The metabolism, tissue distribution and excretion of taxifolin in rat after oral administration of taxifolin encapsulated zein-caseinate Nanoparticles (TZP) were studied. The isomerization of taxifolin in rat small intestine and colon was found. Besides isomers, 16 metabolites of taxifolin were identified in rat feces, plasma and urine by UPLC-QTOF-MS. In colon, taxifolin underwent the metabolism of hydration, dehydration and ring-fission through the gut microflora. The main metabolites of taxifolin found in plasma and urine were its sulfated, glucuronidated, and/or methylated products. The dynamic variation of taxifolin and its metabolites in tissues and urine were quantified by UPLC-QqQ-MS/MS. Taxifolin and its metabolites could be quickly absorbed and distributed in the tissues, and relatively low concentrations were found in the heart and brain. The feces excretion of taxifolin was determined by HPLC. The total excretion during 24 h was 2.83 ± 0.80% to its given does, and the maximum excretion was found during 8–10 h post administration. Compared with feces, the excretion of taxifolin and its metabolites in urine was much faster, and the total excretion was 1.96 ± 0.23% during 12 h.

研究了大鼠口服紫杉叶素包封的玉米醇溶蛋白-酪蛋白纳米颗粒(TZP)后紫杉叶素在大鼠体内的代谢、组织分布和排泄。在大鼠小肠和结肠中发现紫杉叶素异构化。除异构体外，通过 UPLC-QTOF-MS 在大鼠粪便、血浆和尿液中鉴定出紫杉叶素的 16 种代谢物。在结肠中，紫杉叶素通过肠道菌群进行水合、脱水和环状裂变的代谢。在血浆和尿液中发现的紫杉叶素的主要代谢物是其硫酸化、葡萄糖醛酸化和/或甲基化产物。通过 UPLC-QqQ-MS/MS 对紫杉叶素及其代谢物在组织和尿液中的动态变化进行定量。紫杉叶素及其代谢物可迅速吸收并分布于组织中，在心脏和大脑中发现的浓度相对较低。采用高效液相色谱法测定紫杉叶素的粪便排泄量。24 小时内的总排泄量为其给定剂量的 2.83 ± 0.80%，最大排泄量出现在给药后 8-10 小时内。与粪便相比，紫杉叶素及其代谢物在尿液中的排泄要快得多，12 h内总排泄量为1.96±0.23%。