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IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-23 DOI: 10.1016/S0003-4509(24)00148-2
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引用次数: 0
Design of in-situ implant for the brain-targeted drug delivery using cross-linked gellan gum polymer through response surface methodology. 通过响应面方法学设计使用交联结冷胶聚合物的脑靶向药物原位植入物。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-16 DOI: 10.1016/j.pharma.2024.10.004
Imran Kazmi, Hemant K S Yadav, Fahad A Al-Abbasi, Muhammad Afzal, Muhammad Shahid Nadeem, Hisham N Altayb, Abhay Raizaday, Md Sadique Hussain, Haider Ali, Faisal Imam, Gaurav Gupta

The analysis aimed to prepare an in-situ implant (ISFI) formulation holding dimethyl fumarate as (a model drug) using cross-linked gellan gum by homogenization method. Cross-linking of gellan gum was done with L-cysteine to improve its gelation properties. Fourier transform infrared spectroscopy (FTIR) and (DSC) Differential scanning calorimetry were used to test the compatibility of the drug-polymer. The diverse formulations were prepared and tested using Design Expert® ver 8.0.1 software to optimize the experiment technique and employ the response surface. The tissue compatibility of the test verified the existence of non-irritants in the established formulation. All preparations contained the drug content from approximately 97.98 to 99.88%. Viscosities are ideal for injection in the optimized formulation (1,55 percent w/w in water). The optimized formula was monitored, and up to 156hours, it was found to be 95.7%. The result was that ISFI can effectively monitor and control the delivery of several powerful drug products.

该分析旨在利用均质化方法,使用交联结冷胶制备一种以富马酸二甲酯为模型药物的原位植入(ISFI)制剂。用 L-半胱氨酸对结冷胶进行交联,以改善其凝胶特性。傅立叶变换红外光谱法(FTIR)和差示扫描量热法(DSC)用于测试药物与聚合物的相容性。使用 Design Expert® ver 8.0.1 软件制备和测试了各种配方,以优化实验技术并采用响应面。组织相容性测试验证了既定配方中无刺激性物质的存在。所有制剂的药物含量约为 97.98 % 至 99.88 %。优化配方的粘度(在水中的重量比为 1.55%)非常适合注射。对优化配方进行了监测,结果表明,在 156 小时内,其药物含量为 95.7%。结果表明,ISFI 可以有效监测和控制几种强效药物的输送。
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引用次数: 0
Development and in vitro-in vivo evaluation of ocular insert containing ketorolac tromethamine and moxifloxacin hydrochloride. 开发含有酮咯酸氨基丁三醇和盐酸莫西沙星的眼药水,并对其进行体外-体内评估。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-15 DOI: 10.1016/j.pharma.2024.10.002
Krishna Koradia, Arjun Dedakia, Hiral Koradia

Purpose: Conjunctivitis is a common eye disorder that causes swelling and inflammation of the conjunctiva. Topical dosage form containing antibiotics and non-steroidal anti-inflammatory drugs are prescribed for the treatment and in order to overcome problems of conventional dosage forms the present study aims to develop an ocular insert containing moxifloxacin HCl and ketorolac tromethamine.

Methods: Insert was prepared by a solvent casting method by taking different polymers PVA, PVP K-30, and a combination of both as film-forming polymer, and glycerol as a plasticizer and characterized by various parameters like thickness, folding endurance, pH, swelling index, drug content, mechanical properties, in vitro and in vivo release study.

Results: The formulation prepared by a combination of both polymers demonstrated significantly improved properties including % elongation, tensile strength, swelling index, drug content and drug release compared to the formulation made with single polymer. The in vitro release data indicated that the batch R8 exhibited sustain release of drug (85% release in 10 hr) and following the Higuchi model for release kinetics. In vivo, study in rabbit eyes revealed the sustained release of the drug up to 16 hr with a good correlation between in vitro and in vivo release data.

Conclusion: From the study, it can be concluded that the developed ocular insert can be a promising formulation for rational therapy of conjunctivitis.

