Metronidazole

甲硝唑
  • 文章类型: Journal Article
    本研究旨在研究储存条件对沙特阿拉伯市售甲硝唑(MTZ)片剂溶出性能的影响;这些被编码为参考和测试A,试验B,和测试C产品。此外,测量硬度和崩解时间。利用UV分光光度分析技术来定量MTZ。所有的控制片,收到后进行了测试,满足USP要求,因为在60分钟内溶解了不少于85%的标记量的MTZ。MTZ参考在60分钟后释放91.79%±1.23,而产品A,B,C释放率分别为87.96%±2.60、93.26%±2.01和88.61%±2.04。对所有对照片剂计算的不同溶出参数表明,MTZ产品A和B具有最佳溶出性能并且被认为与参考产品相似。产物C显示出显著降低的溶出性能,并且被认为与参照不同。在40℃±2℃/75%RH±5%下储存6个月的MTZ片剂的体外溶出表明片剂保持符合USP要求。MTZ参考在60分钟后释放89.36%±3.64,而产品A,B,C释放率分别为95.79%±3.91、88.52%±2.52和87.79%±5.04。然而,在应激条件下储存的前3个月期间观察到30分钟后释放的百分比(%DE30)的轻微降低和平均溶解时间(MDT)的轻微增加。在相同条件下储存6个月后,这些变化更加明显。此外,在40°C±2°C/75%RH±5%下储存3个月并进一步防止高湿度的产品C的体外溶出表明,由于两种包装形式所发挥的类似保护作用,溶出参数有所改善。此外,研究表明,储存条件如湿度和温度会影响MTZ上市片剂的体外溶出度,这可能会影响效率和患者安全。
    This study aimed to investigate the impact of storage conditions on the dissolution performance of commercial metronidazole (MTZ) tablets available in Saudi Arabia; these were coded as the reference and Test A, Test B, and Test C products. Moreover, the hardness and the disintegration time were measured. The UV spectrophotometrically analytical technique was utilized to quantify MTZ. All the control tablets, which were tested upon receipt, met the USP requirement as not less than 85 % of the labeled amount of MTZ was dissolved in 60 min. The MTZ reference released 91.79 % ± 1.23 after 60 min, while the products A, B, and C released 87.96 % ± 2.60, 93.26 % ± 2.01, and 88.61 % ± 2.04, respectively. The different dissolution parameters calculated for all the control tablets showed that the MTZ products A and B had optimal dissolution performances and were considered similar to the reference product. The product C showed a significantly reduced dissolution performance and was considered different from the reference. The in vitro dissolution of the MTZ tablets stored at 40oC ± 2 oC/75 % RH ± 5 % for 6 months indicated that the tablets maintained compliance with the USP requirement. The MTZ reference released 89.36 % ± 3.64 after 60 min, while the products A, B, and C released 95.79 % ± 3.91, 88.52 % ± 2.52, and 87.79 % ± 5.04, respectively. However, a slight reduction in the percentage released after 30 min (% DE30) and a slight increase in the mean dissolution time (MDT) were observed during the first 3 months of storage under stressed conditions. These changes were more obvious after 6 months of storage under the same conditions. Furthermore, in vitro dissolution of the product C stored at 40oC ± 2 oC/75 % RH ± 5 % for 3 months with further protection against high humidity revealed an improvement in the dissolution parameters due to the similar protective effects exerted by the two packaging forms. Furthermore, the study shows that storage conditions such as humidity and temperature affect in vitro dissolution of MTZ marketed tablets which may have an impact on efficiency and patient safety.
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  • 文章类型: Case Reports
    背景:可以从受牙髓和牙周感染影响的人类口腔中分离出来,以及健康个体的牙菌斑,使其成为口腔微生物群中的常见细菌。然而,它在引起人类胸膜感染中的作用很少见。
    方法:1例老年胃癌手术患者出院后不久出现脓性胸腔积液。通过实验室培养确定感染是由专性厌氧菌引起的,并通过16SrRNA基因序列分析进一步鉴定为引起胸膜感染的马氏Hoylesella。药敏试验指导头孢哌酮-舒巴坦和甲硝唑的精确治疗。患者的临床症状迅速改善,实验室检测指标逐渐恢复正常,病人最终康复了.
