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Formulation and evaluation of fast dissolving tablets of haloperidol solid dispersion

PURPOSE: The aim of this study was to design fast dissolving tablets (FDT) of the anti –psychiatric drug haloperidol in solid dispersion forms as a way to enhance its dissolution profile and anti-psychiatric effect. METHODS: Solubility studies of haloperidol in various polymers solutions were invest...

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Autores principales: Eisa, Aya M., El-Megrab, Nagia A., El-Nahas, Hanan M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9715955/
https://www.ncbi.nlm.nih.gov/pubmed/36465849
http://dx.doi.org/10.1016/j.jsps.2022.09.002
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author Eisa, Aya M.
El-Megrab, Nagia A.
El-Nahas, Hanan M.
author_facet Eisa, Aya M.
El-Megrab, Nagia A.
El-Nahas, Hanan M.
author_sort Eisa, Aya M.
collection PubMed
description PURPOSE: The aim of this study was to design fast dissolving tablets (FDT) of the anti –psychiatric drug haloperidol in solid dispersion forms as a way to enhance its dissolution profile and anti-psychiatric effect. METHODS: Solubility studies of haloperidol in various polymers solutions were investigated. The selected polymer with high drug solubility (Poly ethylene glycol 4000) was used for preparation of solid dispersion through two methods solvent evaporation method and melting method. Haloperidol solid dispersion mixed with other solid powder excipients and compressed into tablets. The resulted tablets were evaluated according to British Pharmacopoeia (B.P.) specifications. Pre- and post -compression studies were performed to determine the flow properties and evaluate the solid dispersion systems, followed by in vivo studies through forced swimming test (FST) RESULTS: Pre-compression studies showed adequate flowability and compatibility of polymer and solid excipients with haloperidol. The selected solid dispersion tablet (SD2) demonstrated the best disintegration and water absorption ratio in addition to satisfactory friability and hardness. Attempts of in vitro dissolution results and thermodynamic stability studies showed acceptable results for (SD2) formulation containing PEG 4000 polymer prepared by melting method.The in vivo study of (SD2) formulation revealed the highest immobility time to rats compared to control rats and others treated with commercial haloperidol product. CONCLUSION: Fast dissolving tablets prepared from solid dispersion of haloperidol with PEG4000 expressed rapid onset of action with enhanced anti-psychiatric effect of haloperidol.
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spelling pubmed-97159552022-12-03 Formulation and evaluation of fast dissolving tablets of haloperidol solid dispersion Eisa, Aya M. El-Megrab, Nagia A. El-Nahas, Hanan M. Saudi Pharm J Original Article PURPOSE: The aim of this study was to design fast dissolving tablets (FDT) of the anti –psychiatric drug haloperidol in solid dispersion forms as a way to enhance its dissolution profile and anti-psychiatric effect. METHODS: Solubility studies of haloperidol in various polymers solutions were investigated. The selected polymer with high drug solubility (Poly ethylene glycol 4000) was used for preparation of solid dispersion through two methods solvent evaporation method and melting method. Haloperidol solid dispersion mixed with other solid powder excipients and compressed into tablets. The resulted tablets were evaluated according to British Pharmacopoeia (B.P.) specifications. Pre- and post -compression studies were performed to determine the flow properties and evaluate the solid dispersion systems, followed by in vivo studies through forced swimming test (FST) RESULTS: Pre-compression studies showed adequate flowability and compatibility of polymer and solid excipients with haloperidol. The selected solid dispersion tablet (SD2) demonstrated the best disintegration and water absorption ratio in addition to satisfactory friability and hardness. Attempts of in vitro dissolution results and thermodynamic stability studies showed acceptable results for (SD2) formulation containing PEG 4000 polymer prepared by melting method.The in vivo study of (SD2) formulation revealed the highest immobility time to rats compared to control rats and others treated with commercial haloperidol product. CONCLUSION: Fast dissolving tablets prepared from solid dispersion of haloperidol with PEG4000 expressed rapid onset of action with enhanced anti-psychiatric effect of haloperidol. Elsevier 2022-11 2022-09-09 /pmc/articles/PMC9715955/ /pubmed/36465849 http://dx.doi.org/10.1016/j.jsps.2022.09.002 Text en © 2022 The Author(s) https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Original Article
Eisa, Aya M.
El-Megrab, Nagia A.
El-Nahas, Hanan M.
Formulation and evaluation of fast dissolving tablets of haloperidol solid dispersion
title Formulation and evaluation of fast dissolving tablets of haloperidol solid dispersion
title_full Formulation and evaluation of fast dissolving tablets of haloperidol solid dispersion
title_fullStr Formulation and evaluation of fast dissolving tablets of haloperidol solid dispersion
title_full_unstemmed Formulation and evaluation of fast dissolving tablets of haloperidol solid dispersion
title_short Formulation and evaluation of fast dissolving tablets of haloperidol solid dispersion
title_sort formulation and evaluation of fast dissolving tablets of haloperidol solid dispersion
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9715955/
https://www.ncbi.nlm.nih.gov/pubmed/36465849
http://dx.doi.org/10.1016/j.jsps.2022.09.002
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