和肝理脾颗粒的包合及制粒工艺研究

摘要

OBJECTIVE:To optimize the inclusion and granulating technology of Hegan lipi granules. METHODS:Using yield of inclusion complex and inclusion rate as comprehensive index,the ratio of β-CD to volatile oil,inclusion temperature,in-clusion time as factors,orthogonal test was adopted to optimize the inclusion technology of volatile oil from Hegan lipi granules. Using the comprehensive score of moldability,dissolubility,mobility and hygroscopicity as index,the ratio of drug to excipients, volume fraction and amount of ethanol as factors,orthogonal test was adopted to optimize the granulating technology of Hegan lipi granule powdered extract. The quality of prepared granule was evaluated. RESULTS:The optimal inclusion technology of volatile oil was that the ratio of volatile oil to β-CD was 1∶6 and the inclusion time was 1 h with inclusion temperature of 50 ℃ by saturat-ed aqueous solution method. The optimal granulating technology was that the ratio of drug to excipients was 1∶1 (extract pow-der-soluble starch-dextrin ratio was 5∶3∶2),90% ethanol were used as the wetting agent with a weight of 20% extract powder. The verification tests showed that comprehensive scores of 3 batches of granules were 96.8,95.7,95.9(RSD=0.65%,n=3). The quality of them were all in line with the requirement. CONCLUSIONS:Optimized inclusion and granulating technology of Hegan li-pi granules are stable and reliable,and can be used for the industrialized production.%目的：优化和肝理脾颗粒的包合及制粒工艺条件。方法：以包合物得率和包合率的综合评分为指标，以β-环糊精（β-CD）与挥发油配比、包合温度、包合时间为考察因素，采用正交试验优化和肝理脾颗粒总挥发油包合工艺；以成型率、溶化率、流动性和吸湿率的综合评分为指标，以药辅比、润湿剂乙醇的体积分数及用量为因素，采用正交试验优选和肝理脾颗粒浸膏粉的制粒工艺；对所制颗粒进行质量评价。结果：总挥发油最优包合工艺为总挥发油与β-CD之比为1∶6，50℃恒温条件下采用饱和水溶液法包合1 h；浸膏粉的最优制粒工艺为药辅比1∶1（浸膏粉-可溶性淀粉-糊精之比为5∶3∶2），90％乙醇用量为浸膏粉用量的20％。验证试验中3批颗粒的综合评分分别为96.8、95.7、95.9分（RSD＝0.65％，n＝3），且质量均符合要求。结论：优化所得和肝理脾颗粒的包合及制粒工艺稳定、可靠，可用于工业化大生产。