Arhiv za Farmaciju最新文献

{"title":"Docking studies of some pyrazole containing compounds in the cyclooxygenase-2 active site","authors":"J. Savić, Marija Antonijević, Milkica Crevar, J. Brborić","doi":"10.5937/arhfarm73-44720","DOIUrl":"https://doi.org/10.5937/arhfarm73-44720","url":null,"abstract":"Whereas nonselective nonsteroidal anti-inflammatory drugs, such as aspirin, ibuprofen and diclofenac, inhibit both cyclooxygenase-1 and cyclooxigenase-2 enzymes, selective inhibitors target cyclooxygenase-2, which is overexpressed in inflammation, but also in cancer, atherosclerosis, Alzheimer's disease, and Parkinson's disease. Potential cardiovascular and hepatic side effects of cyclooxygenase-2 inhibitors have limited their use. The development of selective and safe cyclooxygenase-2 inhibitors remains a high priority in drug discovery. Based on the structure of previously investigated newly synthesized b-hydroxy-b-arylpropanoic acids, two groups of compounds were designed: analogs in which one of the benzene rings was replaced by a pyrazole, while the carboxyl group was retained, and amides of b-hydroxy-b-arylpropanoic acids with pyrazole. The compounds were docked into the 3D structure of the catalytic site of the enzyme cyclooxygenase-2 using AutoDock Vina 1.2.0. and the obtained interactions were compared with the interactions of celecoxib, a selective inhibitor. The amides had lower binding energies than the designed acids, which makes them attractive target compounds for synthesis and further examination.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199805","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}

{"title":"Dietary interventions through supplementation with antioxidant compounds","authors":"V. Todorović, B. Đorđević","doi":"10.5937/arhfarm73-45141","DOIUrl":"https://doi.org/10.5937/arhfarm73-45141","url":null,"abstract":"Dietary supplements (DS) are manufactured products consisting of one or more dietary ingredients; they are intended to supplement the diet and provide additional nutrients or other beneficial compounds that are lacking or insufficient in a regular diet. Dietary supplements containing antioxidant compounds have been shown to have positive effects in various (pato)physiological processes, i.e., any condition that is fundamentally redox imbalanced (cardiovascular diseases, cancer, aging, intense exercise). The most common antioxidants in dietary supplements are clearly antioxidant micronutrients such as vitamin C, vitamin E, zinc, and selenium, but also various secondary plant compounds, including polyphenols and carotenoids. The dosage of antioxidants administered through dietary supplements may not always be optimal, so some dietary interventions through supplementation with antioxidant compounds have been shown to have an effect that it is limited, or completely absent. Therefore, any dietary supplementation should be done only under appropriate guidance from health care professionals to ensure that it is safe, effective, and appropriate for the individual's condition and needs.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199856","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}

{"title":"Methods for the determination of antioxidant activity of plant extracts in vitro","authors":"J. Kukić-Marković","doi":"10.5937/arhfarm73-38573","DOIUrl":"https://doi.org/10.5937/arhfarm73-38573","url":null,"abstract":"Plants are rich sources of secondary metabolites that exhibit diverse biological and pharmacological effects. Some plant ingredients, primarily phenolics, have significant in vitro antioxidant activity, which implies their contribution to the maintenance of redox balance in the body. These potential antioxidant agents are structurally very diverse, having different mechanisms of antioxidant activity. Since there is a growing necessity to detect, develop and understand effective antioxidant compounds, interest in the identification and the measurement of antioxidants in various plant isolates is persistently growing and many methods are being established. Most of the available in vitro tests are affordable and easy to perform, but due to the complex composition of plant extracts, different kinetics, mechanisms and specificity of the chemical reactions underlying these tests, there is no universal parameter for the assessment of antioxidant activity. In this paper, some of the currently most used in vitro methods for investigating and evaluating antioxidant activity of plant extracts are presented, emphasizing their advantages and weaknesses.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199537","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}

{"title":"Comparative risk assessment study of elemental impurities in Montelukast chewable tablets and film-coated tablets","authors":"Stefan Angelevski, Irena Slaveska-Spirevska, Elena Lazarevska-Todevska, Tanja Bakovska-Stoimenova, M. Glavaš-Dodov, Maja Simonoska-Crcarevska, R. Slaveska-Raički","doi":"10.5937/arhfarm73-41263","DOIUrl":"https://doi.org/10.5937/arhfarm73-41263","url":null,"abstract":"It is well documented that elemental impurities (EIs) are critical in the field of pharmaceutical development since they could affect the quality, efficacy and safety of the finished dosage form (FDF). The responsibility of pharmaceutical manufacturers is to demonstrate via assessment approach, risk-based control strategy and/or required data analysis that the FDFs are compliant with ICH Q3D (R2). The aim of this research is to conduct a comprehensive comparative EIs risk assessment study of three different Montelukast dosage forms produced as chewable tablets (4 mg and 5 mg) and film-coated tablets 10 mg. The inductively coupled plasma-mass spectrometry (ICP-MS) system was used for the determination of EIs in samples of Montelukast sodium as the active pharmaceutical ingredient (API), placebos for all FDFs, and FDFs. Moreover, the analyses were also conducted on three batches from all three studied FDFs. Based on ICH Q3D (R2) guidelines, the tested products for EIs Class 1 and Class 2A showed that EIs levels in the API and placebos are well below the ICH Option 1 oral and parenteral limits. For the examined batches of each FDF strength (total of 9), none of the EI exceeds their concentration limits.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199589","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}

