戊己丸胃漂浮微丸制备工艺

摘要

We prepared the Wuji gastric-floating pellets and evaluated their characteristics in vitro.Carrier material of pellets was the sodium alginate, and the gastric-floating pellets were manufactured by ionic gelation. The influence of sodium alginate concentration, the ratio of sodium alginate and calcium carbonate, the ratio of sodium alginate and solid dispersion, calcium chloride concentration, acetic acid concentration and the ratio of Eudragit L100 and extracts were evaluated by single factor experiment. Central composite design/response surface method was used to optimize the formula, with the floating capacity of pellets as indicator.In the optimal formula,sodium alginate concentration was 20 g/L,the mass ratio of sodium alginate and calcium carbonate was 3. 5, the mass ratio of sodium alginate and solid dispersion was 2,calcium chloride concentration was 46 g/L,acetic acid concentration was 68 g/L,and the mass ratio of Eudragit L100 and extracts was 2. The optimal gastric-floating pellets can float for more than 10 hours and release the drug following the requirements of the sustained release formulation. The preparation condition was mild and process was simple, and the model established by response surface method showed good predictability.%以海藻酸钠为微丸载体材料，离子凝胶法制备戊己丸胃漂浮微丸。单因素实验考察了海藻酸钠质量浓度、CaCO3与海藻酸钠质量比、海藻酸钠与固体分散体质量比、CaCl2质量浓度、醋酸质量浓度、Eudragit L100与提取物质量比对微丸的影响。在此基础上以持漂率为指标，采用星点设计效应面法进一步优化其处方。筛选出最优处方：海藻酸钠20 g／L、CaCO3与海藻酸钠质量比3．5、海藻酸钠与固体分散体质量比2、CaCl246 g／L、醋酸68 g／L、Eudragit L100与提取物质量比2。最终制备微丸体外持续漂浮超10 h，体外释放性能满足缓释制剂要求。此方法制备条件温和，制备工艺简单，效应面法所建立数学模型预测性好。