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[Emergence of antifungal resistance: A creeping environmental threat?] 抗真菌耐药性的出现:一种逐渐蔓延的环境威胁?]
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-12-13 DOI: 10.1016/j.pharma.2024.12.010
Guillaume Decocq, Jean-Noël Colin, Anne-Lise Bienvenu

Antifungal resistance in humans is a clinical reality of increasing incidence that raises problems for patient care. In this current event, we discuss the link that can be made between the presence of antifungals in the environment and the development of resistance in humans, as well as the ecotoxicology of antifungals. The presence of antifungals in the environment has a health, but also an ecological impact. A "One Health" approach will help to address this environmental health challenge.

人类抗真菌药耐药是一种发病率不断增加的临床现实,给患者护理带来了问题。在本次事件中,我们讨论了环境中抗真菌药物的存在与人类耐药性的发展之间的联系,以及抗真菌药物的生态毒理学。抗真菌剂在环境中的存在不仅对健康有影响,而且对生态也有影响。“同一个健康”办法将有助于应对这一环境卫生挑战。
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引用次数: 0
Amorolfine hydrochloride loaded solid lipid nanoparticles: Preparation, characterization and ex vivo nail permeation study to treat onychomycosis. 盐酸阿莫罗芬载固体脂质纳米颗粒:制备、表征及体外甲渗透治疗甲癣的研究。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-12-10 DOI: 10.1016/j.pharma.2024.12.002
Tasleem Ahmed, Nithya Shanthi, Arun Kumar Mahato

Onychomycosis is a disease of the nail plate caused by fungi, leading to the progressive defacing of the nail. The infection requires a longer period of treatment orally and topically. The treatment with the topical route is difficult due to the low availability of drugs across the infected nail. This failure in topical treatment is the drawback of the conventional drug delivery system (DDS), particularly drug penetration issues across the nail plate. The solid lipid nanoparticle (SLN) approach was used to overcome such issues. The drug amorolfine hydrochloride (AOF) was incorporated into SLN by using the micro-emulsion cold dilution method. Monostrearin and stearic acid were used as solid lipids in the formulation of drug-loaded SLNs. The nanoparticle formulation was optimized by varying the type of solid lipids and bile salts. Sodium taurocholate (STC) and sodium tauroglycholate (STG) are the bile salts used as biosurfactants in the formulation. The SLNs prepared with stearic acid and STG demonstrated higher drug encapsulation efficiency (71.73%) and drug loading efficiency (13.03%) than monostearin. Bile salts have affected the particle size range and STG was found to produce smaller size particles with stearic acid (406nm) than STC. Process parameter homogenization speed was also optimized and 403 relative centrifugal force (RCF) was optimal to produce smaller-size particles (406nm). The drug permeation through the nail plate and anti-fungal studies were also performed for AOF-SLNs loaded cream and marketed cream (Amfocin). The SLNs have improved the permeation (1.63-fold) and anti-fungal activity (2.50-fold) of AOF. Transmission electron microscopy (TEM) images revealed a spherical shape of SLNs with no aggregation. The physical stability was performed and SLNs have higher stability at refrigeration storage. The SLNs were incorporated in cream for the final application for onychomycosis. The analytical method of high-performance liquid chromatography (HPLC) was used for the quantification of AOF in the formulations.

甲真菌病是一种由真菌引起的甲板疾病,导致甲的进行性损伤。这种感染需要较长时间的口服和局部治疗。局部途径的治疗是困难的,因为药物在感染指甲的低可用性。这种局部治疗的失败是传统药物输送系统(DDS)的缺点,特别是药物穿过甲板的渗透问题。固体脂质纳米颗粒(SLN)方法被用来克服这些问题。采用微乳冷稀释法将盐酸阿莫罗芬(AOF)掺入SLN。以单链素和硬脂酸为固体脂质,制备载药sln。通过改变固体脂质和胆汁盐的类型,优化了纳米颗粒的配方。牛磺酸胆酸钠(STC)和牛磺酸胆酸钠(STG)是配方中用作生物表面活性剂的胆汁盐。以硬脂酸和STG为原料制备的sln包封效率为71.73%,载药效率为13.03%。胆汁盐影响颗粒大小范围,发现STG与硬脂酸(406 nm)产生的颗粒比STC更小。同时对工艺参数进行了优化,以403相对离心力(RCF)为最优,可制得较小粒径(406 nm)的颗粒。载aof - sln乳膏和市售乳膏(Amfocin)也进行了甲板药物渗透和抗真菌研究。sln提高了AOF的渗透性(1.63倍)和抗真菌活性(2.50倍)。透射电子显微镜(TEM)图像显示sln为球形,无聚集。结果表明,sln在冷藏条件下具有较高的稳定性。sln被掺入乳膏中,最终用于治疗甲癣。采用高效液相色谱法(HPLC)定量测定制剂中AOF的含量。
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引用次数: 0
Handling and decontamination of live medications: What challenges for hospital pharmacies in France? 活药的处理和消毒:法国医院药房面临的挑战是什么?
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-12-09 DOI: 10.1016/j.pharma.2024.12.003
Adélie Riazi, Élodie Allouis, Céline Sakr, Muriel Paul, Morgane Renault-Mahieux, Muriel Carvalho

Objectives: To review the literature and national practices concerning the handling and decontamination of live medications, in order to revise our local practices.

