Abstract
Panaxadiol is a novel antitumor agent extracted from the Chinese medical herb
Panax ginseng. This agent is being developed for the treatment of
tumor diseases. A rapid, selective, and simple method based on ultrafast
liquid chromatography-tandem mass spectrometry was established and validated
to determine panaxadiol in rat plasma following oral and sublingual
intravenous administration of panaxadiol. The plasma samples were pretreated
with acetic ether, and chromatographic separation was achieved on a
Shim-pack XR-ODS III column using isocratic elution with the mobile phase of
0.1 % formic acid and acetonitrile. Analytes and protopanaxadiol (internal
standard) were analyzed and identified using electrospray positive
ionization mass spectrometry in the multiple reaction-monitoring mode. The
MS/MS detection was carried out by monitoring the fragmentation of
m/z 461.45 → m/z 127.1 for panaxadiol and m/z 425.4
→ m/z 95.1 for protopanaxadiol (internal standard) on a
triple-quadrupole mass spectrometer. The result showed good linearity over a
wide concentration range (0.1–20 ng/mL) (R2 > 0.999) and its
lower limit of detection and quantification were 0.03 and 0.1 ng/mL,
respectively. The intra- and interday precision (RSD %) was within 15 % and
the accuracy ranged from 94.9 % to 112.0 %. The absolute bioavailability was
12.5 %. The method was fully validated and successfully applied to the
pharmacokinetic study of a single dose of panaxadiol.
Key words
Panax ginseng
- Araliaceae - panaxadiol - UFLC-MS/MS - pharmacokinetics