Taste-Masked Pellets of Warfarin Sodium : Formulation towards the Dose Personalisation
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Date
2024-05
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Abstract
The bitter drug, warfarin, has a narrow therapeutic index (NTI) and is used in paediatrics and geriatrics. The aim of this feasibility study was to formulate the taste-masked warfarin-containing pellets to be applicable for dose personalisation and to improve patient compliance, as well as to investigate the effect of the core type (PharSQ® Spheres M, CELPHERE™ CP-507, and NaCl) on the warfarin release from the Kollicoat® Smartseal taste-masking-coated pellets. The cores were successfully drug-loaded and coated in a fluid-bed coater with a Wurster insert. An increase in particle size and particle size distribution was observed by optical microscopy. In saliva-simulated pH, at the Kollicoat® Smartseal level of 2 mg/cm2, none of the pellets demonstrated drug release, confirming their efficient taste-masking. However, in a stomach-simulated pH, a faster drug release was observed from PharSQ® Spheres M- and CELPHERE™ CP-507-coated pellets in comparison with NaCl cores. Additional experiments allowed us to explain the slower drug release from NaCl-containing pellets because of the salting-out effect. Despite the successful taste masking, the drug release from pellets was relatively slow (not more than 91% per 60 min), allowing for further formulation improvements.
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Publisher Copyright: © 2024 by the authors.
Keywords
warfarin, pellets, taste, taste masking, cores, microcrystalline cellulose, dibasic calcium phosphate, sodium chloride, Kollicoat® Smartseal, dibutyl sebacate, salting-out effect, 1.4 Chemical sciences, 2.4 Chemical engineering, 2.5 Materials engineering, 3.1 Basic medicine, 1.1. Scientific article indexed in Web of Science and/or Scopus database
Citation
Kovalenko, L, Kukuls, K, Berga, M & Mohylyuk, V 2024, 'Taste-Masked Pellets of Warfarin Sodium : Formulation towards the Dose Personalisation', Pharmaceutics, vol. 16, no. 5, 586. https://doi.org/10.3390/pharmaceutics16050586