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壬苯醇醚-9在妊娠大鼠体内的经阴道吸收与处置

Transvaginal absorption and disposition of nonoxynol-9 in gravid rats.

作者信息

Buttar H S

出版信息

Toxicol Lett. 1982 Oct;13(3-4):211-6. doi: 10.1016/0378-4274(82)90214-4.

Abstract

The placental transfer, maternal tissue distribution and elimination of [14C]-nonoxynol-9 (25 mg/kg) were studied during the first 6 h in 15-day pregnant rats treated intravaginally. Blood concentrations of 14C reached a maximum of 2.0 +/- 0.06 micrograms/ml in 1 h, declining slowly in 3 h, and remaining steady thereafter. At 6 h, the highest levels of 14C were recorded in the maternal urinary bladder, followed by those in the liver, kidney, adrenal and thyroid. The maternal brain showed lowest uptake of 14C among all tissues examined. After 6 h, the 14C concentrations in the uterus or placenta were similar to that of maternal plasma, whereas the mean concentrations of 14C both in the amniotic fluid and fetus were approx. one-third of that of the maternal plasma. About 44% of the administered dose was absorbed from the vagina, and nearly 17% of the per vaginum applied radioactivity was recovered in the urine and feces over 6 h. The results show that nonoxynol-9 (N-9) is rapidly absorbed into the blood stream from the vagina of gravid rat and that the fetal uptake of 14C is much lower than that of the placenta.

摘要

对经阴道给予[14C]-壬苯醇醚-9(25毫克/千克)的15天孕鼠在最初6小时内进行了研究,观察其胎盘转运、母体组织分布及消除情况。14C的血药浓度在1小时内达到最高值2.0±0.06微克/毫升,3小时内缓慢下降,此后保持稳定。6小时时,母体膀胱中14C水平最高,其次是肝脏、肾脏、肾上腺和甲状腺。在所检查的所有组织中,母体大脑对14C的摄取最低。6小时后,子宫或胎盘中14C浓度与母体血浆相似,而羊水中和胎儿体内14C的平均浓度约为母体血浆的三分之一。约44%的给药剂量从阴道吸收,在6小时内,经阴道给予的放射性物质近17%在尿液和粪便中回收。结果表明,壬苯醇醚-9(N-9)可从妊娠大鼠阴道迅速吸收进入血流,且胎儿对14C的摄取远低于胎盘。

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