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Pharmaceutics 2019, 11(1), 28; https://doi.org/10.3390/pharmaceutics11010028

A New Generation of Dihydropyridine Calcium Channel Blockers: Photostabilization of Liquid Formulations Using Nonionic Surfactants

1
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy
2
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara 06100, Turkey
*
Author to whom correspondence should be addressed.
Received: 13 December 2018 / Revised: 3 January 2019 / Accepted: 8 January 2019 / Published: 11 January 2019
(This article belongs to the Special Issue Non-Ionic Surfactant Vesicles for Drug Delivery)
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Abstract

The stability profile of a new 1,4-dihydropyridine derivative (DHP), representative of a series with a hexahydroquinoline ring, was studied to design light-stable liquid formulations. This molecule, named M3, has been shown among the analogs to have a high capacity to block both L- and T-type calcium channels. The ethanol solution of the drug was subjected to a photodegradation test, in accordance with standard rules. The concentrations of the drug and its byproducts were estimated using multivariate curve resolution, applied to the spectral data collected during the test. The improvement of both the photostability and water solubility of M3 was investigated by adding the surfactant polysorbate 20 in a 1:5 ratio to aqueous solutions of the drug. These formulations were exposed to stressing light in containers of bleu polyethylene terephthalate (PET), amber PET, and covered amber PET. The best results were obtained when using the covered amber PET container, reaching a degradation percentage of the drug less than 5% after 12 h under an irradiance power of 450 W/m2. The stability of the compound was compared to that of nimodipine (NIM) under the same conditions. View Full-Text
Keywords: 1,4-dihydropyridines; L- and T-type calcium channel blockers; photodegradation test; light-stable formulation; micellar solution; PET containers 1,4-dihydropyridines; L- and T-type calcium channel blockers; photodegradation test; light-stable formulation; micellar solution; PET containers
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Ioele, G.; Gündüz, M.G.; Spatari, C.; De Luca, M.; Grande, F.; Ragno, G. A New Generation of Dihydropyridine Calcium Channel Blockers: Photostabilization of Liquid Formulations Using Nonionic Surfactants. Pharmaceutics 2019, 11, 28.

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