载体材料类型对黄体酮固体分散体体外性质的影响  

Effect of type of carrier material on the in vitro properties of solid dispersions of progesterone

作　　者：权静楠 程艺 周静宇 李蒙 王增明 刘楠 赵子明 张慧 郑爱萍 QUAN Jing-nan;CHENG Yi;ZHOU Jing-yu;LI Meng;WANG Zeng-ming;LIU Nan;ZHAO Zi-ming;ZHANG Hui;ZHENG Ai-ping(School of Pharmacy,Xuzhou Medical University,Xuzhou 221004,China;Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Academy of Military Sciences,Beijing 100850,China)

机构地区：[1]徐州医科大学药学院,江苏徐州221004 [2]军事科学院军事医学研究院毒物药物研究所,北京100850

出　　处：《药学学报》2024年第3期735-742,共8页Acta Pharmaceutica Sinica

基　　金：国家重点研发计划资助项目(2023YFC2706100).

摘　　要：本研究考察了不同载体材料对黄体酮固体分散体体外性质的影响,以流变学性质为考察指标,采用热熔挤出技术制备难溶性药物黄体酮固体分散体,并对固体分散体的体外性质进行表征。扫描电子显微镜显示固体分散体具有粗糙的表面和团聚的微观结构,呈不规则块状颗粒。差示扫描量热法和粉末X-射线衍射法显示固体分散体中黄体酮晶型的变化,由结晶态转变为无定型态。体外溶出度研究显示不同载体材料制备的固体分散体可以有效地改善药物的溶出速度。研究结果表明,载体材料类型对固体分散体的体外性质具有显著影响,为固体分散体在难溶性药物控释方面的研究提供了参考。This study investigated the effect of different carrier materials on the in vitro properties of progesterone solid dispersions.The solid dispersions of the insoluble drug progesterone were prepared by hot melt extrusion technique using rheological properties as the index of investigation,and the in vitro properties of the solid disper-sions were characterized.Scanning electron microscope revealed solid dispersions with rough surfaces and agglomerated microstructures into irregular lumpy particles.Differential scanning calorimetry and powder X-ray diffraction showed the change of progesterone crystalline form in solid dispersions from crystalline to amorphous state.In vitro dissolution studies showed that solid dispersions prepared with different carrier materials can effectively improve the dissolution rate of drugs.The results of the study showed that the type of carrier material had a significant effect on the in vitro properties of solid dispersions,providing a reference for the study of solid dispersions in the controlled release of insoluble drugs.

关 键 词：黄体酮 热熔挤出 载体材料 固体分散体 溶出度 

分 类 号：R943[医药卫生—药剂学]