Utility of microcrystalline cellulose to prevent drug segregation in direct powder compression

Abstract

Direct powder compression is the simplest process method for tableting; however, when drug content is low, segregation tends to occur, making it more difficult to manufacture tablets with assured drug content uniformity. Using fine microcrystalline cellulose (MCCIM) which can influence drug dispersibility in pharmaceutical powders, we assessed the influence of the addition of MCCIM on drug content uniformity, and the utility of MCCIM as a segregation inhibitor. The formulated tablet had one of two types of acetaminophen of different particle sizes, lactose hydrate, cornstarch, MCCIM (0%, 10%, 20%), croscarmellose sodium, and magnesium stearate (Mg-St). Flowability index of the pharmaceutical powder was measured, and flowability evaluated. With MCCIM addition, flowability slightly decreased. Tableting using a rotary-type tableting press, and physical properties of tablets were evaluated. In the prepared tablets, hardness increased and disintegration time decreased with increasing amounts of added MCCIM. Adding MCCIM also decreased drug content variation, and this effect was remarkable for the drug with a large particle size. However, even when commonly used MCC was added, a decrease in drug content variation did not occur. Therefore, MCCIM in a tablet formulation may improve drug content uniformity and would be useful as an agent to prevent segregation.