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

Autor: Patrick Kunz, Andreas Steingoetter, Werner Schwizer, Karsten Mäder, Peter Boesiger, Miriam Thumshirn, Hans Lengsfeld, Michael Fried, Dominik Weishaupt
Rok vydání: 2003
Předmět:
Zdroj: Pharmaceutical Research, 20 (12)
ISSN: 0724-8741
DOI: 10.1023/b:pham.0000008049.40370.5a
Popis: 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%); p0.05). 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.
Databáze: OpenAIRE