benzocaine

苯佐卡因
  • 文章类型: Journal Article
    目的本研究的目的是评估5%低共熔混合物局部麻醉药(EMLA)乳膏和20%苯佐卡因凝胶在减轻非龋齿宫颈病变(NCCL)的橡皮坝夹放置过程中疼痛的有效性。方法学在这项单盲随机临床试验中,从门诊部抽取50名成年受试者。试验组采用5%EMLA乳膏治疗3分钟,并记录视觉模拟量表(VAS)评分。对照组使用20%苯佐卡因凝胶处理,并与测试组一样重复程序。记录VAS分数后,两组的NCCL均采用复合修复法进行修复。结果在纳入的50名参与者中,70%是男性,年龄在31-67岁之间。EMLA组3分钟的平均VAS评分明显低于苯佐卡因组。结论在成人NCCL患者中,与使用20%苯佐卡因凝胶相比,使用5%EMLA乳膏3分钟在橡皮坝夹放置期间显示出更大的疼痛减轻。
    Aim The aim of this study was to evaluate the effectiveness of 5% eutectic mixture of local anesthetics (EMLA) cream and 20% benzocaine gel in reduction of pain during rubber dam clamp placement in the treatment of non-carious cervical lesions (NCCLs). Methodology In this split-mouth single-blind randomized clinical trial, 50 adult participants were selected from the outpatient department. The test group was treated using 5% EMLA cream for three minutes, and visual analog scale (VAS) scores were recorded. The comparison group was treated using 20% benzocaine gel and procedure was repeated as that in the test group. After recording the VAS scores, NCCLs in both the groups were restored using composite restoration. Results In the included 50 participants, 70% were males, with an age group of 31-67 years. The mean VAS score at 3 minutes in EMLA group was significantly lower than that in benzocaine group. Conclusion Application of 5% EMLA cream for 3 minutes showed greater pain reduction during rubber dam clamp placement as compared to 20% benzocaine gel in adult patients with NCCLs.
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  • 文章类型: Journal Article
    纳米结构脂质载体(NLC)已成为创新的药物递送系统,与其他基于脂质的载体相比,具有明显的优势,如脂质体和固体脂质纳米颗粒。苯佐卡因(BZC),使用中最古老的局部麻醉剂,通过假胆碱酯酶进行代谢,导致对氨基苯甲酸的形成,与长期使用BZC相关的过敏反应的病原体。为了减轻不良反应和提高生物利用度,BZC封装在NLC内。利用23阶乘设计,包含棕榈酸鲸蜡酯(固体脂质)的制剂,丙二醇单辛酸酯(液体脂质),并系统地制备了以PluronicF68为表面活性剂,随着固体/液体脂质质量比(60:40-80:20%)的变化,总脂质含量(15-25%),和BZC浓度(1-3%)。通过动态光散射对优化的配方进行表征,差示扫描量热法,拉曼成像,X射线衍射,小角度中子散射,纳米裂纹分析,透射电子显微镜(TEM)/低温TEM,提供对纳米颗粒结构和BZC掺入其脂质基质的见解。NLCBZC表现出显著的包封效率(%EE=96%)和在25°C下储存时的1年稳定性。在小鼠中进行的体外动力学研究和体内镇痛试验表明,NLCBZC有效地持续药物释放超过20小时,并将BZC的麻醉效果延长至18小时。因此,我们建议使用NLCBZC来减少苯佐卡因的有效麻醉浓度(从20到3%或更低),从而最大程度地减少局部施用这种麻醉剂后的过敏反应,潜在的,为疼痛管理中BZC给药的新途径铺平了道路。
    Nanostructured lipid carriers (NLC) have emerged as innovative drug delivery systems, offering distinct advantages over other lipid-based carriers, such as liposomes and solid lipid nanoparticles. Benzocaine (BZC), the oldest topical local anesthetic in use, undergoes metabolism by pseudocholinesterase, leading to the formation of p-aminobenzoic acid, a causative agent for allergic reactions associated with prolonged BZC usage. In order to mitigate adverse effects and enhance bioavailability, BZC was encapsulated within NLC. Utilizing a 23 factorial design, formulations comprising cetyl palmitate (solid lipid), propylene glycol monocaprylate (liquid lipid), and Pluronic F68 as surfactants were systematically