New Excipients for Solubilizing APIs: Expansion of the HPMCAS Chemistry Space

July 1, 2013

 

Morgen, M., D. Lyon, R. Schmitt, M. Brackhagen, and O. Petermann, “New Excipients for Solubilizing APIs: Expansion of the HPMCAS Chemistry Space,” Tablets & Capsules, 11:5(2013)10-16.

 

An estimated 40 to 80 percent of new chemical entities (NCEs) have low aqueous solubility and are therefore susceptible to poor oral absorption. Amorphous solid dispersions—which comprise an active pharmaceutical ingredient (API) molecularly dispersed in enabling polymeric excipients—can be used to increase the oral bioavailability of such poorly water-soluble APIs. Hydroxypropyl methylcellulose (HPMC) ester derivatives, in particular, have shown superior performance as solubilization polymers in amorphous dispersions.

This article describes the expansion of the current commercial chemistry space for hydroxypropyl methylcellulose acetate succinate (HPMCAS) to improve solubilization performance by selecting optimal polymers for specific APIs using a robust design-space analysis. In addition, we describe novel HPMCAS polymers that can increase the manufacturing throughput of amorphous dispersions.

 

 

Topics: 
Bioavailability Enhancement