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Formulation of Modified-Release Bilayer Tablets of Atorvastatin and Ezetimibe: An In-Vitro and In-Vivo Analysis
The objective of this work was to formulate co-loaded bilayer tablets containing ezetimibe (EZB) and atorvastatin (ATC). ATC loaded in the immediate-release (IR) layer is an HMG CoA reductase inhibitor, while EZB, added in the sustained-release (SR) layer, is a lipid-lowering agent. This study was c...
Autores principales: | , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9506081/ https://www.ncbi.nlm.nih.gov/pubmed/36145914 http://dx.doi.org/10.3390/polym14183770 |
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author | Mubeen, Iqra Zaman, Muhammad Farooq, Muhammad Mehmood, Asim Azeez, Fahad Khan Rehman, Wajiha Akhtar, Sohail Chaudhry, Mueen Ahmad Butt, Muhammad Hammad Shamim, Qurat-ul-ain Adnan, Sherjeel Khan, Muhammad Rizwan Atta-ur-Rehman, |
author_facet | Mubeen, Iqra Zaman, Muhammad Farooq, Muhammad Mehmood, Asim Azeez, Fahad Khan Rehman, Wajiha Akhtar, Sohail Chaudhry, Mueen Ahmad Butt, Muhammad Hammad Shamim, Qurat-ul-ain Adnan, Sherjeel Khan, Muhammad Rizwan Atta-ur-Rehman, |
author_sort | Mubeen, Iqra |
collection | PubMed |
description | The objective of this work was to formulate co-loaded bilayer tablets containing ezetimibe (EZB) and atorvastatin (ATC). ATC loaded in the immediate-release (IR) layer is an HMG CoA reductase inhibitor, while EZB, added in the sustained-release (SR) layer, is a lipid-lowering agent. This study was conducted to evaluate the effects of polymer on the formulation and characterization of bilayer tablets, as well as the therapeutic impact of the concurrent use of both drugs having a sequential release pattern. To obtain the optimized results, four different formulations with variable compositions were developed and evaluated for different parameters. The drug release studies were carried out using a type II dissolution apparatus, using phosphate buffer solution (PBS) of 1.2 pH for IR of EZB for an initial 2 h, followed by 24 h studies for ATC in PBS 6.8 pH. The IR layer showed rapid drug release (96%) in 2 h, while 80% of the ATC was released in 24 h from the SR layer. Locally obtained, 6-week-old female albino rats were selected for in vivo studies. Both preventive and curative models were applied to check the effects of the drug combination on the lipid profile, atherosclerosis and physiology of different organs. Studies have shown that the administration of both drugs with different release patterns has a better therapeutic effect (p < 0.05), both in preventing and in curing hyperlipidemia. Conclusively, through the sequential release of ATC and EZB, a better therapeutic response could be obtained. |
format | Online Article Text |
id | pubmed-9506081 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-95060812022-09-24 Formulation of Modified-Release Bilayer Tablets of Atorvastatin and Ezetimibe: An In-Vitro and In-Vivo Analysis Mubeen, Iqra Zaman, Muhammad Farooq, Muhammad Mehmood, Asim Azeez, Fahad Khan Rehman, Wajiha Akhtar, Sohail Chaudhry, Mueen Ahmad Butt, Muhammad Hammad Shamim, Qurat-ul-ain Adnan, Sherjeel Khan, Muhammad Rizwan Atta-ur-Rehman, Polymers (Basel) Article The objective of this work was to formulate co-loaded bilayer tablets containing ezetimibe (EZB) and atorvastatin (ATC). ATC loaded in the immediate-release (IR) layer is an HMG CoA reductase inhibitor, while EZB, added in the sustained-release (SR) layer, is a lipid-lowering agent. This study was conducted to evaluate the effects of polymer on the formulation and characterization of bilayer tablets, as well as the therapeutic impact of the concurrent use of both drugs having a sequential release pattern. To obtain the optimized results, four different formulations with variable compositions were developed and evaluated for different parameters. The drug release studies were carried out using a type II dissolution apparatus, using phosphate buffer solution (PBS) of 1.2 pH for IR of EZB for an initial 2 h, followed by 24 h studies for ATC in PBS 6.8 pH. The IR layer showed rapid drug release (96%) in 2 h, while 80% of the ATC was released in 24 h from the SR layer. Locally obtained, 6-week-old female albino rats were selected for in vivo studies. Both preventive and curative models were applied to check the effects of the drug combination on the lipid profile, atherosclerosis and physiology of different organs. Studies have shown that the administration of both drugs with different release patterns has a better therapeutic effect (p < 0.05), both in preventing and in curing hyperlipidemia. Conclusively, through the sequential release of ATC and EZB, a better therapeutic response could be obtained. MDPI 2022-09-09 /pmc/articles/PMC9506081/ /pubmed/36145914 http://dx.doi.org/10.3390/polym14183770 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Mubeen, Iqra Zaman, Muhammad Farooq, Muhammad Mehmood, Asim Azeez, Fahad Khan Rehman, Wajiha Akhtar, Sohail Chaudhry, Mueen Ahmad Butt, Muhammad Hammad Shamim, Qurat-ul-ain Adnan, Sherjeel Khan, Muhammad Rizwan Atta-ur-Rehman, Formulation of Modified-Release Bilayer Tablets of Atorvastatin and Ezetimibe: An In-Vitro and In-Vivo Analysis |
title | Formulation of Modified-Release Bilayer Tablets of Atorvastatin and Ezetimibe: An In-Vitro and In-Vivo Analysis |
title_full | Formulation of Modified-Release Bilayer Tablets of Atorvastatin and Ezetimibe: An In-Vitro and In-Vivo Analysis |
title_fullStr | Formulation of Modified-Release Bilayer Tablets of Atorvastatin and Ezetimibe: An In-Vitro and In-Vivo Analysis |
title_full_unstemmed | Formulation of Modified-Release Bilayer Tablets of Atorvastatin and Ezetimibe: An In-Vitro and In-Vivo Analysis |
title_short | Formulation of Modified-Release Bilayer Tablets of Atorvastatin and Ezetimibe: An In-Vitro and In-Vivo Analysis |
title_sort | formulation of modified-release bilayer tablets of atorvastatin and ezetimibe: an in-vitro and in-vivo analysis |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9506081/ https://www.ncbi.nlm.nih.gov/pubmed/36145914 http://dx.doi.org/10.3390/polym14183770 |
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