The Disintegration Process in Microcrystalline Cellulose Based Tablets I.: Influence of Temperature, Porosity and Superdisintegrants
Goodwin, Daniel J
Journal of Pharmaceutical Sciences
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Yassin, S., Goodwin, D. J., Anderson, A., Sibik, J., Wilson, I., Gladden, L., & Zeitler, A. (2015). The Disintegration Process in Microcrystalline Cellulose Based Tablets I.: Influence of Temperature, Porosity and Superdisintegrants. Journal of Pharmaceutical Sciences, 104 3440-3450. https://doi.org/10.1002/jps.24544
Disintegration performance was measured by analysing both water ingress and tablet swelling of pure microcrystalline cellulose (MCC) and in mixture with croscarmellose sodium using terahertz pulsed imaging (TPI). Tablets made from pure MCC with porosities of 10% and 15% showed similar swelling and transport kinetics: within the first 15 s, tablets had swollen by up to 33% of their original thickness and water had fully penetrated the tablet following Darcy flow kinetics. In contrast, MCC tablets with a porosity of 5% exhibited much slower transport kinetics, with swelling to only 17% of their original thickness and full water penetration reached after 100 s, dominated by case II transport kinetics. The effect of adding superdisintegrant to the formulation and varying the temperature of the dissolution medium between 20°C and 37°C on the swelling and transport process was quantified. We have demonstrated that TPI can be used to non-invasively analyse the complex disintegration kinetics of formulations that take place on timescales of seconds and is a promising tool to better understand the effect of dosage form microstructure on its performance. By relating immediate-release formulations to mathematical models used to describe controlled release formulations, it becomes possible to use this data for formulation design.
terahertz pulsed imaging, structure-transport relationship, porosity, swelling, solid dosage forms, polymeric drug delivery systems, formulation, superdisintegrants
S.Y. would like to thank the U. K. Engineering and Physical Sciences Research Council (EPSRC) for a studentship. J.S. and J.A.Z. would like to acknowledge the EPSRC for funding (EP/J007803/1).
External DOI: https://doi.org/10.1002/jps.24544
This record's URL: https://www.repository.cam.ac.uk/handle/1810/248535
Attribution 2.0 UK: England & Wales
Licence URL: http://creativecommons.org/licenses/by/2.0/uk/