星点设计-效应面法优化莲心总碱固体分散体渗透泵控释片处方

Optimization of osmotic pump controlled release tablets of liensinine solid dispersion by central composite design-response surface methodology

目的优选莲心总碱固体分散体渗透泵控释片的处方工艺,考察莲心总碱固体分散体渗透泵控释片体外释药特征。方法以莲心碱在2、6、12 h的累积释放度(Y_2、Y_6、Y_(12))为评价指标,采用3因素5水平星点设计,考察促渗剂Na Cl的用量(X_1)、致孔剂PEG 400的用量(X_2)、包衣增重(X_3)对药物累积释放度的影响,对结果进行二项式拟合,效应面法筛选出最佳处方,进行预测分析和验证试验,并对莲心总碱固体分散体渗透泵控释片体外释药行为进行模型拟合。结果莲心总碱固体分散体渗透泵控释片的最优处方为NaCl用量为166.0 mg,PEG400用量为80.5%,包衣增重为3.5%。结论采用星点设计-效应面法得到了莲心总碱固体分散体渗透泵控释片的处方优化模型,该模型预测性良好,制备的莲心总碱固体分散体渗透泵控释片符合设计要求,且其体外溶出实验符合零级释放特征。

Objective To optimize the prescription of liensinine solid dispersion osmotic pump controlled release tablet and research its release characteristics in vitro. Methods The cumulative release percent in 2, 6, and 12 h and the linear correlation coefficient of cumulative release curve were taken as evaluation indexes to select the optimal prescription by using the central composite designresponse surface methodology（CCD-RSM）. The main factors of influence on drug release, which were the dosage of Na Cl and PEG 400, and coating agent thickness. Results The optimal prescription for liensinine solid dispersion osmotic pump controlled release tablet were as follows： Na Cl dose was 166.0 mg, PEG 400 content was 80.5%, and the coating weight gain was 3.5%. Conclusion The prescription optimization model of liensinine solid dispersion osmotic pump controlled release tablet is optimized by CCD-RSM, and it is proved to follow zero-order release kinetics.