磷酸奥司他韦前药（奥司他韦膦酸）经雾化或静脉给药后在大鼠肺部的药代动力学
Pulmonary Pharmacokinetics of Oseltamivir Carboxylate in Rats after Nebulization or Intravenous Administration of Its Prodrug, Oseltamivir Phosphate.
机构信息
INSERM, U1070, UFR de Médecine Pharmacie, Université de Poitiers, TSA 51106, Poitiers, France.
Université de Poitiers, UFR Médecine-Pharmacie, Poitiers, France.
出版信息
Antimicrob Agents Chemother. 2019 May 24;63(6). doi: 10.1128/AAC.00074-19. Print 2019 Jun.
Abstract
The aim of this study was to investigate the pharmacokinetics of oseltamivir phosphate, a prodrug, and its active moiety in plasma and lung after its nebulization and intravenous administration in rats. Only 2% of prodrug was converted into active moiety presystematically, attesting to a low advantage of oseltamivir phosphate nebulization, suggesting that oseltamivir phosphate nebulization is not a good option to obtain a high exposure of the active moiety at the infection site within lung.
摘要
本研究旨在探讨磷酸奥司他韦（前药）及其活性代谢物在大鼠雾化和静脉给药后血浆和肺部的药代动力学。仅有 2%的前药在给药前转化为活性代谢物，这证明了磷酸奥司他韦雾化的优势较低，表明磷酸奥司他韦雾化不是在肺部感染部位获得高活性代谢物暴露的好选择。
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