高速熔融搅拌法制备双氯芬酸钾缓释微丸的处方工艺考察

Studies on preparation of diclofenac potassium sustained-release pellets by the melt pelletization in a high-speed mixer

采用高速熔融搅拌法制备含药微丸,以微丸体外累积释放度为指标考察工艺因素对微丸体外释放的影响,并设计正交实验对处方进行筛选。结果表明,确定的最佳的处方为每粒胶囊含有主药60 mg,固体石蜡100 mg,预胶化淀粉16 mg,柠檬酸8 mg及硫酸钙适量,所制备的双氯芬酸钾缓释微丸的体外释放行为符合Higuchi方程Q=0.248 7 t1/2+0.063 1(0.997 6)。采用高速熔融搅拌法制备的双氯芬酸钾缓释微丸表面光滑,圆整度高,具有良好的缓释效果。

Drug-contained pellets were prepared by the melt pelletization in a high-speed mixer, and the influencing factors of formulation and technique on pellets releasing profile were investigated used cumulative release as the indicator, and an orthogonal test was designed to optimize the prescription. Results shows that the best prescription for each capsule contains main drug 60 mg, paraffin wax 100 mg,pregela- tinized starch 16 rag,citric acid 8 mg and the amount of calcium sulfate,and the release of the drug from pellet was in accordance with Higuchi equation ： Q = 0. 248 7 t1/2 ±0. 063 1 （0. 997 6）. The diclofenac po- tassium sustained-release pellets made by this technique was smooth surface, high roundness and provided a rather good sustained-release profile.