Diclofenac sodium

双氯芬酸钠
  • 文章类型: Journal Article
    内镜胰胆管造影术(ERCP)是广泛用于胰胆管疾病的诊断和治疗工具。其主要并发症之一是胰腺炎。本研究旨在了解使用直肠双氯芬酸和吲哚美辛作为预防措施后ERCP术后胰腺炎的发生率。我们从PubMed检索了2870篇文章,ScienceDirect,和谷歌学者数据库。使用PubMed中的医学主题词(MeSH)策略,我们选择了过去五年发表的研究文章。排除标准包括付费全文文章,摘要,给编辑的信,未接受ERCP的患者,年龄超过45岁,动物研究,和非英语学习。在我们的系统评价设计中使用了2020年系统评价和荟萃分析(PRISMA)标准的首选报告项目。发现医学界仍在争论直肠双氯芬酸和吲哚美辛是否有益于避免ERCP后胰腺炎(PEP)。使用直肠双氯芬酸。尽管由于混合的发现和对某些结果的担忧,其有效性存在争议,在特定情况下也被认为是有益的,例如在ERCP之前。直肠吲哚美辛的研究也产生矛盾的结果;虽然一些强调药物的PEP发病率的大幅降低,尤其是在低风险人群中,其他人质疑它的功效。我们需要进一步的研究来澄清剩余的不确定性。
    Endoscopic cholangiopancreatography (ERCP) is a widely used diagnostic and therapeutic tool for pancreaticobiliary conditions. One of its major complications is pancreatitis. This study aims to understand the incidence of post-ERCP pancreatitis after using rectal diclofenac and Indomethacin as prophylactic measures. We retrieved 2870 articles from the PubMed, ScienceDirect, and Google Scholar databases. Using the Medical Subject Headings (MeSH) strategy in PubMed, we chose research articles published in the last five years. Exclusion criteria included paid full-text articles, abstracts, letters to editors, patients not undergoing ERCP, ages more than 45 years, animal studies, and non-English studies. The 2020 Preferred Reporting Items for Systematic Reviews and Meta-Analysis (PRISMA) criteria were used in the design of our systematic reviews. It was found that the medical world is still debating whether rectal diclofenac and Indomethacin are beneficial in avoiding post-ERCP pancreatitis (PEP). Rectal diclofenac is used. Although its effectiveness is debated due to mixed findings and concerns about certain outcomes, it is also considered beneficial in specific circumstances, such as before ERCP. Studies on rectal Indomethacin also yield contradictory results; while some emphasize the drug\'s large reduction in PEP incidence, especially in low-risk people, others question its efficacy. We need further studies to clarify the remaining uncertainties.
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  • 文章类型: Journal Article
    药品和个人护理产品和染料的生物降解性低,毒性高,严重威胁人类健康和生态环境。因此,寻求有效的去除方法成为研究的重点。在这项研究中,通过溶剂热一锅法合成了银基金属有机骨架(Ag-MOF)和壳聚糖(CS)杂化吸附剂(Ag-MOF-CS),以去除水中的双氯芬酸钠(DCF)和酸性红1(AR1)。Ag-MOF-CS的形态和结构通过各种表征得到证实。通过改变吸附剂用量考察了吸附剂对吸附的影响,pH和其他条件。吸附动力学,吸附等温线和热力学分析。Ag-MOF-CS具有较高的吸附能力。Ag-MOF-CS对DCF和AR1的最大吸附量分别为351.75mg/g和678.83mg/g,分别。与DCF和AR1结合的吸附剂可以通过静电力,π-π相互作用,氢键。即使经过四个周期的Ag-MOF-CS,DCF去除仍可高于80%。生态友好的Ag-MOF-CS显示出处理废水的巨大潜力。
    Pharmaceuticals and personal care products and dyes have low biodegradability and high toxicity, seriously threaten the human health and ecological environment. Therefore, seeking effective removal methods has become the focus of research. In this study, silver-based metal-organic framework (Ag-MOF) and chitosan (CS) hybrid adsorbent (Ag-MOF-CS) was synthesized via solvothermal one-pot synthesis to remove diclofenac sodium (DCF) and acid Red 1 (AR1) from water for the first time. The morphology and structure of Ag-MOF-CS were confirmed by various characterizations. The effect on adsorption was investigated by changing the adsorbent dosage, pH and other conditions. The adsorption kinetics, adsorption isotherms and thermodynamics were analyzed. Ag-MOF-CS showed a high adsorption capacity. And the maximum adsorption capacity of Ag-MOF-CS for DCF and AR1 was 351.75 mg/g and 678.83 mg/g, respectively. The adsorbent bound to DCF and AR1 may via electrostatic forces, π-π interactions, hydrogen bonding. Even after four cycles of Ag-MOF-CS, the DCF removal can still be higher than 80 %. The eco-friendly Ag-MOF-CS demonstrated significant potential for utilization in treating wastewater.
