Evidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.

The work investigates the adhesive/cohesive molecular and physical interactions together with nanoscopic features of commonly used orally disintegrating tablet (ODT) excipients microcrystalline cellulose (MCC) and D-mannitol. This helps to elucidate the underlying physico-chemical and mechanical mec...

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Autores principales: Ali Al-Khattawi, Hamad Alyami, Bill Townsend, Xianghong Ma, Afzal R Mohammed
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Publicado: Public Library of Science (PLoS) 2014
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Acceso en línea:https://doaj.org/article/43f815b63c724f55b2d419571b86af99
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spelling oai:doaj.org-article:43f815b63c724f55b2d419571b86af992021-11-25T06:08:26ZEvidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.1932-620310.1371/journal.pone.0101369https://doaj.org/article/43f815b63c724f55b2d419571b86af992014-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/25025427/pdf/?tool=EBIhttps://doaj.org/toc/1932-6203The work investigates the adhesive/cohesive molecular and physical interactions together with nanoscopic features of commonly used orally disintegrating tablet (ODT) excipients microcrystalline cellulose (MCC) and D-mannitol. This helps to elucidate the underlying physico-chemical and mechanical mechanisms responsible for powder densification and optimum product functionality. Atomic force microscopy (AFM) contact mode analysis was performed to measure nano-adhesion forces and surface energies between excipient-drug particles (6-10 different particles per each pair). Moreover, surface topography images (100 nm2-10 µm2) and roughness data were acquired from AFM tapping mode. AFM data were related to ODT macro/microscopic properties obtained from SEM, FTIR, XRD, thermal analysis using DSC and TGA, disintegration testing, Heckel and tabletability profiles. The study results showed a good association between the adhesive molecular and physical forces of paired particles and the resultant densification mechanisms responsible for mechanical strength of tablets. MCC micro roughness was 3 times that of D-mannitol which explains the high hardness of MCC ODTs due to mechanical interlocking. Hydrogen bonding between MCC particles could not be established from both AFM and FTIR solid state investigation. On the contrary, D-mannitol produced fragile ODTs due to fragmentation of surface crystallites during compression attained from its weak crystal structure. Furthermore, AFM analysis has shown the presence of extensive micro fibril structures inhabiting nano pores which further supports the use of MCC as a disintegrant. Overall, excipients (and model drugs) showed mechanistic behaviour on the nano/micro scale that could be related to the functionality of materials on the macro scale.Ali Al-KhattawiHamad AlyamiBill TownsendXianghong MaAfzal R MohammedPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 9, Iss 7, p e101369 (2014)
institution DOAJ
collection DOAJ
language EN
topic Medicine
R
Science
Q
spellingShingle Medicine
R
Science
Q
Ali Al-Khattawi
Hamad Alyami
Bill Townsend
Xianghong Ma
Afzal R Mohammed
Evidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.
description The work investigates the adhesive/cohesive molecular and physical interactions together with nanoscopic features of commonly used orally disintegrating tablet (ODT) excipients microcrystalline cellulose (MCC) and D-mannitol. This helps to elucidate the underlying physico-chemical and mechanical mechanisms responsible for powder densification and optimum product functionality. Atomic force microscopy (AFM) contact mode analysis was performed to measure nano-adhesion forces and surface energies between excipient-drug particles (6-10 different particles per each pair). Moreover, surface topography images (100 nm2-10 µm2) and roughness data were acquired from AFM tapping mode. AFM data were related to ODT macro/microscopic properties obtained from SEM, FTIR, XRD, thermal analysis using DSC and TGA, disintegration testing, Heckel and tabletability profiles. The study results showed a good association between the adhesive molecular and physical forces of paired particles and the resultant densification mechanisms responsible for mechanical strength of tablets. MCC micro roughness was 3 times that of D-mannitol which explains the high hardness of MCC ODTs due to mechanical interlocking. Hydrogen bonding between MCC particles could not be established from both AFM and FTIR solid state investigation. On the contrary, D-mannitol produced fragile ODTs due to fragmentation of surface crystallites during compression attained from its weak crystal structure. Furthermore, AFM analysis has shown the presence of extensive micro fibril structures inhabiting nano pores which further supports the use of MCC as a disintegrant. Overall, excipients (and model drugs) showed mechanistic behaviour on the nano/micro scale that could be related to the functionality of materials on the macro scale.
format article
author Ali Al-Khattawi
Hamad Alyami
Bill Townsend
Xianghong Ma
Afzal R Mohammed
author_facet Ali Al-Khattawi
Hamad Alyami
Bill Townsend
Xianghong Ma
Afzal R Mohammed
author_sort Ali Al-Khattawi
title Evidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.
title_short Evidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.
title_full Evidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.
title_fullStr Evidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.
title_full_unstemmed Evidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.
title_sort evidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.
publisher Public Library of Science (PLoS)
publishDate 2014
url https://doaj.org/article/43f815b63c724f55b2d419571b86af99
work_keys_str_mv AT alialkhattawi evidencebasednanoscopicandmolecularframeworkforexcipientfunctionalityincompressedorallydisintegratingtablets
AT hamadalyami evidencebasednanoscopicandmolecularframeworkforexcipientfunctionalityincompressedorallydisintegratingtablets
AT billtownsend evidencebasednanoscopicandmolecularframeworkforexcipientfunctionalityincompressedorallydisintegratingtablets
AT xianghongma evidencebasednanoscopicandmolecularframeworkforexcipientfunctionalityincompressedorallydisintegratingtablets
AT afzalrmohammed evidencebasednanoscopicandmolecularframeworkforexcipientfunctionalityincompressedorallydisintegratingtablets
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