Open Access

Peer-reviewed

Research Article

Main Article Content

Xinghua Zhaocorresponding author
Jiaojiao Zhang
Yutong Liang
Jie Li
Shi Ding
Yang Wang
Ye Chen
Ju Liu

Abstract

Purpose: A simple, sensitive and specific HPLC–MS/MS method was established to analysis the pharmacokinetics of CB1107 in mouses. Methods: A simple, selective, and sensitive high-throughput liquid chromatography-tandem mass spectrometry (LC-MS-MS) method has been developed and validated for quantitative determination of CB1107 in rat serum.Chromatographic separation was achieved on a Zorbax Extend C18 Rapid Resolution HD column (4.6 mm × 50 mm, 1.8 μm). The column temperature was maintained at 35℃ and at flow rate of 0.6 mL/min. Injection volume was 20 μL. The mobile phases consisted of 0.1% formic acid in water (mobile phase A)and 0.1% formic acid in acetonitrile (mobile phase B), and total run time was 30min. MS-MS detection was performed in the selected monitoring mode of electrospray positive ionization reaction. Results: The pharmacokinetic characteristics of CB1107 in mice belong to the two-compartment model.When the doses were 400 mg/kg, 600 mg/kg and 800 mg/kg, corresponding area under the plasma concentration-time curve (AUC) respectively were 20.011±1.24 mg/h/L, 26.778±2.19 mg/h/L, 38.82±1.44 mg/h/L, suggesting that CB1107 have a good absorption in the body.And the AUC of three doses are proportional, indicating that CB1107 conforms to linear pharmacokinetics in vivo. Conclusion: This method was successfully applied to study the pharmacokinetics at three different doses of CB1107 after oral administration in mouses. In this study, the bioactivity mechanism of CB1107, by the pharmacokinetic investigation of CB1107 in vivo.

Keywords
chronic myelogenous leukemia, Cyclobentinib (CB1107), pharmacokinetics

Article Details

Supporting Agencies
This work was supported by the Science and technology plan project of Shenyang (Grant No. 18-006-9-02).
How to Cite
Zhao, X., Zhang, J., Liang, Y., Li, J., Ding, S., Wang, Y., Chen, Y., & Liu, J. (2021). Pharmacokinetics study of potential anti-CML drug Cyclobentinib (CB1107) by HPLC–MS/MS. Journal of Pharmaceutical and Biopharmaceutical Research, 3(1), 169-175. https://doi.org/10.25082/JPBR.2021.01.001

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