Abstract

Finding the optimal form for drug development can involve a number of different screening activities, including a search for polymorphs, salts, cocrystals, and/or amorphous solid dispersions. High‐risk compounds will require special formulations that include amorphous solid dispersions. An amorphous dispersion screen is performed to find a suitable amorphous dispersion that exhibits acceptable properties. The screening performed in early development may focus on parameters such as solubility, supersaturation, short‐term physical and chemical stability, and animal bioavailability to get into early‐phase clinical trials quickly and establish proof of concept. Before starting an amorphous dispersion screen project, information on the active pharmaceutical ingredient (API) is needed. This may include chemical structure, solid form, physical stability, chemical stability, log P, hydrogen bond donors/acceptors, calculated solubility parameters, and known solubilities of the solid in various solvents/biorelevant media.

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