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  • 文章类型: Journal Article
    多重耐药(MDR)革兰氏阴性菌的持续增加对全球公共卫生构成了严重威胁。粘菌素(COL),用作抗MDR病原体的最后一线抗生素,由于粘菌素抗性(COL-R)细菌的出现,现在处于危险之中,可能导致不良的患者结局。在这项研究中,当多粘菌素和双氯芬酸钠(DS)联合使用并用于大肠杆菌的临床COL-R菌株时,观察到了协同活性(E。大肠杆菌),肺炎克雷伯菌(K.肺炎),鲍曼不动杆菌(A.鲍曼尼),和铜绿假单胞菌(P.铜绿假)在体外和体内。棋盘法和杀时试验表明,DS,当与COL结合时,与DS和COL单一疗法相比,抗菌活性增强。结晶紫染色和扫描电镜显示,与单药治疗相比,COL-DS抑制生物膜形成。体内实验表明,DS和COL的组合降低了感染的小鼠大腿中的细菌负荷。当COL和DS联合使用时,观察到协同活性对临床COL-R菌株的大肠杆菌,肺炎克雷伯菌,鲍曼不动杆菌和铜绿假单胞菌在体外和体内。COL-DS组合的协同抗菌作用已通过进行各种体外和体内实验得到证实,这为MDR细菌引起的感染提供了新的治疗策略。
    The continuous rise of multidrug-resistant (MDR) Gram-negative bacteria poses a severe threat to public health worldwide. Colistin(COL), employed as the last-line antibiotic against MDR pathogens, is now at risk due to the emergence of colistin-resistant (COL-R) bacteria, potentially leading to adverse patient outcomes. In this study, synergistic activity was observed when colistin and diclofenac sodium (DS) were combined and used against clinical COL-R strains of Escherichia coli (E. coli), Klebsiella pneumoniae (K. pneumoniae), Acinetobacter baumannii (A. baumannii), and Pseudomonas aeruginosa (P. aeruginosa) both in vitro and in vivo. The checkerboard method and time-killing assay showed that DS, when combined with COL, exhibited enhanced antibacterial activity compared to DS and COL monotherapies. Crystal violet staining and scanning electron microscopy showed that COL-DS inhibited biofilm formation compared with monotherapy. The in vivo experiment showed that the combination of DS and COL reduced bacterial loads in infected mouse thighs. Synergistic activity was observed when COL and DS were use in combination against clinical COL-R strains of E. coli, K. pneumoniae, A. baumannii and P. aeruginosa both in vitro and in vivo. The synergistic antibacterial effect of the COL-DS combination has been confirmed by performing various in vitro and in vivo experiments, which provides a new treatment strategy for infections caused by MDR bacteria.
