Key Formulation Variables in Tableting of Coated Pellets

Multiple unit controlled release dosage forms offer various advantages over their single unit counterparts. Most of these advantages are associated with the uniform distribution of multiparticulates throughout the gastrointestinal tract. Though coated pellets can be filled into hard gelatin capsules, tablet formulation is the preferred one because of various advantages associated with it. However, compression of coated pellets is a challenging task necessitating the optimization of various formulation and process variables. The key formulation variables include composition, porosity, size, shape and density of the pellets; type and amount of polymer coating; nature, size and amount of tableting excipients. The pellet core should be strong with some degree of plasticity. It should be highly porous, small, with an irregular shape. The critical density to achieve prolonged release was reported to lie between 2.4 and 2.8 g/cm(3). Acrylic polymer films are more flexible and more suitable for the coating of pellets to be compressed into tablets. Thicker coatings offer better resistance to frictional forces. Solvent based coatings are more flexible and have a higher degree of mechanical stability than the aqueous based ones. The tableting excipients should have cushioning property. They should not be significantly different in size and density from those of the pellet cores in order to avoid segregation. Addition of 30%-60% of tableting excipients is necessary to avoid any damage to the polymer coat and to retain its functional property.