穿心莲内酯固体分散体片的处方优化及初步稳定性考察  

Formulation Optimization of Andrographolide Solid Dispersion Tablets and Preliminary Stability Analysis

作　　者：蔡萍 曾庆云 赵国巍 欧丽泉 高翠芸 CAI Ping;ZENG Qingyun;ZHAO Guowei;OU Liquan;GAO Cuiyun(Key Lab.of Modern Preparation of Traditional Chinese Medicine,Ministry of Education,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004;School of Pharmacy,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004)

机构地区：[1]江西中医药大学现代中药制剂教育部重点实验室,江西南昌330004 [2]江西中医药大学药学院,江西南昌330004

出　　处：《中国医药工业杂志》2021年第7期928-933,共6页Chinese Journal of Pharmaceuticals

基　　金：江西省中医药管理局科技计划项目(2019A010);江西省教育厅科学技术项目(GJJ201233);国家自然科学基金地区科学基金项目(81560654)。

摘　　要：首先以聚乙烯吡咯烷酮(PVP K30)为载体、穿心莲内酯(1)为模型药制备固体分散体(1-SD),再基于1-SD制备固体分散体片(1-SDT)。然后采用单因素试验、星点设计-响应面法,以片剂崩解时间、120 min时溶出率为评价指标,优化1-SDT的处方。确定的最佳处方为:α-乳糖17.4%,交联聚维酮12%,硬脂酸镁1%。将所得的1-SD和1-SDT于(40±2)℃、相对湿度(75±5)%放置90 d,初步考察其稳定性。结果显示,放置60和90 d时,1-SD和1-SDT的溶出性能均较初始时显著下降(P<0.05);1-SDT的重结晶程度比1-SD更高,但二者120 min时的溶出率无显著差异(P>0.05)。With andrographolide(1)as a model drug,the solid dispersions(1-SDs)was prepared with polyvinylpyrrolidone(PVP K30)as a carrier,then the solid dispersion tablets(1-SDTs)were prepared.The formulation of 1-SDTs was optimized by single factor experiment and central composite design-response surface methodology with disintegration time and the dissolution rate at 120 min as the evaluation indicators.The optimal formulation was as follows:17.4%of α-lactose,12%of cross-linked povidone and 1%of magnesium stearate.The preliminary stabilities of 1-SDs and 1-SDTs stored at(40±2)℃and relative humidity of(75±5)%for 90 days were investigated.The results showed that the dissolution stability profiles of 1-SD and 1-SDT stored for 60 and 90 days were significantly declined compared with the initial products(P<0.05).The recrystallization degrees of 1 from the 1-SDTs stored for 60 and 90 days were higher than those of the corresponding 1-SDs.However,there was no significant difference in dissolution rate at 120 min between 1-SDs and 1-SDTs stored for 60 and 90 days.

关 键 词：穿心莲内酯 固体分散体 片剂 稳定性 重结晶 溶出度 

分 类 号：R944.4[医药卫生—药剂学]