Improved blend and tablet properties of fine pharmaceutical powders via dry particle coating

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Abstract

The improvements in the flow and packing of fine pharmaceutical powder blends due to dry coating of micronized acetaminophen (mAPAP, ˜11 μm), a model poorly flowing drug, are quantified. Poor flow and packing density of fine excipients (˜20 μm) allowed testing the hypothesis that dry coating of cohesive API may counteract poor flow and packing of fine pharmaceutical powder blends. Further, fine excipients could improve compaction and reduce segregation tendency. It was found that flow function coefficient (FFC) and bulk density enhancements for 10%, 30%, and 60% (w/w), API loading blends with dry coated API are significantly higher than those without coated silica. At the highest API loading, for which coarser excipients were also used as reference, the flow and packing of dry coated mAPAP blends were significantly increased regardless of the excipient particle size, exceeding those of a well compacting excipient, Avicel 102. In addition, tensile strength of tablets with fine excipients was significantly higher, indicating improved compactibility. These results show for the first time that dry coating of fine, cohesive API powder leads to significantly improved flow and packing of high API loading blends consisting of fine excipients, while achieving improved tablet compactibility, suggesting suitability for direct compaction.

Graphical abstract

Dry coating of micronized APAP (˜11 μm) leads to improved flow as well as tablet tensile strength at 60% (w/w) API loading. Tensile strength with fine excipients is much higher and well within the proposed range (shaded region) for direct compression tableting.

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