125I-力达霉素在小鼠和大鼠体内的组织分布与排泄
Tissue distribution and excretion of 125I-lidamycin in mice and rats.
作者信息
Liu You-Ping, Li Quan-Sheng, Huang Yu-Rong, Liu Chang-Xiao
机构信息
National Key Laboratory of Pharmakinetics and Pharmacodynamics, Tianjin Institute of Pharmaceutical Research, 308 An-Shan West Road, Tianjin 300193, China.
出版信息
World J Gastroenterol. 2005 Jun 7;11(21):3281-4. doi: 10.3748/wjg.v11.i21.3281.
AIM
To investigate the tissue distribution, urinary and fecal excretions of (125)I-lidamycin ((125)I-C-1027) in mice and its biliary excretion in rats.
METHODS
The total radioactivity assay (RA method) and the radioactivity assay after precipitation with 200 mL/L trichloroacetic acid (TCA-RA method) were used to determine the tissue distribution, and the urinary and fecal excretions of (125)I-C-1027 in mice and its biliary excretion in rats.
RESULTS
Tissue concentrations reached the peak at the fifth minute after administration of (125)I-C-1027 to mice. The highest concentration was in kidney, and the lowest in brain at all test-time points. The organs of the concentrations of (125)I-C-1027 from high to low were kidney, lung, liver, stomach, spleen, uterus, ovary, intestine, muscle, heart, testis, fat, and brain in mice. The accumulative excretion amounts of 0-24 h, and 0-96 h after administration of (125)I-C-1027 were 68.36 and 71.64% in urine, and 2.60 and 3.21% in feces of mice, respectively, and the accumulative excretion amount of 0-24 h was 3.57% in bile in rats.
CONCLUSION
Our results reflect the characteristics of the tissue distribution, urinary and fecal excretions of (125)I-C-1027 in mice and the biliary excretion of (125)I-C-1027 and its metabolites in rats, and indicate that (125)I-C-1027 and its metabolites are mainly distributed in kidney, and excreted in urine.
目的
研究（125）I-力达霉素（（125）I-C-1027）在小鼠体内的组织分布、尿液和粪便排泄情况以及在大鼠体内的胆汁排泄情况。
方法
采用总放射性测定法（RA法）和用200 mL/L三氯乙酸沉淀后的放射性测定法（TCA-RA法）来测定（125）I-C-1027在小鼠体内的组织分布、尿液和粪便排泄情况以及在大鼠体内的胆汁排泄情况。
结果
给小鼠注射（125）I-C-1027后第5分钟，组织浓度达到峰值。在所有检测时间点，浓度最高的是肾脏，最低的是脑。在小鼠体内，（125）I-C-1027浓度由高到低的器官依次为肾脏、肺、肝脏、胃、脾脏、子宫、卵巢、肠道、肌肉、心脏、睾丸、脂肪和脑。给小鼠注射（125）I-C-1027后0-24小时和0-96小时的累积排泄量，尿液中分别为68.36%和71.64%，粪便中分别为2.60%和3.21%，大鼠胆汁中0-24小时的累积排泄量为3.57%。
结论
我们的结果反映了（125）I-C-1027在小鼠体内的组织分布、尿液和粪便排泄特点以及（125）I-C-1027及其代谢产物在大鼠体内的胆汁排泄特点，表明（125）I-C-1027及其代谢产物主要分布在肾脏，并通过尿液排泄。
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