title: Pharmacokinetics and bioavailability study of polydatin in rat plasma by using a LC-MS/MS method.
abstract: 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.
authors.affiliation: Department of Pharmacy, Shanghai First People's Hospital, Shanghai Jiao Tong University, Shanghai, China.
authors.forename: Xueying
authors.initials: X
authors.lastname: Ding
authors.affiliation: Laboratory of Toxicology &amp; Pharmacology, Faculty of Tropical Medicine and Public Health, The Second Military Medical University, Shanghai, China.
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Hou
authors.affiliation: Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai, China.
authors.forename: Shouhong
authors.initials: S
authors.lastname: Gao
authors.affiliation: Laboratory of Toxicology &amp; Pharmacology, Faculty of Tropical Medicine and Public Health, The Second Military Medical University, Shanghai, China.
authors.forename: Mingxue
authors.initials: M
authors.lastname: Sun
authors.affiliation: China-Japan Union Hospital of Jilin University, Changchun, China.
authors.forename: Fengwu
authors.initials: F
authors.lastname: Lin
authors.affiliation: Department of Pharmacology, School of Pharmacy, Second Military Medical University, Shanghai, China.
authors.forename: Guojun
authors.initials: G
authors.lastname: Cai
authors.affiliation: Laboratory of Toxicology &amp; Pharmacology, Faculty of Tropical Medicine and Public Health, The Second Military Medical University, Shanghai, China.
authors.forename: Kai
authors.initials: K
authors.lastname: Xiao
mesh_terms: D000818:Animals; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004355:Drug Stability; D005960:Glucosides / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D013267:Stilbenes / Q000737:chemistry / Q000493:pharmacokinetics*; D053719:Tandem Mass Spectrometry / Q000379:methods*
chemical_list: D005960:Glucosides; D013267:Stilbenes; C058229:polydatin