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Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine

Ali, Joseph; Zgair, Atheer; Hameed, Ghaidaa S.; Garnett, Martin C.; Roberts, Clive J.; Burley, Jonathan C.; Gershkovich, Pavel

Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine Thumbnail


Authors

Joseph Ali

Atheer Zgair

Ghaidaa S. Hameed

Martin C. Garnett



Abstract

The oral cavity is of great importance to the performance of orally retained formulations, including: orally disintegrating tablets, taste-masked formulations, and buccal/sublingual delivery systems. With regards to in vitro dissolution assessment of these dosage forms, human saliva should be represented by the dissolution media. Currently there is no general consensus regarding oral cavity dissolution. In this study pooled human saliva was characterised and utilised as dissolution media for biorelevant oral cavity dissolution studies and to assess drug release. Lipophilic drug felodipine with challenging biopharmaceutical properties was selected for assessment in oral cavity dissolution studies. These saliva dissolution studies investigated for the first time how biorelevant dissolution can be implemented as a screening tool to guide the formulation development process and to predict dosage form performance within the mouth. In this study a combination of three dissolution enhancement strategies (cryomilling, solid dispersion, and inclusion complexation) were employed to eventually increase the concentration of felodipine in saliva 150-fold. Using this successful formulation strategy orally disintegrating tablets of felodipine were produced. Interestingly, the percentage release of felodipine in compendial dissolution apparatus was shown to be over 80% after 10 minutes. On the other hand, salivabased dissolution showed that percentage release of felodipine was only 0.2% after 10 minutes using the same formulation. This discrepancy in drug release between dissolution media highlights the need for biorelevant dissolution apparatus for the oral cavity to reliably assess performance of relevant dosage forms in vitro.

Citation

Ali, J., Zgair, A., Hameed, G. S., Garnett, M. C., Roberts, C. J., Burley, J. C., & Gershkovich, P. (2019). Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine. International Journal of Pharmaceutics, 555, 228-236. https://doi.org/10.1016/j.ijpharm.2018.11.051

Journal Article Type Article
Acceptance Date Nov 17, 2018
Online Publication Date Nov 19, 2018
Publication Date Jan 30, 2019
Deposit Date Nov 19, 2018
Publicly Available Date Nov 20, 2019
Journal International Journal of Pharmaceutics
Print ISSN 0378-5173
Electronic ISSN 1873-3476
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 555
Pages 228-236
DOI https://doi.org/10.1016/j.ijpharm.2018.11.051
Keywords Biorelevant dissolution; Human saliva; Oral cavity; Felodipine; Orally disintegrating tablets
Public URL https://nottingham-repository.worktribe.com/output/1284067
Publisher URL https://www.sciencedirect.com/science/article/pii/S0378517318308755?via%3Dihub
Additional Information This article is maintained by: Elsevier; Article Title: Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine; Journal Title: International Journal of Pharmaceutics; CrossRef DOI link to publisher maintained version: https://doi.org/10.1016/j.ijpharm.2018.11.051; Content Type: article; Copyright: © 2018 The Authors. Published by Elsevier B.V.
Contract Date Nov 19, 2018

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