靶向给药系统的体内药物动力学模型

Pharmacokinetics Model for Targeted Drug Delivery Systems

作者根据实验观测,建立了靶向给药系统的体内多室线性循环动力学模型。利用大型电子计算机推导出了靶向给药系统的血液药时函数式和靶器官药时函数式,据此,可由血药数据求得靶器官的药时曲线,并进一步求出靶器官的药物动力学参数。作者还用自行研制的肝靶向给药系统—毫微球在动物体内的血药曲线和肝脏药时曲线验证了该模型的正确性,并根据由靶器官药时函数式计算出的肝脏药时曲线,用统计矩方法分析了该靶向给药系统的肝脏药代动力学规律,给出了肝脏药物动力学参数。提出用相对靶向性指数作为靶向给药系统靶向性的定量评价指标。对模型的特点及有关问题进行了较深入的讨论。

Analyzing the observedphenomena and the data collected in re-search, we developed a multi-compartmentlinear recirculation model for targeteddrug delivery systems and figured out thefunction formulas of the drug concentra-tion-time in blood and target organ bycomputing. According to this model, thedrug concentration-time curve for the tar-get organ can be plotted with referenceto the data on blood; the pharmacokine-tics parameters of the target organ canalso be obtained. We further detected thepracticability of the model by using thecurves of drug concentration-time in bloodand target organ(liver) of liver-targetingnanoparticles obtained from animal tests.Based on the liver drug concentration-time curve calculated by the function for-mula of target organ and the statisticalmoment, the pharmacokinetics behaviour ofthe target organ(liver) was analysed andthe pharmacokinetics parameters of liverwere obtained. We suggest that the 'rela-tive targeting index' be used for quan-titative evaluation of the targeted drugdelivery system.