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1.
公开(公告)号:EP3272852A1
公开(公告)日:2018-01-24
申请号:EP17186423.4
申请日:2014-11-26
摘要: Application of the present invention enables quantification of fractions of candidate pharmaceutical compounds (a parent compound and its metabolites), one excreted to the basolateral (Basal/Basolateral)-side via transporters and by diffusion, one excreted to the lumen (Apical)-side, and one remained in the hepatocyte cells. This enables determination of the total amount of the administered candidate pharmaceutical compounds and the distribution ratio of the fractions. The kinetics of the administered candidate pharmaceutical compounds can be evaluated, thereby enabling in vitro screening of an enormous number of candidate pharmaceutical compounds for drug candidates exhibiting the efficacy. The object of the present invention is to provide an apparatus and method for understanding a total picture of pharmacokinetics in vitro by quantifying a fraction of basolateral (Basal/Basolateral) efflux, a fraction of lumen (Apical)-side excretion, and a fraction remaining in a cell of a drug which has been administered to the cell to determine the distribution ratio of each fraction.
摘要翻译: 本发明的应用使得能够量化候选药物化合物(母体化合物及其代谢物)的部分,其中一部分通过转运蛋白和通过扩散而排泄至基底外侧(基底/基底外侧)侧,一个排泄至内腔(顶端)侧 ,一个留在肝细胞中。 这使得能够确定施用的候选药物化合物的总量以及这些级分的分配比例。 可以评估施用的候选药物化合物的动力学,由此能够体外筛选显示功效的候选药物的大量候选药物化合物。 本发明的目的是提供一种用于通过定量分析基底外侧(基底/基底外侧)外排,内腔部分(顶端)侧排泄和剩余部分的分数来理解体外药代动力学总图的装置和方法 在已经给予细胞的药物的细胞中以确定每个部分的分配比率。
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2.
公开(公告)号:EP3023489B1
公开(公告)日:2017-11-01
申请号:EP14866627.4
申请日:2014-11-26
CPC分类号: G01N33/5067 , C12M25/00 , C12M29/00 , C12M41/46 , C12M47/20 , G01N33/15 , G01N33/502 , G01N2035/00425 , G01N2035/0418
摘要: Application of the present invention enables quantification of fractions of candidate pharmaceutical compounds (a parent compound and its metabolites), one excreted to the basolateral (Basal/Basolateral)-side via transporters and by diffusion, one excreted to the lumen (Apical)-side, and one remained in the cells. This enables determination of the total amount of the administered candidate pharmaceutical compounds and the distribution ratio of the fractions. The kinetics of the administered candidate pharmaceutical compounds can be evaluated, thereby enabling in vitro screening of an enormous number of candidate pharmaceutical compounds for drug candidates exhibiting the efficacy. The object of the present invention is to provide an apparatus and method for understanding a total picture of pharmacokinetics in vitro by quantifying a fraction of basolateral (Basal/Basolateral) efflux, a fraction of lumen (Apical)-side excretion, and a fraction remaining in a cell of a drug which has been administered to the cell to determine the distribution ratio of each fraction.
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公开(公告)号:EP3272852B1
公开(公告)日:2020-03-18
申请号:EP17186423.4
申请日:2014-11-26
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