Pidgeon C, Ong S, Liu H, Qiu X, Pidgeon M, Dantzig A H, Munroe J, Hornback W J, Kasher J S, Glunz L
Department of Medicinal Chemistry, School of Pharmacy, Purdue University, West Lafayette, Indiana 47907.
J Med Chem. 1995 Feb 17;38(4):590-4. doi: 10.1021/jm00004a004.
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.
当扩散限制摄取时,流体细胞膜是药物吸收的主要屏障。固定化人工膜(IAMs)是流体膜的固相模型,可预测一组同源头孢菌素在小鼠体内的口服药物吸收情况。IAMs还可预测药物透过Caco-2细胞的通透性。由于已知Caco-2细胞中的药物通透性与人类药物口服吸收相关,因此IAMs也可模拟人类的药物吸收情况。IAM分析在实验上很简单,并且可以对实验化合物进行大体积筛选以研究药物吸收。