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Plant-derived polyphenols are bioactive compounds with potential health-promoting properties including antioxidant, anti-inflammatory, and anticancer activity. However, their beneficial effects and biomedical applications may be limited due to their low bioavailability. In the present study, we have considered a microencapsulation-based drug delivery system to investigate the anticancer effects of polyphenol-rich (apigenin, caffeic acid, and luteolin) fractions, extracted from a cereal crop pearl millet (Pennisetum glaucum), using three phenotypically different cellular models of breast cancer in vitro, namely triple negative HCC1806, ER-positive HCC1428, and HER2-positive AU565 cells. Encapsulated polyphenolic extract induced apoptotic cell death in breast cancer cells with different receptor status, whereas it was ineffective against non-tumorigenic MCF10F cells. Encapsulated polyphenolic extract was also found to be cytotoxic against drug-resistant doxorubicin-induced senescent breast cancer cells that were accompanied by increased levels of apoptotic and necrotic markers, cell cycle inhibitor p21 and proinflammatory cytokine IL8. Furthermore, diverse responses to the stimulation with encapsulated polyphenolic extract in senescent breast cancer cells were observed, as in the encapsulated polyphenolic extract-treated non-proliferating AU565 cells, the autophagic pathway, here cytotoxic autophagy, was also induced, as judged by elevated levels of beclin-1 and LC3b. We show for the first time the anti-breast cancer activity of encapsulated polyphenolic extract of pearl millet and postulate that microencapsulation may be a useful approach for potentiating the anticancer effects of phytochemicals with limited bioavailability.
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The reaction of glycerol with CO2 to produce glycerol carbonate was performed successfully in the presence of gold nanoparticles (AuNPs) supported by a metal-organic framework (MOF) constructed from mixed carboxylate (terephthalic acid and 1,3,5-benzenetricarboxylic acid). The most efficient were two AuNPs@MOF catalysts prepared from pre-synthesized MOF impregnated with Au3+ salt and subsequently reduced to AuNPs using H2 (catalyst 4%Au(H2)@MOF1) or reduced with NaBH4 (catalyst 4%Au@PEI-MOF1). Compared to existing catalysts, AuNPs@MOFs require simple preparation and operate under mild and sustainable conditions, i.e., a much lower temperature and the lowest CO2 overpressure ever reported, with MgCO3 having been found to be the optimal dehydrating agent. Although the yield of the process is still not competitive with previously developed systems, the most promising advantage is the highest TOF (78 h-1) ever reported for this reaction. The optimal parameters observed for AuNPs were also tested on AgNPs and CuNPs with promising results, suggesting their great potential for industrial application. The catalysts were characterized by XRD, TEM, SEM-EDS, ICP-MS, XPS, and porosity measurements, confirming that AuNPs are present in low concentration, uniformly distributed, and confined to the cavities of the MOF.
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The surface modification of magnetite nanoparticles (Fe3O4 NPs) is a promising approach to obtaining biocompatible and multifunctional nanoplatforms with numerous applications in biomedicine, for example, to fight cancer. However, little is known about the effects of Fe3O4 NP-associated reductive stress against cancer cells, especially against chemotherapy-induced drug-resistant senescent cancer cells. In the present study, Fe3O4 NPs in situ coated by dextran (Fe3O4@Dex) and glucosamine-based amorphous carbon coating (Fe3O4@aC) with potent reductive activity were characterized and tested against drug-induced senescent breast cancer cells (Hs 578T, BT-20, MDA-MB-468, and MDA-MB-175-VII cells). Fe3O4@aC caused a decrease in reactive oxygen species (ROS) production and an increase in the levels of antioxidant proteins FOXO3a, SOD1, and GPX4 that was accompanied by elevated levels of cell cycle inhibitors (p21, p27, and p57), proinflammatory (NFκB, IL-6, and IL-8) and autophagic (BECN1, LC3B) markers, nucleolar stress, and subsequent apoptotic cell death in etoposide-stimulated senescent breast cancer cells. Fe3O4@aC also promoted reductive stress-mediated cytotoxicity in nonsenescent breast cancer cells. We postulate that Fe3O4 NPs, in addition to their well-established hyperthermia and oxidative stress-mediated anticancer effects, can also be considered, if modified using amorphous carbon coating with reductive activity, as stimulators of reductive stress and cytotoxic effects in both senescent and nonsenescent breast cancer cells with different gene mutation statuses.