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  • 文章类型: Journal Article
    在这项工作中,首次使用自动溶出系统(dissoBOT)进行溶出测试。测定对乙酰氨基酚(PA)和双氯芬酸钠(DS)的disoBOT的残留(CO),它们是活性药物成分(API)。最初,通过定义检测限(LOD)进行PA和DS测定的UV-VIS分光光度法的部分方法验证,定量限(LOQ),准确度,和精度。两种API的LOD和LOQ均小于0.01mg/L。确定的线性浓度范围为PA为1.00mg/L至30.00mg/L,DS为0.50mg/L至3.50mg/L(相关系数的平方均大于0.9990,质量系数均小于1.00%)。通过计算已知浓度的标准溶液的回收率(Re)来评估该方法的准确性。两种原料药的方法被认为是准确的(PA和DS的平均Re分别为99.81%和101.43%,分别)。通过计算相对标准偏差(RSD)评价精密度。PA和DS的方法被认为是精确的,由于PA的RSD值为0.13%,DS为0.38%。在由dissoBOT系统执行的两个清洁循环中洗涤介质的体积(V),以及介质分配V,建立,其中培养基分配V符合美国药典要求。DISSOBOT系统的CO,使用自来水作为洗涤介质,被确定为两种API都低于1.00%。V为2mL的采样站的一个清洁循环的CO值在1.24-1.54%的范围内,对于5mL的V,在0.78-0.93%的范围内,并且对于10mL的V在0.27-0.36%的范围内。此外,DISSOBOT的CO,当使用两个清洁循环时,采样站(每个V为10mL)减少(CO<0.20%)。最后,DISSOBOT成功用于溶出度PA和DS表。
    In this work, an automated dissolution system (dissoBOT) was used for dissolution testing for the first time. Carry-over (CO) of the dissoBOT was determined for paracetamol (PA) and diclofenac sodium (DS), which are active pharmaceutical ingredients (APIs). Initially, partial method validation of the UV-VIS spectrophotometry method for PA and DS determination was performed by defining the limit of detection (LOD), the limit of quantification (LOQ), linear concentration range, accuracy, and precision. The LODs and LOQs were less than 0.01 mg/L for both APIs. The determined linear concentration ranges were from 1.00 mg/L to 30.00 mg/L for PA and from 0.50 mg/L to 3.50 mg/L for DS (the square of the correlation coefficient was greater than 0.9990, and the quality coefficient was less than 1.00 % for both APIs). The accuracy of the method was evaluated by calculating the recovery (Re) of the solutions of standards with known concentrations. The method for both APIs was deemed to be accurate (the average Re for PA and DS were 99.81 % and 101.43 %, respectively). Precision was evaluated by calculating the relative standard deviation (RSD). The method for PA and DS was deemed to be precise, as the RSD value for PA was 0.13 %, and for DS was 0.38 %. The volume (V) of the washing medium in both cleaning cycles performed by the dissoBOT system, as well as the medium dispensing V, were established, where the medium dispensing V was in accordance with the United States Pharmacopeia requirements. The CO of the dissoBOT system, using tap water as the washing medium, was determined to be less than 1.00 % for both APIs. The CO values for one cleaning cycle of the sampling station with a V of 2 mL was in the range of 1.24-1.54 %, for V of 5 mL was in the range of 0.78-0.93 %, and for V of 10 mL was in the range of 0.27-0.36 %. In addition, the CO of the dissoBOT, when employing two cleaning cycles of the sampling station (each V of 10 mL) was reduced (CO <0.20 %). Finally, the dissoBOT was successfully employed for the dissolution PA and DS tables.
