维A酸微球的制备及性能考察

Preparation and characterization of tretinoin microspheres

目的以乙基纤维素为材料制备维A酸微球,并对其粒径和载药量等性质进行考察。方法采用O/W型乳化-溶剂挥发法制备维A酸微球。考察乳化剂聚乙烯醇及载体材料乙基纤维素的浓度等处方因素对微球粒径及形态的影响,通过HPLC测定载药微球的载药量及包封率;利用透析法测定载药微球的释放度;通过正交试验优化处方。结果最优处方下制备的微球外观圆整,粒径较均匀,平均粒径为80μm,载药量质量分数为3.0%。结论该法具有耗时短、制备工艺简单、重现性好,制备的微球粒径小、粒度分布窄等特点。

Objective To prepare ethyl cellulose(EC) microspheres of tretinoin. Methods The EC microspheres were prepared by solvent diffusion –evaporation method using ethyl cellulose as polymer. Formulation and process factors such as the concentration of polyvinyl alcohol(PVA), ethyl cellulose, etc. were investigated with respect to the size and morphology of microspheres. The drug-loading,encapsulation efficiency and release rate of microspheres were tested by HPLC. Preparation parameters were optimized by orthogonal experiments and microspheres having good dispersion were obtained. Results The prepared microspheres were spherical and smooth in appearance, the particle size was uniform with average size of 80 μm. The drug loading were found to be 3.0%(w). Conclusion This preparation method of microspheres is simple and reproducible. These microspheres show narrow particle size distribution.