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Chinese Medical Journal 2010年第17期123卷 2471-2474页

作者： GAO Ling-gen YAO Xiu-ping ZHANG Lin WEN Dan LUO Fang ZHOU Xian-liang HUI Ru-tai Department of Cardiology Fu Wai Hospital and Cardiovascular Institute Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100037 China Sino-German Laboratory for Molecular Medicine Key Laboratory for Clinical Cardiovascular Genetics Ministry of Education Fu Wai Hospital and Cardiovascular Institute Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100037 China Very Important Person Health Care Department The General Hospital of Chinese People's Armed Police Forces Beijing 100039 China

Heart failure is currently one of the most common and most cost-intensive of the chronic diseases The main cause of chronic heart failure （CHF） is the abnormalities of both cardiac contractile performance and myocardial energy metabolism. Elevated levels of reactive oxygen species （ROS） have been proposed to contribute to both of them. Xanthine oxidoreductase （XO） is a major source of ROS in the cardiovascular system. XO inhibitors （XOIs） have been the cornerstone of the clinical management of gout and conditions associated with hyperuricemia for several decades.

关键词： febuxostat reactive oxygen species xanthine oxidase inhibitors chronic heart failure signaling pathways

Characteristic dysbiosis in gout and the impact of a uric acid-lowering treatment,febuxostat on the gut microbiota

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Journal of Genetics and Genomics 2021年第9期48卷 781-791页

作者： Suxian Lin Tao Zhang Lingxiao Zhu Kun Pang Saisai Lu Xin Liao Senhong Ying Lixia Zhu Xin Xu Jinyu Wu Xiaobing Wang Rheumatology Department Wenzhou People's HospitalWenzhouZhejiang 325000China State Key Laboratory for Conservation and Utilization of Bio-Resources in Yunnan School of Life SciencesYunnan UniversityKunming 650091China Rheumatology Department The First Affiliated Hospital of Wenzhou Medical UniversityWenzhouZhejiang 325000China Institute of Genomic Medicine Wenzhou Medical UniversityWenzhouZhejiang 325000China Department of Rheumatology and Immunology Shanghai Changzheng HospitalSecond Affiliated Hospital of Naval Medical UniversityShanghai 200003China

Gut dysbiosis is suggested to play a critical role in the pathogenesis of *** aim of our study was to identify the characteristic dysbiosis of the gut microbiota in gout patients and the impact of a commonly used uric acid-lowering treatment,febuxostat on gut microbiota in gout.16S ribosomal RNA sequencing and metagenomic shotgun sequencing was performed on fecal DNA isolated from 38 untreated gout patients,38 gout patients treated with febuxostat,and 26 healthy controls.A restriction of gut microbiota biodiversity was detected in the untreated gout patients,and the alteration was partly restored by *** metabolic indexes involved in liver and kidney metabolism were significantly associated with the gut microbiota composition in gout *** analysis revealed that the gut microbiome of gout patients had an enriched function on carbohydrate metabolism but a lower potential for purine metabolism,which was comparatively enhanced in the febuxostat treated gout patients.A classification microbial model obtained a high mean area under the curve up to ***,gut dysbiosis characterizings gout could potentially serve as a noninvasive diagnostic tool for gout and may be a promising target of future preventive interventions.

关键词： Gout Gut microbiota febuxostat Metabolism Gene sequencing

Effects of febuxostat on atrial remodeling in a rabbit model of atrial fibrillation induced by rapid atrial pacing

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Journal of Geriatric Cardiology 2019年第7期16卷 540-551页

作者： Yong-Yan FAN Feng XU Chao ZHU Wen-Kun CHENG Jian LI Zhao-Liang SHAN Yang LI Yu-Tang WANG College of Medicine Nankai UniversityTianjinChina Department of Cardiology Chinese PLA General HospitalBeijingChina Department of Bone&Joint Shijingshan Teaching Hospital of Capital Medical UniversityBeijing Shijingshan HospitalBeijingChina Department of Heart Center Beijing Friendship HospitalCapital Medical UniversityBeijingChina Department of Geriatric Cardiology Chinese PLA General HospitalBeijingChina

