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Preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: Solubility enhancement, taste-masking, and digestive acidic protection

Azithromycin, a macrolide antibiotics, is one of the frequently used drugs in the children and elder. However, due to these population difficulty in swallowing and inefficient absorption, and azithromycin inherent poor solubility, bitter taste, and instability in the stomach acidic condition, it is...

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Autores principales: Huynh, Duyen Thi My, Hai, Huynh Thien, Hau, Nguyen Minh, Lan, Huynh Kim, Vinh, Truong Phu, Tran, Van De, Pham, Duy Toan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10245243/
https://www.ncbi.nlm.nih.gov/pubmed/37292293
http://dx.doi.org/10.1016/j.heliyon.2023.e16592
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author Huynh, Duyen Thi My
Hai, Huynh Thien
Hau, Nguyen Minh
Lan, Huynh Kim
Vinh, Truong Phu
Tran, Van De
Pham, Duy Toan
author_facet Huynh, Duyen Thi My
Hai, Huynh Thien
Hau, Nguyen Minh
Lan, Huynh Kim
Vinh, Truong Phu
Tran, Van De
Pham, Duy Toan
author_sort Huynh, Duyen Thi My
collection PubMed
description Azithromycin, a macrolide antibiotics, is one of the frequently used drugs in the children and elder. However, due to these population difficulty in swallowing and inefficient absorption, and azithromycin inherent poor solubility, bitter taste, and instability in the stomach acidic condition, it is a challenge to reach high oral bioavailability of this drug. To overcome these issues, we developed and characterized the effervescent granules containing azithromycin solid dispersion. Firstly, the solid dispersion was prepared, employing both wet grinding and solvent evaporation methods, with different types/amounts of polymers. The optimal solid dispersion with β-cyclodextrin at a drug:polymer ratio of 1:2 (w/w), prepared by the solvent evaporation method, significantly enhanced the azithromycin solubility 4-fold compared to the free drug, improved its bitterness from “bitter” to “normal”, possessed intermolecular bonding between the drug and polymer, and transformed the azithromycin molecules from crystalline to amorphous state. Secondly, the effervescent granules incorporating the solid dispersion were formulated with varied excipients of sweeteners, gas-generators, pH modulators, and glidants/lubricants. The optimal formula satisfied all the properties stated in the Vietnamese Pharmacopoeia. In summary, the final effervescent granules product could be further investigated in in-vivo and in clinical settings to become a potential azithromycin delivery system with high bioavailability for the children and elder.
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spelling pubmed-102452432023-06-08 Preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: Solubility enhancement, taste-masking, and digestive acidic protection Huynh, Duyen Thi My Hai, Huynh Thien Hau, Nguyen Minh Lan, Huynh Kim Vinh, Truong Phu Tran, Van De Pham, Duy Toan Heliyon Research Article Azithromycin, a macrolide antibiotics, is one of the frequently used drugs in the children and elder. However, due to these population difficulty in swallowing and inefficient absorption, and azithromycin inherent poor solubility, bitter taste, and instability in the stomach acidic condition, it is a challenge to reach high oral bioavailability of this drug. To overcome these issues, we developed and characterized the effervescent granules containing azithromycin solid dispersion. Firstly, the solid dispersion was prepared, employing both wet grinding and solvent evaporation methods, with different types/amounts of polymers. The optimal solid dispersion with β-cyclodextrin at a drug:polymer ratio of 1:2 (w/w), prepared by the solvent evaporation method, significantly enhanced the azithromycin solubility 4-fold compared to the free drug, improved its bitterness from “bitter” to “normal”, possessed intermolecular bonding between the drug and polymer, and transformed the azithromycin molecules from crystalline to amorphous state. Secondly, the effervescent granules incorporating the solid dispersion were formulated with varied excipients of sweeteners, gas-generators, pH modulators, and glidants/lubricants. The optimal formula satisfied all the properties stated in the Vietnamese Pharmacopoeia. In summary, the final effervescent granules product could be further investigated in in-vivo and in clinical settings to become a potential azithromycin delivery system with high bioavailability for the children and elder. Elsevier 2023-05-26 /pmc/articles/PMC10245243/ /pubmed/37292293 http://dx.doi.org/10.1016/j.heliyon.2023.e16592 Text en © 2023 The Authors https://creativecommons.org/licenses/by/4.0/This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Research Article
Huynh, Duyen Thi My
Hai, Huynh Thien
Hau, Nguyen Minh
Lan, Huynh Kim
Vinh, Truong Phu
Tran, Van De
Pham, Duy Toan
Preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: Solubility enhancement, taste-masking, and digestive acidic protection
title Preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: Solubility enhancement, taste-masking, and digestive acidic protection
title_full Preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: Solubility enhancement, taste-masking, and digestive acidic protection
title_fullStr Preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: Solubility enhancement, taste-masking, and digestive acidic protection
title_full_unstemmed Preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: Solubility enhancement, taste-masking, and digestive acidic protection
title_short Preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: Solubility enhancement, taste-masking, and digestive acidic protection
title_sort preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: solubility enhancement, taste-masking, and digestive acidic protection
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10245243/
https://www.ncbi.nlm.nih.gov/pubmed/37292293
http://dx.doi.org/10.1016/j.heliyon.2023.e16592
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