    结论:马氏Hoylesella可引起人类胸膜感染。临床微生物学实验室在常规需氧培养不显示细菌生长但涂片染色可见细菌时,应特别注意专性厌氧菌的培养。当传统的鉴定方法无法鉴定细菌时,基于高度保守的16SrRNA基因序列的分析可以准确、特异地鉴定细菌,指导临床医生制定精确的抗感染策略。
    BACKGROUND: Hoylesella marshii can be isolated from human oral cavities affected by dental pulp and periodontal infections, as well as from the dental plaque of healthy individuals, making it a common bacterium within the oral microbiota. However, its role in causing pleural infections in humans is rare.
    METHODS: A case of purulent pleural effusion occurred shortly after discharge in an elderly patient who had undergone surgery for gastric cancer. The infection was identified as being caused by an obligate anaerobe through laboratory culture, and was further identified as Hoylesella marshii causing pleural infection through 16 S rRNA gene sequence analysis. Susceptibility testing guided precise treatment with cefoperazone-sulbactam and metronidazole. The patient\'s clinical symptoms improved rapidly, laboratory test indicators gradually returned to normal, and the patient ultimately recovered.
    CONCLUSIONS: Hoylesella marshii can cause pleural infections in humans. Clinical microbiology laboratories should pay special attention to the cultivation of obligate anaerobes when routine aerobic cultures do not show bacterial growth but bacteria are visible on smear staining, and when conventional identification methods fail to identify the bacterium, analysis based on the highly conserved 16 S rRNA gene sequence can accurately and specifically identify the bacterium, guiding clinicians in formulating precise anti-infection strategies.
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  • 文章类型: Case Reports
    尽管胸腔引流和抗生素治疗,胸膜脓胸仍可导致显著的发病率和死亡率。需要新颖的微创干预措施。核梭杆菌是在人类口腔和肠道微生物群中发现的一种专性厌氧菌。测序和穿刺技术的进步使在脓胸病例中检测厌氧菌变得普遍。在这份报告中,我们描述了一例65岁的高血压患者,出现左侧包裹性胸腔积液.使用宏基因组下一代测序(mNGS)进行的初始流体分析显示存在核梭杆菌和黑曲霉。不幸的是,尽管引流和抗菌治疗,患者胸腔积液恶化.最终,通过胸膜腔内甲硝唑治疗联合全身抗生素治疗成功.本病例表明,胸膜腔内抗生素治疗是治疗胸膜脓胸的有希望的措施。
    Pleural empyema can lead to significant morbidity and mortality despite chest drainage and antibiotic treatment, necessitating novel and minimally invasive interventions. Fusobacterium nucleatum is an obligate anaerobe found in the human oral and gut microbiota. Advances in sequencing and puncture techniques have made it common to detect anaerobic bacteria in empyema cases. In this report, we describe the case of a 65-year-old man with hypertension who presented with a left-sided encapsulated pleural effusion. Initial fluid analysis using metagenomic next-generation sequencing (mNGS) revealed the presence of Fusobacterium nucleatum and Aspergillus chevalieri. Unfortunately, the patient experienced worsening pleural effusion despite drainage and antimicrobial therapy. Ultimately, successful treatment was achieved through intrapleural metronidazole therapy in conjunction with systemic antibiotics. The present case showed that intrapleural antibiotic therapy is a promising measure for pleural empyema.
