for Physical Chemists by Physical Chemists


Supersaturation effects in solubility enhancing excipients and biorelevant media

Karl Box, Sirius Analytical, UK

Currently, there is a great deal of interest in supersaturating dosage forms as a means of improving the bioavailability of drugs with poor aqueous solubility. This presentation will describe methods for assessing the amount of supersaturation present in an in-vitro system in early phase drug discovery by studying dissolution and precipitation events in real-time.

Solubility enhancement in the presence of formulation excipients will be presented, showing how this can be used as an opportunity for promoting a molecule’s class in the Biopharmaceutics Classification System. The effects of bio-relevant media (e.g., simulated intestinal fluids) will also be explored. Understanding solubility enhancement may be critical to designing optimal supersaturating dosage forms as well as improving predictive models for absorption by taking into account supersaturation and precipitation events in-vivo.

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Last modified: 28 April 2008