Magnetic resonance imaging for the in vivo evaluation of gastric-retentive tablets

To develop a magnetic resonance imaging (MRI) technique for assessing in vivo properties of orally ingested gastric-retentive tablets under physiologic conditions. Tablets with different floating characteristics (tablet A-C) were marked with superparamagnetic Fe3O4 particles to analyze intragastric...

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Bibliographic Details
Published in:Pharmaceutical research 2003-12, Vol.20 (12), p.2001-2007
Main Authors: STEINGOETTER, Andreas, WEISHAUPT, Dominik, KUNZ, Patrick, MÄDER, Karsten, LENGSFELD, Hans, THUMSHIRN, Miriam, BOESIGER, Peter, FRIED, Michael, SCHWIZER, Werner
Format: Article
Language:English
Subjects:
Analysis
Biological and medical sciences
Delayed-Action Preparations
Drug Delivery Systems
Ferric Compounds - chemistry
General pharmacology
Heterocyclic Compounds
Humans
Image Processing, Computer-Assisted
Magnetic Resonance Imaging
Medical sciences
Organometallic Compounds
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Stomach - anatomy & histology
Tablets
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Summary:To develop a magnetic resonance imaging (MRI) technique for assessing in vivo properties of orally ingested gastric-retentive tablets under physiologic conditions. 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). 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. The use of MRI allows the assessment of galenic properties of orally ingested tablets in humans in seated position.
ISSN:0724-8741
1573-904X
DOI:10.1023/b:pham.0000008049.40370.5a