Kibwage I O, Michiels M, Hendriks R, Cachet T, Verbruggen A, Hoogmartens J, Vanderhaeghe H
Instituut voor Farmaceutische Wetenschappen, Katholieke Universiteit, Leuven, Belgium.
Eur J Drug Metab Pharmacokinet. 1989 Jan-Mar;14(1):7-14. doi: 10.1007/BF03190835.
Tissue distribution and excretion of radioactively labelled compounds was studied in the Wistar rat after i.v. administration of [N-methyl-14C]-erythromycin A. Whole-body autoradiography and liquid scintillation counting was used to investigate the tissue localization of radioactivity in pregnant and non-pregnant rats. Tissue levels were maximal within 20 min, except for lachrymal glands, thymus and brain. Large amounts of radioactively labelled compounds, partly originating from active secretion, were present in the small intestine and caecum. Marked concentration of radioactively labelled compounds was also observed in the liver, spleen, lachrymal and salivary glands, lymph nodes, mammary glands, skin, bone marrow, and, to a lesser extent, in the lung, kidney and skeletal muscle. During six hours of experimental follow-up, plasma levels remained lower than corresponding tissue levels. At 1 h the radioactivity in fetuses was about three times lower than that in maternal blood. Within 48 h, more than 90% of the administered radioactivity was excreted. The amounts of radioactivity recovered in urine, faeces and expired air were about 19%, 48% and 24% respectively. After 48 h, 8% of the administered radioactivity was found in the carcass.
静脉注射[N-甲基-¹⁴C]-红霉素A后,在Wistar大鼠中研究了放射性标记化合物的组织分布和排泄情况。采用全身放射自显影和液体闪烁计数法研究了怀孕和未怀孕大鼠体内放射性的组织定位。除泪腺、胸腺和脑外,组织水平在20分钟内达到最高。小肠和盲肠中存在大量放射性标记化合物,部分源于主动分泌。在肝脏、脾脏、泪腺和唾液腺、淋巴结、乳腺、皮肤、骨髓中也观察到放射性标记化合物的明显浓度,在肺、肾和骨骼肌中的浓度较低。在6小时的实验随访期间,血浆水平始终低于相应的组织水平。1小时时,胎儿体内的放射性比母体血液中的低约三倍。在48小时内,超过90%的给药放射性被排泄。尿液、粪便和呼出气体中回收的放射性量分别约为19%、48%和24%。48小时后,在 carcass 中发现8%的给药放射性。 (注:“carcass”此处可能有误,推测可能是“body”之类的词,若有误请根据实际情况调整译文)