CORRELATION BETWEEN ORAL-DRUG ABSORPTION IN HUMANS AND APPARENT DRUG PERMEABILITY COEFFICIENTS IN HUMAN INTESTINAL EPITHELIAL (CACO-2) CELLS
CORRELATION BETWEEN ORAL-DRUG ABSORPTION IN HUMANS AND APPARENT DRUG PERMEABILITY COEFFICIENTS IN HUMAN INTESTINAL EPITHELIAL (CACO-2) CELLS
复制标题
DOI：
10.1016/0006-291x(91)91647-u
复制
发表时间：
1991-03-29
影响因子：
3.1
通讯作者：
KARLSSON, J
中科院分区：
文献类型：
--
作者：
ARTURSSON, P;KARLSSON, J
单层的分化良好的人肠上皮细胞系，Caco-2，被用作模型来研究被动药物吸收通过肠上皮。吸收速率常数（表观渗透系数表示），测定了20种药物和具有不同结构特性的肽。渗透系数范围约为5 × 10− 8 ~ 5 × 10−5cm/s。在人体吸收数据和Caco-2模型结果之间获得了良好的相关性。人体完全吸收的药物渗透系数大于1 × 10−6cm/s。吸收> 1%但< 100%的药物的渗透系数为0.1 - 1.0 × 10 - 6cm/s，而吸收< 1%的药物和肽的渗透系数≤ 1 × 10 - 7 cm/s。结果表明，Caco-2细胞单层可作为研究药物肠道吸收的模型。
Monolayers of a well differentiated human intestinal epithelial cell line, Caco-2, were used as a model to study passive drug absorption across the intestinal epithelium. Absorption rate constants (expressed as apparent permeability coefficients) were determined for 20 drugs and peptides with different structural properties. The permeability coefficients ranged from approximately 5 × 10−8to 5 × 10−5cm/s. A good correlation was obtained between data on aral absorption in humans and the results in the Caco-2 model. Drugs that are completely absorbed in humans had permeability coefficients > 1 × 10−6cm/s. Drugs that are absorbed to > 1% but < 100% had permeability coefficients of 0.1−1.0 × 10−6cm/s while drugs and peptides that are absorbed to < 1% had permeability coefficients ≤ 1 × 10−7cm/s. The results indicate that Caco-2 monolayers can be used as a model for studies on intestinal drug absorption.