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DEVELOPMENT AND CHARACTERIZATION OF SELF-HEALING TRANSDERMAL PATCH OF LIDOCAINE FOR THE MANAGEMENT OF PAIN 利多卡因自愈性透皮贴片治疗疼痛的研究进展
Pub Date : 2023-07-07 DOI: 10.24092/crps.2023.130204
P. P, Neha Chopra, A. Chaudhuri, Harshit Kumar, Anshu Gurjar, Nidhi Sharma
Pain management is a significant challenge due to the side effects associated with commonly prescribed medications like NSAIDs and opioids. Local anesthetics, such as lidocaine, offer an alternative with fewer side effects when formulated in topical patches. Transdermal delivery systems, including heated patches, enhance drug absorption and provide targeted pain relief. This research paper aims to develop and characterize a self-heating transdermal patch of lidocaine for pain management. The drug sample of lidocaine was characterized using UV-visible spectrophotometric analysis, melting point determination, and differential scanning calorimetry. The results confirmed the purity of the drug sample. Pre-formulation studies were conducted to determine the solubility and partition coefficient of lidocaine, as well as drug-excipient interaction studies. The formulation of the lidocaine transdermal patch included the selection of excipients such as solvents, adhesives, solubilizers, and permeation enhancers. The patch was developed in three trial batches, with the final batch prepared using a drug-in-adhesive type approach. The developed patch was evaluated for physical characteristics, solvent residual content, rolling ball test, shear strength, drug crystallization, drug content, and in-vitro permeation. The results of the evaluation showed that the developed lidocaine transdermal patch had the desired physical characteristics, uniform thickness, good folding endurance, and appropriate solvent residual content. It exhibited satisfactory rolling ball test and shear strength. Microscopic examination confirmed the absence of drug crystallization. The drug content of the patch was determined to be within the desired range, and the in-vitro permeation study demonstrated successful drug release through the dialysis membrane. In conclusion, the development and characterization of a self-heating transdermal patch of lidocaine for pain management provide a promising approach for effective and targeted pain relief. The patch formulation demonstrated suitable physical properties, drug content, and permeation characteristics, suggesting its potential as an alternative pain management solution. KEYWORDS: Lidocaine, transdermal patch, pain management, self-heating, drug delivery
由于非甾体抗炎药和阿片类药物等常用处方药的副作用,疼痛管理是一项重大挑战。局部麻醉剂,如利多卡因,在局部贴剂中配制时,提供了副作用较小的替代方案。经皮给药系统,包括加热贴片,增强药物吸收并提供有针对性的疼痛缓解。本研究旨在开发和表征一种用于疼痛管理的利多卡因自热透皮贴片。采用紫外可见分光光度法、熔点测定法和差示扫描量热法对利多卡因样品进行了表征。结果证实了药物样品的纯度。进行了处方前研究,以确定利多卡因的溶解度和分配系数,以及药物与辅料的相互作用研究。利多卡因透皮贴剂的配制包括溶剂、胶粘剂、增溶剂和渗透促进剂等辅料的选择。该贴片分三批试验开发,最后一批采用药物黏附型方法制备。对制备的贴片进行物理特性、溶剂残留量、滚球试验、抗剪强度、药物结晶、药物含量和体外渗透等评价。评价结果表明,制备的利多卡因透皮贴剂具有理想的物理特性,厚度均匀,可折叠性好,溶剂残留量适中。具有良好的滚球试验性能和抗剪强度。镜检证实无药物结晶。测定该贴片的药物含量在期望范围内,体外渗透研究表明药物通过透析膜释放成功。总之,开发和表征用于疼痛管理的自热利多卡因透皮贴片为有效和有针对性的疼痛缓解提供了一种有前途的方法。该贴片配方表现出合适的物理性质、药物含量和渗透特性,表明其作为替代疼痛管理解决方案的潜力。关键词:利多卡因,透皮贴剂,疼痛管理,自热,给药
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引用次数: 0