目的:结膜炎是一种常见的眼部疾病,会导致结膜肿胀和发炎。为了克服传统剂型存在的问题,本研究旨在开发一种含有盐酸莫西沙星和甲氧氯雷他敏的眼部插件:采用不同的聚合物 PVA、PVP K 30 和两者的组合作为成膜聚合物,以甘油作为增塑剂,通过溶剂浇铸法制备眼药水,并通过厚度、耐折度、pH 值、膨胀指数、药物含量、机械性能、体外和体内释放研究等各种参数对其进行表征:结果:与单一聚合物制备的配方相比,两种聚合物混合制备的配方在伸长率、拉伸强度、膨胀指数、药物含量和药物释放等方面都有明显改善。体外释放数据表明,批次 R8 表现出持续的药物释放(10 小时内释放 85%),并遵循 Higuchi 释放动力学模型。在兔子眼睛中进行的体内研究表明,药物的持续释放时间长达 16 小时,体外和体内释放数据之间具有良好的相关性:从这项研究中可以得出结论,所开发的眼用插入物是一种很有前途的配方,可用于结膜炎的合理治疗。
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引用次数: 0
An investigative review for pharmaceutical analysis of angiotensin receptor blockers: Olmesartan medoxomil. 血管紧张素受体阻滞剂的药物分析研究综述:奥美沙坦酯。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-15 DOI: 10.1016/j.pharma.2024.10.001
Vinod Ambalal Chaure, Atul Arun Shirkhedkar

Hypertension is often asymptomatic and can substantially elevate the risk of cardiovascular complications. Olmesartan medoxomil works by competitively blocking the angiotensin II receptors, preventing angiotensin II from constructing the blood vessels and releasing aldosterone. This discussion is focused on the critical analytical methods used to analyze olmesartan medoxomil in pharmaceutical and biological samples. A variety of analytical methods have been employed to both qualitatively and quantitatively determine the analyte, including high-performance thin-layer chromatography (HPTLC), high-performance liquid chromatography (HPLC), voltammetry, capillary zone electrophoresis, UV/Vis spectrophotometry, and 96-microwell assays. The review also includes official methods published in the Indian Pharmacopoeia. Based on existing literature, simple spectrophotometry and liquid chromatography are commonly used to analyze olmesartan medoxomil. These findings provide a solid foundation for future olmesartan medoxomil drug analysis research.

高血压通常没有症状,但会大大增加心血管并发症的风险。奥美沙坦酯氨丁三醇通过竞争性阻断血管紧张素 II 受体,阻止血管紧张素 II 构建血管和释放醛固酮而发挥作用。本讨论的重点是用于分析药物和生物样本中奥美沙坦酯甲珂米的关键分析方法。采用了多种分析方法来定性和定量测定该分析物,包括高效薄层色谱法(HPTLC)、高效液相色谱法(HPLC)、伏安法、毛细管区带电泳法、紫外/可见分光光度法和 96 微孔测定法。综述还包括印度药典中公布的官方方法。根据现有文献,简单的分光光度法和液相色谱法常用于分析奥美沙坦酯。这些发现为今后的奥美沙坦酯药物分析研究奠定了坚实的基础。
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引用次数: 0
Anti-malarial evaluation of selected medicinal plants traditionally used for treatment of fever, by inhibition test of heme polymerization. 通过血红素聚合抑制试验,对传统上用于治疗发烧的某些药用植物进行抗疟疾评估。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-14 DOI: 10.1016/j.pharma.2024.10.003
Arian Salimi, Maryam Hamzeloo-Moghaddam, Mahboobeh Irani, Somayeh Esmaeili

Objectives: World Health Organization (WHO) has reported 249 million cases infected by malaria worldwide and 608 thousands deaths in 2022. Investigations for new antimalarial drugs from traditional medicine have proven to be more effective and less expensive. The medicinal plants that have been used for treatment of malaria, generally known as types of fevers in traditional medicine, can be suitable candidates for evaluating antimalarial effects. The aim of the present study was to evaluate the in-vitro mechanism of antimalarial action of selected medicinal plants by inhibition test of heme detoxification (ITHD).

Material and methods: The methanol extract and fractions were prepared through maceration of the dry powdered plants. The ITHD method was carried in 96-wells plate and the percentage of heme polymerization inhibition was determined. The cytotoxicity of the effective plants were examined on MDBK cell line by MTT assay. Bioassay guided fractionation was performed exposing to size exclusion column chromatography and liquid-liquid fractionation and was assayed by the ITHD method for the sample with the least IC50 value and lowest cytotoxic effect.

Results: The methanol fraction of Viola odorata whole plant showed the most considerable results among the tested plants with IC50 171.8 μg.mL-1 beside the lowest cytotoxic effects. This fraction by the bioassay guided fractionation led to fraction SB2 and this fraction demonstrated the most effective result with lowest IC50 = 14.8 ± 3µg.mL-1 in ITHD assay.

