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The objective of the present research is to develop a new particulate preparation process for dry powder inhalation by which peptide-loaded poly(DL-lactic-co-glycolic acid) nanospheres are granulated with sugar alcohol (mannitol, around 4 μm in diameter). A spray-drying fluidized bed granulator was used to form soft matrix composite granules. A nanosphere suspension can be readily obtained by dispersing the composite granules in distilled water. The composite granules showed inhalation performance superior to that of freeze-dried nanosphere powder. More than 50% of composite granules were delivered to the bronchioles and alveoli of a rat. The composite granules of insulin-loaded nanosphere have a strong and prolonged pharmacological effect compared to the inhalation of insulin solution. [ABSTRACT FROM AUTHOR]

Recently, owing to their pharmaceutical and clinical utility, mini-tablets have been well studied by researchers. Mini-tablets are usually manufactured by compression molding using a multiple-tip tool in a rotary tableting machine. Owing to their special structure, ensuring uniformity is a very important challenge in the manufacturability of mini-tablets using the multiple-tip tool. In this study, we aimed to evaluate the weight variation in mini-tablets produced by a multiple-tip tool, which is considered to be the root cause affecting the uniformity, and to investigate the physical properties of drug granules and tableting conditions in a rotary tableting machine that could reduce this weight variation. In addition, the relationship between these factors and response was visualized using response surface analysis. It was shown that the weight variation in mini-tablets produced by a multiple-tip tool was reduced when using a forced feeder compared with an open feeder. Furthermore, in the case of an open feeder, the optimal range of the average particle size diameter of drug granules and the rotational speed of the rotating disc in the rotary tableting machine were determined from response surface analysis. It was suggested that it is possible to reduce the weight variation in the mini-tablets by selecting drug granules with an average particle size diameter of 100-150 µm and using tableting conditions with a rotational speed of 40-60 rpm. This study elucidated the factors that affect uniformity and determined their optimal range for the manufacture of mini-tablets.