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Composition of Lipid Based Nanoemulsion for Oral Delivery of Orlistat 口服奥利司他的脂基纳米乳的组成
Pub Date : 2023-11-08 DOI: 10.36348/merjps.2023.v03i06.001
Payghan Santosh, Vaishali Kate, Sanjeevani Desai, Bhise Sandesh, Pradip Deshmukh, Atul Deshmukh
Aim: The present work focused on to formulate, evaluate and optimize lipid based nanoemulsion of orlistat to enhance drug release. Materials and Methods: Nanoemulsion was prepared using Olive oil, Tween 80, and Distilled water as components. Lipid based nanoemulsion was evaluated for its pH, Rheology study, zeta potential, conductivity, particle size analysis, transmission electron microscopy (TEM) and stability. Central composite design was utilized for the optimization purpose. Formulation variables such as the concentration of Oil (ml) (X1) and Water (ml) (X2) were investigated for their effect on viscosity (Y1) and drug content (Y2). Optimized formulation evaluated for the various parameters. Result and Discussion: The responses Y1 and Y2 for the optimized formulation were found to be 0.167 cps and 99%. Orlistat release from the optimized formulation was faster than other formulations obtained from DOE. Increased in vitro drug release of the drug from lipid based nanoemulsion suggests that the nanoemulsion could serve as potential formulation strategy for Orlistat. Conclusion: The lipid based nanoemulsion can be used as a possible alternative to traditional formulations of orlistat to improve its dissolution rate leading to enhanced bioavailability.
目的:研究奥利司他脂基纳米乳的制备、评价和优化,以促进药物释放。材料与方法:以橄榄油、吐温80和蒸馏水为原料制备纳米乳液。对脂基纳米乳的pH、流变性、zeta电位、电导率、粒径分析、透射电子显微镜(TEM)和稳定性进行了评价。采用中心组合设计进行优化设计。考察了油(ml) (X1)和水(ml) (X2)的浓度对黏度(Y1)和药物含量(Y2)的影响。对各参数进行了优化评价。结果与讨论:优化后的配方Y1和Y2的响应值分别为0.167 cps和99%。优化后的配方释放奥利司他的速度快于其他配方。脂基纳米乳的体外药物释放增加,表明该纳米乳可作为奥利司他的潜在配方策略。结论:脂基纳米乳可替代奥利司他的传统剂型,提高其溶出度,提高生物利用度。
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引用次数: 0
Study of Organophosphorus Poisoning at a Tertiary Care Teaching Hospital 某三级教学医院有机磷中毒的调查研究
Pub Date : 2023-10-23 DOI: 10.36348/merjps.2023.v03i05.001
Rumaisa Ayoub, Gulnar Fatima, Yawar Nazir
Introduction: Organophosphate (OP) insecticides inhibit both cholinesterase and pseudo-cholinesterase activities. The inhibition of acetylcholinesterase causes accumulation of acetylcholine at synapses, and overstimulation of neurotransmission occurs as a result of this accumulation. The mortality rate of OP poisoning is high. Early diagnosis and appropriate treatment is often life saving. Treatment of OP poisoning consists of intravenous atropine and oximes. The clinical course of OP poisoning may be quite severe and may need intensive care management. Methods: A retrospective study was performed on the patients with OP poisoning. Fifty patients were included. Diagnosis was performed from the history taken either from the patient or from the patient's relatives about the agent involved in the exposure. Diagnosis could was confirmed with serum and red blood cell anticholinesterase levels. Intravenous atropine and pralidoxime was administered as soon as possible. Other measures for the treatment were gastric lavage and administration of activated charcoal via nasogastric tube, and cleansing the patient's body with soap and water. The patients were intubated and mechanically ventilated if the patients had respiratory failure, a depressed level of consciousness, which causes an inability to protect the airway, and hemodynamic instability. Mechanical ventilation was performed as synchronized intermittent mandatory ventilation + pressure support mode, either as volume or pressure control. Positive end expiratory pressure was titrated to keep SaO2 above 94% with 40% FIO2. Weaning was performed using either T-tube