Application of submicron-sized binder particles in dry granulation using a roller compactor and its evaluation

Abstract

The method to improve the properties of dry granules was investigated by introducing pre-coating process with an active pharmaceutical ingredient (API) and a submicron-sized binder prior to conventional roller compaction. Hydroxypropylcellulose (HPC) and acetaminophen (APAP) were used as models of a binder and a low-compactible API, respectively. The submicron-sized HPC (HPC-subMP) was obtained by a lab-scale spray dryer. The APAP particles were pre-coated with 5–10% of the HPC-subMP by a high shear mixer, formed into granules using a lab-scale roller compactor, mixed with other excipients and then compressed to make them tablets containing 50% APAP. The tablets prepared with the HPC-subMP showed a high tensile strength without significant retardation of the disintegration time in comparison to those with a raw HPC particle, indicating that the use of API particles pre-coated with submicron-sized binder particles in roller compaction was effective to prepare granules suitable for tableting without any fundamental changes of materials and manufacturing processes.