Abstract: Validamycin-loaded silica hollow microspheres were prepared by in situ hydrolysis of tetraethyl orthosilicate (TEOS) in Water-Oil (W/O) emulsions. The microspheres were characterized by SEM, XRD, FT-IR and particle size distribution. The results indicated that the drug-loaded microspheres had an amorphous hollow spherical structure with the diameters of 7.5~15 mm. The amount of validamycin entrapped in the microspheres was about 31.9%(w). Sustained-releasing studies showed that the release time was about 240 min and more than 90% of the loaded drug in the microspheres was delivered, indicating good sustained release behavior of the drug-loaded microspheres.

Key words: hollow microcapsules, in situ preparation, validamycin, sustained release, silica

摘要： 利用正硅酸乙酯在W/O乳液中的原位水解聚合，成功制备了包埋井冈霉素的二氧化硅载药空心微球. 对所得产品进行了SEM, XRD, FT-IR和粒径分布等分析，结果表明，载药空心微球粒径分布窄，范围在7.5~15 mm，球状形貌良好，具有空心结构，呈无定型态. 热重分析表明载药空心微球的药物负载量约为31.9%(w)，缓释溶出实验显示载药空心微球药物释放持续时间约240 min，最终释放量达总载药量的90%以上.

关键词: 空心微球, 原位制备, 井冈霉素, 缓释, 二氧化硅