prepared, with variations in the solid/liquid lipid mass ratios (60:40-80:20%), total lipid contents (15-25%), and BZC concentrations (1-3%). The optimized formulation underwent characterization by dynamic light scattering, differential scanning calorimetry, Raman imaging, X-ray diffraction, small-angle neutron scattering, nanotracking analysis, and transmission electron microscopy (TEM)/cryo-TEM, providing insights into the nanoparticle structure and the incorporation of BZC into its lipid matrix. NLCBZC exhibited a noteworthy encapsulation efficiency (%EE = 96%) and a 1 year stability when stored at 25 °C. In vitro kinetic studies and in vivo antinociceptive tests conducted in mice revealed that NLCBZC effectively sustained drug release for over 20 h and prolonged the anesthetic effect of BZC for up to 18 h. We therefore propose the use of NLCBZC to diminish the effective anesthetic concentration of benzocaine (from 20 to 3% or less), thus minimizing allergic reactions that follow the topical administration of this anesthetic and, potentially, paving the way for new routes of BZC administration in pain management.
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  • 文章类型: Journal Article
    进行这项研究是为了评估比斯坎湾国家公园的基线事件,佛罗里达,四种有机污染物:紫外线过滤器氧苯酮,二氧基苯甲酮,和二苯甲酮,以及局部止痛药苯佐卡因。从公园内的五个地点共抽取了35个样本,四个靠近屏障的岛屿,一个在珊瑚礁。使用与高分辨率质谱联用的液相色谱进行分析。在公园中26%的样品中检测到氧苯酮,浓度高达31ng/L。在公园中49%的样品中检测到二苯甲酮,浓度高达131ng/L。在任何样品中均未检测到苯佐卡因和二氧基苯酮。
    This research was carried out in order to assess a baseline occurrence in Biscayne National Park, Florida, of four organic contaminants: the UV filters oxybenzone, dioxybenzone, and benzophenone, as well as the topical pain reliever benzocaine. A total of 35 samples were taken from five locations within the park, four near barrier islands, and one at a coral reef. Analyses were carried out using liquid chromatography coupled to high-resolution mass spectrometry. Oxybenzone was detected in 26% of samples from the park at concentrations up to 31 ng/L. Benzophenone was detected in 49% of samples from the park at concentrations up to 131 ng/L. Benzocaine and dioxybenzone were not detected in any of the samples.
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  • 文章类型: Journal Article
    腭注射通常是痛苦的。我们的目的是比较局部冰和20%苯佐卡因凝胶在大腭神经阻滞(GPNB)注射前的预注射麻醉。
    在15-60岁需要双侧注射GPNB的患者中进行了一项随机的口开式临床试验。来自60名患者的总共120个腭部位被随机分配到A组(局部冰)或B组(20%苯佐卡因凝胶)。使用声音评估疼痛,眼睛,电机(SEM),两组均采用视觉模拟量表(VAS)。使用Mann-WhitneyU检验进行推断分析。
    参与者的平均年龄为20.5±3.9岁。A组的中位VAS评分为11分(Q1-Q3:5.25-21.75),略高于B组报告的10(Q1-Q3:4.0-26.75)。差异无统计学意义(P=0.955)。A组和B组的中位SEM评分分别为3.5(Q1-Q3:3.0-4.0)和4.0(Q1-Q3:3.0-4.0),分别,差异无统计学意义(P=0.869)。
    使用冰作为局部麻醉剂的形式用于在GPNB之前实现预注射麻醉与20%苯佐卡因凝胶一样有效。
    UNASSIGNED: Palatal injections are often painful. We aimed to compare topical ice and 20% benzocaine gel for pre-injection anesthesia before greater palatine nerve block (GPNB) injections.
