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Comment · Tue, June 2, 2015 · Ceretropic

Tianeptine free acid

Original post in this thread

Suck_a_gerbils_dick · 7 points

So, newmind was out of tianeptine sodium and the only form I could buy was the free acid. Now, I've read some disturbing reports online that it isn't active? Please, tell me this isnt true and it just has lower bioavailability?

Thanks in advance for answers.

What they were answering

liftmode · 4 points

In the Tianeptine sulfate patent, reference is made to the Form II polymorph of Tianeptine (free acid) - also referenced in Tianeptine free acid patent.

The takeaway:

Tianeptine is a high permeability molecule. Biopharmaceutics_Classification_System

*Tianeptine sodium is Class I
*Tianeptine free acid is Class II
*Tianeptine hemisulfate is borderline Class I / Class II

Speed to Physically Dissolve when in contact with water:

*Tianeptine sodium: Rapid (swift physical disintegration, very high solubility in local area of high pH)

*Tianeptine free acid: Slow

*Tianeptine hemisulfate: Slow

Solubility in low pH, high HCl environments (such as stomach)

*Tianeptine sodium: high (very high solubility in local area of high pH)

*Tianeptine free acid: 1 - 3 mg / mL (50mg completely but slowly dissolves in about 25mL)

*Tianeptine hemisulfate: 0.2 - 0.3 mg / mL (50mg completely but slowly dissolves in about 200mL)

Main equilibrium form of undissolved solid in low pH, high HCl environments (such as stomach)

*Tianeptine sodium: Tianeptine free acid

*Tianeptine free acid: Tianeptine free acid

*Tianeptine hemisulfate: Tianeptine hemisulfate

Absorption through stomach

*Tianeptine sodium: rapid and…

u/MisterYouAreSoDumb · Ceretropic

Excellent explanation! Good work on all the absorption research. We can certainly agree that keeping absorption slow and steady is best. Too many people are abusing Tianeptine Sodium right now. I hope it does not become an issue.

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