Methods: Literature searches and questionnaire sent to establishments handling live medications on several themes, including: preparation activity, circuits, preparation equipment, decontamination techniques and agents, personal protective equipment, viruses and genetically modified organisms.

Results: Twenty establishments responded to the questionnaire (response rate: 66%) with 16 responses usable. The main live medications handled were viral vector (n=16) or cell-based gene therapies (n=14). The majority of respondents handled at least three types of live medication. The most popular and the most used preparation equipment was the biosafety cabinet (13/16). Handling was carried out in 9/16 establishments on a single piece of equipment, and in 7/16 on several. All the establishments decontaminated between two preparations of different types of live medication, and 15/16 between two preparations of the same type. None used ultraviolet decontamination. Although recommended in the literature, only five respondents distinguished between naked and enveloped viruses for decontamination. Seven out of 16 establishments had specific decontamination procedures for genetically modified organisms. There were few or no guidelines from French competent authorities or learned societies.

Conclusions: The diversification of live medications is not accompanied by guidelines or scientific publications, which makes risk assessment difficult for hospital pharmacists. Nevertheless, this work has enabled us to take stock of current practices and revise our protocols, even if the decisions we take are still based on free will.

目的:回顾有关活药处理和去污的文献和国家实践,以改进我国的做法。方法:对处理活药的机构进行文献检索和问卷调查,主题包括:制剂活动、电路、制剂设备、去污技术和制剂、个人防护装备、病毒和转基因生物。结果:20家机构回复了问卷(回复率:66%),其中16份回复可用。处理的主要活体药物是病毒载体(n=16)或基于细胞的基因治疗(n=14)。大多数受访者至少使用过三种现场用药。使用最多的制备设备是生物安全柜(13/16)。2016年9月,各机构对一件设备进行了处理,2016年7月对几件设备进行了处理。两种不同类型的活药制剂之间的所有场所进行消毒,同一类型制剂之间的15/16进行消毒。没有人使用紫外线消毒。虽然在文献中建议,但只有五个答复者区分裸病毒和包膜病毒进行净化。16家机构中有7家对转基因生物有特定的净化程序。法国主管当局或学术团体很少或根本没有指导方针。结论:活药多样化缺乏相关指南和科学出版物,给医院药师的风险评估带来困难。尽管如此,这项工作使我们能够评估当前的实践并修改我们的协议,即使我们做出的决定仍然基于自由意志。
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引用次数: 0
Drug shortages in Canada, 2019-2023: A descriptive study. 2019-2023年加拿大药品短缺:一项描述性研究
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-12-05 DOI: 10.1016/j.pharma.2024.12.001
Ilona Béatrix, Elsa Bonnabry, Suzanne Atkinson, Denis Lebel, Jean-François Bussières

Context: Drug shortages impact patients from all countries. According to the Pharmaceutical Group of the European Union, most Europe countries reported a worsening of shortages in 2023.

Objective: To describe drug shortage episodes in Canada over a recent 4-year period.

Methods: This study focused on drug shortage episodes over the 52-month period from September 1, 2019, to December 31, 2023. Two data sources were used: the Canadian mandatory reporting website (both community and hospital settings) and hospital wholesaler data. Only descriptive statistical analyses were performed.

Results: From September 1, 2019, to December 31, 2023, a total of 10,975 drug shortage episodes and 1087 discontinuations were reported on the Canadian website, whereas 2562 drug shortage episodes were reported by the hospital wholesaler. The median duration of episodes was 51days according to reports at the Canadian website data versus 145days according to the wholesaler's data. The Canadian website data referred to a total of 184 manufacturers, whereas wholesaler data encompassed 83 manufacturers. Only 86 episodes were rated as Tier 3.

Conclusions: This study highlights the high number of drug shortages in Canada in recent years, both in the overall market and in the hospital market. Although the median duration of episodes has decreased across the country, the number of manufacturers involved has increased. The danger lies in considering the current situation as inevitable, normal and persistent.

