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A methodological evaluation and predictive in silico investigation into the multi-functionality of arginine in directly compressed tablets

A methodological evaluation and predictive in silico investigation into the multi-functionality of arginine in directly compressed tablets

Elshaer, Amr, Kaialy, Waseem, Akhtar, Noreen, Lyire, Affiong, Hussain, Tariq, Alany, Raid and Mohammed, Afzal (2015) A methodological evaluation and predictive in silico investigation into the multi-functionality of arginine in directly compressed tablets. European Journal of Pharmaceutics and Biopharmaceutics, 96. pp. 272-281. ISSN 0939-6411 (Print), 0939-6411 (Online) (doi:/10.1016/j.ejpb.2015.07.028)

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Abstract

The acceleration of solid dosage form product development can be facilitated by the inclusion of excipients that exhibit poly-/multi-functionality with reduction of the time invested in multiple excipient optimisations. Because active pharmaceutical ingredients (APIs) and tablet excipients present diverse densification behaviours upon compaction, the involvement of these different powders during compaction makes the compaction process very complicated. The aim of this study was to assess the macrometric characteristics and distribution of surface charges of two powders: indomethacin (IND) and arginine (ARG); and evaluate their impact on the densification properties of the two powders. Response surface modelling (RSM) was employed to predict the effect of two independent variables; Compression pressure (F) and ARG percentage (R) in binary mixtures on the properties of resultant tablets. The study looked at three responses namely; porosity (P), tensile strength (S) and disintegration time (T). Micrometric studies showed that IND had a higher charge density (net charge to mass ratio) when compared to ARG; nonetheless, ARG demonstrated good compaction properties with high plasticity (Y = 28.01 MPa). Therefore, ARG as filler to IND tablets was associated with better mechanical properties of the tablets (tablet tensile strength (r) increased from 0.2 ± 0.05 N/mm2 to 2.85 ± 0.36 N/mm2 upon adding ARG at molar ratio of 8:1 to IND). Moreover, tablets’ disintegration time was shortened to reach few seconds in some of the formulations. RSM revealed tablet porosity to be affected by both compression pressure and ARG ratio for IND/ARG physical mixtures (PMs). Conversely, the tensile strength (r) and disintegration time (T) for the PMs were influenced by the compression pressure, ARG ratio and their interactive term (FR); and a strong correlation was observed between the experimental results and the predicted data for tablet porosity. This work provides clear evidence of the multi-functionality of ARG as filler, binder and disintegrant for directly compressed tablets.

Item Type: Article
Uncontrolled Keywords: Indomethacin; Arginine; Compressibility; Compactibility; Tabletability; Disintegration time; Multifunctional excipient; Direct compression
Subjects: Q Science > QD Chemistry
Faculty / Department / Research Group: Faculty of Engineering & Science
Faculty of Engineering & Science > Department of Applied Engineering & Management
Last Modified: 29 Nov 2016 16:48
Selected for GREAT 2016: None
Selected for GREAT 2017: None
Selected for GREAT 2018: None
URI: http://gala.gre.ac.uk/id/eprint/13884

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