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The newly-published paper, Predictions of Biorelevant Solubility Change During Dispersion and Digestion of Lipid-based Formulations, discusses the use of in-line UV probes (Rainbow Dynamic Dissolution Monitor, Pion, Inc.) to measure the concentration of poorly water-soluble drugs pre- and post-digestion using the MicroDISS Profiler configuration of the Rainbow system. The results show that cationic drugs tend to have higher concentrations post-digestion, while non-ionized drugs do not exhibit a significant change. Anionic drugs tend to have lower or unchanged concentrations post-digestion.
The study concludes that the model developed can support a computationally-guided strategy for developing poorly water-soluble drugs by predicting biorelevant solubility changes during dispersion and digestion. This will facilitate more data-informed decision making and efficient use of formulation screening resources.
Some key points from the article include:
* Cationic drugs tend to have higher concentrations post-digestion, while non-ionized drugs do not exhibit a significant change.
* Anionic drugs tend to have lower or unchanged concentrations post-digestion.
* Partial least squares modeling can be used to predict changes in solubility ratio pre- and post-digestion.
* Multiple linear regression equations can be used to predict solubility ratio pre- and post-digestion using molecular descriptors such as melting point, LogD, and number of aromatic rings.
* The model developed can support a computationally guided strategy for developing poorly water-soluble drugs.