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  • 文章类型: Journal Article
    在这项研究中,磷酸活化用于从香菇(香菇)残留物中合成氮掺杂的中孔活性炭(称为MR1),同时旨在有效去除对乙酰氨基酚(APAP),卡马西平(CBZ),和甲硝唑(MNZ)来自水溶液。我们使用扫描电子显微镜(SEM)表征了所产生的吸附剂的物理化学性质,氮吸附等温线,和X射线光电子能谱(XPS)。使用1、2和3mL/g的磷酸浸渍比例制备MR1,MR2和MR3,分别。值得注意的是,MR1表现出显著的介孔结构,其体积为0.825cm3/g,季氮含量为2.6%。这赋予了MR1对APAP的高吸附能力,CBZ,和MNZ,将其定位为净水应用的有希望的候选者。污染物的吸附行为遵循Freundlich等温线模型,表明多层吸附过程。值得注意的是,MR1表现出优异的耐久性和可回收性,在五个再生循环后保持其初始吸附效率的95%,并表明其在水处理过程中可持续使用的潜力。
    In this study, phosphoric acid activation was employed to synthesize nitrogen-doped mesoporous activated carbon (designated as MR1) from Lentinus edodes (shiitake mushroom) residue, while aiming to efficiently remove acetaminophen (APAP), carbamazepine (CBZ), and metronidazole (MNZ) from aqueous solutions. We characterized the physicochemical properties of the produced adsorbents using scanning electron microscopy (SEM), nitrogen adsorption isotherms, and X-ray photoelectron spectroscopy (XPS). MR1, MR2, and MR3 were prepared using phosphoric acid impregnation ratios of 1, 2, and 3 mL/g, respectively. Notably, MR1 exhibited a significant mesoporous structure with a volume of 0.825 cm3/g and a quaternary nitrogen content of 2.6%. This endowed MR1 with a high adsorption capacity for APAP, CBZ, and MNZ, positioning it as a promising candidate for water purification applications. The adsorption behavior of the contaminants followed the Freundlich isotherm model, suggesting a multilayer adsorption process. Notably, MR1 showed excellent durability and recyclability, maintaining 95% of its initial adsorption efficiency after five regeneration cycles and indicating its potential for sustainable use in water treatment processes.
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  • 文章类型: Journal Article
    能够激活成像探针和前药的细菌硝基还原酶是用于基因导向的酶前药疗法和靶向细胞消融模型的有价值的工具。我们最近设计了一种硝基还原酶(E.coliNfsBF70A/F108Y)用于显着增强的5-硝基咪唑PET探针还原,SN33623,它允许用氧不敏感的细菌硝基还原酶标记的载体的热成像。该突变酶还显示出改善的DNA烷基化前药CB1954和甲硝唑的活化。为了阐明这些增强背后的机制,我们将突变酶的晶体结构解析为1.98µ,并将其与野生型酶进行了比较。结构分析揭示了扩展的衬底通道和新的氢键相互作用。此外,SN33623,CB1954和甲硝唑在突变和野生型酶的活性位点结合的计算模型揭示了底物取向和相互作用的关键差异,在突变模型中,异咯嗪的N5-H与底物硝基氧之间的距离减小反映了活性的改善。这些发现加深了我们对硝基还原酶底物特异性和催化机理的理解,并对在癌症治疗中开发更有效的治疗影像策略具有潜在的意义。
    Bacterial nitroreductase enzymes capable of activating imaging probes and prodrugs are valuable tools for gene-directed enzyme prodrug therapies and targeted cell ablation models. We recently engineered a nitroreductase (E. coli NfsB F70A/F108Y) for the substantially enhanced reduction of the 5-nitroimidazole PET-capable probe, SN33623, which permits the theranostic imaging of vectors labeled with oxygen-insensitive bacterial nitroreductases. This mutant enzyme also shows improved activation of the DNA-alkylation prodrugs CB1954 and metronidazole. To elucidate the mechanism behind these enhancements, we resolved the crystal structure of the mutant enzyme to 1.98 Å and compared it to the wild-type enzyme. Structural analysis revealed an expanded substrate access channel and new hydrogen bonding interactions. Additionally, computational modeling of SN33623, CB1954, and metronidazole binding in the active sites of both the mutant and wild-type enzymes revealed key differences in substrate orientations and interactions, with improvements in activity being mirrored by reduced distances between the N5-H of isoalloxazine and the substrate nitro group oxygen in the mutant models. These findings deepen our understanding of nitroreductase substrate specificity and catalytic mechanisms and have potential implications for developing more effective theranostic imaging strategies in cancer treatment.
