European Pharmaceutical Journal最新文献

{"title":"Synthesis and Correlation of Aggregation and Antimicrobial Properties of Homochiral Quaternary Ammonium Bromides Derived from Camphoric Acid","authors":"R. Mikláš, N. Miklášová, M. Bukovský","doi":"10.2478/afpuc-2020-0017","DOIUrl":"https://doi.org/10.2478/afpuc-2020-0017","url":null,"abstract":"Abstract A group of homochiral quaternary ammonium salts bearing hydrophobic camphoric acid-derived moiety was synthesized and characterized. The aggregation properties of the prepared compounds were evaluated by surface tension measurements, and the critical micelle concentration (CMC) was calculated. The novel quaternary ammonium bromides were tested as antimicrobial and antifungal agents, and their minimal inhibitory concentration (MIC) was evaluated and compared to clinically used benzalkonium bromide (BAB). Correlation of MIC with CMC reveals that monomers of prepared cationic surfactants, instead of micelles, are primarily responsible for antimicrobial activity.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":"68 1","pages":"10 - 16"},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47555656","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":"Formulation and Evaluation of Tablets Compressed from Granules Prepared by Thermoplastic Granulation","authors":"D. Kloc, T. Wolaschka, F. Ruttkay","doi":"10.2478/afpuc-2021-0003","DOIUrl":"https://doi.org/10.2478/afpuc-2021-0003","url":null,"abstract":"Abstract The aim of this formulation study was to determine the effect of the binder used in the preparation of granules by thermoplastic granulation on the release of propranolol from experimental tablets. Another aim was to select suitable excipients and their ratio in the granules to ensure a trouble-free formulation of the tablets. This study proved that the binder affects the flow properties of the granules, disintegration of the tablets and, subsequently, also the method of drug release, which can be used for the preparation of tablets with modified or prolonged drug release.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":"68 1","pages":"72 - 75"},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48607573","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":"The Antioxidant Analysis of Selected Types of Climbing Plants with Therapeutic Effect","authors":"M. Hrúzová, E. Mňahončáková, J. Šimková","doi":"10.2478/afpuc-2020-0008","DOIUrl":"https://doi.org/10.2478/afpuc-2020-0008","url":null,"abstract":"Abstract Climbing plants with therapeutic effects are relatively little studied group of medicinal species. In the collection of climbing species planted in 2019 in the Botanical Garden of the Slovak University of Agriculture (SUA) in Nitra, we observed the growth and potential food, horticulture and healing use. For the antioxidant analysis, 7 species from 152 plants of 13 genera and 22 species were selected. The highest antiradical activity was recorded in the species Vigna sinensis, where reached average measured values achieved up to 73.79%. However, the related species Vigna unguiculata achieved only 26% of antioxidant activity. Of the fruits, the highest activity was Momordica charantia in immature state (73%). Other fruits showed very low antiradical activity","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":"67 1","pages":"1 - 4"},"PeriodicalIF":0.0,"publicationDate":"2020-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42238923","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":"Study of the Qualitative Composition and Quantitative Content of Parthenolide in the Feverfew (Tanacetum Parthenium) Herb Cultivated in Ukraine","authors":"K. Hordiei, T. Gontova, S. Gubar, M. Yaremenko, E. Kotova","doi":"10.2478/afpuc-2020-0011","DOIUrl":"https://doi.org/10.2478/afpuc-2020-0011","url":null,"abstract":"Abstract Feverfew is a well-known medicinal plant as a source of the sesquiterpene lactones, the main one is a parthenolide (about 85%). Owing to the parthenolide, feverfew herb has anti-inflammatory activity and it is widely used for prevention of migraine. The aim was to study the qualitative composition and quantitative content of the parthenolide in the samples of the feverfew herb cultivated in Ukraine and to study the influence of environmental factors on the accumulation of parthenolide. Methods The identification in the samples of the feverfew herb by the thin-layer chromatography method was carried out on silica gel 60 F254 plates, Merck. For the quantitative determination of the parthenolide, a high-performance liquid chromatography ProStar equipped with a diode-matrix detector, were used. Results The chromatographic profile of the samples of the feverfew herb was studied using a TLC method. In the chromatograms of test solutions from all samples, the blue zones were detected at the level of parthenolide. The quantitative content of parthenolide ranged between 0.16% and 0.39%. The highest content was observed in the sample from the Central region of Ukraine. The data obtained indicate that the optimal conditions for parthenolide accumulation in feverfew herb are as follows: black soils, solar insolation not higher than 5.25 kWh/m2/day, average air temperature from +20°C to +25°C. All the calculated validation parameters of the parthenolide quantitative determination method meet the necessary acceptance criteria. Conclusion The study of the qualitative composition and quantitative content of parthenolide in the samples of feverfew herb cultivated in different regions of Ukraine has been conducted. According to the methodology of Eur.Ph. and SPhU, a parthenolide was identified in all the samples. HPLC method was used to determine the quantitative content of parthenolide in the samples studied. The optimal conditions for parthenolide accumulation in feverfew herb were established.