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目的研究最大耐受量下香加皮中杠柳毒苷及苷元在小鼠体内的代谢规律。方法小鼠单次腹腔注射给予最大耐受量的香加皮水提物,高效液相色谱法测定给药后不同时间点血浆及心脏组织中杠柳毒苷及苷元的浓度。结果小鼠给药后,血浆中杠柳毒苷及杠柳毒苷苷元均出现多峰,其中杠柳毒苷在0～45 min时间段为吸收相,符合零级动力学,拟合方程为C=0.320 t,在45 min和120 min出现两个高峰,120～720 min时间段符合二室模型,t1/2α=1.694 min,t1/2β=344.049 min。在药后12 h内心脏组织中杠柳毒苷及杠柳毒苷苷元的含量相对稳定,没有显著降低。结论杠柳毒苷及苷元在体内存在肝肠循环,且苷元吸收较快;杠柳毒苷及苷元在心脏内有一定的蓄积。
OBJECTIVE To study the metabolic regularity of glucosides and aglycons in the body of mice treated with maximal tolerance. Methods The mice were given intraperitoneal injections of maximal tolerant aqueous extracts of Pericarpium citrifolia. The concentration of sarsasapogenin and aglycone in the plasma and cardiac tissues at different time points after administration was determined by high performance liquid chromatography. RESULTS: After administration of the mice, there were multiple peaks in both plasma and liuliuxin glycosides in the plasma. The glucosides were absorbed phase from 0 to 45 min, which was in accordance with zero-order kinetics. For C=0.320 t, there were two peaks at 45 min and 120 min, and the 120-720 min period met the two-compartment model with t1/2α=1.694 min and t1/2β=344.049 min. Within 12 hours after drug administration, the contents of arbutin and arbutin in the heart tissue were relatively stable and did not decrease significantly. Conclusion There is hepatic enteric circulation in the body of arbutin and aglycones in the body, and aglycone is rapidly absorbed. There is a certain accumulation of sarsasapogenin and aglycone in the heart.