Conclusion: Regarding the results of the present study and the traditional use of V. odorata for overcoming fever in Iranian traditional medicine, the final fraction of the plant could be proper candidate for further phytochemical and antimalarial studies.

目标:世界卫生组织(WHO)报告称,2022 年全球疟疾感染病例将达到 2.49 亿例,死亡人数将达到 60.8 万。研究证明,从传统医药中提取新的抗疟疾药物更有效、成本更低。用于治疗疟疾的药用植物(在传统医学中一般被称为发烧类型)可作为评估抗疟效果的合适候选药物。本研究的目的是通过血红素解毒抑制试验(ITHD)评估所选药用植物的体外抗疟作用机制:材料和方法:通过浸泡干粉植物制备甲醇提取物和馏分。在 96 孔板中进行血红素脱毒抑制试验,测定血红素聚合抑制率。通过 MTT 法检测有效植物对 MDBK 细胞系的细胞毒性。生物测定指导下的分馏是通过尺寸排阻柱层析和液-液分馏进行的,并采用 ITHD 法检测 IC50 值最小、细胞毒性作用最低的样品:结果:在所测试的植物中,Viola odorata 全株的甲醇馏分显示出最显著的结果,其 IC50 值为 171.8 μg.mL-1,细胞毒性效果最低。通过生物测定引导分馏,得到了馏分 SB2,该馏分在 ITHD 试验中的 IC50 = 14.8 ± 3µg.mL-1 最低,显示出最有效的结果:根据本研究的结果以及伊朗传统医学中使用 V. odorata 来治疗发烧的传统,该植物的最终馏分可作为进一步植物化学和抗疟疾研究的适当候选成分。
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引用次数: 0
[Epigenetic changes in alcohol addiction and therapeutic perspectives]. [酒精成瘾的表观遗传学变化与治疗视角]。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-05 DOI: 10.1016/j.pharma.2024.09.009
Olivier Pierrefiche

Alcohol consumption is a major public health issue. Patients with Alcohol Use Disorder (AUD) can benefit from five treatments that preferentially target membrane receptors, and whose efficacy is generally modest. However, a large body of experimental evidence points to an important role for epigenetics in the effects of alcohol consumption, and epidrugs that modify the epigenome offer an interesting alternative to current therapeutic options. This article reviews the most striking experimental evidence obtained at different ages in animal models, before comparing it with data obtained in humans and concluding on the relevance of using epidrugs. Finally, a new therapeutic option is suggested between psychedelics, recent molecules of interest, and epigenetic factors in alcohol intake.

酒精消费是一个重大的公共健康问题。酒精使用障碍(AUD)患者可以从五种优先针对膜受体的治疗方法中获益,这些治疗方法的疗效一般都不高。然而,大量实验证据表明,表观遗传学在酒精消费的影响中扮演着重要角色,而改变表观基因组的表观药物为目前的治疗方案提供了一个有趣的替代选择。本文回顾了在不同年龄的动物模型中获得的最引人注目的实验证据,然后将其与在人类中获得的数据进行比较,并就使用表观药物的相关性得出结论。最后,文章在迷幻药、最新的相关分子和酒精摄入中的表观遗传因素之间提出了一种新的治疗方案。
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引用次数: 0
[Risk analysis applied to the monitoring of immunosuppressor concentrations in lung transplant recipients]. [应用于肺移植受者免疫抑制剂浓度监测的风险分析]。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-29 DOI: 10.1016/j.pharma.2024.09.010
Agathe Landoas, Romane Chapuis, Amandine Briault, Quentin Perrier, Pierrick Bedouch

Mastering and monitoring immunosuppressant concentrations is central to the care of lung transplant patients and involves multiple stakeholders. The objective is to conduct a risk analysis to evaluate the impact of various actions taken. The lung transplantation team was convened to carry out a failure mode effect analysis. The process was divided into stages where different risks were identified. The risk priority number (RPN) (severity, frequency, detectability) and risk level of criticality (frequency, severity) were established before implementation of actions (before 2009) and then after (in 2022) to classify risks according to four levels of criticality. The implemented actions included the establishment of a quality assurance process, computerization of monitoring, and double analysis by a physician/pharmacist pair. Thirty-two risks were identified during the four stages of the process: biological sampling (n=13), reception (n=3), analysis and treatment of levels (n=5), transmission of information/prescriptions to the patient (n=11). The total raw RPN (before 2009) was 839, with 12 major risks. The current total RPN (in 2022) was 452 (a decrease of 46.1%), with 7 major risks identified. The analysis enabled the objective evaluation of the effectiveness of the actions taken. The most secure stage of the process is the reception of residual level results. Efforts should focus on empowering and involving patients, as well as engaging local stakeholders in collaboration with the specialized transplantation team.

