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LC–MS–MS Quantitative Determination of Gefitinib in Human Serum and Cerebrospinal Fluid

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Abstract

A specific, sensitive, and rapid method based on high-performance liquid chromatography coupled to tandem mass spectrometry (LC–MS–MS) was developed for determination of gefitinib in human serum and cerebrospinal fluid (CSF). The analyte was detected by tandem mass spectrometry operating in positive electrospray ionization mode with multiple reaction monitoring (MRM). Gefitinib was extracted from serum or CSF samples with ethyl acetate using icotinib as internal standard. The method was validated over the concentration range of 1.00–1,000 ng mL−1 in human serum and 0.05–50.0 ng mL−1 in CSF. For both matrices, inter- and intraday precision (CV%) were less than 15% and accuracy was within 85–115%. Average extraction recoveries were 78.9 and 61.8% in human serum and CSF, respectively. Linearity, recovery, matrix effects, and stability were validated in the two matrices. The method was successfully used for analysis of clinical samples from lung cancer patients with brain metastases treated with gefitinib in the dosage range of 250–500 mg day−1.

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Correspondence to Qian Zhao or Wei Zhong.

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Zheng, X., Hu, P., Liu, J. et al. LC–MS–MS Quantitative Determination of Gefitinib in Human Serum and Cerebrospinal Fluid. Chromatographia 74, 41–49 (2011). https://doi.org/10.1007/s10337-011-2042-2

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  • DOI: https://doi.org/10.1007/s10337-011-2042-2

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