trials or pressure support weaning. The chi-square test was used for statistical analysis. Data are presented as mean ± standard deviation. Results: There were 26 female and 24 male patients. Thirty-five were suicide attempts and 15 were accidental exposure. The gastrointestinal route was the main route in 44 patients. The most frequent signs were meiosis, change in mental status, hypersalivation and fasciculations. Ten patients (20.0%) required mechanical ventilation. Complications were observed in 35 patients. These complications were respiratory failure (14 patients), aspiration pneumonia (10 patients), urinary system infection (6 patients), convulsion (4 patients) and septic shock (1 patient). The duration of the intensive care stay was 5.2 ± 3.0 days. Discussion: Ingestion of OP compounds for suicidal purposes is a major problem, especially in developing countries. Thirty-five of our patients used the OP insecticide for suicide. The average respiratory rate of these patients increased from 22 to 38 breaths/min, which is an important sign of respiratory distress. The nurse to patient ratio was increased after these events. Early recognition of respiratory failure resulting in intubation and mechanical ventilation is a life-saving intervention for patients with OP poisoning. Respiratory failure is the most troublesome complication, which wa
有机磷杀虫剂对胆碱酯酶和伪胆碱酯酶活性均有抑制作用。乙酰胆碱酯酶的抑制导致突触中乙酰胆碱的积累,这种积累导致神经传递的过度刺激。OP中毒的死亡率很高。早期诊断和适当治疗往往可以挽救生命。OP中毒的治疗包括静脉注射阿托品和肟。OP中毒的临床过程可能相当严重,可能需要重症监护管理。方法:对OP中毒患者进行回顾性研究。纳入50例患者。诊断是根据从患者或患者亲属处取得的有关暴露所涉病原体的病史进行的。血清及红细胞抗胆碱酯酶水平可确诊。尽快静脉注射阿托品和普拉多肟。其他治疗措施为洗胃和鼻胃管给药活性炭,并用肥皂和水清洗患者身体。如果患者有呼吸衰竭,意识水平下降,导致无法保护气道和血流动力学不稳定,则对患者进行插管和机械通气。机械通气采用同步间歇强制通气+压力支持模式,控制容积或压力。滴定呼气末正压,使SaO2≥94%,FIO2≥40%。使用t管试验或压力支持脱机进行脱机。统计学分析采用卡方检验。数据以平均值±标准差表示。结果:女性26例,男性24例。35人是自杀未遂,15人是意外暴露。44例以胃肠道途径为主要途径。最常见的症状是减数分裂、精神状态改变、多涎和抽搐。10例(20.0%)患者需要机械通气。35例患者出现并发症。并发症为呼吸衰竭14例、吸入性肺炎10例、泌尿系统感染6例、惊厥4例、感染性休克1例。重症监护时间为5.2±3.0 d。讨论:以自杀为目的摄入有机磷化合物是一个主要问题,特别是在发展中国家。我们的病人中有35人使用OP杀虫剂自杀。这些患者的平均呼吸频率从22次/分增加到38次/分,这是呼吸窘迫的重要标志。在这些事件之后,护士与病人的比例增加了。早期识别导致插管和机械通气的呼吸衰竭是OP中毒患者的救命干预措施。呼吸衰竭是最麻烦的并发症,在35例患者中观察到。OP中毒患者可能因多种原因导致呼吸衰竭,包括胃内容物误吸、分泌物过多、肺炎和败血症合并急性呼吸窘迫综合征。结论:OP杀虫剂中毒是一种严重的疾病,需要快速诊断和治疗。由于呼吸衰竭是死亡的主要原因,因此仔细监测、适当管理和早期识别这一并发症可能会降低这些患者的死亡率。
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引用次数: 0
Flavonoids as Potent Inhibitor of SARS-CoV-2 Nsp13 Helicase: Grid Based Docking Approach 类黄酮作为SARS-CoV-2 Nsp13解旋酶的有效抑制剂:基于网格的对接方法
Pub Date : 2023-08-25 DOI: 10.36348/merjps.2023.v03i04.001
Shikha Singh, Jitender K Malik, G. Pavan Kumar, Sunil Kumar, Gyan Singh, Vinay Siroliya
The corona virus (COVID-19) is an enveloped RNA virus with diverse origins in both people and wildlife. It has been determined that six separate species are the cause of human disease. Viral infections have a significant impact on human disease, and one of the most recent worldwide epidemics is the emergence of the new corona. The SS-RNA virus from the enveloped corona virus family is what caused the potentially lethal SARS (Severe Acute Respiratory Syndrome) virus. In many countries throughout the world, sickness is spreading quickly. As of March 26, 2020, there has been 462,684 confirmed cases and 20,834 fatalities documented abroad. COVID-19 was deemed a pandemic by the World Health Organisation (WHO) on March 11, 2020. Numerous drug studies are now underway, and some of the results are positive. The only way to combat the virus, however, is through preventative measures as there is no vaccination. The goal of the current study was to use a molecular docking approach to evaluate flavonoids's potential against SAR-CoV-2 infection. Elucidation of the proposed mechanism of action of natural flavonoid (Quercetin, Isorhametin, Rutin and Tamaraxiten) against SAR-CoV-2 infection.
