Formulation Design for Orally Disintegrating Tablets Containing Enteric-Coated Particles

摘要

The purpose of this study was to investigate the applicability of our newly developed technology (RACTAB? technology) for preparing orally disintegrating tablets (ODTs) containing enteric-coated particles. Tamsulosin hydrochloride (TAM) was used as a model drug contained in the enteric-coated particles. Enteric-coated particles containing TAM (ECP-T) were prepared by spray coating a mixture of TAM with controlled-release materials. ECP-T was then mixed with rapidly disintegrating granules (RDGs), which were prepared using the suspension spray-coating method, and was tableted to form ODTs (ODT_RAC). ODT_RAC was evaluated for its hardness, thickness, internal structure (X-ray-CT scanning), functional properties (controlled-release profile), and in vivo disintegration time. Since RDGs with micronized ethylcellulose (MEC) increased tablet hardness by increasing the contact frequency between granules, ODT_RAC containing ECP-T exhibited high hardness (>50?N) and low friability (RAC remained intact and no damage was observed on the surface. ECP-T recovered from ODT_RAC showed the same dissolution profile of TAM in Japanese Pharmacopoeia (JP) 1st and JP 2nd media as that of intact ECP-T, which indicated that the tableting process did not affect the acid-resistibility of the particle. In addition, ODT_RAC rapidly disintegrated in vivo (< 30?s), even at a high compression force (at 9 kN). These findings clearly suggest that RACTAB? technology is a useful approach to prepare ODTs containing enteric-coated particles.