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Pharmacokinetics and tissue distribution study of obtusifolin in rats by liquid chromatography–tandem mass spectrometry
Author(s) -
Huang Zhu,
Sun Qiao,
Hao Wenwen,
Zhao Junyu
Publication year - 2021
Publication title -
biomedical chromatography
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.4
H-Index - 65
eISSN - 1099-0801
pISSN - 0269-3879
DOI - 10.1002/bmc.5009
Subject(s) - chemistry , chromatography , pharmacokinetics , protein precipitation , analyte , electrospray ionization , mass spectrometry , tandem mass spectrometry , liquid chromatography–mass spectrometry , selected reaction monitoring , electrospray , high performance liquid chromatography , pharmacology , medicine
Abstract This paper reports the validation of an assay for obtusifolin based on liquid chromatography–tandem mass spectrometry (LC–MS/MS) and its application to a preclinical pharmacokinetic study in rats. After sample preparation of plasma and tissue homogenates by protein precipitation, the analyte and internal standard (IS) were separated by a reversed‐phase chromatographic system in a run time of 5.0 min and detected by negative ion electrospray ionization followed by selected reaction monitoring of the precursor‐to‐product ion transitions at m/z 283.0–268.1 for obtusifolin and m/z 329.0–314.1 for IS. The assay was linear in the concentration range 1.0–500 ng/ml with the LLOQ of 1.0 ng/ml. In the pharmacokinetic study of an intragastric administration of 1.3 mg/kg obtusifolin, the maximum plasma concentration of obtusifolin was 152.5 ± 62.3 ng/ml, reached at 0.39 ± 0.17 h. The AUC 0– t and AUC 0–∞ were 491.8 ± 256.7 and 501.7 ± 256.7 ng × h/ml, respectively, with an elimination half‐life of 3.1 ± 0.7 h. Obtusifolin was rapidly distributed into tissues, with the highest distribution in the liver and less in the brain. These results will give some insights for further pharmacological investigation of obtusifolin.