Krumbiegel G, Schulz H U
Department of Pharmacokinetics, Madaus AG, Köln, FRG.
Pharmacology. 1993 Oct;47 Suppl 1:120-4. doi: 10.1159/000139850.
Therapeutic doses of two laxatives (Agiolax and Sennatin) were repeatedly administered to 10 healthy volunteers in a two-way change-over design. Blood samples were collected up to 96 h after the first dose, and plasma levels of total aloe-emodin and rhein were determined simultaneously with a sensitive (lower limit of quantification: 0.5 ng aloe-emodin and 2.5 ng rhein per millilitre plasma) and specific fluorometric HPLC method. Aloe-emodin was not detectable in any plasma sample of any subject. Rhein concentration time courses showed highest levels of 150-160 ng/ml and peak maxima at 3-5 h and 10-11 h after dosing probably according to absorption of free rhein and rhein released from prodrugs (e.g. sennosides) by bacterial metabolism, respectively.
采用双向交叉设计，对10名健康志愿者反复给予两种泻药（Agiolax和番泻叶苷）的治疗剂量。在首次给药后长达96小时采集血样，采用灵敏的（定量下限：每毫升血浆中芦荟大黄素0.5 ng、大黄酸2.5 ng）特异性荧光高效液相色谱法同时测定血浆中总芦荟大黄素和大黄酸的水平。在任何受试者的任何血浆样本中均未检测到芦荟大黄素。大黄酸浓度-时间曲线显示，给药后3-5小时和10-11小时分别出现最高水平150-160 ng/ml和峰值最大值，这可能分别是由于游离大黄酸和前药（如番泻苷）经细菌代谢释放的大黄酸的吸收。
