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泮托拉唑在健康男性受试者单次静脉注射和口服给药后的药代动力学。

Pharmacokinetics of pantoprazole following single intravenous and oral administration to healthy male subjects.

作者信息

Pue M A, Laroche J, Meineke I, de Mey C

机构信息

SmithKline Beecham, Department of Drug Metabolism and Pharmacokinetics, Welwyn, UK.

出版信息

Eur J Clin Pharmacol. 1993;44(6):575-8. doi: 10.1007/BF02440862.

Abstract

The plasma pharmacokinetics of pantoprazole have been investigated following single intravenous infusion and single oral administration at a dose of 40 mg to 12 healthy male subjects in a randomised cross-over study. Both treatments were generally well tolerated and no relevant compound-related adverse events were noted. The plasma pharmacokinetics of pantoprazole following intravenous infusion in this group of subjects were characterised by a total plasma clearance of 0.13 l.h-1 x kg-1 and apparent terminal elimination half-life 1.9 h. The apparent volume of distribution estimated at steady state (0.17 l.kg-1) was compatible with the localization of a major fraction of the compound in extracellular water. Following oral administration as an enteric-coated tablet formulation, a variable onset of absorption was followed by rapid attainment of maximum plasma concentrations of pantoprazole. Pantoprazole was well absorbed following oral administration; the absolute systemic bioavailability of the compound was estimated as 77% (95% CI, 67 to 89%).

摘要

在一项随机交叉研究中,对12名健康男性受试者进行了泮托拉唑单次静脉输注和单次口服40mg剂量后的血浆药代动力学研究。两种治疗方法总体耐受性良好,未观察到与化合物相关的不良事件。该组受试者静脉输注泮托拉唑后的血浆药代动力学特征为总血浆清除率为0.13 l·h⁻¹·kg⁻¹,表观终末消除半衰期为1.9小时。稳态时估计的表观分布容积(0.17 l·kg⁻¹)与该化合物大部分位于细胞外液的定位相符。口服肠溶片剂制剂后,吸收开始时间不一,随后迅速达到泮托拉唑的最大血浆浓度。泮托拉唑口服后吸收良好;该化合物的绝对全身生物利用度估计为77%(95%CI,67%至89%)。

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