论文部分内容阅读
直到最近人们才重视立体化学对药动学、药效学的影响。已报道的药物有:双异丙吡胺、非洛地平和维拉帕米。本文研究了手性药物活性、非活性对映体对药效的影响,提出了消旋药物是药效滞后现象发生的重要原因。对口服单剂量外消旋药物后该药的两种对映体用线性-房室模型进行模拟分析,假定活性对映体和无活性对映体每次只有一个动力学参数不同。药效学拟合采用E_(max)模型,假定无平衡延迟、无活性或拮抗性代谢物的形成及
Until recently people only paid attention to the influence of stereochemistry on pharmacokinetics and pharmacodynamics. Drugs that have been reported are: dipipridylamine, felodipine and verapamil. In this paper, the chiral drug activity, the effect of inactive enantiomers on the efficacy, the race drug is proposed lag phenomenon is an important reason. The two enantiomers of the drug after a single oral dose of a racemic oral administration were simulated using a linear-atrioventricular model, assuming that only one kinetic parameter differs between the active enantiomer and the inactive enantiomer. Pharmacodynamic fit using the E max model, assuming no unbalanced delay, formation of inactive or antagonistic metabolites, and