Pharmacokinetics Study of the Antitumor Drug CYC-116 in Rat Plasma by Using LC–MS Analysis

• Published in: Chromatographia 2012-03, Vol.75 (5-6), p.263-268
• Main Authors: Su, Jing, Chen, Xiaohui, Li, Qing, Yu, Zhiguo, Guan, Xiaoduo, Geng, Lulu, Bi, Kaishun
• Format: Article
• Language: English
• Subjects: Analysis; Analytical Chemistry; Biological and medical sciences; Chemistry; Chemistry and Materials Science; Chromatography; General pharmacology; Laboratory Medicine; Medical sciences; Original; Pharmacology. Drug treatments; Pharmacy; Proteomics
• ISSN: 0009-5893; 1612-1112
• DOI: 10.1007/s10337-011-2175-3

A sensitive and rapid liquid chromatography–mass spectrometry (LC–MS) assay was established for the quantitation of CYC-116, an antitumor drug, in rat plasma. The chromatographic separation was accomplished on a Kromasil C 18 column (150 mm × 4.6 mm i.d., 5 μm particle size) at an isocratic flow rate of 0.8 mL min −1 using acetonitrile–water–formic acid (23.5:76.5:0.1, v/v/v) as the mobile phase. The plasma extraction was performed by liquid–liquid extraction using ethyl acetate as the solvent, and the extracts were subjected to MS analysis using a quadrupole mass spectrometer. The calibration curve of CYC-116 was linear over the concentration range of 5–2,500 ng mL −1 ( r  = 0.9955). The mean recovery was 85.0 ± 8.0%, and the matrix effect ranged from 90.0 to 110.0%. The intra- and interday precisions were less than 11.8 and 6.6%, respectively, and the accuracy was within ±5.8%. The method was successfully applied to study the pharmacokinetics of CYC-116 in rats after oral administration.