Amorphous solid dispersions - Increasing Solubility From API to Tablets
Amorphous solid dispersions (ASDs) have become an established platform to address bioavailability challenges due to low aqueous solubility of new drugs in the pharmaceutical pipeline. Despite the clinical and commercial success of ASDs, with 24 FDA-approved therapies, there are perceived risks that may drive the selection of “simpler” enabling platforms. These include lack of previous experience with ASDs, concerns on physical stability, and the apparent complexity involving the development of ASD formulations. Here, we will discuss and highlight the most relevant aspects of the latter.
The following discusses the main development goals (Figure 1) and presents a framework for a streamlined development of ASD formulations by spray drying (SD). The use of in-silico tools and miniaturized techniques in ASD formulation screening is exemplified as well as the objective gains in development time and material consumption. Also highlighted is the importance of a thorough understanding of the mechanisms and principles behind ASDs, as well as adequate analytical tools, a science-based methodology, and large-scale manufacturing know-how to achieve an optimal formulation. These aspects are essential to reduce issues and delays during early clinical stages that can ultimately impact time-to-market.