A REVIEW ARTICLE ON CURRENT PHARMACOLOGICAL STATUS OF CARDIOPROTECTIVE PLANT 本文就心脏保护植物的药理研究现状作一综述
Pub Date : 2023-04-08 DOI: 10.24092/crps.2023.130103
Sarita Yadav, B. Yadav, Nandini Chaudhary, Rajneesh Kumar, Ravi Yadav, S. Pandey
Cardiovascular diseases involve abnormalities of the heart and blood vessels, such as coronary heart disease, hypertension, and cerebrovascular disease, and are the main cause of the increase in mortality rate in the world. Herbal plants tend to be very useful to prevent cardiovascular disease. The phytoconstituents of herbal medicinal plants like tannins, alkaloids, saponins, flavonoids, and glycosides that have the ability to prevent cardiovascular diseases. Examples such as Nerium oleander, Amaranthus viridis, Ginkgo biloba, Daucus carota, Gingerol, Tinospora cordifolia etc. Many studies investigated the cardioprotective effect of these natural products against experimentally-induced myocardial damage, and their results revealed that their potential phytochemicals exhibited significant antioxidant, anti-apoptotic, anti-inflammatory, anti-atherosclerotic activities. The review highlights the promising mechanisms and probable applications of various herbal plants, and their phytochemicals in the prevention and treatment of cardiovascular diseases. The cardioprotective plants contain a wide- variety of bioactive compound involve with diosgenin, isoflavones, sulforaphane, carotinized, catechin and quercetin are increasing the cardio protection and decreases the chances of cardiac abnormalities. KEYWORDS: Cardiovascular diseases, herbal products, phytochemicals, cardioprotective plant, Trichopus zeylanicus, cardiotoxicity
心血管疾病涉及心脏和血管的异常,如冠心病、高血压和脑血管疾病,是世界上死亡率增加的主要原因。草本植物往往对预防心血管疾病非常有用。草药植物的植物成分,如单宁、生物碱、皂苷、类黄酮和糖苷,具有预防心血管疾病的能力。例如夹竹桃、绿苋菜、银杏、胡萝卜、姜辣素、堇青花等。许多研究调查了这些天然产物对实验性心肌损伤的心脏保护作用,结果表明它们潜在的植物化学物质具有显著的抗氧化、抗凋亡、抗炎、抗动脉粥样硬化活性。本文综述了各种中草药及其化学物质在心血管疾病预防和治疗中的应用前景。心脏保护植物含有多种生物活性化合物,如薯蓣皂苷元、异黄酮、萝卜硫素、胡萝卜素、儿茶素和槲皮素等,具有增强心脏保护和降低心脏异常的作用。关键词:心血管疾病,草药制品,植物化学物质,心脏保护植物,毛霉,心脏毒性
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引用次数: 0
CROCIN AS NEUROPROTECTIVE AGONIST IN OXIDATIVE DAMAGE AND COGNITIVE DYSFUNCTION INDUCED BY ALUMINIUM CHLORIDE AND COLCHICINE IN RODENTS 藏红花素在氯化铝和秋水仙碱诱导的氧化损伤和认知功能障碍中的神经保护激动剂作用
Pub Date : 2023-04-08 DOI: 10.24092/crps.2023.130105
Deepak Tomar, M. M, Dhananjay Taumar, A. A, M. M, P. Jain, Khushi Goel, Amulya Jindal
The main constituent of saffron, Crocus sativus L., is called Crocin (CR). Water-soluble carotenoids in CR possesses anti-inflammatory, analgesic, anti-edematous, as well as anti-oxidant properties, as well as to increase the number of microtubules in sheep brain microtubules and to have neuroprotective effects. For example, Alzheimer's disease (AD), where the harm of hippocampal as well as cortical neurons results in memory as well as cognitive impairment, as well as amyotrophic lateral sclerosis (ALS), where weakness in muscle is brought on by the degeneration of spinal, bulbar, as well as cortical motor neurons, are disorders which are characterized by the progressive and irreversible loss of neurons. In the current investigation, we evaluated CR's ability to protect neurons from the oxidative harm that Colchicine (Col) and Aluminum chloride (ALCL) induce. GSH level, SOD, besides catalase reduced in the Col model's Col-treated group but was practically returned to normal in the group that received CR. When given CR instead of Col, the levels of MDA, acetylcholine esterase, and nitric oxide returned to nearly normal levels. However, in the Morris water maze test, CR significantly reduces the time it takes to reach the platform (escape latency time), indicating learning and cognitive improvement. Corresponding to this, in the passive avoidance test, the transfer delay time did not significantly increase in the CR-treated group but it did in the Col-treated group. Similar outcomes in the aluminium chloride model were attained. Thus, the present study comes to the conclusion that CR can be utilized to treat oxidative stress and illnesses linked to cognitive dysfunction, such as AD as well as Parkinson’s diseases shown against rodents resultantly. KEYWORDS: Crocin, Aluminium Chloride, Alzheimer’s disease, oxidative stress, Neurodegeneration
藏红花的主要成分是藏红花素(Crocus sativus L.)。CR中的水溶性类胡萝卜素具有抗炎、镇痛、消肿、抗氧化等特性,并能增加绵羊脑微管的微管数量,具有神经保护作用。例如,阿尔茨海默病(AD),海马和皮质神经元的损害导致记忆和认知障碍,以及肌萎缩性侧索硬化症(ALS),肌肉无力是由脊髓、球和皮质运动神经元的退化引起的,这些疾病的特征是神经元的进行性和不可逆转的丧失。在目前的研究中,我们评估了CR保护神经元免受秋水仙碱(Col)和氯化铝(ALCL)诱导的氧化损伤的能力。Col模型的Col处理组GSH、SOD和过氧化氢酶水平下降,而CR组基本恢复正常。当CR代替Col时,MDA、乙酰胆碱酯酶和一氧化氮水平恢复到接近正常水平。然而,在Morris水迷宫测试中,CR显著缩短了到达平台所需的时间(逃避潜伏期),表明学习和认知得到改善。与此相对应的是,在被动回避测试中,cr处理组的传递延迟时间没有显著增加,而col处理组有显著增加。在氯化铝模型中也得到了类似的结果。因此,本研究得出结论,CR可以用于治疗氧化应激和与认知功能障碍相关的疾病,如AD和帕金森病,结果显示在啮齿动物身上。关键词:藏红花素,氯化铝,阿尔茨海默病,氧化应激,神经变性
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引用次数: 0
SIMULTANEOUS DETERMINATION OF PHYTONADIONE AND ITS DEGRADANTS BY HPLC IN INJECTABLE EMULSION FORMULATION USED TO TREAT VKDB IN NEWBORNS 高效液相色谱法同时测定新生儿VKDB注射乳剂中植物二酮及其降解物的含量
Pub Date : 2023-04-08 DOI: 10.24092/crps.2023.130104
M. Ullah, Md. Sohel Rana, MD. Shahnowaj Bhuiyan
Phytonadione, also known as Phytomenadione or Vitamin K1 is used as an Injectable emulsion is used to Newborns for the precautionary treatment for Vitamin K Deficiency Bleeding (VKDB) during birth. In the current study, A Gradient, Sensitive & Cost effective HPLC method has been developed to determine and quantify the degradants of Phytonadione and Benzyl Alcohol into Phytonadione Injectable Emulsion. The chromatographic separation was performed by GL Sciences Inert sustain HP™ C18 (250 × 4.6 mm, 3.0 μ) column. The degradants were well separated by a gradient program started with the mixture of 25 mM Ammonium Acetate in water as buffer, pH 3.5 and Methanol in the ratio of 40: 60 V/V at the flow rate of 1.0 mL min­­‑1 and UV detection was performed at 254 nm. The degradation products from Phytonadione and Benzyl Alcohol were well resolved from the main peaks and its other impurities by the developed method. The method was validated by complying specificity/selectivity, linearity, limit of detection (LOD), limit of quantification (LOQ), accuracy and precision following ICH Q2 (R1). The developed method in this study could be applied for the analysis of routine quality control related substances of Phytonadione Injectable Emulsion, since there is no official monograph. KEYWORDS: Phytomenadione, Vitamin K, Method validation, Impurities, Degradants.
