Lusianthridin was reported to possess many biological properties such as anti-oxidant and anti-cancer activities. However, its metabolic profiles and pharmacokinetics in vivo remain unknown. This study was carried out to investigate the metabolic profiles and pharmacokinetics of lusianthridin in rats. The metabolic profiles were obtained by an ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-Q/TOF-MS). A total of eighteen metabolites involved three phase I metabolites and fifteen phase II metabolites were detected and identified. The major metabolic pathways of lusianthridin were demethylation, oxidation, sulfation, glucuronidation and glutathione conjugation. In addition, a simple and sensitive ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was established for determination of lusianthridin in rat plasma. After extracted by protein precipitation, lusianthridin was quantitated in positive ion mode. The method was linear over the range of 0.5-500 ng/mL (r ≥ 0.995) with the LLOQ of 0.5 ng/mL. The intra- and inter- precision and accuracy, extraction recovery, matrix effect and stability were within the acceptable limits. The validated method was applied to the pre-clinical pharmacokinetic study of lusianthridin in rats. After oral administration, lusianthridin was quickly absorbed into plasma and reached the max concentration of 236.22 ng/mL at 22.00 min. The elimination half life of lusianthridin from plasma was approximately 83.05-104.47 min and the oral absolute bioavailability was calculated as 30.93%.

据报道，芦硫吡啶具有许多生物特性，例如抗氧化剂和抗癌活性。然而，其在体内的代谢谱和药代动力学仍然未知。进行了这项研究以调查大鼠中芥子硫磷素的代谢特征和药代动力学。通过超高效液相色谱四极杆飞行时间质谱（UPLC-Q / TOF-MS）获得代谢谱。共检测到18种代谢物，涉及3种I期代谢物，15种II期代谢物。紫杉醇的主要代谢途径是去甲基化，氧化，硫酸化，葡萄糖醛酸化和谷胱甘肽结合。此外，建立了一种简单灵敏的超高效液相色谱串联质谱法（UPLC-MS / MS），用于测定大鼠血浆中的紫杉醇。经蛋白质沉淀提取后，以正离子模式定量测定了香菊酯的含量。该方法在0范围内是线性的。5-500 ng / mL（r≥0.995），LLOQ为0.5 ng / mL。内部和内部精度和准确度，提取回收率，基质效应和稳定性均在可接受的范围内。验证的方法被应用于大鼠紫杉醇的临床前药代动力学研究。口服给药后，卢甜菊酯迅速吸收到血浆中，并在22.00分钟时达到最大浓度236.22 ng / mL。从血浆中消除紫杉醇的半衰期约为83.05-104.47分钟，经计算，口服绝对生物利用度为30.93％。口服给药后，卢甜菊酯迅速吸收到血浆中，并在22.00分钟时达到最大浓度236.22 ng / mL。从血浆中消除紫杉醇的半衰期约为83.05-104.47分钟，经计算，口服绝对生物利用度为30.93％。口服给药后，卢甜菊酯迅速吸收到血浆中，并在22.00分钟时达到最大浓度236.22 ng / mL。从血浆中消除紫杉醇的半衰期约为83.05-104.47分钟，经计算，口服绝对生物利用度为30.93％。