The background: one of the major challenges in pharmaceutical formulation is the low solubility of APIs. A very elegant, but non-trivial way to improve or even control the solubility and therefore bioavailability of an active compound is the formation of a cocrystal.
Combined with non-volatile coformer molecules, the API forms a new crystalline single phase and thereby creates a new material that is different from simple polymorphs or physical mixtures of the API and conventional formulation ingredients. Thus cocrystals may also offer interesting opportunities to circumvent patent issues.
Nevertheless, up to now finding a suitable cocrystal usually requires expert knowledge and a vast variety of experiments. The speaker Carsten Schauerte, with over 20 years of experience in the field, presented a new method to improve the conventional screening approach by a goal-oriented way of using ternary phase diagrams prior to and in combination with the actual screening procedure. The example of carbamazepine with different conformers and solvents explained the approach.
Cocrystallisation offers many advantages, but the complexity and difficulties of cocrystal- screening should not be underestimated. An experienced partner as SOLID-CHEM could significantly save time and open the window for new opportunities.
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Please note: the link to the recorded webinar is available on request.