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Formulation and optimization of liquisolid compact for enhancing dissolution properties of efavirenz by using DoE approach

Efavirenz displays low and variable bioavailability because of its poor aqueous solubility and high log P-value. The present investigation was aimed to improve the dissolution profile of efavirenz by using a simple, scalable and cost-effective technique of liquisolid compact. The drug was dissolved...

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Detalles Bibliográficos
Autores principales: Jaydip, Bhola, Dhaval, Mori, Soniwala, M.M., Chavda, Jayant
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7292870/
https://www.ncbi.nlm.nih.gov/pubmed/32550806
http://dx.doi.org/10.1016/j.jsps.2020.04.016
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author Jaydip, Bhola
Dhaval, Mori
Soniwala, M.M.
Chavda, Jayant
author_facet Jaydip, Bhola
Dhaval, Mori
Soniwala, M.M.
Chavda, Jayant
author_sort Jaydip, Bhola
collection PubMed
description Efavirenz displays low and variable bioavailability because of its poor aqueous solubility and high log P-value. The present investigation was aimed to improve the dissolution profile of efavirenz by using a simple, scalable and cost-effective technique of liquisolid compact. The drug was dissolved in Trancutol-HP for preparing the liquid medicament which was subsequently mixed with carrier and coating material to make free-flowing and compressible powder. 3(2) full factorial design was used to optimize the formulation in which the Neusilin US2/Corn starch ratios and carrier/coating material ratio were selected as independent variables. The results of in-vitro dissolution test proved that liquisolid compacts have significantly higher dissolution rate than tablets containing pure drug. Results of DSC and XRD studies suggested that the high dissolution of the drug from the liquisolid compacts was possibly because of the drug either being in an amorphous state or being molecularly dispersed within the internal matrix of compacts.
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spelling pubmed-72928702020-06-17 Formulation and optimization of liquisolid compact for enhancing dissolution properties of efavirenz by using DoE approach Jaydip, Bhola Dhaval, Mori Soniwala, M.M. Chavda, Jayant Saudi Pharm J Article Efavirenz displays low and variable bioavailability because of its poor aqueous solubility and high log P-value. The present investigation was aimed to improve the dissolution profile of efavirenz by using a simple, scalable and cost-effective technique of liquisolid compact. The drug was dissolved in Trancutol-HP for preparing the liquid medicament which was subsequently mixed with carrier and coating material to make free-flowing and compressible powder. 3(2) full factorial design was used to optimize the formulation in which the Neusilin US2/Corn starch ratios and carrier/coating material ratio were selected as independent variables. The results of in-vitro dissolution test proved that liquisolid compacts have significantly higher dissolution rate than tablets containing pure drug. Results of DSC and XRD studies suggested that the high dissolution of the drug from the liquisolid compacts was possibly because of the drug either being in an amorphous state or being molecularly dispersed within the internal matrix of compacts. Elsevier 2020-06 2020-05-08 /pmc/articles/PMC7292870/ /pubmed/32550806 http://dx.doi.org/10.1016/j.jsps.2020.04.016 Text en © 2020 Published by Elsevier B.V. on behalf of King Saud University. http://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 Article
Jaydip, Bhola
Dhaval, Mori
Soniwala, M.M.
Chavda, Jayant
Formulation and optimization of liquisolid compact for enhancing dissolution properties of efavirenz by using DoE approach
title Formulation and optimization of liquisolid compact for enhancing dissolution properties of efavirenz by using DoE approach
title_full Formulation and optimization of liquisolid compact for enhancing dissolution properties of efavirenz by using DoE approach
title_fullStr Formulation and optimization of liquisolid compact for enhancing dissolution properties of efavirenz by using DoE approach
title_full_unstemmed Formulation and optimization of liquisolid compact for enhancing dissolution properties of efavirenz by using DoE approach
title_short Formulation and optimization of liquisolid compact for enhancing dissolution properties of efavirenz by using DoE approach
title_sort formulation and optimization of liquisolid compact for enhancing dissolution properties of efavirenz by using doe approach
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7292870/
https://www.ncbi.nlm.nih.gov/pubmed/32550806
http://dx.doi.org/10.1016/j.jsps.2020.04.016
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