Monitoring Supersaturation State of Solid Dispersions of Low Solubility Compounds

Purpose.  To prepare and test hot melt extrudates of loratidine or piroxicam with copovidone polymers to improve the API solubility.  A bench-top Dynisco laboratory mixing extruder (LME) was used for preparation of the materials at various temperatures.  Dissolution behavior and solubility enhancement was tested using a small-volume in situ UV dissolution apparatus (μDISS Profiler) to collect concentration-time profiles in biorelevant media such as FaSSIF and FeSSIF.

Conclusions.  The supersaturation of piroxicam hot melt extrudates was quasi-stable for more than 24 hours at 3.5 times the solubility of the neat API.  Loratidine extrudates also exhibited a potential for supersaturation as well.  The µDISS Profiler provided concentration-time profiles with high data density without precipitation artifacts caused by liquid sampling.