Faculty of Pharmacy, Institute of Pharmaceutical Technology, University Ss Cyril and Methodius, Vodnjanska 17, 1000 Skopje, Macedonia.
J Microencapsul. 2013;30(1):81-92. doi: 10.3109/02652048.2012.700957. Epub 2012 Jul 3.
The purpose of this study was to apply factorial design in order to determine the influence of the formulation factors and their interactions on several responses such as particle size, dissolution behaviour at pH 1.2 and pH 7.4 as well as production yield, during the development of budesonide loaded, chitosan coated Ca-alginate microparticles (MPs) intended for treatment of inflammatory diseases in the gastrointestinal tract. Produced drug-loaded MPs were spherical in shape, had smooth surfaces with low porosity and size range between 5 and 11 µm. Production yield for the formulations from the design varied from 19% to 50%. Optimisation was performed using central composite design setting the targets: particle size at 5.5 µm, maximised yield, suppressed dissolution at pH 1.2 and sustained release at pH 7.4. The optimised batches were identified with a combined desirability value of 0.967.
本研究旨在应用析因设计，以确定配方因素及其相互作用对多个响应的影响，如粒径、在 pH 1.2 和 pH 7.4 时的溶解行为以及生产收率，在开发用于治疗胃肠道炎症性疾病的负载布地奈德的壳聚糖包被海藻酸钙微球（MPs）过程中。所制备的载药 MPs 呈球形，表面光滑，孔隙率低，粒径在 5 至 11 μm 之间。设计的制剂的生产收率在 19%至 50%之间变化。通过使用中心复合设计进行优化，设定目标为：粒径为 5.5 μm，收率最大化，在 pH 1.2 时抑制溶解，在 pH 7.4 时持续释放。优化批次的综合适宜性值为 0.967。
