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Hollow fiber based liquid phase microextraction with high performance liquid chromatography for the determination of trace carvedilol (β-blocker) in biological fluids

100%

Makahleh A. , Cheng K. W. , Saad B. , Aboul-Enein H. Y.

Acta Chromatographica

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2020

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tom Vol. 32, no. 2

149--155

EN

A hollow-fiber liquid-phase microextraction (HF-LPME), followed by high-performance liquid chromatography–ultraviolet (HPLC–UV) method for the trace determination of carvedilol (β-blocker) in biological fluids, has been described. The separation was achieved using Inertsil ODS-3 C18 (250 mm × 4.6 mm, 3 μm) column with a mobile phase composition of 10 mM phosphate buffer (pH 4.0)–acetonitrile (50:50, v/v) at a flow rate of 1.0 mL/min, under isocratic elution. Several parameters (i.e., type of organic solvent, donor phase pH, concentration of acceptor phase (AP), stirring rate, extraction time, and salt addition) that affect the extraction efficiency were investigated. The optimum HF-LPME conditions were as follows: dihexyl ether as an organic solvent; donor phase pH, 10.7; 0.1 M HCl (AP); 1100-rpm stirring rate; 60-min extraction time; and no salt addition. These parameters have been confirmed using design of experiments. Under these conditions, an enrichment factor of 273-fold was achieved. Good linearity and correlation coefficient were obtained over the range 5–1000 ng/mL (r2 = 0.9994). Limits of detection and quantitation were 1.2 and 3.7 ng/mL, respectively. The relative standard deviation at 3 different concentration levels (5, 500, and 1000 ng/mL) were less than 13.2%. Recoveries for spiked urine and plasma were in the range 80.7–114%. The proposed method is simple, sensitive, and suitable for the determination of carvedilol in biological fluids.

2

Carvedilol and adrenergic agonists suppress the lipopolysaccharide-induced NO production in RAW 264.7 macrophages via the adrenergic receptors

75%

Pekarova M. , Kralova J. , Kubala L. , Ciz M. , Papezikova I. , Macickova T. , Pecivova J. , Nosal R. , Lojek A.

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tom 60

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nr 1

143-150

EN

The interaction of adrenergic agonists and/or antagonists with the adrenergic receptors expressed on immunologically active cells including macrophages plays an important role in regulation of inflammatory responses. Our study investigated the effects of carvedilol, a unique vasodilating b-adrenergic antagonist, and endogenous adrenergic agonists (adrenalin, noradrenalin, and dopamine) and/or antagonists (prazosin, atenolol) on lipopolysaccharide-stimulated nitric oxide (NO) production from murine macrophage cell line RAW 264.7. The production of NO was determined as the concentration of nitrites in cell supernatants (Griess reaction) and inducible nitric oxide synthase (iNOS) protein expression (Western blot analysis). Scavenging properties against NO were measured electrochemically. Carvedilol in a concentration range of 1, 5, 10 and 25 µM inhibited iNOS protein expression and decreased the nitrite concentration in cell supernatants. Adrenalin, noradrenalin or dopamine also inhibited the iNOS protein expression and the nitrite accumulation. Prazosine and atenolol prevented the effect of both carvedilol and adrenergic agonists on nitrite accumulation and iNOS expression in lipopolysaccharide-stimulated cells. These results, together with the absence of scavenging properties of carvedilol against NO, imply that both carvedilol and adrenergic agonists suppress the lipopolysaccharide-evoked NO production by macrophages through the activation and modulation of signaling pathways connected with adrenergic receptors.

3

Effects of cilostazol on the pharmacokinetics of carvedilol after oral and intravenous administration in rats

63%

Lim T. H. , Cho Y. A. , Choi D. H.

Journal of Physiology and Pharmacology

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2015

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tom 66

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nr 4

4

Electrochemical determination of carvedilol, sildenafil and paracetamol using glassy carbon electrode

63%

Baranowska I. , Koper M. , Markowski P.

Chemia Analityczna

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2008

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tom Vol. 53, No. 6

967-981

5

Development of quantitative HPTLC–Densitometry methods for the analysis of amiodarone HCl, carvedilol, doxylamine succinate, magnesium salicylate, metoprolol succinate, nebivolol HCl, and salicylamide using a model process developed earlier for the transfer of TLC screening methods

63%

Nguyen K. , Sherma J.

Acta Chromatographica

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2018

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tom Vol. 30, no. 4

264--268

EN

A model process, previously developed in a series of studies, allows for the transfer of thin-layer chromatography (TLC) methods for qualitative screening of counterfeit drug products published in the Global Pharma Health Fund (GPHF) Minilab manual and US Food and Drug Administration (FDA) Compendium of Unofficial Methods for Screening of Pharmaceuticals by TLC to quantitative high-performance TLC (HPTLC)–densitometry methods. This article describes HPTLC–densitometry methods developed and validated according to this model process for pharmaceutical products of amiodarone HCl, carvedilol, doxylamine succinate, magnesium salicylate, metoprolol succinate, nebivolol HCl, and salicylamide, for which qualitative screening methods have not been published in the Minilab manual or FDA Compendium. These methods use relatively inexpensive and nontoxic “green solvents” for sample and standard solution and mobile phase preparation, Merck Premium Purity silica gel 60 F254 plates, automated standard and sample solution bandwise application, and automated densitometry for the assessment of peak purity and identity and quantification. Corresponding to the quantitative HPTLC–densitometry methods, qualitative TLC screening methods for these drug products were developed and posted online with open access as supplements to the FDA Compendium.

6

Carvedilol modifies antioxidant status of patients with stable angina

51%

Kowalski J. , Banach M. , Barylski M. , Irzmanski R. , Pawlicki L.

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tom 13

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nr 2

230-239

EN

The aim of this study was to evaluate the effect of carvedilol on the enzymatic antioxidative defence and plasma antioxidative activity in patients with stable angina. The study comprised 30 patients, aged 37–49 years with stable angina. Patients received carvedilol in escalating doses of 12.5 mg/24 h, 25 mg/24 h, and 50 mg/24 h for 4 weeks each. The control group was matched for age and gender, and consisted of 12 healthy volunteers, aged 39-49 years. Blood samples were collected from the cubital vein before and 4, 8 and 12 weeks after the therapy from the patients and once from the control group. For all the subjects, the superoxide dismutase (SOD-1), glutathione peroxidase (GSH-Px), catalase (CAT) activities in the erythrocytes and the antioxidant activity of the blood plasma were determined. The enzymatic antioxidative defence was significantly decreased in patients with stable angina in comparison to the healthy subjects. During the carvedilol therapy, an increase in the SOD-1, GSH-Px and CAT activities was observed. Moreover, 8 and 12 weeks after carvedilol therapy, the GSH-Px activity did not differ significantly from that observed in the group of healthy subjects. Carvedilol also increased the plasma antioxidative activity in patients with stable angina, but its level remained significantly lower than in the control group. In conclusion, carvedilol enhances antioxidant defense mechanisms in patients with chronic stable angina pectoris.

7

Carvedilol induces endogenous hydrogen sulfide tissue concentration changes in various mouse organs

51%

Wilinski B. , Wilinski J. , Somogyi E. , Piotrowska J. , Goralska M. , Macura B.

Folia Biologica

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2011

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tom 59

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nr 3-4

8

Effect of carvedilol on neuronal survival and poly[ADP-ribose] polymerase activity in hippocampus after transient forebrain ischemia

51%

Strosznajder R. P. , Jesko H. , Dziewulska J.

Acta Neurobiologiae Experimentalis

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2005

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tom 65

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nr 2