肺靶向地塞米松微球的制备及体外释药  

Preparation and in vitro characterization of microspheres containing dexamethasone sodium phosphate

作　　者：陶兆武[1] 徐启勇[1] 叶燕青[1] 彭平[1] 汪自然[1] 

机构地区：[1]武汉大学中南医院呼吸内科,湖北武汉430071

出　　处：《中国医院药学杂志》2006年第5期515-517,共3页Chinese Journal of Hospital Pharmacy

基　　金：湖北省科技攻关计划(编号:2004AA301C24)

摘　　要：目的:研究水溶性药物地塞米松磷酸钠肺靶向微球制备工艺的优化。方法:以油/水型乳化-溶剂挥发法制备微球,考察微球的性质及肺靶向性。维持其他条件不变,内相中加入甲醇和改变外相中氯化钠的加入量后,考察微球的载药量变化。结果:所制的微球的平均粒径为(8.37±4.0)μm。突释性好,最初0.5h释药量达48.28%。各器官石蜡切片中,肺组织中有较多微球嵌顿。随着内相中加入甲醇和外相中加入氯化钠,微球载药量提高。结论:地塞米松微球有良好的肺靶向性。采用油/水型乳化-溶剂挥发法制备水溶性地塞米松微球时,内相中加入甲醇和外相中加入氯化钠有助于提高微球的载药量。OBjECTIVE To optimize the preparation technique of microspheres containing dexamethasone sodium phosphate. METHODS Microspheres were prepared by O/W emulsification-evaporation method. Characterizations of microspheres were investigation. Effects of adding methanol in inner phase and sodium chloride in external phase on drug loading were investigation. RF2SULTS The average particle size was （8. 3 ± 4. 1）μm. In the in .vitro release test, the burst stage was notable. Drug released near 48.28% in the initial 11. 5 h. Many microspheres in the lung could be observed in the paraffin section. Methanol in inner phase and sodium chloride in external phase could increase the drug loading. CONCLUSION Lung could be targeted by these microspheres. The drug loading can be enhanced-by using O/W emulsification-evaporation medhad, and adding methanol in inner phase and sodium chloride in external phase.

关 键 词：地塞米松磷酸钠 聚乳酸-聚乙醇酸共聚物 微球 肺靶向 

分 类 号：R965.1[医药卫生—药理学]