Generation of new market opportunities for an established API

Background

A customer desired to investigate the possibilities to improve the bioavailability for an already marketed and established oral product.

Approach

Adroit Science could foresee opportunities to select a more optimum API salt and proposed a complementary salt screen in addition to the already existing ones. Prior to the screen, in-silico energy calculations were performed to rank the theoretical opportunities to form crystalline salts using a range of previously un-tested counter-ions and the results become a vital part of the screen design. The salt screen was performed and a number of candidates were identified and thoroughly characterised regarding stability, solid state properties, processability, scale-up possibilities and not the least regarding impact on dissolution and bioavailability.

Outcome

The selected salt showed a 10-fold improvement in dissolution properties and a confirmed desired change in PK profile. The salt had good solid state and stability properties, excellent formulation and processing behaviour and was shown possible to manufacture in commercial scale with high yield and a robust process. The customer can foresee an immense market potential.