Pharmacokinetics and bioavailability study of polydatin in rat plasma by using a LC–MS/MS method

To investigate the pharmacokinetic and bioavailability of polydatin (pd) in rats after oral and intravenous administration, a simple, rapid and sensitive liquid chromatography-tandem mass spectroscopy (lc-ms/ms) method was developed and validated for the determination of polydation. after precipitating the plasma proteins with methanol, the analytes were separated on a c18 column (3.5μm, 2.1×100 mm) with an isocratic mobile phase consisting of methanol-acetonitrile-0.1% formic acid (18: 15: 67, v/v/v) at a flow rate of 0.3ml/min. the agilent g6410a triple quadrupole lc/ms system was operated under the multiple reaction monitoring (mrm) mode and the electrospray ionization technique was in negative mode. linear responses were obtained for pd ranging from 1.0-5000.0 ng/ml (r= 0.9984) and the lloq was 1.0ng/ml and was sufficient for the pharmacokinetic studies. the intra-day and inter-day accuracy and precision of the assay were less than 8.0%. the method is capable of quantifying pd. the pharmacokinetic parameters of polydatin after intragastric administration of pd with different doses (50, 100 and 300 mg/kg) and intravenous administration at the dose of 20 mg/kg, were obtained, with t1/2 of 200.30 min, 210.30 min, 272.26 min, and 112.5 min, and auc0-∞ of 125626.41 μg/l· min, 250433.47 μg/l·min, 693722.60 μg/l· min and 1723509.57μg/l· min, respectively. the absolute bioavailability of pd was somewhat low to 2.9%. the results were firsly reported, as far as we know, about bioavailability of pd and seem important for linking pd and other phenolic glycosides-related drugs administration to their medicinal effects.