{"title":"Design of Experiments (DoE)-based approach for improvement of dry mixing processes in the production of low-dose Alprazolam tablets using Raman spectroscopy for content uniformity monitoring","authors":"Liljana Makraduli, P. Makreski, Filip Makraduli, Irena Slaveska-Spirevska, Tanja Bakovska-Stoimenova, Elena Lazarevska-Todevska, M. Piponski, Maja Anevska, M. Glavaš-Dodov, Maja Simonoska-Crcarevska, K. Mladenovska, K. Goracinova, Nikola Geškovski","doi":"10.5937/arhfarm73-41376","DOIUrl":"https://doi.org/10.5937/arhfarm73-41376","url":null,"abstract":"A low-dose tablet formulation, containing a potent Benzodiazepine derivative Alprazolam was developed, considering the achievement of appropriate content uniformity of the active substance in powder blends and tablets as a major challenge. Two different types of lactose monohydrate (Tablettose 80 and Granulac 200) and two different types of dry mixing processes (high-shear mixing and \"in bulk\" mixing) were employed. To evaluate the influence of the variables (mixing speed, mixing time, filling level of the high-shear and cube mixer, lactose monohydrate type) and their interactions upon the response (content uniformity of Alprazolam in the powder blends), a Factorial 2 4 design (with 4 factors at 2 levels in 1 block) was generated for each type of mixer. For high-shear dry mixing the Response Surface, D-optimal Factorial 2 4 design (with 2 replications and 31 experiments) was used, while for the \"in bulk\" dry mixing the Response Surface, Central Composite Factorial 2 4 design (with 34 experiments) was used. The process parameters for the high-shear mixer were varied within the following ranges: filling level of 70-100%, impeller mixing speed of 50-300 rpm and mixing time of 2-10 minutes. For the cube mixer the following process parameter ranges were employed: filling level of 30-60%, mixing speed of 20-390 rpm and mixing time of 2-10 minutes. Raman spectroscopy in conjunction with a validated Partial Least Square (PLS) regression model was used as a Process Analytical Technology (PAT) tool for Alprazolam content determination and content uniformity monitoring. The DoE model was further employed to optimize the powder blending process in regard to the achievement of appropriate Alprazolam content uniformity using high-shear mixing and Tabletosse 80 as filler. The desirability function revealed that the following process parameters: a mixing time of 2 minutes, a mixing speed of 300 rpm and a 70% filling level of the mixer would produce powder blends with the lowest variability in Alprazolam content. The three independent lab batches of low-dose Alprazolam tablets, produced with high-shear mixing using these process parameters, conformed to the requirements of the European Pharmacopoeia for content (assay) of Alprazolam and uniformity of the dosage units.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199600","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}

{"title":"Biochemical and hematological parameters in the 1st trimester of pregnancy","authors":"J. Ivanišević, D. Ardalić, A. Zeljković, J. Vekić, T. Gojković, S. Vladimirov, T. Antonić, Jelena Munjas, A. Stefanović","doi":"10.5937/arhfarm73-41999","DOIUrl":"https://doi.org/10.5937/arhfarm73-41999","url":null,"abstract":"The 1st trimester of pregnancy is accompanied with changes in different biochemical and hematological parameters. Analyses scheduled to be performed in the 1st trimester are complete blood count, blood group, Rh factor and the double test. Many experts also suggest the determination of lipid status parameters as a routine analysis in the early pregnancy. Reliable data about maternal and fetal health can be obtained by the assessment of the above-mentioned parameters. They may be helpful in assessing the risk for pregnancy complication development and/or perinatal adverse outcomes.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199611","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}

