IMCD Pharmaceuticals aims to establish a new platform technology for manufacturing low-dose formulations using a sustainable direct compression process.

 

This innovation changes the status quo of manufacturing low-dose active pharmaceutical ingredients (APIs). It is the result of a proactive strategy by IMCD to support quicker production of new drugs, while reducing resource use and improving sustainability across the sector.

Our Mumbai Pharmaceutical Technical Centre launched an internal project to improve the manufacturing of Apixaban immediate release (IR) tablets.

The project was in line with an increasing launch of various directly compressible, novel co-processed excipients from different suppliers.

Apixaban was chosen for the project because the widely used anticoagulation medication is a blockbuster API, with annual sales of $10.76 billion in 2021 and a patent expiring in 2026. Secondly, it is potent at 5 mg, or about 2.5% of the tablet weight. If such molecules can be formulated with simpler and more sustainable processes, the applications can be extended to many other large-volume low-dose APIs.

The reference-listed brand for Apixaban tablets is produced using a dry granulation process that requires up to nine steps. This can be time-consuming for high-volume products.

 

Direct compression, by contrast, needs fewer manufacturing steps and uses fewer resources. With sustainable direct compression, the drug can be manufactured in four or five steps. Key to the process is selecting highly functional excipients that can carry low-dose APIs, as well as an effective mixing plan that supports homogeneity of the final dosage.

 

This new platform technology results in inventory reductions because fewer ingredients are required. Fewer manufacturing steps mean less time cleaning, thus increasing production speed. At the same time, we addressed coating challenges by selecting a polymer with a shorter coating time.

 

The final product is a robust, stable, and efficient formulation that is equivalent to the original.

 

For the industry, the new platform offers a way to resolve supply chain and sustainability challenges while speeding up the development process and unlocking new value.