背景:药物短缺影响着所有国家的患者。据欧盟制药集团(Pharmaceutical Group of European Union)称,大多数欧洲国家报告称,2023年药品短缺将加剧。目的:描述近4年来加拿大药品短缺事件。方法:本研究重点关注2019年9月1日至2023年12月31日52个月期间的药品短缺事件。使用了两个数据来源:加拿大强制性报告网站(社区和医院设置)和医院批发商数据。仅进行描述性统计分析。结果:2019年9月1日至2023年12月31日,加拿大网站共报告了10975起药品短缺事件和1087起停药事件,而医院批发商报告了2562起药品短缺事件。根据加拿大网站数据的报告,发作的中位持续时间为51天,而根据批发商的数据为145天。加拿大网站的数据涉及184家制造商,而批发商的数据包括83家制造商。只有86集被评为三级。结论:这项研究突出了近年来加拿大的药品短缺问题,无论是在整体市场还是在医院市场。尽管全国范围内的平均发作时间有所减少,但涉及的制造商数量却有所增加。危险在于认为目前的情况是不可避免的、正常的和持续的。
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引用次数: 0
Development of mesalamine loaded-fenugreek gum decorated pectin microspheres for colonic drug delivery: Ex-vivo and in-vitro characterizations. 美沙拉胺负载胡芦巴胶装饰果胶微球结肠给药的发展:离体和体外表征。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-11-29 DOI: 10.1016/j.pharma.2024.11.006
Pruthvi P Khamkar, Kalpeshkumar S Wagh, Sopan N Nangare, Sachin S Mali, Gaurav S Patil

Mesalamine (MES) is a preferred therapeutic agent for managing various colon disorders, including inflammatory bowel diseases (IBD). However, conventional oral dosage forms of MES face significant limitations, which reduce their effectiveness in managing these conditions. To overcome these challenges, advanced dosage forms of MES are essential. Fenugreek gum (FG), a natural polysaccharide with non-toxicity, ease of synthesis, biodegradability, and biocompatibility, was selected as a key component for developing a novel delivery system. Calcium ion crosslinked MES-incorporated FG-decorated pectin microspheres (FG@MES/PM) were successfully designed for colon-specific drug delivery using an ionotropic gelation technique. The microspheres exhibited favorable physicochemical characteristics, including a particle size of 586nm, a polydispersity index of 0.348, an entrapment efficiency of 85.20±1.02%, and a drug content of 98.52±0.96%. Ex vivo mucoadhesion tests demonstrated strong mucoadhesive properties, highlighting the potential of FG@MES/PM to adhere effectively to the colonic mucosa. In vitro drug release studies showed a modified release profile, with 99.02±1.80% MES released over 24h. Release kinetics analysis confirmed that FG@MES/PM followed the Higuchi matrix model (R2=0.9867), indicating diffusion-controlled release. The drug release mechanism was characterized as anomalous (non-Fickian) transport, with a release exponent (n) of 0.563. Overall, FG@MES/PM demonstrated promising potential for colon-specific drug delivery, offering sustained release and enhanced mucoadhesion. This study underscores the utility of FG for developing advanced drug delivery systems targeting the colon. Future research should explore the broader application of FG and similar natural polysaccharides in designing efficient and biocompatible colon-targeted formulations to improve therapeutic outcomes for IBD and related conditions.