掌握和监测免疫抑制剂浓度是肺移植患者护理的核心,涉及多个利益相关方。我们的目标是进行风险分析,以评估所采取的各种行动的影响。肺移植团队被召集起来进行故障模式影响分析。该过程被划分为若干阶段,在这些阶段中确定了不同的风险。在实施行动之前(2009 年之前)和实施行动之后(2022 年),分别确定了风险优先级编号(RPN)(严重性、频率、可检测性)和风险临界等级(频率、严重性),将风险按四个临界等级分类。已实施的行动包括建立质量保证流程、监测计算机化以及由一对医生/药剂师进行双重分析。在该流程的四个阶段中发现了 32 项风险:生物采样(13 项)、接收(3 项)、分析和处理水平(5 项)、向患者传输信息/处方(11 项)。原始 RPN 总数(2009 年前)为 839,主要风险为 12。目前的 RPN 总数(2022 年)为 452(下降了 46.1%),发现了 7 个重大风险。该过程中最安全的阶段是接收剩余级结果。工作重点应放在增强患者的能力和参与度上,并让当地利益相关者与专业移植团队合作。
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引用次数: 0
Review on novel pharmaceutical applications of hupu gum: A versatile natural polymer. 综述胡柚胶的新型药物应用:一种多功能天然聚合物。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-19 DOI: 10.1016/j.pharma.2024.09.008
Rajeswari Aleti, Monika Nijhawan, Pavan Kumar Thota, Bhavana Jidige

The pharmaceutical research on natural excipients with diverse physicochemical properties useful in various novel drug delivery systems is a growing interest. The market for natural gums like hupu gum (gum kondagogu) is growing globally, driven by increasing consumer preference for natural and sustainable ingredients. This review covers botanical origin, geographical distribution, chemical constituents, identification tests, toxicology studies and potential applications of hupu gum in novel drug delivery systems. Emphasis is placed on its traditional uses in indigenous medicine and current research findings and patents that highlight its emulsifying, stabilizing, film forming, and thickening properties. Hupu gum is a tree exudate from Cochlospermum religiosum belonging to the family Bixaceae. It is traditionally used for various medicinal and industrial purposes as it has a unique chemical composition and physical properties. Moreover, the current research and use of hupu gum as a biopolymer in the formulation and stabilization of nanoparticles (NP) is expanding the application spectrum of hupu gum. This writeup typically conclude with insights into future research directions, such as, exploring new applications, or enhancing its functional properties through modification.

对具有各种理化特性、可用于各种新型给药系统的天然辅料进行制药研究的兴趣与日俱增。受消费者对天然和可持续成分日益增长的偏好推动,hupu 胶(kondagogu 胶)等天然树胶的市场在全球范围内不断增长。本综述介绍了胡柚胶的植物起源、地理分布、化学成分、鉴定测试、毒理学研究以及在新型给药系统中的潜在应用。重点介绍了其在本土医药中的传统用途,以及突出其乳化、稳定、成膜和增稠特性的当前研究成果和专利。Hupu 树胶是一种从属于 Bixaceae 的 Cochlospermum religiosum 中提取的树木渗出物。由于它具有独特的化学成分和物理特性,传统上被用于各种医药和工业用途。此外,目前将胡柚胶作为一种生物聚合物用于纳米颗粒(NP)的配制和稳定的研究正在扩大胡柚胶的应用范围。本文最后将对未来的研究方向提出见解,如探索新的应用或通过改性提高其功能特性。
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引用次数: 0
Study of the toxicity of the essential oil of Brocchia cinerea. 雏菊精油的毒性研究。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-18 DOI: 10.1016/j.pharma.2024.09.007
Mohammed Tahar Ben Moussa, Said Nadji, Nawel Achachi, Safa Chaira, Rafika Laiche, Soumaya Boudjemaa, Abdelhakim Bounab, Hassina Harkat, Youcef Hadef

