expressed as average percent increases over baseline, are as follows:

Testosterone Increases With Cyclo-Diol™ *

CycloDiol Test

Let's examine the results of this study and compare them to the results that these same seven subjects had a few months earlier with regular oral 100 mg 4-androstenediol capsules:

Testosterone Increases With Androdiol™ *

Androdiol Test

The first thing that strikes the eye is the different times to peak blood values for the SCC versus the straight oral. The time to peak is much sooner for the SCC than it is for the straight oral; 40 minutes versus 90 minutes. Also, the percent increase at peak is much higher for the 25 mg SCC (128%) than it is for the straight oral (49%). That translates to a 261% greater testosterone increase with the SCC over straight oral at one quarter the dosage!

As you can see, the dropoff in the T levels for the 25 mg SCC is quite gradual. Testosterone increases at two hours post-dose were still well above the peak levels experienced with the straight oral 100 mg dosage.

One of the most intriguing findings from this study was that a 50 mg dose was no more effective than a 25 mg dose. From talking to other experts in the field, I've come to believe that this is likely due to the limited capacity for absorption through the sublingual tissues. There's only so much surface area under your tongue. The expression, "trying to stuff ten pounds of potatoes in a five-pound bag" comes to mind.

In fact, we're wondering if a 10 mg dose of Androdiol™ SCC might be equally effective as a 25 mg dose, and, in fact, we're examining that possibility in a new study that's going on right now.

Another note of interest from this study was that the variability of testosterone responses among subjects taking the Androdiol™ SCC was extremely low. This is in contrast to the oral Androdiol™ study where some subjects had increases of testosterone over 100%, while others had increases of barely 25%.

In other words, just about everybody who used SCC experienced the same remarkable surges in free testosterone, whereas those that use(d) oral Androdiol™ experienced across-the-board results.

This leads us to believe that the biggest factor in the variable responses to prohormones may not have anything to do with differing levels of conversion enzymes throughout the body, as is generally assumed. Instead, it looks like it may have more to do with differing absorption capabilities from the gut and/or the differing capacity of people's livers for deactivating orally ingested prohormones upon first pass.

* These data were presented at the International Weightlifting Conference in Lahti, Finland, Nov. 1998. Study funded and supported by LPJ Research Inc. and Subtrate Solutions Inc. The results do not constitute an endorsement of 4-androstenediol by the author or Eastern Michigan University.

Androdiol is a registered trademark of LPJ Research, Inc.

Q: What is the difference between Beta-Cyclodextrin and Hydroxypropyl-Beta-Cyclodextrin

Pat Arnold A: Hydroxypropyl-Beta-Cyclodextrin complexes are many times more water soluble than Beta-Cyclodextrin complexes. Water solubility has everything to do with the effectiveness of cyclodextrin complexes. The solubility of testosterone Beta-Cyclodextrin complexes were found to be 0.13 mg/mL and that of Hydroxypropyl-Beta-Cyclodextrin to be 5.14 mg/mL (Pharmazie 53 (1998) 2). That is why the Beta-Cyclodextrin products dissolve painfully slowly and feel like sand in your mouth while Hydroxypropyl-Beta-Cyclodextrin prohormone products dissolve quickly and cleanly.

Joseph Pitha, who is the renowned expert when it comes to steroid/cyclodextrin complexes (he has several journal articles published as well as several patents), found that Beta-Cyclodextrin complexes of steroid hormones were ineffective and Hydroxypropyl-Beta-Cyclodextrin complexes were highly effective (J. of Pharmaceutical Sciences, 75 (2) 1986)

There is not even room for a debate on the subject of Beta-Cyclodextrin vs. Hydroxypropyl-Beta-Cyclodextrin for increasing the bioavailablity of steroid hormones and other drugs. The literature data is clearly massively in favor of Hydroxypropyl-Beta-Cyclodextrin.
- Patrick Arnold

Q: Which product, Cyclo-Diol or Cyclo-NorDiol, is better?

A: Stacking a C19 (andro) prohormone (Cyclo-Diol) with a 19-nor product (Cyclo-NorDiol) is probably a good idea. Testosterone and 19-nortestosterone both metabolize differently and will affect various tissues differently. To be specific, testosterone will have a stronger affect on tissues that have a high level of 5-alpha reductase (5-AR) while nortestosterone will have a stronger affect on tissues that have a low level of 5-AR. Used together (respective prohormones that is) you should get the best overall androgenic / anabolic "punch".
- Patrick Arnold

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