難溶性薬物のためのドライ・ナノサスペンション技術による 自己ナノ分散型顆粒剤・錠剤の開発

抄録

The “dry nanosuspension” granules and tablet, which could be spontaneously dispersed to submicrom-sized drug particles, were developed using wet milling and sequential fluidized-bed drying technique. Poorly water-soluble drug particles were beads-milled in the aqueous solution of dispersing agents using simple and general-purpose apparatus in laboratory. The milled nanosuspension was sprayed to the carrier particles of lactose in the fluidized-bed granulator to obtain the granulated product. It was found that the polymeric agent loaded as a milling promotor could play a role of binder to support the granulation and that the nano-sized drug particles were uniformly fixed on the surface of granulated particles. The resultant granules could re-construct the original drug nanosuspension within a few minutes in water, resulting in rapid dissolution behavior. Further, it was also found that the tablet prepared by compressing the granules kept their own rapid dispersible and release properties. The present technique via wet milling and fluidized-bed granulation/drying processes would be a novel dissolution-enhanced technology for poorly water-soluble drugs.