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":"67 1","pages":"27 - 33"},"PeriodicalIF":0.0,"publicationDate":"2020-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45290325","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":"Functionality evaluation of co-processed excipients as diluents in tablets manufactured by wet granulation","authors":"Y. Eshovo Apeji, I. Muhammad, A. Kehinde Olowosulu, G. Owoicho Okpanachi, A. Rukayat Oyi","doi":"10.2478/afpuc-2020-0010","DOIUrl":"https://doi.org/10.2478/afpuc-2020-0010","url":null,"abstract":"Abstract Diluents are essential components of a tablet formulation. The type of diluent used in a formulation influences the quality of tablets produced from that formulation. The aim of this study was to evaluate the tableting properties of co-processed excipients (C-PEs) incorporated as diluents in tablet formulation by wet granulation. Metronidazole tablets were prepared by wet granulation incorporating different diluents that were either single component excipients (SCEs) (lactose and microcrystalline cellulose) or C-PEs (Ludipress®, StarLac®, Prosolv® and AVICEL®HFE). The granules obtained for each formulation were evaluated for particle size analysis, flow properties and compression properties. Tablets weighing 500 mg were compressed from the metronidazole granules on a Single Station Tablet Press using a 12 mm punch and die tooling system. The tablets were kept for 24 h post-production, and the properties of weight uniformity, thickness, tensile strength, friability, disintegration time and dissolution profile evaluated subsequently. Results of granule properties showed that variations in parameters evaluated was as a result of differences in the type and composition of diluent used in formulation. Compactibility and tabletability profile of metronidazole granules revealed a better performance with granules processed with C-PE based diluents compared to SCE-based diluents. Tablets formulated with C-PEs as diluents were uniform in tablet weight, disintegrated faster and yielded a faster drug release compared to tablet formulations containing SCEs as diluent. This study reveals the performance advantage of C-PEs as diluents in tablets manufactured by wet granulation and highlights the importance of rational selection of excipients during tablet formulation.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":"67 1","pages":"5 - 14"},"PeriodicalIF":0.0,"publicationDate":"2020-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41698968","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":"Synthesis, antimicrobial and antiradical activity of (3-alkoxymethyl-4-hydroxyphenyl)propan-1-ones, intermediates of biologically active compounds and activity comparison with 3-(alkoxymethyl)-4-(alkylamino-2-hydroxypropoxyphenyl)alkanones type of beta blockers","authors":"R. Čižmáriková, M. Markuliak, L. Habala, J. Valentová, A. Bilková","doi":"10.2478/afpuc-2020-0012","DOIUrl":"https://doi.org/10.2478/afpuc-2020-0012","url":null,"abstract":"Abstract A homologous series of (3-alkoxymethyl-4-hydroxyphenyl)propan-1-ones was prepared by the reaction of (3-chloromethyl-4-hydroxyphenyl)propan-1-ones with the corresponding alcohols (methanol – decan-1-ol, propan-2-ol, 2-methylpropan-1-ol, 3-methylbutan-1-ol, cyclopentanol, benzylalcohol) in the presence of sodium hydrogen carbonate. The composition of the synthesised compounds was elucidated by IR, UV and 1H-NMR and 13C-NMR spectra. Selected compounds were tested against human pathogens: gram-positive bacterium Staphylococcus aureus (CNCTC Mau 29/58), gram-negative bacterium Escherichia coli (CNCTC 377/79) and yeast Candida albicans (CCM 8186). Their antimicrobial activities were expressed as minimum inhibitory concentrations. Antioxidant activity was determined using DPPH and ABTS.+ methods. It could be shown that both biological activities, antimicrobial and antioxidant, were lower in comparison with the (2RS)-bis [3-(4-acetyl-2-propoxymethyl)phenoxy-2-hydroxypropyl]isopropylammonium fumarate type of beta blockers.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":"67 1","pages":"34 - 44"},"PeriodicalIF":0.0,"publicationDate":"2020-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44655728","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":"Preparation and evaluation of an oral mucoadhesive gel containing nystatin-loaded alginate microparticles","authors":"S. Mohammadi Samani, S. Karimaddini, Z. Sobhani, F. Ahmadi","doi":"10.2478/afpuc-2020-0009","DOIUrl":"https://doi.org/10.2478/afpuc-2020-0009","url":null,"abstract":"Abstract Nystatin is an antifungal agent used for prophylaxis and treatment of candidiasis, especially oral mycosis. Efficacy of nystatin conventional dosage forms is limited by the short residence time and bitter taste of the drug. This research aims at designing an optimized formulation of oral mucoadhesive gel of nystatin-loaded alginate microparticles, which can be retained in the mouth. Sodium alginate solution containing nystatin was added to the solution of calcium chloride under stirring. Microparticles containing nystatin were incorporated into the Carbopol gel. Size, loading, and release profile and mucoadhesion were investigated. The most suitable microparticles with particle size of < 250 μm were prepared with alginate concentration of 1%(w/v), calcium chloride of 1%(w/v), drug:polymer concentration 1%, and ratio of alginate solution:calcium chloride of 1:10. This formulation showed 49.1% drug loading and 98.2% encapsulation efficiency. Carbopol 934 gel provided optimal mucoadhesive properties. Release profile proved a burst release, which can be attributed to the surface associated drug, followed by a slower sustained release phase for all microparticles. The developed system with ability to adhere to the oral mucosa has great appeal for treatment of localized infections and can mask bitter taste of the drug and be retained in the mouth for long periods.