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Compaction, compression and drug release characteristics of xanthan gum pellets of different compositions.
Authors:Helton Santos  Francisco Veiga  Ma Eugénia Pina  Jo?o José Sousa
Affiliation:Faculdade de Farmácia, Centro de Estudos Farmacêuticos, Universidade de Coimbra, Rua do Norte, 3000-295, Coimbra, Portugal. helton@ci.uc.pt
Abstract: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.
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