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Antineoplásicos , Neoplasias de la Mama , Hipertermia Inducida , Nanopartículas de Magnetita , Nanopartículas , Humanos , Femenino , Línea Celular Tumoral , Carbono/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Compuestos Férricos/farmacología , Antineoplásicos/farmacología , Autofagia , Nanopartículas Magnéticas de Óxido de HierroRESUMEN
The development of sustainable biomaterials and surfaces to prevent the accumulation and proliferation of viruses and bacteria is highly demanded in healthcare areas. This study describes the assembly and full characterization of two new bioactive silver(I) coordination polymers (CPs) formulated as [Ag(aca)(µ-PTA)]n·5nH2O (1) and [Ag2(µ-ada)(µ3-PTA)2]n·4nH2O (2). These products were generated by exploiting a heteroleptic approach based on the use of two different adamantoid building blocks, namely 1,3,5-triaza-7-phosphaadamantane (PTA) and 1-adamantanecarboxylic (Haca) or 1,3-adamantanedicarboxylic (H2ada) acids, resulting in the assembly of 1D (1) and 3D (2). Antiviral, antibacterial, and antifungal properties of the obtained compounds were investigated in detail, followed by their incorporation as bioactive dopants (1 wt %) into hybrid biopolymers based on acid-hydrolyzed starch polymer (AHSP). The resulting materials, formulated as 1@AHSP and 2@AHSP, also featured (i) an exceptional antiviral activity against herpes simplex virus type 1 and human adenovirus (HAd-5) and (ii) a remarkable antibacterial activity against Gram-negative bacteria. Docking experiments, interaction with human serum albumin, mass spectrometry, and antioxidation studies provided insights into the mechanism of antimicrobial action. By reporting these new silver CPs driven by adamantoid building blocks and the derived starch-based materials, this study endows a facile approach to access biopolymers and interfaces capable of preventing and reducing the proliferation of a broad spectrum of different microorganisms, including bacteria, fungi, and viruses.
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Plata , Virus , Humanos , Plata/farmacología , Plata/química , Polímeros/farmacología , Polímeros/química , Antibacterianos/farmacología , Antibacterianos/química , Bacterias , Antivirales/farmacología , Almidón , Proteínas Sanguíneas , Chaperonas MolecularesRESUMEN
Hepatocellular damage by the harmful effects of xenobiotics, which increase the production of free radicals, is a widespread phenomenon. The extract from the leaves of Cynara scolymus L. available as an artichoke preparation (natural source) of antioxidants may serve as a potential hepatoprotective factor. This study aimed to evaluate the impact of the protective and regenerative properties of artichoke preparation on the liver in three extract doses: 0.5; 1.0; and 1.5 g/kg bw/day. The evaluation was conducted by measuring the levels of oxidative stress parameters, including glutathione (GSH), glutathione S-transferases (GST), nitric oxide (NO), superoxide dismutase (SOD), catalase (CAT), Trolox equivalent antioxidant capacity (TEAC), thiobarbituric acid reactive substances (TBARS), glutathione peroxidase (GPx), paraoxonase 1 (PON1), SH- group, nitrosylated protein (RSNO), as well as such liver enzymes as alanine aminotransferase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase (ALP) in the plasma and liver homogenate of rats with liver damage induced by CCl4 (1 mL/kg bw). Measurements were taken in plasma and liver homogenate. The results have demonstrated that the artichoke preparation, owing to its high antioxidative potential, exhibits protective and regenerative effects on the liver. This is supported by the observation of higher GSH levels in the plasma of rats treated with artichoke extract for two weeks before CCl4 exposure. Furthermore, the artichoke extract has shown regenerative properties, as evidenced by lower ALT, AST, and SOD activity in the group treated with artichoke extract after CCl4 exposure. These findings suggest that the in vivo administration of artichoke preparation may be beneficial for the protection and regeneration of the liver.
