Formulation and Quality – Chemical
Microprecipitation Technology from Concept to Scale-Up --Waseem Malick , Vice-President (Retd.) ,Hoffmann-La Roche , Inc. , Nutley
Over the last two decades, the science of amorphous formulations has developed to a point that scientists feel cautiously optimistic that appropriate formulation and process technologies can lead to commercially viable products . Although hot melt extrusion and spray drying are meeting the needs of a large percentage of poorly soluble compounds , there remains a class of compounds that are not amenable to either of these process technologies either due to their high melting point or low solubility in the solvents suitable for spray drying. Microprecipitation technology was developed to meet the needs of such compounds. This unique technology yields a high energy form of the drug referred to as Microprecipitated Bulk Powder ( MBP). Drug substance and stabilizing polymer are dissolved in a common solvent such as Dimethylacetamide or N-Methylpyrrolidone and this solution is introduced in to an aqueous solvent to produce the amorphous form that is stabilized in a polymer matrix. With the judicious selection of polymer, drug concentration, solvent-antisolvent properties (ratio, solubility , temperature, shear, a commercially viable process can be developed. This presentation will focus on the development of the MBP process from initial screening to scale-up.