Background febuxostat,a novel nonpurine selective inhibitor of xanthine oxidase(XO),may be used in the prevention and management of atrial fibrillation(AF).The purpose of this study was to evaluate the effects of febuxostat on atrial remodeling in a rabbit model of AF induced by rapid atrial pacing(RAP)and the mechanisms by which it *** Twenty-four rabbits were randomly divided into four groups:sham-operated group(Group S),RAP group(Group P),RAP with 5 mg/kg per day febuxostat group(Group LFP),and RAP with 10 mg/kg per day febuxostat group(Group HFP).All rabbits except those in Group S were subjected to RAP at 600 beats/min for four *** effects of febuxostat on atrial electrical and structural remodeling,markers of inflammation and oxidative stress,and signaling pathways involved in the left atrium were *** Shortened atrial effective refractory period(AERP),increased AF inducibility,decreased mRNA levels of Cav1.2 and Kv4.3,and left atrial enlargement and dysfunction were observed in Group P,and these changes were suppressed in the groups treated with *** atrial fibrosis was observed in Group P,as were increased levels of TGF-β1,Collagen I,andα-SMA and decreased levels of Smad7 and *** with febuxostat attenuated these *** in inflammatory and oxidative stress markers induced by RAP were consistent with the protective effects of *** This study is the first to find that febuxostat can inhibit atrial electrical and structural remodeling of AF by suppressing XO and inhibiting the TGF-β1/Smad signaling pathway.

关键词： Atrial fibrillation Atrial remodeling febuxostat Rapid atrial pacing Xanthine oxidase

Preparation, optimization and in vitro–in vivo investigation for capsules of the choline salt of febuxostat

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Asian Journal of Pharmaceutical Sciences 2016年第6期11卷 715-721页

作者： Xuemei Han Wanpeng Qi Wenxiang Dong Mengran Guo Panqin Ma Jing Wang School of Pharmacy Shenyang Pharmaceutical UniversityNo.103Wenhua RoadShenyang 110016China Kangya of Ningxia Pharmaceuticals Co.Ltd No.57FuanWest LaneYinchuan 750002China

The objective of the present study was to exhibit the enhanced water-solubility and in vivo oral absorption when febuxostat(FXT) became the salt formation of choline. The formation of the choline salt of febuxostat was confirmed by X-ray powder diffraction, infrared spectroscopy analysis and differential scanning calorimetry. The direct filling method was used to develop a capsule formulation. Cellactose 80 was used as the filler due to its good fluidity, while cross-linked polyvinylpyrrolidone(PVPP) and magnesium stearate(MS) were used as the disintegrant and lubricant, respectively. Then the in vitro release of the formulation was carried out in five different dissolution media including HCl solution(pH 1.2),acetate buffer(pH 4.5), phosphate buffer(pH 6.8 and pH 7.2) and water. Evident improvement of release for choline febuxostat(CXT) was presented in water while the dissolution degree was decreased for CXT in the medium of phosphate buffer(pH 6.8) in comparison with FXT. Furthermore, the pharmacokinetics of CXT was studied in rats using UPLC-MS/MS compared with FXT. The data acquired illustrated that AUC0-24 h of CXT and FXT were22,245.96 ± 7342.92 μg·h/l and 12,249.70 ± 2024.04 μg·h/l, respectively. The relative bioavailability of CXT to FXT was about 181.6% and the P value of AUC0-24 h was less than 0.05. It showed significant difference between the two drugs after oral administration. In conclusion, the water-solubility and oral bioavailability were both improved remarkably for the choline salt of febuxostat and choline salinization was proved an effective way to increase the in vivo absorption for FXT.

关键词： Choline febuxostat Characterization Preparation In vitro release Bioavailability

The preparation and characteristics of febuxostat SiO2 solid dispersions

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Journal of Chinese Pharmaceutical Sciences 2014年第7期23卷 463-470页