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  • 文章类型: Journal Article
    这项研究的目的是介绍一种用于治疗牙髓炎症(牙髓炎)的牙齿盖帽剂。合成了负载甲硝唑(nHAEA@MTZ)的带有沙枣提取物(nHAEA)的纳米羟基磷灰石,并使用脂多糖(LPS)的牙髓炎体外模型进行了评估。nHAEA通过溶胶-凝胶法合成,并使用扫描电子显微镜进行分析,透射电子显微镜,还有BrunauerEmmettTeller.LPS诱导的人牙髓干细胞(HDPSC)的炎症。划痕测试评估细胞迁移,RTPCR测量细胞因子水平,和茜素红染色定量牙本质形成。nHAEA纳米棒的宽度为17-23nm,长度为93-146nm,平均孔径为27/312nm,表面积为210.89m2/g。具有受控释放的MTZ装载内容物,建议适合治疗应用。nHAEA@MTZ对HDPSCs牙源性能力的影响不超过nHAEA。然而,观察到nHAEA@MTZ表现出更明显的抗炎作用。与其他组相比,用纳米颗粒处理的HDPSC表现出改善的迀移。这些发现表明,nHAEA@MTZ可能是一种有效的盖髓材料,并且可能比nHAEA更有效地减少炎症和激活HDPSC以增强牙髓损伤后的牙髓修复。
    The aim of this study is to introduce a dental capping agent for the treatment of pulp inflammation (pulpitis). Nanohydroxyapatite with Elaeagnus angustifolia L. extract (nHAEA) loaded with metronidazole (nHAEA@MTZ) was synthesized and evaluated using a lipopolysaccharide (LPS) in vitro model of pulpitis. nHAEA was synthesized through sol-gel method and analyzed using Scanning Electron Microscopy, Transmission Electron Microscopy, and Brunauer Emmett Teller. Inflammation in human dental pulp stem cells (HDPSCs) induced by LPS. A scratch test assessed cell migration, RT PCR measured cytokines levels, and Alizarin red staining quantified odontogenesis. The nHAEA nanorods were 17-23 nm wide and 93-146 nm length, with an average pore diameter of 27/312 nm, and a surface area of 210.89 m2/g. MTZ loading content with controlled release, suggesting suitability for therapeutic applications. nHAEA@MTZ did not affect the odontogenic abilities of HDPSCs more than nHAEA. However, it was observed that nHAEA@MTZ demonstrated a more pronounced anti-inflammatory effect. HDPSCs treated with nanoparticles exhibited improved migration compared to other groups. These findings demonstrated that nHAEA@MTZ could be an effective material for pulp capping and may be more effective than nHAEA in reducing inflammation and activating HDPSCs to enhance pulp repair after pulp damage.
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  • 文章类型: Journal Article
    细菌中的抗生素耐药性被认为是导致治疗失败的主要因素。在这项研究中,我们的目的是研究巴勒斯坦幽门螺杆菌对抗生素的耐药性.我们招募了91名消化不良患者,包括49名女性和42名男性。这些参与者接受了食管胃十二指肠镜检查和胃活检。随后对这些活组织检查进行微生物学评估,并测试其对各种抗微生物药物的敏感性。在91名患者中,38例(41.7%)表现出幽门螺杆菌的存在。值得注意的是,环丙沙星对幽门螺杆菌的疗效最高,其次是左氧氟沙星,莫西沙星,和阿莫西林,耐药率为0%,0%,2.6%,和18.4%,分别。相反,甲硝唑和克拉霉素的有效性最低,电阻百分比为100%和47.4%,分别。这项研究的结果强调,巴勒斯坦患者组中的幽门螺杆菌菌株对传统的一线抗生素如克拉霉素和甲硝唑表现出实质性的耐药性。然而,替代药物如氟喹诺酮和阿莫西林仍然是有效的选择.因此,我们建议支持以喹诺酮为基础的幽门螺杆菌感染治疗方案,并在巴勒斯坦人群中采用更明智的抗生素使用方法.
