Santos Helton, Veiga Francisco, Pina Ma Eugénia, Sousa João José
Faculdade de Farmácia, Centro de Estudos Farmacêuticos, Universidade de Coimbra, Rua do Norte, 3000-295, Coimbra, Portugal.
Eur J Pharm Sci. 2004 Feb;21(2-3):271-81. doi: 10.1016/j.ejps.2003.10.016.
Compaction and compression of xanthan gum (XG) pellets were evaluated and drug release from tablets made of pellets was characterised. Three formulations were prepared by extrusion-spheronisation and included, among other excipients, diclofenac sodium (Dic Na), at 10% (w/w); xanthan gum, at 16% (w/w); and one of three different fillers (lactose monohydrated (LAC), tribasic calcium phosphate (TCP) and beta-cyclodextrin (beta-CD)), at 16% (w/w). Five hundred milligrams of pellets (fraction 1000-1400microm) were compacted in a single punch press at maximum punch pressure of 125MPa using flat-faced punches (diameter of 1.00cm). Physical properties of pellets and tablets were analysed. Dissolution was performed according to the USP paddle method. Pellets showed close compressibility degrees (49.27% LAC; 51.32% TCP; and 50.48% beta-CD) but densified differently (3.57% LAC; 14.84% TCP; 3.26% beta-CD). Permanent deformation and densification were the relevant mechanisms of compression. Fragmentation was regarded as non-existent. The release behaviour of tablets made of pellets comprising LAC or beta-CD was anomalous having diffusional exponent (n) values of 0.706 and 0.625, respectively. Drug diffusion and erosion were competing mechanisms of drug release from those tablets.
对黄原胶(XG)微丸的压实和压缩进行了评估,并对由微丸制成的片剂的药物释放特性进行了表征。通过挤出滚圆法制备了三种制剂,除其他辅料外,还包括10%(w/w)的双氯芬酸钠(Dic Na)、16%(w/w)的黄原胶以及三种不同填充剂(一水乳糖(LAC)、磷酸三钙(TCP)和β-环糊精(β-CD))之一,填充剂含量为16%(w/w)。使用平面冲头(直径1.00cm)在单冲压片机上以最大冲压力125MPa压实500毫克微丸(粒径1000 - 1400微米)。分析了微丸和片剂的物理性质。按照美国药典桨法进行溶出度测定。微丸显示出相近的压缩程度(LAC为49.27%;TCP为51.32%;β-CD为50.48%),但致密化程度不同(LAC为3.57%;TCP为14.84%;β-CD为3.26%)。永久变形和致密化是压缩的相关机制。破碎现象被认为不存在。由包含LAC或β-CD的微丸制成的片剂的释放行为呈非正规扩散,扩散指数(n)值分别为0.706和0.625。药物扩散和溶蚀是这些片剂药物释放的竞争机制。