3 replies to this topic

[Linux]

Understanding the physicochemical properties and degradation kinetics of nicotinamide riboside, a promising vitamin B3nutritional supplement

 

"Nicotinamide riboside (NR), a newly recognised form of vitamin B3 and a precursor to nicotinamide adenine dinucleotide (NAD+), has been demonstrated to show therapeutic potential and the possibility of becoming a drug compound in addition to its proven role in rejuvenating ageing cells in mice.

 

However, current literature is devoid of information relating to the physicochemical characterisation of NR and its respective impact upon formulation and final product processing. 

 

A simple and rapid HPLC method confirms a base-catalysed hydrolysis degradation of nicotinamide riboside chloride (NRCl) to nicotinamide and sugar in simulated gastrointestinal (GI) fluids. Given the antagonising effect of nicotinamide against NR, the presented data have a profound impact on how NRCl should be handled both during formulation and storage to prevent formation and to limit accumulation of nicotinamide."

 

• In this paper, key physicochemical properties of NR including pKa, log P, solubility, melting point, degradation mechanics, and kinetics, with a special focus on its stability under thermal and physiologically relevant conditions, were investigated.

 

• The results have shown that NRCl is a labile molecule that degrades to form a possibly antagonistic product when exposed to either gastric fluid or elevated temperature.

 

https://www.ncbi.nlm...les/PMC6878970/

Edited by Linux, 07 December 2019 - 01:49 PM.

[able]

Those quotes sound bad for NR, but those were in reference to testing at 55,65,or 75 Centigrade.

 

At body temperatures it is not so bad.

 

At 2 hours in simulated Intestinal fluid,  over 93% NR survived.

 

2 hours in simulated gastric fluids, over 97% NR survived.

 

In human body, NR might see 2 hours of gastric fluid, then a few hours of intestinal fluid.  

 

Would a fair approximation be that adding those 2 together and you would see something like 90% NR survive the GI tract of humans?

 

In the three gastric simulated fluids tested, NRCl displayed very little degradation under physiological temperature and agitation of 75rpm. After 2 h, there was 97.64 ± 0.08%, 98.59 ± 0.10%, and 97.17 ± 0.19% of NRCl remaining in HCl, USPSGF without pepsin, and USPSGF, respectively (Fig. 6A). More pronounced degradation was observed in the simulated intestinal fluids. After 2 h, there was 94.32 ± 1.16% NRCl remaining in intestinal SIF and 94.71 ± 2.66% remaining in USP SIF, respectively. Another 2 h exposure to the same SIFs resulted in 92.71 ± 0.81% and 93.54 ± 2.37% remaining NRCl content in the respective medium (Fig. 6B). In the 24-h GI simulation experiment, there was 90.51 ± 0.82% remaining after 8 h and 79.18 ± 2.68% remaining by the final time point at 24 h (Fig. 6C).

 

Edited by able, 07 December 2019 - 04:13 PM.

[MikeDC]

Those quotes sound bad for NR, but those were in reference to testing at 55,65,or 75 Centigrade.

At body temperatures it is not so bad.

At 2 hours in simulated Intestinal fluid, over 93% NR survived.

2 hours in simulated gastric fluids, over 97% NR survived.

In human body, NR might see 2 hours of gastric fluid, then a few hours of intestinal fluid.

Would a fair approximation be that adding those 2 together and you would see something like 90% NR survive the GI tract of humans?

I agree with you on this. The headline is misleading. The results are much better than expected.

[Linux]

The authors reinforce the need for more stable formulations of NR than the current labile formulations that degrades into nicotinamide post stomach in the GI-tract.

”While there appears to be negligible degradation of NR in simulated gastric media, this was to be expected according to the predicted degradation scheme.

However, there appears to be significant degradation in simulated intestinal media due to the increased pH of these simulated environments.”

AND

”NR has significant potential as a nutritional supplement.

However, here we have reported that NR is a labile molecule with defined and absolute upper limits for processing and handling.

An active effort must be made to preclude breakdown of the NR molecule during the development of new NR products and upon its delivery for supplementation.

NR is predicted to not be stable in the GI tract, post stomach transit.”

Edited by Linux, 24 December 2019 - 10:09 AM.