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Title: A rapid and sensitive UHPLC–MS/MS method for quantification of 83b1 in plasma and its application to bioavailability study in rats
Authors: Wen, D
Guo, J
Jiang, F
Huang, C
Zhao, Z
Lu, G
Chen, J
Qin, L
Li, Z
Wang, X
Deng, Z
Huang, M
Chi, CAS
Tang, JOC 
Zhong, G
Keywords: 83b1
Method validation
Issue Date: 2017
Publisher: Elsevier
Source: Journal of pharmaceutical and biomedical analysis, 2017, v. 134, p. 71-76 How to cite?
Journal: Journal of pharmaceutical and biomedical analysis 
Abstract: Great attentions have been drawn by quinoline for its broad bioactivity as anti-fungal, anti-bacterial and anti-tumor activities. Compared with cisplatin, 83b1, a quinoline derivative, showed equal activity in anti-tumor and lower cyctotoxicity in normal cell. In this study, a simple, rapid and sensitive method for determination of 83b1 in rat plasma using UHPLC–MS/MS was developed for the first time. Loratadine was used as an internal standard (IS). Separation was performed on an Xterra MS C18 column by isocratic elution using acetonitrile: water solution with 1‰ formic acid (90:10, v/v) as mobile phase at a flow rate of 0.3 mL/min. A triple quadrupole mass spectrometer operating in the positive ion-switching electron spray ionization mode with selection reaction monitoring (SRM) was employed to determine 83b1 and IS transitions of m/z 321.82 → 147.84, 382.71 → 258.76 for 83b1 and Loratadine, respectively. The values of specificity, linearity and lower limit of quantification, intra- and inter- day precision and accuracy, extraction recovery, matrix effect and stability for this method satisfied the acceptable limits. The lower limit of quantification was 0.5 ng/mL with a linear range of 0.5–1500 ng/mL. The validated method was employed to study the bioavailability of 83b1 in rat by dosing with intravenous injection (1 mg/kg) and gavage (10 mg/kg), and the oral bioavailability of 83b1 in rat was calculated as 20.9 ± 8.8%.
EISSN: 0731-7085
DOI: 10.1016/j.jpba.2016.11.011
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