期刊
出版社
ELSEVIER
DOI: 10.1016/j.jchromb.2021.122671
关键词
Aloperine; Bioavailability; LC-MS; MS; Pharmacokinetics; Rat plasma
资金
- Science and Technology Commission of Shanghai Municipality [18430760400]
- Clinical Advantage Discipline of Health System of Putuo District in Shanghai
- ECNU Multifunctional Platform for Innovation [011]
This study established an efficient and sensitive method for quantifying aloperine in rat plasma, and conducted pharmacokinetic studies in Sprague-Dawley rats. The method was validated in compliance with FDA bioanalytical method validation guidelines.
Aloperine, a novel natural active alkaloid derived from Sophora alopecuroides L., has attracted much attention for its anti-inflammatory, antiviral, anti-tumor, anti-allergy and other pharmacological activities. In this study, we first established and validated an efficient and sensitive high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the quantification of aloperine in rat plasma. Cytisine was used as the internal standard (IS). The separation of aloperine and IS was conducted on a Phenomenex Luna Omega Polar C18 column (2.1 x 50 mm, 1.6 mu m) with 0.3% (v/v) formic acid aqueous (containing 5 mM ammonium acetate) and 0.3% (v/v) formic acid acetonitrile using isocratic elution condition at a flow rate of 0.20 mL/min. Aloperine and IS were determined under the transitions of m/z 233.2 -* 98.1 and m/z 191.2 -* 148.2 (positive ionization mode), respectively. The calibration curve of aloperine was established in the range of 5 (LLOQ) to 2000 ng/mL (r2 = 0.994). The well validated method was full compliance with the bioanalytical method validation of FDA, and was applied to the pharmacokinetic study of aloperine in Sprague-Dawley rats after 50 mg/kg oral administration and 5 mg/kg intravenous injection. This study provides valuable references for the further study of Sophora alopecuroides L., especially for the drug development and clinical application of aloperine.
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