岩白菜素包合物渗透泵片制备工艺研究

Studies on Preparation of Bergenin Inclusion Compound Osmotic Pump Tablets

关键词:  岩白菜素  包合物  渗透泵片  制备工艺  控制释放

Key words:  bergenin  inclusion compound  osmotic pump tablets  preparation process  controlled release

摘要:

目的　利用β-环糊精(β-CD)包合技术改善微溶性药物岩白菜素的体外溶出行为，进而考察片芯及包衣处方对岩白菜素包合物渗透泵片体外释药性质的影响，并优选最佳片芯及包衣处方。方法 采用饱和水溶液法制备岩白菜素β-CD包合物，并测定其溶出速率和溶解度；根据不同时间的累积释放度，考察药物的释放情况，通过单因素考察及正交试验设计优化片芯及包衣处方。结果 聚氧乙烯的分子量和用量及甘露醇的用量，对岩白菜素包合物渗透泵片体外释药行为有影响。最后所得处方可在12 h内稳定释药且累积释放度可达到90%以上。结论 以岩白菜素β-CD包合物为中间体，可以制成零级释药特征显著的单室单层渗透泵片。

Abstract:

OBJECTIVE To improve the release character in vitro of slightly soluble bergenin by using β-cyclodextrin (β-CD) inclusion technology. And investigate the effect of the formulation of core tablets and coating on bergenin inclusion compound osmotic pump tablets release in vitro and optimize the formulation. METHODS The bergenin-β-CD inclusion complex was prepared by saturation water-solution. And the phase solubility and dissolution test was also determined. The release in vitro was studied through cumulative release measuring. And the optimal formulation of bergenin inclusion compound osmotic pump tablets was selected via the single-factor method and orthogonal design. RESULTS The molecular weight of polyethylene oxide (PEO), the amount of PEO and mannitol agents were all found to have great effect on release in vitro of bergenin inclusion compound osmotic pump tablets. The tablets with optimized formulation could achieve the desired zero-order release profile in 12 hours and the cumulative release over 90%. CONCLUSION The bergenin inclusion compound monolithic osmotic pump tablets could deliver drug constantly for 12 h based on the intermediat of bergenin-β-CD inclusion complex.