Abstract
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.
Highlights
The first of the 1,4-dihydropyridine (DHP) drugs, nifedipine, was synthesized in 1969 and approved by the Food and Drug Administration (FDA) in 1981
They are characterized by a long receptor half-life, due to the ability to rapidly abandon the blood flow to pass into the vessel wall, where they interact with the calcium channels
Some previously published papers refer to pioneering studies on the topic or are still today the only studies dedicated to the photostabilization of some DHP drugs
Summary
The first of the 1,4-dihydropyridine (DHP) drugs, nifedipine, was synthesized in 1969 and approved by the Food and Drug Administration (FDA) in 1981. DHP drugs have established themselves as the most prescribed antihypertensives [1] The drugs for this pathology are currently classified as DHP and non-DHP derivatives, including among these the verapamil and diltiazem congeners [2], mainly used as antiarrhythmics [3,4,5]. The most used DHP drugs are those of the third generation, including amlodipine, barnidipine, lacidipine, lercanidipine, and manidipine. They are characterized by a long receptor half-life, due to the ability to rapidly abandon the blood flow to pass into the vessel wall, where they interact with the calcium channels. Some previously published papers refer to pioneering studies on the topic or are still today the only studies dedicated to the photostabilization of some DHP drugs
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