美沙拉明(MES)是治疗包括炎症性肠病(IBD)在内的各种结肠疾病的首选治疗剂。然而,MES的传统口服剂型面临重大限制,这降低了它们在管理这些疾病方面的有效性。为了克服这些挑战,先进的MES剂型至关重要。葫芦巴胶(FG)是一种天然多糖,具有无毒、易于合成、生物降解和生物相容性等优点,是开发新型给药系统的关键成分。钙离子交联mes - fg修饰果胶微球(FG@MES/PM)成功设计用于结肠特异性药物递送。该微球具有良好的理化性能,粒径为586 nm,多分散指数为0.348,包封效率为85.20±1.02%,药物含量为98.52±0.96%。体外黏附试验显示出强大的黏附特性,突出了FG@MES/PM有效粘附结肠粘膜的潜力。体外释药研究表明,该药物在24 h内的释药率为99.02±1.80%。释放动力学分析证实FG@MES/PM符合Higuchi矩阵模型(R²= 0.9867),为扩散控制释药。药物释放机制为异常(非菲克式)转运,释放指数(n)为0.563。总体而言,FG@MES/PM显示出有希望的结肠特异性药物递送潜力,提供持续释放和增强粘膜粘附。这项研究强调了FG在开发针对结肠的先进药物输送系统中的实用性。未来的研究应探索FG和类似天然多糖在设计高效、生物相容性强的结肠靶向制剂方面的更广泛应用,以改善IBD及相关疾病的治疗效果。
{"title":"Development of mesalamine loaded-fenugreek gum decorated pectin microspheres for colonic drug delivery: Ex-vivo and in-vitro characterizations.","authors":"Pruthvi P Khamkar, Kalpeshkumar S Wagh, Sopan N Nangare, Sachin S Mali, Gaurav S Patil","doi":"10.1016/j.pharma.2024.11.006","DOIUrl":"10.1016/j.pharma.2024.11.006","url":null,"abstract":"<p><p>Mesalamine (MES) is a preferred therapeutic agent for managing various colon disorders, including inflammatory bowel diseases (IBD). However, conventional oral dosage forms of MES face significant limitations, which reduce their effectiveness in managing these conditions. To overcome these challenges, advanced dosage forms of MES are essential. Fenugreek gum (FG), a natural polysaccharide with non-toxicity, ease of synthesis, biodegradability, and biocompatibility, was selected as a key component for developing a novel delivery system. Calcium ion crosslinked MES-incorporated FG-decorated pectin microspheres (FG@MES/PM) were successfully designed for colon-specific drug delivery using an ionotropic gelation technique. The microspheres exhibited favorable physicochemical characteristics, including a particle size of 586nm, a polydispersity index of 0.348, an entrapment efficiency of 85.20±1.02%, and a drug content of 98.52±0.96%. Ex vivo mucoadhesion tests demonstrated strong mucoadhesive properties, highlighting the potential of FG@MES/PM to adhere effectively to the colonic mucosa. In vitro drug release studies showed a modified release profile, with 99.02±1.80% MES released over 24h. Release kinetics analysis confirmed that FG@MES/PM followed the Higuchi matrix model (R<sup>2</sup>=0.9867), indicating diffusion-controlled release. The drug release mechanism was characterized as anomalous (non-Fickian) transport, with a release exponent (n) of 0.563. Overall, FG@MES/PM demonstrated promising potential for colon-specific drug delivery, offering sustained release and enhanced mucoadhesion. This study underscores the utility of FG for developing advanced drug delivery systems targeting the colon. Future research should explore the broader application of FG and similar natural polysaccharides in designing efficient and biocompatible colon-targeted formulations to improve therapeutic outcomes for IBD and related conditions.</p>","PeriodicalId":8332,"journal":{"name":"Annales pharmaceutiques francaises","volume":" ","pages":""},"PeriodicalIF":1.0,"publicationDate":"2024-11-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142765842","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
Validation of spectrophotometric and colorimetric method for the specific quantification of sofosbuvir From luminar capsule microneedle in liver tissue through ex vivo and in vivo applications. 光度法和比色法在离体和体内应用于肝组织中荧光胶囊微针索非布韦特异性定量的验证。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-11-27 DOI: 10.1016/j.pharma.2024.11.005
Abigael Alik Samma, Christopher Kosasi Ko, Musyfira Sahra, Nurul Fitrayani, Felicia Virginia Thios, Andi Dian Permana

An antiviral prodrug that has received regulatory approval and primarily employed in the treatment of hepatitis C is sofosbuvir (SOF). It is therefore imperative to develop advanced delivery methods for SOF in order to address existing absor ption issue and maximize the efficacy. In this study, we developed microneedle-integrated SOF (MN-SOF) which were elongated with branches and coated capsules to form luminar capsule microneedles (LUCAMs). To facilitate the formulation of LUCAMs, analytical methods for SOF in ethanol, artificial intestinal fluid (AIF), and artificial gastric fluid (AGF) were developed using a UV-vis spectrophotometer and colorimetric techniques in liver tissue. These methods were validated by combi ning the samples with ammonium metavanadate reagent. The validation process was conducted in order to ensure the accuracy, precision, linearity, specificity, and sensitivity of the methods. These methods exhibited a correlation coefficient of 0.9999, with a coefficient of variation below 25%. The methods demonstrate high accuracy and precision, with relative standard deviation (RSD) values ranging from 0.67% to 9.42% across different medium. The limit of detection (LOD) and limit of quantification (LOQ) values of SOF on each calibration curve of ethanol, artificial gastric fluid (AGF), artificial intestinal fluid (AIF), and rabbit liver tissue are 0.54μg/mL and 1.65μg/mL; 0.54μg/mL and 1.64μg/mL; 0.39μg/mL and 1.21μg/mL; 0.27μg/mL and 0.83μg/mL. As a significant outcome, the analytical method was validated and demonstrated suitability for determining the amount of SOF in the LUCAMs formulation through in vitro solubility, ex vivo permeation profiles, and in vivo drug delivery studies.

