Selection and development of an amorphous formulation is often viewed as time, cost, and material intensive. Screening and preparation of amorphous formulations often must wait until tens or hundreds of grams of material are synthesized. A number of small-scale experimental methods based on solvent evaporation have been developed for creating a wide array of solid dispersions using only milligrams of material. Such experiments can aid in polymer and excipient selection, drug:polymer ratio, and whether or not the desired oral exposures can be achieved with an amorphous formulation.  Critical factors such as drug:polymer miscibility and apparent solubility gains can be evaluated to help select the optimal formulation to move into in vivo studies. Case studies using model drugs indomethacin, itraconazole, and a development candidate illustrate the utility of the method.  Earlier screening, selection, and characterization can significantly help to reduce the risk, time, and cost of developing an amorphous formulation.

Material sparing methods for amorphous solid dispersion screening

244th National Meeting (2012)

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