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BACKGROUND: Glioblastoma (GBM) is the most frequently occurring primary malignant central nervous system tumor, with a poor prognosis and median survival below two years. Administration of a combination of non-steroidal anti-inflammatory drugs and natural compounds that exhibit a curative or prophylactic effect in cancer is a new approach to GBM treatment. This study aimed to investigate the synergistic antitumor activity of etoricoxib (ETO) and cannabidiol (CBD) in a GBM cell line model, and to develop poly(lactic-co-glycolic acid) (PLGA)-based nanoparticles (NPs) for these two substances. METHODS: The activity of ETO+CBD was determined using the MTT test, cell-cycle distribution assay, and apoptosis analysis using two GBM cell lines, namely, T98G and U-138 MG. The PLGA-based NPs were developed using the emulsification and solvent evaporation method. Their physicochemical properties, such as shape, size, entrapment efficiency (EE%), in vitro drug release, and quality attributes, were determined using scanning electron microscopy, diffraction light scattering, high-performance liquid chromatography, infrared spectroscopy, and differential scanning calorimetry. RESULTS: The combination of ETO and CBD reduced the viability of cells in a dose-dependent manner and induced apoptosis in both tested GBM cell lines. The developed method allowed for the preparation of ETO+CBD-NPs with a spherical shape, mean particle size (MPS) below 400 nm, zeta potential (ZP) values from -11 to -17.4 mV, polydispersity index (PDI) values in the range from 0.029 to 0.256, and sufficient EE% of both drugs (78.43% for CBD, 10.94% for ETO). CONCLUSIONS: The combination of ETO and CBD is a promising adjuvant therapeutic in the treatment of GBM, and the prepared ETO+CBD-NPs exhibit a high potential for further pharmaceutical formulation development.
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The selective oxidation of alcohols, leading to appropriate aldehydes, is widely recognised as one of the most important reactions in organic synthesis. With ever-increasing environmental concerns, much attention has been directed toward developing catalytic protocols that use molecular oxygen as an oxidant. An ideal green oxidation process should employ a highly active, selective and recyclable catalyst that can work with oxygen under mild conditions. This paper presents a successful application of densely grafted silver nanostructures with stable nitroxide radicals (N-AgNPs) as an effective, easily-recovered and regenerable catalyst for the selective oxidation of alcohols. The fabricated ultra-small and narrow dispersive silver nanoparticles have been fully characterised using physicochemical methods (TEM, DLS, XPS, TGA). N-AgNPs have been successfully applied to oxidise several model alcohols: benzyl alcohol, 4-pyridinemethanol, furfuryl alcohol, 1-phenyl ethanol, n-heptanol and allyl alcohol under mild conditions using oxygen as a stoichiometric oxidant. Notably, the fabricated nitroxide grafted silver nanoparticles (N-AgNPs) were reused more than ten times in the oxidation of a series of primary alcohols to corresponding aldehydes under mild conditions with very high yields and a selectivity close to 100%.
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Coordination polymers have emerged as a new class of potent biologically active agents due to a variety of important characteristics such as the presence of bioactive metal centers and linkers, low toxicity, stability, tailorable structures, and bioavailability. The research on intermediate metabolites has also been explored with implications toward the development of selective anticancer, antimicrobial, and antiviral therapeutic strategies. In particular, quinolinic acid (H2quin) is a recognized metabolite in kynurenine pathway and potent neurotoxic molecule, which has been selected in this study as a bioactive building block for assembling a new silver(I) coordination polymer, [Ag(Hquin)(µ-PTA)]n·H2O (1). This product has been prepared from silver oxide, H2quin, and 1,3,5-triaza-7-phosphaadamantane (PTA), and fully characterized by standard methods including single-crystal X-ray diffraction. Compound 1 has revealed distinctive bioactive features, namely (i) a remarkable antiviral activity against herpes simplex virus type 1 (HSV-1) and adenovirus 36 (Ad-36), (ii) a significant antibacterial activity against clinically important bacteria (Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa), and (iii) a selective cytotoxicity against HeLa (human cervix carcinoma) cell line. The present work widens a growing family of bioactive coordination polymers with potent antiviral, antibacterial, and antiproliferative activity.
