In vitro metabolism of fenofibric acid by carbonyl reducing enzymes
Publication date: 25 October 2016 Source:Chemico-Biological Interactions, Volume 258 Author(s): Petra Malátková, Matthildi Kanavi, Milan Nobilis, Vladimír Wsól Fenofibric acid is a hypolipidemic drug that is used as an active ingredient per se or is administered in the form of fenofibrate that releases fenofibric acid after absorption. The metabolism of fenofibric acid is mediated primarily by glucuronidation. However, the other part of fenofibric acid is excreted as reduced fenofibric acid. Enzymes responsible for the formation of reduced fenofibric acid as well as their subcellular localization have remained un...
Source: Chemico Biological Interactions - September 5, 2016 Category: Biochemistry Source Type: research
In vitro metabolism of fenofibric acid by carbonyl reducing enzymes
Publication date: Available online 4 September 2016 Source:Chemico-Biological Interactions Author(s): Petra Malátková, Matthildi Kanavi, Milan Nobilis, Vladimír Wsól Fenofibric acid is a hypolipidemic drug that is used as an active ingredient per se or is administered in the form of fenofibrate that releases fenofibric acid after absorption. The metabolism of fenofibric acid is mediated primarily by glucuronidation. However, the other part of fenofibric acid is excreted as reduced fenofibric acid. Enzymes responsible for the formation of reduced fenofibric acid as well as their subcellular localization have remai...
Source: Chemico Biological Interactions - September 3, 2016 Category: Biochemistry Source Type: research
Absolute oral bioavailability of fenofibric acid and choline fenofibrate in rats determined by ultra-performance liquid chromatography tandem mass spectrometry.
Abstract
Choline fenofibrate is the choline salt of fenofibric acid, which releasing free fenofibric acid in the gastrointestinal tract. To estimate the absolute oral bioavailability of fenofibric acid and choline fenofibrate, a novel and sensitive UPLC-MS/MS method with liquid-liquid extraction procedure was developed for the determination of fenofibric acid in rat plasma. The separation was achieved on a Phenomenex Kinetex C18 column (50 × 2.1 mm, 2.6 µm) containing 2mM ammonium acetate-methanol with a gradient elution program. Validations of this method including specificity, sensitivity (limit of...
Source: Biomedical Chromatography : BMC - September 3, 2016 Category: Biomedical Science Authors: Wei X, Li P, Liu M, Du Y, Wang M, Zhang J, Wang J, Liu H, Liu X Tags: Biomed Chromatogr Source Type: research
In vitro metabolism of fenofibric acid by carbonyl reducing enzymes.
Abstract
Fenofibric acid is a hypolipidemic drug that is used as an active ingredient per se or is administered in the form of fenofibrate that releases fenofibric acid after absorption. The metabolism of fenofibric acid is mediated primarily by glucuronidation. However, the other part of fenofibric acid is excreted as reduced fenofibric acid. Enzymes responsible for the formation of reduced fenofibric acid as well as their subcellular localization have remained unknown until now. We have found that the predominant site of fenofibric acid reduction is the human liver cytosol, whereas liver microsomes reduc...
Source: Chemico-Biological Interactions - September 2, 2016 Category: Molecular Biology Authors: Malátková P, Kanavi M, Nobilis M, Wsól V Tags: Chem Biol Interact Source Type: research
Analytical methodologies based on LC –MS/MS for monitoring selected emerging compounds in liquid and solid phases of the sewage sludge
Publication date: 2016 Source:MethodsX, Volume 3 Author(s): C. Boix, M. Ibáñez, D. Fabregat-Safont, E. Morales, L. Pastor, J.V. Sancho, J.E. Sánchez-Ramírez, F. Hernández In this work, two analytical methodologies based on liquid chromatography coupled to tandem mass spectrometry (LC–MS/MS) were developed for quantification of emerging pollutants identified in sewage sludge after a previous wide-scope screening. The target list included 13 emerging contaminants (EC): thiabendazole, acesulfame, fenofibric acid, valsartan, irbesartan, salicylic acid, diclofenac, carbamazepine, 4-aminoantipyrine (4-...
