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Photodegradation of the
H1 antihistaminics
topical formulations
photodegradation kinetics
photodegradation pathways
phototoxicity
reactive oxygen species
In this study, important H1 antihistaminic drugs, i.e., emedastine (EME), epinastine (EPI), and ketotifen (KET), were irradiated with UV/Vis light (300–800 nm) in solutions of different pH values. Next, they were analyzed by new high performance liquid chromatography (HPLC) methods, in order to estimate the percentage of degradation and respective kinetics. Subsequently, ultra-performance liquid chromatography tandem-mass spectrometry (UPLC-MS/MS) was used to identify their photodegradation products and to propose degradation pathways. In addition, the peroxidation of linoleic acid and generation of singlet oxygen (SO) and superoxide anion (SA) were examined, together with the molar extinction coeffcient (MEC) evaluation, to estimate their phototoxic risk. The photodegradation of all EME, EPI, and KET followed pseudo first-order kinetics. At pH values of 7.0 and 10.0, EPI was shown to be rather stable. However, its photostability was lower at pH 3.0. EME was shown to be photolabile in the whole range of pH values. In turn, KET was shown to be moderately labile at pH 3.0 and 7.0. However, it degraded completely in the buffer of pH 10.0. As a result, several photodegradation products were separated and identified using the UPLC-MS/MS method. Finally, our ROS assays showed a potent phototoxic risk in the following drug order: EPI < EME < KET. All of these results may be helpful for manufacturing, storing, and applying these substantial drugs, especially in their ocular formulations.
cris.lastimport.scopus | 2024-04-07T15:38:02Z | |
dc.abstract.en | In this study, important H1 antihistaminic drugs, i.e., emedastine (EME), epinastine (EPI), and ketotifen (KET), were irradiated with UV/Vis light (300–800 nm) in solutions of different pH values. Next, they were analyzed by new high performance liquid chromatography (HPLC) methods, in order to estimate the percentage of degradation and respective kinetics. Subsequently, ultra-performance liquid chromatography tandem-mass spectrometry (UPLC-MS/MS) was used to identify their photodegradation products and to propose degradation pathways. In addition, the peroxidation of linoleic acid and generation of singlet oxygen (SO) and superoxide anion (SA) were examined, together with the molar extinction coeffcient (MEC) evaluation, to estimate their phototoxic risk. The photodegradation of all EME, EPI, and KET followed pseudo first-order kinetics. At pH values of 7.0 and 10.0, EPI was shown to be rather stable. However, its photostability was lower at pH 3.0. EME was shown to be photolabile in the whole range of pH values. In turn, KET was shown to be moderately labile at pH 3.0 and 7.0. However, it degraded completely in the buffer of pH 10.0. As a result, several photodegradation products were separated and identified using the UPLC-MS/MS method. Finally, our ROS assays showed a potent phototoxic risk in the following drug order: EPI < EME < KET. All of these results may be helpful for manufacturing, storing, and applying these substantial drugs, especially in their ocular formulations. | pl |
dc.affiliation | Wydział Farmaceutyczny : Zakład Chemii Analitycznej | pl |
dc.affiliation | Wydział Farmaceutyczny : Zakład Chemii Leków | pl |
dc.cm.date | 2020-12-02 | |
dc.cm.id | 100047 | |
dc.contributor.author | Gumieniczek, Anna | pl |
dc.contributor.author | Berecka-Rycerz, Anna | pl |
dc.contributor.author | Hubicka, Urszula - 129734 | pl |
dc.contributor.author | Żmudzki, Paweł - 214411 | pl |
dc.contributor.author | Lejwoda, Karolina | pl |
dc.contributor.author | Kozyra, Paweł | pl |
dc.date.accession | 2020-07-16 | pl |
dc.date.accessioned | 2020-12-02T10:30:40Z | pl |
dc.date.available | 2020-12-02T10:30:40Z | pl |
dc.date.issued | 2020 | pl |
dc.date.openaccess | 0 | |
dc.description.accesstime | w momencie opublikowania | |
dc.description.number | 6 | pl |
dc.description.points | 100 | pl |
dc.description.version | ostateczna wersja wydawcy | |
dc.description.volume | 12 | pl |
dc.identifier.articleid | 560 | pl |
dc.identifier.doi | 10.3390/pharmaceutics12060560 | pl |
dc.identifier.eissn | 1999-4923 | pl |
dc.identifier.project | ROD UJ / OP | pl |
dc.identifier.uri | https://ruj.uj.edu.pl/xmlui/handle/item/257909 | |
dc.identifier.weblink | https://www.mdpi.com/1999-4923/12/6/560 | pl |
dc.language | eng | pl |
dc.language.container | eng | pl |
dc.rights | Udzielam licencji. Uznanie autorstwa 4.0 Międzynarodowa | * |
dc.rights.licence | CC-BY | |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/legalcode.pl | * |
dc.share.type | otwarte czasopismo | |
dc.subject.en | H1 antihistaminics | pl |
dc.subject.en | topical formulations | pl |
dc.subject.en | photodegradation kinetics | pl |
dc.subject.en | photodegradation pathways | pl |
dc.subject.en | phototoxicity | pl |
dc.subject.en | reactive oxygen species | pl |
dc.subtype | Article | pl |
dc.title | Photodegradation of the $H^{1}$ antihistaminic topical drugs emedastine, epinastine, and ketotifen and ROS tests for estimations of their potent phototoxicity | pl |
dc.title.journal | Pharmaceutics | pl |
dc.type | JournalArticle | pl |
dspace.entity.type | Publication |
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