Phillips J C, Bex C, Walters D G, Gaunt I F
British Industrial Biological Research Association, Carshalton, Surrey, England.
Food Chem Toxicol. 1987 Dec;25(12):927-35. doi: 10.1016/0278-6915(87)90286-9.
The absorption, metabolism and excretion of 14C-labelled carmoisine has been studied in the rat, mouse and guinea-pig. Following administration of a single oral dose of either 0.5 or 50 mg/kg body weight, substantially all of the dose was recovered in the excreta within 72 hr, mainly in the faeces. Although the urinary excretion of radioactivity was similar in the rat and the mouse, the proportion of the radioactivity found in the urine of the guinea-pig was significantly greater than that of the other species at both dose levels. Pretreating male rats with unlabelled colouring in the diet (0.05%, w/w) for 28 days prior to dosing with 14C-labelled colouring had no effect on the route of excretion or the time taken to eliminate the majority of the labelled dose. Following a single oral dose of 14C-labelled colouring to previously untreated rats, mice and guinea-pigs or to rats pretreated as above, no marked accumulation of radioactivity in any tissue was found. Pregnant rats eliminated a single oral dose of 14C-labelled colouring at a similar rate to non-pregnant females, and the concentration of radioactivity in the foetuses was similar to that in the other tissues. Naphthionic acid was the major urinary metabolite in all three species. In the rat and mouse, most of the remaining radioactivity co-chromatographed with 2-amino-1-naphthol-4-sulphonic acid (2-ANS), but in the guinea-pig radioactivity also co-chromatographed with 1,2-naphthoquinone-4-sulphonate (1,2-NQS). Only a trace amount of unchanged carmoisine was detected in the urine of the species examined. Naphthionic acid was also found in the faeces of all three species, but neither carmoisine, 2-ANS or 1,2-NQS was detected. At least five other radioactive metabolites were found in the faecal extracts of all three species, including a substantial amount of a compound with chromatographic properties similar to those of a trace metabolite in the urine. Two of the faecal metabolites were hydrolysed by beta-glucuronidase and sulphatase treatment. In studies on the absorption of carmoisine at concentrations of 50, 500 or 5000 ppm from isolated intestinal loops, no significant absorption was detected in the rat, mouse or guinea-pig.
对14C标记的胭脂红在大鼠、小鼠和豚鼠体内的吸收、代谢及排泄情况进行了研究。给予单次口服剂量为0.5或50mg/kg体重后,基本上所有剂量在72小时内均可从排泄物中回收,主要是在粪便中。虽然大鼠和小鼠放射性物质的尿排泄情况相似,但在两个剂量水平下,豚鼠尿液中发现的放射性物质比例均显著高于其他物种。在给雄性大鼠用14C标记色素给药前28天,在饮食中添加未标记色素(0.05%,w/w)进行预处理,对排泄途径或消除大部分标记剂量所需时间没有影响。对先前未经处理的大鼠、小鼠和豚鼠或上述预处理的大鼠单次口服14C标记色素后,未发现任何组织中有明显的放射性物质蓄积。怀孕大鼠消除单次口服14C标记色素的速率与未怀孕雌性大鼠相似,胎儿中的放射性物质浓度与其他组织中的相似。萘胺酸是所有三个物种的主要尿代谢产物。在大鼠和小鼠中, 大部分剩余放射性物质与2-氨基-1-萘酚-4-磺酸(2-ANS)共色谱,但在豚鼠中,放射性物质也与1,2-萘醌-4-磺酸盐(1,2-NQS)共色谱。在所检查物种的尿液中仅检测到痕量未变化的胭脂红。在所有三个物种的粪便中也发现了萘胺酸,但未检测到胭脂红、2-ANS或1,2-NQS。在所有三个物种的粪便提取物中至少发现了另外五种放射性代谢产物,包括大量色谱性质与尿液中一种痕量代谢产物相似的化合物。两种粪便代谢产物经β-葡萄糖醛酸酶和硫酸酯酶处理后被水解。在对大鼠、小鼠或豚鼠离体肠袢中浓度为50、500或5000ppm的胭脂红吸收研究中,未检测到明显吸收。