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Pharmacokinetics, tissue distribution and excretion study of dl-praeruptorin A of Peucedanum praeruptorum in rats by liquid chromatography tandem mass spectrometry.

Abstract
dl-Praeruptorin A (Pd-Ia), isolated from Chinese traditional herbal medicine Peucedanum praeruptorum Dunn, has been proved to be a novel Ca²+-influx blocker and K+-channel opener, and displayed bright prospects in prevention and therapy of cardiac diseases. The aim of this study was to investigate the pharmacokinetics, tissue distribution and excretion of Pd-Ia in rats following a single intravenous (i.v.) administration. The levels of Pd-Ia in plasma, tissues, bile, urine and feces were measured by a rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. The results showed that Pd-Ia was rapidly distributed and then eliminated from rat plasma and manifested linear dynamics in dose range of 5-20 mg/kg. The mean elimination half-life (t(½) of Pd-Ia for 5, 10 and 20 mg/kg dose were 57.46, 60.87 and 59.01 min, respectively. The major distribution tissues of Pd-Ia in rats were spleen, heart and lung, and low polarity enabled Pd-Ia to cross the blood-brain barrier. There was no long-term accumulation of Pd-Ia in rat tissues. Total recoveries of Pd-Ia within 24 h were low (0.097% in bile, 0.120% in urine and 0.009% in feces), which might be resulted from liver first pass effect.
AuthorsZ Zhang, Y Y Liu, M Q Su, X F Liang, W F Wang, X Zhu
JournalPhytomedicine : international journal of phytotherapy and phytopharmacology (Phytomedicine) Vol. 18 Issue 6 Pg. 527-32 (Apr 15 2011) ISSN: 1618-095X [Electronic] Germany
PMID21036581 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2010 Elsevier GmbH. All rights reserved.
Chemical References
  • Coumarins
  • Plant Extracts
  • praeruptorin A
Topics
  • Animals
  • Apiaceae (chemistry)
  • Bile (metabolism)
  • Blood-Brain Barrier (metabolism)
  • Brain (metabolism)
  • Chromatography, Liquid (methods)
  • Coumarins (metabolism, pharmacokinetics)
  • Feces (chemistry)
  • Half-Life
  • Lung (metabolism)
  • Male
  • Myocardium (metabolism)
  • Plant Extracts (metabolism, pharmacokinetics)
  • Rats
  • Rats, Sprague-Dawley
  • Spleen (metabolism)
  • Tandem Mass Spectrometry (methods)
  • Tissue Distribution
  • Urine (chemistry)

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