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Antibacterianos/farmacología , Antineoplásicos/farmacología , Complejos de Coordinación/farmacología , Polímeros/farmacología , Ácido Quinolínico/farmacología , Plata/farmacología , Antibacterianos/síntesis química , Antibacterianos/química , Antineoplásicos/síntesis química , Antineoplásicos/química , Proliferación Celular/efectos de los fármacos , Complejos de Coordinación/síntesis química , Complejos de Coordinación/química , Ensayos de Selección de Medicamentos Antitumorales , Escherichia coli/efectos de los fármacos , Células HeLa , Humanos , Pruebas de Sensibilidad Microbiana , Polímeros/síntesis química , Polímeros/química , Pseudomonas aeruginosa/efectos de los fármacos , Ácido Quinolínico/química , Plata/química , Staphylococcus aureus/efectos de los fármacosRESUMEN
Sulforaphane(SFN) and erucin(ERN) are isothiocyanates (ITCs) bearing, respectively, methylsulfinyl and methylsulfanyl groups. Their chemopreventive and anticancer activity is attributed to ability to modulate cellular redox status due to induction of Phase 2 cytoprotective enzymes (indirect antioxidant action) but many attempts to connect the bioactivity of ITCs with their radical trapping activity failed. Both ITCs are evolved from their glucosinolates during food processing of Cruciferous vegetables, therefore, we studied antioxidant behaviour of SFN/ERN at elevated temperature in two lipid systems. Neither ERN nor SFN inhibit the oxidation of bulk linolenic acid (below 100 °C) but both ITCs increase oxidative stability of soy lecithin (above 150 °C). On the basis of GC-MS analysis we verified our preliminary hypothesis (Antioxidants2020, 9, 1090) about participation of sulfenic acids and methylsulfinyl radicals as radical trapping agents responsible for the antioxidant effect of edible ITCs during thermal oxidation of lipids at elevated temperatures (above 140 °C).
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Antioxidantes/química , Isotiocianatos/química , Succinatos/química , Ácidos Sulfénicos/química , Sulfuros/química , Sulfóxidos/química , Tiocianatos/química , Brassicaceae/química , Manipulación de Alimentos , Glucosinolatos/química , Oxidación-ReducciónRESUMEN
In this communication we demonstrate that two natural isothiocyanates, sulforaphane (SFN) and erucin (ERN), inhibit autoxidation of lipids at 140 °C but not below 100 °C. This effect is due to thermal decomposition of ERN and SFN to sulfenic acids and methylsulfinyl radicals, species able to trap lipidperoxyl radicals. Our observations shed new light on thermal processing of vegetables containing these two isothiocyanates.
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Hepatitis C virus (HCV) affects approx. 3% of the world's population and accounts for ca 300â¯000 deaths per year. 80% of individuals with HCV develop chronic symptoms which, when untreated, may cause cirrhosis (27%) or hepatocellular carcinoma (25%). The hepatitis C virus is a (+)ssRNA enveloped virus of the family Flaviviridae. Seven major HCV genotypes and their subtypes (a, b) have been identified. In the 1990s, interferons alpha-2 were used in the treatment of HCV and in the next decade HCV therapy was based on pegylated interferon alpha-2 in combination with ribavirin. Since 2011, interferons alpha, DNA and RNA polymerase inhibitors, NS3/4A RNA protease inhibitors, NS5 RNA serine protease inhibitors, NS5B RNA polymerase inhibitors have been approved for clinical use. Monotherapy is avoided in medication due to rapidly developing viral resistance. A total of 113 papers were included comprising original publications and reviews. The paper reviews the molecular targets and chemical structures of drugs used in HCV treatment. Indications and contraindications for anti-HCV drugs are also discussed together with application regimens.