作者：宋文丁杜若宋平钟婷张卫强赵阳王超张烜张强北京大学医学部药学院药剂学系北京100191 北京大学医学部药学院天然药物及仿生药物国家重点实验室北京100191

In the present research, we selected Sylysia as a porous material and febuxostat（FBT） as model drug to prepare the FBT SiO2 solid dispersions using a solvent evaporation method. We firstly established an HPLC method for determining FBT in our prepared FBT SiO2 solid dispersions. And then, the characteristics of FBT SiO2 solid dispersions were investigated, including differential scanning calorimetry（DSC）, powder X-ray diffraction（PXRD）, scanning electron microscope（SEM）, particle size and distribution. The solubility and dissolution of FBT SiO2 solid dispersion were also evaluated. The results of DSC and PXRD showed that the FBT existed in an amorphous state in FBT SiO2 solid dispersions. The SEM and particle size results indicated that the shape and average particle size of FBT SiO2 solid dispersions was similar to the Sylysia. The solubility and dissolution of FBT in FBT SiO2 solid dispersions were significantly enhanced compared with the pure FBT. In conclusion, we successfully prepared FBT SiO2 solid dispersions to increase the solubility and dissolution rate of the poorly water-soluble FBT.

关键词： febuxostat Sylysia Solid dispersion Solubility and dissolution

Green UHPLC Method for Simultaneous Determination of febuxostat and Diclofenac in Pharmaceutical Dosage Form and Human Plasma

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Journal of Analytical Sciences, Methods and Instrumentation 2021年第4期11卷 29-45页

作者： Shimaa A. Mahmoud Amira M. El-Kosasy Fatma A. Fouad Pharmaceutical Analytical Chemistry Department Faculty of Pharmacy Al-Azhar University Cairo Egypt Pharmaceutical Analytical Chemistry Department Faculty of Pharmacy Ain Shams University Cairo Egypt

Eco-friendly Ultra-high-performance liquid chromatography (UHPLC) with green aqueous-organic mobile phase was applied for the simultaneous determination of febuxostat (FEB) and diclofenac (DIC) with the composition of water:ethanol (85:15 v/v) utilizing phenomenex Kinetex C18 column (4.6 × 100 mm 2.6 μm), flow rate 1 ml/min and UV detection at 280 nm with linear ranges of 0.4 - 4.0 μg/mL and 0.5 - 5.0 μg/mL for FEB and DIC, respectively. The proposed method was also successfully applied to analyze the two drugs in pharmaceutical dosage form and human plasma. The results obtained were validated and statistically analyzed and found to be in accordance with those given by reported methods. Moreover, the greenness of the developed method is assessed using suitable analytical Eco-Scale and GAPI tools and comparison with the previously published methods have been carried out to indicate the priority of the proposed method. UHPLC is considered eco-friendly method regarding uses of safe solvents, simple, accurate and short time of analysis.

关键词： febuxostat Diclofenac Ultra-High-Performance Liquid Chromatography Eco-Scale Green Analytical Procedure Index Tools

Perturbation of Quorum Sensing in <i>Pseudomonas aeruginosa</i>by febuxostat

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Advances in Microbiology 2018年第8期8卷 650-664页

作者： Hisham Abdel Monem Abbas Wafaa Ezz Elarab Soliman Moutaz Ahamed Shaldam Department of Microbiology and Immunology Faculty of Pharmacy Zagazig University Zagazig Egypt Department of Microbiology and Biotechnology Faculty of Pharmacy Delta University for Science and Technology Mansoura Egypt Department of Medicinal Chemistry Faculty of Pharmacy Delta University for Science and Technology Mansoura Egypt

Quorum sensing is a signal-based communication system in bacteria. It is an attractive target because it regulates the production of virulence factors in Pseudomonas aeruginosa. As a result, interference with quorum sensing could result in inhibition of virulence of Pseudomonas aeruginosa with the merit of lack of selective pressure on growth that leads to development of resistance. This study investigated the anti-quorum sensing and anti-virulence activities of febuxostat in Pseudomonas aeruginosa PAO1 strain. At 1/8 MIC of febuxostat, the production of the quorum-sensing regulated violacein pigment of Chromobacterium violaceum CV026 was significantly reduced. Moreover, it markedly reduced pyocyanin, hemolysin, protease and elastase production. Significant inhibitory activities were also found against biofilm, swimming, twitching and swarming motilities. Molecular docking showed the ability of febuxostat to inhibit quorum sensing by competing with the autoinducers to bind with LasR and RhlR receptors. febuxostat could bind to both receptors by hydrogen bonding and hydrophobic interaction. From the Molecular docking scores, febuxostat is a very promising quorum sensing inhibitor. febuxostat could also significantly decrease the level of expression of all QS genes LasI, LasR, RhlI, RhlR, PqsA and PqsR that regulate the production of virulene factors as confirmed by qRT-PCR.

