Comment · Sun, December 27, 2015 · Ceretropic & Nootropics Depot
Is anyone selling tianeptine SULFATE besides Ceretropic?
Original post in this thread
SickleInThePickle · 30 points
Not talking about the sodium version; everyone and their mother is selling that. As great as Ceretropic is, more vendors will naturally lead to competitive pricing. Is anyone selling the sulfate besides Ceretropic?
What they were answering
Jackolysis · 2 points
There's no evidence for this.
u/MisterYouAreSoDumb · Ceretropic & Nootropics Depot
There is no scientific human pharmacodynamic evidence for the powder itself. However, from the solubility differences, we can estimate the effects. Pair that with the thousands of anecdotes of people using it, and it is clear that it lasts longer for most people. It's all about the differences in solubility over ranges of pH.
From LiftMode:
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 substantial (implied by [this Tianeptine review article](http://link.springer.com/article
/10.2165/00023210-200115030-00006#page-1), [this GI absorption review article](faculty.mercer.edu/strom_jg/pha837/r_read/abs_3.pdf), etc)
*Tianeptine free acid: limited by rate to dissolve, but not by solubility, some degree of absorption expected
*Tianeptine hemisulfate: limited by rate to dissolve, on empty stomach may also be limited by solubility ceiling at low pH, less absorption expected
Solubility in near-neutral pH environments (such as small intestine)
*Tianeptine sodium: high (very high solubility in local area of high pH)
*Tianeptine free acid: 0.04 - 0.06 mg / mL (50mg requires about 1L = possible partial precipitation / eventual absorption)
*Tianeptine hemisulfate: 0.1 - 0.2 mg / mL (50mg remains dissolved in 250-500mL)
Main equilibrium form of undissolved solid in near-neutral pH environments (such as small intestine)
*Tianeptine sodium: Tianeptine free acid
*Tianeptine free acid: Tianeptine free acid
*Tianeptine hemisulfate: Tianeptine free acid
It's true, there would presumably be a lower ceiling on dissolved Tianeptine free acid concentration in the small intestine compared to Tianeptine hemisulfate. Thus if a particularly large amount of Tianeptine free acid were consumed p.o., the concentration of dissolved Tianeptine leaving the stomach might be high enough that some fraction of the Tianeptine free acid would precipitate during the pH change upon reaching the small intestine.
However, Tianeptine free acid is nonetheless soluble enough at near-neutral pH, the volume of fluid transiting and being reabsorbed by the small intestine per hour is high enough, the several hour transit time through the small intestine is long enough, and the mg quantities involved are low enough, that the Tianeptine free acid not dissolved and absorbed through the stomach (up to a few 100 mg) would likely be slowly and largely absorbed through the small intestine over the several hour transit time.
Tianeptine is high permeability, and Tianeptine free acid is low solubility at neutral pH, so solubility is the limiting factor for rate of absorption. The small intestine processes and reabsorbs 500mL - 1000mL of fluid per hour, a volume which is sufficient to dissolve 25mg - 50mg of precipitated Tianeptine free acid particles per hour at near-neutral pH. As absorption of dissolved Tianeptine free acid proceeded, any excess precipitated Tianeptine free acid would be expected to gradually but steadily come back into solution, maintaining a relatively stable concentration in the small intestine with a low ceiling that would lead to steady, prolonged absorption.
Most people would agree, it is not a good idea for people to absorb more than a few 100mg of Tianeptine over the course of a few hours. The limited solubility of Tianeptine free acid at near-neutral pH, allowing for not more than roughly 50mg to be absorbed through the small intestine per hour, might provide some degree of built in protection against highly excessive Tianeptine consumption relative to more soluble forms of Tianeptine such as Tianeptine sodium (which has massive solubility when present in amounts sufficient to raise the surrounding pH).
Similar to Tianeptine sulfate, Tianeptine free acid is stable and easy to store and handle relative to Tianeptine sodium. Its lack of solubility wards off the risk of certain dangerous forms of tianeptine abuse that have occasionally been noted. Tianeptine free acid would also likely be more compatible with sublingual use than Tianeptine sodium due to its noncaustic & low solubility characteristics.
So while using the patent for the controlled release tablets should not be used as direct evidence of it lasting longer, there is data out there to explain why it would. Pair that with the anecdotal reports, and there is certainly evidence that it lasts longer and is smoother in effects.