Ohshima N, Kotaki H, Saitoh Y, Nakagawa F, Tamura Z
Hospital Pharmacy, Faculty of Medicine, University of Tokyo, Japan.
J Pharmacobiodyn. 1989 Jul;12(7):371-7. doi: 10.1248/bpb1978.12.371.
The order of plasma levels of clioquinol and its conjugates in male rats after intraduodenal administration of 32.7 mumol/kg dose of clioquinol was clioquinol sulfate (C-Sul) greater than glucuronide (C-Glu) much greater than clioquinol, whereas that in female rats was C-Glu greater than C-Sul much greater than clioquinol. Total (urine + bile) recovery was almost the same among male and female rats. The percentage of excretion amounts of C-Sul (urine + bile) to the total excretion amounts for 24 h in male rats after intravenous administration of clioquinol was about twice that in female rats, while the percentage of excretion amounts of C-Glu to the total excretion amounts in male rats was smaller than that in female rats. In intravenous administration of 16.4 mumol/kg dose of C-Glu, C-Sul and clioquinol other than C-Glu were found in bile and urine of male and female rats. The percentage of excretion amounts of C-Sul and C-Glu (urine + bile) to the total excretion amounts was similar among male and female rats, respectively. In intravenous administration of 16.4 mumol/kg dose of C-Sul, C-Glu and clioquinol other than C-Sul were found in bile and urine of male and female rats, and the percentage of excretion amounts of C-Sul (urine + bile) to the total excretion amounts in male rats was 1.3 fold that in female rats.(ABSTRACT TRUNCATED AT 250 WORDS)
十二指肠内给予雄性大鼠32.7 μmol/kg剂量的氯碘羟喹后，氯碘羟喹及其结合物的血浆水平顺序为硫酸氯碘羟喹（C-Sul）大于葡萄糖醛酸结合物（C-Glu）且远大于氯碘羟喹，而雌性大鼠中的顺序为C-Glu大于C-Sul且远大于氯碘羟喹。雄性和雌性大鼠的总（尿液 + 胆汁）回收率几乎相同。静脉注射氯碘羟喹后，雄性大鼠中C-Sul（尿液 + 胆汁）排泄量占24小时总排泄量的百分比约为雌性大鼠的两倍，而雄性大鼠中C-Glu排泄量占总排泄量的百分比小于雌性大鼠。静脉注射16.4 μmol/kg剂量的C-Glu后，在雄性和雌性大鼠的胆汁和尿液中发现了除C-Glu外的C-Sul和氯碘羟喹。雄性和雌性大鼠中C-Sul和C-Glu（尿液 + 胆汁）排泄量占总排泄量的百分比分别相似。静脉注射16.4 μmol/kg剂量的C-Sul后，在雄性和雌性大鼠的胆汁和尿液中发现了除C-Sul外的C-Glu和氯碘羟喹，雄性大鼠中C-Sul（尿液 + 胆汁）排泄量占总排泄量的百分比是雌性大鼠的1.3倍。（摘要截短于250字）