sofosbuvir (SOF)是一种获得监管部门批准的抗病毒前药,主要用于治疗丙型肝炎。因此,为了解决现有的吸收问题并最大限度地发挥其功效,开发先进的运载方法势在必行。在这项研究中,我们开发了微针集成微针(MN-SOF),该微针通过分支拉长并包覆胶囊形成发光胶囊微针(LUCAMs)。为方便LUCAMs的制备,建立了肝组织中乙醇、人工肠液(AIF)和人工胃液(AGF)中sofa的紫外-可见分光光度法和比色法分析方法。将样品与偏氰酸铵试剂结合,验证了上述方法的有效性。为了确保方法的准确性、精密度、线性度、特异性和灵敏度,进行了验证过程。相关系数为0.9999,变异系数小于25%。该方法具有较高的准确度和精密度,在不同介质中的相对标准偏差(RSD)在0.67% ~ 9.42%之间。乙醇、人工胃液(AGF)、人工肠液(AIF)和兔肝组织各校准曲线上sofd的检出限(LOD)和定量限(LOQ)分别为0.54µg/mL和1.65µg/mL;0.54µg/mL和1.64µg/mL;0.39µg/mL和1.21µg/mL;0.27µg/mL和0.83µg/mL。作为一个重要的结果,通过体外溶解度、体外渗透谱和体内给药研究,验证了分析方法的有效性,并证明了该方法适用于确定LUCAMs制剂中SOF的含量。
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引用次数: 0
The therapeutic potential of Ribes orientale in hypertension: Improving electrolyte balance, enhancing antioxidant activity, and modulating the muscarinic pathway 东方核果对高血压的治疗潜力:改善电解质平衡、增强抗氧化活性和调节毒蕈碱途径。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-11-22 DOI: 10.1016/j.pharma.2024.11.004
Ambreen Malik Uttra , Suhail Ahmad , Taseer Ahmad , Sumera Qasim , Hafiza Sara Afzal , Waqas Younis
<div><div>Cardiovascular diseases like hypertension require diuretics, but their effectiveness and side effects limit their use. Alternatives like <em>Ribes orientale</em> extract are being investigated for potential diuretic. In acute diuretic action, the extract and fractions of <em>Ribes orientale</em> were investigated in saline-loaded rats at doses of 12.5, 25, and 50<!--> <!-->mg/kg, p.o., while prolonged diuretic activity was also performed by administration of the most potent and significant dose of <em>Ribes orientale</em> butanol fraction (ROBF) for 7<!--> <!-->days. ROBF diuretic action was confirmed through parameters like urine volume, electrolyte concentration, pH and conductivity. The study found that 50<!--> <!-->mg/kg of ROBF had the most potent and significant diuretic activity, like furosemide (10<!--> <!-->mg/kg). It also produced significant natriuresis and insignificant kaliuresis in electrolyte excretion. ROBF increased diuretic activity significantly from the first and 7th days. In the mechanistic study, it has been evaluated that nitric oxide and prostaglandins pathways are not involved in the diuretic effect of ROBF, while cholinergic pathway might be responsible for the diuretic effect of ROBF. Hematological, renal function tests and histopathological studies confirmed the safety of <em>Ribes orientale</em> at 50<!--> <!-->mg/kg. Results showed slight changes in blood count parameters and no significant changes in creatinine and blood urea nitrogen levels compared to the negative control. Furthermore, downregulation of aldosterone by ROBF prolonged activity enhances the local bradykinin availability that results in marked diuretic and natriuretic activity. It is evident from the decreased level of malondialdehyde (MDA) that <em>Ribes orientale</em> reduces the oxidative stress while increased level of superoxide dismutase (SOD) depicts improving level of antioxidant activity. We conclude that the butanol fraction of <em>Ribes orientale</em> roots possesses a considerable diuretic effect. Therefore, more study is needed to identify the exact mechanism of action and the real efficacy of <em>Ribes orientale</em> as diuretic.</div></div><div><div>Les maladies cardiovasculaires comme l’hypertension nécessitent des diurétiques, mais leur efficacité et leurs effets secondaires limitent leur utilisation. Des alternatives comme l’extrait de Ribes orientale sont à l’étude pour leur potentiel diurétique. En ce qui concerne l’action diurétique aiguë, l’extrait et les fractions de Ribes orientale ont été étudiés chez des rats’ chargés en solution saline à des doses de 12,5, 25 et 50<!--> <!-->mg/kg, p.o., tandis qu’une activité diurétique prolongée a également été réalisée par l’administration de la dose la plus puissante et la plus significative de fraction butanol orientale Ribes (ROBF) pendant 7 jours. L’action diurétique du ROBF a été confirmée par des paramètres tels que le volume d’urine, la concentration d’électrolytes, le pH
高血压等心血管疾病需要利尿剂,但其有效性和副作用限制了利尿剂的使用。目前正在研究东方核果提取物等替代品的潜在利尿作用。在急性利尿作用方面,研究人员以 12.5、25 和 50 毫克/千克的剂量,对盐水负荷大鼠进行了东方核果提取物和馏分的急性利尿作用研究,同时还对东方核果丁醇馏分(ROBF)进行了为期 7 天的长效利尿作用研究。ROBF 的利尿作用通过尿量、电解质浓度、pH 值和电导率等参数得到证实。研究发现,与呋塞米(10 毫克/千克)一样,50 毫克/千克的 ROBF 具有最有效、最显著的利尿活性。在电解质排泄方面,它也能产生明显的利尿作用,而不明显的利尿作用。ROBF 从第 1 天和第 7 天开始明显增加了利尿活性。机理研究表明,一氧化氮和前列腺素途径没有参与 ROBF 的利尿作用,而胆碱能途径可能是 ROBF 利尿作用的原因。血液学、肾功能测试和组织病理学研究证实,50 毫克/千克的东方核果是安全的。结果:与阴性对照组相比,血细胞计数参数略有变化,肌酐和血尿素氮水平无明显变化。此外,ROBF 延长活动对醛固酮的下调增强了局部缓激肽的可用性,从而产生明显的利尿和利钠活性。从丙二醛(MDA)水平的降低可以看出,东方核果可以减少氧化应激,而超氧化物歧化酶(SOD)水平的提高则表明抗氧化活性水平的提高。我们的结论是,东方赤松根的丁醇部分具有相当大的利尿作用。因此,还需要进行更多的研究,以确定东方核果作为利尿剂的确切作用机制和真正功效。
