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普罗替林在大鼠和食蟹猴体内的药代动力学。

Pharmacokinetics of proterguride in rat and cynomolgus monkey.

作者信息

Krause W, Hümpel M

机构信息

Department of Pharmacokinetics, Schering AG, Berlin, FR Germany.

出版信息

Xenobiotica. 1988 Jan;18(1):41-8. doi: 10.3109/00498258809055135.

DOI:10.3109/00498258809055135
PMID:3354231
Abstract
  1. The pharmacokinetics of proterguride were studied in rat and cynomolgus monkey using 3H- and 14C-labelled drug and a radioimmunoassay for concentration measurements of unchanged drug. 2. Proterguride was rapidly and completely absorbed at low doses but not completely at higher dose levels, especially in rat. 3. Bioavailability was 18% in the monkey (low and high doses) and 79% (low doses) and 38% (high dose), respectively, in the rat. 4. Proterguride was able to pass the blood-brain barrier achieving concentrations in brain similar to those in plasma. 5. Excretion of labelled compounds was mainly in the faeces in rat, but in monkey elimination was equal in faeces and urine.
摘要
  1. 使用3H和14C标记的药物以及用于测量未变化药物浓度的放射免疫分析法,在大鼠和食蟹猴中研究了普罗替林的药代动力学。2. 普罗替林在低剂量时迅速且完全吸收,但在较高剂量水平时不完全吸收,尤其是在大鼠中。3. 在猴子中(低剂量和高剂量)生物利用度为18%,在大鼠中分别为79%(低剂量)和38%(高剂量)。4. 普罗替林能够通过血脑屏障,在脑中达到与血浆中相似的浓度。5. 标记化合物在大鼠中的排泄主要在粪便中,但在猴子中,粪便和尿液中的排泄量相等。

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