岩白菜素高载药量渗透泵型控释片的制备

Preparation of Bergenin Osmotic Pump Tablets with High Drug Loading

目的:制备难溶性药物岩白菜素高载药量单室单层渗透泵型控释片。方法:以渗透泵片常用辅料为混合载体材料制备固体分散体,利用等渗原理优化片芯处方;以岩白菜素累积释放度为指标,采用星点设计-效应面法优化包衣处方。结果:PEG 1500质量分数1.30%,包衣增重9.5%时,制得的岩白菜素高载药量渗透泵片累积释放度接近80%,符合零级释药特征。结论:充分发挥辅料多种功能可有效提高渗透泵片载药量;优化片芯与衣膜处方的方法能显著缩短试验周期,为渗透泵制剂处方设计提供一种新思路。

Objective： To prepare single-chamber and single-layer osmotic pump-controlled release tablets of bergenin with high drug loading, which was a poorly water-soluble drug. Method： Solid dispersion was prepared with common excipients of osmotic pump tablets as mixed carrier material, prescription of tablets core was optimized by isoosmotic principle; With cumulative release of bergenin as index, coating formulation was selected by central composite design-response surface methodology. Result： When the mass fraction of PEG 1500 was 1.30% and coating gain was 9.5% , cumulative release of prepared osmotic pump tablets of bergenin with high drug loading was nearly 80%, it fitted zero-order release profile. Conclusion： It could effectively increase drug loading of osmotic pump tablets by giving full play to functions of excipients; Methods of optimizing formulation of tablet core and coating could significantly shorten experiment cycle, and this study could provide a new approaches of prescription design of osmotic pump preparation.