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1,4-Dihydropyridine Antihypertensive Drugs: Recent Advances in Photostabilization Strategies

The 1,4-dihydropyridine (DHP) drugs are nowadays the most used drugs in the treatment of hypertension. However, all the structures in this series present a significant sensitivity to light, leading to the complete loss of pharmacological activity. This degradation is particularly evident in aqueous...

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Detalles Bibliográficos
Autores principales: De Luca, Michele, Ioele, Giuseppina, Ragno, Gaetano
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6409574/
https://www.ncbi.nlm.nih.gov/pubmed/30781584
http://dx.doi.org/10.3390/pharmaceutics11020085
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author De Luca, Michele
Ioele, Giuseppina
Ragno, Gaetano
author_facet De Luca, Michele
Ioele, Giuseppina
Ragno, Gaetano
author_sort De Luca, Michele
collection PubMed
description The 1,4-dihydropyridine (DHP) drugs are nowadays the most used drugs in the treatment of hypertension. However, all the structures in this series present a significant sensitivity to light, leading to the complete loss of pharmacological activity. This degradation is particularly evident in aqueous solution, so much so that almost all DHP drugs on the market are formulated in solid preparations, especially tablets. The first and main process of photodegradation consists in the aromatization of the dihydropyridine ring, after which secondary processes can take place on the various substituents. A potential danger can result from the formation of single oxygen and superoxide species that can in turn trigger phototoxic reactions. Several strategies for the photostabilisation of DHP drugs have been proposed in recent years, in particular with the aim to formulate these drugs in liquid preparations, as well as to limit any toxicity problems related to light degradation. This review summarizes and describes the main aspects of the studies conducted in recent years to obtain photostable formulations of DHP drugs.
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spelling pubmed-64095742019-03-29 1,4-Dihydropyridine Antihypertensive Drugs: Recent Advances in Photostabilization Strategies De Luca, Michele Ioele, Giuseppina Ragno, Gaetano Pharmaceutics Review The 1,4-dihydropyridine (DHP) drugs are nowadays the most used drugs in the treatment of hypertension. However, all the structures in this series present a significant sensitivity to light, leading to the complete loss of pharmacological activity. This degradation is particularly evident in aqueous solution, so much so that almost all DHP drugs on the market are formulated in solid preparations, especially tablets. The first and main process of photodegradation consists in the aromatization of the dihydropyridine ring, after which secondary processes can take place on the various substituents. A potential danger can result from the formation of single oxygen and superoxide species that can in turn trigger phototoxic reactions. Several strategies for the photostabilisation of DHP drugs have been proposed in recent years, in particular with the aim to formulate these drugs in liquid preparations, as well as to limit any toxicity problems related to light degradation. This review summarizes and describes the main aspects of the studies conducted in recent years to obtain photostable formulations of DHP drugs. MDPI 2019-02-17 /pmc/articles/PMC6409574/ /pubmed/30781584 http://dx.doi.org/10.3390/pharmaceutics11020085 Text en © 2019 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
De Luca, Michele
Ioele, Giuseppina
Ragno, Gaetano
1,4-Dihydropyridine Antihypertensive Drugs: Recent Advances in Photostabilization Strategies
title 1,4-Dihydropyridine Antihypertensive Drugs: Recent Advances in Photostabilization Strategies
title_full 1,4-Dihydropyridine Antihypertensive Drugs: Recent Advances in Photostabilization Strategies
title_fullStr 1,4-Dihydropyridine Antihypertensive Drugs: Recent Advances in Photostabilization Strategies
title_full_unstemmed 1,4-Dihydropyridine Antihypertensive Drugs: Recent Advances in Photostabilization Strategies
title_short 1,4-Dihydropyridine Antihypertensive Drugs: Recent Advances in Photostabilization Strategies
title_sort 1,4-dihydropyridine antihypertensive drugs: recent advances in photostabilization strategies
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6409574/
https://www.ncbi.nlm.nih.gov/pubmed/30781584
http://dx.doi.org/10.3390/pharmaceutics11020085
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