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

2.50
Hdl Handle:
http://hdl.handle.net/2436/601308
Title:
A methodological evaluation and predictive in silico investigation into the multi-functionality of arginine in directly compressed tablets
Authors:
ElShaer, Amr; Kaialy, Waseem; Akhtar, Noreen; Iyire, Affiong; Hussain, Tariq; Alany, Raid; Mohammed, Afzal R.
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.
Citation:
A methodological evaluation and predictive in silico investigation into the multi-functionality of arginine in directly compressed tablets 2015, 96:272 European Journal of Pharmaceutics and Biopharmaceutics
Publisher:
Elsevier
Journal:
European Journal of Pharmaceutics and Biopharmaceutics vol 96 (2015) 272–281
Issue Date:
Oct-2015
URI:
http://hdl.handle.net/2436/601308
DOI:
10.1016/j.ejpb.2015.07.028
Additional Links:
http://linkinghub.elsevier.com/retrieve/pii/S0939641115003318
Type:
Article
Language:
en
ISSN:
09396411
Appears in Collections:
Pharmacy and Natural Products Research Group

Full metadata record

DC FieldValue Language
dc.contributor.authorElShaer, Amren
dc.contributor.authorKaialy, Waseemen
dc.contributor.authorAkhtar, Noreenen
dc.contributor.authorIyire, Affiongen
dc.contributor.authorHussain, Tariqen
dc.contributor.authorAlany, Raiden
dc.contributor.authorMohammed, Afzal R.en
dc.date.accessioned2016-03-14T15:32:57Zen
dc.date.available2016-03-14T15:32:57Zen
dc.date.issued2015-10en
dc.identifier.citationA methodological evaluation and predictive in silico investigation into the multi-functionality of arginine in directly compressed tablets 2015, 96:272 European Journal of Pharmaceutics and Biopharmaceuticsen
dc.identifier.issn09396411en
dc.identifier.doi10.1016/j.ejpb.2015.07.028en
dc.identifier.urihttp://hdl.handle.net/2436/601308en
dc.description.abstractThe 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.en
dc.language.isoenen
dc.publisherElsevieren
dc.relation.urlhttp://linkinghub.elsevier.com/retrieve/pii/S0939641115003318en
dc.rightsArchived with thanks to European Journal of Pharmaceutics and Biopharmaceuticsen
dc.subjectIndomethacinen
dc.subjectArginineen
dc.subjectCompressibilityen
dc.subjectCompactibilityen
dc.subjectTabletabilityen
dc.subjectDisintegration timeen
dc.subjectDisintegration timeen
dc.subjectMultifunctional excipienten
dc.subjectDirect compressionen
dc.titleA methodological evaluation and predictive in silico investigation into the multi-functionality of arginine in directly compressed tabletsen
dc.typeArticleen
dc.identifier.journalEuropean Journal of Pharmaceutics and Biopharmaceutics vol 96 (2015) 272–281en
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