植物二酮,也被称为植物二酮或维生素K1,是一种可注射乳剂,用于新生儿在出生期间预防维生素K缺乏性出血(VKDB)。本研究建立了一种梯度、灵敏、高效的高效液相色谱法,用于测定和定量植物二酮注射乳中苯甲醇和植物二酮的降解物。色谱分离采用GL Sciences Inert sustain HP™C18 (250 × 4.6 mm, 3.0 μ)柱。以25 mM乙酸铵水溶液为缓冲液,pH为3.5,以甲醇为缓冲液,以40:60 V/V为缓冲液,流速为1.0 mL min - 1,采用梯度分离程序,在254 nm处进行紫外检测。该方法能较好地分离出植物二酮和苯甲醇的降解产物及其杂质。方法符合ICH Q2 (R1)的特异性/选择性、线性、检出限(LOD)、定量限(LOQ)、准确度和精密度验证。由于尚无正式的专著,本方法可用于植物二酮注射乳剂的常规质量控制相关物质的分析。关键词:植物烯二酮,维生素K,方法验证,杂质,降解物
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引用次数: 0
IMPROVEMENT OF DISSOLUTION RATE OF REPAGLINIDE BY UTILIZING SOLID DISPERSION TECHNIQUE 利用固体分散技术提高瑞格列奈的溶出度
Pub Date : 2023-04-08 DOI: 10.24092/crps.2023.130107
Mahendra Patel, A. Indurkhya, M. Khan
The recent study's objective was to prepare and evaluate the Repaglinide (RG) solid dispersion. RG is poorly water soluble, BCS class II drug. Repaglinide solid dispersion (RG-SD) was prepared by solvent evaporation method using different proportion of PVP K30. The prepared RG-SD was evaluated for solubility studies, drug content, in vitro dissolution, DSC studies and XRD studies. DSC and XRD studies results indicate that RG exists in amorphous form in solid dispersion. The solubility of pure RG was enhanced from 34.41±0.68 to 370.3±1.52 μg/mL in distilled water at 370 C. RG-SD (RG:PVP K30) (1:10) showed high burst release (65%) in the first 30 min. Current research concludes that Repaglinide solid dispersions using PVP-K30 (1:10) as a carrier in solid dispersions showed promising results in enhancement of repaglinide properties. KEYWORDS: Repaglinide, Solid Dispersion, PVK K30, Dissolution Rate, Solvent evaporation
最近的研究目的是制备和评价瑞格列奈(RG)的固体分散体。RG为低水溶性BCS II类药物。采用不同比例的PVP K30,采用溶剂蒸发法制备瑞格列奈固体分散体(RG-SD)。对制备的RG-SD进行溶解度研究、药物含量、体外溶出度、DSC研究和XRD研究。DSC和XRD研究结果表明,RG以非晶形式存在于固体分散体中。纯RG在370℃蒸馏水中的溶解度从34.41±0.68提高到370.3±1.52 μg/mL。RG- sd (RG:PVP K30)(1:10)在前30 min内具有较高的爆发释放(65%)。目前的研究表明,以PVP-K30(1:10)为载体的固体分散体在增强瑞格列奈性能方面表现出良好的效果。关键词:瑞格列奈,固体分散体,PVK K30,溶出率,溶剂蒸发
{"title":"IMPROVEMENT OF DISSOLUTION RATE OF REPAGLINIDE BY UTILIZING SOLID DISPERSION TECHNIQUE","authors":"Mahendra Patel, A. Indurkhya, M. Khan","doi":"10.24092/crps.2023.130107","DOIUrl":"https://doi.org/10.24092/crps.2023.130107","url":null,"abstract":"The recent study's objective was to prepare and evaluate the Repaglinide (RG) solid dispersion. RG is poorly water soluble, BCS class II drug. Repaglinide solid dispersion (RG-SD) was prepared by solvent evaporation method using different proportion of PVP K30. The prepared RG-SD was evaluated for solubility studies, drug content, in vitro dissolution, DSC studies and XRD studies. DSC and XRD studies results indicate that RG exists in amorphous form in solid dispersion. The solubility of pure RG was enhanced from 34.41±0.68 to 370.3±1.52 μg/mL in distilled water at 370 C. RG-SD (RG:PVP K30) (1:10) showed high burst release (65%) in the first 30 min. Current research concludes that Repaglinide solid dispersions using PVP-K30 (1:10) as a carrier in solid dispersions showed promising results in enhancement of repaglinide properties. KEYWORDS: Repaglinide, Solid Dispersion, PVK K30, Dissolution Rate, Solvent evaporation","PeriodicalId":11053,"journal":{"name":"Current Research in Pharmaceutical Sciences","volume":"5 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-04-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78676931","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A CONCISE REVIEW ON SPANSULES: A NEW METHOD OF DRUG DELIVERY 扼要回顾了胶囊:一种新的给药方法