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Hepatitis C/tratamiento farmacológico , Terapia Molecular Dirigida/métodos , Animales , Antivirales/química , Antivirales/farmacología , ARN Polimerasas Dirigidas por ADN/antagonistas & inhibidores , Inhibidores Enzimáticos/uso terapéutico , Humanos , Estructura Molecular , Terapia Molecular Dirigida/efectos adversos , Inhibidores de Proteasas/uso terapéuticoRESUMEN
OBJECTIVES: As plasma and salivary total antioxidant capacity (TAC) is mainly contributed by uric acid (UA), the present study measures non-urate TAC (Nu-TAC). The aim of the study was to correlate plasma native TAC, Nu-TAC and UA with their salivary analogues, and compare the UA contribution in both body fluids using two different methods. METHODS: The study involved 55 middle-aged and older subjects (66.7 ± 4.5 years). TAC was determined simultaneously with two methods (ferric reducing ability of plasma - FRAP, 2.2-diphenyl-1-picryl-hydrazyl - DPPH and countertypes for saliva - FRAS and DPPHS test), with and without UA (native TAC and Nu-TAC, respectively). Plasma UA and salivary UA (SUA) were assessed. RESULTS: Subjects with increased FRAP, DPPH and UA had higher FRAS, DPPHS and SUA, respectively (P < 0.05). Plasma Nu-TAC indices did not correlate with salivary Nu-TAC. The contribution of UA to the plasma and salivary DPPH tests was similar: 75.7 ± 10.3% and 75.2 ± 14.0%, respectively. However, the contribution of UA to FRAS was higher than that for FRAP (71.6 ± 13.9% vs. 64.0 ± 8.1%; P < 0.001). DISCUSSION: Our findings suggest that saliva is a good predictor for native plasma TAC but not for Nu-TAC. UA level is comparably dominant in saliva and in plasma according to DPPH, but lower in plasma according to FRAP.
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Antioxidantes/análisis , Ayuno/fisiología , Saliva/metabolismo , Anciano , Inhibidores de la Enzima Convertidora de Angiotensina/uso terapéutico , Aspirina/uso terapéutico , Ayuno/sangre , Femenino , Humanos , Hipoglucemiantes/uso terapéutico , Masculino , Persona de Mediana Edad , Saliva/química , Ácido Úrico/análisis , Ácido Úrico/sangreRESUMEN
Hydrochloride of 10-{2-hydroxy-3-[N,N-bis-(2-hydroxyethyl)amino]propyl}-2-trifluoromethylphenothiazine (Flu-A) is a analogue of neuroleptic fluphenazine. Flu-A exhibits anti-multidrug resistance, antimutagenic, proapoptopic, and cancer-chemopreventive activities in screening studies. To define identity, quality, and purity of new active substance it is necessary to develop a appropriate analytical method and to establish a degradation profile. Thus, a stability-indicating reversed-phase high-performance liquid chromatography method was developed and validated for quantitative determination of Flu-A in the presence of its degradation products generated under stress conditions. The compound was subjected to oxidation, photolysis, and degradation in aqueous solutions (neutral and acidic), and solid state according to the International Council for Harmonisation Guidelines. The method was also found to be suitable for intermediate and accelerated studies and for the evaluation of kinetic mechanism of Flu-A degradation in aqueous solutions (pH 5.1-7.5, 353 K). The structures of main potential degradation products were established using high-performance liquid chromatography-Electrospray Ionization-mass spectrometry method.
