Biopharmaceutical and pharmacokinetic characterization of matrine as determined by a sensitive and robust UPLC-MS/MS method

Zhen Yang, Song Gao, Taijun Yin, Kaustubh H. Kulkarni, Yang Teng, Ming You, Ming Hu

Research output: Contribution to journalArticlepeer-review

37 Scopus citations


The purpose of this research was to develop a sensitive and reproducible UPLC-MS/MS method to analyze matrine, an anticancer compound, and to use it to investigate its biopharmaceutical and pharmacokinetic behaviors in rats. A sensitive and fast UPLC-MS/MS method was successfully applied to determine matrine in rat plasma, intestinal perfusate, bile, microsomes, and cell incubation media. The absolute oral bioavailability of matrine is 17.1 ± 5.4% at a dose of 2 mg/kg matrine. Matrine at 10 μM was shown to have good permeability (42.5 × 10-6 cm/s) across the Caco-2 cell monolayer, and the ratio of PA-B to PB-A was approximately equal to 1 at two different concentrations (1 and 10 μM). Perfusion study showed that matrine displayed significant differences (P < 0.05) in permeability at different intestinal regions. The rank order of permeability was ileum (highest, Pw = 6.18), followed by colon (Pw = 2.07), duodenum (Pw = 0.61) and jejunum (Pw = 0.52). Rat liver microsome studies showed that CYP and UGTs were not involved in matrine metabolism. In conclusion, a sensitive and reliable method capable of measuring matrine in a variety of matrixes was developed and successfully used to determine absolute oral bioavailability of matrine in rats, transport across Caco-2 cell monolayers, absorption in rat intestine, and metabolism in rat liver microsomes.

Original languageEnglish (US)
Pages (from-to)1120-1127
Number of pages8
JournalJournal of Pharmaceutical and Biomedical Analysis
Issue number5
StatePublished - Apr 6 2010


  • Caco-2 cells
  • Matrine
  • Microsomes
  • Pharmacokinetics
  • Rat intestine perfusion

ASJC Scopus subject areas

  • Analytical Chemistry
  • Pharmaceutical Science
  • Drug Discovery
  • Spectroscopy
  • Clinical Biochemistry


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