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  • 文章类型: Journal Article
    近年来,固体剂型在儿科治疗中获得了兴趣,因为它们可以在剂量准确性和稳定性方面提供有价值的益处。特别是对于口腔分散膜(ODF),文献证明可接受性和剂量灵活性增加。在获得ODF的各种可用技术中,如溶剂浇铸,热熔挤出,和油墨印刷技术,无溶剂制备方法具有显著的优点。这项研究调查了真空压缩成型(VCM)作为一种无溶剂的制造方法,用于制备灵活剂量的儿科口腔分散膜。实验方法侧重于选择合适的增塑剂和活性药物成分的比例,双氯芬酸钠,然后研究它们对机械性能的影响,崩解时间,和ODF的药物释放曲线。进行了其他研究以获得有关固态特性的见解。VCM获得的ODF在其关键特性方面表现出足够的质量。因此,这项概念验证研究显示了如何将VCM用作生产小规模ODF的独立方法,使剂量的定制,以满足儿科患者的个性化需求。
    In recent years, solid dosage forms have gained interest in pediatric therapy because they can provide valuable benefits in terms of dose accuracy and stability. Particularly for orodispersible films (ODFs), the literature evidences increased acceptability and dose flexibility. Among the various available technologies for obtaining ODFs, such as solvent casting, hot-melt extrusion, and ink printing technologies, the solvent-free preparation methods exhibit significant advantages. This study investigated Vacuum Compression Molding (VCM) as a solvent-free manufacturing method for the preparation of flexible-dose pediatric orodispersible films. The experimental approach focused on selecting the appropriate plasticizer and ratios of the active pharmaceutical ingredient, diclofenac sodium, followed by the study of their impacts on the mechanical properties, disintegration time, and drug release profile of the ODFs. Additional investigations were performed to obtain insights regarding the solid-state properties. The ODFs obtained by VCM displayed adequate quality in terms of their critical characteristics. Therefore, this proof-of-concept study shows how VCM could be utilized as a standalone method for the production of small-scale ODFs, enabling the customization of doses to meet the individual needs of pediatric patients.
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  • 文章类型: Journal Article
    这些毒性研究旨在评估含有聚维酮K12(80mg/mL)作为关键赋形剂的新型静脉内双氯芬酸钠(37.5mg/mL)制剂在Wistar大鼠中的安全性和耐受性。该制剂以3、7和15mg/kg/天的剂量进行测试,并通过静脉内途径每天施用28天。毒物动力学估计显示血浆暴露于双氯芬酸的剂量成比例增加。该制剂在男性中耐受性良好;然而,在最高剂量(15mg/kg/天)下观察到女性(2/15)的死亡率.在15mg/kg/天的剂量下,注意到与NSAIDS相关的不良胃肠道事件以及对临床和解剖病理学的一些其他治疗相关影响,在2周恢复期结束时恢复正常。此外,在拟议的新制剂中,赋形剂聚维酮K12的含量高于批准的非活性成分数据库(IID)限值.通过在Wistar大鼠中通过静脉内途径进行的单独的28天重复剂量毒性研究,它是合格的。发现聚维酮K12在165mg/kg/天的剂量下具有良好的耐受性和安全性。在这项研究中没有观察到治疗相关的不良反应。总之,发现在雌性大鼠和雄性大鼠中重复施用含有双氯芬酸钠的新型静脉内制剂直至7mg/kg/天和15mg/kg/天的剂量是安全的。
    These toxicity studies aimed to assess the safety and tolerability of a novel intravenous diclofenac sodium (37.5 mg/mL) formulation containing povidone K12 (80 mg/mL) as the key excipient in Wistar rats. This formulation was tested at doses of 3, 7, and 15 mg/kg/day and was administered daily for 28 days by intravenous route. Toxicokinetic estimation revealed a dose-proportional increase in plasma exposure to diclofenac. The formulation was well tolerated in males; however, mortality was observed in females (2/15) at the highest dose (15 mg/kg/day). Adverse gastrointestinal events related to NSAIDS and a few other treatment-related effects on clinical and anatomic pathology were noted at the 15 mg/kg/day dose, which normalized at the end of the 2-week recovery period. In addition, the excipient povidone K12 was present in a higher amount than the approved Inactive Ingredient Database (IID) limit in the proposed novel formulation. It was qualified through a separate 28-day repeated dose toxicity study by intravenous route in Wistar rats. Povidone K12 was found to be well tolerated and safe up to a dose of 165 mg/kg/day. No treatment-related adverse effects were observed in this study. In conclusion, repeated administration of a novel intravenous formulation containing diclofenac sodium was found to be safe up to the dose of 7 mg/kg/day in female rats and 15 mg/kg/day in male rats.
