Abstract
Spray-drying is an increasingly popular technology for the production of amorphous solid dispersions (ASDs) in the pharmaceutical industry that is used in the early evaluation and industrial production of formulations. Efficient screening of ASD in the earliest phase of drug development is therefore critical. A novel miniaturized atomization equipment for screening spray-dried solid dispersions (SDSDs) in early formulation and process development was developed. An in-depth comparison between the equipment/process parameters and performance of our novel screening device and a laboratory Büchi B290 mini spray-dryer was performed. Equipment qualification was conducted by comparing the particle/powder attributes, i.e., miscibility/solid state, residual solvent, and morphological properties of binary SDSDs of itraconazole prepared at both screening and laboratory scales. The operating mode of the miniaturized device was able to reproduce similar process conditions/parameters (e.g., outlet temperature (Tout)) and to provide particles with similar drug–polymer miscibility and morphology as laboratory-scale SDSDs. These findings confirm that the design and operation of this novel screening equipment mimic the microscale evaporation mechanism of a larger spray-dryer. The miniaturized spray-dryer was therefore able to provide a rational prediction of adequate polymer and drug loading (DL) for SDSD development while reducing active pharmaceutical ingredient (API) consumption by a factor of 120 and cycle time by a factor of 4.
Highlights
Spray-drying is a widely used process in the pharmaceutical industry to transform a solution, suspension, or emulsion into a powder [1,2]
This can be explained on the basis that the rapid solvent evaporation that occurs during the process minimizes the time window for phase separation and recrystallization and favors the formation of an amorphous system [8]
Prior to the development of the miniaturized screening device, design criteria and user requirements specifications were established to design a system that mimics the operating mode of a spray-dryer and that allows the adjustment of process and formulation variables in the range of values typically found at laboratory/pilot scale
Summary
Spray-drying is a widely used process in the pharmaceutical industry to transform a solution, suspension, or emulsion into a powder [1,2]. Droplet-air contact via a cocurrent configuration where an atomized solution and drying gas are flowing in the same direction is the most prevalent method in the pharmaceutical industry. This configuration allows for the processing of heat-sensitive compounds because exposure to high temperatures is very limited due to solvent. The use of spray-drying has been suitable for the preparation of amorphous solid dispersions (ASDs) at the industrial scale [7] This can be explained on the basis that the rapid solvent evaporation that occurs during the process minimizes the time window for phase separation and recrystallization and favors the formation of an amorphous system [8].
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