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":"67 1","pages":"15 - 21"},"PeriodicalIF":0.0,"publicationDate":"2020-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43341262","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":"Toxicity of primulic acid 1 against a daphnid species Simocephalus expinosus s.l.","authors":"M. Lukáč, M. Pisárčik, R. Horáková, M. Bajcura, B. Horváth, F. Devínsky","doi":"10.2478/afpuc-2020-0013","DOIUrl":"https://doi.org/10.2478/afpuc-2020-0013","url":null,"abstract":"Abstract Primulic acid 1 is the main saponin present in Primula elatior. The present study describes the isolation of this amphiphilic compound from primula root. It was performed by ultrasonic maceration, reverse-phase column chromatography and crystallization. Investigations of its physicochemical property are represented by the determination of critical micelle concentration (cmc). The cmc value of the amphiphile was 9.4 × 10−5 mol·dm−3. The evaluation of environmental toxicity was performed on a daphnid species Simpocephalus expinosus s.l., which was very sensitive to primulic acids 1. The results from acute immobilisation test show that the tested compound has half maximal effective concentration after 24 hours (EC50-24 h) equal to 6.9 mg·l−1. Saponin can be classified as a toxic compound for aquatic organisms.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":"67 1","pages":"22 - 26"},"PeriodicalIF":0.0,"publicationDate":"2020-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41810843","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":"Chitosan Hydrogel Improves Bioavailability of Megosin","authors":"É. Sultanova, M. Salakhutdinova, Y. I. Oshchepkova, A. Asrorov, M. J. Oripova, U. J. Ishimov, S. Salikhov","doi":"10.2478/afpuc-2020-0006","DOIUrl":"https://doi.org/10.2478/afpuc-2020-0006","url":null,"abstract":"Abstract Background The aim of this study was to obtain chitosan hydrogels containing megosin, an antiviral medicinal substance, to prolong its bioavailability. Megosin as an immunomodulating agent possesses at least twice higher virostatic and virucidal activities than gossypol, the megosin precursor, and other imine derivatives of gossypol. Materials and Methods Chitosan, used in this paper, was obtained by deacetylation of chitin; megosin was obtained on the bases of gossypol. Different concentrations of sodium tripolyphosphate (STPP) were used as the cross-linking agent. The release of megosin from hydrogel samples into blood was conducted on five white rats in four groups. Results Infrared spectral data demonstrated cross-linkage that the band responsible for NH bending of the uncross-linked chitosan reduced its intensity and moved to a lower wavelength, 1636 cm−1. It has been proven that megosin contained in gels does not penetrate into the blood and organs after vaginal administration. Release kinetics of megosin from chitosan hydrogels revealed that within 7 h, up to 52% of megosin is allowed into acidic solution (pH 4.5). Conclusion This study demonstrates the possibility to prolong bioavailability of megosin for at least 7 h, during which time it is not released into blood. The obtained results show the possibility to use the gel composition to treat vaginal herpes.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":"67 1","pages":"1 - 6"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47862732","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":"Synthesis, antibacterial and free radical scavenging activity of some newer N-((10-nitro-1H-indolo [1, 2-c]quinazolin-12-yl)methylene)benzenamines","authors":"A. Dixit, D. Pathak, G. Sharma","doi":"10.2478/afpuc-2020-0002","DOIUrl":"https://doi.org/10.2478/afpuc-2020-0002","url":null,"abstract":"Abstract Present research is oriented on the synthesis of some novel 12-(N-arylmethaniminyl)indolo[1,2-c]quinazoline analogs (4b1–4b11) and their characterization by 1H NMR, 13C NMR, FTIR and mass spectrophotometry. Their free radical scavenging activity and antibacterial potential were also evaluated. Many derivatives have shown a marked free radical scavenging capacity in all the concentrations but specifically compounds 4b7, 4b8 and 4b11 have shown good antioxidant potential with an IC50 value of 25.18 μmol/L, 28.09 μmol/L & 44.22 μmol/L, respectively (DPPH method) and 39.46 μmol/L, 44.47 μmol/L & 35.61 μmol/L, respectively (H2O2 method). The antibacterial evaluation was carried out against B. subtilis and E. coli by agar well diffusion method and it revealed that all the compounds in the series were having marked antibacterial activity but compounds 4b9 and 4b11 have shown best antibacterial potential. Then, it was concluded that the derivatives which were containing substituted anilines (4-Nitro, 4-Fluoro, 4-Bromo & 4-Chloro-2-nitro) on the carbon attached on the 12th position of indoloquinazoline moiety were having marked potential as an antibacterial and free radical scavenger.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":"67 1","pages":"7 - 16"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49132413","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}