Unique crystalline structures
We have been pioneers in the cocrystal field since 2006. Contact us to know their potential!
The big advantage of cocrystals compared to salts is that cocrystallisation is also applicable to non-ionisable molecules where salt formation is not possible. Compared to amorphous solid forms, cocrystals tend to be more stable and have a more predictable behaviour. Cocrystals are also less prone to polymorphic transformations due to the higher complexity of their crystal structure when compared to single component systems, thus avoiding undesirable downstream processing surprises.
As a result of the increasing relevance of these solid forms, both the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have issued guideline documents related to their regulatory classification.
We have been a pioneer in the cocrystal field, working in the area since 2006 and gaining significant expertise. Cocrystals offer great potential:
- Improvement of solid state properties: several important characteristics of pharmaceutical substances like solubility, bioavailability, stability, hygroscopicity, morphology, filtration and flowability can be modified by means of cocrystal formation. In the case of APIs, it is noteworthy that the number of pharmaceutically-acceptable coformers is larger than the number of counterions for salt formation.
- Chiral resolution: selective diastereomeric cocrystallisation can be achieved using an
- Separation and purification: cocrystals can be a good purification option, especially with non-ionisable products, consequently avoiding expensive chromatographic techniques.
- Crystallisation of non-solid products: liquids, pastes and oily products can become a solid form by means of cocrystallisation, leading to more robust and efficient manufacturing processes.
Over the last years, the number of pharmaceutical cocrystals has been increasing dramatically. Their novelty, utility and not obvious preparation make cocrystals an interesting approach from the point of view of intellectual property. In the case of commercial APIs, a patent of a cocrystal with better drug properties than previously known forms could be of high commercial value.
Cocrystals do not involve structural modification of the parent molecules, therefore, in the case of designing cocrystals of marketed drugs, their development programs (including clinical trials) will be significantly shorter and less risky than those of New Chemical Entities (NCEs).