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  • 文章类型: Journal Article
    表皮葡萄球菌是一种机会性病原体,通常与医疗器械相关的感染有关。其形成生物膜的倾向不仅导致慢性感染,而且加剧了抗生素耐药性的问题,需要高剂量的抗菌治疗。在这项研究中,我们探索了双氯芬酸钠的使用,一种非甾体抗炎药,作为抗表皮葡萄球菌的抗生物膜剂。在这项研究中,结晶紫染色和共聚焦激光扫描显微镜分析表明,在亚抑制浓度(0.4mM),在甲氧西林敏感型和耐甲氧西林型表皮葡萄球菌分离株中,生物膜的形成均受到显著抑制.MTT测定表明,与未处理的对照相比,0.4mM双氯芬酸钠使生物膜的代谢活性降低25.21-49.01%。此外,双氯芬酸钠的治疗导致初始细菌粘附显着降低(56.01-65.67%),生物膜发育的关键早期阶段。值得注意的是,双氯芬酸钠减少多糖细胞间粘附素(PIA)的产生,表皮葡萄球菌生物膜基质的关键成分,以剂量依赖的方式。实时定量PCR分析显示双氯芬酸钠处理下调生物膜相关基因icaA,fnba,和sigB并上调负调控基因icaR和luxS,提供潜在的机械见解。这些发现表明双氯芬酸钠通过影响初始细菌粘附和PIA合成来抑制表皮葡萄球菌生物膜形成。这强调了双氯芬酸钠作为辅助抗微生物剂在对抗葡萄球菌生物膜相关感染中的潜力。
    Staphylococcus epidermidis is an opportunistic pathogen commonly implicated in medical device-related infections. Its propensity to form biofilms not only leads to chronic infections but also exacerbates the issue of antibiotic resistance, necessitating high-dose antimicrobial treatments. In this study, we explored the use of diclofenac sodium, a non-steroidal anti-inflammatory drug, as an anti-biofilm agent against S. epidermidis. In this study, crystal violet staining and confocal laser scanning microscope analysis showed that diclofenac sodium, at subinhibitory concentration (0.4 mM), significantly inhibited biofilm formation in both methicillin-susceptible and methicillin-resistant S. epidermidis isolates. MTT assays demonstrated that 0.4 mM diclofenac sodium reduced the metabolic activity of biofilms by 25.21-49.01% compared to untreated controls. Additionally, the treatment of diclofenac sodium resulted in a significant decrease (56.01-65.67%) in initial bacterial adhesion, a crucial early phase of biofilm development. Notably, diclofenac sodium decreased the production of polysaccharide intercellular adhesin (PIA), a key component of the S. epidermidis biofilm matrix, in a dose-dependent manner. Real-time quantitative PCR analysis revealed that diclofenac sodium treatment downregulated biofilm-associated genes icaA, fnbA, and sigB and upregulated negative regulatory genes icaR and luxS, providing potential mechanistic insights. These findings indicate that diclofenac sodium inhibits S. epidermidis biofilm formation by affecting initial bacterial adhesion and the PIA synthesis. This underscores the potential of diclofenac sodium as a supplementary antimicrobial agent in combating staphylococcal biofilm-associated infections.