    UNASSIGNED: A randomized split-mouth clinical trial was conducted among patients aged 15-60-years needing bilateral GPNB injections. A total of 120 palatal sites from 60 patients were randomly allocated to Group A (topical ice) or Group B (20% benzocaine gel). Pain was evaluated using sound, eye, motor (SEM), and the visual analog scale (VAS) in both groups. Inferential analysis was performed using the Mann-Whitney U test.
    UNASSIGNED: The mean age of the participants was 20.5 ± 3.9 years. The median VAS score for group A was 11 (Q1 - Q3: 5.25 - 21.75), which was slightly higher than the 10 (Q1 - Q3: 4.0 - 26.75) reported in group B. However, the difference was not statistically significant (P = 0.955). The median SEM score for group A and group B was 3.5 (Q1 - Q3: 3.0 - 4.0) and 4.0 (Q1 - Q3: 3.0 - 4.0), respectively, which was statistically insignificant (P = 0.869).
    UNASSIGNED: Using ice as a form of topical anesthetic for achieving pre-injection anesthesia before GPNB was as effective as 20% benzocaine gel.
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  • 文章类型: Journal Article
    五味子对人类疾病的临床效果是有据可查的;然而,关于其在控制植物病原体中的应用研究有限。这里,我们研究了它对链格孢菌生长的抑制作用,一种导致苹果收获后严重损失的真菌,被称为黑斑病。S.Chinensis果实提取物对A的生长具有很强的抑制作用,EC50为1882.00mg/L。高效液相色谱-质谱联用技术在提取物中鉴定出157个化合物,其中苯佐卡因占提取物的14.19%。抗真菌实验表明,苯佐卡因对A的抑制活性比粗提物高43.77倍。根据扫描电子显微镜,在苹果上接种A.alternata之前和之后应用苯佐卡因可以防止病原体感染并导致菌丝变形。转录组分析显示,在用苯佐卡因处理和未处理的A.alternata感染的苹果之间,有4226个基因差异表达。代谢组学分析导致了155种代谢物的鉴定。转录组和代谢组之间的相关性分析显示,苯佐卡因可能通过β-丙氨酸代谢途径抑制交替草的生长。总的来说,S.chinensis提取物和苯佐卡因是环境友好的植物基杀菌剂,具有控制A.alternata的潜力。
    The clinical effects of Schisandra chinensis against human disease are well-documented; however, studies on its application in controlling plant pathogens are limited. Here, we investigated its inhibitory effect on the growth of Alternaria alternata, a fungus which causes significant post-harvest losses on apples, known as black spot disease. S. chinensis fruit extract exhibited strong inhibitory effects on the growth of A. alternata with an EC50 of 1882.00 mg/L. There were 157 compounds identified in the extract by high performance liquid chromatography-mass spectrometry, where benzocaine constituted 14.19% of the extract. Antifungal experiments showed that the inhibitory activity of benzocaine on A. alternata was 43.77-fold higher than the crude extract. The application of benzocaine before and after A. alternata inoculation on apples prevented the pathogen infection and led to mycelial distortion according to scanning electron microscopy. Transcriptome analysis revealed that there were 4226 genes differentially expressed between treated and untreated A. alternata-infected apples with benzocaine. Metabolomics analysis led to the identification of 155 metabolites. Correlation analysis between the transcriptome and metabolome revealed that benzocaine may inhibit A. alternata growth via the beta-alanine metabolic pathway. Overall, S. chinensis extract and benzocaine are environmentally friendly plant-based fungicides with potential to control A. alternata.
