Formulation in a drop - Templated granulation and compaction analysis

Abstract

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.