Complexing Ethylphenidate with suitable Cyclodextrin to alleviate insufflation pain?
I believe that Cyclodextrins (good ol' cyclodextrins) might be able to offer a part-solution to my quest, or at least an improvement on the current pain endured on insufflation. I, like others, am a little obsessed by the possible ways Cyclodextrins might improve our drug
taking experience. I like to daydream...
But recently I've grown more and more fond of this idea. So much so, I'm risking (yet again) looking like the fool of DF, in the quest for enlightenment.
Many will no doubt be familiar with the employment of Cyclodextrins to improve the water solubility of drugs
which might otherwise be hopeless. This is not even the tip of the iceberg.
Forget the Nbome complexing some users may have stumbled across. Cyclodextrins are allowing ever more novel drug delivery systems to become reality. Nasal delivery of Benzodiazepines anyone?
To the layman (me) it does seem that Cyclodextrins really are worth pursuing to enhance recreational drug use, of course, only where their application is clearly beneficial. In my opinion, at this present time, there is no more worthy a pursuit than the reduction of insufflation pain associated with Ethylphenidate.
The majority of recreational drugs do not have any problem with water solubility, and administration routes/methods are (on the whole) effective, time tested and established as efficient. But is it not possible that the efficiency or palatability of at least some, can be improved?
Below is a list of possible advantages of the use of Cyclodextrins, typed word for word from 'Cyclodextrins: An excipient tool in drug delivery'. See end of post for full details, I have uploaded the file to the archive - well worth a quick read. I have highlighted in bold the claims which are most relevant to my goal; reduction of insufflation pain.
1. CDs help in improving the aqueous solubility of many poorly soluble drugs.
2. CDs enhances the dissolution thus helps in enhancing the bioavailability of drugs.
3. CDs complexation improves the chemical, physical and thermal stability of drugs.
4. CDs inclusion complexation helps in ameliorating the irritancy of the drug moiety that irrates the stomach, skin or eye.
5. CDs cloak the unpleasant odour and bitter taste of drugs.
6. Complexing oily or sticky substances with CDs into microcrystalline or amorphus powders help in improving the material handling properties.
7. Formulation of modified release preparations.
8. CDs helps in decreasing the toxic effects associated with drugs.
9. CDs have also been used in the novel pharmaceutical applications. *1
So, for my goal...
Which Cyclodextrin might be suitable for Ethylphenidate, if any?
No idea. As of yet
... Anything I would suggest will be a poor guess. I am seeking help with this, though if anyone cares to chime in I would be most grateful.
This is going to be largely trial and error with regard to method of producing the complex. Some methods will be out of the question for me, for example freeze drying and methods which involve supercritical fluids.
The majority of the established techniques, I believe I will be able to emulate. Again, I expect trial and error to dominate the methodology throughout.
I have no idea which would be most suitable for any given compound/cyclodextrin goal - though I'll most likely start with the easiest methods, and work my way up.
If, when scrutinised, it appears there might be some merit in this idea - everything will be approached methodically, thoroughly documented, and this thread will be updated.
Maybe the best I could ever hope for is a gooey mess? I just don't know...
There is lots more coming, but I may have to wait until tomorrow, or at the best later tonight. Any input in the meantime greatly appreciated.
Mental state disclaimer:
For the record,I'm not completely mad. I've been aware of Cyclodextrins for a long time, and in no way do I think they are a magic 1-up for every recreational drug. I don't personally have the knowledge to tackle this alone, as such I have largely refrained from ranting, raving and asking endless daft questions... "Will drug ABC fit in Cyclodextrin XYC?" repeatedly. Yes, my post is very much pro-cyclodextrin... and I can't lie, it does get me excited. I think other people should know about their applications.
^ That being said, I would really like to address this issue of insufflation pain, and if complexation with a suitable Cyclodextrin might offer some hope of alleviation, I will really put my back into this. Any tips would be massively appreciated.
After my dream is either swiftly crushed, slowly destroyed or *maybe* yields something close to a result; I will continue to dream about the possibilities of Cyclodextrins in silence and not bother anyone again.
EDIT: OK, Damnit! I now know this is never going to work with Ethylphenidate. Grrr...
*1 Cyclodextrins: An Excipient tool in drug delivery. Ali Nasir, Harikumar S.L. and Kaur Amanpreet.