干扰素-α微球的制备及其体外释药性能研究  

Study on the preparation and in vitro release of interferon-α microspheres

作　　者：杨帆[1,2] 张永明[1,3] 赵耀明[4] 李丹涛[5] 宋凤兰[5] 徐安龙[1] 

机构地区：[1]中山大学生命科学学院 [2]广东药学院药科学院,广东广州510224 [3]中山大学附属第三医院,广东广州510630 [4]华南理工大学材料学院 [5]广东药学院药科学院

出　　处：《中国医院药学杂志》2005年第9期807-809,共3页Chinese Journal of Hospital Pharmacy

基　　金：广东省自然科学基金资助项目(编号:020885)

摘　　要：目的:通过正交设计试验优化干扰素-α聚乳酸-羟乙酸共聚物微球的制备工艺,并考察其体外释药性能。方法:采用复乳-溶剂挥发法制备干扰素微球,通过L9(3)4正交试验设计优选微球最佳制备工艺条件,并对制备工艺的重现性、微球的性质及体外释药性能进行了考察。结果:干扰素微球的最佳制备工艺稳定、重现性好,微球的形态圆整,粒度分布均匀,平均粒径为10.71μm,干扰素被证明包裹在微球中,载药量为8.06%,包封率为36.97%。干扰素微球在61h的累积释药量约为86%,t1/2为10.8h。结论:本研究获得了较满意的干扰素微球制备工艺,其体外释药性能符合长效制剂特征。OBJECTIVE To optimize the preparation conditions of interferon-α in Poly（lactide-co-glycolide） microspheres by orthogonal test. The release in vitro of microspheres were tested. METHODS Interferon-α microspheres were made by W/O/W-liquid drying process. The L9 （3）^4 orthogonal test design was used to optimize the preparation techniques. The reappearances of pharmaceutical technology, the characters and the release in vitro of microspheres were examined. RESULTS The pharmaceutical technology of interferon-α microspheres was stable, the microspheres were regular in their morphology. The average particle size was 10. 71μm and the distribution was narrow. Interferon-α was enveloped in microspheres. The drug loading and the incorporation efficiency were 8. 06% and 36. 97% respectively. The accumulated release percent of interferon-α microspheres was 86% after 61 h. The release half-life T1/2 was 10.8 h and Higuchi equation was Y = 9. 962 9t^1/2 ＋ 13. 095, r = 0. 930 7. CONCLUSION This paper describes the optimized preparation conditions of interferon-α in Poly（lactide-co-glycolide） microspheres. The release in vitro of interferon-α microspheres showed significant sustained release.

关 键 词：干扰素 聚乳酸-羟乙酸共聚物 微球 制备工艺 体外释药性能 

分 类 号：R944.9[医药卫生—药剂学]