- 06-17-2004, 10:28 AM
Reads this article, sounds very interesting, anybody got any thoughts on it, is this form of administration common place?
Just trying to learn a little....
Cyclodextrins are a form of linked carbohydrates. They're formed by an enzymatic synthesis that begins with starch. The enzymes, called transglycosidases, are derived from bacteria. What these enzymes do is couple the starch molecules together to form a truncated, conical, molecular structure with a hollow cavity inside.
The inside of this cyclodextrin "cone" is just about the perfect shape and volume to accommodate a steroid molecule. It's also a non-polar molecule, which means that it has some of the same properties as a fat or oil. The steroid molecule doesn't just sit inside the cone, it actually attaches to the inside of it. Also, it won't dissolve in water. However, while the inside of the cyclodextrin cone is non-polar, the outside is polar, which means that it will dissolve in water. What's the significance of all of this? When a steroid molecule and a cyclodextrin molecule hook up, they form a 1:1 complex. So, while the steroids themselves won't dissolve in water, a cyclodextrin/steroid complex will. The upshot is that steroid complexes become more absorbable through the oral mucosa.
A lot of clinical research has been published on the use of sublingual cyclodextrin complexes (SCCs) in humans. At the forefront of much of this research has been Josef Pitha of the US Department of Health and Human Services. Pitha has several patents on sublingual cyclodextrin complexes. He's also authored a journal article where he details the results of an SCC of testosterone on men. In a nutshell, Pitha found that an SCC containing 10mg of testosterone per tablet raised testosterone levels astronomically high (900% over baseline at one hour) and at two hours the levels were still elevated 485%. Compare that with another study that used regular testosterone at 20 times the dosage used in Pitha's study. Regular testosterone - not complexed with cyclodextrin - only raised testosterone around 500% at the peak.
Another study performed by Stuenkel et.al. showed that testosterone SCCs of 2.5 and 5.0mg raised testosterone levels in hypogonadal men 2341% and 4270% (absolute increases of 1765 ng/dL and 2406 ng/dL) respectively! It took an average of 20 to 30 minutes to achieve maximum blood testosterone levels, but even after eight hours post-dose, the testosterone levels were still elevated 126% for the 2.5mg dose and 195% for the 5.0mg dose. Interestingly enough, the peak levels for estradiol only increased 300% and 340% over baseline, respectively. Remarkable, considering that one usually sees estradiol levels increase proportionally with testosterone levels when other forms of administration are used (i.e. injectable esters and TU orals).
- 06-17-2004, 12:26 PM
Cyclodextrins are great for drug delivery and for masking the horrid taste of some chemicals. That said, you should know that they are useless for methylated "prohormones" - I've tried. These drugs are useless until they are metabolized (broken down) in the liver - or to put it otherwise, it is not the drug itself that has the effect, it is the metabolites. It will make non-methylated prohormones much more bioavailable, but you will have to make a nasal spray. Sublingual works somewhat, but then you end up swallowing most of the cyclo-drug complex. Also, if you want to make a fine tasting solution out of a drug powder, cyclodextrins are what to get. I think only 1fast400 carries them.
I have another post around here about them, last week or so.
06-17-2004, 02:42 PM
Cyclodextrin prohormones never panned out. I think they were marketed over 2 years ago and never really gave decent absorption, better off with transdermals. As mentioned, they are worthless for methyl compounds. As for buying cyclodextrin and mixing in your ph I just don't see how that would work.
06-17-2004, 03:22 PM
No. They gave great absorption, the trouble was that with the crappy prohormones available, you had to take far more than could be conveniently absorbed at once, so you would have to take cyclo-complexes like 10x a day, and even that probably would not be enough to see good results.Originally Posted by ersatz
Secondly, buying cyclodextrin and mixing in your ph is easy. I know it does work, why do you think it wouldn't work? There is a 'how to' on this which can be found easily through Google. I think the post is over at AvantLabs.
06-17-2004, 11:43 PM
True, the prohormones of a few years ago aren't nearly as potent as say 1-test. I just remember the marketing from back then that the cyclodextrin was like a sock that covered the prohormone and allowed for sublingual absorption. Companies were bashing one another saying that not all products were created equally. It had to be altered/produced in some manner that allowed the prohormone to fit inside the cyclodextrin. Do you have any idea on the availability percentage-wise of a cyclodextrin based compound? I know methyls are over 95% and transdermals are in the 30-40% range.Originally Posted by Strateg0s
06-18-2004, 12:43 AM
Cyclodextrins make bioavailability pretty high, but they are limited by surface area. Short of doing things I will neither consider nor mention, the greatest available surface area of a mucous membrane is in the nose. Sublingual absorption is not as high because it gets suspended in your saliva (held away from the membrane) then you swallow it. Apparently only 25mg (of prohormone) can be delivered through the membrane in one dose, so if the daily amount of oral was supposed to be 500mg transdermally, at ~35%, you'd have to do 7 doses of cyclo-complex to deliver the same 175mg. I suspect that intransal delivery via cyclodextrins would be >85%, oral much lower for the above mentioned reasons.
06-18-2004, 04:17 AM
'Short of doing things I will neither consider nor mention,'
Yeah! strictly one way traffic in that area!
Thank you both for your feedback and knowledge.
06-18-2004, 04:50 AM
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