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Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology
Tolmetin sodium (TLM) is a non-steroidal anti-inflammatory drug (NSAIDs). TLM is used to treat inflammation, skeletal muscle injuries, and discomfort associated with bone disorders. Because of the delayed absorption from the gastro intestinal tract (GIT), the currently available TLM dosage forms hav...
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/PMC9027483/ https://www.ncbi.nlm.nih.gov/pubmed/35456714 http://dx.doi.org/10.3390/pharmaceutics14040880 |
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author | Elsayed, Mahmoud M. A. Aboelez, Moustafa O. Elsadek, Bakheet E. M. Sarhan, Hatem A. Khaled, Khaled Ali Belal, Amany Khames, Ahmed Hassan, Yasser A. Abdel-Rheem, Amany A. Elkaeed, Eslam B. Raafat, Mohamed Elsadek, Mahmoud Elkot Mostafa |
author_facet | Elsayed, Mahmoud M. A. Aboelez, Moustafa O. Elsadek, Bakheet E. M. Sarhan, Hatem A. Khaled, Khaled Ali Belal, Amany Khames, Ahmed Hassan, Yasser A. Abdel-Rheem, Amany A. Elkaeed, Eslam B. Raafat, Mohamed Elsadek, Mahmoud Elkot Mostafa |
author_sort | Elsayed, Mahmoud M. A. |
collection | PubMed |
description | Tolmetin sodium (TLM) is a non-steroidal anti-inflammatory drug (NSAIDs). TLM is used to treat inflammation, skeletal muscle injuries, and discomfort associated with bone disorders. Because of the delayed absorption from the gastro intestinal tract (GIT), the currently available TLM dosage forms have a rather protracted start to the effect, according to pharmacokinetic studies. The aim of this study was to create a combination for TLM fast dissolving tablets (TLM-FDT) that would boost the drug’s bioavailability by increasing pre-gastric absorption. The TLM-FDTs were developed using a Box-Behnken experimental design with varied doses of crospovidone (CP), croscarmellose sodium (CCS) as super-disintegrants, and camphor as a sublimating agent. In addition, the current study used response surface approach to explore the influence of various formulation and process factors on tablet qualities in order to verify an optimized TLM-FDTs formulation. The optimized TLM-FDTs formula was subsequently evaluated for its in vivo anti-inflammatory activity. TLM-FDTs have good friability, disintegration time, drug release, and wetting time, as well as fast disintegration and dissolution behavior. Significant increase in drug bioavailability and reliable anti-inflammatory efficacy were also observed, as evidenced by considerable reductions in paw thickness in rats following carrageenan-induced rat paw edema. For optimizing and analyzing the effect of super-disintegrants and sublimating agents in the TLM-FDTs formula, the three-factor, three-level full factorial design is a suitable tool. TLM-FDTs are a possible drug delivery system for enhancing TLM bioavailability and could be used to treat rheumatoid arthritis. |
format | Online Article Text |
id | pubmed-9027483 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-90274832022-04-23 Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology Elsayed, Mahmoud M. A. Aboelez, Moustafa O. Elsadek, Bakheet E. M. Sarhan, Hatem A. Khaled, Khaled Ali Belal, Amany Khames, Ahmed Hassan, Yasser A. Abdel-Rheem, Amany A. Elkaeed, Eslam B. Raafat, Mohamed Elsadek, Mahmoud Elkot Mostafa Pharmaceutics Article Tolmetin sodium (TLM) is a non-steroidal anti-inflammatory drug (NSAIDs). TLM is used to treat inflammation, skeletal muscle injuries, and discomfort associated with bone disorders. Because of the delayed absorption from the gastro intestinal tract (GIT), the currently available TLM dosage forms have a rather protracted start to the effect, according to pharmacokinetic studies. The aim of this study was to create a combination for TLM fast dissolving tablets (TLM-FDT) that would boost the drug’s bioavailability by increasing pre-gastric absorption. The TLM-FDTs were developed using a Box-Behnken experimental design with varied doses of crospovidone (CP), croscarmellose sodium (CCS) as super-disintegrants, and camphor as a sublimating agent. In addition, the current study used response surface approach to explore the influence of various formulation and process factors on tablet qualities in order to verify an optimized TLM-FDTs formulation. The optimized TLM-FDTs formula was subsequently evaluated for its in vivo anti-inflammatory activity. TLM-FDTs have good friability, disintegration time, drug release, and wetting time, as well as fast disintegration and dissolution behavior. Significant increase in drug bioavailability and reliable anti-inflammatory efficacy were also observed, as evidenced by considerable reductions in paw thickness in rats following carrageenan-induced rat paw edema. For optimizing and analyzing the effect of super-disintegrants and sublimating agents in the TLM-FDTs formula, the three-factor, three-level full factorial design is a suitable tool. TLM-FDTs are a possible drug delivery system for enhancing TLM bioavailability and could be used to treat rheumatoid arthritis. MDPI 2022-04-18 /pmc/articles/PMC9027483/ /pubmed/35456714 http://dx.doi.org/10.3390/pharmaceutics14040880 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 Elsayed, Mahmoud M. A. Aboelez, Moustafa O. Elsadek, Bakheet E. M. Sarhan, Hatem A. Khaled, Khaled Ali Belal, Amany Khames, Ahmed Hassan, Yasser A. Abdel-Rheem, Amany A. Elkaeed, Eslam B. Raafat, Mohamed Elsadek, Mahmoud Elkot Mostafa Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology |
title | Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology |
title_full | Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology |
title_fullStr | Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology |
title_full_unstemmed | Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology |
title_short | Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology |
title_sort | tolmetin sodium fast dissolving tablets for rheumatoid arthritis treatment: preparation and optimization using box-behnken design and response surface methodology |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9027483/ https://www.ncbi.nlm.nih.gov/pubmed/35456714 http://dx.doi.org/10.3390/pharmaceutics14040880 |
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