A simple and fast bioanalytical method for the quantification of kavain in mice plasma was developed using liquid chromatography (LC)-tandem mass spectrometry (MS/MS). A full method validation was performed, according to regulatory guidelines, employing isotopically labeled kavain as the internal standard (racemic-kavain-d3). For the quantification, [M+H]⁺ was formed using an electrospray ionization (ESI) source in the positive ion mode and multiple reaction monitoring (MRM) was employed using a quadrupole-linear ion trap (4000 QTRAP®) instrument. The monitored MRM transitions were 231.0→115.1 and 231.0→152.8 for kavain; and 234.2→199.2 for the internal standard. A linear response was obtained at the concentration range of 10 to 200 ng/mL with intra- and inter-day variations within the acceptable criteria for all quality control samples. After validation, the method was successfully applied for the quantification of kavain in mice plasma after oral administration of the kavain standard and Kava-kava extract. The plasma concentration over time results were applied for a pharmacokinetics study. The obtained pharmacokinetic parameters indicated a considerably higher bioavailability for kavain when Kava-kava extract was administered due to a pharmacokinetic synergism between the analyte and the other compounds present in the extract.

使用液相色谱（LC）-串联质谱（MS / MS）建立了一种简单快速的生物分析方法，用于定量小鼠血浆中的卡瓦因。根据法规指南，使用同位素标记的卡瓦因作为内标（racemic-kavain-d3），进行了完整的方法验证。为了定量，[M + H] ⁺使用正离子模式下的电喷雾电离（ESI）源形成离子阱，并使用四极线性离子阱（4000QTRAP®）仪器进行多反应监测（MRM）。卡瓦因监测到的MRM跃迁为231.0→115.1和231.0→152.8; 内部标准为234.2→199.2。在所有质量控制样品可接受的标准范围内，日内和日间变化在10至200 ng / mL的浓度范围内获得线性响应。验证后，该方法成功应用于口服卡瓦因标准品和卡瓦-卡瓦提取物后，在小鼠血浆中对卡瓦因进行定量。随时间的血浆浓度结果被用于药代动力学研究。