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目的:制备布洛芬/星形聚乳酸载药微球,研究制备工艺参数对载药微球的药物包封率的影响,并对其体外释放特性进行表征。方法:以星形聚L-乳酸(s-PLLA)为聚合物基材,采用溶剂挥发法制备布洛芬/星形聚乳酸载药微球(s-PLLA/IBU),采用正交试验设计的方法安排试验,研究s-PLLA/IBU的体外缓释特性,并用傅里叶变换红外光谱计(FTIR)和扫描电镜(SEM)对微球进行表征。结果:通过极差分析与方差分析建立s-PLLA/IBU的药物包封率与制备工艺参数之间的关系,并在此基础上遴选出优化工艺。IBU与s-PLLA结合良好,s-PLLA/IBU微球缓释7d后,s-PLLA出现部分降解。采用优化工艺所制备的s-PLLA/IBU微球的释放特性符合一级方程。结论:采用溶剂挥发法制备的s-PLLA/IBU微球的药物包封率高、体外释药平稳。
OBJECTIVE: To prepare ibuprofen / star polylactic acid drug-loaded microspheres and study the influence of preparation parameters on drug entrapment efficiency of drug-loaded microspheres. The in vitro release characteristics were also characterized. Methods: s-PLLA / IBU was prepared by solvent evaporation method using s-PLLA as the polymer substrate. The orthogonal experimental design The experiments were conducted to study the in vitro sustained release properties of s-PLLA / IBU. The microspheres were characterized by Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). Results: The relationship between the entrapment efficiency of s-PLLA / IBU and the process parameters was established by range analysis and ANOVA. Based on this, the optimization process was selected. IBU and s-PLLA binding well, s-PLLA / IBU microspheres after 7d sustained release, s-PLLA partial degradation. The release characteristics of s-PLLA / IBU microspheres prepared by the optimization process accord with the first-order equation. Conclusion: The drug entrapment efficiency of s-PLLA / IBU microspheres prepared by solvent evaporation method is high and the drug release in vitro is stable.