IAM CHROMATOGRAPHY - AN IN-VITRO SCREEN FOR PREDICTING DRUG MEMBRANE-PERMEABILITY

被引:246
作者
PIDGEON, C
ONG, SW
LIU, HL
QIU, XX
PIDGEON, M
DANTZIG, AH
MUNROE, J
HORNBACK, WJ
KASHER, JS
GLUNZ, L
SZCZERBA, T
机构
[1] ELI LILLY & CO,LILLY CORP CTR,LILLY RES LABS,INDIANAPOLIS,IN 46285
[2] REGIS CHEM CO,MORTON GROVE,IL 60053
关键词
D O I
10.1021/jm00004a004
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Fluid cell membranes are the main barrier to drug absorption when diffusion limits uptake. Immobilized artificial membranes (IAMs) are solid phase models of fluid membranes that predicted oral drug absorption in mice for a homologous set of cephalosporins. IAMs also predicted drug permeability through Caco-2 cells. Since drug permeability in Caco-2 cells is known to correlate with the oral absorption of drugs in humans, IAMs may also model drug absorption in humans. IAM analysis is experimentally simple, and large-volume screening of experimental compounds for drug absorption is possible.
引用
收藏
页码:590 / 594
页数:5
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