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目的:制备氧化苦参碱聚乳酸-羟基乙酸共聚物(PLGA)微球,并考察其体外释药性能。方法:以二氯甲烷和丙酮的混合溶剂为有机相,采用W/O/W乳化溶剂挥发法制备氧化苦参碱PLGA微球,采用正交实验优化处方,并对其形态、载药量、包封率和体外释药性质进行了研究。结果:最佳工艺制备的氧化苦参碱PLGA微球形态圆整,表面光滑,粒径分布均匀,平均粒径为(98.3±3.4)μm,平均包封率为(70.14±3.47)%,平均载药量为(21.59±1.07)%,工艺稳定,重现性良好。微球240 h体外累积释药率为84.63%,体外释药符合Higuchi释药模型:Q=4.7999t1/2+9.6042,r2=0.9713。结论:乳化溶剂挥发法可成功制备氧化苦参碱PLGA微球,体外释药研究表明,该微球具有良好的缓释性能。
Objective: To prepare oxymatrine poly (lactic-co-glycolic acid) (PLGA) microspheres and study its in vitro drug release properties. METHODS: Oxymatrine PLGA microspheres were prepared by a mixed solvent of dichloromethane and acetone as the organic phase by W / O / W emulsification solvent. The orthogonal test was used to optimize the formulation. The morphology, drug loading, Encapsulation efficiency and in vitro release properties were studied. Results: The best morphology of PLGA microspheres prepared was spherical, smooth and uniform in size. The average particle size was (98.3 ± 3.4) μm and the average entrapment efficiency was (70.14 ± 3.47)%. The average Drug loading was (21.59 ± 1.07)%, the process was stable and reproducible. In vitro cumulative release rate of microspheres 240 h was 84.63%. In vitro release was consistent with Higuchi release model: Q = 4.7999t1 / 2 + 9.6042, r2 = 0.9713. Conclusion: The emulsified solvent evaporation method can successfully prepare oxymatrine PLGA microspheres. The in vitro release studies show that the microspheres have good sustained-release properties.