Paliwal J K, Ramesh D, Gupta R C
Pharmacokinetics and Metabolism Division, Central Drug Research Institute, Lucknow, India.
Int J Clin Pharmacol Res. 1997;17(1):23-30.
CDRI compound 81/470 (AH) is a new broad-spectrum anthelminthic agent under development for clinical and veterinary application. We herewith report the synthesis of 14C-labelled AH, and a study of the tissue distribution and excretion of radioactivity after administering a single 1 mg/kg p.o. or i.v. dose in young male rats. After oral administration of the dose, percent radioactivity recovered in 24-h urine, faeces and tissues were 17.9, 59.7 and 22.9 respectively. The levels were below detection limit in brain and gonads up to 24 h. In bile-duct-cannulated rats, the majority (37.8 +/- 2.8 and 43.8 +/- 6.4) of the radioactivity was excreted in the bile within 24 h of p.o. and i.v. administration, respectively. After an oral dose (1 mg/kg), the urinary excretion of radioactivity in rats was found to be approximately one-half (21 +/- 5.7, 18.3 +/- 2.1) of that obtained by i.v. administration of an equal dose (40.2 +/- 3.1 and 35 +/- 1.3), in bile-duct-intact and cannulated rats respectively.
CDRI化合物81/470（AH）是一种正在开发用于临床和兽医应用的新型广谱驱虫剂。我们在此报告14C标记的AH的合成，以及在年轻雄性大鼠中单次口服或静脉注射1 mg/kg剂量后放射性的组织分布和排泄研究。口服该剂量后，24小时尿液、粪便和组织中回收的放射性百分比分别为17.9、59.7和22.9。在长达24小时内，脑和性腺中的水平低于检测限。在胆管插管大鼠中，口服和静脉注射给药后24小时内，大部分放射性（分别为37.8±2.8和43.8±6.4）经胆汁排泄。口服剂量（1 mg/kg）后，在胆管完整和插管的大鼠中，放射性的尿排泄量分别约为静脉注射同等剂量（40.2±3.1和35±1.3）的一半（分别为21±5.7和18.3±2.1）。