    Antibiotic resistance among bacteria is recognized as the primary factor contributing to the failure of treatment. In this research, our objective was to examine the prevalence of antibiotic resistance in H. pylori bacteria in Palestine. We enlisted 91 individuals suffering from dyspepsia, comprising 49 females and 42 males. These participants underwent esophagogastroduodenoscopy procedures with gastric biopsies. These biopsies were subsequently subjected to microbiological assessments and tested for their susceptibility to various antimicrobial drugs. Among the 91 patients, 38 (41.7%) exhibited the presence of H. pylori. Notably, Ciprofloxacin displayed the highest efficacy against H. pylori, followed by Levofloxacin, Moxifloxacin, and Amoxicillin, with resistance rates of 0%, 0%, 2.6%, and 18.4%, respectively. On the contrary, Metronidazole and Clarithromycin demonstrated the lowest effectiveness, with resistance percentages of 100% and 47.4%, respectively. The outcomes of this investigation emphasize that H. pylori strains within the Palestinian patient group exhibit substantial resistance to conventional first-line antibiotics like clarithromycin and metronidazole. However, alternative agents such as fluoroquinolones and amoxicillin remain efficacious choices. Consequently, we recommend favoring quinolone-based treatment regimens for H. pylori infections and adopting a more judicious approach to antibiotic usage among the Palestinian population.
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    文章类型: Journal Article
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  • 文章类型: Journal Article
    甲硝唑(MTZ)是针对阴道毛滴虫的最常见药物(T。阴道)感染;然而,已经报道了滴虫的治疗失败和高复发率,提示阴道毛虫对MTZ存在抗性。因此,针对阴道毛虫感染的新治疗选择的研究变得越来越紧迫。本研究通过体外药敏试验研究了5种咪唑氨基甲酸酯化合物(AGR-1、AGR-2、AGR-3、AGR-4和AGR-5)的滴虫活性,以确定各化合物的IC50值。所有五个化合物都显示出有效的滴虫活性,IC50值在纳摩尔范围内,AGR-2是最有效的(IC50为400nM)。为了深入了解与AGR诱导的阴道毛虫细胞死亡相关的分子事件,我们分析了暴露于AGR化合物和MTZ的滋养体中一些代谢基因的表达谱。发现AGR和MTZ化合物均降低了糖酵解基因的表达(CK,PFK,TPI,和ENOL)和参与代谢的基因(G6PD,TKT,TALDO,NADHOX,ACT,和浴缸),这表明干扰这些关键代谢基因会改变阴道毛虫的存活,并且它们可能具有相似的作用机制。此外,这些化合物在Caco-2和HT29细胞系中显示出低的细胞毒性,ADMET分析结果表明这些化合物具有与MTZ相似的药代动力学性质。这些发现提供了重要的见解,可以作为该化合物作为针对阴道毛虫的潜在新疗法的未来体内研究的基础。
    Metronidazole (MTZ) is the most common drug used against Trichomonas vaginalis (T. vaginalis) infections; however, treatment failures and high rates of recurrence of trichomoniasis have been reported, suggesting the presence of resistance in T. vaginalis to MTZ. Therefore, research into new therapeutic options against T. vaginalis infections has become increasingly urgent. This study investigated the trichomonacidal activity of a series of five imidazole carbamate compounds (AGR-1, AGR-2, AGR-3, AGR-4, and AGR-5) through in vitro susceptibility assays to determine the IC50 value of each compound. All five compounds demonstrated potent trichomonacidal activity, with IC50 values in the nanomolar range and AGR-2 being the most potent (IC50 400 nM). To gain insight into molecular events related to AGR-induced cell death in T. vaginalis, we analyzed the expression profiles of some metabolic genes in the trophozoites exposed to AGR compounds and MTZ. It was found that both AGR and MTZ compounds reduced the expression of the glycolytic genes (CK, PFK, TPI, and ENOL) and genes involved in metabolism (G6PD, TKT, TALDO, NADHOX, ACT, and TUB), suggesting that disturbing these key metabolic genes alters the survival of the T. vaginalis parasite and that they probably share a similar mechanism of action. Additionally, the compounds showed low cytotoxicity in the Caco-2 and HT29 cell lines, and the results of the ADMET analysis indicated that these compounds have pharmacokinetic properties similar to those of MTZ. The findings offer significant insights that can serve as a basis for future in vivo studies of the compounds as a potential new treatment against T. vaginalis.
