Simulation of roller compaction with subsequent tableting and characterization of lactose and microcrystalline cellulose.

Tablets are by far the most common solid oral dosage forms, and many drugs need to be granulated before they can be tableted. Increasingly roller compaction is being used as a dry granulation technique; however it is a very time and material intensive method. Thus some mini roller compactors and simulations of the roller compaction process have been developed as a means of studying the technique at small scale. An important factor in the selection of materials for roller compaction is their ability to be recompressed into tablets after the initial roller compaction and milling steps. In this paper the roller compaction process was simulated on the basis of some models by Gereg and Cappola (2002) and Zinchuk et al. (2004). An eccentric tableting machine was used to make compacts from alpha-lactose monohydrate, anhydrous beta-lactose, spray-dried lactose and microcrystalline cellulose at different maximum relative densities (rho rel,max 0.6-0.9). These compacts were milled immediately to granules with a rotary granulator. The properties of the granules were analyzed and compared to the properties of the original powders. These granules and powders were then tableted at different maximum relative densities (rho rel,max 0.75-0.95) and their properties including elastic recovery, crushing force and 3D-model were analyzed. The properties of the tablets made from the granules were compared to the properties of the tablets made from the powders to determine which excipients are most suitable for the roller compaction process. The study showed that anhydrous beta-lactose is the preferred form of lactose for use in roller compaction since compaction did not affect tablet crushing force to a large extent. With the simulation of roller compaction process one is able to find qualified materials for use in roller compaction without the necessity of a great deal of material and time.