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Solid State Screening - Salt /Co-crystal Screen

Identification of the optimum salt form (or co-crystal) is an important part of drug development. A range of chemico-physical properties of the API can be altered significantly by salt/co-crystal formation including aqueous solubility, hygroscopicity and stability as well as simplifying processing steps such as purification. The objective of any salt/co-crystal screen is to identify and compare a set of salts/co-crystals prepared from a range of suitable and safe counter-ions/co-formers. The selection of the counter-ions/co-formers to be screened is based on safety aspects as described in the FDA GRAS list and on the intended application. Typically those counter-ions selected will have a pKa that is more than 2 units different to the active candidate.

Our initial approach will be to undertake a comprehensive study of the chemical and physical properties of the material to allow for efficient experimental design. Once identified suitable crystalline samples will be further characterized and the best solid forms identified based on:

Solubility/dissolution rate
Hygroscopicity
Melting point
Stability