摘要
目的:制备长春西汀聚乳酸-聚乙醇酸(PLGA)缓释微球,并研究其药剂学性质。方法:采用改良O/W乳化-溶剂挥发法制备微球,以PLGA浓度、理论载药量、有机相与分散介质的比例和分散介质中明胶的浓度为4因素,每个因素选定3个水平,按L9(34)的正交设计方案,以载药量、包封率和粒径分布为指标,优化处方。用扫描电镜观察微球的形态,用光学显微镜观察并计算微球的粒径分布,用差示扫描量热(DSC)法研究药物在载体中的分散状态,用紫外分光光度法检测微球中长春西汀含量并计算载药量和包封率,用动态透析释药法进行微球的体外释放研究。结果:最佳处方为PLGA浓度16%,理论载药量20%,有机相与分散介质的比例1:10,分散介质中明胶的浓度1%;制备的长春西汀PLGA缓释微球的形态圆整、光滑,粒径分布均匀,平均粒径为(10.0±0.18)μm(n=500),DSC法分析药物确已被包裹于微球中,载药量为(18.46±0.26)%,包封率为(91.30±0.98)%(n=3),24h累积释药率约为18%。结论:长春西汀PLGA缓释微球制备工艺稳定,质量符合药剂学要求,缓释性好。
OBJECTIVE： To prepare Polylactic-glycolic acid sustained-release microspheres loaded with vinpocetine, and to study pharmaceutical property of it. METHODS： Modified O/W emulsified solvent evaporation method was used to prepare the mi- crospheres. Preparation technology was optimized by L9（34） orthogonal design with 3 levels each for 4 factors. PLGA concentra- tion, theoretical drug-loading amount, the ratio of organic phase to disperse medium and gelatin concentration of disperse medium as factors using drug loading amount, entrapment rate and particle size distribution as index. The surface morphology of micro- spheres was observed under scanning electron microscope, and the distribution of particle size was observed and calculated by opti- cal microscope. The dispersion of vinpocetine was studied using DSC, and the content of vinpocetine in microspheres was detected by UV spectrophotometry. Dialysis method was used to examine the in vitro drug release. RESULTS： The optimal formulation was as follows： PLGA concentration 16%, theoretical drug loading 20%, the volume ratio of organic phase to disperse phase 1 ： 10 and gelatin concentration of disperse medium 1%. PLGA sustained-release microspheres loaded with vinpocetine were round, complete and smooth, and particle size was well-distributed with average particle size of （10.0 ＋ 0.18） pm （n= 500）. DSC analysis showed drug were coated in microspheres. Drug-loading amount was （18.46 ＋ 0.26）% and the entrapment rate was （91.30 ＋ 0.98）% （n= 3）. Accumulative drug release rate was 18% in 24 h. CONCLUSION： The preparation technology of PLGA sustained-release micro- spheres loaded with vinpocetine is stable; the microsphere exhibits good sustained-release property, and it is up to the requirements of pharmacy.
出处
《中国药房》
CAS
CSCD
2012年第13期1203-1206,共4页
China Pharmacy
关键词
长春西汀
聚乳酸-聚乙醇酸
微球
制备
处方优化
体外释放
Vinpocetine
Polylactic-glycolic acid
Microspheres
Preparation
Formulation optimization
Drug release in vitro