Pub Date : 2023-04-08 DOI: 10.24092/crps.2023.130102
Abhilasha Bhadoriya, Trupti Shukla
Spansules are considered as an Advanced Drug Delivery System because they allow for controlled and sustained release of medication over an extended period of time. This type of delivery system can provide a constant plasma drug concentration over a wide range of time, which can improve treatment outcomes and reduce the risk of side effects. In addition to providing sustained release, Spansules can also be used to deliver multiple drugs in a single dosage form. The multi-drug regimen capability of Spansules is also beneficial, as it allows for the delivery of multiple drugs in a single dosage form. This can improve patient compliance with their medication regimen, simplify dosing, and reduce the risk of drug interactions. This can be particularly useful in cases where a patient requires treatment with multiple medications to manage a complex medical condition. Spansules can act as biphasic release drug delivery system that can be used to provide both immediate and sustained release of medication. These systems can be useful in cases where a patient requires rapid relief of symptoms followed by ongoing management over a longer period of time. Overall, Spansules are a versatile and effective drug delivery system that can provide several benefits to patients and healthcare providers. KEYWORDS: Spansules, Biphasic, Controlled release, Sustained release, Drug
胶囊被认为是一种先进的药物输送系统,因为它们允许在较长时间内控制和持续释放药物。这种类型的给药系统可以在很长的时间范围内提供恒定的血浆药物浓度,这可以改善治疗结果并降低副作用的风险。除了提供持续释放外,Spansules还可以在单一剂型中用于递送多种药物。Spansules的多药方案能力也是有益的,因为它允许在单一剂型中递送多种药物。这可以提高患者对其药物治疗方案的依从性,简化剂量,并减少药物相互作用的风险。这在患者需要多种药物治疗以控制复杂医疗状况的情况下尤其有用。胶囊可以作为两相释放给药系统,可以提供药物的即时和持续释放。这些系统在患者需要快速缓解症状并在较长时间内持续治疗的情况下是有用的。总的来说,Spansules是一种多功能和有效的药物输送系统,可以为患者和医疗保健提供者提供多种好处。关键词:胶囊,双相,控释,缓释,药物
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引用次数: 0
DEVELOPMENT AND CHARACTERIZATION OF TRANDOLAPRIL IMMEDIATE RELEASE TABLETS USING DIFFERENT SUPERDISINTEGRATING AGENTS 不同超崩解剂对特兰多普利速释片的研制与表征
Pub Date : 2023-04-08 DOI: 10.24092/crps.2023.130106
ARPNA INDURKHYA, MAHENDRA PATEL, MASHEER AHMED KHAN
A potent non-sulfhydryl prodrug, trandolapril is transformed into the active substance, trandolaprilat, in the liver. For obese individuals with mild-to-moderate essential hypertension, Trandolapril is effective and safe. The elimination t1/2 of trandolapril and trandolaprilat are approximately 6 hours and 16–24 hours, respectively. The goal of present work is to develop the Trandolapril immediate release tablet using various superdisintegrants. Crospovidone, Sodium starch glycolate and Croscarmellose sodium in concentrations of 2%, 4%, and 6% were used as superdisintegrating agents for the optimization. Direct compression technique was used to make nine formulations (IRTR 1 to IRTR 9). The powder