Severino Patrícia, de Oliveira George G G, Ferraz Humberto G, Souto Eliana B, Santana Maria H A
Department of Biotechnological Processes, School of Engineering Chemical, University of Campinas, Campinas 13083-970, Brazil.
Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo 05508-900, Brazil.
J Pharm Anal. 2012 Jun;2(3):188-192. doi: 10.1016/j.jpha.2012.02.005. Epub 2012 Feb 22.
The purpose of this work was to introduce a new concept of coated pellets containing chitosan microspheres loaded with didadosine for oral administration, aiming at reducing the frequency of administration and improving the bioavailability by a suitable release profile. Chitosan microspheres were produced under fluidized bed, followed by extrusion and spheronization to obtain pellets with a mean diameter of about 1 mm. The pellets were then coated with Kollidon VA64 and Kollicoat MAE100P in water dispersion to depict a sustained release profile. Conventional hard gelatine capsules were loaded with these pellets and tested in vitro for their release profile of didadosine. Dissolution testing confirmed that chitosan microsphere pellets provides appropriate sustained release up to 2 h behavior for didanosine.
这项工作的目的是引入一种含有载有去羟肌苷的壳聚糖微球的包衣微丸用于口服给药的新概念，旨在通过合适的释放曲线降低给药频率并提高生物利用度。壳聚糖微球在流化床中制备，然后通过挤出和滚圆获得平均直径约为1毫米的微丸。然后将微丸用聚维酮VA64和聚丙烯酸树脂MAE100P水分散体包衣以描绘缓释曲线。将这些微丸装入传统硬明胶胶囊中，并在体外测试其去羟肌苷的释放曲线。溶出度测试证实壳聚糖微球微丸为去羟肌苷提供了长达2小时的适当缓释行为。
