吸收、代谢和排泄的盐酸tamsulosin男人。
文章的细节
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引用
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渡边Soeishi Y, Matsushima H, T, Higuchi年代,Cornelissen K,病房J
吸收、代谢和排泄的盐酸tamsulosin男人。
Xenobiotica。1996年6月26日(6):637 - 45。
- PubMed ID
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8810034 (在PubMed]
- 文摘
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1。吸收、排泄和代谢tamsulosin盐酸盐(TMS),一个强有力的α1-adrenoceptor阻断剂,研究了在四个健康男性受试者单一口服后14 c-tms剂量为0.2毫克。2。血浆和血液放射性浓度达到峰值(Cmax)给药后1小时内,然后拒绝biphasically。意思是终端消除半衰期11.8 h对等离子体和9.1 h血。各自的意思是放射性浓度时间曲线下的面积(AUC0-infinity)分别为122.8和57.8 ng等价物h /毫升。3所示。意思是不变的等离子Cmax TMS 13.0 ng / ml。等离子体的TMS拒绝biphasically水平。的意思是终端消除半衰期和AUC0-infinity 8.4 h和90.3 ng / ml。 The percentage of unchanged TMS to total radioactivity was 91% for Cmax and 74% for AUC0-infinity indicating small amounts of metabolites in plasma. 4. By 1 week post-dosing, 76.4% of the administered radioactivity was recovered in urine and 21.4% in faeces. The major part of radioactivity excreted in urine was recovered within the first 24 h (62.2% of the dose). 5. Unchanged TMS and 11 metabolites in 0-24-h urine samples were quantified. TMS accounted for 8.7% of the dose. Extensive excretion of the sulphate of the O-deethylated metabolite (M-1-Sul) and o-ethoxyphenoxy acetic acid (AM-1) was seen, accounting for 15.7 and 7.5% of the dose respectively.