{"title":"The therapeutic potential of Ribes orientale in hypertension: Improving electrolyte balance, enhancing antioxidant activity, and modulating the muscarinic pathway","authors":"Ambreen Malik Uttra ,&nbsp;Suhail Ahmad ,&nbsp;Taseer Ahmad ,&nbsp;Sumera Qasim ,&nbsp;Hafiza Sara Afzal ,&nbsp;Waqas Younis","doi":"10.1016/j.pharma.2024.11.004","DOIUrl":"10.1016/j.pharma.2024.11.004","url":null,"abstract":"&lt;div&gt;&lt;div&gt;Cardiovascular diseases like hypertension require diuretics, but their effectiveness and side effects limit their use. Alternatives like &lt;em&gt;Ribes orientale&lt;/em&gt; extract are being investigated for potential diuretic. In acute diuretic action, the extract and fractions of &lt;em&gt;Ribes orientale&lt;/em&gt; were investigated in saline-loaded rats at doses of 12.5, 25, and 50&lt;!--&gt; &lt;!--&gt;mg/kg, p.o., while prolonged diuretic activity was also performed by administration of the most potent and significant dose of &lt;em&gt;Ribes orientale&lt;/em&gt; butanol fraction (ROBF) for 7&lt;!--&gt; &lt;!--&gt;days. ROBF diuretic action was confirmed through parameters like urine volume, electrolyte concentration, pH and conductivity. The study found that 50&lt;!--&gt; &lt;!--&gt;mg/kg of ROBF had the most potent and significant diuretic activity, like furosemide (10&lt;!--&gt; &lt;!--&gt;mg/kg). It also produced significant natriuresis and insignificant kaliuresis in electrolyte excretion. ROBF increased diuretic activity significantly from the first and 7th days. In the mechanistic study, it has been evaluated that nitric oxide and prostaglandins pathways are not involved in the diuretic effect of ROBF, while cholinergic pathway might be responsible for the diuretic effect of ROBF. Hematological, renal function tests and histopathological studies confirmed the safety of &lt;em&gt;Ribes orientale&lt;/em&gt; at 50&lt;!--&gt; &lt;!--&gt;mg/kg. Results showed slight changes in blood count parameters and no significant changes in creatinine and blood urea nitrogen levels compared to the negative control. Furthermore, downregulation of aldosterone by ROBF prolonged activity enhances the local bradykinin availability that results in marked diuretic and natriuretic activity. It is evident from the decreased level of malondialdehyde (MDA) that &lt;em&gt;Ribes orientale&lt;/em&gt; reduces the oxidative stress while increased level of superoxide dismutase (SOD) depicts improving level of antioxidant activity. We conclude that the butanol fraction of &lt;em&gt;Ribes orientale&lt;/em&gt; roots possesses a considerable diuretic effect. Therefore, more study is needed to identify the exact mechanism of action and the real efficacy of &lt;em&gt;Ribes orientale&lt;/em&gt; as diuretic.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;div&gt;Les maladies cardiovasculaires comme l’hypertension nécessitent des diurétiques, mais leur efficacité et leurs effets secondaires limitent leur utilisation. Des alternatives comme l’extrait de Ribes orientale sont à l’étude pour leur potentiel diurétique. En ce qui concerne l’action diurétique aiguë, l’extrait et les fractions de Ribes orientale ont été étudiés chez des rats’ chargés en solution saline à des doses de 12,5, 25 et 50&lt;!--&gt; &lt;!--&gt;mg/kg, p.o., tandis qu’une activité diurétique prolongée a également été réalisée par l’administration de la dose la plus puissante et la plus significative de fraction butanol orientale Ribes (ROBF) pendant 7 jours. L’action diurétique du ROBF a été confirmée par des paramètres tels que le volume d’urine, la concentration d’électrolytes, le pH","PeriodicalId":8332,"journal":{"name":"Annales pharmaceutiques francaises","volume":"83 2","pages":"Pages 389-400"},"PeriodicalIF":1.0,"publicationDate":"2024-11-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142709019","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
The implications of the EU ban on titanium dioxide: A comprehensive review of safety concerns and alternatives. 欧盟二氧化钛禁令的影响:对安全问题和替代品的全面审查。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-11-15 DOI: 10.1016/j.pharma.2024.11.002
Varsha Pokharkar, Sejal Chandak, Rutika Pawar, Akshay Khandke

