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Online Journal of Veterinary Research

Volume 25(1): 46-60, 2021.

Pharmacokinetics of anti-allergenic and anti-inflammatory bioactives

in nettle Urtica dioica extract oral lozenge in female volunteers


Ayers S, Roschek B Jr, Williams JM, Alberte RS.


Herbal Science Group LLC., Naples FL 34110, USA.




Ayers S, Roschek B Jr, Williams JM, Alberte RS., Pharmacokinetics of anti-allergy and inflammation bioactives in nettle extract Urtica dioica lozenge in female volunteers, Onl J Vet Res., 25 (1): 46-60, 2021. We report pharmacokinetics by Direct Analysis in Real Time Time-of-Flight Mass Spectrometry (DART TOF-MS) uptake of bioactives in a nettle (Urtica dioica) extract delivered orally as a lozenge. In five female healthy subjects, average serum concentrations of adenine reached 35.2 nmol L-1, nicotinamide 8.7 nmol L-1, osthole 11.0 nmol L-1 and synephrine 107.4 nmol L-1 equivalent to 0.3%, 0.2%, 0.2%, and 1.6% oral bioavailability. Urine concentrations reached 4.9 nmol L-1 adenine, 2.5 nmol L-1 nicotamide, 6.6 nmol L-1 osthole and 0.2 nmol L-1 synephrine. Cmax decreased 2-16 fold in urine compared with serum, Tmax increased 2-12 fold, and T1/2 by 2-10-fold. Molecular modeling suggested these compounds were not likely to cross the blood-brain barrier to avoid drowsiness. Our findings suggest that anti-inflammatory and anti-allergenic compounds in nettle are readily absorbed and excreted when given in an oral lozenge. DART TOF-MS is useful in quantifying multiple components in biological matrices with little or no sample preparation.


Key Words: Urtica dioica, nettle, allergies, inflammation, DART TOF-MS.