摘要
目的:研究无定形聚合物聚丙烯酸树脂Ⅱ(EudragitⅡ)制备的穿心莲内酯固体分散体的优良性质,为固体分散体的载体选择提供参考依据。方法:以无定形聚合物EudragitⅡ为载体材料,按穿心莲内酯-载体质量比为1∶3,采用喷雾干燥法制备穿心莲内酯固体分散体,并用傅里叶变换红外光谱(FTIR)、热重分析(TG)、X-射线衍射(XRD)、差示扫描量热(DSC)、扫描电镜(SEM)、比表面积、粒径和溶出度测定穿心莲内酯固体分散体的理化性质及溶出行为。结果:FTIR光谱和TG分析说明在穿心莲内酯固体分散体和物理混合物中穿心莲内酯与EudragitⅡ之间都存在分子间相互作用,其中穿心莲固体分散体具有更好的热稳定性;DSC和XRD分析说明无定形载体EudragitⅡ制备的固体分散体中穿心莲内酯主要以无定形形式存在;SEM显示,固体分散体中穿心莲内酯由块状晶体形态变为了不规则的圆形形态;同时与物理混合物相比,穿心莲内酯固体分散体具有更大的比表面积、更大的孔体积和更小的粒径等粉体学性质;溶出实验表明穿心莲内酯固体分散体具有增大溶出的优势,效果明显。结论:以无定形载体EudragitⅡ制备的穿心莲内酯固体分散体具有优良的理化性质,同时比表面积大,孔体积大的特征更有利于水分子的进入,从而有效地增大穿心莲内酯的溶出速率。
OBJECTIVE To study the excellent properties of andrographolide solid dispersion prepared by the amorphous carrierEudragit Ⅱ, so as toprovide a reference for the carrier selection of solid dispersion. METHODS The solid dispersions of andrographolide were prepared by spray drying method with amorphous polymer Eudragit Ⅱ as carrier material and the mass ratio of andrographolide to carrier was 1∶3. The physicochemical properties and dissolution behavior of andrographolide solid dispersion were determined by fourier transform infrared spectroscopy(FTIR), thermogravimetric analysis(TG), X-ray diffraction(XRD), differential scanning calorimetry(DSC), scanning electron microscopy(SEM), specific surface area, particle size, and dissolution. RESULTS FTIR and TG indicated that there was an intermolecular interaction between andrographolide and Eudragit Ⅱ in the andrographolide solid dispersion and physical mixture, in which andrographolide solid dispersions had better thermal stability;DSC and XRD analysis indicated that andrographolide in the solid dispersion was mainly present in amorphous form. SEM showed that the andrographolide in the solid dispersion changed from a block crystal form to an irregular circular shape. Meanwhile, the andrographolide solid dispersion had larger specific surface area, larger pore volume and smaller particle size than the physical mixture. The dissolution results showed that the andrographolide solid dispersion could significantly increase the dissolution percentage of andrographolide. CONCLUSION The andrographolide solid dispersion prepared by the amorphous carrier Eudragit Ⅱ had excellent physicochemical properties. At the same time, the larger specific surface area and larger pore volume of andrographolide solid dispersion were more condusivel to the entry of water molecules, therebyincreasing the dissolution rate of andrographolide in the andrographolide solid dispersion.
作者
张守德
赵国巍
衷友泉
曾庆云
欧丽泉
梁新丽
董伟
ZHANG Shou-de;ZHAO Guo-wei;ZHONG You-quan;ZENG Qing-yun;OU Li-quan;LIANG Xin-li;DONG Wei(Key Lab.of Modern Preparation of Traditional Chinese Medicine,Ministry of Education,Jiangxi University of Traditional Chinese Medicine,Jiangxi Nanchang 330004,China;School of Pharmacy,Jiangxi University of Traditional Chinese Medicine,Jiangxi Nanchang 330004,China;Key Lab.of Applied Surface and Colloid Chemistry,Ministry of Education,School of Chemistry and Chemical Engineering,Shaanxi Normal University,Shaanxi Xi'an 710119,China)
出处
《中国医院药学杂志》
CAS
北大核心
2019年第23期2370-2374,共5页
Chinese Journal of Hospital Pharmacy
基金
国家自然科学基金地区科学基金项目(编号:81560654)
江西省卫生计生委中医药科研课题项目(编号:2015A055)
江西省教育厅科学技术研究项目(编号:GJJ170735)
中药学一流学科科研启动基金专项课题(编号:JXSYLXK-ZHYAO058)
关键词
穿心莲内酯
固体分散体
理化性质
溶出度
andrographolide
solid dispersion
physicochemical property
dissolution
