Method development and validation of bicalutamide an anti-prostate anticancer drug in rat plasma by using UPLC-MS/MS-ESI method and application to pharmacokinetic study

Abstract A simple, rapid, sensitive, and selective liquid chromatographic method using a tandem mass spectrometer was developed and validated for quantification of Bicalutamide in rat plasma, with Telmisartan as the internal standard (IS). The method employs protein precipitation extraction to isolate the drug and IS from rat plasma. Chromatographic separation was achieved on Waters XBridge C18 (75 × 4.6 mm ID, 3.5 μm particle size) column, using mobile phase consisted of acetonitrile (Phase A) and formic acid (Phase B) in an 80:20 v/v ratio, with a flow rate of 0.80 mL min −1 was employed. The set column oven and autosample cooler temperatures were 40 and 5 °C, respectively. The multiple reaction monitoring (MRM) transitions were m / z 429.08 → 254.90 for Bicalutamide and m / z 513.54 → 287.30 for the IS, providing high selectivity in the analysis. The method demonstrated excellent linearity and selectivity in the range of 0.995–1290.105 ng mL −1 , with a lower limit of quantification (LLOQ) of 0.9 ng mL −1 . The method met ICH guidelines for selectivity, sensitivity, precision, accuracy, and stability. The developed method has successfully applied to report the pharmacokinetic parameters of Bicalutamide in rats.