Walter B A, Agha B J, Digenis G A
Division of Medicinal Chemistry, College of Pharmacy, University of Kentucky, Lexington 40536-0081.
Toxicol Appl Pharmacol. 1988 Nov;96(2):258-68. doi: 10.1016/0041-008x(88)90085-3.
The disposition of nonoxynol-9 labeled with carbon-14 at the ethylene oxide units was studied following an iv or vaginal administration to female Sprague-Dawley rats. The results from the vaginal administration studies indicate 12.8% absorption of 14C radioactivity in 6.0 hr and 37.7% in 24.0 hr. Tissue distribution studies showed that the small and large intestines, including their contents, had the highest 14C activity by either route of administration. Radiomonitored HPLC of bile collected at 6.0 hr and urine at 6.0, 24.0, and 48.0 hr following an iv injection of [14C]nonoxynol-9 showed that the compound was completely metabolized in the body of the rat. The metabolites were primarily excreted in the feces and secondarily in the urine. Analysis of urinary metabolites containing the carbon-14 label, 6.0 hr following an iv dose, indicated the presence of highly polar neutral (53.27%) and acidic (39.23%) species.
在对雌性斯普拉格-道利大鼠进行静脉注射或阴道给药后,研究了环氧乙烷单元标记有碳-14的壬苯醇醚-9的处置情况。阴道给药研究结果表明,6.0小时内14C放射性的吸收率为12.8%,24.0小时内为37.7%。组织分布研究表明,无论采用哪种给药途径,小肠和大肠(包括其内容物)的14C活性最高。在静脉注射[14C]壬苯醇醚-9后6.0小时收集的胆汁以及6.0、24.0和48.0小时收集的尿液的放射性监测HPLC显示,该化合物在大鼠体内完全代谢。代谢产物主要通过粪便排出,其次通过尿液排出。静脉给药剂量后6.0小时对含碳-14标记的尿液代谢产物进行分析,结果表明存在高极性中性(53.27%)和酸性(39.23%)物质。