将聚合物载药微球的溶解扩散模型与药代动力学模型相结合,计算了载药微球的药物控释性能的浓度时间曲线.采用叠加法计算了多次投药所产生的稳态药物浓度特征,探讨了释放速率、给药时间间隔对药物浓度曲线的影响.相对于口服药物溶液,微球中的药物通过载体的控制释放,血药浓度峰值有很大的降低,多次给药时载药微球的药物浓度波动也有大幅度的减小;适当的溶解速率可减小药物浓度波动,同时也满足治疗所要求的浓度值.
The drug release model of the polymer microspheres was combined with the pharmaco-kinetics model. Drug release, absorption, and elimination were integrated in a general model, with which the drug concentration in plasma was estimated. Based on drug concentration profiles of a single dose, the superposition method was used to estimate the accumulation for steady state, by which the effects of drug release and dosing interval were evaluated. In comparison to oral administration of drug solution, the microspheres released drug at a sustained rate, generating much lower peak concentration, and the drug concentration fluctuation was also decreased significantly for multiple dosages.