Only focusing on the circulating levels is insufficient for the comprehensive understanding of the physiological disposition of herbal medicine in vivo. Therefore, we conducted the comprehensive investigation on the in vivo dynamic process of orally administrated Gouteng-Baitouweng (GB), a classical herb pair with anti-Parkinson potentials. Serving as the technical base, a sensitive and selective liquid chromatography–tandem mass spectrometry method was established and validated in the plasma, liver and brain, for simultaneous determination of five alkaloids (rhynchophylline, isorhynchophylline, corynoxeine, isocorynoxeine and geissoschizine methyl ether) and three saponins (anemoside B4, anemoside A3 and 23-hydroxybetulinic acid). Following liquid-liquid extraction, favorable chromatographic behaviors of eight analytes were obtained on Waters Xbrigde C18 column within 13 min. This method elicited good linearity for the analytes at the concentration range of 0.3–1000 or 1.8–6000 ng/mL with favorable precision, accuracy and stability. Following oral administration of GB (25 g/kg) in rats, this method was applied to the quantitative analysis in the portal vein plasma, liver, systemic plasma, and brain. Consequently, anemoside B4 was of the highest exposure, followed by 23-hydroxybetulinic acid, anemoside A3, rhynchophylline and isocorynoxeine in vivo. Notably, three saponins were all observed with certain exposure in the brain, along with rhynchophylline at low levels. Besides, five alkaloids and 23-hydroxybetulinic acid underwent serious liver first-pass effect. Hence, the pharmacokinetics, liver first-pass effect, liver and brain distribution of ingredients in GB were clarified, which laid a solid foundation for interpreting its efficacy and safety.

仅关注循环水平不足以全面了解体内草药的生理特性。因此，我们进行的全面调查体内口服的动态过程钩藤-白头翁（GB），具有抗帕金森电位的经典草药对。建立了灵敏且选择性的液相色谱-串联质谱法作为技术基础，并在血浆，肝和脑中进行了验证，可同时测定五个生物碱（儿茶碱，异去甲茶碱，皮质类固醇，异corynoxeine和geissoschizine甲基醚）和三种皂苷（阿莫糖苷B4，阿莫糖苷A3和23-羟基贝丁酸）。液-液萃取后，在13分钟内在Waters Xbrigde C18色谱柱上获得了8种分析物的有利色谱行为。此方法在0.3–1000或1.8–6000 ng / mL的浓度范围内对分析物具有良好的线性，并具有良好的精密度，准确性和稳定性。在大鼠中口服GB（25 g / kg）后，该方法用于门静脉血浆，肝脏，全身血浆和脑中的定量分析。因此，最大的暴露部位是氨基苯乙酰胺B4，其次是23-羟基贝丁酸，氨基苯乙胺苷A3，乙酰胆碱和异corynoxeine体内。值得注意的是，在大脑中有一定的暴露量，同时观察到了三种皂苷以及低水平的乙酰胆碱。此外，有5种生物碱和23-羟基贝丁酸经历了严重的肝脏首过效应。因此，阐明了GB中各成分的药代动力学，肝首过效应，肝和脑分布，为解释其功效和安全性奠定了坚实的基础。