Titanium dioxide, a naturally occurring compound, has been extensively utilized across various industries such as food, pharmaceuticals, and cosmetics. In the food sector, it was commonly employed as a color and opacity enhancer under the designation E171. However, due to safety concerns, the EU has prohibited its use as a food additive, effective August 2022, following a six-month transition period. The decision was based on scientific research highlighting risks associated with inhaling titanium dioxide nanoparticles and its potential genotoxic effects. This review also summarizes the implications of this ban on the pharmaceutical industry, where titanium dioxide is utilized in drug manufacturing. While the safety of titanium dioxide in tablets remains inconclusive, the EU's regulatory action has prompted a closer examination of alternative options. While alternatives exist, they may not provide the same benefits as TiO2, particularly in pharmaceuticals. Further research is needed to determine the safety and effectiveness of TiO2 and its alternatives in these applications.

二氧化钛是一种天然化合物,已被广泛应用于食品、药品和化妆品等各个行业。在食品行业,二氧化钛通常被用作增色剂和不透明剂,其名称为 E171。然而,出于安全考虑,欧盟已禁止将其用作食品添加剂,并在六个月的过渡期后于 2022 年 8 月生效。这一决定是基于科学研究,研究强调了吸入纳米二氧化钛颗粒的相关风险及其潜在的基因毒性影响。本评论还总结了这一禁令对制药业的影响,因为二氧化钛被用于药物生产。虽然片剂中使用二氧化钛的安全性仍无定论,但欧盟的监管行动促使人们更仔细地研究替代方案。虽然存在替代品,但它们可能无法提供与二氧化钛相同的优点,尤其是在药品中。要确定二氧化钛及其替代品在这些应用中的安全性和有效性,还需要进一步的研究。
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引用次数: 0
Identification of utilization deficiencies post SAP enterprise resource planning implementation in the Algerian Pharmaceutical Sector 确定阿尔及利亚制药部门实施 SAP 企业资源规划后的使用缺陷。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-11-14 DOI: 10.1016/j.pharma.2024.11.003
Mariah Khaldi , Redouane Amine Cherif , Houssem Belmekki
<div><h3>Objectives</h3><div>Enterprise Resource Planning like SAP are software solutions integrating various functional aspects. The study investigates the utilization challenges after the adoption of SAP ERP within a pharmaceutical firm. It is driven by four interrelated objectives: comprehending the operation of the SAP, the motivations behind its implementation, identifying the utilization deficiencies, and examining the relation between deficiencies and implementation challenges.</div></div><div><h3>Materials and methods</h3><div>A triangulation approach was adopted. The methods employed are based on batch monitoring, data collection, semi-structured interviews, a literature review, an overview of the software package, a comparison of the SAP with the previous management system, and an in-depth implementation study.</div></div><div><h3>Results</h3><div>Thirty-eight challenges were found in the literature, in a causal relationship with 11 identified utilization deficiencies in the study field. This analysis emphasized the significance of the human dimension, particularly the training of users, as a critical element in SAP implementation.</div></div><div><h3>Conclusion</h3><div>The advantages gained from implementing an ERP primarily revolve around the users and the processes. Deployment in itself is not an improvement. By recognizing the importance of the human factor, organizations can focus on improving training programs and enhancing user proficiency to maximize the benefits of SAP implementation.</div></div><div><h3>Objectif</h3><div>Les progiciels de gestion intégrés tels que SAP sont des solutions logicielles qui intègrent divers aspects fonctionnels. L’étude examine les difficultés d’utilisation après l’adoption de SAP ERP au sein d’une entreprise pharmaceutique, et est motivée par quatre objectifs interdépendants: comprendre le fonctionnement de SAP, les motivations derrière sa mise en œuvre, identifier les lacunes d’utilisation, et examiner la relation entre les lacunes d’utilisation et les difficultés de mise en œuvre.</div></div><div><h3>Matériels et méthodes</h3><div>Une approche par triangulation méthodologique a été adoptée. Les méthodes employées sont basées sur le suivi des lots, la collecte de données, des entretiens semi-structurés et une revue de la littérature.</div></div><div><h3>Résultats</h3><div>Une liste de 38 défis a été trouvée dans la littérature, en relation causale avec 11 déficiences d’utilisation identifiées dans le domaine de l’étude. Cette analyse a mis en évidence l’importance de la dimension humaine, en particulier la formation des utilisateurs, en tant qu’élément critique de la mise en œuvre de SAP.</div></div><div><h3>Conclusion</h3><div>Les avantages d’un ERP concernent principalement les utilisateurs et les processus. Le déploiement en lui-même n’est pas une amélioration. En reconnaissant l’importance du facteur humain, les organisations peuvent se focaliser sur l’amélioration des programmes de formatio
目标:SAP 等企业资源规划系统是集成了各种功能的软件解决方案。本研究调查了一家制药公司在采用 SAP ERP 后在使用方面遇到的挑战。本研究由四个相互关联的目标驱动:理解 SAP 的运作、实施 SAP 背后的动机、确定使用方面的不足以及研究不足与实施挑战之间的关系:采用三角测量法。采用的方法包括批量监测、数据收集、半结构式访谈、文献综述、软件包概述、SAP 与之前管理系统的比较以及深入的实施研究:结果:在文献中发现了 38 项挑战,与研究领域中发现的 11 项使用缺陷存在因果关系。这项分析强调了人的因素的重要性,尤其是对用户的培训,这是 SAP 实施的关键因素:实施企业资源规划系统的优势主要围绕用户和流程。部署本身并不是一种改进。通过认识到人的因素的重要性,企业可以集中精力改进培训计划,提高用户的熟练程度,从而最大限度地提高 SAP 实施的效益。
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引用次数: 0
Montmorillonite: An advanced material with diverse pharmaceutical and medicinal applications. 蒙脱石:一种具有多种制药和药用用途的先进材料。
IF 1 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-11-06 DOI: 10.1016/j.pharma.2024.11.001
Sagar Fatale, Javesh K Patil, Chandrakantsing V Pardeshi, Vishal V Pande, Mangesh A Bhutkar, Komal Parashar, Raju O Sonawane

