Scientific article
English

Microenvironmental pH and microviscosity inside pH-controlled matrix tablets: An EPR imaging study

Published inJournal of controlled release, vol. 112, no. 1, p. 72-78
Publication date2006-05-01
First online date2006-02-14
Abstract

Incorporation of pH modifiers is a commonly used strategy to enhance the dissolution rate weakly basic drugs from sustained release solid dosage forms. Electron paramagnetic resonance imaging (EPRI) was applied to spatially monitor pHM and the rotational correlation time (τR), a parameter which is closely related to the surrounding microviscosity inside HPMC (hydroxypropylmethylcellulose) matrix tablets. Fumaric, citric, and succinic acid were employed as pH modifiers. 4-(methylamino)-2-ethyl-5,5-dimethyl-4-pyridine-2-yl-2,5-dihydro-1H-imidazole-1-oxyl (MEP) was used as spin label. Fumaric and citric acid reduced the pHM to equal extents in the initial phase. With the progress of hydration, the more soluble citric acid diffused out from the tablet resulting in an increase in pHM, originating at the outer layers. In contrast, fumaric acid maintained a constantly reduced pHM inside the entire tablet. Due to its lower acidic strength, succinic acid did not reduce the pHM as effectively as the other pH modifiers used. The more water-soluble acids stimulated the water penetration into the matrix system, thereby rapidly decreasing τR. Once the matrix tablets were hydrated, the included pH modifiers influenced τR insignificantly. EPRI, a novel approach for monitoring pHM and τR non-invasively and spatially resolved, was used successfully for the optimization of an pH-controlled formulation.

Keywords
  • EPR imaging
  • Microenvironmental pH
  • Microviscosity
  • HPMC
  • Controlled release
Citation (ISO format)
SIEPE, Stefanie et al. Microenvironmental pH and microviscosity inside pH-controlled matrix tablets: An EPR imaging study. In: Journal of controlled release, 2006, vol. 112, n° 1, p. 72–78. doi: 10.1016/j.jconrel.2005.12.021
Main files (1)
Article (Published version)
accessLevelRestricted
Identifiers
Journal ISSN0168-3659
192views
0downloads

Technical informations

Creation02/03/2023 10:38:00
First validation02/03/2023 10:38:00
Update16/03/2023 10:54:49
Status update16/03/2023 10:54:49
Last indexation01/11/2024 04:26:53
All rights reserved by Archive ouverte UNIGE and the University of GenevaunigeBlack