冠状病毒(COVID-19)是一种包膜RNA病毒,在人和野生动物中都有不同的来源。已经确定,六种不同的物种是导致人类疾病的原因。病毒感染对人类疾病有重大影响,最近的全球流行病之一是新冠病毒的出现。来自包膜冠状病毒家族的SS-RNA病毒是导致潜在致命的SARS(严重急性呼吸系统综合症)病毒的原因。在世界上许多国家,疾病正在迅速蔓延。截至2020年3月26日,国外共有462684例确诊病例和20834例死亡病例。2020年3月11日,世界卫生组织(世卫组织)将新冠肺炎列为大流行。目前正在进行大量的药物研究,其中一些结果是积极的。然而,对抗这种病毒的唯一方法是通过预防措施,因为没有疫苗接种。本研究的目的是利用分子对接方法评估类黄酮抗sars - cov -2感染的潜力。阐明天然类黄酮(槲皮素、异沙梅素、芦丁和他玛拉西坦)抗新冠病毒感染的作用机制。
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引用次数: 0
Oxcarbazepine: Preformulation Studies of Authoritative Part of Formulation Design 奥卡西平:处方设计权威部分的预处方研究
Pub Date : 2023-05-24 DOI: 10.36348/merjps.2023.v03i03.001
N. Sharma, Priyanka Ahirwar
Preformulation research is a stage that is started before the novel molecule is seeded. In a larger sense, it connects with studies of a molecule's physical, chemical, analytical, and medicinal properties and offers ideas about appropriate modifications that could be made to improve performance. The analysis of preformulation characteristics can contribute to the development of pharmaceutical formulations that are efficient, safe, dependable, and stable. Oxcarbazepine is an antiepileptic drug. It controls seizures or fits by declining the abnormal and excessive activity of the nerve cells in the brain.
预制剂研究是在新分子播种之前开始的一个阶段。从更大的意义上说,它与分子的物理、化学、分析和药用特性的研究有关,并提供有关适当修改以提高性能的想法。预制剂特性的分析有助于研制高效、安全、可靠、稳定的制剂。奥卡西平是一种抗癫痫药物。它通过降低大脑中神经细胞的异常和过度活动来控制癫痫发作或痉挛。
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引用次数: 0
Potential of Hepatoprotective Activity of Abelmoschus Moschatus Seed: In-Silico Validation 沙鼠种子保肝活性的潜力:计算机验证
Pub Date : 2023-04-27 DOI: 10.36348/merjps.2023.v03i02.004
Rizwan Mirza, Sunil Kumar, J. Malik
A type of wound healing known as hepatic fibrosis arises in response to chronic liver damage brought on by viruses, toxins, and medications that are detrimental to the liver. The syndrome is characterized by inflammation, which is followed by the deposition of extracellular matrix proteins and the development of scar tissue. Ephrin receptor A2 is a host cofactor that has been associated to Hepatitis C virus (HCV) entry (EphA2). The Abelmoschus moschatus seed belong to family Malvaceae. It contains sitosterol b. total phenol, flavonoids which are responsible for antioxidant, antimicrobial and free radical scavenging activity. The exact mechanism of action for the hepatoprotective action of Myricetin was still not revealed. With intent to propose the most probable mechanism of action of Myricetin the docking based computational analysis has been performed against the hepatoprotective drug targets like PPARα enzyme. Research Article
一种被称为肝纤维化的伤口愈合是对由病毒、毒素和对肝脏有害的药物引起的慢性肝损伤的反应。该综合征的特点是炎症,随后是细胞外基质蛋白沉积和瘢痕组织的发展。Ephrin受体A2是一种与丙型肝炎病毒(HCV)进入(EphA2)相关的宿主辅助因子。麻瓜属麻瓜科。它含有谷甾醇、总酚、黄酮类化合物,具有抗氧化、抗菌和清除自由基的活性。杨梅素保肝作用的确切机制尚未揭示。为了提出杨梅素最可能的作用机制,我们对PPARα酶等肝保护药物靶点进行了对接计算分析。研究文章
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引用次数: 0
Ageing and Insulin: Inter Alia Diabetes, Obesity and Fitness Concerns 老龄化和胰岛素:除其他外,糖尿病,肥胖和健康问题
Pub Date : 2023-04-27 DOI: 10.36348/merjps.2023.v03i02.005
C. Sr
