摘要
近年来,吸入制剂由于安全、高效等特点得到了越来越广的应用。为达到有效的肺部沉积,药物粒子的空气动力学粒径通常控制在6μm以下。喷雾冷冻干燥技术(spray freeze drying,SFD)作为一种新型的粉末制备技术,主要包括雾化、冷冻和干燥3个步骤,是传统喷雾干燥与冷冻干燥技术的结合。该技术具有以下优点:①低温操作避免了制备过程中的加热环节,适合于热敏感药物;②细小雾滴的快速冻结减少了药物的结晶或相分离;③干燥过程中,冻结的细颗粒能更加快速、均匀地生成粒径可控的多孔球形颗粒。SFD技术有助于改善粉末的理化性质,所得制品空气动力学粒径较小,适用于肺部给药。本文综述了SFD技术的过程、特点和分类,以及近年来在小分子药物和生物大分子吸入制剂中的应用进展。
Preparations for inhalation have been increasingly widely used in recent years because of their safety and high efficiency. To achieve an effective pulmonary deposition, inhalable drug particles should have an aerodynamic diameter below 6 μm. Spray freeze drying（SFD） technology is a relatively new dry powder formation technique that involves a three-step process of atomization, freezing and drying. As a combination of conventional spray drying with freeze drying, SFD technology has several advantages：① no heat treatment in the process, which is applicable to thermally labile ingredients;② ultra-fast freezing of fine droplets minimizes the crystallization and phase separation of drug;③ frozen fine particles are conductive to forming highly porous spherical particles with controllable size during the process of frozen drying. The dry powders obtained by SFD exhibit improved physicochemical characteristics and low aerodynamic diameters, thus rendering it suitable for pulmonary administration. This review describes the process, characteristics and classification of SFD technology, as well as the application in inhalation preparations for small molecules and biomacromolecules in recent years.
作者
王珏
朱壮志
张晓红
WANG Jue;ZHU Zhuangzhi;ZHANG Xiaohong(Dept.of Chemistry,Hehai University,Shanghai 200433;National Pharmaceutical Engineering and Research Center,China State Institute of Pharmaceutical Industry,Shanghai 201203;Shanghai Shyndec Pharmaceutical Co.,Ltd.,Shanghai 200137)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2018年第8期1083-1090,共8页
Chinese Journal of Pharmaceuticals
关键词
吸入制剂
喷雾冷冻干燥
制备方法
小分子药物
生物大分子
inhalation preparation
spray freeze-drying
preparation method
small molecule
biomacromolecule