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  • 文章类型: Journal Article
    苯佐卡因是一种广泛使用的局部麻醉剂;然而,关于其在眼科产品中的安全性,临床前和临床证据明显缺乏。为了解决这个问题,提出了一种综合策略,包括计算机和体外方法,用于评估苯佐卡因的眼部毒性,而无需动物试验。为了收集电脑证据,使用QSAR工具箱(v4.5)。通过体外方法评估单次暴露于两种苯佐卡因浓度(2%和20%)。进行鸡卵绒毛尿囊膜试验(HET-CAM)以评价对结膜的影响。为了研究角膜的完整性,短时间暴露试验(STE)和牛角膜不透明度和渗透性(BCOP)测定,然后进行组织病理学分析,进行了。计算机模拟和体外方法的结果都将苯佐卡因归类为无刺激性。组织病理学分析进一步肯定了在滴眼液中使用苯佐卡因的安全性,因为在评估的角膜层中没有观察到改变。这项研究提出了一种有用的联合策略,以提供有关局部麻醉剂安全性的证据,特别是表明2%和20%的苯佐卡因溶液不会引起眼睛刺激或角膜损伤。支持苯佐卡因在眼科麻醉产品开发中的潜在用途。
    Benzocaine is a widely employed local anaesthetic; however, there is a notable dearth of preclinical and clinical evidence regarding its safety in ophthalmological products. To address this, a comprehensive strategy incorporating in silico and in vitro methodologies was proposed for assessing benzocaine\'s ocular toxicity without animal testing. To collect the in silico evidence, the QSAR Toolbox (v4.5) was used. A single exposure to two benzocaine concentrations (2% and 20%) was evaluated by in vitro methods. Hen\'s Egg Chorioallantoic Membrane Test (HET-CAM) was performed to evaluate the effects on the conjunctiva. To study corneal integrity, Short Time Exposure test (STE) and Bovine Corneal Opacity and Permeability (BCOP) assay, followed by histopathological analysis, were carried out. Results from both in silico and in vitro methodologies categorize benzocaine as non-irritating. The histopathological analysis further affirms the safety of using benzocaine in eye drops, as no alterations were observed in evaluated corneal strata. This research proposes a useful combined strategy to provide evidence on the safety of local anaesthetics and particularly show that 2% and 20% benzocaine solutions do not induce eye irritation or corneal damage, supporting the potential use of benzocaine in the development of ophthalmic anesthetic products.
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  • 文章类型: Journal Article
    现代药物载体技术,例如具有小液滴尺寸和高表面积的微乳液,提高低水溶性活性成分的渗透和定位能力。这项研究的目的是创建包含夫西地酸(FA)的伤口愈合微乳液制剂,一种抗菌剂,和苯佐卡因(BNZ),局部麻醉剂.进行了表征研究,包括粘度,液滴大小,和zeta电位。载药微乳具有稳定的结构,具有-3.014±1.265mV的ζ电位和19.388±0.480nm的液滴尺寸。在体外释放和离体渗透性研究中,将微乳液与Fucidin乳膏和油性BNZ溶液进行比较。根据药物释放研究,BNZ从微乳液和BNZ溶液中的释放显示出相似的曲线(p>0.05),与Fucidin乳膏相比,FA从微乳中的释放具有更高的药物释放(p<0.001)。微乳剂对两种活性成分均呈现较低的药物渗透(p>0.05),另一方面,与对照制剂相比提供了更高的药物积累。此外,根据体外伤口愈合活性的结果,微乳剂显示出剂量依赖性的伤口愈合潜力,在最高浓度下具有最高的伤口愈合活性。据我们所知,这种开发的BNZ和FA负载的微乳液将是一个有希望的候选人,创造新的伤口愈合的机会,由于目前的活性成分,水溶性低,在单一制剂中,并实现比对照制剂更高的积累。
    Modern drug carrier technologies, such as microemulsions with small droplet sizes and high surface areas, improve the ability of low water solubility active ingredients to permeate and localize. The goal of this study was to create microemulsion formulations for wound healing that contained both fusidic acid (FA), an antibacterial agent, and benzocaine (BNZ), a local anesthetic. Studies on characterization were carried out, including viscosity, droplet size, and zeta potential. The drug-loaded microemulsion had a stable structure with -3.014 ± 1.265 mV of zeta potential and 19.388 ± 0.480 nm of droplet size. In both in vitro release and ex vivo permeability studies, the microemulsion was compared with Fucidin cream and oily BNZ solution. According to the drug release studies, BNZ release from the microemulsion and the BNZ solution showed a similar profile (p > 0.05), while FA release from the microemulsion had a higher drug release compared to Fucidin cream (p < 0.001). The microemulsion presented lower drug permeation (p > 0.05) for both active ingredients, on the other hand, provided higher drug accumulation compared to the control preparations. Moreover, according to the results of in vitro wound healing activity, the microemulsion indicated a dose-dependent wound healing potential with the highest wound healing activity at the highest concentrations. To the best of our knowledge, this developed BNZ- and FA-loaded microemulsion would be a promising candidate to create new opportunities for wound healing thanks to present the active ingredients, which have low water solubility, in a single formulation and achieved higher accumulation than control preparations.
