Tuesday, December 18, 2007

R-Lipoic Acid Pharmacokinetics in Humans.

Remember my previous blog post with pictures from Aug 9th about participating in a R-lipoic pk study at Geronova? Well the results are now published. Here is the PDF of the Human R-Lipoic Pharmacokinetic Study. (Also available on PubMed at this link: PK Study)

It is important to note this paper is co-authored by the "father" of modern lipoic and antioxidant research, Dr. Lester Packer - Dept of Pharmacology and Pharmaceutical Sciences, University of S. California and by Dr. Anthony R Smith of the Linus Pauling Institute, an expert in the use of RLA for vascular disease and author of seven peer reviewed papers.


Unstabilized (pure) r-lipoic (as found in most r-lipoic supplements) barely registered plasma levels above baseline(!), and "is not suitable for use in pharmaceutical or nutraceutical supplements".

Geronova's NaRLA provides a quick, high plasma peak. Much more so than than an unstabilized r-lipoic (anything other than manufactured by Geronova) or an alpha-lipoic acid. This is a good thing and thought to trigger the metabolic switches the same as exercise does.

Lipoic Acid is now being considered much more as a "stressor" (stimulation of Phase II and antioxidant response elements, not "stress" like emotional stress) than as an antioxidant. Provoking this cellular stressing is thought to offer anti-aging benefits.

"RESULTS: As anticipated from the preliminary study, NaRLA is less prone to polymerization, completely soluble in water, and displays significantly higher Cmax and AUC values and decreased time to maximum concentration (Tmax) and T1/2 values than RLA or rac-LA."

NaRLA is used in the formulation of Geronova's:

K-RALA (100 mg capsules) and K-RALA 300 mg capsules.
R-PLUS Curcumin
R-PLUS N-Acetyl-Cysteine

In case you were wondering, Geronova natural sustained release lipoic acid products work synergistically and with a somewhat different mechanism than the quick release products above. The natural sustained release products are:

R-PLUS and R-PLUS 120 count

The researcher's current opinion (when I asked them) is that it is preferable to combine both a quick release r-lipoic with a natural sustained release product in your supplement regimen to achieve maximum benefits.

Your purchase of these products supports and enables the kind of research usually only done by pharmaceutical companies. Geronova is the world leader in lipoic technology.

Closing anecdote: I was subject number 6 in the pk study. Of note, my lipoic plasma peak (Cmax) was 2-3 times as high as the other participants. More testing is planned in 2008.

Oops, late edit: Want to discuss this post? Log in to the Relentless Improvement Lipoic Acid Forum!