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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 gout.The 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 febuxostat.Biochemical metabolic indexes involved in liver and kidney metabolism were significantly associated with the gut microbiota composition in gout patients.Functional 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 0.973.Therefore,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 acts.Methods 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 weeks.The effects of febuxostat on atrial electrical and structural remodeling,markers of inflammation and oxidative stress,and signaling pathways involved in the left atrium were examined.Results 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 febuxostat.Prominent atrial fibrosis was observed in Group P,as were increased levels of TGF-β1,Collagen I,andα-SMA and decreased levels of Smad7 and eNOS.Treatment with febuxostat attenuated these differences.Changes in inflammatory and oxidative stress markers induced by RAP were consistent with the protective effects of febuxostat.Conclusions 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

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

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

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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

Cardiovascular events in hyperuricemia population and a cardiovascular benefit-risk assessment of urate-lowering therapies:a systematic review and meta-analysis

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Chinese Medical Journal 2020年第8期133卷 982-993页

作者： Li Zhao Ling Cao Tian-Yi Zhao Xue Yang Xiao-Xia Zhu He-Jian Zou Wei-Guo Wan Yu Xue Department of Rheumatology Huashan HospitalFudan UniversityShanghai 200040China Institute of Rheumatology Immunology and AllergyFudan UniversityShanghai 200040China

Background:Hyperuricemia and gout have become public health concerns;many important guidelines have recommended xanthine oxidase inhibitors(XOIs)as the first-line urate-lowering therapies(ULTs)to treat chronic gout with hyperuricemia.However,whether treating hyperuricemia and gout with ULTs modifies cardiovascular risks remains controversial.The aim of this study was to assess the incident risk of cardiovascular(CV)events(CVE)in hyperuricemia population,assess the cardiovascular benefit-risk of ULTs in hyperuricemia patients with or without gout in diverse cardiovascular risk sub-groups,and specify the safety of different ULTs.Methods:We searched PubMed,Embase,the Cochrane Library,Wanfang,Chongqing VIP(CQVIP,***),and China National Knowledge Infrastructure Database for prospective cohort studies and randomized controlled trials(RCTs)in English and Chinese.Potential medications included XOIs,and uricosurics.RCTs were divided into sub-groups analysis based on blinding status and patients’history of CV diseases.Risk ratios(RRs)were calculated and were reported with corresponding 95%confidence intervals(CIs)by fixed-effects or random-effects model.Results:Seven prospective cohort studies and 17 RCT studies were included.The risks of both major adverse cardiovascular events(MACE)(RR=1.72,95%CI 1.28-2.33)and CVE(RR=1.35,95%CI 1.12-1.62)were higher in the hyperuricemia population than non-hyperuricemia one.In seven RCT studies where XOIs were compared with no-treatment or placebo,the results of five low CV risk studies showed that XOIs lowered the risks of both MACE(RR=0.35,95%CI 0.20-0.62)and CVE(RR=0.61,95%CI 0.44-0.85);whereas two high CV risk studies showed that XOIs lowered the risk of CVE(RR=0.69,95%CI 0.54-0.88)rather than MACE(RR=0.62,95%CI 0.29-1.35).In nine RCT studies where the cardiovascular safety between febuxostat and allopurinol were compared,no statistical difference was found in the risk of MACE or CVE.Conclusions:The hyperuricemia population does have a higher incidence of CVE,and the results suggeste

关键词： Hyperuricemia Gout Cardiovascular event febuxostat Allopurinol

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抗痛风药物febuxostat的合成

中国药物化学杂志 2008年第4期18卷 259-262页

作者：武瑊王春辉李松郑志兵军事医学科学院毒物药物研究所北京100850 沈阳药科大学制药工程学院辽宁沈阳110016

目的合成新型抗痛风药物febuxostat(1)。方法以羟基苯腈为原料,经硫代甲酰化得到对羟基硫代苯甲酰胺(3),3经环合得到2-(4-羟基苯基)-4-甲基-噻唑-5-羧酸乙酯(4),4与乌洛托品反应,得到中间体2-(3-甲酰基-4-羟基苯基)-4-甲基-噻唑-5-羧酸... 详细信息

目的合成新型抗痛风药物febuxostat(1)。方法以羟基苯腈为原料,经硫代甲酰化得到对羟基硫代苯甲酰胺(3),3经环合得到2-(4-羟基苯基)-4-甲基-噻唑-5-羧酸乙酯(4),4与乌洛托品反应,得到中间体2-(3-甲酰基-4-羟基苯基)-4-甲基-噻唑-5-羧酸乙酯(5),之后再经醚化、氰化、水解得到目标产物(1)。结果与结论中间体及目标化合物的结构经1H-NMR和FAB-MS确证。该合成路线中使用的原料和试剂价廉易得,反应条件温和易控,操作简便。

关键词： febuxostat 黄嘌呤氧化酶抑制剂抗痛风药合成

febuxostat治疗妇女痛风的效果优于AUopurinol

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基础医学与临床 2013年第3期33卷 381-381页

据美国WebMD医学新闻网（2011-12-15）报道，根据已发表期刊的资料中，回顾性分析参与第3期比较实验222名高尿酸妇女的数据显示，每天80 mg febuxostat降低血清尿酸值低于6．0mg／dL之效果优于每天100、200或300mg的allopurinol。芝加... 详细信息

据美国WebMD医学新闻网（2011-12-15）报道，根据已发表期刊的资料中，回顾性分析参与第3期比较实验222名高尿酸妇女的数据显示，每天80 mg febuxostat降低血清尿酸值低于6．0mg／dL之效果优于每天100、200或300mg的allopurinol。芝加哥大学Pritzker医学院和武田全球研发小组的Saima Chohan医生等人，比较了痛风患者使用febuxostat、allopurinol和安慰荆的随机控制实验数据进行了事后分析，这些数据共包括了4101名患者，其中226名女性，有4名女性在开始时的血清尿酸值低于8．0mg／dL，所以仅纳入其他222名患者。

关键词： febuxostat 痛风患者 allopurinol febuxostat 妇女治疗数据显示芝加哥大学