Pharmacokinetics and tissue distribution of a bioactive sesquiterpenoid from Polygonum jucundum following oral and intravenous administrations to rats.

Polygonum jucundum is a traditional Chinese medicine used for the treatment of diseases. The major bioactive compound in the ethanol extract of P. jucundum is 2α-hydroxyl-3β-angeloylcinnamolide (HAC), a drimane-type sesquiterpenoid, which possesses anti-inflammatory activities. The purpose of this study was to investigate in vivo pharmacokinetics and tissue distribution of HAC after oral and intravenous administrations to rats by using a reversed-phase high performance liquid chromatography in conjunction with mass spectrometry (LC-MS). Chromatographic separation was achieved on a C18 column within 8 min. Quality control samples for both tissues and plasma demonstrated accuracy and precision within 94.59-107.74% of the nominal values and 1.65-10.77% relative standard derivative (RSD), respectively. The pharmacokinetic profiles, estimated by using non-compartment models, revealed that HAC was rapidly absorbed into the systemic circulation and was widely distributed throughout the body, followed by a rapid elimination phase. The highest amount of HAC was found in kidney, followed in order by lung, heart, spleen and liver. The current paper was the first report on the pharmacokinetic profiles of HAC in rat plasma and tissues after oral and intravenous administrations. It could provide a meaningful insight for the clinical applications of this bioactive compound extracted from the traditional Chinese medicine.