Abstract
Purpose. To develop a magnetic resonance imaging (MRI) technique for assessing in vivo properties of orally ingested gastric-retentive tablets under physiologic conditions.
Methods. Tablets with different floating characteristics (tablet A-C) were marked with superparamagnetic Fe3O4 particles to analyze intragastric tablet position and residence time in human volunteers. Optimal Fe3O4 concentration was determined in vitro. Intragastric release characteristic of one slow-release tablet (tablet D) was analyzed by embedding gadolinium chelates (Gd-DOTA) as a drug model into the tablet. All volunteers underwent MRI in the sitting position. Tablet performance was analyzed in terms of relative position of tablet to intragastric meal level (with 100% at meal surface), intragastric residence time (min) and Gd-DOTA distribution volume (% of meal volume).
Results. Intragastric tablet floating performance and residence time of tablets (tablet A-D) as well as the intragastric Gd-DOTA distribution of tablet D could be monitored using MRI. Tablet floating performance was different between the tablets (A, 93%(95 − 9%); B, 80%(80 − 68%); C, 38%(63 − 32%); p < 0.05). The intragastric distribution volume of Gd-DOTA was 19.9% proximally and 35.5% distally.
Conclusions. The use of MRI allows the assessment of galenic properties of orally ingested tablets in humans in seated position.
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Steingoetter, A., Weishaupt, D., Kunz, P. et al. Magnetic Resonance Imaging for the in Vivo Evaluation of Gastric-Retentive Tablets. Pharm Res 20, 2001–2007 (2003). https://doi.org/10.1023/B:PHAM.0000008049.40370.5a
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DOI: https://doi.org/10.1023/B:PHAM.0000008049.40370.5a