The biological fate of sodium prasterone sulfate after vaginal administration. I. Absorption and excretion in rats.

M Sakaguchi, T Sakai, Y Adachi, T Kawashima, N Awata
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引用次数: 7

Abstract

The absorption and excretion of sodium prasterone sulfate (PS) (sodium dehydroepiandrosterone sulfate) were studied in rats after vaginal administration of 14C-PS. In late pregnant rats, maximum plasma level (Cmax) appeared at 2-4 h after dosing and both Cmax and the area under the plasma concentration-time curve (AUC) increased proportionally with increased dose up to 4.0 mg/kg. The radioactivity administered was almost completely recovered from urine and feces during a 72 h postdosing period. The percentages of radioactivity excreted in urine and feces were 58% and 40% of the dose, respectively. The biliary excretion was 46% of the dose within 48 h and about half of the radioactive biliary excreta entered the enterohepatic circulation system. The vaginal absorption of PS was markedly affected by the estrous cycle stage and the progress of pregnancy. The vaginal absorption of PS was predominant at metestrus and diestrus and during late pregnancy.

阴道给药后硫酸普酮钠的生物学命运。1 .大鼠吸收排泄。
研究14C-PS阴道给药后大鼠对硫酸脱氢表雄酮钠(PS)的吸收和排泄。妊娠晚期大鼠在给药后2 ~ 4 h出现最大血药浓度(Cmax), Cmax和血药-时曲线下面积(AUC)均随剂量增加成比例增加,最高可达4.0 mg/kg。在给药后72小时内,给药的放射性几乎完全从尿液和粪便中恢复。通过尿液和粪便排出的放射性百分比分别为剂量的58%和40%。48 h内胆道排出量为剂量的46%,约一半的放射性胆道排出物进入肠肝循环系统。PS的阴道吸收受发情周期和妊娠进程的影响明显。PS的阴道吸收主要发生在初潮、初潮和妊娠后期。
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