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Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion formation

Taste masking of paracetamol was achieved by preparing amorphous solid dispersion (ASD) using modified coacervation method. The method is based on dissolving the drug and polymeric carrier in water adjusted to certain pH level. Then, precipitation of ASD granules is performed by gradually changing p...

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Autores principales: Al-kasmi, Basheer, Alsirawan, M. H. D. Bashir, Paradkar, Anant, Nattouf, Abdul-Hakim, El-Zein, Hind
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8076289/
https://www.ncbi.nlm.nih.gov/pubmed/33903654
http://dx.doi.org/10.1038/s41598-021-88312-6
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author Al-kasmi, Basheer
Alsirawan, M. H. D. Bashir
Paradkar, Anant
Nattouf, Abdul-Hakim
El-Zein, Hind
author_facet Al-kasmi, Basheer
Alsirawan, M. H. D. Bashir
Paradkar, Anant
Nattouf, Abdul-Hakim
El-Zein, Hind
author_sort Al-kasmi, Basheer
collection PubMed
description Taste masking of paracetamol was achieved by preparing amorphous solid dispersion (ASD) using modified coacervation method. The method is based on dissolving the drug and polymeric carrier in water adjusted to certain pH level. Then, precipitation of ASD granules is performed by gradually changing pH level. Therefore, the chosen drug and polymer should obtain appropriate acidic or basic groups to enable pH-dependent solvation. Moreover, using solubility enhancing additives such as sodium lauryl sulphate (SLS) and low viscosity polyethylene glycol (PEG 400) found to be essential in aiding drug/polymer aqueous solvation which enhanced amorphization, hence taste masking and drug loading. Solid dispersion between Paracetamol and Eudragit E was formed and that proved by FT-IR, DSC, PXRD and SEM. Also, Paracetamol was released after 2 min in 0.1 N hydrochloric acid medium and the taste of masking forms are accepted from all volunteers. Modified coacervation method does not involve organic solvents, high temperatures, or sophisticated instruments commonly used in taste masking methods. Using PEG 400 resulted in significantly higher drug loading and dissolution rate compared to SLS granules. Moreover, using previously reported scoring system for the evaluation of taste masking methods shows that pH dependent coacervation obtained high scoring over common methods and thus display a robust potential for industrial applications.
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spelling pubmed-80762892021-04-27 Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion formation Al-kasmi, Basheer Alsirawan, M. H. D. Bashir Paradkar, Anant Nattouf, Abdul-Hakim El-Zein, Hind Sci Rep Article Taste masking of paracetamol was achieved by preparing amorphous solid dispersion (ASD) using modified coacervation method. The method is based on dissolving the drug and polymeric carrier in water adjusted to certain pH level. Then, precipitation of ASD granules is performed by gradually changing pH level. Therefore, the chosen drug and polymer should obtain appropriate acidic or basic groups to enable pH-dependent solvation. Moreover, using solubility enhancing additives such as sodium lauryl sulphate (SLS) and low viscosity polyethylene glycol (PEG 400) found to be essential in aiding drug/polymer aqueous solvation which enhanced amorphization, hence taste masking and drug loading. Solid dispersion between Paracetamol and Eudragit E was formed and that proved by FT-IR, DSC, PXRD and SEM. Also, Paracetamol was released after 2 min in 0.1 N hydrochloric acid medium and the taste of masking forms are accepted from all volunteers. Modified coacervation method does not involve organic solvents, high temperatures, or sophisticated instruments commonly used in taste masking methods. Using PEG 400 resulted in significantly higher drug loading and dissolution rate compared to SLS granules. Moreover, using previously reported scoring system for the evaluation of taste masking methods shows that pH dependent coacervation obtained high scoring over common methods and thus display a robust potential for industrial applications. Nature Publishing Group UK 2021-04-26 /pmc/articles/PMC8076289/ /pubmed/33903654 http://dx.doi.org/10.1038/s41598-021-88312-6 Text en © The Author(s) 2021 https://creativecommons.org/licenses/by/4.0/Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) .
spellingShingle Article
Al-kasmi, Basheer
Alsirawan, M. H. D. Bashir
Paradkar, Anant
Nattouf, Abdul-Hakim
El-Zein, Hind
Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion formation
title Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion formation
title_full Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion formation
title_fullStr Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion formation
title_full_unstemmed Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion formation
title_short Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion formation
title_sort aqueous and ph dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion formation
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8076289/
https://www.ncbi.nlm.nih.gov/pubmed/33903654
http://dx.doi.org/10.1038/s41598-021-88312-6
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