Source: MethodsX - July 20, 2016 Category: Science Source Type: research
Fenofibrate improves high-fat diet-induced and palmitate-induced endoplasmic reticulum stress and inflammation in skeletal muscle
Publication date: Available online 11 June 2016 Source:Life Sciences Author(s): Fang Dai, Tian Jiang, Ying-ying Bao, Guan-jun Chen, Li Chen, Qiu Zhang, Yun-xia Lu Aims Fenofibrate (FF) is commonly used clinically as a lipid-lowering drug, but whether it participates in endoplasmic reticulum (ER) stress and decreases inflammation in skeletal muscle is still unknown. The aim of this study is to determine whether FF treatment reduces insulin resistance (IR) by alleviating ER stress and downstream inflammation in skeletal muscle tissues and cells. Main methods Female SD rats were randomly divided into group...
Source: Life Sciences - June 10, 2016 Category: Biology Source Type: research
Comparisons of Pharmacokinetics and NO-releasing of Nitrofibriate and Fenofibrate after Oral Administration in Rats.
This study showed that nitrofibriate, as nitric oxide donor, could slowly release NO in vivo. This study provided biopharmaceutical basis for further study of nitrofibriate. This article is protected by copyright. All rights reserved.
PMID: 27270950 [PubMed - as supplied by publisher] (Source: Biomedical Chromatography : BMC)
Source: Biomedical Chromatography : BMC - June 5, 2016 Category: Biomedical Science Authors: Yang Y, Cheng Q, Liu X, Liu Z, Li T, Jiang X, Wang L Tags: Biomed Chromatogr Source Type: research
Development and Validation of Bioanalytical UHPLC-UV Method for Simultaneous Analysis of Unchanged Fenofibrate and Its Metabolite Fenofibric Acid in Rat Plasma: Application to Pharmacokinetics
Publication date: Available online 26 May 2016 Source:Saudi Pharmaceutical Journal Author(s): Rayan G. Alamri, Kazi Mohsin, Ajaz Ahmad, Mohammad Raish, Fars K. Alanazi A simple, precise, selective and fast ultra-high performance liquid chromatography (UHPLC-UV) method has been developed and validated for the simultaneous determination of a lipid regulating agent fenofibrate and its metabolite fenofibric acid in rat plasma. The chromatographic separation was carried out on a reversed-phase Acquity® BEH C18 column using methanol-water (65:35, v/v) as the mobile phase. The isocratic flow was 0.3 ml/min with rap...
Source: Saudi Pharmaceutical Journal - May 26, 2016 Category: Drugs & Pharmacology Source Type: research
Analytical methodologies based on LC–MS/MS for monitoring selected emerging compounds in liquid and solid phases of the sewage sludge
Publication date: Available online 27 April 2016 Source:MethodsX Author(s): C. Boix, M. Ibáñez, D. Fabregat-Safont, E. Morales, L. Pastor, J.V. Sancho, J.E. Sánchez-Ramírez, F. Hernández In this work, two analytical methodologies based on liquid chromatography coupled to tandem mass spectrometry (LC–MS/MS) were developed for quantification of emerging pollutants identified in sewage sludge after a previous wide-scope screening. The target list included 13 emerging contaminants (EC): thiabendazole, acesulfame, fenofibric acid, valsartan, irbesartan, salicylic acid, diclofenac, carbamazepine, 4-ami...
Source: MethodsX - April 29, 2016 Category: Science Source Type: research
Analytical methodologies based on LC-MS/MS for monitoring selected emerging compounds in liquid and solid phases of the sewage sludge
Publication date: Available online 27 April 2016 Source:MethodsX Author(s): C. Boix, M. Ibáñez, D. Fabregat-Safont, E. Morales, L. Pastor, J.V. Sancho, J.E. Sánchez-Ramírez, F. Hernández In this work, two analytical methodologies based on liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) were developed for quantification of emerging pollutants identified in sewage sludge after a previous wide-scope screening. The target list included 13 emerging contaminants (EC): thiabendazole, acesulfame, fenofibric acid, valsartan, irbesartan, salicylic acid, diclofenac, carbamazepine, 4-amino...