Brocchia cinerea is a North African plant belonging to the Asteraceae family, widely utilized in Algerian folk medicine to treat a variety of illnesses. These therapeutic virtues are mainly due to the plant essential oil. The chemical components of this oil were identified using GC-MS, and the variability in these components' levels was examined in nine samples that were taken at different times from two locations in Algeria's northern Sahara. The contents of the essential oil were found to consist of eight components, varying in concentrations: beta-thujone (46.80%), 1-Methyl-2-(1' methylethenyl) -3'- ethenylcyclopropylmethanol (14.59%), 1,8-Cineole (12.63%), limonen-10-ol (9.47%), 1(7),3,8 o Menthatriene (3.45%), and (-)-Camphor (2.11%). Toxicity studies were conducted in order to assess the safety of the essential oil, namely: LD50 estimation and biochemical blood parameters evaluation. The results showed an LD 50 of 507.5mg/kg close to the LD50 of Beta-thujone (442mg/kg): the main component of the essential oil, making it accountable for the major toxicity. The apparition of seizures as toxic manifestations for higher concentrations confirmed that. The essential oil of Brocchia was noted to be classified as slightly, weakly toxic, and the Beta-thujone contents showed to be within the regulatory accepted values, which makes the use of Brocchia safe within the indicated standards.

Brocchia cinerea 是一种属于菊科的北非植物,在阿尔及利亚民间医学中被广泛用于治疗各种疾病。这些治疗功效主要归功于植物精油。我们使用气相色谱-质谱(GC-MS)对这种精油的化学成分进行了鉴定,并在阿尔及利亚撒哈拉沙漠北部两个地方不同时间采集的九个样本中研究了这些成分含量的变化。研究发现,精油中含有八种不同浓度的成分:β-�侧酮(46.80%)、1-甲基-2-(1'甲基乙烯基)-3'-乙烯基环丙基甲醇(14.59%)、1,8-噌烯(12.63%)、柠檬烯-10-醇(9.47%)、1(7),3,8 邻薄荷三烯(3.45%)和 (-)- 樟脑(2.11%)。为了评估精油的安全性,我们进行了毒性研究,即半数致死剂量估计和血液生化参数评估。结果显示,LD50 为 507.5 毫克/千克,接近精油主要成分 Beta-Thujone 的 LD50(442 毫克/千克),因此它是主要的毒性成分。更高浓度的毒性表现为癫痫发作,这也证实了这一点。人们注意到,肉桂精油被归类为轻微、弱毒性,而 Beta-Thujone 的含量显示在监管机构认可的值范围内,这使得肉桂的使用在指定标准内是安全的。
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引用次数: 0
[Construction of a methodology for clinical evaluation of medical devices using simulation tools and illustration through three studies]. [利用模拟工具构建医疗器械临床评估方法并通过三项研究加以说明]。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-12 DOI: 10.1016/j.pharma.2024.09.003
Cordélia Salomez-Ihl, Claire Chapuis, Pierre Albaladejo, Marielle Picard, Aline Baron, Paz Pardo Garcia, Jean-Noël Evain, Joris Giai, Maud Barbado, Alexandre Moreau-Gaudry, Jean-Luc Bosson, Julien Picard, Pierrick Bedouch

Introduction: European regulations have recently moved towards more stringent requirements for demonstrating the safety and performance of medical devices (MDs).

Objective: To apply an innovative testing method using medical simulation to the evaluation of three medical devices at different stages of their life cycle.

Method: The methodology for evaluating DMs using simulation is based on seven stages: definition of the context, training, construction of a scenario to test the DM, validation of the scenario, realization of the scenario, evaluation of the scenario by the players and validation and exploitation of the results.

Results: Our evaluation methodology enabled us to assess three DMs at different stages of their development: a respiratory protection device at the initial stage (prototype definition), a respiratory protection mask (prototype optimization) and bottle adapters (post-marketing).

Conclusion: Simulation is a valuable tool for evaluating DM. The proposed methodology enables it to be used and adapted to different contexts. It responds to the specificities of clinical evaluation of this class of products, and helps to better anticipate certain risks.

导言:欧洲法规最近对医疗设备(MD)的安全性和性能提出了更严格的要求:目的:采用一种创新的测试方法,利用医学模拟对三种医疗器械在其生命周期的不同阶段进行评估:方法:使用模拟评估 DM 的方法基于七个阶段:定义背景、培训、构建测试 DM 的情景、验证情景、实现情景、参与者评估情景以及验证和利用结果:我们的评估方法使我们能够评估处于不同开发阶段的三种 DM:初始阶段的呼吸保护装置(原型定义)、呼吸保护面罩(原型优化)和瓶子适配器(上市后):结论:模拟是评估 DM 的重要工具。结论:模拟是评估 DM 的重要工具,建议的方法使其能够在不同情况下使用和调整。它符合这类产品临床评估的特殊性,有助于更好地预测某些风险。
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引用次数: 0
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Annales pharmaceutiques francaises
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