Bioavailability and safety study of resveratrol 500 mg tablets in healthy male and female volunteers

Sergides,Christakis; Chirilă,Marinela; Silvestro,Luigi; Pitta,Daphne; Pittas,Andreas

doi:10.3892/etm.2015.2895

Bioavailability and safety study of resveratrol 500 mg tablets in healthy male and female volunteers

Authors:
- Christakis Sergides
- Marinela Chirilă
- Luigi Silvestro
- Daphne Pitta
- Andreas Pittas
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Affiliations: Research and Development Department, Medochemie Ltd., Limassol 3011, Cyprus, Medical Team Department, Medochemie Ltd., Bucharest 011437, Romania, Mass Spectrometry Laboratory, S‑Pharmacological Consultation and Research GmbH, Harpstedt 27243, Germany
Published online on: November 25, 2015 https://doi.org/10.3892/etm.2015.2895
Pages: 164-170

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Abstract

Over the past few decades, trans-resveratrol has received widespread attention as a preventive agent for numerous diseases. Several studies have demonstrated that it has significant biological and pharmacological properties. Trans-resveratrol has been reported to possess anti-oxidant, anti-inflammatory, anticarcinogenic, antidiabetic, anti‑aging, cardioprotective and neuroprotective properties, which can be relevant in chronic diseases and longevity in humans. The aim of the present study was to investigate the rate and extend of absorption, and also the safety of resveratrol following a single 500 mg oral dose. This was an open label, single dose, one period, bioavailability study in 15 healthy volunteers under fasting conditions. Blood samples were collected at predefined time points up to 24 h after resveratrol administration, and plasma concentrations of resveratrol and its conjugated (glucuronated and sulphated) metabolites were determined using a validated high performance liquid chromatography/tandem mass spectrometry method. Pharmacokinetic parameters, including Cmax, AUC0‑t, AUC0‑inf, Tmax, T1/2 and MRT, were determined from plasma concentration‑time profiles and found to be in good agreement with previously reported data. Cmax and AUC0‑inf were lower for resveratrol when compared with the values for its glucuronated and sulphated metabolites. Cmax for resveratrol, glucuronated resveratrol and sulphated resveratrol were 71.2±42.4 ng/ml, 4,083.9±1,704.4 ng/ml and 1,516.0±639.0 ng/ml, respectively, while the AUC0‑inf values were 179.1±79.1 ng/ml, 39,732.4±16,145.6 ng/ml and 14,441.7±7,593.2 ng/ml, respectively. No adverse reactions associated with resveratrol were reported during the study. The plasma concentrations of resveratrol (free and conjugated) were in agreement with those mentioned in the literature, and were adequate to promote the pharmacological activities of resveratrol. In conclusion, resveratrol 500 mg tablets were well-tolerated by all participants of the study.

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