乙酰半胱氨酸片的制备及处方优化

Preparation and Formulation Optimization of Acetylcysteine Tablets

关键词:  乙酰半胱氨酸  DOE  粉末直压

Key words:  acetylcysteine tablets  DOE  powder direct pressing

摘要:

摘要：目的 乙酰半胱氨酸（N-Acety-L-cysteine, NAC）原料带有类似蒜的嗅味，对酸碱湿热等氧化条件极为敏感，限制了其制剂工艺的开发。进行NAC片不同制备工艺的对比，筛选质量稳定可控、操作可行性高、更具市场竞争力的工艺进行处方优化，得出最佳处方。方法 根据参比制剂信息和先验知识确定初处方。首先筛选出较优工艺，然后进行处方筛选和DOE设计，以溶出度、脆碎度和产品稳定性为考察指标，优化处方。结果 确定粉末直压法为较优工艺，NAC的粒度分布对产品质量有显著影响，筛选得到较优的NAC的粒度分布范围为150-400 μm。结论 粉末直压工艺适用于NAC片的制备，工艺重现性好、产品适口性佳，关键质量符合要求。

Abstract:

ABSTRACT：OBJECTIVE Acetylcysteine has an odor similar to garlic, and is extremely sensitive to oxidation conditions such as moisture and heat, which limits the development of its preparation process. Different preparation processes of NAC tablets were compared, and the optimum prescription was obtained by selecting the process with stable and controllable quality, high operation feasibility, and more market competitiveness. METHODS Initial prescription was determined based on reference formulation information and prior knowledge. The optimal process was selected , then the formulation was screened and DOE design was carried out to optimize the prescription, and the dissolution, friability and stability were taken as the inspection indexes . RESULTS Powder direct compression method was determined as the optimal process, the particle size distribution of NAC had a significant effect on the stability. The optimal particle size distribution of NAC was 150-400 μm. CONCLUSION The powder direct compression method is suitable for preparation of NAC tablets , which has good reproducibility, palatability, and the key quality meets the requirements.