Hempelmann F W, Heinz N, Flasch H
Arzneimittelforschung. 1978;28(12):2182-5.
Intestinal absorption of 15 cardenolides has been examined in cats. The 3H-labelled substances were injected intraluminally into ligated duodenal loops of anaesthetized animals. 3H-Concentrations were followed in the portal circulation and in the bile. 1 h after drug administration the duodenal sac was removed, and the residual in the lumen then was washed out and assayed radiochemically. The decrease of radioactivity during 1 h was calculated as extent of absorption (QR). Cardenolide absorption was compared with the corresponding in vitro parameters of lipophilicity like octanol/water partition coefficients and Rm values from reversed phase thin-layer chromatography. The Spearman rank sum correlation test revealed coefficients of 0.95 to 0.97. The result lends support to the use of the easily available Rm values as a good tool to predict intestinal absorption of various cardenolides.
已在猫身上研究了15种强心苷的肠道吸收情况。将3H标记的物质经肠腔注入麻醉动物结扎的十二指肠肠袢中。监测门静脉循环和胆汁中的3H浓度。给药1小时后,取出十二指肠囊,冲洗肠腔内的残留物并进行放射化学分析。计算1小时内放射性的降低作为吸收程度(QR)。将强心苷的吸收与相应的亲脂性体外参数如正辛醇/水分配系数和反相薄层色谱的Rm值进行比较。Spearman秩和相关检验显示系数为0.95至0.97。该结果支持将易于获得的Rm值用作预测各种强心苷肠道吸收的良好工具。