Kotaki H, Yamamura Y, Tanimura Y, Saitoh Y, Nakagawa F, Tamura Z
J Pharmacobiodyn. 1983 Nov;6(11):881-7. doi: 10.1248/bpb1978.6.881.
Plasma concentrations of clioquinol and its metabolites after single or repeated oral administration of clioquinol, absorption region of clioquinol in gastrointestinal tract, and intestinal metabolism were studied in rats. Plasma concentrations of clioquinol after oral administration of four different doses (20, 100, 200 and 400 mg/kg) were lower than those of the two metabolites, clioquinol glucuronide and sulfate. Mean maximal plasma concentration of unchanged drug was in the range of 1-8 nmol/ml. Clioquinol was absorbed poorly from the stomach and fairly from the small intestine. Bile was an important route for excretion of clioquinol in rats. The mesenteric venous plasma from the closed intestinal loops of both jejunal and ileal regions was analyzed for clioquinol and the metabolites and it was found that clioquinol glucuronide was formed predominantly in both regions. From the results of the present studies, intestinal metabolism of clioquinol can be pointed out as a major factor for difficulty to cause clioquinol intoxication.
研究了大鼠单次或重复口服氯碘羟喹后其血浆浓度及其代谢产物、氯碘羟喹在胃肠道的吸收部位以及肠道代谢情况。口服四种不同剂量（20、100、200和400mg/kg）氯碘羟喹后，其血浆浓度低于两种代谢产物氯碘羟喹葡糖苷酸和硫酸酯。原形药物的平均最大血浆浓度在1-8nmol/ml范围内。氯碘羟喹在胃中吸收较差，在小肠中吸收较好。胆汁是大鼠体内氯碘羟喹排泄的重要途径。分析空肠和回肠区域封闭肠袢的肠系膜静脉血浆中的氯碘羟喹及其代谢产物，发现氯碘羟喹葡糖苷酸在这两个区域均主要形成。根据本研究结果，氯碘羟喹的肠道代谢可被认为是导致氯碘羟喹中毒困难的主要因素。