Source: MethodsX - April 27, 2016 Category: Science Source Type: research
Effect of magnesium carbonate on the solubility, dissolution and oral bioavailability of fenofibric acid powder as an alkalising solubilizer.
Abstract
To investigate the possibility of developing a novel oral pharmaceutical product using fenofibric acid instead of choline fenofibrate, the powder properties, solubility, dissolution and pharmacokinetics in rats of fenofibrate, choline fenofibrate and fenofibric acid were compared. Furthermore, the effect of magnesium carbonate, an alkalising agent on the solubility, dissolution and oral bioavailability of fenofibric acid was assessed, a mixture of fenofibric acid and magnesium carbonate being prepared by simple blending at a weight ratio of 2/1. The three fenofibrate derivatives showed different p...
Source: Archives of Pharmacal Research - March 18, 2016 Category: Drugs & Pharmacology Authors: Kim KS, Kim JH, Jin SG, Kim DW, Kim DS, Kim JO, Yong CS, Cho KH, Li DX, Woo JS, Choi HG Tags: Arch Pharm Res Source Type: research
Lack of an Effect of Ritonavir Alone and Lopinavir‐Ritonavir on the Pharmacokinetics of Fenofibric Acid in Healthy Volunteers
ConclusionIn contrast to a significant interaction between gemfibrozil and lopinavir‐ritonavir, neither lopinavir‐ritonavir nor ritonavir alone altered the pharmacokinetics of fenofibric acid in healthy volunteers. These data suggest that fenofibrate remains an important option in human immunodeficiency virus–infected patients receiving common ritonavir‐boosted therapy. (Source: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy)
Source: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy - January 21, 2016 Category: Drugs & Pharmacology Authors: Lori A. Gordon, Christine Y. Malati, Colleen Hadigan, Mary McLaughlin, Raul M. Alfaro, Mónica M. Calderón, Joseph A. Kovacs, Scott R. Penzak Tags: Original Research Article Source Type: research
A review on the rationale and clinical use of concomitant rosuvastatin and fenofibrate/fenofibric acid therapy.
Authors: Strain JD, Farver DK, Clem JR
Abstract
Mixed dyslipidemia, characterized by a lipid triad of elevated triglycerides (TG), elevated low-density lipoprotein-cholesterol (LDL-C) and reduced high-density lipoprotein-cholesterol (HDL-C), is a common and frequently difficult to manage condition. The use of combination medications is often needed to effectively treat the lipid triad. The co-administration of statins and fibrates may provide the desired endpoints but safety issues such as toxicity to the muscles, liver and kidneys are a concern. Given the potency of rosuvastatin to lower LDL-C and fenofib...
Source: Clinical Pharmacology: Advances and Applications - November 29, 2015 Category: Allergy & Immunology Tags: Clin Pharmacol Source Type: research
Development and application of a UPLC-MS/MS method for simultaneous determination of fenofibric acid and berberine in rat plasma: Application to the drug-drug pharmacokinetic interaction study of fenofibrate combined with berberine after oral administration in rats.
This article is protected by copyright. All rights reserved.
PMID: 26577601 [PubMed - as supplied by publisher] (Source: Biomedical Chromatography : BMC)
Source: Biomedical Chromatography : BMC - November 17, 2015 Category: Biomedical Science Authors: Li G, Yang F, Liu M, Su X, Zhao M, Zhao L Tags: Biomed Chromatogr Source Type: research
Nonstatin Therapies for Management of Dyslipidemia: A Review.
Abstract
PURPOSE: Cardiovascular disease (CVD) is the leading cause of morbidity and mortality in the United States. Recently published cholesterol treatment guidelines emphasize the use of statins as the preferred treatment strategy for both primary and secondary prevention of CVD. However, the optimal treatment strategy for patients who cannot tolerate statin therapy or those who need additional lipid-lowering therapy is unclear in light of recent evidence that demonstrates a lack of improved cardiovascular outcomes with combination therapy. The purpose of this review is to summarize and interpret eviden...
Source: Clinical Therapeutics - September 24, 2015 Category: Drugs & Pharmacology Authors: Sando KR, Michelle Knight P Tags: Clin Ther Source Type: research