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  • 文章类型: Journal Article
    接受动物疼痛的可能性通常需要满足各种标准。一个这样的标准是有害刺激或伤口会在刺激部位引起定向摩擦或修饰。还期望局部麻醉剂将减少这些对损害的反应。这些期望已经在十足的甲壳类动物中实现,但有人批评缺乏复制。这里,我们报道了一个关于有毒化学物质影响的实验,氢氧化钠,适用于玻璃大虾的一只眼柄。这引起了立即的逃生甩尾反应。然后,它在经过处理的眼柄上引起了齿齿的挤压和采摘,但在另一种眼柄上则不然。先前用苯佐卡因治疗也导致了立即甩尾和定向行为,这表明这个特工是令人厌恶的。随后,然而,它减少了苛性钠引起的定向行为。因此,我们证明了与十足甲壳类动物的疼痛观念一致的反应。
    Acceptance of the possibility of pain in animals usually requires that various criteria are fulfilled. One such criterion is that a noxious stimulus or wound would elicit directed rubbing or grooming at the site of the stimulus. There is also an expectation that local anaesthetics would reduce these responses to damage. These expectations have been fulfilled in decapod crustaceans but there has been criticism of a lack of replication. Here, we report an experiment on the effects of a noxious chemical, sodium hydroxide, applied to one eyestalk of the glass prawn. This caused an immediate escape tail-flick response. It then caused nipping and picking with the chelipeds at the treated eyestalk but much less so at the alternative eyestalk. Prior treatment with benzocaine also caused an immediate tail-flick and directed behaviour, suggesting that this agent is aversive. Subsequently, however, it reduced the directed behaviour caused by caustic soda. We thus demonstrated responses that are consistent with the idea of pain in decapod crustaceans.
