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Published on: July 4, 2014
Characterizing the Impact of Spray Dried Particle Morphology on Tablet Dissolution Using Quantitative X-Ray
Shawn Zhang1, Paul A Stroud2, Aiden Zhu1
1DigiM Solution LLC, 67 South Bedford Street, Suite 400 West, Burlington, MA United States.
Three-dimensional X-ray microscopy and AI image analysis revealed how spray-dried particle microstructure impacts tablet dissolution. This advanced characterization links particle properties to drug product performance, aiding formulation development.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Chemical Engineering
Background:
- Oral solid dosage form performance is linked to powder and particle characteristics.
- Characterizing particle structure's impact on tablet compaction and dissolution remains a challenge.
- 3D non-invasive tomographic imaging offers micro-scale insights beyond traditional methods.
Purpose of the Study:
- To investigate the relationship between spray-dried particle (SDP) microstructure and tablet dissolution behavior.
- To apply 3D X-Ray Microscopy and AI image analytics for quantitative characterization of merestinib SDPs and tablets.
- To correlate microstructural properties with observed dissolution performance.
Main Methods:
- Analysis of two merestinib spray-dried particle (SDP) batches and their corresponding tablets using 3D X-Ray Microscopy.
- Application of artificial intelligence-based image analytics to quantify particle microstructural properties (porosity, pore size, surface area, connectivity).
- Correlation of image-derived physical properties with dissolution behavior and validation against conventional measurements.
Main Results:
- 3D X-Ray Microscopy and AI image analytics successfully quantified microstructural differences in merestinib SDPs.
- Quantitative insights into porosity, pore size distribution, surface area, and pore connectivity were obtained.
- These microstructural differences were directly correlated with and explained variations in tablet dissolution rates.
Conclusions:
- Microstructure of spray-dried particles significantly influences tablet compaction and dissolution performance.
- 3D X-Ray Microscopy combined with AI image analysis provides valuable quantitative data for understanding drug product performance.
- This approach enables tracing root causes of performance variations to the particle level, aiding formulation optimization.
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