Keller F, Scholle J
J Pharm Sci. 1981 Feb;70(2):195-8. doi: 10.1002/jps.2600700221.
The first-pass effect results from metabolism during the first liver passage of a drug given by mouth. The metabolism is described by the Michaelis-Menten equation, but the integrated form of the Michaelis-Menten equation has no explicit solution for concentration and its handling requires a computer. However, the presented nonlinear equation of the first-pass effect is an explicit integration of the Michaelis-Menten equation and involves only general mathematics. However, the problem of evaluating the Michaelis-Menten constants Vm and Km is not resolved. Therefore, linear equations are also derived, which correspond to previous clearance models.
首过效应源于口服给药后药物在肝脏首次通过时的代谢。这种代谢由米氏方程描述,但米氏方程的积分形式没有关于浓度的显式解,其处理需要计算机。然而,所提出的首过效应非线性方程是米氏方程的显式积分,只涉及一般数学。然而,评估米氏常数Vm和Km的问题尚未解决。因此,还推导了与先前清除模型相对应的线性方程。