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  • 文章类型: Journal Article
    通过具有呋喃和马来酰亚胺基团的两种类型的纤维素纳米晶体(CNCs)的Diels-Alder反应进行共价交联,获得了纤维状水凝胶。已在20至60°C范围内的各种组分比率和温度下研究了凝胶化。结果表明,可以通过改变组分的浓度和比例来优化水凝胶的流变特性。由于CNCs的刚性结构,水凝胶可以在至少5重量%的浓度下形成;然而,它在pH为5或7的水中或在HBSS缓冲液中几乎不溶胀。由于亚胺键的形成,醛基引入CNCs允许含有伯氨基的生理活性分子的缀合。这里,我们使用苯佐卡因作为与CNC水凝胶缀合的模型药物。所得药物缀合的水凝胶证明了制剂在pH7下的稳定性和苯佐卡因的pH敏感性释放,这是由于在pH<7下亚胺键的加速水解裂解。开发的药物偶联水凝胶有望作为局部麻醉的伤口敷料。
    A fibrillar hydrogel was obtained by covalent crosslinking via Diels-Alder reaction of two types of cellulose nanocrystals (CNCs) with furan and maleimide groups. Gelation has been studied at various ratios of components and temperatures in the range from 20 to 60 °C. It was shown that the rheological properties of the hydrogel can be optimized by varying the concentration and ratio of components. Due to the rigid structure of the CNCs, the hydrogel could be formed at a concentration of at least 5 wt%; however, it almost does not swell either in water with pH 5 or 7 or in the HBSS buffer. The introduction of aldehyde groups into the CNCs allows for the conjugation of physiologically active molecules containing primary amino groups due to the formation of imine bonds. Here, we used benzocaine as a model drug for conjugation with CNC hydrogel. The resulting drug-conjugated hydrogel demonstrated the stability of formulation at pH 7 and a pH-sensitive release of benzocaine due to the accelerated hydrolytic cleavage of the imine bond at pH < 7. The developed drug-conjugated hydrogel is promising as wound dressings for local anesthesia.
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  • 文章类型: Journal Article
    这项研究的目的是评估丁香酚的作用,苯佐卡因,镇静剂期间还有冰水,麻醉或安乐死过程对成年草鱼(Ctenpharyngodonidella)的福利。实验设计是随机的,并将动物分成8组。62只动物经历了适应期。用于获取草鱼基础数据的中性组不进行处理,但麻醉以收集血样并通过髓切片安乐死。其他7组接受了8次重复的7次治疗(对照组;乙醇;丁香酚50mgL-1,丁香酚250mgL-1,苯佐卡因100mgL-1,苯佐卡因300mgL-1和冰水2:1),他们的行为被观察到。收集血液样品,然后通过髓切片进行安乐死。测量生物特征数据并收集肝脏的一部分用于肝糖原分析。各组间达到麻醉阶段所需的时间有统计学差异(p<0.01)。较高浓度的苯佐卡因和丁香酚对镇静剂和麻醉剂的反应最快,分别。接受较高麻醉浓度的动物达到第五阶段,并且没有从麻醉中返回。因此,苯佐卡因和丁香酚是有效的安乐死剂。最低浓度的苯佐卡因显示出最高浓度的葡萄糖和皮质醇(p<0.05)。尽管100mgL-1浓度的苯佐卡因被广泛用作鱼类的麻醉剂,这项研究证明了它作为应激源的用途。首次提供了草鱼的压力参数基础数据。
    The aim of this study was to evaluate the effects of eugenol, benzocaine, and ice water during the sedative, anesthetic or euthanasia processes on the welfare of adult grass carp (Ctenopharyngodon idella). The experimental design was randomized and the animals were divided into eight groups. Sixty-two animals underwent an acclimation period. The neutral group used to obtain basal data of grass carp were not subjected to treatments, but anesthetized to collect blood samples and euthanized by medullary section. The others seven groups were submitted to seven treatments with eight repetitions (control group; ethanol; eugenol 50 mgL-1, eugenol 250 mgL-1, benzocaine 100 mgL-1, benzocaine 300 mgL-1, and ice water 2:1), their behavior was observed. Blood samples was collected and then euthanized by medullary sectioning. Biometric data were measured and a part of the liver was collected for hepatic glycogen analysis. There was a statistically significant difference in the time required to reach the anesthetic stage between the groups (p < 0.01). Benzocaine and eugenol at the higher concentration provided the fastest responses to sedatives and anesthetics, respectively. The animals subjected to higher anesthetic concentrations reached stage five and did not return from anesthesia, therefore, benzocaine and eugenol were effective euthanizing agents. Benzocaine at the lowest concentration showed the highest concentrations of glucose and cortisol (p < 0.05). Although benzocaine at 100 mgL-1 concentrations is widely used as an anesthetic in fish, this study demonstrated its use as a stressor agent. Basal data of grass carp for stress parameters are presented for the first time.
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