硝苯地平生物黏附微球的制备及释药机制研究  

Study on Preparation and Release Mechanism of Nifedipine Bioadhesive Microspheres

作　　者：周晓东[1] 于立军[1] 

机构地区：[1]南京军区南京总医院汤山分院药械科,南京211131

出　　处：《中国药房》2012年第17期1599-1601,共3页China Pharmacy

摘　　要：目的:制备硝苯地平生物黏附微球并考察其体外释药情况。方法:在单因素考察的基础上应用正交设计筛选硝苯地平生物黏附微球的最佳处方,因素为加热温度、聚乙烯醇(PVA)用量、司盘浓度和戊二醛用量,评价指标为累积释药率;考察优化处方所制微球的质量指标如体外黏附力和累积释药率等,研究其释药机制。结果:优化处方工艺为:加热温度60℃、PVA用量0.6 g、司盘浓度5%、戊二醛用量0.6 mL;优化处方所制微球体外黏附力较高,平均载药量约为15%,包封率约为85%,平均粒径约为20μm;微球可持续24 h释药,释药符合Higuchi方程,释药机制符合非Fick扩散机制,即以溶蚀和扩散2种模式释放。结论:硝苯地平生物黏附微球制备工艺简单,具有较好的体外黏附性能和缓释效果。OBJECTIVE： To prepare Nifedipine bioadhesive microspheres and drug release of it in vitro.METHODS： The orthogonal design was used to optimize the formulation of Nifedipine bioadhesive microspheres on the base of the single factor experiment with heating temperature,amount of PVA,span concentration and amount of glutaraldehyde as factors using accumulative drug release rate as index.The in vitro adhesion,accumulative drug release and other quality index were investigated to study drug release mechanism.RESULTS： The optimized formulation was as follows： heating temperature 60 ℃,PVA 0.6 g,span concentration 5% and glutaraldehyde 0.6 mL.Prepared microspheres had great adhesive ability.Average drug-loading amount was 15%,encapsulation coefficency 85% and mean particle size 20 μm.Prepared microspheres could release continuously for 24 h,which was in line with Higuchi equation.Drug release mechanism was up to Non-Fick diffusion mechanism,i.e.corrosion model and diffusion model.CONCLUSION： The preparation process of the Nifedipine bioadhesive microspheres is simple,and the microspheres have good adhesion properties in vitro and sustained-release effect.

关 键 词：硝苯地平 生物黏附微球 制备 黏附力 处方优化 正交试验 缓释性 释药机制 

分 类 号：R943[医药卫生—药剂学] R972[医药卫生—药学]