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  • 文章类型: Journal Article
    建立了一种结合针灸和双氯芬酸钠(DS)给药的新型治疗方法,用于类风湿关节炎(RA)的潜在治疗。DS是一种常用的抗炎和镇痛药物,但持续时间短,不良反应少。穴位是经络系统中的关键联系,并且是药物递送的潜在候选者。在这里,我们制造了一种负载DS的多层修饰针灸针(DS-MMAN),并研究了其抑制RA的能力。该DS-MMAN具有持续释放特性和体外抗炎作用。实验结果表明,与口服或关节内剂量的DS相比,微剂量的DS-MMAN可以增强镇痛作用并有效缓解关节肿胀。此外,穴位和DS的组合对炎症和关节损伤具有协同改善作用。血清中的细胞因子和T细胞分析表明,DS-MMAN的应用抑制了促炎因子的水平,并增加了抗炎因子的水平。此外,通过DS-MMAN穴位给药可以减少DS在肝脏和肾脏中的积累,这可能表现出更好的治疗效率和低毒性。本研究表明,针灸针有可能在针灸和药物之间架起桥梁,这将是传统和现代医学结合的有希望的替代方案。
    A novel therapeutic approach combining acupuncture and diclofenac sodium (DS) administration was established for the potential treatment for rheumatoid arthritis (RA). DS is a commonly used anti-inflammatory and analgesic drug but has short duration and adverse effects. Acupoints are critical linkages in the meridian system and are potential candidates for drug delivery. Herein, we fabricated a DS-loaded multilayer-modified acupuncture needle (DS-MMAN) and investigated its capacity for inhibiting RA. This DS-MMAN possesses sustained release properties and in vitro anti-inflammatory effects. Experimental results showed that the DS-MMAN with microdoses can enhance analgesia and efficiently relieve joint swelling compared to the oral or intra-articular administration of DS with gram-level doses. Moreover, the combination of acupoint and DS exerts a synergistic improvement in inflammation and joint damage. Cytokine and T cell analyses in the serum indicated that the application of DS-MMAN suppressed the levels of pro-inflammatory factors and increased the levels of anti-inflammatory factors. Furthermore, the acupoint administration via DS-MMAN could decrease the accumulation of DS in the liver and kidneys, which may express better therapeutic efficiency and low toxicity. The present study demonstrated that the acupuncture needle has the potential to build a bridge between acupuncture and medication, which would be a promising alternative to the combination of traditional and modern medicine.
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  • 文章类型: Journal Article
    目前的工作提出了一个新的,超敏绿色功能化传感器测定抗炎药双氯芬酸钠(DCF)。氧化铝(Al2O3)和氧化铈(CeO2)纳米颗粒(NPs)由于其超功能潜力而在电位和感官研究中用作出色的电活性纳米复合材料,因此引起了极大的兴趣。已使用各种光谱和显微技术证实了所形成的纳米颗粒。本研究中开发的茴香提取物介导的Al2O3/CeO2纳米复合材料(Al2O3/CeO2NCS)改性的涂覆线膜传感器用于量化散装和商业产品中的DCF。双氯芬酸钠与磷钼酸(PMA)偶联,在聚氯乙烯(PVC)和邻硝基苯基辛基醚(o-NPOE)存在的情况下,生成双氯芬酸磷钼酸盐(DCF-PM)作为活性离子对。分别使用Al2O3和CeO2的UV-可见光谱法测量270和303nm处的清晰峰,带隙为4.59eV和4.09eV。对于Al2O3,CeO2和Al2O3/CeO2NCS,XRD确定形成的纳米颗粒的微晶尺寸为30.13±8、17.72±3和35.8±0.5nm,分别。开发的传感器对DCF的测量和测定显示出极好的响应,线性在1.0×10-9和1.0×10-2molL-1之间。得出EmV=(57.76)log[DCF]+622.69。另一方面,典型的DCF-PM型电位响应范围为1.0×10-5-1.0×10-2molL-1,回归方程为EmV=(56.97)log[DCF]367.16。所提出的功能化传感器成功地测定其商业片剂中的DCF,回收率为99.95±0.3。方法验证已用于提高建议的电位技术的适用性,通过研究有关国际理事会对分析方法的协调要求的各种参数。
    The current work suggests a new, ultrasensitive green functionalized sensor for the determination of anti-inflammatory medication diclofenac sodium (DCF). Alumina (Al2O3) and cerium oxide (CeO2) nanoparticles (NPs) have attracted great interest for their use as outstanding and electroactive nanocomposite in potentiometric and sensory research due to their ultrafunctional potential. The formed nanoparticles have been confirmed using various spectroscopic and microscopic techniques. The fennel extract-mediated Al2O3/CeO2 nanocomposite (Al2O3/CeO2 NCS) modified coated wire membrane sensor developed in this