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Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability

Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was developed using sesame and soybean oils along wit...

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Autores principales: Sawatdee, Somchai, Atipairin, Apichart, Sae Yoon, Attawadee, Srichana, Teerapol, Changsan, Narumon, Suwandecha, Tan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6471907/
https://www.ncbi.nlm.nih.gov/pubmed/30897738
http://dx.doi.org/10.3390/pharmaceutics11030134
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author Sawatdee, Somchai
Atipairin, Apichart
Sae Yoon, Attawadee
Srichana, Teerapol
Changsan, Narumon
Suwandecha, Tan
author_facet Sawatdee, Somchai
Atipairin, Apichart
Sae Yoon, Attawadee
Srichana, Teerapol
Changsan, Narumon
Suwandecha, Tan
author_sort Sawatdee, Somchai
collection PubMed
description Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was developed using sesame and soybean oils along with surfactant/co-surfactants, and the tablets were prepared by wet granulation using superdisintegrants and adsorbents. Infra-red (IR) spectral studies revealed no interaction between the drug and excipients, and all physical and chemical parameters were within acceptable limits. Stability studies for the formulation indicated no significant change over time. An in vitro release study indicated 100% drug release within 30 min, and in vivo plasma concentrations indicated that the area under the curve (AUC) of albendazole in rats administered SMEDDS chewable tablets was significantly higher than in those administered commercial tablets or powder (p-value < 0.05). The systemic bioavailability of albendazole achieved through the SMEDDS tablets was 1.3 times higher than that achieved by the administration of comparable quantities of albendazole commercial tablets. This was due to the higher dissolution of albendazole SMEDDS in the chewable tablets. We conclude that the SMEDDS chewable formulation can be used to improve the dissolution and systemic availability of poorly water-soluble drugs.
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spelling pubmed-64719072019-04-27 Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability Sawatdee, Somchai Atipairin, Apichart Sae Yoon, Attawadee Srichana, Teerapol Changsan, Narumon Suwandecha, Tan Pharmaceutics Article Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was developed using sesame and soybean oils along with surfactant/co-surfactants, and the tablets were prepared by wet granulation using superdisintegrants and adsorbents. Infra-red (IR) spectral studies revealed no interaction between the drug and excipients, and all physical and chemical parameters were within acceptable limits. Stability studies for the formulation indicated no significant change over time. An in vitro release study indicated 100% drug release within 30 min, and in vivo plasma concentrations indicated that the area under the curve (AUC) of albendazole in rats administered SMEDDS chewable tablets was significantly higher than in those administered commercial tablets or powder (p-value < 0.05). The systemic bioavailability of albendazole achieved through the SMEDDS tablets was 1.3 times higher than that achieved by the administration of comparable quantities of albendazole commercial tablets. This was due to the higher dissolution of albendazole SMEDDS in the chewable tablets. We conclude that the SMEDDS chewable formulation can be used to improve the dissolution and systemic availability of poorly water-soluble drugs. MDPI 2019-03-20 /pmc/articles/PMC6471907/ /pubmed/30897738 http://dx.doi.org/10.3390/pharmaceutics11030134 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Sawatdee, Somchai
Atipairin, Apichart
Sae Yoon, Attawadee
Srichana, Teerapol
Changsan, Narumon
Suwandecha, Tan
Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title_full Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title_fullStr Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title_full_unstemmed Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title_short Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability
title_sort formulation development of albendazole-loaded self-microemulsifying chewable tablets to enhance dissolution and bioavailability
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6471907/
https://www.ncbi.nlm.nih.gov/pubmed/30897738
http://dx.doi.org/10.3390/pharmaceutics11030134
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