Suzuki T, Sakai A, Morishita M, Muranishi S
Jpn J Antibiot. 1987 Mar;40(3):531-8.
Transmigration of 14C-radioactivity to fetus or milk were studied in 17-18 day-pregnant rats and mother rats on the 14th day after parturition after a single oral administration of 14C-rokitamycin (TMS-19-Q) at a dose of 200 mg/kg. The blood concentration of the drug in the mother reached a maximum level of 22.8 micrograms/ml at 2 hours after administration. Maximum concentrations of TMS-19-Q in placenta, ovary and uterus were attained in 2 hours, and were 28.9, 26.0 and 26.2 micrograms/g, respectively. The distribution to these tissues were considered good. The maximum concentration of TMS-19-Q in the amniotic fluid was attained in 2 hours, at a level of 5.4 micrograms/ml. The transmigration to the amniotic fluid was considered poor. The maximum concentration of the drug in the fetus was achieved in 2 hours at a level of 13.7 micrograms/g. Maximum concentrations of the drug in fetal liver and brain were attained in 4 hours, and were 32.8 and 11.4 micrograms/g, respectively. Whole body autoradiography was done when the radioactivity in maternal blood reached peak concentration. It was found that radioactivities in placenta and fetal membrane were similar to the radioactivity in maternal blood, while the radioactivity in fetal brain was considerably lower than that in maternal blood. Maximum concentrations were found at 1 hour in the blood and at 4 hours in the milk, and were 14.8 and 21.5 micrograms/ml, respectively. Transmigration to the milk was good.
在怀孕17 - 18天的大鼠以及产后第14天的母鼠中，研究了单次口服200mg/kg剂量的14C - 罗他霉素（TMS - 19 - Q）后14C放射性向胎儿或乳汁的转移情况。给药后2小时，母鼠血液中药物浓度达到最高水平，为22.8微克/毫升。胎盘、卵巢和子宫中TMS - 19 - Q的最高浓度在2小时时达到，分别为28.9、26.0和26.2微克/克。认为该药物在这些组织中的分布良好。羊水内TMS - 19 - Q的最高浓度在2小时时达到，为5.4微克/毫升。向羊水的转移情况较差。胎儿体内药物的最高浓度在2小时时达到，为13.7微克/克。胎儿肝脏和大脑中药物的最高浓度在4小时时达到，分别为32.8和11.4微克/克。当母鼠血液中的放射性达到峰值浓度时进行了全身放射自显影。结果发现，胎盘和胎膜中的放射性与母鼠血液中的放射性相似，而胎儿大脑中的放射性明显低于母鼠血液中的放射性。血液中的最高浓度在1小时时出现，乳汁中的最高浓度在4小时时出现，分别为14.8和21.5微克/毫升。向乳汁的转移情况良好。
