Direct to market with direct compression

By David Bain, General Manager - Formulation Technologies (Colorcon) and Tina Dasbach, Global Product Development Manager (Dow Wolf Cellulosics)

In today’s environment, the pharmaceutical formulator is increasingly challenged to deliver innovative medicines faster in spite of shorter timelines, fewer resources and increasing quality demands. At the same time, ‘evergreening’ existing products by innovator companies has increased due to the patent cliff. Generic companies are also seeking to improve their position and expand indications. Drug delivery is playing a key role in meeting these challenges.

Finding simpler ways to produce robust formulations such as use of fewer excipients and processing steps can reduce the number of variables, therefore reducing scale-up risk and development time. New presentations and/or new applications of existing products are therefore needed to reduce variability, improve quality and increase throughput. Using controlled release polymers that facilitate direct compression (DC) is an attractive proposition particularly for water sensitive actives.

Developing effective DC polymers requires balancing several, sometimes conflicting, features such as powder flow, compressibility, segregation, and controlled drug release. Present in 80 percent of new matrix formulations licensed by the FDA since 2007, hydroxypropyl methylcellulose (HPMC) shows poor flow and limits its use in DC applications, forcing manufactures to move to granulation operations. Previous solutions were co-formulated with other excipients or used novel materials which complicated, rather than simplified, development. 

METHOCEL^TM DC was recently launched as an alternative for DC applications using a trusted CR polymer and meeting the monograph requirements for HPMC 2208. Good flow and compressibility combine to provide controlled release equivalent to standard HPMC grades, and allow processes and development programs to be significantly simplified.  Conversion to METHOCEL DC for matrix formulations has high potential to reduce the development time and overall costs for the pharmaceutical formulator.

METHOCEL is a trademark of the Dow Chemical Company