Background:
Ferruginol (FRGN) exhibits a broad range of pharmacological properties
which make it a promising candidate for chemoprevention. However, little is known about its absorption,
distribution, metabolism, excretion, and toxicity (ADMET) properties.
Methods:
A rapid, sensitive and specific HPLC-DAD method was established to quantify FRGN in the
plasma and tissues of Wistar rats. After extraction of FRGN with ethyl acetate (EtOAc), chromatographic
separation was performed on a YMC ODS C18 column (250 × 4.6 mm I.D., 5 µm) with a mobile
phase consisting of methanol-water (92:8, v/v) at a flow rate of 0.9 mL/min. Detection was conducted
with a wavelength of 273 nm at 25 °C.
Results:
The calibration curves for FRGN were linear in the concentration range of 0.5-20 µg/mL for
plasma, 0.5-10 µg/mL for heart, liver, spleen, lung, kidney, stomach, intestine, brain and muscle. After
three cycles of freezing and thawing, the concentration variations were within ± 7% of nominal concentrations,
indicating no significant substance loss during repeated thawing and freezing. The assay was
applied to pharmacokinetic and tissue distribution study in rats. Results suggested that lung, heart, liver,
spleen and kidney were the major distribution tissues of FRGN in rats, and FRGN could permeate the
blood-brain barrier to distribute in the brain of rats.
Conclusion:
The information provided by this research is very useful for gaining knowledge of the
pharmacokinetic process and tissue distribution of FRGN.
Simultaneous Determination of Vinpocetine and its Major Active Metabolite Apovincaminic Acid in Rats by UPLC-MS/MS and its Application to the Brain Tissue Distribution Study
