摘要
目的 制备适合粉末吸入肺部定位给药的环丙沙星白蛋白缓释微球 ,探讨热变性对微球体外释药的调节机制。方法 采用水溶液系统 ,运用喷雾干燥微囊化工艺一步制得粉末微球 ,分析粉末微球吸入的剂量控制 ,并考察热变性微球的体外释药情况。结果 粉末微球流动性好 ,不含任何有机溶剂 ,外观呈圆球型 ,粒径为 1～ 5 μm ,给药剂量可控。微球的体外释药符合Higuchi方程 ,热变性程度越深 ,药物释放愈缓慢 ,这与白蛋白微球二级结构的空间构像及其降解特性有关。 结论 粉末热变性对喷雾干燥白蛋白微球体外释药具有可调节性 ,所制备的环丙沙星微球适于干粉末吸入肺部定位给药 。
OBJECTIVE: To prepare the dry powder inhaled sustained release albumin microspheres for lung specific delivery of ciprofloxacin. To investigate the mechanism of the modification of thermal denaturation on drug release in vitro. METHODS: The spray drying process was used to prepare the powdered microspheres ciprofloxacin encapsulated in the microspheres, contribute to the inhaled dosage, was analyzed. The characteristics of drug release from the microspheres after heating were studied in vitro. RESULTS: The obtained microspheres, with well flowability, were organic solvent free. The diameters of the spherical microspheres were in the range of 1 ∼ 5 μm. The drug release profiles in vitro were fitted well to the Higuchi equation. The higher the extent for thermal denaturation the slower the ciprofloxacin released from the microspheres in vitro. This was caused by the change of the secondary structure and the degradation properties of the albumin matrix. CONCLUSION: The drug release from the albumin microspheres, prepared by spray drying, was modified by different thermal denaturation conditions. The prepared microspheres were suitable for being used as the dry powder inhaled lung-sited delivery system.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2002年第2期110-113,共4页
Chinese Pharmaceutical Journal