study was used to quantify DCF in bulk and commercial products. Diclofenac sodium was coupled with phosphomolybdic acid (PMA) to generate diclofenac phosphomolybdate (DCF-PM) as an active ion-pair in the existence of polyvinyl chloride (PVC) and o-nitrophenyl octyl ether (o-NPOE). Clear peaks at 270, and 303 nm with band gaps of 4.59 eV and 4.09 eV were measured using UV-vis spectroscopy of Al2O3 and CeO2, respectively. The crystallite sizes of the formed nanoparticles were XRD-determined to be 30.13 ± 8, 17.72 ± 3, and 35.8 ± 0.5 nm for Al2O3, CeO2, and Al2O3/CeO2 NCS, respectively. The developed sensor showed excellent response for the measurement and assay of DCF, with a linearity between 1.0 × 10-9 and 1.0 × 10-2 mol L-1. EmV = (57.76) log [DCF] +622.69 was derived. On the other hand, the typical type DCF-PM presented a potentiometric response range of 1.0 × 10-5-1.0 × 10-2 mol L-1 and a regression equation of EmV = (56.97) log [DCF]+367.16. The functionalized sensor that was proposed was successful in determining DCF in its commercial tablets with percent recovery 99.95 ± 0.3. Method validation has been used to improve the suitability of the suggested potentiometric technique, by studying various parameters with respect to the international council harmonization requirements for analytical methodologies.
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  • 文章类型: Journal Article
    神经性疼痛是由体感神经系统的病变或疾病引起的慢性疼痛。神经性疼痛,发病率高,发病机制复杂,是临床医学和基础研究的重要领域之一。目前,处方治疗仍然不能令人满意或效果有限。需要一种减轻神经性疼痛并延长作用时间的药物制剂,尚未被发现。在这项研究中,以MIL-101(Fe)为药物载体调控双氯芬酸钠的释放,从而达到镇痛和缓释的效果。释放曲线表明,双氯芬酸钠可从MIL-101(Fe)中连续释放超过48h。MIL-101(Fe)的安全性通过苏木精和伊红以及体内ELISA测试得到证实。行为测试的结果,药代动力学,RNA测序分析表明,负载双氯芬酸钠的MIL-101(Fe)能提高机械戒断阈值,减轻备用神经损伤引起的冷异常性疼痛,将工作时间延长三天。结果表明,MIL-101(Fe)具有良好的生物相容性,而MIL-101(Fe)-DS表现出镇痛和控释特性。这些发现为神经性疼痛的临床管理和新型制剂的开发提供了科学依据。
    Neuropathic pain is chronic pain caused by a lesion or disease of the somatosensory nervous system. Neuropathic pain, with a high incidence and complex pathogenesis, is one of the most significant areas of clinical medicine and basic research. Currently, prescribed treatments are still unsatisfactory or have limited effectiveness. A medicinal preparation is required that relieves the neuropathic pain and prolongs action time, which has not yet been discovered. In this study, MIL-101 (Fe) was employed as a drug carrier to regulate the release of diclofenac sodium, thereby achieving the effect of analgesia and sustained release. The release curves demonstrated that diclofenac sodium could be continuously released from MIL-101 (Fe) for more than 48 h. There was no toxicity in vitro and in vivo, and the safety of MIL-101 (Fe) was confirmed by hematoxylin and eosin as well as ELISA tests in vivo. The results of behavioral testing, pharmacokinetics, and RNA sequencing analysis showed that MIL-101 (Fe) loaded with diclofenac sodium could enhance the mechanical withdrawal threshold and alleviate cold allodynia induced by Spared Nerve Injury, prolonging the work time by three days. The results indicated that MIL-101 (Fe) exhibited excellent biocompatibility, while the MIL-101 (Fe)-DS demonstrated analgesic and controlled-release properties. These findings provide a scientific foundation for the clinical management of neuropathic pain and the development of a novel formulation.
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