热熔挤出技术在药剂学研究中的应用  

Application of hot-melt extrusion technique in pharmaceutical research

作　　者：于宁 何承辉 黄伟[2] 邢建国 刘宣麟 

机构地区：[1]新疆维吾尔自治区药物研究所,乌鲁木齐830004 [2]中国医学科学院北京协和医学院药物研究所药物制剂研究室,北京100050

出　　处：《国际药学研究杂志》2014年第4期437-443,共7页Journal of International Pharmaceutical Research

基　　金：新疆维吾尔自治区科技基础条件平台建设项目;维吾尔药口服新制剂释药技术平台项目(PT1304)

摘　　要：热熔挤出技术是指将药物、增塑剂或聚合物等辅料在熔融状态下混合,以一定的压力、速度和形状挤出形成产品的技术。它结合固体分散体技术和机械制备的诸多优势,具有连续化操作、减少粉尘、挤出过程持续时间短、不使用有机溶剂和水、不需加热干燥,不易发生水解等优点。该技术在提高难溶性药物溶出度、掩盖药物异味、增强药物稳定性和维持药物释放等方面具有突出优势,并有良好的重现性、极高的生产效率和在线监测。因此,近年来被广泛应用于药剂研究开发中,制备各种不同类型的制剂,如速释制剂、缓释制剂、胃肠定位释放制剂和经皮给药制剂等。本文将综述热熔挤出技术用于药剂研究的优点及其近年来在药剂研究中的应用。Hot-melt extrusion （HME） is the process of pumping raw materials with a rotating screw under the elevated temperature and pressure through a die to from a product with the uniform shape. This technique combines many advantages of solid dispersion technology and mechanical preparation, including dust reduction, short duration of extrusion process, without use of organic solvents and water, without heat drying and hydrolysis, etc. In addition, it has the superiority in solubility, taste masking, drug stability and drug release. Besides, this technique has good reproducibility, high production efficiency, and it can be online monitored in the mass production. Therefore, this technique is widely used in the research and development of drug dosage forms involved in rapid and immediate drug release, sustained drug release, gastrointestinal drug site-specific release, transdermal drug delivery systems and so on. This paper reviews the advantages of HME and its recent application in the pharmaceutical research.

关 键 词：热熔挤出技术 难溶性药物 溶解度 掩味 稳定性 

分 类 号：R94[医药卫生—药剂学]