Yunaconitine and indaconitine are active ingredients from the rhizomes of Aconitum plants. In this study, an ultra-high-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was developed to measure the concentrations of the yunaconitine and indaconitine in mouse blood, and the method was applied in measuring the pharmacokinetics of the two alkaloids after oral and intravenous administration. A UPLC HSS T3 column (2.1 mm × 100 mm, 1.8 μm particle size) was used for chromatographic separation by gradient elution using acetonitrile–water (0.1% formic acid) as the mobile phase at a flow rate of 0.4 mL/min. Multiple reaction monitoring (MRM) mode and electrospray ionization (ESI) (positive-ion mode) were used to monitor the transitions of each analyte by tandem mass spectrometry for quantitative analysis. Yunaconitine and indaconitine were administered to the mice orally at 2 mg/kg and intravenously at 0.05 mg/kg. Blood was collected at various time intervals, and the blood samples were processed after collection and analyzed by UPLC-MS/MS. The standard curve generated for each analyte was linear over the concentration range of 0.5–500 ng/mL. The intra-day and inter-day accuracy of yunaconitine and indaconitine were 90%–103% and 86%–106%, respectively, and the precision (RSD, %) was less than 15% for both intra-day and inter-day measurements. The matrix effect ranged from 96% to 109%, and the recovery was higher than 72%. The UPLC-MS/MS method developed herein was successfully applied to measuring the pharmacokinetic parameters of yunaconitine and indaconitine in mice after intravenous and oral administration. The bioavailability of yunaconitine and indaconitine were 27.4% and 25.8%, respectively.

Yunaconitine 和 indaconitine 是来自乌头植物根茎的活性成分。本研究建立了一种超高效液相色谱串联质谱法（UPLC-MS/MS）测定小鼠血液中云南乌头碱和茚达乌碱的浓度，并将该方法应用于测定两者的药代动力学。口服和静脉给药后的生物碱。使用 UPLC HSS T3 柱（2.1 mm × 100 mm，1.8 μm 粒径）进行色谱分离，梯度洗脱使用乙腈-水（0.1% 甲酸）作为流动相，流速为 0.4 mL/min。多反应监测 (MRM) 模式和电喷雾电离 (ESI)（正离子模式）用于通过串联质谱法监测每种分析物的跃迁进行定量分析。以 2 mg/kg 口服和静脉注射 0.05 mg/kg 给予小鼠尤乌乌碱和茚达乌碱。在不同的时间间隔收集血液，收集后处理血样并通过 UPLC-MS/MS 进行分析。为每种分析物生成的标准曲线在 0.5–500 ng/mL 的浓度范围内呈线性。云乌碱和茚达碱的日内和日间准确度分别为 90%–103% 和 86%–106%，日内和日间精密度（RSD，%）均小于 15%测量。基质效应为96%~109%，回收率高于72%。本文开发的 UPLC-MS/MS 方法成功应用于测量小鼠静脉和口服给药后云南乌头碱和茚达乌碱的药代动力学参数。