blends of all batches were evaluated for different parameters to know the powder flow characteristics and it was found that the powder blend had excellent flow and compressibility characteristics. Then, compressed tablets were tested for quality control parameters as per the IP. In formulation IRTR1-IRTR9, disintegration time was observed 30.23 to 71.67 Sec and more than 70% drug was released in 30 min. Thus, based on evaluation results, it is concluded that formulation of immediate release (IR) tablets of Trandolapril were successfully developed. Minimum disintegration time 30.23 seconds 90.56% drug release in 30 min was obtained with IRTR3. KEYWORDS: Trandolapril, Immediate release, Crospovidone, Sodium starch glycolate, crocarmellose sodium
一种有效的非巯基前药,曲多乐普利在肝脏中转化为活性物质曲多乐普利。对于伴有轻中度原发性高血压的肥胖患者,曲多普利是安全有效的。trandolapril和trandolaprilat的消除时间分别约为6小时和16-24小时。本研究的目的是利用不同的超崩解剂制备特兰多普利速释片。以浓度分别为2%、4%和6%的交叉聚维酮、淀粉乙醇酸钠和交叉卡蜜糖钠作为超崩解剂进行优化。采用直接压缩技术制备了9个配方(IRTR 1 ~ IRTR 9),并对各批次的粉末共混物进行了不同参数的评价,以了解粉末的流动特性,发现该粉末共混物具有良好的流动特性和压缩特性。然后,根据IP测试压缩片剂的质量控制参数。制剂IRTR1-IRTR9的崩解时间为30.23 ~ 71.67秒,30 min内释药率超过70%。综合评价结果,认为特兰多乐普即刻释放片研制成功。崩解时间最短30.23 s, 30 min释药率为90.56%。关键词:曲度普利,速释型,交叉旋维酮,乙醇酸淀粉钠,豆胶糖钠
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引用次数: 0
HERBAL COMPONENTS AS AN ADVANTAGEOUS REMEDY FOR PIMPLE AND ACNE IN FACE-WASH: A SYSTEMIC REVIEW 草药成分作为一个有利的补救痘痘和痤疮在洗脸:一个系统的审查
Pub Date : 2023-04-08 DOI: 10.24092/crps.2023.130101
Naman Agarwal, A. A., Amulya Jindal
erbal formulations are in high demand on the global market. The human epidermis is the most vulnerable organ in the body to infections and disease-causing microbes. It also acts as the majorly responsible body part for respiration. As a result, it needs a great deal of care and protection. Many skin issues can occur throughout puberty due to internal component imbalances and hormone imbalances. The most prevalent skin condition is acne. The most commonly afflicted areas are the face and neck. The removal of oil from the face is a preventative measure. This will need proper cleaning and washing. Antibiotic gels and anti-acne washes or masks containing synthetic medicines are presently available on the market. Unfortunately, in addition to treating illnesses and killing infections, these medicines may have adverse effects. Various studies have demonstrated the effectiveness of herbal-based compositions for cleansing and oil removal. As a result of this necessity, we came up with the notion of using herbs and various plant derived components markedly useful in the various treatments of skin-related conditions. The characteristics of various face wash and their efficacy are reviewed in the current study comprehensively. The main objective of this study is the comparison of Ingredients used in various formulations of face wash like Neem, Aloe vera, Belpatra, Curry, Haldi, Lemon, Indian madder, Sweet flag, Lodhra, Gelling agent, Preservative, Neutralizer, Humectants, Vehicle, Perfume, Chelating agent, on the basis of evaluation and effective development of emerging techniques used in the markedly available face wash which reportedly proven as an advantageous measure of treatment.