Montmorillonite (MMT) clay is composed of naturally layered silicate. The clays were more popular in the pharmaceutical and other various fields due to their beneficial physicochemical properties viz. non-toxicity, high surface area, efficient adsorption capability, high swellability, high dispersibility, thixotropic behaviour, and cation exchange capacity. Chemically modified clay provides significant opportunities in variety of applications. MMT finds very crucial place in pharmaceutical field owing to its medicinal properties, which may be used to delay the drug release in chronic physiological conditions and the targeted drug release as well. It is also used to improve the dissolution rate of certain drug molecules, which increased the attention of the researchers to explore the MMT for drug delivery applications. MMT clay has been used as pharmaceutical aids viz. suspending agent, lubricant, anticaking agent, diluent, emulsifier, nanocomposites-forming material, and sometimes filler. MMT clay have been investigated in the fabrication of different pharmaceutical formulations viz. hydrogel, films, nanocomposites, and matrix-based systems. MMT has obtained industrial importance due to its adsorption property and also finds use in wastewater treatment. Other than this, MMT also finds applications in cosmetic industry, food industry, and paper industry. Considering the wide applicability of MMT, it is need of an hour to explore the MMT for further commercial exploitation.

蒙脱石(MMT)粘土矿物由天然层状硅酸盐组成。由于粘土具有无毒、高比表面积、高效吸附能力、高膨胀性、高分散性、触变性和阳离子交换能力等有益的物理化学特性,因此在制药和其他各个领域都很受欢迎。化学改性粘土为各种应用提供了重要机会。由于其药用特性,MMT 在制药领域具有非常重要的地位,可用于延缓药物在慢性生理条件下的释放和靶向药物释放。它还可用于提高某些药物分子的溶解速率,这使研究人员更加关注 MMT 在药物输送方面的应用。MMT 粘土可用作药物助剂,即悬浮剂、润滑剂、抗结块剂、稀释剂、乳化剂、纳米复合材料,有时也用作填料。已对 MMT 粘土在不同药物配方(即水凝胶、薄膜、纳米复合材料和基质系统)的制造中的应用进行了研究。MMT 因其吸附特性而具有重要的工业价值,还可用于废水处理。除此之外,MMT 还可用于化妆品行业、食品行业和造纸行业。考虑到 MMT 的广泛适用性,当务之急是探索 MMT 的进一步商业开发。
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引用次数: 0
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Annales pharmaceutiques francaises
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