Ibuprofen-Loaded Calcium Stearate Matrix-Pellets: Impact of the Drying Temperature on the Final Pellet Characteristics

摘要

Although drying is one of the standard unit operations in the manufacturing of pharmaceuticals, its potential to affect the final product characteristics (even under moderate conditions) is often underrated. Pellets that are produced via the wet extrusion/speronization technique contain a certain amount of liquid after spheronization and need to be dried in a final step. The impact of drying may be two-fold: First, drying causes variations in the pellet micro-structure as it controls the extent and mechanism of matrix shrinkage [1,2]. Second, drying modifies the physicochemical properties of the active pharmaceutical ingredient (API) due to migration and re-crystallization phenomena [3]. APIs that are freely dissolved in the granulation liquid are prone to intra-particular migration upon drying as a function of the drying rate. This may yield non-homogeneous final API distribution profiles. Once a supersaturated solution is created during drying due to liquid evaporation, the API recrystallizes, which may be associated with solid state modifications [3].