Meissner J, Klostermann H
Int J Clin Pharmacol Biopharm. 1976 Jan;13(1):27-35.
Tritium-labelled fenoterol hydrobromide was infused into an ear-vein of pregnant rabbits over a period of 4 hours. Two doses were used. The tritum concentrations in the blood of the dams and the amniotic fluid were determined from samples obtained during infusion and up to 11 hours after completion of infusion. The tritium concentrations were also determined in selected organ samples from dams and fetuses, taken immediately and 5 and 11 hours after infusion. Within 1.5 hours after commencement of infusion, the tritium activity in the whole blood of the dams reached a plateau on a level corresponding to the dose administered. Immediately after completion of infusion, the level of radioactivity fell rapidly. The tritium concentration in the amniotic fluid began to rise far more slowly after a time lag, so that approximately 2 hours after completion of infusion, the concentrations in maternal whole blood and amniotic fluid were equal. As the amniotic fluid level fell at a slower rate than the maternal whole blood level, the former somewhat exceeded the latter at this advanced stage of the study. The tritium distribution patterns of the dams indicate rapid elimination via kidneys and intestine. The tritium concentration in all the tissue fell rapidly after completion of infusion. The lung and uterus have a slightly greater affinity. The tritium concentrations in the fetal organs remained below those in the organs of the dams for the whole duration of the study. The highest radioactive concentration in the fetuses was found in the urine. Further observation of the rapid conversion of fenoterol hydrobromide into conjugates leads us to expect only minimal amounts of active substance to be found in the fetuses after infusion.
将氚标记的氢溴酸非诺特罗在4小时内注入怀孕兔子的耳静脉。使用了两种剂量。在注入期间及注入完成后长达11小时内采集样本,测定母兔血液和羊水中的氚浓度。还在注入后立即、5小时和11小时采集母兔和胎儿的选定器官样本,测定其中的氚浓度。注入开始后1.5小时内,母兔全血中的氚活性达到与给药剂量相应的稳定水平。注入完成后,放射性水平迅速下降。羊水氚浓度在有一段时间延迟后开始上升得慢得多,因此注入完成后约2小时,母兔全血和羊水的浓度相等。由于羊水水平下降速度比母兔全血水平慢,在研究的这个后期阶段,前者略超过后者。母兔的氚分布模式表明通过肾脏和肠道快速消除。注入完成后,所有组织中的氚浓度迅速下降。肺和子宫的亲和力略大。在整个研究期间,胎儿器官中的氚浓度一直低于母兔器官中的浓度。胎儿中放射性浓度最高的是尿液。对氢溴酸非诺特罗迅速转化为结合物的进一步观察使我们预计注入后在胎儿中只能发现极少量的活性物质。