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Development of a Microgram Scale Video-Microscopic Method to Investigate Dissolution Behavior of Poorly Water-Soluble
Malte Bøgh Senniksen1, Juliane Fjelrad Christfort2, Riccardo Marabini3
1Department of Pharmacy, University of Copenhagen, Universitetsparken 2, DK-2100, Copenhagen Ø, Denmark.
AAPS Pharmscitech
|June 23, 2022
Summary
A new video-microscopic method screens drug dissolution rates efficiently. This material-efficient approach aids in grouping poorly water-soluble drugs by their dissolution behavior.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Poor aqueous solubility is a major challenge for oral drug bioavailability.
- Efficient methods for testing drug solubility and dissolution rates are needed.
Purpose of the Study:
- To develop a microgram-scale video-microscopic method for screening dissolution rates of poorly water-soluble drugs.
- To track particle behavior and phase transformations during dissolution.
- To assess the method's applicability across various drugs and media.
Main Methods:
- Utilized optical video-microscopy to track particle surface area changes over time.
- Applied the method to six model drugs in fasted state simulated intestinal fluid (FaSSIF) and buffers.
- Investigated drug dissolution in customized media and tracked phase transformations of carbamazepine.
Main Results:
- The video-microscopic method effectively screened dissolution rates and particle behavior.
- Miniaturized UV spectroscopy yielded similar drug grouping and pH effects.
- Lysophospholipid was found to enhance the dissolution rates of diazepam and dipyridamole.
Conclusions:
- The developed video-microscopic setup provides a material-efficient screening approach for drug dissolution.
- Optical microscopy enables high sample throughput for dissolution rate assessment.
- The method aids in grouping drugs based on their dissolution characteristics.
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