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

机译:1,4-二氢吡啶类降压药:光稳定策略的最新进展

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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.
机译:1,4-二氢吡啶(DHP)药物是当今治疗高血压最常用的药物。但是,该系列中的所有结构都表现出对光的显着敏感性,从而导致药理活性完全丧失。这种降解在水溶液中尤为明显,以至于如此,市场上几乎所有的DHP药物都以固体制剂制成制剂,尤其是片剂。光降解的第一个也是主要的过程是二氢吡啶环的芳构化,之后可以在各种取代基上进行第二步。潜在的危险可能是由于形成单一的氧气和超氧化物类而引起的,而氧气和超氧化物类又会引发光毒性反应。近年来已经提出了几种使DHP药物光稳定的策略,特别是旨在将这些药物配制成液体制剂,并限制与光降解有关的任何毒性问题。这篇综述总结并描述了近年来为获得DHP药物的光稳定制剂而进行的研究的主要方面。

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