Abstract
The present study was designed to investigate the pharmacokinetics following oral
and intravenous administration of Riccardin D, an anticancer drug candidate isolated
from Chinese liverworts Dumortiera hirsute, in Wistar rats. An HPLC-MS/MS analytical method was developed and validated. The
results demonstrated that Riccardin D’s bioavailability was 13.4%, 11.4%, and 9.8%
after oral administration at 20 mg/kg, 40 mg/kg, and 80 mg/kg, respectively. There
was no significant difference in the elimination half-time of Riccardin D at these
doses, suggesting that Riccardin D may have linear pharmacokinetic characteristics
in rats. The metabolite of Riccardin D in rat was identified as the glucuronide of
Riccardin D. Riccardin D showed a wide distribution in various tissues followed by
a rapid elimination from most of the tissues tested. Riccardin D was found to distribute
widely in the tissues 0.5 h after oral and intravenous administration. The tissue
concentrations were markedly decreased 8 h and 6 h after oral and intravenous dosing,
respectively. Both Riccardin D and its conjugated metabolite were detected in urine
and bile samples while only Riccardin D was detected in feces. Taken together, the
study provided valuable pharmacokinetic data for further drug development of Riccardin
D.
Key words
Riccardin D - absorption - distribution - metabolism - excretion
