不同载体材料、制备方法对穿心莲内酯固体分散体稳定性的影响  

Effects of different carrier materials and preparation methods on the stability of andrographolide solid dispersions

作　　者：欧丽泉 曾庆云 赵国巍 蔡萍 衷友泉[2] OU Li-quan;ZENG Qing-yun;ZHAO Guo-wei;CAI Ping;ZHONG You-quan(Ministry of Education Key Laboratory for Modern Preparations of Traditional Chinese Medicine,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,China;College of Pharmacy,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,China)

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：《中成药》2020年第12期3117-3122,共6页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金地区科学基金项目(81560654);江西省中医药管理局科技计划项目(2019A010);江西省中医药大学博士科研启动基金课题(2019WBZR001);中药学一流学科科研启动项目(JXSYLXK-ZHYAO058)。

摘　　要：目的考察不同载体材料、制备方法对穿心莲内酯固体分散体稳定性的影响。方法以聚乙二醇8000(PEG8000)十二酸酯、PEG8000十六酸酯、PEG8000二十二酸酯为载体材料,真空干燥法、喷雾干燥法为制备方法,在高温[(40±2)℃]、高湿[(75±5)%]下测定固体分散体含水量、相对结晶度、溶出度。结果各固体分散体60 d内吸湿稳定性良好,含水量小于2%。PEG8000二十二酸酯固体分散体相对结晶度低于PEG8000十二酸酯、PEG8000十六酸酯固体分散体。与真空干燥法比较,喷雾干燥法制备的固体分散体相对结晶度更低,穿心莲内酯溶出曲线变化更小。结论提高载体材料(PEG8000饱和脂肪酸酯)亲脂性、应用喷雾干燥法有利于改善穿心莲内酯固体分散体重结晶稳定性和溶出稳定性。AIM To investigate the effects of different carrier materials and preparation methods on the stability of andrographolide solid dispersions.METHODS With polyethylene glycol 8000(PEG8000)laurate,PEG8000 palmitate,PEG8000 behenate as carrier materials,and vacuum drying method,spray drying method as preparation methods,the water content,relative crystallinity degree and dissolution rate of solid dispersions were determined under high temperature[(40±2)℃]and high humidity[(75±5)%].RESULTS Various solid dispersions demonstrated good moisture absorption stability within 60 d,along with the water contents of less than 2.0%.PEG8000 behenate solid dispersions displayed lower relative crystallinity degree than PEG8000 laurate solid dispersions and PEG8000 palmitate solid dispersions.The solid dispersions prepared by spray drying method exhibited lower relative crystallinity degree as compared with those prepared by vacuum drying method,and the dissolution curves for andrographolide showed smaller changes.CONCLUSION Enhancing the lipophilicity of carrier materials(PEG8000 saturated fatty acid esters)and applying spray drying method can help to improve the recrystallization stability and dissolution stability of andrographolide solid dispersions.

关 键 词：穿心莲内酯 固体分散体 载体材料 制备方法 稳定性 

分 类 号：R944[医药卫生—药剂学]