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Magnetic Resonance Imaging for the in Vivo Evaluation of Gastric-Retentive Tablets

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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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Authors and Affiliations

  1. Biophysics group, Institute of Biomedical Engineering, University and ETH Zurich Gloriastrasse, 35 CH-8092, Zurich, Switzerland

    Andreas Steingoetter

  2. Department of Radiology, University Hospital Zurich, Switzerland

    Dominik Weishaupt

  3. F. Hoffmann-LaRoche, Basel, Switzerland

    Patrick Kunz, Karsten Mäder & Hans Lengsfeld

  4. Department of Gastroenterology, University Hospital Zurich, Switzerland

    Miriam Thumshirn, Michael Fried & Werner Schwizer

  5. Biophysics group, Institute of Biomedical Engineering, University and ETH Zurich Gloriastrasse, 35 CH-8092, Zurich, Switzerland

    Peter Boesiger

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  1. Andreas Steingoetter
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  2. Dominik Weishaupt
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  3. Patrick Kunz
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  4. Karsten Mäder
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  5. Hans Lengsfeld
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  7. Peter Boesiger
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  8. Michael Fried
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  9. Werner Schwizer
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Correspondence to Andreas Steingoetter.

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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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