圧力スイング造粒法による粉末吸入剤用2成分複合顆粒の調製と肺内in vitro吸入特性の評価

抄録

A pressure swing granulation method was used to produce two-drug composite granules for dry powder inhalation using sodium salicylate (SS) and calcium gluconate (GLCa) as a model drug powder. In vitro aerosol performance of the granules was evaluated using a cascade impactor. In addition to the one-drug system that we studied previously, spherical two-drug composite granules were prepared successfully and exhibited high content uniformity. In the aerosol performance study, the amount of SS and GLCa remaining in a capsule was greatly decreased by granulation compared to powdered form, with the deposition percent to respirable fraction (RF) of the two drugs increased. The deposition percent to RF of the single component granules of SS and GLCa was about 15% and 20%, respectively. Conversely, the deposition percent to RF of the two-drug composite granules changed depending on the SS/GLCa ratio, reaching approximately 45% at an SS/GLCa ratio of 3/7. These results suggest that effective dry powder inhalation can be prepared by pressure swing granulation without needing additives such as binders or carriers.