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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2020, Vol. 25 ›› Issue (10): 1105-1110.doi: 10.12092/j.issn.1009-2501.2020.10.004

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Pharmacokinetics and tissue distribution characteristics of sunitinib#br#

CHEN Aiying, CHENG Min, MIAO Yunping, YE Xiaodi, TIAN Xuejun, ZHENG Gaoli   

  1. Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province, Institute of Medica Materia, Zhejing Academy of Medicine, Hangzhou 310013, Zhejiang, China
  • Received:2019-11-25 Revised:2020-05-22 Online:2020-10-26 Published:2020-11-03

Abstract: AIM: To establish a HPLC-UV method to determine sunitinib in rat plasma and mouse tissues, and to study its pharmacokinetics in rats and tissue distribution characteristics in mice.  METHODS: The biotic samples were prepared by protein precipitation followed by a stereoselective analysis of sunitinib was achieved on Waters XBridgeTM C18 (4.6 mm×250 mm, 5 μm) with a mobile phase composing of methanol-0.02 mol/L sodium dihydrogen phosphate (70∶30) at a flow rate of 1.0 mL/min. The detection wavelength was 310 nm, and the column temperature was 25 ℃. RESULTS: The calibration curve for rat plasma sunitinib was linear in the range of 0.019 2-15.34 μg/mL. The linear ranges in mice brain and kidney were 0.038 3-11.50 and 0.038 3-69.00 μg/mL, respectively. After intragastric administration of sunitinib at a dose of 20 mg/kg to rats, the pharmacokinetic characteristics were Tmax=9.0 h, Cmax=0.194 mg/L, t1/2=18.4 h, AUC(0-∞)=6.8 mg·L-1·h. And the absolute bioavailablity was 47.1%. It was indicated that sunitinib could permeate the blood brain barrier, but the concentration was lower in brain and higher in kidney. CONCLUSION: A HPLC-UV method for the determination of sunitinib in rat plasma and mouse tissues was established. The method is simple, rapid, reliable, and provides a reference for the clinical application of sunitinib.

Key words: HPLC-UV,  sunitinib, pharmacokinetics, tissue distribution, chromatographic condition

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