(95ac) Use of Advanced Imaging Techniques in Tablet Disintegration Study

Dvorak, J., University of Chemistry and Technology
Lizonova, D., University of Chemistry and Technology
Schongut, M., University of Chemistry and Technology
Stepanek, F., University of Chemistry and Technology
Beranek, J., Zentiva k.s., a Sanofi Group company
Certified testing of tablet disintegration and dissolution provides us useful information. However, there are many more that are hidden due to techniques' restrictions. Such information is e.g. mechanism of disintegration, change of surface morphology or uniformity of the substances' distribution in the tablet. Therefore, there are many techniques used to obtain the remaining information such as Magnetic Resonance Imaging (MRI), Fourier Transform Infra-Red (FTIR) or Raman spectroscopy and microscopy, Terahertz spectroscopy, Scanning Electron Microscopy (SEM) and other.

Presented work uses tablet made by direct compression of binary mixture of ibuprofen and lactose (based on previous results there was 0.2 - 0.5 w/w of ibuprofen content used) pressed at different compaction pressures (low, medium and high). The tablets were subjected to several solutions and were studied by techniques that have insight into the tablet (MRI) and ones that can see the surface (FTIR and SEM).

MRI experiments provided us with several interesting and several expectable results. As the content of ibuprofen was increasing so was increasing the dissolution time and the wetted layer was decreasing. Similar results were observed when the compaction pressure was increased. When the tablets were submerged to dissolution limiting solutions (saturated lactose solution and solution saturated with both lactose and ibuprofen) the disintegration was severely limited and some tablets began to increase their volume. However, in case of 0.2 w/w ibuprofen tablets it didn't matter whether there was dissolution discriminating solution or not, it disintegrated anyway.

FTIR microscopy showed, that not only the amount, but also the shape and size of the particles from which the tablets were compacted can be determined. These findings were further supplemented by the dry state information obtained by Scanning Electron Microscopy after different dissolution times. Further the FTIR-ATR imaging technique helped to understand the basic mechanisms of the tablet disintegration and to study the dissolution and water penetration into the model ibuprofen-lactose tablets.