Snorting - Complexing ethylphenidate with suitable cyclodextrin to alleviate insufflation pain?

[Bad Rabbits]

Complexing Ethylphenidate with suitable Cyclodextrin to alleviate insufflation pain?

Please see several posts down for more information. Thanks for looking!




Original post: (Now defunct)

Will the addition of Sodium Bicarbonate to Ethylphenidate (in its HCL salt form) alleviate some of the obvious corrosive effects on insufflation?

Theory:

1) I understand that when the HCL salt form of a drug is insufflated, free water protons react with the salt, resulting in the formation of Hydrochloric acid.

Am I correct in assuming that this is where the majority of the burning sensation comes from?

2) Assuming the above is correct, there are a few candidates which might be used as an admixture, to hopefully neutralise the Hydrochloric acid.

I am thinking that Bicarbonate of Soda would be most ideal, as it is water soluble and should present no safety concerns (it is administered IV to counteract acidic blood/body tissue). It's ability to safely neutralise Acids aswell as Bases, of course means it is always within arms reach during any kitchen chemistry.

Background:

I've been growing increasingly fond Ethylphenidate as of late. My preferred ROA is insufflation, oral consumption doesn't touch me like insufflation does. I won't change my administration method... Needles are out of the question, as is sticking drugs in my rusty sheriffs badge.

Ethylphenidate genuinely feels like one of the most corrosive compounds I have repeatedly insufflated. No doubt there are worse out there, but with repeated administration I really feel the need to reduce the harm to my nasal passages. OK, 2CX's are bad, but you don't redose every hour or two.

I have access to a small quantity of Lidocaine, which I have pre-administered in the past to help deal with insufflation pain. Of course this works, but it is mearly masking the pain - it isn't addressing the issue of the corrosive nature of the drug. I don't see this as a solution to my problem, and I won't be able to obtain anymore once the (very limited) supply has run out.

Ideally, aswell as addressing the pain - I want to know that I am protecting my nasal passages from destruction.

While I refer to Ethylphenidate repeatedly, it would of course be great to apply this to all manner of drugs in their HCL form.

Bad Rabbits added 29 Minutes and 58 Seconds later...

EDIT: Of course I will trial this at some stage if I don't get any feedback, but I would really appreciate any input on whether this might be effective or not. Any suggestions or criticism welcome. Many thanks.

[Lodewijkp]

i use this to make my body more alkaline and to decalcify my system ( bad calcium deposits)
baking soda is a cancer killer - there is much work done on this subject just google or youtube it.

[Zeni]

I think the possible problem with that is that a basic substance converts the ethylphenidate in its freebase, which is water insoluble. Even if one mixes bicarb and EP dry, the conversion can still happen fast enough in one's nose or when some water is present causing it to clog ones nose instead of dissolving and entering the body through the mucous membrane. Swallowing an non polar substance is less of a problem since it will probably get protonated in the acidic environment of the stomach and still enter the body's blood stream. But insufflation of insoluble substances will just lead to clogging.

[TheFakeBass]

Originally Posted by Bad Rabbits

1) I understand that when the HCL salt form of a drug is insufflated, free water protons react with the salt, resulting in the formation of Hydrochloric acid.

Am I correct in assuming that this is where the majority of the burning sensation comes from?

If that were the case, tasting table salt would give you horrible acid burns on your tongue, and soy sauce could be used as a substitute for muriatic acid. Yes, putting the soluble hydrochloride salt of an drug in water will result in dissociation of the ions into DrugH+ and Cl-. Yes, the Cl- will coexist with the water's short-lived natural H30+ ions. But Cl- is a pretty weak base, and it's harmless in reasonably small quantities, as you've noticed if you've ever tasted salty foods or beverages.

The problem is the protonated drug, DrugH+. It will dissociate into H+, which will react with water's short-lived natural OH- ions to give a molecule of water, and freebase Drug, which is the real problem.

The HCl decreases the caustic effect rather than increasing it. Uncharged compounds with an amine group tend to be rather basic (e.g. ammonia), and they become weak acids when protonated (e.g. ammonium ions). Weak acids are much less irritating to mucous membranes than the basic amines. If you don't believe me, try snorting freebase ethylphenidate. (Or most other freebase amines--if you get pleasure from other people's pain, read some anecdotes from people who've snorted freebase DMT, or even touched it with their tongue.)

Reputation Comments on this Post:

Great explanation of the stinging feeling that occurs when insufflating amine salt drugs.

[Bad Rabbits]

I had completely forgotten about this thread, I only came across it again through Google (looking into the same subject). Woopsy...

I'd like to thank everyone for their informative replies. TheFakeBass has made some excellent points, and in retrospect it seems that I asked a particularly daft question - though I'm glad to be wiser for it.

I'm going to continue to experiment with ways to minimise damage to nasal cavities... or at least, the associated sensation. I'll report back if anything proves worthwhile.

Thanks again for the top replies, I really appreciate your input.

[Bad Rabbits]

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.

Cyclodextrins?

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.

Practical

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.