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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 Vinpocetine Polyglycolic Acid (PLGA) sustained-release microspheres and study its pharmacological properties. Methods: The microspheres were prepared by a modified O / W emulsification - solvent evaporation method. The PLGA concentration, the theoretical drug loading, the ratio of organic phase to the dispersion medium and the gelatin concentration in the dispersion medium were 4 factors and 3 Level, according to L9 (34) orthogonal design, drug loading, encapsulation efficiency and particle size distribution as an indicator to optimize the prescription. The morphology of the microspheres was observed by scanning electron microscopy. The particle size distribution of the microspheres was observed with an optical microscope. The dispersion of the drug in the carrier was studied by differential scanning calorimetry (DSC) Vinpocetine content and calculation of drug loading and encapsulation efficiency, dynamic dialysis release microspheres in vitro release studies. Results: The best prescription was PLGA concentration 16%, theoretical loading 20%, ratio of organic phase to dispersion medium 1:10 and gelatin concentration 1% in dispersion medium. The morphology of PLGA sustained-release microspheres The average particle size was (10.0 ± 0.18) μm (n = 500). The DSC analysis showed that the drug was indeed encapsulated in the microspheres and the drug loading was (18.46 ± 0.26)%, The encapsulation efficiency was (91.30 ± 0.98)% (n = 3), and the cumulative drug release rate was about 18% after 24h. CONCLUSION: Vinpocetine PLGA sustained-release microspheres have stable preparation process, good quality and good pharmacokinetics.