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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| Format: | Article |
| Language: | English |
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Elsevier
2023-06-01
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| Series: | Heliyon |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2405844023037994 |
| _version_ | 1797814380415418368 |
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| author | Duyen Thi My Huynh Huynh Thien Hai Nguyen Minh Hau Huynh Kim Lan Truong Phu Vinh Van De Tran Duy Toan Pham |
| author_facet | Duyen Thi My Huynh Huynh Thien Hai Nguyen Minh Hau Huynh Kim Lan Truong Phu Vinh Van De Tran Duy Toan Pham |
| author_sort | Duyen Thi My Huynh |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-03-13T08:06:50Z |
| format | Article |
| id | doaj.art-f88bd2d5c4614f7ab907a34df5e24875 |
| institution | Directory Open Access Journal |
| issn | 2405-8440 |
| language | English |
| last_indexed | 2024-03-13T08:06:50Z |
| publishDate | 2023-06-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Heliyon |
| spelling | doaj.art-f88bd2d5c4614f7ab907a34df5e248752023-06-01T04:36:34ZengElsevierHeliyon2405-84402023-06-0196e16592Preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: Solubility enhancement, taste-masking, and digestive acidic protectionDuyen Thi My Huynh0Huynh Thien Hai1Nguyen Minh Hau2Huynh Kim Lan3Truong Phu Vinh4Van De Tran5Duy Toan Pham6Department of Pharmaceutical and Pharmaceutical Technology, Faculty of Pharmacy, Can Tho University of Medicine and Pharmacy, Can Tho, 900000, Viet NamFaculty of Pharmacy, Can Tho University of Medicine and Pharmacy, Can Tho, 900000, Viet Nam; Corresponding author.Faculty of Pharmacy, Can Tho University of Medicine and Pharmacy, Can Tho, 900000, Viet NamFaculty of Pharmacy, Can Tho University of Medicine and Pharmacy, Can Tho, 900000, Viet NamFaculty of Pharmacy, Can Tho University of Medicine and Pharmacy, Can Tho, 900000, Viet NamDepartment of Health Organization and Management, Can Tho University of Medicine and Pharmacy, Can Tho, 900000, Viet NamDepartment of Chemistry, College of Natural Sciences, Can Tho University, Can Tho, 900000, Viet Nam; Corresponding author.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.http://www.sciencedirect.com/science/article/pii/S2405844023037994AzithromycinSolid dispersionEffervescentBitterSolubility |
| spellingShingle | Duyen Thi My Huynh Huynh Thien Hai Nguyen Minh Hau Huynh Kim Lan Truong Phu Vinh Van De Tran Duy Toan Pham Preparations and characterizations of effervescent granules containing azithromycin solid dispersion for children and elder: Solubility enhancement, taste-masking, and digestive acidic protection Heliyon Azithromycin Solid dispersion Effervescent Bitter Solubility |
| 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 | Azithromycin Solid dispersion Effervescent Bitter Solubility |
| url | http://www.sciencedirect.com/science/article/pii/S2405844023037994 |
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