{"title":"Redox homeostasis, oxidative stress and antioxidant system in health and disease: The possibility of modulation by antioxidants","authors":"J. Kotur-Stevuljević, J. Savić, Milena Simić, J. Ivanišević","doi":"10.5937/arhfarm73-45369","DOIUrl":"https://doi.org/10.5937/arhfarm73-45369","url":null,"abstract":"Redox imbalance occurs when the factors of oxidative stress, known as prooxidants, outweigh the mechanisms of antioxidant protection. In a healthy state, homeostatic mechanisms ensure the balanced production of free radicals and a complete series of antioxidants responsible for their safe removal. The generation of free radicals is a part of physiological processes in a healthy organism, some of which act as specific signaling molecules, and their presence and activity are necessary in these processes. In various diseases such as cancer, cardiovascular disease, diabetes, autoimmune diseases, rheumatic diseases, systemic lupus, and skin diseases, the generation of free radicals overwhelms the protective mechanisms, leading to the development of \"oxidative stress\" that damages cells and tissues. To prevent the harmful effects of free radicals within cells, there exists a system of enzymatic antioxidant protection composed of superoxide dismutase (SOD), glutathione peroxidase (GSHPx), glutathione reductase (GR), glutaredoxin, reduced/oxidized glutathione (GSH/GSSG), and thioredoxin (TRX). The examples of non-enzymatic antioxidants are: antioxidant vitamins such as A, C and E, dihydrolypoic acid, metallothioneins, ceruloplasmin, coenzyme Q 10, urea, creatinine, etc. Redox balance is influenced by the circadian rhythm and external factors that constitute the \"exposome\", including dietary habits and lifestyle. Antioxidant supplementation has become increasingly popular for maintaining optimal body function. However, it is important to note that some antioxidants can exhibit prooxidant activity, emphasizing the need for controlled use. The relationship between the redox status of the body and the action of antioxidants enables the development of multidisciplinary research that connects biochemistry, molecular biology, nutritional science, natural product chemistry, and clinical practice.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199868","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}

{"title":"Principles and applications of interfacial rheology in (pre)formulation development of pharmaceutical preparations","authors":"Veljko Krstonošić, Nebojša Pavlović, Dejan Ćirin","doi":"10.5937/arhfarm73-46316","DOIUrl":"https://doi.org/10.5937/arhfarm73-46316","url":null,"abstract":"Rheology is a science that deals with the movement and deformation of materials, while interfacial rheology is a branch of rheology that focuses on the study of the mechanical properties of fluid interfaces, such as liquid-liquid and liquid-gas interfaces. The behavior of fluid interfaces differs significantly from that of bulk materials, and standard rheological measurements of bulk materials cannot adequately describe their properties. Interfacial rheology is a specialized approach to the study of viscoelasticity and interfacial tension at liquid interfaces and provides valuable insight into intermolecular interactions and surface forces. This knowledge is particularly important for the development of advanced formulations and systems with tailored properties and functionalities. Interfacial rheology is a rapidly growing research field with diverse applications in science and industry. It plays a pivotal role in the development and optimization of pharmaceutical formulations and design of innovative drug delivery carriers with improved stability, enhanced drug release profiles, and targeted delivery capabilities. This review article aims to provide a comprehensive overview of interfacial rheology, its principles, measurement techniques, and applications in various industries. By exploring recent advancements and emerging trends in the field, we aim to highlight the significance of interfacial rheology in optimizing formulations, enhancing product performance, and driving innovations, particularly in pharmaceutical science.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134982036","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}

{"title":"Antioxidant activity of plant secondary metabolites","authors":"M. Marčetić, Jelena Arsenijević","doi":"10.5937/arhfarm73-45560","DOIUrl":"https://doi.org/10.5937/arhfarm73-45560","url":null,"abstract":"Oxidative stress can induce the development of many different disorders. Plant secondary metabolites may act as antioxidants by neutralisation of free radicals and by stimulation of endogenous antioxidant mechanisms. One of the important secondary plant metabolites with antioxidant activity are polyphenols. They can exert activity through different mechanisms depending on their structure. Polyphenols are widely present in herbal drugs, and some of the commonly used ones are aronia berry (Aroniae fructus) and bilberry fruit (Myrtilli fructus), both rich in anthocyanins and tannins and with high antioxidant activity. The main compounds in turmeric rhizome (Curcumae rhizome) are curcuminoides that manifest antioxidant and anti-inflammatory activity. Furthermore, tea leaf (Camelliae sinensis folium) and coffee bean (Coffeae semen), highly present in everyday life, significantly contribute to the daily intake of antioxidants and provide necessary protection of the organism from the consequences of oxidative stress.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199503","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}

{"title":"Agri-food by-products as a source of sustainable ingredients for the production of functional foods and nutraceuticals","authors":"Nevena Ivanović, Tijana Ilić, Milica Zrnić-Ćirić, V. Todorović, I. Đuričić, Nevena Dabetić","doi":"10.5937/arhfarm73-44481","DOIUrl":"https://doi.org/10.5937/arhfarm73-44481","url":null,"abstract":"The disposal of waste generated in the agri-food industry is one of the greatest challenges in achieving sustainable development. Although agri-food residues are a potential source of bioactive compounds with proven health benefits, they are largely unused and disposed of as organic waste. The recovery of bioactive compounds from agri-food waste to obtain products with high biological value, such as functional foods and nutraceuticals, is an idea that stems from the concept of bioeconomy and combines environmental issues with economically viable production. Some of the main agri-food wastes in Serbia that have the potential to be recycled into value-added products are apple, plum, grape, tomato, and beet pomace, and oilseed cakes. Bioactive compounds isolated from these wastes include polyphenols, fibers, essential fatty acids, minerals, various volatiles and pigments. This article focuses on the most common food wastes and the potential reuse of these undervalued material to produce value-added products such as functional foods, nutraceuticals or food additives.","PeriodicalId":39173,"journal":{"name":"Arhiv za Farmaciju","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71199887","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}