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Method for building drug-oral-taking absorption forecasting and screening models

A technology for establishing methods and models, which is applied in the establishment of drug oral absorption prediction and screening models, and in the field of drug oral absorption prediction and screening, which can solve problems such as inability to cope with high-throughput screening and long experimental periods, and achieve cost and efficiency , easy operation and cost-saving effect

Inactive Publication Date: 2012-07-04
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The establishment method of the traditional Caco-2 cell model is: after the cells are plated, they are cultured on the basal medium for 21 days, the medium is changed every other day for the first 7 days, and the medium is changed every day for the next 14 days; however, the obvious defect of this model is that it takes up to The 21-day incubation time makes it too long for the experimental period when it is applied to predict the oral absorption of drugs, and cannot cope with the high-throughput screening required after the emergence of a large number of lead compounds today

Method used

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  • Method for building drug-oral-taking absorption forecasting and screening models
  • Method for building drug-oral-taking absorption forecasting and screening models
  • Method for building drug-oral-taking absorption forecasting and screening models

Examples

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Embodiment 1

[0036] Model building.

[0037] figure 1 For the transport pathways of drugs in cells in the Caco-2 cell model, the present invention establishes a fast Caco-2 cell monolayer model according to these transport pathways, that is, the above-mentioned drug oral absorption prediction and screening model, and the specific steps of the establishment method are as follows:

[0038] (1) DMEM (Dulbecco’s modified Eagle medium) was used as the basal medium, which contained 20% fetal bovine serum by volume, 1% non-essential amino acids, 100 U·mL -1 penicillin and 100 U·mL -1 Streptomycin; Caco-2 cells were cultured in 25 cm 2 Place in a card-type disposable culture bottle, place it in a 37°C incubator, and feed it with 5% CO 2 , cultivated under the condition of relative humidity of 90%, and replaced the basal medium every other day;

[0039] (2) Plate with rat tail collagen the day before seeding. The preparation method of rat tail collagen is as follows: take 100ml ultrapure water...

Embodiment 2

[0044]Using several standard substrates or markers to carry out transport experiments in the drug oral absorption prediction and screening model (hereinafter referred to as 7-day cell model) established in Example 1, the integrity, permeability, and paracellular The transport and expression of P-glycoprotein (P-gp) were verified, and further morphological investigations were carried out, and the experimental results were compared with the traditional 21-day Caco-2 cell model.

[0045] 1. The integrity of the cell model

[0046] The cell resistance value is an index to evaluate the integrity of the Caco-2 cell model. In this study, we use the cell potential meter (EVOM) to measure the resistance value of the fast Caco-2 model: the resistance value of the Transwell plate mold is measured before the cell seeding plate, and it is a blank value Ω1, and the resistance value measured when the plate is received is The final resistance value is Ω2, that is, Ω(TEER)=Ω1-Ω2.

[0047] ...

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Abstract

The invention relates to a method for building drug-oral-taking absorption forecasting and screening models. On the basis of a 21-day Caco-2 cell model built in early days forecasting compound absorption, a forecasting method of a 7-day Caco-2 cell model is further built, optimized and verified, and the testing index and the cell morphology of the model are optimized and verified, so that a most fitting Caco-2 cell model with drug-oral-taking absorption and high throughput screening is obtained. According to the method, the culture time of the cell model can be greatly shortened, so that the possibility of appearing pollution in the 21-day long-term culture of cells can be greatly reduced, the labor strength is reduced, and the oral-taking absorption forecasting and screening of a lot of lead compounds existing today are responded.

Description

technical field [0001] The invention relates to the field of drug screening models, in particular to a method for establishing a drug oral absorption prediction and screening model, which can be applied to the prediction and screening of drug oral absorption. Background technique [0002] Caco-2 cells (the human colon carcinoma cell line, Caco-2 for short) are derived from human colon cancer cells and are currently recognized as one of the most classic in vitro models for predicting drug absorption in the human intestine. Caco-2 cells can undergo epithelial differentiation spontaneously under culture conditions and can form tight junctions to differentiate into villi and basal surfaces. Their morphology, functional expression of marker enzymes, and infiltration characteristics are similar to those of small intestinal epithelial cells. Therefore, this This kind of cells can mimic small intestinal epithelial cells and is widely used in the study of physical and biochemical bar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12Q1/02
Inventor 黄民蔡伊科毕惠嫦胡晋卿蔡大可
Owner SUN YAT SEN UNIV
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