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奈替米星在大鼠体内的吸收、分布、代谢及排泄(IV)。在肾脏中的分布及向胎儿或乳儿的转移(作者译)

[Absorption, distribution, metabolism and excretion of netilmicin in rats (IV). Distribution in kidney and transmigration to fetus or suckling (author's transl)].

作者信息

Fujino A, Uda F, Nomura A, Tokiwa T

出版信息

Jpn J Antibiot. 1982 Apr;35(4):979-86.

PMID:7097992
Abstract

Distribution in kidney and transmigration to fetus or suckling in rats were studied in male, pregnant or lactating rats after intramuscular administration of 14C-netilmicin (20 mg/kg). 1. After administration to male rats, the radioactivity in the kidney declined slowly with a half-life of approximately 6 days. 2. The radioactivity in the kidney was distributed in the renal cortex. The distribution pattern was further investigated by means of microautoradiography. The radioactivity was specifically observed in lysosomal granules of the proximal tubules at 6 hours after administration and reached maximum at 24 hours after administration, then declined gradually. On the other hand, the radioactivity in the distal tubules was lower than that of the proximal tubules. The highest radioactivity in the distal tubules was detected later than 24 hours after administration. 3. In pregnant rats (20th day of gestation), the distribution of radioactivity in the tissues were almost the same as those in the male rat. The small amount of radioactivity was detected in the fetal kidney and bone. 4. In mother rats (14 days after parturition), the radioactivity in the milk was 3 approximately 4 mcg equivalent of netilmicin/ml during 24 hours after administration. The small amount of radioactivity (0.13% of dose) was observed in the gastrointestinal contents of a suckling with 6 hours after administration.

摘要

对雄性、怀孕或哺乳期大鼠肌肉注射14C-奈替米星(20mg/kg)后,研究了其在大鼠肾脏中的分布以及向胎儿的转运或对幼崽的哺乳情况。1. 给雄性大鼠给药后,肾脏中的放射性缓慢下降,半衰期约为6天。2. 肾脏中的放射性分布于肾皮质。通过显微放射自显影进一步研究了分布模式。给药后6小时在近端小管的溶酶体颗粒中特异性观察到放射性,给药后24小时达到最大值,然后逐渐下降。另一方面,远端小管中的放射性低于近端小管。远端小管中的最高放射性在给药后24小时后才检测到。3. 在怀孕大鼠(妊娠第20天)中,组织中的放射性分布与雄性大鼠几乎相同。在胎儿肾脏和骨骼中检测到少量放射性。4. 在母鼠(分娩后14天)中,给药后24小时内乳汁中的放射性约为3至4μg等效奈替米星/毫升。给药后6小时在一只幼崽的胃肠道内容物中观察到少量放射性(占剂量的0.13%)。

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