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  • 文章类型: Journal Article
    目的:评价盐酸米诺环素联合甲硝唑与单用甲硝唑治疗种植体周围炎的疗效及对特异性炎症指标的影响。
    方法:对2018年1月至2021年1月的107例种植体周围炎患者进行了回顾性研究。患者单独使用甲硝唑治疗(Con组,n=57)或额外的盐酸米诺环素(实验组,n=50)。炎症标志物,包括白细胞介素-6(IL-6),白细胞介素-1β(IL-1β),肿瘤坏死因子α(TNF-α),治疗前后测定基质金属蛋白酶-8(MMP-8)。使用菌斑指数(PLI)确定临床结果,龈沟出血指数(SBI),和牙周探诊深度(PD)。此外,受试者操作特征(ROC)曲线分析了标记物的临床相关性。采用Logistic回归分析影响患者疗效的危险因素。
    结果:Exp组表现出更有利的临床结果,并显示较低水平的IL-6,IL-1β,TNF-α,和MMP-8比Con组。IL-1β,TNF-α,MMP-8水平与治疗成功率显著相关(P<0.05),但IL-6无统计学意义(P>0.05)。IL-1β和TNF-α的ROC曲线明显优于IL-6和MMP-8(P<0.05)。Logistic回归分析显示,只有IL-1β和TNF-α是影响患者疗效的独立危险因素。
    结论:与单独使用甲硝唑相比,盐酸米诺环素与甲硝唑联合治疗种植体周围炎效果更好。在分析的因素中,只有IL-1β和TNF-α作为可靠的独立疗效指标出现。
    OBJECTIVE: To evaluate the efficacy of minocycline hydrochloride combined with metronidazole versus metronidazole alone in treating peri-implantitis and their impact on specific inflammatory markers.
    METHODS: A retrospective review was undertaken of 107 patients with peri-implantitis from January 2018 to January 2021. Patients were treated either with metronidazole alone (Con group, n = 57) or with additional minocycline hydrochloride (Exp group, n = 50). Inflammatory markers, including interleukin-6 (IL-6), interleukin-1 beta (IL-1β), tumor necrosis factor alpha (TNF-α), and matrix metalloproteinase-8 (MMP-8) were determined before and after treatment. Clinical outcomes were determined using the plaque index (PLI), gingival sulcus bleeding index (SBI), and periodontal probing depth (PD). Furthermore, receiver operator characteristic (ROC) curves analyzed the clinical relevance of the markers. Logistic regression was conducted to analyze the risk factors affecting efficacy in patients.
    RESULTS: The Exp group exhibited more favorable clinical outcomes and showed lower levels of IL-6, IL-1β, TNF-α, and MMP-8 than the Con group. IL-1β, TNF-α, and MMP-8 levels were significantly correlated with treatment success (P < 0.05), but IL-6 was not (P > 0.05). The ROC curves for IL-1β and TNF-α significantly outperformed those for IL-6 and MMP-8 (P < 0.05). Logistic regression analysis showed that only IL-1β and TNF-α were independent risk factors affecting efficacy in patients.
    CONCLUSIONS: Combining minocycline hydrochloride with metronidazole yields better outcomes for peri-implantitis compared to metronidazole alone. Of the factors analyzed, only IL-1β and TNF-α emerged as dependable independent efficacy indicators.
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