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反卷积原理在药物吸收及肠内首过消除估计中的应用。

Use of the deconvolution principle in the estimation of absorption and pre-systemic intestinal elimination of drugs.

作者信息

Pithavala Y K, Soria I, Zimmerman C L

机构信息

Graduate Program in Pharmaceutics, College of Pharmacy, University of Minnesota.

出版信息

Drug Metab Dispos. 1997 Nov;25(11):1260-5.

PMID:9351902
Abstract

The deconvolution principle was used to evaluate the extent of absorption and first-pass elimination of selected drugs. In the first example, deconvolution of the portal blood profiles of etretinate (ET, a synthetic retinoid) indicated that there was significant gut-wall conversion of ET to acitretin (ETA, the primary metabolite of ET) during a 60-min intestinal perfusion of ET. In the second example, deconvolution was used to confirm that the extent of carbovir disappearing from the gastrointestinal lumen was matched by the extent of carbovir appearance in the portal blood. Thus, deconvolution has several important applications in the study of absorption and intestinal first-pass metabolism.

摘要

反卷积原理用于评估所选药物的吸收程度和首过消除情况。在第一个例子中,对阿维A(ET,一种合成类维生素A)门静脉血药浓度曲线进行反卷积分析表明,在对ET进行60分钟的肠道灌注期间,ET在肠壁有显著转化为阿维A酸(ETA,ET的主要代谢产物)的情况。在第二个例子中,反卷积用于确认从胃肠道腔中消失的卡波韦的量与门静脉血中出现的卡波韦的量相匹配。因此,反卷积在吸收和肠道首过代谢研究中有几个重要应用。

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