This article argues the essence of insulin sensitivity versus secretion including insulin resistance in the clinical strategy for the treatment, lifestyle changes, prompt interventions and control of diabetes. Progressive decline of glucose tolerance as advanced age occurs has been associated with the pathogenesis of type 2 diabetes due to peripheral insulin resistance and impaired β cell function. In elderly persons, insulin secretion is deranged concomitantly with decreased insulin clearance rate and augmented circulating proinsulin level that ostensibly explicates age-related hyperglycemia. Insulin is associated with numerous pathophysiological processes exhibited during brain function in learning and memory, as well as the regulation of ageing, metabolic syndrome, obesity, diabetes and cardiovascular diseases in Man. Elevated chronic peripheral insulin, decreased insulin action and brain insulin contents are pathognomonic of the insulin resistance syndrome. All these are associated through specific mechanisms in the pathophysiology of ageing and insulin in concert with risk factors and the concomitant complications. Ostensibly, progressive excess insulin induces synchronous elevated levels of oxidative stress and inflammatory impacts which exacerbate or are exacerbated by advancing age, culminating as inimical consequences to healthy lifestyles, longevity or extended lifespan. Therapeutics and other healthcare measures may be beneficial in order to prevent, mitigate or amend insulin aberrations in the elderly and during the ageing process. The mainstay in managing an elderly patient with perturbed insulin action, is control of therapeutic application, as it can reverse acute terminal states. Treatment necessitates stringent and thorough expertise, knowledge and skills for optimum provision and effective cerebral, cardiovascular and skeletal protection for a healthier lifespan and longevity. This article will be of immense contribution in the understanding of the prevention, control and treatment of insulin resistance, metabolic syndrome, diabetes, obesity, cardiovascular and neurological disorders during ageing.
本文论述了胰岛素敏感性与胰岛素抵抗在糖尿病临床治疗策略、生活方式改变、及时干预和控制中的本质。随着年龄的增长,糖耐量的逐渐下降与2型糖尿病的发病机制有关,这是由于外周胰岛素抵抗和β细胞功能受损。在老年人中,胰岛素分泌紊乱伴随着胰岛素清除率降低和循环胰岛素原水平升高,这表面上解释了年龄相关性高血糖。胰岛素与学习和记忆中大脑功能中表现出的许多病理生理过程有关,也与人类衰老、代谢综合征、肥胖、糖尿病和心血管疾病的调节有关。慢性外周胰岛素升高,胰岛素作用和脑胰岛素含量降低是胰岛素抵抗综合征的典型症状。所有这些都是通过衰老和胰岛素病理生理的特定机制与危险因素和伴随的并发症相关联的。表面上看,进行性胰岛素过量导致氧化应激和炎症影响水平同步升高,随着年龄的增长而加剧或加剧,最终对健康的生活方式、寿命或延长产生不利影响。治疗和其他保健措施可能有助于预防、减轻或纠正老年人和老龄化过程中的胰岛素异常。管理胰岛素作用紊乱的老年患者的主要是控制治疗应用,因为它可以逆转急性终末期状态。治疗需要严格和全面的专业知识、知识和技能,以提供最佳和有效的大脑、心血管和骨骼保护,以实现更健康的寿命和长寿。这篇文章将对理解胰岛素抵抗、代谢综合征、糖尿病、肥胖、心血管和神经系统疾病的预防、控制和治疗做出巨大贡献。
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引用次数: 0
Adherence to Medication and Treatment Guidelines: Most Important but Mostly Avoided 遵守药物和治疗指南:最重要但大多避免
Pub Date : 2023-04-24 DOI: 10.36348/merjps.2023.v03i02.001
Abdul Kader Mohiuddin
To cure any disease, proper use of medicine or taking medicine in the correct order is required. Even patients from developed countries struggle to maintain their drug compliance. There is an odd parallel between underdeveloped, emerging nations and the so-called developed world in the West when it comes to improper medicine use. The understanding and perception of the disease is the most important factor influencing whether patients stick to their treatment plan.
