公开(公告)号：US20180106783A1

公开(公告)日：2018-04-19

申请号：US15847092

申请日：2017-12-19

Applicant: Hitachi High-Technologies Corporation

Inventor： Ryosuke TAKAHASHI ,  Katsuhiro KANDA ,  Yusuke SHIMIZU ,  Hisashi ICHIKAWA

IPC: G01N33/50 ,  G01N33/15 ,  C12M1/00 ,  C12M1/12 ,  C12M1/34 ,  G01N35/00 ,  G01N35/04

Abstract: 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.

公开(公告)号：US20160209403A1

公开(公告)日：2016-07-21

申请号：US14914278

申请日：2014-11-26

Applicant: HITACHI HIGH-TECHNOLOGIES CORPORATION

Inventor： Ryosuke TAKAHASHI ,  Katsuhiro KANDA ,  Yusuke SHIMIZU ,  Hisashi ICHIKAWA

IPC: G01N33/50 ,  C12M1/34 ,  C12M1/00 ,  G01N33/15 ,  C12M1/12

CPC classification number: G01N33/5067 ,  B01L3/5085 ,  C12M25/00 ,  C12M29/00 ,  C12M41/46 ,  C12M47/20 ,  G01N33/15 ,  G01N33/502 ,  G01N2035/00425 ,  G01N2035/0418

Abstract: 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.

Abstract translation: 本发明的应用使得能够定量分离出候选药物化合物（母体化合物及其代谢物），一种通过转运蛋白和扩散物排泄到基底外侧（基底/基底外侧），一个排泄到内腔（Apical） ，还有一个留在细胞中。 这使得能够确定所施用的候选药物化合物的总量和分数的分配比。 可以评估给药的候选药物化合物的动力学，从而能够体外筛选展示功效的药物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量化基底外侧（基底/基底外侧）流出的一部分（一部分管腔（Apical）侧排泄物）和剩余部分来了解体外药代动力学总体图像的装置和方法 在已经施用于细胞以确定每个级分的分配比例的药物的细胞中。