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Single-dose pharmacokinetics of atrasentan, an endothelin-A receptor antagonist.
The Journal of Clinical Pharmacology ( IF 2.4 ) Pub Date : 2001-04-18 , DOI: 10.1177/00912700122010258
E Samara 1 , S Dutta , G Cao , G R Granneman , M S Dordal , R J Padley
Affiliation  

The pharmacokinetics of 1, 10, 23.25, and 139.5 mg doses of atrasentan was assessed in a placebo-controlled, double-blind, single oral dose study in 24 healthy male subjects. Atrasentan was well tolerated. Atrasentan pharmacokinetics was linear in the 1 to 23.25 mg dose range, with some dose dependency in the highest dose group. Harmonic mean terminal half-life was similar across all dose groups (20-25 h). Apparent oral clearance was low (12 L/h) for the highest dose group compared with the other three dose groups (21-27 L/h). The apparent volume of distribution was large (approximately 6 L/kg), consistent with extensive tissue distribution.

中文翻译:

阿托森坦(一种内皮素-A受体拮抗剂)的单剂量药代动力学。

在安慰剂对照,双盲,单次口服剂量研究中,对24位健康男性受试者评估了1、10、23.25和139.5 mg剂量的阿曲生坦的药代动力学。阿曲生坦耐受性良好。在1至23.25 mg剂量范围内,阿曲生坦的药代动力学是线性的,在最高剂量组中有一定的剂量依赖性。所有剂量组(20-25小时)的谐波平均终末半衰期均相似。与其他三个剂量组(21-27 L / h)相比,最大剂量组的表观口腔清除率低(12 L / h)。表观分布量大(约6 L / kg),与广泛的组织分布一致。
更新日期:2019-11-01
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