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.