全球市场对文字配方的需求量很大。人体表皮是人体中最容易受到感染和致病微生物侵害的器官。它也是负责呼吸的主要身体部位。因此,它需要大量的照顾和保护。由于体内成分失衡和激素失衡,许多皮肤问题会在青春期发生。最普遍的皮肤状况是痤疮。最常见的受累部位是脸部和颈部。去除脸上的油脂是一种预防措施。这需要适当的清洁和清洗。目前市场上有抗生素凝胶和含有合成药物的抗痤疮洗剂或面膜。不幸的是,除了治疗疾病和杀死感染,这些药物可能有副作用。各种研究已经证明了草药成分在清洁和去油方面的有效性。由于这种必要性,我们提出了使用草药和各种植物衍生成分的概念,这些成分在各种皮肤相关疾病的治疗中显着有用。本文对目前研究的各种洗面奶的特点及其功效进行了综述。本研究的主要目的是比较各种洗面奶配方中使用的成分,如印度楝树、芦荟、Belpatra、咖喱、Haldi、柠檬、印度madder、Sweet flag、Lodhra、胶凝剂、防腐剂、中和剂、保湿剂、助剂、香水、螯合剂,在评估和有效开发的基础上,在明显可用的洗面奶中使用的新兴技术,据报道,这些技术被证明是一种有利的治疗措施。
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引用次数: 0
RISK FACTORS OR PREDICTORS OF DEVELOPING CIPROFLOXACIN, TRIMETHOPRIM/SULFAMETHOXAZOLE AND THIRD GENERATION CEPHALOSPORIN RESISTANCE IN ESCHERICHIA COLI INFECTIONS: A SYSTEMATIC REVIEW AND META-ANALYSIS 大肠杆菌感染中发生环丙沙星、甲氧苄啶/磺胺甲恶唑和第三代头孢菌素耐药的危险因素或预测因素:一项系统综述和荟萃分析
Pub Date : 2023-01-08 DOI: 10.24092/crps.2022.120402
Deshwal Pr, Reddy Ns, F. R., A. M, T. P
The Centers for Disease Control and Prevention (CDC) estimates that by 2050, ten million people a year could be dying as a result of Anti-Microbial Resistance (AMR). An increase in resistance has been observed for trimethoprim/sulfamethoxazole followed by ciprofloxacin and third-generation cephalosporins in the management of Escherichia coli infections. To identify risk factors for ciprofloxacin (Cip-REC), trimethoprim/sulfamethoxazole (TMP/SMX-REC,) and third-generation cephalosporin (TGC-REC) resistance in Escherichia coli infection relative to controls patients. A systematic search of MEDLINE/PubMed and Embase databases identified case-control, cohort, and cross-sectional studies on risk factors for Cip-REC, TMP/SMX-REC, and TGC-REC-infected patients. A random-effects model was used to pool odds ratios (ORs) of developing resistant E. coli infection. This study was registered with PROSPERO (CRD42022297043). A total of 23 studies were included (9891 participants). Overall, 22, 8, and 11 risk factors were identified for developing Cip-REC, TMP/SMX-REC, and TGC-REC infections respectively. The prior antibiotic use [OR=3.19] reported high pooled ORs for Cip-REC infection. TMP/SMX-REC infection was associated with genitourinary abnormalities [OR=2.91]. Further analysis unveiled potential factors for TGC-REC infection; prior history of admission [OR=3.14] and hemodialysis [OR=2.20]. Prior antibiotic usage, genitourinary disorders, and admission history increase the risk of Cip-REC, TMP/SMX-REC, and TGC-REC infections. Modifiable risk factors may help prevent resistant E. coli infection. KEYWORDS: Escherichia coli, Ciprofloxacin, Trimethoprim, Sulfamethoxazole, Third Generation Cephalosporin
