Advanced Technologies To Improve Solubility And Spray Drying Throughput For Brick Dust Compounds

By David Lyon, Ph.D., Senior Fellow, and Molly Adam, Lonza R&D Spray Drying Expert, Bioavailability Enhancement, Lonza Small Molecules

Low solubility is a drug development challenge that has plagued the industry for decades, with 70% to 80% of the development pipeline drugs today consisting of poorly soluble molecules. As a result, solubility is regarded as a key driver for improving bioavailability and efficacy. Several formulation strategies can be used to improve solubility, with conversion to amorphous solid dispersion (ASD) being the most frequently used technology from 2000 to 2020. 

The most common technique for the manufacture of ASD systems is spraying drying, due to its fast drying rate, enabling kinetic trapping of the drug in amorphous form, and scalability. For this process to yield an amorphous product, all of the components that begin in the solution tank must be fully dissolved before the spray drying process. However, the increased number of brick dust compounds ― compounds that have poor solubility in water and organic solvents ― can make this especially challenging and, if not addressed, can ultimately render a drug ineffective in patients. These candidates call on expertise and methodologies that can help overcome these challenges.

Download the full paper to learn more about three approaches used by experts at Lonza Small Molecules to address poor solubility in organic solvents for spray drying as well as case studies outlining their successful application during development.