In Situ Monitoring of Supersaturation State for Solid Dispersions of Low Soluble Compounds

Purpose. Solid dispersion technology is used to create amorphous APIs with enhanced solubility potentially leading to improved bioavailability. The objective of the study was to monitor dissolution and precipitation behavior of supersaturating solutions of low soluble compounds. Solubility enhancement was tested using a small-volume in situ UV dissolution apparatus μDISS Profiler™ (Pion Inc.) by collecting concentration-time profiles in biorelevant media (e.g., FaSSIF and FeSSIF).

Conclusions. Hot melt extrudates with Copovidone provide opportunity to improve bioavailability of low soluble compounds. The μDISS Profiler allows real-time concentration monitoring of limited amount of material in small volumes of media thus providing a valuable tool for studying meta-stable solubility of amorphous form of API.