Novel coprocessed excipients composed of lactose, HPMC, and PVPP for tableting and its application.

New coprocessed excipients composed of α-lactose monohydrate (a filler), HPMC E3 (a binder), and PVPP (a superdisintegrant) were developed by spray drying in this study to improve the tableting properties of lactose. Factors affecting the properties of the coprocessed excipients were investigated by a 3 × 3 × 2 factorial design. These factors include lactose grade (90 M, 200 M, and 450 M), percentage of HPMC (3.5%, 7.0%, and 10.5%), and percentage of PVPP (0% and 3.5%). The results show that the compactability of the excipients could be significantly improved by increasing either the percentage of HPMC or the primary particle size of lactose. The addition of 3.5% PVPP had little effect on the compactability, but significantly improved the disintegration ability. The developed coprocessed excipients have much lower yield pressures and much higher working efficiency during tableting compared to the main raw material (α-lactose monohydrate). These improvements are mainly attributed to the addition of HPMC and the proximately 30% amorphous lactose formed during process. Both HPMC and amorphous lactose were homogeneously distributed on the surface of the secondary particles, maximizing their effect. Furthermore, the low hygroscopicity and high glass transition temperature of HPMC led to a high yield. The drug loading capacity of the newly coprocessed excipients is also excellent. In summary, the tri-component coprocessed excipients investigated are promising and worthy of further development.