<br/>Amorphous pharmaceuticals have demonstrated benefits over their crystalline counterparts, including increased solubility/dissolution rate. Hydrophobic new molecular entities in development often require delivery as an amorphous phase as the only path to clinically feasible oral bioavailability. However, the bioperformance of amorphous pharmaceutical materials manufactured by traditional routes can be complicated by challenges including poor physical stability during processing, phase separation/heterogeneities of components in the amorphous administration vehicle, and a lack of robustness at increasing scale. To combat such difficulties, precipitation has emerged as a new method to generate amorphous solid dispersions as an alternative to traditional approaches such as spray drying or hot melt extrusion. In this talk, the use of precipitation—as well as particle engineering approaches uniquely enabled by a precipitative route—will be described for a number of amorphous Merck compounds. These examples will highlight the ability of novel manufacturing technologies to alleviate challenges in the development pipeline. Additionally, the engineering of particle architecture at the microscale via precipitation will be discussed to demonstrate how control over material and bulk powder properties of amorphous materials can mitigate challenges in pharmaceutical development.

Precipitating engineered amorphous solid dispersions to solve challenges in the development of amorphous pharmaceuticals

ACS Fall 2021

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