Maeda T, Sakai H, Hayakawa H, Hayashi K, Yoneda K
Research Laboratory, Toyama Chemical Co., Ltd.
Jpn J Antibiot. 1989 Apr;42(4):854-67.
Absorption, distribution and excretion of T-3262 were studied in rats and mice after oral administration of 14C-T-3262. The obtained results are summarized as follows. 1. 14C-T-3262 was absorbed from the upper small intestine such as duodenum in rats. 2. Serum levels of radioactivity in rats reached the highest concentration at 1 hour after an oral administration, then gradually diminished. 3. Urinary excretion was 35% and 42% of the dosed radioactivity in rats and mice, respectively, and fecal excretion was about 65% and 56% of the dosed radioactivity in rats and mice, respectively. 4. Biliary excretion in rats was about 27% of the dosed radioactivity after an oral administration of 14C-T-3262, and a half amount of excreted radioactivity was reabsorbed from the intestine. 5. Radioactivity was distributed the most into the kidney and the liver among all organs other the stomach and the intestine. Radioactivity was widely distributed into other organs such as spleen, adrenal, pancreas, lung, heart and thymus. But the distribution of radioactivity into the brain was little. 6. The distribution of 14C-T-3262 was also studied with whole body autoradiography in normal male mice and pregnant mice. The radioactivity was distributed widely to whole tissues except brain, spinal cord and eye ball. In pregnant mice, radioactivity levels in the fetuses were the same as the blood level of the mother mice. 7. The binding rate of 14C-T-3262 to rats and mice serum proteins was 63-66%. 8. Urinary and fecal excretion patterns of radioactivity in mice after multiple oral administration of 14C-T-3262 for 10 days were similar to those after a single administration. This result suggests that T-3262 did not accumulate in body. 9. After oral administration of 14C-T-3262 to nursing rats, the secreted radioactivity level in the milk was higher than the blood level.
在大鼠和小鼠口服14C-T-3262后，对T-3262的吸收、分布和排泄情况进行了研究。所得结果总结如下。1. 14C-T-3262在大鼠中从十二指肠等小肠上段吸收。2. 大鼠口服给药后1小时血清放射性水平达到最高浓度，然后逐渐下降。3. 大鼠和小鼠尿排泄量分别为给药放射性的35%和42%，粪便排泄量分别约为给药放射性的65%和56%。4. 大鼠口服14C-T-3262后胆汁排泄量约为给药放射性的27%，排泄放射性的一半从肠道重新吸收。5. 在胃和肠道以外的所有器官中，放射性在肾脏和肝脏中的分布最多。放射性广泛分布于脾脏、肾上腺、胰腺、肺、心脏和胸腺等其他器官。但放射性在大脑中的分布很少。6. 还通过全身放射自显影术研究了正常雄性小鼠和怀孕小鼠中14C-T-3262的分布情况。放射性广泛分布于除脑、脊髓和眼球以外的所有组织。在怀孕小鼠中，胎儿的放射性水平与母鼠的血液水平相同。7. 14C-T-3262与大鼠和小鼠血清蛋白的结合率为63-66%。8. 小鼠多次口服14C-T-3262 10天后，尿和粪便放射性排泄模式与单次给药后相似。该结果表明T-3262在体内不会蓄积。9. 给哺乳期大鼠口服14C-T-3262后，乳汁中分泌的放射性水平高于血液水平。