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Electrocatalytic determination of NADH using a hybrid surface-modified electrode with multi-wall carbon nanotubes (MWCNTs) and a novel electrogenerated redox mediator is described. The redox mediator precursor - fluphenazine (Flu) was adsorbed on MWCNT-modified glassy carbon (GC) electrode which was then subjected to electrochemical activation in 0.1 M H2SO4 using cyclic voltammetry (CV) over a range of potentials -0.2 to 1.5 V vs. Ag/AgCl (6 scans at 100 mV s(-1)). Cyclic voltammograms of Flu indicated the formation of a stable electroactive material presenting one reversible redox couple at the formal potential of -0.115 vs. Ag/AgCl in a phosphate buffer (pH7.0) as a supporting electrolyte. The peaks increased linearly with increasing scan rate indicating electroactive molecules anchored to the electrode surface. The GC/MWCNT/Flu electrode efficiently catalyzed the oxidation of NADH with a decrease in the overpotential of about 600 mV and 150 mV compared to the bare GC and GC/MWCNT electrode, respectively. This modified electrode was successfully used as the working electrode in the chronoamperometric analysis. The peak current response to NADH was linear over its concentration range from 15 µM to 84 µM, and correlation coefficient 0.998. The limits of detection (5 µM) and quantitation (15 µM) were evaluated.
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Electroquímica/métodos , Flufenazina/química , NAD/análisis , NAD/química , Nanotubos de Carbono/química , Calibración , Catálisis , Electroquímica/instrumentación , Electrodos , Límite de Detección , Oxidación-ReducciónRESUMEN
The risk of cardiovascular diseases is closely related to hypertension, high cholesterol levels, and diabetes. When these risk factors appear together they are referred to as a metabolic syndrome. In the treatment of cardiovascular diseases, a combination of antihypertensive, hypolipemiant, and antidiabetic drugs is often applied. Diuretics (chlortalidone, hydrochlorothiazide, etc.) and angiotensin II receptors antagonist (sartans) are used to control hypertension, whereas statins (fluvastatin, simvastatin, etc.) are used to reduce cholesterol levels. This review is concerned with methods for the analysis of sartans in various matrices, such as pharmaceutical formulations, environmental and biological samples, and discusses the current status of stability studies of sartans . It also presents analytical methods for the simultaneous determination of sartans, diuretics, and statins.
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Bloqueadores del Receptor Tipo 1 de Angiotensina II/farmacología , Bloqueadores del Receptor Tipo 1 de Angiotensina II/uso terapéutico , Animales , Diuréticos/farmacología , Diuréticos/uso terapéutico , Humanos , Inhibidores de Hidroximetilglutaril-CoA Reductasas/farmacología , Inhibidores de Hidroximetilglutaril-CoA Reductasas/uso terapéuticoRESUMEN
A simple and sensitive extractive spectrophotometric method have been developed and validated for determination of amantadine hydrochloride (AM), memantine hydrochloride (MM) and rimantadine hydrochloride (RM) in pure and pharmaceutical formulations. The method is based on the reaction of these active compounds with bromophenol blue (BB) in acetate buffer (0.1 M) pH 3.5 to form an orange-colored products which have absorption maxima at 408 nm. The procedure of complexation was optimized with regard to such factors as concentrations of BB, pH of medium, a kind of extracting solvents and a number of extractions. Under the optimum conditions, linear relationships A408 = f(c) with good correlation coefficients (≥0.996) and low limit of detection were obtained in the ranges of 50.0-220.0 µg·mL(-1), 20.0-150.0 µg·mL(-1) or 10.0-110.0 µg·mL(-1) for AM, MM and RM, respectively, for the spectrophotometric methods. The proposed method could be applied to the determination of AM, MM and RM in dosage forms. The recovery was 95.3-101.9%. The method was linear, precise and accurate.
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Adamantano/análisis , Azul de Bromofenol/química , Preparaciones Farmacéuticas/química , Espectrofotometría Ultravioleta/métodos , Indicadores y Reactivos/química , Límite de DetecciónRESUMEN
The possibility of application of fluorescein and radioactive 99mTc as tracers for determination of residence time distribution of liquid phase and for diagnosing hydrodynamic conditions in apparatuses for membrane separation was studied. Two different ultrafiltration systems with diverse arrangement of liquid flow: the apparatus with helical flow generated by the movable element (inner cylinder) and the tubular module with cross flow filtration, were tested by the RTD technique. The tracer studies were supplemented with modelling. The optimal conditions enabling to handle the plug flow-like structure in the helical apparatus were determined. The minimum of dimensionless variance (vard) was obtained at P=0.765 bar, Q(R)=121.88 l/h and Ω=2887.5 rpm. In spite of higher linear velocities attained in the tubular cross-flow module, the flow structure in the helical apparatus was more similar to the ideal plug flow pattern that was demonstrated by higher Peclet numbers and lower values of the dimensionless variance. Application of movable part and Couette-Taylor flow in the membrane apparatus may balance the advantages coming from high flow rates applied in cross-flow filtration systems minimising formation of the deposit on the membrane surface and reducing membrane fouling.
