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Cyclizine Hcl to water soluble salt??

Tryptamite

Bluelighter
Joined
Dec 5, 2006
Messages
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Normally I would have 20-40 50mg tablets which would make a 1-2g acid base easier.

Now I have only 500mg.

What I do is isolate the cyclizine Hcl from the tablets using h20 and MeOH. Then cool the solution and add NaOH. Cyclizine base precipitates out and can be collected in a paper filter and washed with h2o and left to dry.

A solution can then be made to desired concentration 50ish mg/ml using water and lactic acid or citric acid. These two salts I know to be h2o soluble.

Citric acid is easier for me to obtain

Can anyone think of an easier way to go from Hcl to citrate cutting down on steps to avoid mechanical losses which will inevitably occur with such a small amount of product?

Any input appreciated!! Thank you.
 
Why bother converting it to the freebase and back to a salt? Just extract the pills into ph 5 water, filter, and you should be fine.
 
The Hcl salt is soluble only at 1mg/ml. Lactate and citrate at least 50mg/ml.

Sorry for double posting please delete other posts thanks
 
Here's an idea. I have little product and ghetto equipment no paper filters at moment this the only reason for considering this.

Crush 100mg cyc Hcl in spoon. Water wash with a few ml of h20 and filter with syringe and smoke filter. Get rid of some water soluble inactives. Base appropriately with correct amount of baking soda (preferred safer for this sloppy tek) or NaOH + h2o + heat.

Now have cyclizine base and other byproducts and inactives in the spoon. Water wash again same procedure. Add correct amount of citric acid + h2o + heat. Let cool. Filter and draw water soluble cylizine citrate into syringe.

Will work up amounts and reaction later. I realise it's sloppy and lazy and far from perfect. But surely better than injecting crushed pills???
 
Cyclizine Hcl + NaHCO3 = cylizine base + H2O + CO2

Cyclizine base + Citric acid = water soluble cyclizine citrate.

In a messy fashion. If I have more pills to play with I will post how I get on. Any tips appreciated in the mean time.
 
That would work, it's a classic chemistry trick to 'telescope' extractions/reactions without isolation of intermediates to improve yield...
 
Thanks sekio. One last question. Is it mole for mole for 0.3 moles?
I remember citric is a tribasic acid.
 
For NaOH and other "strong bases", try 0.33 mol acid per mol of base, plus at least 1 mol of acid for the cyclizine itself.

Be sure to test pH too.
 
Could I just inject the fact that in the UK, our 'analgesic of last defense' isn't diamorphine, it's Diconal. Diconal is a mixture of 10mg dipipanone (potent opioid and NMDA ligand) and 30mg of cyclizine. Back in the 80s, people would wash out the excipients by forcing solubilized 'strawberry milkshakes' through filters. Just load up barrel with pills, add hot water, force through cigarette filter... but there were and are 2 big problems. One is 'dirty hits' which were quite common and seizures which were VERY common. The cyclizine caused the seizures. I know this because people would buy Valoid (cyclizine) motion sickness tablets and shoot them alone, just for the cyclizine rush. This then led to people approximating a 'Dike' rush by adding cyclizine to methadone (with same results) and latterly with other 1st generation antihistamines.

Please don't think that someone that is OTC is automatically safer than illegal drugs. I have never seen a happy ending, I've seen too many people go over. LOTS of DVTs It really is a bad idea.

If it is for other uses, sorry to waste the space but please trust me, it is bad.
 
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