Yuasa H, Miyamoto Y, Iga T, Hanano M
J Pharmacobiodyn. 1984 Aug;7(8):604-6. doi: 10.1248/bpb1978.7.604.
A laminar flow absorption model for a carrier-mediated transport was developed to analyze the data of the intestinal single perfusion experiment. By using this model, we calculated the absorption rate and the concentration of the substance (drug) at the aqueous-intestinal membrane interface (cwall). The absorption rate was smaller than that predicted by the Michaelis Menten equation, using the concentration at the inlet (c0). The apparent Michaelis constant (Km,app) was larger than the true Michaelis constant (Km), if the data were analyzed by using the simulation curve of the absorption rate vs. c0 as the usual method. This is because cwall was smaller than c0. But the maximal transport velocity (Vmax) was little affected, because cwall became almost equal to c0 when c0 was high. By using this model, we can determine the values of Vmax and Km which are not biased by the unstirred water layer in the intestinal tract.
我们建立了一个载体介导转运的层流吸收模型,用于分析肠道单次灌注实验的数据。通过使用该模型,我们计算了物质(药物)在水-肠膜界面处的吸收速率和浓度(cwall)。使用入口处的浓度(c0)时,吸收速率小于米氏方程预测的值。如果按照常规方法使用吸收速率与c0的模拟曲线分析数据,表观米氏常数(Km,app)大于真实米氏常数(Km)。这是因为cwall小于c0。但是最大转运速度(Vmax)受影响较小,因为当c0较高时,cwall几乎等于c0。通过使用该模型,我们可以确定不受肠道中未搅动水层影响的Vmax和Km值。