机械球磨法制备吲哚美辛包合物及其溶解性研究  

Preparation and Solubility of Indomethacin Inclusion Compound by Mechanical Ball Milling

作　　者：肖银 金婷毓 耿雪荣 Alexander V.Dushkin 朱兴一[1,2] XIAO Yin;JIN Ting-yu;GENG Xue-rong;Alexander V.Dushkin;ZHU Xing-yi(Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals,Zhejiang University of Technology,Hangzhou 310014,China;College of Pharmaceutical Sciences,Zhejiang University of Technology,Hangzhou 310014,China)

机构地区：[1]浙江工业大学长三角绿色制药协同创新中心,杭州310014 [2]浙江工业大学药学院,杭州310014

出　　处：《中国药学杂志》2022年第13期1099-1106,共8页Chinese Pharmaceutical Journal

基　　金：浙江省基础公益研究计划项目资助(No.LGF20H300011)。

摘　　要：目的研究机械球磨法制备的吲哚美辛(Indometacin,IMC)包合物对其溶解度及溶出度的影响。方法采用机械球磨法制备IMC/羟丙基-β-环糊精(HP-β-CD)和IMC/阿拉伯半乳聚糖(AG)包合物体系。通过相溶解度实验、差示扫描量热法、X射线衍射法、红外光谱、扫描电子显微镜、体外溶出和稳定性实验等对制备的包合物进行考察。结果相溶解度实验及表征实验表明IMC以无定型状态按照摩尔比1∶1被包合在辅料空腔中,包合物体系被成功制备且明显提高了药物的体外溶出速率。结论IMC/HP-β-CD和IMC/AG包合物对IMC均有良好的增溶效果。OBJECTIVE To study the effect of the inclusion complex of indomethacin(IMC)prepared by mechanical ball milling on its solubility and dissolution.METHODS The inclusion complex of IMC/hydroxypropyl-β-cyclodextrin(HP-β-CD)and IMC/arabinogalactan(AG)were prepared by mechanical ball milling.The inclusion complex was characterized by phase solubility,differential scanning calorimetry,powder X-ray diffractometry,Fourier-transformed infrared spectrophotometry,scanning electron microscope,as well as in vitro dissolution and stability test.RESULTS The phase solubility and characterization experiment showed that IMC was encapsulated in the cavity of excipients in an amorphous state with the molar ratio of 1∶1,the inclusion complex system was successfully prepared and significantly improved the dissolution rate of the drug in vitro.CONCLUSION The solubilization of IMC in inclusion complex of IMC/HP-β-CD and IMC/AG are improved.

关 键 词：机械球磨法 包合物 羟丙基-Β-环糊精 吲哚美辛 阿拉伯半乳聚糖 溶解度 

分 类 号：R944[医药卫生—药剂学]