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Metformin-NSAIDs Molecular Salts: A Path towards Enhanced Oral Bioavailability and Stability

According to the World Health Organization, more than 422 million people worldwide have diabetes. The most common oral treatment for type 2 diabetes is the drug metformin (MTF), which is usually formulated as a hydrochloride to achieve higher water solubility. However, this drug is also highly hygro...

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Autores principales: Acebedo-Martínez, Francisco Javier, Domínguez-Martín, Alicia, Alarcón-Payer, Carolina, Garcés-Bastida, Carolina, Verdugo-Escamilla, Cristóbal, Gómez-Morales, Jaime, Choquesillo-Lazarte, Duane
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9966766/
https://www.ncbi.nlm.nih.gov/pubmed/36839770
http://dx.doi.org/10.3390/pharmaceutics15020449
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author Acebedo-Martínez, Francisco Javier
Domínguez-Martín, Alicia
Alarcón-Payer, Carolina
Garcés-Bastida, Carolina
Verdugo-Escamilla, Cristóbal
Gómez-Morales, Jaime
Choquesillo-Lazarte, Duane
author_facet Acebedo-Martínez, Francisco Javier
Domínguez-Martín, Alicia
Alarcón-Payer, Carolina
Garcés-Bastida, Carolina
Verdugo-Escamilla, Cristóbal
Gómez-Morales, Jaime
Choquesillo-Lazarte, Duane
author_sort Acebedo-Martínez, Francisco Javier
collection PubMed
description According to the World Health Organization, more than 422 million people worldwide have diabetes. The most common oral treatment for type 2 diabetes is the drug metformin (MTF), which is usually formulated as a hydrochloride to achieve higher water solubility. However, this drug is also highly hygroscopic, thus showing stability problems. Another kind of worldwide prescribed drug is the non-steroidal anti-inflammatory drug (NSAID). These latter, on the contrary, show a low solubility profile; therefore, they must be administered at high doses, which increases the probability of secondary effects. In this work, novel drug-drug pharmaceutical solids combining MTF-NSAIDs have been synthesized in solution or by mechanochemical methods. The aim of this concomitant treatment is to improve the physicochemical properties of the parent active pharmaceutical ingredients. After a careful solid-state characterization along with solubility and stability studies, it can be concluded that the new molecular salt formulations enhance not only the stability of MTF but also the solubility of NSAIDs, thus giving promising results regarding the development of these novel pharmaceutical multicomponent solids.
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spelling pubmed-99667662023-02-26 Metformin-NSAIDs Molecular Salts: A Path towards Enhanced Oral Bioavailability and Stability Acebedo-Martínez, Francisco Javier Domínguez-Martín, Alicia Alarcón-Payer, Carolina Garcés-Bastida, Carolina Verdugo-Escamilla, Cristóbal Gómez-Morales, Jaime Choquesillo-Lazarte, Duane Pharmaceutics Article According to the World Health Organization, more than 422 million people worldwide have diabetes. The most common oral treatment for type 2 diabetes is the drug metformin (MTF), which is usually formulated as a hydrochloride to achieve higher water solubility. However, this drug is also highly hygroscopic, thus showing stability problems. Another kind of worldwide prescribed drug is the non-steroidal anti-inflammatory drug (NSAID). These latter, on the contrary, show a low solubility profile; therefore, they must be administered at high doses, which increases the probability of secondary effects. In this work, novel drug-drug pharmaceutical solids combining MTF-NSAIDs have been synthesized in solution or by mechanochemical methods. The aim of this concomitant treatment is to improve the physicochemical properties of the parent active pharmaceutical ingredients. After a careful solid-state characterization along with solubility and stability studies, it can be concluded that the new molecular salt formulations enhance not only the stability of MTF but also the solubility of NSAIDs, thus giving promising results regarding the development of these novel pharmaceutical multicomponent solids. MDPI 2023-01-29 /pmc/articles/PMC9966766/ /pubmed/36839770 http://dx.doi.org/10.3390/pharmaceutics15020449 Text en © 2023 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
Acebedo-Martínez, Francisco Javier
Domínguez-Martín, Alicia
Alarcón-Payer, Carolina
Garcés-Bastida, Carolina
Verdugo-Escamilla, Cristóbal
Gómez-Morales, Jaime
Choquesillo-Lazarte, Duane
Metformin-NSAIDs Molecular Salts: A Path towards Enhanced Oral Bioavailability and Stability
title Metformin-NSAIDs Molecular Salts: A Path towards Enhanced Oral Bioavailability and Stability
title_full Metformin-NSAIDs Molecular Salts: A Path towards Enhanced Oral Bioavailability and Stability
title_fullStr Metformin-NSAIDs Molecular Salts: A Path towards Enhanced Oral Bioavailability and Stability
title_full_unstemmed Metformin-NSAIDs Molecular Salts: A Path towards Enhanced Oral Bioavailability and Stability
title_short Metformin-NSAIDs Molecular Salts: A Path towards Enhanced Oral Bioavailability and Stability
title_sort metformin-nsaids molecular salts: a path towards enhanced oral bioavailability and stability
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9966766/
https://www.ncbi.nlm.nih.gov/pubmed/36839770
http://dx.doi.org/10.3390/pharmaceutics15020449
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