吸入用布地奈德混悬液的处方和制备工艺的优化

Formulation and preparation optimization of Budesonide suspensions for inhalation

目的 优化吸入用布地奈德混悬液的处方与制备工艺。方法 以沉降体积比与再分散性的综合评分为指标,采用正交试验法对处方进行优化;采用高压均质技术制备布地奈德混悬液,以单因素试验法优化制备工艺。结果 优选的助悬剂为羧甲基纤维素钠,润湿剂为吐温80,絮凝剂为枸橼酸钠,其用量分别为0.10%、0.05%、0.05%;优化的工艺条件为低压、均质2-3次;按优化后的处方和工艺所制备的布地奈德混悬液的平均粒径为1.70±0.15μm,平均Zeta电位为-24.1±0.4 m V,布地奈德的含量为标示量的99.3%。结论 按优化后的处方和工艺所制备的混悬液的理化稳定性良好,达到了吸入用混悬液的质量要求。

OBJECTIVE To optimize the formulation and preparation process of Budesonide （Bud） suspensions for inhalation. METHODS Bud suspensions was prepared by high - pressure homogeneous technique. Formulation optimization was carried out by orthogonal test with composite score of sedimentation ratio and re - dispersibility as index. Single factor experiment was applied to optimize the preparation process. RESULTS The optimized suspending agent, wetting agent and flocculant were sodium carboxymethylcel- lulose,tween 80 and sodium citrate. Their formula dosage were 0.10% ,0.05% and 0.05% respectively in optimum formulation. The suspension was prepared by high - pressure homogeneous technique with a relatively low pressure repeated to 2 - 3 times. The mean diameter and Zeta potential of the prepared suspension were 1.70 ± 0. 15 μm and - 24.1 ± 0.4 mV respectively, and the average content of Bud was 99.3% of the labeled amount. CONCLUSION The physicochemical stabilities of the prepared suspension with optimized formulation and preparation process are good, and meets the quality requirements of the suspensions for inhalation.