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脑室注射后¹¹¹铟-二乙三胺五乙酸在大鼠和小鼠体内的行为(作者译)

[In vivo behavior of 111In-DTPA in rat and mouse after intra-ventricular administration (author's transl)].

作者信息

Matsushima H, Kato M, Sugimura Y, Hazue M

出版信息

Radioisotopes. 1977 Nov;26(11):784-9. doi: 10.3769/radioisotopes.26.11_784.

Abstract

In vivo behavior of 111In-DTPA in rat and mouse after intra-ventricular administration was studied. Thus, 50 muCi and 35 muCi of 111In-DTPA was injected intra-ventricularly to rat and mouse respectively. At specific time intervals, the animals were sacrificed, then distribution in organs was determined by radioactivity counting and autoradiographic method. Urinary and fecal excretion were separately collected and excretion rates were estimated. Metabolites in urine of rat were examined with chromatography. A part of 111In-DTPA injected intra-ventricularly to the animals migrated to subarachnoid space, then radioactivity in cerebrospinal fluid effused into blood with about 1 hr initial half-life. Blood clearance was also rapid, about 1 hr after administration the blood level reached maximum and then decreased showing an initial half-life of about 1 hr. The predominant excretion route in rat was urinary and about 90% and 5% of administered dose were excreted within 48 hr through urine and feces respectively. Judging from the Rf-value of radioactivity peak on chromatograms, 111In-DTPA seems to be excreted without suffering any metabolic change. Concerning to the behavior of 111In-DTPA in male and female rat, no difference was observed, and the distribution pattern of 111In-DTPA in mouse was similar to that of rat.

摘要

研究了经脑室注射后¹¹¹铟-二乙三胺五乙酸(¹¹¹In-DTPA)在大鼠和小鼠体内的行为。因此,分别向大鼠和小鼠脑室内注射50微居里和35微居里的¹¹¹In-DTPA。在特定时间间隔处死动物,然后通过放射性计数和放射自显影法确定器官中的分布。分别收集尿液和粪便排泄物并估算排泄率。用色谱法检测大鼠尿液中的代谢产物。向动物脑室内注射的部分¹¹¹In-DTPA迁移至蛛网膜下腔,然后脑脊液中的放射性以约1小时的初始半衰期渗入血液。血液清除也很快,给药后约1小时血药浓度达到峰值,然后下降,显示初始半衰期约为1小时。大鼠的主要排泄途径是尿液,给药剂量的约90%和5%分别在48小时内通过尿液和粪便排出。从色谱图上放射性峰的比移值判断,¹¹¹In-DTPA似乎在未发生任何代谢变化的情况下排出。关于¹¹¹In-DTPA在雄性和雌性大鼠中的行为,未观察到差异,¹¹¹In-DTPA在小鼠中的分布模式与大鼠相似。

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