Poorly water-soluble drugs present a wide range of challenges during development and, if not addressed, can ultimately render a drug ineffective in patients. While the issue of poor solubility is not new, the increased use of techniques such as combinatorial chemistry and high-throughput screening in drug discovery has led to a growing number of compounds that have low solubility in both water and organic solvents. Referred to as “brick dust compounds,” these candidates call on expertise and methodologies that can help overcome these challenges. This paper presents 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.

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