Novel Screening Tools for Hot-Melt Extrusion - Early Prediction of Formulation Performance

3/11/2020 10:20 - 10:55

  • Amorphous solid dispersions
  • Polymer screening
  • Screening tools
  • Hot melt extrusion
  • Formulation development
  • Differential scanning calorimetry
  • Vacuum compression molding

Hot melt extrusion (HME) is an ever more widely applied technology for the creation of amorphous solid dispersions to enhance the bioavailability of low soluble drug substances.

Frequently solvent film casting is applied in early screening. The process itself differs significantly form the later HME process. Therefore its predictability is rather limited. 

To ensure a successful formulation development an identification of suitable polymers needs to be addressed already at early stages. Different screening technologies are compared to allow a prediction of performance and stability of a hot melt extruded formulation.

Two interesting technologies are identified for early screening:

Differential scanning calorimetry (DSC)

Vacuum compression molding (VCM)

Both evaluated technologies DSC as well as VCM show a high potential to estimate the performance of the final HME formulation. The DSC method can be easily established on existing devices and is highly interesting for preliminary tests. Limitations are the restricted sample amount as well as the direct relation of release characteristics to the performance of HME formulations.

In contrast VCM technology provides the advantage of a more versatile and homogenous sample generation offering a high reliability in sample preparation. An increased sample amount allows further processing steps resulting in a realistic estimation of formulation performance.

Thomas Kipping, Head of Drug Carriers, Merck