要治愈任何疾病,都需要正确用药或按正确的顺序服药。即使是来自发达国家的患者也很难保持服药的依从性。不发达的新兴国家和所谓的西方发达国家在不当用药方面有着奇怪的相似之处。对疾病的认识和认知是影响患者是否坚持治疗计划的最重要因素。
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引用次数: 0
Hepatoprotective Efficacy of Selegiline: Molecular Insight 斯来吉兰的肝保护作用:分子观察
Pub Date : 2023-04-22 DOI: 10.36348/merjps.2023.v03i02.002
Megha Mishra, Sunil Kumar, J. Malik
Liver fibrosis is a form of wound healing that develops in response to persistent liver injury brought on by viruses, poisons, and medicines that are harmful to the liver. Inflammation is a hallmark of the condition, which is then followed by the formation of scar tissue via the deposition of extracellular matrix proteins. Hepatitis C virus (HCV) entrance has been linked to the host cofactor ephrin receptor A2 (EphA2). Selegiline hydrochloride is a levorotatory acetylenic derivative of phenethylamine. It is commonly referred to in the clinical and pharmacological literature as l-deprenyl. Selegiline (deprenyl) is a selective inhibitor of cerebral monoamine oxidase type B at the dosage (10 mg/day) used in patients with Parkinson's disease. Through this activity, the drug increases nigrostriatal dopamine levels, and may protect neurons against damage by free radicals and possibly exogenous neurotoxins.The exact mechanism of action for the hepatoprotective action of Selegiline was still not revealed. With intent to propose the most probable mechanism of action of Selegiline the docking based computational analysis has been performed against the hepatoprotective drug targets like PPARα enzyme.
肝纤维化是一种伤口愈合的形式,是对病毒、毒药和对肝脏有害的药物引起的持续肝损伤的反应。炎症是这种情况的一个标志,然后通过细胞外基质蛋白的沉积形成疤痕组织。丙型肝炎病毒(HCV)的进入与宿主辅助因子ephrin受体A2 (EphA2)有关。盐酸塞来吉兰是苯乙胺的左旋乙炔衍生物。在临床和药理学文献中,它通常被称为l-去戊烯醇。Selegiline (deprenyl)是一种选择性脑单胺氧化酶B型抑制剂,剂量(10mg /天)用于帕金森病患者。通过这种活性,药物增加黑质纹状体多巴胺水平,并可能保护神经元免受自由基和可能的外源性神经毒素的损害。斯来吉兰肝保护作用的确切作用机制尚不清楚。为了提出Selegiline最可能的作用机制,我们对PPARα酶等肝保护药物靶点进行了对接计算分析。
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引用次数: 0
Molecular Mechanistic Insight Spirulina as Anti-stress Agent 螺旋藻作为抗应激剂的分子机制
Pub Date : 2023-04-22 DOI: 10.36348/merjps.2023.v03i02.003
Priyanka Mishra, Sunil Kumar, J. Malik
When under stress, our body reacts by releasing hormones and triggering the nervous system. The hypothalamic-pituitary-adrenal axis, which transmits the stress response, is in charge of the neuroendocrine adaptation of the stress response. Corticotrophin releasing hormone neurons control hypothalamic-pituitary-adrenal function Increased. Many metabolic and neurological problems linked to stress are associated with the synthesis of corticotrophin releasing hormone. Gamma-aminobutyric acid (GABA) and GABAergic inhibition both play a significant role in controlling the activity of CRH neurons. Several synthetic medicines that target the GABAa receptor and activate GABAa activity are used to lessen the effects of stress. These treatments have relaxing effects but also come with a variety of negative effects. As they have no adverse effects and are harmless, anti-stress herbs are utilised as an alternative therapy to help the adrenal system. Spirulina platensis (commonly referred to as ‘Spirulina’), are well for their Immune system modulation; anti-viral activity; cancer preventive properties, and cardiovascular benefits. In present work an attempt had been made to evaluate the anti-stress potential of active constituent of spirulina by molecular docking.