美国疾病控制与预防中心(CDC)估计,到2050年,每年可能有1000万人死于抗微生物耐药性(AMR)。在处理大肠杆菌感染时,观察到甲氧苄啶/磺胺甲恶唑的耐药性增加,其次是环丙沙星和第三代头孢菌素。目的:确定大肠杆菌感染中环丙沙星(cipc - rec)、甲氧苄啶/磺胺甲恶唑(TMP/SMX-REC)和第三代头孢菌素(TGC-REC)耐药的危险因素。对MEDLINE/PubMed和Embase数据库进行系统检索,确定了Cip-REC、TMP/SMX-REC和tgc - rec感染患者的危险因素的病例对照、队列和横断面研究。随机效应模型用于汇总发生耐药大肠杆菌感染的优势比(ORs)。本研究已在PROSPERO注册(CRD42022297043)。共纳入23项研究(9891名受试者)。总体而言,分别确定了22、8和11个发生Cip-REC、TMP/SMX-REC和TGC-REC感染的危险因素。既往抗生素使用[OR=3.19]报告了Cip-REC感染的高累积OR。TMP/SMX-REC感染与泌尿生殖系统异常相关[OR=2.91]。进一步分析揭示了TGC-REC感染的潜在因素;既往入院史[OR=3.14]和血液透析史[OR=2.20]。既往抗生素使用、泌尿生殖系统疾病和住院史增加了Cip-REC、TMP/SMX-REC和TGC-REC感染的风险。可改变的风险因素可能有助于预防耐药大肠杆菌感染。关键词:大肠杆菌、环丙沙星、甲氧苄啶、磺胺甲恶唑、第三代头孢菌素
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引用次数: 0
IN SILICO STUDY OF PHYTOCONSTITUENTS OF MORINGA OLEIFERA AGAINST TREHALOSE–6–PHOSPHATE PHOSPHATASE (TPP) ENZYMES 辣木植物成分抗海藻糖- 6 -磷酸磷酸酶(tpp)酶的硅片研究
Pub Date : 2023-01-08 DOI: 10.24092/crps.2022.120404
P. Bhatnagar, Neha Dangi
Numerous pathogenic microorganisms use the enzymes trehalose-6-phosphate phosphatase (TPP) to biosynthesize the sugar trehalose from trehalose-6-phosphate (T6P) as part of their infection and proliferation processes. In order to build new generation candidate medications to inhibit TPP using in silico approaches, the current work is being done. The majority of the 10 phytochemicals from Moringa oleifera that were used in docking studies with the 3D model of TPP had good binding affinities to the enzyme, with campesterol and stigmat-4-en-3-one showing the highest affinities (Binding energies of - 7.8 kcal/mole and -8.0 kcal/mole, respectively), when compared to the commonly used commercial drug isoniazid (Binding energy of –6.0 kcal/mole).The active site of TPP sequences, which coordinates Mg2+ and is necessary for catalysis, has been discovered to bind to phytochemical leads during docking. Binding poses and distance measurement of TPP-phytochemical complexes of 5-Hydroxymethylfurfural, Citronellol, Xylitol, 2,4-Di-tert-butylphenol, Palmitoleic acid, cis-Vaccenic acid, Phytol, Cyclopentane, 1,1-[3-(2-cyclopentylethyl)-1,5-pentanediyl]bis-, Campesterol and Stigmat-4-en-3-one reveals that the lead phytochemicals were in close proximity with most of the active site amino acids (distance range from 1.88 to 3.77 Aº). This demonstrates the close affinity between the enzyme and the leads, which may open the door to the development of new generation medications to treat diseases caused by pathogenic microorganisms that produce TPP. KEYWORDS: Trehalose–6–phosphate phosphatase, Binding affinity, In silico, Phytochemical, Moringa oleifera
许多病原微生物利用海藻糖-6-磷酸磷酸酶(TPP)从海藻糖-6-磷酸(T6P)生物合成海藻糖,作为其感染和增殖过程的一部分。为了利用计算机方法构建新一代抑制TPP的候选药物,目前的工作正在进行中。与TPP 3D模型对接研究的10种辣木植物化学物质中,大多数与该酶具有良好的结合亲和力,与常用的商业药物异烟酰胺(结合能为- 6.0 kcal/mol)相比,油菜甾醇和4-烯-3- 1的亲和力最高(结合能分别为- 7.8 kcal/mol和-8.0 kcal/mol)。TPP序列的活性位点协调Mg2+,是催化所必需的,已被发现在对接过程中与植物化学导联结合。5-羟甲基糠醛、香茅醇、木糖醇、2,4-二叔丁基酚、棕榈油酸、顺式异戊酸、叶绿醇、环戊烷、1,1-[3-(2-环戊乙基)-1,5-戊二基]双-、油菜籽醇和柱头-4-烯-3-one等植物化学配合物的结合姿态和距离测量表明,这些植物化学配合物与大多数活性位点氨基酸的距离为1.88 ~ 3.77 Aº。这证明了该酶与先导物之间的密切亲和力,这可能为开发新一代药物来治疗由产生TPP的病原微生物引起的疾病打开大门。关键词:海藻糖- 6 -磷酸磷酸酶,结合亲和力,硅,植物化学,辣木
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Current Research in Pharmaceutical Sciences
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