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Physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives

BACKGROUND AND THE PURPOSE OF THE STUDY: The success of any direct-tableting procedure is strongly affected by the quality of the crystals used in the process. Ibuprofen is a poorly compactible drug with a high tendency for capping. In order to use ibuprofen in direct compression formulations, physi...

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Autores principales: Nokhodchi, A., Amire, O., Jelvehgari, M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Tehran University of Medical Sciences 2010
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3304370/
https://www.ncbi.nlm.nih.gov/pubmed/22615598
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author Nokhodchi, A.
Amire, O.
Jelvehgari, M.
author_facet Nokhodchi, A.
Amire, O.
Jelvehgari, M.
author_sort Nokhodchi, A.
collection PubMed
description BACKGROUND AND THE PURPOSE OF THE STUDY: The success of any direct-tableting procedure is strongly affected by the quality of the crystals used in the process. Ibuprofen is a poorly compactible drug with a high tendency for capping. In order to use ibuprofen in direct compression formulations, physico-mechanical properties of ibuprofen should be improved considerably. The aim of the present investigation was to employ crystallization techniques in order to improve the physico- mechanical properties of ibuprofen for direct compression. METHODS: The experimental methods involved the preparation of ibuprofen crystals by solvent change technique. Ibuprofen was dissolved in ethanol and crystallized out with water in the absence or presence of various hydrophilic additives (PEG 6000, 8000, Brij 98P and polyvinyl alcohol 22000, PVA (22000)) with different concentrations. The physico-mechanical properties of the ibuprofen crystals were studied in terms of flow, density, tensile strength and dissolution behaviour. Morphology of ibuprofen crystals was studied by scanning electron microscopic (SEM). Solid state of the recrystallized particles was also investigated using differential scanning calorimeter (DSC) and FT-IR. RESULTS: Ibuprofen samples crystallized in the presence of PEG 6000 and 8000 and PVA showed remarkable increase in the tensile strengths of the directly compressed tablets, while some other additives, i.e. Brij 98P did not produce improved ibuprofen crystals. Ibuprofen powders made from particles obtained in the presence of PVA and Brij 98P showed similar dissolution profiles to the commercial ibuprofen particles. DSC and FT-IR results ruled out any significant interaction between ibuprofen and additives except for the samples crystallized in the presence of PEG 8000. CONCLUSION: The crystal habit of ibuprofen can be altered successfully by the crystallization technique which was developed in this study. The crystals developed in the presence of certain additives can be recommended for direct compression.
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spelling pubmed-33043702012-05-21 Physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives Nokhodchi, A. Amire, O. Jelvehgari, M. Daru Original Article BACKGROUND AND THE PURPOSE OF THE STUDY: The success of any direct-tableting procedure is strongly affected by the quality of the crystals used in the process. Ibuprofen is a poorly compactible drug with a high tendency for capping. In order to use ibuprofen in direct compression formulations, physico-mechanical properties of ibuprofen should be improved considerably. The aim of the present investigation was to employ crystallization techniques in order to improve the physico- mechanical properties of ibuprofen for direct compression. METHODS: The experimental methods involved the preparation of ibuprofen crystals by solvent change technique. Ibuprofen was dissolved in ethanol and crystallized out with water in the absence or presence of various hydrophilic additives (PEG 6000, 8000, Brij 98P and polyvinyl alcohol 22000, PVA (22000)) with different concentrations. The physico-mechanical properties of the ibuprofen crystals were studied in terms of flow, density, tensile strength and dissolution behaviour. Morphology of ibuprofen crystals was studied by scanning electron microscopic (SEM). Solid state of the recrystallized particles was also investigated using differential scanning calorimeter (DSC) and FT-IR. RESULTS: Ibuprofen samples crystallized in the presence of PEG 6000 and 8000 and PVA showed remarkable increase in the tensile strengths of the directly compressed tablets, while some other additives, i.e. Brij 98P did not produce improved ibuprofen crystals. Ibuprofen powders made from particles obtained in the presence of PVA and Brij 98P showed similar dissolution profiles to the commercial ibuprofen particles. DSC and FT-IR results ruled out any significant interaction between ibuprofen and additives except for the samples crystallized in the presence of PEG 8000. CONCLUSION: The crystal habit of ibuprofen can be altered successfully by the crystallization technique which was developed in this study. The crystals developed in the presence of certain additives can be recommended for direct compression. Tehran University of Medical Sciences 2010 /pmc/articles/PMC3304370/ /pubmed/22615598 Text en © 2010 Tehran University of Medical Sciences http://creativecommons.org/licenses/by/3.0/ This work is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License which allows users to read, copy, distribute and make derivative works for non-commercial purposes from the material, as long as the author of the original work is cited properly.
spellingShingle Original Article
Nokhodchi, A.
Amire, O.
Jelvehgari, M.
Physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives
title Physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives
title_full Physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives
title_fullStr Physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives
title_full_unstemmed Physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives
title_short Physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives
title_sort physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3304370/
https://www.ncbi.nlm.nih.gov/pubmed/22615598
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AT jelvehgarim physicomechanicalanddissolutionbehavioursofibuprofencrystalscrystallizedinthepresenceofvariousadditives