Scientists from the National Center for Natural Products Research at the University of Mississippi and Cambridge Health Alliance / Harvard Medical School report that, of the 23 vinpocetine supplements tested, six (or 26% of the products tested) did not contain any vinpocetine, while 17 contained vinpocetine with quantities ranging from 0.3 to 32mg per recommended daily serving.
For the 31 picamilon supplements tested, 30 contained picamilon in quantities ranging from 2.7 to 721.5mg per recommended daily serving, with no picamilon detected in one supplement.
“The newly developed UHPLC-PDA method facilitated the detection of vinpocetine and picamilon,” wrote the authors in Drug Testing and Analysis. “This method exhibited excellent performance in terms of sensitivity and is a suitable method for rapid analysis of vinpocetine and picamilon in dietary supplements.
“We found that consumers cannot obtain accurate information from supplement labels regarding the presence or quantity of vinpocetine and picamilon.”
Vinpocetine, a compound positioned for brain health formulations, is derived from vincamine obtained from the lesser periwinkle plant (Vinca minor L.) and there is evidence to support its role as a vasodilator – or increasing blood flow to the brain. It’s being investigated as a drug in many countries but is not permitted as a pharmaceutical in the US, instead being sold as a supplement.
Vinpocetine is considered a new dietary ingredient (NDI) after the FDA acknowledged notifications in the late 1990s from Amrion Inc (1997), Leiner Health Products (1998 & 1999), GNC (1999), and Pharmavite (1999). Vinpocetine is used in over 350 supplement brands, according to the Natural Medicines Comprehensive Database.
The American Herbal Products Association’s Botanical Safety Handbook (Second Edition, 2013) notes that there are no known side effects for Vinca minor L.
“Lesser periwinkle contains small amounts (0.02-0.13%) of the compound vincamine,” explains the Handbook. “Vincamine and the closely related compound vinpocetine have been widely studied, and vinpocetine is sold as a dietary supplement.”
Some supplement brands list vinpocetine as a constituent of lesser periwinkle on their product labels, said the researchers. However, it is not a constituent of the plant, they added, according to tests performed on dried leaves of Vinca minor L.
“Thirty-nine percent (9/23) of the vinpocetine supplements were misbranded because they either did not contain any vinpocetine or vinpocetine was represented as a natural constituent of lesser periwinkle,” wrote the authors, led by Dr Bharathi Avula. “Seventy-four percent (17/23) of the supplement labels did not provide any information on the quantity of vinpocetine.”
“For the 6 supplements that did list the quantity of vinpocetine on the label, the actual amount ranged from 95.6% to 107.4% of labelled content.
“Total amounts of vinpocetine that would be consumed daily based on recommended serving sizes varied almost 100-fold from 0.32 mg/day to 32 mg/day. These dosages range from trivial to prescription levels as vinpocetine is prescribed in dosages of 5 mg to 40 mg,” they wrote.
Picamilon (also known as nicotinoyl-GABA) is a derivative of GABA (gamma-aminobutyric acid) and nicotinic acid. It was reportedly developed by the All-Union Vitamin Research Institute in 1970 as a way of helping GABA cross the blood brain barrier, where it would exhibit anti-anxiety and anti-convulsant effects (orally consumed GABA on its own does not cross the blood brain barrier).
A search on PubMed for picamilon produces 48 results, with 39 of those being in Russian. A further five papers were published in Ukranian.
“While GABA and nicotinic acid are both found in nature, to our knowledge, picamilon has only been produced synthetically and has no known natural source,” wrote Dr Avula and her co-authors.
“The FDA has never approved picamilon for use in the USA, but picamilon is used in Russia to treat various neurological conditions,” they added.
Since no analysis has previously been published to assess “the accuracy of the information available on the label” of picamilon supplements, the researchers used the UHPLC-PDA method to assess 31 picamilon supplements purchased from two major retailers.
“In the 30 supplements that contained picamilon, the quantity of picamilon consumed by following the label's recommended maximum daily serving ranged from 2.7 mg/day to 721.5 mg/day,” they wrote. “These dosages range from trivial to exceeding prescription dosages.”
“Our study demonstrates that some pharmaceutical drugs prescribed in other countries are sold openly in dietary supplements in the USA,” wrote Avula et al. “The first step to sell a new ingredient in dietary supplements in the USA is to notify the FDA by submitting a New Dietary Ingredient notification.
“It is interesting to note that a notification for vinpocetine to be sold as a new ingredient in supplements was submitted to the FDA as early as 1997, but we are not aware of a similar notification for picamilon having been submitted to the FDA.”
Marianna Naum, PhD, strategic communications and public engagement staff in the Office of Foods and Veterinary Medicine at the FDA, told NutraIngredients-USA: “According to the FDA’s review, picamilon does not satisfy the definition of a dietary ingredient. Therefore, FDA does not consider picamilon to be either an old dietary ingredient or a new dietary ingredient.”
Source: Drug Testing and Analysis
Published online ahead of print, doi: 10.1002/dta.1853
“Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States”
Authors: B. Avula, A.G. Chittiboyina, S. Sagi, Y-H. Wang, M. Wang, I.A. Khan, P.A. Cohen