Application of a three-fluid nozzle for the preparation of amorphous solid dispersions

Abstract

In this work, the manufacture of amorphous solid dispersions of poorly water-soluble carbamazepine using a laboratory spray drying setup with a three-fluid nozzle and two separate liquid feed solutions of (a) the active and (b) the polymeric excipient (copovidone or basic butylated methacrylate copolymer) was investigated and compared to a traditional two-fluid nozzle setup. Results show that particles with the desired drug content were manufactured using the three-fluid nozzle setup. Amorphous solid dispersion could be obtained up to a drug load of 50% (w/w) processing solutions with miscible solvents and copovidone as polymer. Higher active concentrations, the use of immiscible solvents or switching of the capillaries led to a substantial crystallization of carbamazepine as seen in XRD and DSC analysis. The polymorphic form IV of carbamazepine was formed in the presence of copovidone at high solid concentrations of the liquid feed.