A mesoporous silica based platform to enable tablet formulations of low dose drugs by direct compression

Abstract Achieving adequate content uniformity (CU) is a significant challenge in the development and manufacturing of low dose oral tablets. Using four model active pharmaceutical ingredients (APIs), we show that loading APIs into a grade of mesoporous silica, Aeroperl®, is effective for achieving excellent CU. All APIs in the Aeroperl® composites were amorphous. After six months under accelerated stability conditions, the drug-Aeoperl composites exhibited good physical stability for all four APIs. The performance of Aeroperl®-based formulations was robust since their good CU and manufacturability were insensitive to model APIs. In addition, the dissolution rate of composite-based formulations was higher than corresponding physical mixtures. Overall, the Aeroperl®-based platform formulation is a promising approach for successfully developing low dose oral tablet products.