穿心莲内酯固体分散体的初步稳定性研究  

Preliminary Stability Study of Andrographolide Solid Dispersions

作　　者：张守德 赵国巍 刘梦 敖腾 冯唐德 ZHANG Shoude;ZHAO Guowei;LIU Meng;AO Teng;FENG Tangde(PET Center,Dept.of Radiology,the First Affiliated Hospital of Nanchang University,Nanchang 330006;Hubei Key Lab.of Purification and Application of Plant Anti-cancer Active Ingredients,Hubei University of Education,Wuhan 430205;Key Lab.of Modern Preparation of Traditional Chinese Medicine,Ministry of Education,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004;Dept.of Pharmacy,Afiliated Hospital of Jiangxi University of Traditional Chinese Medicine,Nanchang 330006)

机构地区：[1]南昌大学第一附属医院影像科,PET中心,江西南昌330006 [2]湖北第二师范学院植物抗癌活性物质提纯与应用湖北省重点实验室,湖北武汉430205 [3]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 [4]江西中医药大学附属医院药学部,江西南昌330006

出　　处：《中国医药工业杂志》2025年第2期217-223,共7页Chinese Journal of Pharmaceuticals

基　　金：江西省中医药管理局科技计划项目(2023A0374);江西省卫生健康委科技计划资助项目(202211402);江西中医药大学现代中药制剂教育部重点实验室2024年立项开发基金(Zdsys-202404);湖北第二师范学院引进人才科研启动基金(ESRC20240004)。

摘　　要：该研究以Soluplus^(■)为载体,采用喷雾干燥法制备了穿心莲内酯固体分散体,并以固体分散体的吸湿性、分子间相互作用、热稳定性、相对结晶度及溶出行为作为评价指标,考察了制品在不同温度[(40±2)和(60±2)℃]、不同相对湿度[(55±5)%、(75±5)%、(95±5)%]条件下的贮存稳定性。结果显示,受温度和相对湿度的影响,穿心莲内酯固体分散体的吸湿性、分子间相互作用、热稳定性、相对结晶度均发生了显著变化,进而导致溶出速率及溶出率下降。体外溶出结果还显示,在(40±2)℃的贮存条件下,虽然固体分散体的溶出率随相对湿度的增加而下降,但相较于原料药仍具有增溶优势;而在(60±2)℃的贮存条件下,即使相对湿度较低(55%),固体分散体的溶出率也已经下降到与原料药相仿的程度,增溶优势被完全破坏。结果表明,高温对该穿心莲内酯固体分散体的溶出稳定性影响较大。因此,该制剂应在温度≤(40±2)℃、相对湿度≤(55±5)%的环境下贮存。The andrographolide solid dispersions with Soluplus^(■) as a carrier were prepared by spray drying method.The hygroscopicity,intermolecular interaction,thermal stability,relative crystallinity,and dissolution behavior of the solid dispersions were used as evaluation indicators to investigate the storage stability of the products under different temperature[(40±2) and (60±2)℃]and relative humidity[(55±5)%,(75±5)% and (95±5)%]conditions.The results indicated that the hygroscopicity,intermolecular interaction,thermal stability,and relative crystallinity of andrographolide solid dispersions were significantly altered by the effects of temperature and relative humidity,which in turn led to adecrease in dissolution rate and dissolution.The results of dissolution in vitro also showed that under the storage conditionof (40±2)℃,although the dissolution of solid dispersion decreased with the increasing of relative humidity,it still hada solubilization advantage compared to the bulk drug.However,under the storage condition of (60±2)℃,even with arelative humidity(55%),the dissolution of the solid dispersions had decreased to a level similar to that of API,indicating that the solubilization advantage of solid dispersion was completely destroyed.These results showed that high temperature had a more significant impact on the dissolution stability of andrographolide solid dispersions.Therefore,this product should be stored in an environment with a temperature of no more then (40±2)℃ and a relative humidity of no more then (55±5)%.

关 键 词：穿心莲内酯 难溶性药物 Soluplus^(■) 固体分散体 贮存稳定性 温度 相对湿度 体外溶出 

分 类 号：R943[医药卫生—药剂学] R944.9[医药卫生—药学]