摘要
目的:优选石丹颗粒中挥发油的包合工艺,为该制剂的临床应用与推广提供参考。方法:以挥发油包封率和包合物得率为综合评价指标,通过单因素试验比较饱和水溶液法和研磨法对包合效果的影响,采用正交试验考察挥发油与β-环糊精(β-CD)的投料比、加水量和研磨时间对包合工艺的影响,挥发油包合物进行TLC鉴别、UV鉴别、显微鉴别及稳定性考察。结果:采用研磨法包合,最佳包合工艺为β-CD与挥发油的投料比8∶1,加3倍量水研磨3 h;挥发油包封率87.04%,包合物得率89.12%。β-CD包合物在第0,1,3天的挥发油保留率分别为100%,89.23%,78.46%。结论:挥发油进入了β-CD空腔中形成相对稳定的β-CD包合物,制剂的稳定性显著提高。优选的包合工艺稳定可行,适合石丹颗粒的工业大生产。
Objective： To optimize inclusion process of volatile oil in Shidan granules, in order to provide a reference for clinical application and promotion of this preparation. Method： With inclusion rate of volatile oil and inclusion yield as comprehensive evaluation index, effects of saturated water solution and trituration method on inclusion were compared by single factor tests. Orthogonal design was used to optimize inclusion technology with ratio of volatile oil to β-eyclodextrin （β-CD）, the amount of water and grinding time as factors, inclusion complex of volatile oil were detected by TLC, UV and microscopic imaging, then its stability was investigated. Result： Trituration method was adopted, the best inclusion conditions were as follows： β-CD- volatile oil （8：1 ） , triturated 3 hours with 3 times the amount of water; encapsulation efficiency of volatile oil was 87.04% and yield of inclusion complex was 89. 12%. Volatile oil retention rates of β-CD inclusion complex in the zeroth, first, third day were 100% , 89.23% and 78.46%. Conclusion： Volatile oil is packed into cavity of β- CD and relatively stable β-CD inclusion complex is formed, stability of Shidan granules significantly increases. This optimized technology is stable and feasible, which is suitable for large-scale production of this preparation.
出处
《中国实验方剂学杂志》
CAS
CSCD
北大核心
2015年第1期32-34,共3页
Chinese Journal of Experimental Traditional Medical Formulae
关键词
石丹颗粒
挥发油
包合
Β-环糊精
研磨法
Shidan granules
volatile oil
inclusion
β-cyclodextrin
trituration method