当处于压力之下时,我们的身体会通过释放激素和触发神经系统来做出反应。传递应激反应的下丘脑-垂体-肾上腺轴负责应激反应的神经内分泌适应。促肾上腺皮质激素释放激素神经元控制下丘脑-垂体-肾上腺功能增高。许多与压力有关的代谢和神经问题都与促肾上腺皮质激素释放激素的合成有关。γ -氨基丁酸(GABA)和GABA能抑制均在控制CRH神经元的活性中发挥重要作用。几种针对GABAa受体并激活GABAa活性的合成药物被用来减轻压力的影响。这些疗法有放松的效果,但也有各种各样的负面影响。由于它们没有副作用并且是无害的,抗压力草药被用作帮助肾上腺系统的替代疗法。螺旋藻(通常被称为“螺旋藻”),对它们的免疫系统调节很好;抗病毒活动;预防癌症,对心血管有益。本文尝试用分子对接的方法评价螺旋藻活性成分的抗胁迫潜力。
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引用次数: 0
A Brief Review on Acne Vulgaris: Chronic Inflammatory Disease 寻常痤疮:一种慢性炎症性疾病
Pub Date : 2023-01-30 DOI: 10.36348/merjps.2023.v03i01.002
N. Verma, A. Singh, A. Maurya, A. Rai, A. Chaurasiya
Acne vulgaris (AV) is a chronic inflammatory disease rather than a natural part of the life cycle as colloquially viewed of the pilosebaceous unit (comprising the hair follicle, hair shaft and sebaceous gland) and is among the most common dermatological conditions worldwide. Some of the key mechanisms involved in the development of acne include disturbed sebaceous gland activity associated with hyperseborrhoea (that is, increased sebum production) and alterations in sebum fatty acid composition, dysregulation of the hormone microenvironment, interaction with neuropeptides, follicular hyperkeratinization, induction of inflammation and dysfunction of the innate and adaptive immunity. Grading of acne involves lesion counting and photographic methods. However, there is a lack of consensus on the exact grading criteria, which hampers the conduction and comparison of randomized controlled clinical trials evaluating treatments. Prevention of acne relies on the successful management of modifiable risk factors, such as underlying systemic diseases and lifestyle factors. Several treatments are available, but guidelines suffer from a lack of data to make evidence-based recommendations. In addition, the complex combination treatment regimens required to target different aspects of acne pathophysiology lead to poor adherence, which undermines treatment success. Acne commonly causes scarring and reduces the quality of life of patients. New treatment options with a shift towards targeting the early processes involved in acne development instead of suppressing the effects of end products will enhance our ability to improve the outcomes for patients with acne.
寻常痤疮(AV)是一种慢性炎症性疾病,而不是皮脂腺单位(包括毛囊、毛干和皮脂腺)生命周期的自然组成部分,是世界上最常见的皮肤病之一。痤疮发生的一些关键机制包括与脂腺分泌过多(即皮脂分泌增加)相关的皮脂腺活动紊乱、皮脂脂肪酸组成改变、激素微环境失调、与神经肽的相互作用、滤泡角化过度、炎症诱导以及先天免疫和适应性免疫功能障碍。痤疮的分级包括病变计数和照相方法。然而,对确切的分级标准缺乏共识,这阻碍了评估治疗的随机对照临床试验的进行和比较。痤疮的预防依赖于可改变的风险因素的成功管理,如潜在的全身性疾病和生活方式因素。有几种治疗方法可用,但指南缺乏数据,无法提出基于证据的建议。此外,针对痤疮病理生理的不同方面需要复杂的联合治疗方案,导致依从性差,这破坏了治疗的成功。痤疮通常会造成疤痕,降低患者的生活质量。新的治疗方案转向针对痤疮发展的早期过程,而不是抑制最终产品的影响,这将增强我们改善痤疮患者预后的能力。
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引用次数: 0
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Middle East Research Journal of Pharmaceutical Sciences
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