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目的制备川芎嗪PLGA微球并考察其物理化学性质及体外释药性。方法采用O/W型乳化-溶剂挥发法制备川芎嗪PLGA微球,正交试验设计优化处方组成和制备工艺,对微球的外观形态、粒径及粒度分布、包封率和载药量等理化性质进行了检测。结果以优化处方制备的川芎嗪PLGA微球为圆球形,粒度分布较均匀,平均粒径为(10±2.2)μm,包封率为(81.36±1.15)%,载药量为(8.2±0.43)%,药物体外释放可延长至768h,释药特性符合Weibull方程,经差示扫描量热法(DSC)分析证明,形成了新的物相,表明载药微球确已形成。结论采用O/W型乳化-溶剂挥发法制备的川芎嗪PLGA微球包封率和载药量高,粒径均匀,具有明显的缓释作用。
Objective To prepare tetramethylpyrazine (PLGA) microspheres and study its physicochemical properties and in vitro release. Methods Ligustrazine PLGA microspheres were prepared by O / W emulsification-solvent evaporation method. The formulation and preparation process of Ligustrazine PLGA microspheres were optimized by orthogonal design. The morphology, particle size, particle size distribution, entrapment efficiency and drug loading of microspheres Physical and chemical properties were tested. Results The Ligustrazine PLGA microspheres prepared by optimized formulation were spherical with a uniform particle size distribution. The average particle size was (10 ± 2.2) μm, the entrapment efficiency was (81.36 ± 1.15)% and the drug loading was (8.2 ± 0.43 )%, The in vitro release of the drug can be extended to 768h, the release characteristics in line with the Weibull equation, differential scanning calorimetry (DSC) analysis showed that the formation of a new phase, indicating that the drug-loaded microspheres have indeed been formed. Conclusion The encapsulation efficiency and drug loading of ligustrazine-loaded PLGA microspheres prepared by O / W emulsification-solvent evaporation method are high, with uniform particle size and sustained release.