Krause W, Kühne G
Steroids. 1982 Jul;40(1):81-90. doi: 10.1016/0039-128x(82)90114-3.
The plasma level of spirorenone was determined 3 h after 1, 8, 22 and 46 daily oral administrations of 20 mg/kg to two female and two male monkeys (Macaca fascicularis). A fifth animal, female, was treated with eight daily doses of tritium-labelled drug and was completely bled from the carotid vein 4 h after the last administration in order to isolate and identify plasma metabolites. After repeated daily doses of spirorenone the mean plasma level of unchanged drug was 711 +/- 213 ng/ml. In the plasma of the fifth animal four radioactively labelled compounds could be detected after extraction and subsequent HPLC separation. Mass spectrometric identification of three of the substances indicated 1,2-dihydrospirorenone, hydroxy-1,2-dihydrospirorenone and the unchanged drug itself.
对两只雌性和两只雄性食蟹猴（猕猴属）每日口服20mg/kg螺内酯，连续给药1天、8天、22天和46天后3小时测定血浆中螺内酯水平。第五只雌性动物每日给予八剂氚标记药物，在最后一次给药后4小时从颈动脉完全放血，以分离和鉴定血浆代谢物。每日重复给予螺内酯后，未变化药物的平均血浆水平为711±213ng/ml。在第五只动物的血浆中，经提取及随后的高效液相色谱分离后可检测到四种放射性标记化合物。对其中三种物质进行质谱鉴定，结果表明为1,2-二氢螺内酯、羟基-1,2-二氢螺内酯和未变化的药物本身。
