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目的:为防治增殖性玻璃体视网膜病变,以聚乳酸(Poly-L-lactide,PLLA)为材料,制备苦参碱缓释亚微球。方法:采用有机相分散-溶剂扩散法制备苦参碱PLLA亚微球,应用星点设计-效应面优化法优化制备工艺,并对其体外释放特性进行评估。结果:以载药量、包封率、粒径及多分散系数为评价指标,考察内相PLLA浓度、理论载药量和外相明胶浓度对制备工艺的影响,对因素-指标分别进行多元线性回归和二次多项式拟合,结果表明采用二次多项式拟合的效果较好,用效应面法选取的最佳工艺条件为PLLA浓度12%,理论载药量13%,明胶浓度1.5%,按优化工艺制得的亚微球光滑圆整,载药量、包封率、粒径及多分散系数分别为6.526%,50.2%,679.2nm,0.005。亚微球体外释放30d累积释放率达80.66%。结论:制得的亚微球满足缓释长效的要求,所建立的模型预测性良好。
Objective: To prevent and treat proliferative vitreoretinopathy, polylactide (PLLA) was used as material to prepare matrine sustained-release sub-microspheres. Methods: Matrine PLLA submicrospheres were prepared by organic phase dispersion - solvent diffusion method. The preparation process was optimized by the method of apical design - response surface optimization. The in vitro release characteristics were evaluated. Results: The drug loading, entrapment efficiency, particle size and polydispersity index were used as evaluation indexes to investigate the effect of PLLA concentration, theoretical drug loading and gelatin concentration on the preparation process. Multiple linear regression And quadratic polynomial fitting, the results show that the use of quadratic polynomial fitting effect is better, the optimum conditions selected by the effect surface method for the PLLA concentration of 12%, 13% of the theoretical drug loading, gelatin concentration of 1.5%, according to the optimization The submicrospheres prepared by the process were smooth and rounded. The drug loading, encapsulation efficiency, particle size and polydispersity were 6.526%, 50.2%, 679.2nm and 0.005 respectively. The cumulative release rate of sub-microspheres in vitro for 30 days reached 80.66%. Conclusion: The prepared sub-microspheres meet the requirements of long-term sustained release, the model established is of good predictability.