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环丙沙星白蛋白微球的制备及体外释药特性

李凤前*, 胡晋红, 陆彬, 朱全刚, 孙华君   

  1. 1.华西医科大学药学院, 成都 610041;
    2.第二军医大学长海医院药学部, 上海 200433
  • 收稿日期:2000-08-23 修回日期:2000-12-18 出版日期:2001-03-15 发布日期:2001-03-15
  • 通讯作者: 李凤前*

Ciprofloxacin Loaded Bovine Serum Albumin Microspheres: Preparation and Drug Release Characterization In Vitro

Li Fengqian*, Hu Jinhong, Lu Bin, Zhu Quangang, Sun Huajun   

  1. 1. School of Pharmacy, West China University of Medical Sciences, Chengdu 610041;
    2. Department of Pharmacy, Shanghai Hospital, Second Military Medical University, Shanghai 200433
  • Received:2000-08-23 Revised:2000-12-18 Online:2001-03-15 Published:2001-03-15
  • Contact: Li Fengqian*

摘要: 以牛血清白蛋白为囊材, 采用喷雾干燥工艺将环丙沙星制成微球。以水溶液系统制备的白蛋白微球不含任何有机溶剂, 外观呈圆球型,微球粒径在1~5 μm之间, 符合干粉末肺部吸入给药的要求。以不同的环丙沙星/白蛋白比例(1:11:21:4)配制喷雾干燥样品, 制得微球的载药量分别为46.93%32.96% 20.56% (n = 3), 药物的包封产率均在90% 以上。采用不同的粉末加热变性温度(100~120 °C) 和时间(3~6~12 小时), 对喷雾干燥制得的粉末白蛋白微球进行热变性处理,考察热变性后微球的体外释药情况, 热变性程度越大, 药物释放愈缓慢, 说明可通过改变热变性条件调控微球中药物的释放。

关键词: 喷雾干燥, 微球, 环丙沙星, 热变性, 体外释放

Abstract: Ciprofloxacin loaded microspheres were prepared by spray drying technique, with bovine serum albumin as the natural biodegradable wall materials. The obtained microspheres, using aqueous system, were organic solvent-free. The diameters of the spherical microspheres were in the range of 1~5 μm. The drug entrapment of microspheres, formulated with different ciprofloxacin/albumin ratios as 1:1, 1:2 and 1:4, were 46.93%, 32.96% and 20.56% (n = 3). And the encapsulation efficiencies for ciprofloxacin during spray drying were higher than 90%. Thermal denaturation programs at different temperatures (100~120 °C) for different time intervals (3~6~12 h) were further processed to stabilize the spray-dried microspheres. The higher the extent for thermal denaturation, the slower the rate of ciprofloxacin released from microspheres in vitro. So the release rate of ciprofloxacin from microspheres can be controlled by modifing the conditions of thermal denaturation.

Key words: Spray drying, Microspheres, Ciprofloxacin, Thermal denaturation, Drug release in vitro

Supporting: *Corresponding author. Now carry on postdoctoral research at Department of Pharmacy, Shanghai Hospital, Second Military Medical University, Shanghai 200433.