替硝唑聚乳酸微球的制备及其体外释药性能  

Preparation and in vitro release of poly(DL-lactide) microspheres containing tinidazole

作　　者：覃宇悦[1] 程春生[1] 樊建[1] 袁明伟[2] 李伟[3] 

机构地区：[1]昆明理工大学生物与化学工程学院,云南昆明650224 [2]四川琢新生物材料研究有限公司,四川成都610041 [3]四川大学口腔生物医学工程教育部重点实验室,四川成都610041

出　　处：《中国医院药学杂志》2007年第6期735-737,共3页Chinese Journal of Hospital Pharmacy

摘　　要：目的:采用聚乳酸[poly(DL-lactide)]制备替硝唑微球。方法:考察分散递质明胶溶液的浓度、油相中聚乳酸的浓度、投药比和搅拌速度等因素的影响,应用正交实验优选最佳制备工艺条件。结果:替硝唑聚乳酸微球的最佳制备工艺稳定、重复性好,微球表面圆整,粒径分布均匀,微球平均粒径为30.2μm,平均载药量为6.7%,平均包封率为64.5%。该微球在14d的药物累积释放率达81.2%。结论:替硝唑聚乳酸微球缓释时间长达14d,用于牙周炎的治疗是有效的。OBJECTIVE The objective of this study was to prepare poly （DL-lactide） microspheres for tinidazole. METHODS The formulation parameters evaluated in this study included concentration of modifier, PLA concentration, tinidazole/ PLA and agitate rate and orthogonal design was used to optimize the formulation. RESULTS The PLA microspheres containing tinidazole was shown to have good spherical geometry, a smooth surface and suitable size distribution under scanning electronic micrographs. The average diameter of microspheres was 30. 2 μm, drug loading was 6. 7% and incorporation efficiency was 64. 5%. The cumulative release rate was 81.2% after 14 d. CONCLUSION The PLA microspheres provided sustained release of tinidazole over a 14-day period and can be significantly decreased symptoms of periodontitis.

关 键 词：聚乳酸 替硝唑 微球 制备 体外释药 

分 类 号：R944.9[医药卫生—药剂学]