Formulation in a drop - Templated granulation and compaction analysis

Binder-powder interactions were investigated using single drop penetration on pharmaceutically relevant static powder beds. Experimental effects included polymer binder type, binder concentration, drug load, and pre-wetting of the powder bed. These screening effects are relevant to formulations requiring binder granulation, especially challenging formulations having high levels of micronized active ingredients. Interactions were explored using dynamic droplet imaging to measure drop penetration, contact angle, and drop diameter. The structure of the templated granules was analyzed via uniaxial compaction, focusing on the intermediate range of the compaction curve (granule deformation and closure of interstitial porosity in the compact). The results provide guidance in pharmaceutical formulation including the dynamics of granule formation and resulting compaction behavior. The approach is especially useful for early-stage development when only small quantities of drug substance are available. [Display omitted] •Drop penetration analysis enables small scale pharmaceutical formulation screening.•Drug load, binder polymer, viscosity and pre-wetting all affect penetration time.•Video analysis aided understanding of drop spreading and penetration mechanisms.•Isolated drop penetration granules were analyzed using compaction curve analysis.•Drug load had competing springback effects versus pre-wetting and penetration time.