关键词： febuxostat Pseudomonas aeruginosa Quorum Sensing Virulence Inhibition Molecular Docking

Pharmacokinetics and Safety of febuxostat Following a Single and Multiple Oral Doses in Healthy Chinese Volunteers

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Pharmacokinetics and Safety of Febuxostat Following a Single...

New synthesis route of febuxostat

第十三次全国临床药理学学术大会

作者： Jiang Bo MD,RUAN Zourong,Chen Jinliang,PhD,Lou Honggang,MS,Yu Lingyan,MS Division of Clinical Pharmacology,2nd Affiliated Hospital,School of Medicine,Zhejiang University, Hangzhou.Address for correspondence:RUAN Zourong,Division of Clinical Pharmacology,2nd Affiliated Hospital,School of Medicine,Zhejiang University,88 Jiefang Road,Hangzhou,310009 China

The pharmacokinetics and safety of febuxostat were assessed in healthy Chinese *** the single-dose study,a randomized open-label,2-way crossover design was *** were assigned to receive 40 or 80 mg febuxostat by oral administration with a 1-week washout *** concentration of febuxostat in human plasma was determined by LC-MS/*** levels of febuxostat were found to be proportional to dose,with the mean Cmax and AUCO-oo range from 4.0 to 7.7 mg/L and 11.9 to 26.2 mg·h/L over the dose range *** the multiple-dose study,80 mg febuxostat was administered once daily for 7 *** drug accumulation was *** mean steady-state Cmax,AUCO-co,and AUCss were 7.2 mg/L,23.4 mg·h/L and 22.9 mg·h/L,***,the value of Cmax and AUC in Chinese were almost one fold over that of the Western healthy volunteers in the corresponding *** was rapidly cleared from plasma with t1/2z 4.5 hours,which was similar to the single dose value(5.4～5.7 hours).No serious AEs and no pattern of dose-related AEs were reported during the *** results showed that the drug was well tolerated in dose range from 40～80 mg in Chinese healthy volunteers,but the dose used in the Chinese gout patients should be re-explored.

关键词： febuxostat pharmacokinetics safety single dose multiple dose

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New synthesis route of febuxostat

febuxostat对痛风伴高尿酸血症患者的血液流变学和血小板活化功能的影响

中国化学会第27届学术年会

作者： Chuan-Fei Liu, Yan-Feng Dai*, Yuan Li Department of Chemistry, Nanchang University, 330031, Nanchang

＜正＞febuxostat, an antipodagrics, was synthesized from 4-hydroxybenzoic acid by reactions of etherfication （protection）, ammoniation and thioformylation to give 4-Methoxythiobenzamide,

关键词： febuxostat anti gout drug xanthine oxidase inhibitor synthesis.

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基础医学与临床 2018年第11期38卷 1568-1571页

作者：刘青员祁广东陈鑫江苏省滨海县人民医院内分泌科江苏滨海224500 南通大学附属医院神经内科江苏南通226001

目的探讨febuxostat(非布司他)对痛风伴高尿酸血症患者血液流变学及血小板活化功能的影响。方法选取滨海县人民医院2015年4月至2017年3月收治的痛风伴高尿酸血症患者68例,随机分为对照组(35例)(给予别嘌醇治疗)和观察组(33例)(给予febux... 详细信息

目的探讨febuxostat(非布司他)对痛风伴高尿酸血症患者血液流变学及血小板活化功能的影响。方法选取滨海县人民医院2015年4月至2017年3月收治的痛风伴高尿酸血症患者68例,随机分为对照组(35例)(给予别嘌醇治疗)和观察组(33例)(给予febuxostat治疗)。比较两组患者的临床疗效、血液流变学变化以及血小板活化功能的变化。结果治疗总有效率,观察组患者高于对照组患者(Pfebuxostat治疗能有效地降低痛风伴高尿酸血症患者的高尿酸状态,改善患者的血液流变学与血小板活化功能,疗效优于别嘌醇。

关键词： febuxostat 别嘌醇高尿酸血症痛风血液流变学血小板活化功能