CRYSFORMA: Salt and Co-crystal screenings to get new patents and to optimize your drug substance

Do you need to optimize the chemical properties of a drug? Looking for a new patent with different substance properties?

Salt and co-crystal screening studies are crucial in the development of drugs for the pharmaceutical industry. Such studies bring to companies the discovery of derivates of their drug substances with enhanced properties, which can lead to make new patent applications, to optimize the production and commercialization conditions, and to improve the physicochemical properties of the drug substance.

The pharmaceutical solid-state unit of the Institute of Chemical Research of Catalonia (ICIQ-CERCA), Crysforma, is specialized in developing systematic both salt and co-crystal screening studies to discover and select the optimal solid-state properties of an API (Active Pharmaceutical Ingredient).

The screenings help to discover and select the optimal solid-state properties of an API.

• Salt screenings: Preparation of a salt is the classical strategy employed to optimize the solid-state properties of an active pharmaceutical ingredient which contain an ionizable functional group. Salt derivatives can improve crystallinity, solubility and stability of a pharmaceutical compound, and are often chosen instead of the free form. In this sense, Crysforma owns a salt screening methodology based in the use of selected crystallization procedures in an optimized group of crystallization solvents. The methodology allows performing a large number of crystallization experiments from 10 g of starting API under controlled conditions.

• Co-crystal screenings: Co-crystals serve as a substitute for salts in cases where salts lack the necessary solid-state properties or cannot be formed due to the absence of ionizable sites in the API. Crysforma has developed its own co-crystal screening methodology adequate for co-crystal formers with very different properties. The methodology combines several crystallization procedures, specifically useful to generate co-crystals, as solid-state grinding, solvent evaporation, reaction crystallization and crystallization from the melt.

When a new drug derivate (salt/co-crystal) is found, it needs to obtain the approval from the corresponding Medicine Agency before it can be commercialized according their different regulation.

Besides the modification and improvement of the physicochemical properties of an API, all new salt and co-crystal forms of an API are considered patentable in terms of intellectual property and certainly represent a commercial opportunity.