A rapid and sensitive LC/ESI–MS/MS method for quantitative analysis of docetaxel in human plasma and its application to a pharmacokinetic study

Docetaxel is a taxane family antineoplastic agent widely employed in cancer chemotherapy. We developed a liquid chromatography/tandem mass spectrometry method for the determination of docetaxel in human plasma. Plasma samples were deproteinized by acetonitrile containing internal standard paclitaxel. Chromatographic separation was performed on a TSKgel ODS-100V 3 μm (50 mm × 2.0 mm i.d.) column using a mobile phase composed of acetonitrile–methanol–water–formic acid (50:5:45:0.1, v/v/v/v). Detection was performed on a triple-quadrupole tandem mass spectrometer with multiple reaction monitoring (MRM) mode via electrospray ionization (ESI) source. This method covered a linearity range of 5–5000 ng/mL with the lower limit of quantification of 5 ng/mL. The intra-day precision and inter-day precision (R.S.D.) of analysis were less than 6.7%, and the accuracy (R.E.) was within ±9.0% at the concentrations of 5, 20, 200, and 2000 ng/mL. The total run time was 5.0 min. This method was successfully applied for clinical pharmacokinetic investigation.

► We developed a LC/ESI–MS/MS method for the determination of docetaxel in human plasma.
► One-step protein precipitation method was used for sample pretreatment without evaporation step.
► This method covered a linearity range of 5–5000 ng/mL with the lower limit of quantification of 5 ng/mL.
► The developed method was fully validated.
► This method was successfully applied for clinical pharmacokinetic investigation.