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[14C标记的7-[D(-)-α-(4-乙基-2,3-二氧代-1-哌嗪甲酰胺基)-α-(4-羟基苯基)乙酰胺基]-3-[(1-甲基-1H-四氮唑-5-基)硫甲基]-3-头孢烯-4-羧酸酯(14C-头孢哌酮)在大鼠和小鼠体内分布的放射自显影研究]

[The autoradiographic studies on the distribution of 14C-labelled sodium 7-[D(-)-alpha-(4-ethyl-2, 3-dioxo-1-piperazinecarboxamido)-alpha-(4-hydroxyphenyl)-acetamido]-3-[(1-methyl -1 H-tetrazol-5-yl) thiomethyl]-3-cephem-4-carboxylate (14C-cefoperazone) in rats and mice].

作者信息

Saikawa I, Takai A, Nakashima Y, Ikegami T, Hayakawa H, Takagi T, Yamauchi H

出版信息

Jpn J Antibiot. 1980 Oct;33(10):1097-103.

PMID:6451723
Abstract

The distribution of cefoperazone (CPZ), a new semisynthetic cephalosporin antibiotic, was studied by macroautoradiography following a single intravenous or subcutaneous administration of 100 mg/kg 14C-CPZ to rats, mice, pregnant mice and experimental pyelonephritic mice. (1) In whole body autoradiograms of rats administered subcutaneously and mice administered subcutaneously and intravenously, their distribution patterns of the radioactivity were found to be similar to each case. The radioactivity was distributed at high concentration in liver, kidney, lung, tongue, salivary gland, skin, gastrointestinal tracts and retina. The radioactivity was rapidly excreted in urine and bile. And it was observed that the radioactivity excreted through bile was not reabsorbed from gastrointestinal tracts. (2) In pregnant mice administered intravenously, the radioactivity was observed the same level as whole blood level in placenta, while was hardly observed in fetuses. (3) In the experimental pyelonephritic mice administered intravenously, a considerable radioactivity was concentrated on the acute inflammatory area.

摘要

通过宏观放射自显影术研究了新型半合成头孢菌素抗生素头孢哌酮(CPZ)的分布情况,给大鼠、小鼠、怀孕小鼠和实验性肾盂肾炎小鼠单次静脉注射或皮下注射100mg/kg的14C-CPZ。(1)在皮下给药的大鼠以及皮下和静脉给药的小鼠的全身放射自显影片中,发现每种情况下放射性的分布模式相似。放射性在肝脏、肾脏、肺、舌头、唾液腺、皮肤、胃肠道和视网膜中高浓度分布。放射性迅速经尿液和胆汁排泄。并且观察到经胆汁排泄的放射性不会从胃肠道重新吸收。(2)在静脉给药的怀孕小鼠中,在胎盘中观察到的放射性与全血水平相同,而在胎儿中几乎未观察到。(3)在静脉给药的实验性肾盂肾炎小鼠中,相当数量的放射性集中在急性炎症区域。

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