Moreau J P, Moreau S, Skinner S
Biopharm Drug Dispos. 1985 Jul-Sep;6(3):325-34. doi: 10.1002/bdd.2510060307.
The in vitro microbial degradation and the urinary excretion and biliary secretion in rats of two anthraquinone glycosides (sennosides A and B) and four aglycones (sennidins A and B, rhein, and danthron) were studied using a high performance liquid chromatographic system with gradient elution and amperometric detection. Microbial degradation of sennosides A and B occurred almost exclusively in the presence of mice caecum inoculae and was associated with the release of sennidins A and B. Rhein and danthron were indiscriminately metabolized by bacteria sampled from all regions of mice intestine, whereas sennidins lacked stability in biological media. The fraction of the dose administered orally to rats and recovered as aglycones or as glucuronides in bile and urine after 48 hours was five times greater for rhein (15 per cent) and danthron (13.4 per cent) than for sennosides A (1.8 per cent) and B (2.8 per cent) excreted or secreted as sennidins. These results support the concept that anthraquinone glycosides are less likely to enter the systemic circulation and, thus, are able to exert their laxative effect at lower doses than aglycones.
使用具有梯度洗脱和安培检测功能的高效液相色谱系统，研究了两种蒽醌糖苷（番泻苷A和B）以及四种苷元（番泻素A和B、大黄酸和丹蒽醌）在大鼠体内的体外微生物降解、尿液排泄和胆汁分泌情况。番泻苷A和B的微生物降解几乎只在存在小鼠盲肠接种物的情况下发生，并且与番泻素A和B的释放有关。大黄酸和丹蒽醌被从小鼠肠道所有区域采集的细菌无差别地代谢，而番泻素在生物介质中缺乏稳定性。口服给予大鼠的剂量在48小时后以苷元或葡萄糖醛酸苷形式在胆汁和尿液中回收的比例，大黄酸（15%）和丹蒽醌（13.4%）比以番泻素形式排泄或分泌的番泻苷A（1.8%）和B（2.8%）高五倍。这些结果支持了这样一种概念，即蒽醌糖苷进入体循环的可能性较小，因此，与苷元相比，能够以较低剂量发挥其泻药作用。
