Zheng X L, Zhao F, Meng X S, Yang L X, Gao J G
Zhongguo Yao Li Xue Bao. 1989 Nov;10(6):561-4.
The blood radioactivity-time curve after iv calcium [3H]metronidazola-mate in mice was to be a diexponential model. It was rapidly distributed in various tissues. The highest radioactivities were found in liver and kidney, followed by lung, blood, heart, spleen, and the lowest in brain and testes. Bile and bone marrow contained only a slight radioactivity. In 7 d the cumulative excretion of radioactivity was 52 +/- 17% of the iv dose in urine and 10.3 +/- 2.4% in feces. The measurement by TLC and liquid scintillation counting of urine taken at 24 h after iv calcium [3H] metronidazolamate to mice revealed that approximately 77% of the total radioactivity in urine was excreted as the drug in unchanged form and 7% as its hydrolysate, metronidazole. Calcium [3H]metronidazolamate remained at a high level in blood on account of its longer T1/2 beta (34 h) and 20% were bound to plasma protein, thus making it available for longterm fractional radiotherapy of tumors.
静脉注射[³H]甲硝唑钙镁后，小鼠血液放射性-时间曲线呈双指数模型。它在各种组织中迅速分布。肝脏和肾脏中的放射性最高，其次是肺、血液、心脏、脾脏，而大脑和睾丸中的放射性最低。胆汁和骨髓中仅含有少量放射性。7天内，放射性的累积排泄量在尿液中为静脉注射剂量的52±17%，在粪便中为10.3±2.4%。对静脉注射[³H]甲硝唑钙镁的小鼠在24小时后采集的尿液进行薄层色谱法和液体闪烁计数测量显示，尿液中总放射性的约77%以未改变形式的药物排出，7%以其水解产物甲硝唑排出。由于[³H]甲硝唑钙镁的β半衰期较长（34小时），其在血液中保持较高水平，并且20%与血浆蛋白结合，因此可用于肿瘤的长期分次放疗。
