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romealone

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Jan 28, 2010
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Hello, I have a quick question about what Results when making a solution of Tianeptine free acid dissolved in a solution of water and sodium bicarb.

Tianeptine sodium is readily soluble in water but the free acid form is not. I did some research that said the free acid form can be dissolved in a solution of water/baking soda.

Indeed this does work, however I'm
Unsure as to whether the bicarb allows for better solubility in water, or if I have simply converted the free acid into the salt form when dissolving it in the bicarb solution.
 
On a related subject, I'm have a general question I'm hoping someone can elucidate. And while general, tianeptine serves as a perfect example for my question.

Many here have seen the horrific damage suffered by Russian addicts who inject 50+ pills of Tianeptine (Coaxil, Stablon, etc). However the waters get muddied with regards to the etiology of the resultant ischemia/necrosis as they are injecting the pills, usually poorly if at all filtered, and these pills contain some of the most dangerous fillers/binders (talc, silica, etc). So while there is NO question these fillers play a large role in these unfortunate cases, does Tianeptine itself, have inherent properties that make it likely that even pure Tianeptine sodium would be liable to cause similar complications?

So this is where my real question comes in-Tianeptine Sodium is extremely water soluble, however if one were to drop some of dissolved solution on their hand or anything else, they would find that it quickly dries and becomes a thin and extremely sticky glue.
Obviously injecting something that has glue-like properties sounds like a recipe for disaster, but since this only occurs when dry, would this property actually pose a threat when administered IV, as it's completely water soluble, and once in the venous system, I fail to see how it would "dry" and revert to its glue like state.

What do you guys think?
 
So this is where my real question comes in-Tianeptine Sodium is extremely water soluble, however if one were to drop some of dissolved solution on their hand or anything else, they would find that it quickly dries and becomes a thin and extremely sticky glue.
Click to expand...

So does glucose or sucrose (sugar). Stickiness is not a sign of toxicity.

It's easy to tell if the sodium salt forms: if a reaction occurs to form the salt, you'll see fizzing (CO2 bubbles) as the bicarbonate reacts. Otherwise you may need to use a stronger base like sodium carbonate.
 
sekio said:
So does glucose or sucrose (sugar). Stickiness is not a sign of toxicity.

It's easy to tell if the sodium salt forms: if a reaction occurs to form the salt, you'll see fizzing (CO2 bubbles) as the bicarbonate reacts. Otherwise you may need to use a stronger base like sodium carbonate.
Click to expand...

Well said. I didn't exactly have concerns that the sticky nature of the tianeptine sodium suggested it was toxic-the concern was more regarding what physical properties the tianeptine may take once in the bloodstream. As it's highly water soluble, I would expect that once in the vein, it remains dissolved and doesn't become a sticky mess within the vasculature. However, I will say that if one were to miss even a bit, a hard sub-q ball forms as it seems the tianeptine begins to solidy.

I'm really stuck on this one. The Russian epidemic cannot be used as a model for the dangers of IV tianeptine since it's unclear whether its the tianeptine itself, or rather the insoluble binders. Is there anything about tihr properties of tianeptine itself that you find to be cause for concern in terms of IV use, or do you not find anything to suggest it is likely to pose any more dangers than other water soluble drugs?

NOW...as far as your tip as to how to determine if the sodium had been made-
When 200mg tianeptine free acid (which is NOT water soluble) was added to a solution of water with a moderate concentration of sodium bicarbonate, the solution instantly became milky in color, DID NOT fizz, but did seem to completely dissolve with minimal stirring. This solution was placed briefly in the microwave and the solution became crystal clear, even after solution cooled.

This clear solution of the tian free acid dissolved in the sodium bicarbonate wart was passed through 0.22um filter and was found to be quite active.

So...according to your tip, no fizz means no sodium was made. I can accept that, but if the sodium was not formed, why did the tianeptine become soluble-is it that the free acid is soluble in aqueous sodium bicarbonate solution but not in pure water?

Thanks, as always, for your help.
 
Not soluble is a poor blanket term founded by misunderstandings, all drugs with ionizable functional groupz are soluble in water to an EXTENT. One charge usually accommodates 20-30 carbon atoms. In order to actually determine some degree of solubility we recognize the pka of Tianeptine, an amphoteric molecule, pka =4.4(acidic), pka =6.86(basic), in normal water it will probably exhibit intramolecular h bonding between the carboxylate anion(the carbon chain is an arm) and the positive N-methyl sulfonammonium (positive charge). This charge neutralized structure has poor solubility because of this paired ion effect. Thereby accommodating itself in the body for membrane transport.

In normal water though this may have occurred but a more likely scenario is that goo material is a combination of hydrates and wierd crystal polymorphism. This is very common with any drug if you evaporate on a thin layer or recrystalize with a different solvent yoy recieve a very different material in lattice structure.

Do not inject Tianeptine the drug is way too acidic do not even snort it, yoy will have a bad time, it hurts so bad,. Acidic drugs are not fun for membranes, they are more suited for them surviving the stomach(acidic) and ending up in the intestines (basic).

If you want a Tianeptine injectable safe ish drug you need to form prodrug and I doubt you have any acetic anhydride.
Zedz
 
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