UPLC-MS/MS quantification of quercetin in plasma and urine following parenteral administration

Abstract

Background: Study of pharmacokinetics of quercetin (Qu) and its derivatives after infusion is required in order to better understand mechanisms of therapeutic action of the formulation and development the strategic approaches to treat the underlying disease and pathologically similar syndromes. A pharmacokinetic study of Qu products is a complex analytical problem. Results: We developed and validated a new method for quantification of Qu and its metabolites in human plasma and urine following intravenous administration of Qu formulation. The method is based on the solid-phase extraction with the help of Oasis® HLB cartridges and ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) quantification. The calibration curves plotted for concentration range of 25-3000 ng/ml for Qu and isorhamnetin in blood plasma and of 100-8000 ng/ml for the same substances in urine were best described by a quadratic function. Qu conjugates underwent preliminary hydrolysis by the mixture of enzymes of sulphatase and β-glucuronidase. The antioxidant L-cysteine mixed with ascorbic acid was used for stabilization of Qu and its metabolites during handling of samples and chromatographic runs with mass detection. The method validation as well as the stability study results confirmed that the developed method meets the established requirements (selectivity, lower limit of quantification, accuracy, precision, recovery). The main pharmacokinetic parameters of Qu and its metabolites were determined in blood plasma and urine after intravenous administration of Corvitin® (parenteral formulation combining Qu and polyvinylpyrrolidone at a ratio of 1:9) in 12 healthy volunteers. Conclusions: We showed that the method development for Qu quantification in biological matrixes is valuable and reliable.

Evaluation of Antioxidant Activity and Biotransformation of Opuntia Ficus Fruit: The Effect of In Vitro and Ex Vivo Gut Microbiota Metabolism

“…The first detected flavonol was isorhamnetin glycoside in peak 12 with [M-H] − at m/z 541.2307 (C 26 H 38 O 12 ) − , with product ions at m/z 315.13 [M-C 9 H 8 O-H] − corresponding to isorhamnetin aglycone [ 1 ]. Likewise, peaks 17 and 19 were detected with molecular formulas of (C 25 H 24 O 15 ) − and (C 15 H 10 O 7 − ) and a common ion at m/z 301.03, annotated as quercetin aglycone and quercetin glycoside, respectively [ 25 ]. Glycosides denote that the metabolite gave the characteristic product ion of their corresponding aglycone; however, the sugar part was undetermined unequivocally, which is why they were annotated as glycosides in general and not of a specific sugar.…”

Impact of different processing methods on the phenolics and neuroprotective activity of Fragaria ananassa Duch. extracts in a d-galactose and aluminum chloride-induced rat model of aging

“…51 Few metabolites at peaks 16 and 23 showed the characteristic product ion of quercetin at m / z 301 and hence were annotated as quercetin glycosides. 52 Likewise, peak 21 showed a product ion at m / z 315 characteristic of isorhamnetin aglycone and was annotated as isorhamnetin glucuronide. Rutin was detected at peak 36 with [M − H] − at m / z 609.119 (C 27 H 30 O 16 ), producing product ions at m / z 301 [M − C 12 H 20 O 9 − H] − .…”

Розробка Технології Лікування COVID-19-асоційованої Пневмонії Лікарськими Препаратами, Що Містять Флавоноїд Кверцетин

“…Особливо це питання стає актуальним для груп населення, які мають протипоказання до вакцинації. Саме Квертин завдяки особливостям технології виробництва, має переваги у біодоступності серед інших кверцетинвмісних ЛЗ та дієтичних добавок до раціону харчування [29]. Окрім того, нагальним стає питання дослідження ролі кверцетину у лікуванні постковідного синдрому, отже, негативний тест полімеразної ланцюгової реакції не означає повного одужання, а все більше з'являється пацієнтів саме з цим синдромокомплексом, і їх реабілітація триває декілька місяців (>12 тиж, за визначенням National Institute for Health and Care Excellence (NICE), Велика Британія, або >6 міс, на думку фахівців Гарвардської медичної школи).…”