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The content of pyridoxine hydrochloride in two-component pharmaceutical preparations containing various magnesium compounds was examined. The UV differentiation spectrophotometry was devised and compared with the reference method of high performance liquid chromatography (HPLC). The analysis of the absorbance spectra (A) and its first (D1) and second (D2) derivatives made it possible to establish the appropriate analytical wavelengths (A: 290 nm; D1: 302 nm; D2: 308 nm). It was proved that spectrum differentiation significantly corrects errors resulting from overlapping background especially when the magnesium hydroaspartate, lactate or magnesium lactogluconate is present together with vitamin B6.
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Compuestos de Magnesio/análisis , Preparaciones Farmacéuticas/análisis , Piridoxina/análisis , Espectrofotometría Ultravioleta , Tecnología Farmacéutica/métodos , Vitamina B 6/análisis , Ácido Aspártico/análisis , Calibración , Cromatografía Líquida de Alta Presión , Estabilidad de Medicamentos , Gluconatos/análisis , Estándares de Referencia , Espectrofotometría Ultravioleta/normas , Tecnología Farmacéutica/normasRESUMEN
The influence of temperature and relative air humidity on the stability of epidoxorubicin hydrochloride (EP) was investigated. The degradation of the substance studied was determined: (a) in dry air at 393K, (b) at relative air humidity ~76% at 333K, 343K, 353K, 363K and 373K, (c) in the relative air humidity range 50-90% at 363K. The degradation of EP in the atmosphere of increased relative air humidity was a first-order reaction relative to substance concentration and in dry, hot air (RH 0%; 393K) is a reversible first-order reaction relative to substance concentration. The dependences lnk=f(1/T) and lnk=f(RH%) were described by the equation: lnk=(35.1±10.9)-(16,250±3823)(1/T) and lnk=(3.79±3.34) × 10(-2) (RH%)-(12.9±2.4), respectively. The kinetic and thermodynamic parameters of EP degradation were calculated. The parameters of separation were following: LiChrospher RP-18 column, 5 µm, 250 mm × 4 mm; mobile phase: the mixture of equal volume of acetonitrile and the solution containing 2.88 gl(-1) of sodium laurisulfate and 2.25 ml l(-1) of phosphoric acid (V) 85%; flow rate: 1.0 ml min (-1); UV detection - 254 nm.
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Antibióticos Antineoplásicos/análisis , Epirrubicina/análisis , Tecnología Farmacéutica , Algoritmos , Cromatografía Líquida de Alta Presión , Daunorrubicina/análisis , Doxorrubicina/análisis , Estabilidad de Medicamentos , Calor/efectos adversos , Humedad/efectos adversos , Cinética , Polvos , TermodinámicaRESUMEN
The stability of N-[2-(4-o-fluorophenylpiperazin-1-yl)ethyl]-2,5-dimethyl-1-phenylpyrrole-3,4-dicarboximide (PDI; a derivative with an analgesic activity) was studied in order to investigate its degradation mechanism and identify its degradation products in aqueous-organic solutions. The stability of PDI and its two degradation products (A and B) was performed with an HPLC method: (LiChrospher C18 column (250 x 4 mm LD., dp = 5 microm), mobile phase: 3.5 g/L solution of sodium lauryl sulfate and 1.6 mL of phosphoric acid(V)-acetonitrile (40:60, v/v), UV detector: 240 nm, flow rate: 1 ml/min). The identification of products A and B was conducted using HPLC-ES-MS and 1H- and 13C-NMR methods.