均匀设计在马来酸噻吗洛尔缓释片研究中的应用

Uniform Design of Timolol Maleate Sustained Release Tablet

设计了缓释制剂的药物动力学体外模拟方法，根据马来酸噻吗洛尔缓释片的体外释放特征，模拟其体内药物动力学，求算模拟血药浓度；并以模拟血药曲线的半峰宽与峰值的比值作为定量指标，评价缓释片的释放特性。应用均匀设计法对处方和工艺条件进行优化，得到最佳处方和工艺。统计结果及相关性分析表明，按最佳处方和工艺制备的马来酸噻吗洛尔缓释片的体内测定结果与模拟值具有一定的相关性。

The reported research established the pharmacokinetics simulation method of sustained release system. The calculation of the plasma concentration and pharmacokinetic parameters in timolol maleate sustained release tablet was based on the simulation method. The ratio of half peak width to the peak height of simulated plasma levels of timolol maleate was defined as the key parameter for uniform disign of the sustained release tablet to optimize the formula and production process conditions. The correlation and statistic comparison of in vivo data and in vitro simulation data of the timolol maleate sustained release tablets prepared by the optimized formula and production process proved that the uniform design and in vitro simulation method were acceptable.