Improvement of Dissolution Property of Poorly Water-Soluble Drug by the Combination of Wet Grinding Method and Fluidized-bed Coating Method

We aimed to establish a method to prepare and functionalize nano-particles, e.g., a very rapid dissolution rate, even after changing to an internal dosage form, such as a tablet. Particles of a poorly water-soluble drug, flurbiprofen (FP), suspended in 5% HPC-SL solution, were passed through a high pressure homogenizer at 200MPa five times, and a nano-suspension (around 100nm mean diameter) was prepared. It was then sprayed onto the surface of lactose, used as core particles, with a fluidized-bed coater and a centrifugal rotary fluidized-bed coater. It was revealed that the dissolution property of FP from a tablet prepared with particles coated by a fluidized-bed coater with top-spray was as rapid as the nano-suspension. Moreover, when using a centrifugal rotary fluidized-bed coater with a tangential spray, addition of 2% light anhydrous silicic acid or 2% D-mannitol to the nano-suspension improved the dissolution rate. Therefore, a coating method which could maintain the performance of nano-particles was established in this study.