Enhancing The Solubility Characteristics Of High Lipophilicity Drugs Via Spray Drying

By Anthony Qu, VP of Research & Development, Adare Pharma Solutions

An R&D project has shown that the solubility and dissolution characteristics for Itraconazole can be improved by helping them to maintain an amorphous state after spray drying with selected hydrophillic polymers. This paper explores the concept of converting a crystalline drug into amorphous spray dried dispersion (SDD) to increase the dissolution rates relative to crystalline form. The high super saturated concentration state attained following the conversion indicates an amorphous solubility enhancement. The paper outlines the spray drying process and solution parameters used to achieve enhanced solubility. Thermal analysis using differential scanning calorimetry was used to evaluate the amorphous characteristics of the SDDs.

This technique can be a useful tool for solubility enhancement when dealing with drugs with low solubility in BCS Class II and IV. Download the complete White Paper in PDF to explore the R&D work which establishes proof-of-concept for the solubility enhancement of Itraconazole by amorphous solid dispersion using a Buchi-290 spray dryer.