Title:Quantitative Determination of Quercitrin Levels in Rat Plasma Using
UHPLC-MS/MS and its Application in a Pharmacokinetic Study after the
Oral Administration of Polygoni cuspidati Folium Capsules
Volume: 23
Issue: 3
Author(s): Shi-tang Ma , Xin-yuan Zhang , Ning Zhang , Xiao-lin Bi *Cheng-Tao Feng *
Affiliation:
- College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China
- School of Chemical Engineering, Anhui University of Science and Technology,
Huainan, 232001, China
Keywords:
Polygoni cuspidati folium capsules, quercitrin, UHPLC-MS/MS, pharmacokinetics, plasma, spectrometry.
Abstract: Background: Quercitrin is widely found in herbal medicines, and it is particularly important
in the design of new therapeutic agents. Because of its wide range of biological activities, methods for
detecting quercitrin and its pharmacokinetics in biological samples must be investigated.
Objectives: To develop and validate a sensitive and reliable ultra-high-performance liquid chromatography-
tandem mass spectrometry (UHPLC-MS/MS) method for the quantitative determination of quercitrin
levels in rat plasma, and test its application in a pharmacokinetic investigation after the oral administration
of Polygoni cuspidati folium capsules (HC).
Methods: First, a rapid analytical method implementing UHPLC-MS/MS for the quantification of quercitrin
levels in rat plasma was developed and validated. The analyte and internal standard (IS) tinidazole
were extracted from rat plasma via protein precipitation with 800 μL of methanol and 50 μL of 1% formic
acid solution. Chromatographic separation was performed using an Agilent ZORBAX C18 column
within 4 min. Mass spectrometry was performed for quantification using a triple-quadrupole mass spectrometer
employing electrospray ionization in the negative ion mode. The MRM transitions for quercitrin
and IS were m/z 447.2→229.9 and m/z 246.0→125.8, respectively. The UHPLC-MS/MS method
for the quantitative determination of quercitrin levels in rat plasma was then applied to investigate its
pharmacokinetics after the oral administration of HC in rats.
Results: The developed UHPLC-MS/MS method for detecting quercitrin in rat plasma was linear over
the range of 0.1–160 ng/mL. The linear regression equation was Y = (0.7373 ± 0.0023)X − (0.0087 ±
0.0021) (r2 = 0.9978). The intra- and interday precision values were within 7.8%, and the recoveries of
quercitrin and IS exceeding 67.3%. The UHPLC-MS/MS method was successfully applied to characterize
the pharmacokinetic profile of quercitrin in eight rats after the oral administration of HC. The experimentally
obtained values were fit to a one-compartment, first-order pharmacokinetic model, and they
appeared to fit the concentration–time curve.
Conclusion: Quercitrin was proven to be stable during sample storage, preparation, and the analytical
procedures. The pharmacokinetic parameters suggested that quercitrin may be present in the peripheral
tissues of rats.