Abstract

Tableting of sticking active pharmaceutical ingredients (APIs) may cause time-consuming and costly complications. Therefore, the aim of this study was to identify and to analyze critical factors influencing sticking of ibuprofen during direct compaction with a laboratory tableting set-up and to find the optimum settings for sticking reduction using a design of experiments (DoE) approach. Moreover, the influence of the tablet punch wear on the sticking tendency was evaluated. In addition, the applicability of the small-scale experiments to production-scale tablet manufacture was investigated. The results of the DoE revealed that “compaction force”, “punch tip coating” and their interaction had the strongest impact on ibuprofen sticking to the punch tips. Furthermore, the wear of the punches had a pronounced influence on the anti-sticking properties of the different punch tip coatings. An additional minor influencing factor turned out to be the selection of the lubricant whereas the lubricants had a significant effect on the disintegration time of the tablets. This observation was in contrast to the expectations resulting from the lubricant hydrophobicity. The findings of the laboratory-scale tableting experiments were confirmed by the experiments conducted on the production scale.

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