Determination and pharmacokinetic study of pirfenidone in rat plasma by UPLC-MS/MS

作者：Sun Wei; Jiang Zhe li; Zhou Lei; Chen Rui min; Wang Zhe; Li Wan shu; Jiang Shuo min; Hu Guo xin; Chen Rui jie^*

来源：Journal of Chromatography B-Analytical Technologies in the Biomedical and Life Sciences, 2015, 981: 14-18.

DOI：10.1016/j.jchromb.2014.12.027

• Pirfenidone
• UPLC-MS/MS
• Rat plasma
• Pharmacokinetics

A rapid, sensitive and selective ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) was developed and validated for the determination and pharmacokinetic investigation of pirfenidone in rat plasma. Sample preparation was accomplished through a simple one-step deproteinization procedure with 0.2 mL of acetonitrile to a 0.1 mL plasma sample. Plasma samples were separated by UPLC on an Acquity UPLC BEH C18 column using a mobile phase consisting of acetonitrile-0.1% formic acid in water with gradient elution. The total run time was 3.0 min and the elution of pirfenidone was at 1.39 min. The detection was performed on a triple quadrupole tandem mass spectrometer in the multiple reaction-monitoring (MRM) mode using the respective transitions m/z 186.2 -> 92.1 for pirfenidone and m/z 237.1 -> 194.2 for carbamazepine (IS), respectively. The calibration curve was linear over the range of 5-2000 ng/mL with a lower limit of quantitation (LLOQ) of 5 ng/mL. Mean recovery of pirfenidone in plasma was in the range of 80.4-84.3%. Intra-day and inter-day precision were both <12.1%. This method was successfully applied in pharmacokinetic study after oral administration of 10.0 mg/kg pirfenidone in rats.

• 出版日期2015-2-15
• 单位温州医科大学