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Wyniki wyszukiwania dla: DRUK TRÓJWYMIAROWY
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Cell Density-Dependent Cytological Stage Profile and Its Application for a Screen of Cytostatic Agents Active Toward Leukemic Stem Cells
PublikacjaProliferation and expansion of leukemia is driven by leukemic stem cells (LSCs). Multidrug resistance (MDR) of LSCs is one of the main reasons of failure and relapses in acute myeloid leukemia (AML) treatment. In this study, we show that maintaining HL-60 at low cell culture density or applying a 240-day treatment with anthrapyridazone (BS-121) increased the percentage of primitive cells, which include LSCs determining the overall...
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Analytical procedures for determination of cocaine and its metabolites in biological samples
PublikacjaThe dangerous effects and increased usage of illicit drugs have inspired the development of analytical methodologies. We based our review of analytical procedures for determination of cocaine (COC) and its metabolites on literature from the past two decades. Our main aim was to compare the capabilities of different analytical techniques. The diversity of matrices from which COC is determined (e.g., blood, hair, saliva, plasma,...
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Physical and Mechanical Evaluation of Silicone-Based Double-Layer Adhesive Patch Intended for Keloids and Scar Treatment Therapy
PublikacjaGrowing interest in silicone elastomers for pharmaceutical purposes is due to both theirbeneficial material effect for scar treatment and their potential as drug carriers. Regarding their morphological structure, silicone polymers possess unique properties, which enable a wide range of applicability possibilities. The present study focused on developing a double-layer adhesive silicone film (DLASil) by evaluating its physical...
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Molecular dynamics and verisimilitude - to what extent can one trust a computational simulation?
PublikacjaFor the last several tens of years, computer simulations have become of undeniable importance. Molecular Dynamics (MD) simulation techniques are used to examine the phenomena which occur at the level that cannot be observed directly. Thus, they can be successfully exploited in many different scientific fields such as: materials science, applied mathematics and theoretical physics, biochemistry, biophysics or drug design. Despite...
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Influence of the addition of citric acid on the physico-chemical properties of poly(sorbitol sebacate-co- butylene sebacate)
PublikacjaThe article presents the results of the physicochemical properties of poly(sorbitol sebacate- co-butylene sebacate) (PSBS) obtained with 0.25; 0.5; 0.75; 1 mol of citric acid (KC). It was shown that PSBS obtained with 0.25 and 0.5 mol KC is characterized by the most optimal mechanical and thermal properties. As a result of the study, it was found that the use of sorbitol and citric acid allows obtaining ester materials with...
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Development of polyurethanes for bone repair
PublikacjaThe purpose of this paper is to review recent developments on polyurethanes aimed at the design, synthesis, modifications, and biological properties in the field of bone tissue engineering. Different polyurethane systems are presented and discussed in terms of biodegradation, biocompatibility and bioactivity. A comprehensive discussion is provided of the influence of hard to soft segments ratio, catalysts, stiffness and hydrophilicity...
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Novel 1,2,3-Triazole Derivatives as Mimics of Steroidal System—Synthesis, Crystal Structures Determination, Hirshfeld Surfaces Analysis and Molecular Docking
PublikacjaHerein, we present the synthesis and crystal structures determination of five 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives containing halogen atoms, 6a–e, which may be used as an excellent mimic of steroids in the drug development process. Good quality crystals obtained for all of the synthesized compounds allowed the analysis of their molecular structures. Subsequently, the determined crystal structures were used to calculate...
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Diminshed toxicity of C-1748, 4-methyl-9-hydroxyethylamino-1-nitroacridine, compared with its demethyl analog, C-857, corresponds to its resistance to metabolism in HepG2 cells
PublikacjaThe narrow "therapeutic window" of anti-tumour therapy may be the result of drug metabolism leading to the activation or detoxification of antitumour agents. The aim of this work is to examine (i) whether the diminished toxicity of a potent antitumour drug, C-1748, 9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine, compared with its 4-demethyl analogue, C-857, results from the differences between the metabolic pathways for the...
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The Metal-Free Regioselective Deuteration of 2-Methylquinolin-8-ol and 2,5-Dimethylquinolin-8-ol, Spectroscopic and Computational Studies
PublikacjaAbstract: Aim and Background: Introducing deuterium to a molecule is of interest to a wide variety of research, including investigation of reaction mechanisms or kinetics, analysis of drug metabolism, structural elucidation of molecules, and syntheses of isotopically labeled materials used for NMR spectroscopy and medicinal research. Objective: The transition-metal-free regioselective deuteration of 2-methylquinolin-8-ol...
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Removal of selected sulfonamides and sulfonamide resistance genes from wastewater in full-scale constructed wetlands
PublikacjaSulfonamides are high-consumption antibiotics that reach the aquatic environment. The threat related to their presence in wastewater and the environment is not only associated with their antibacterial properties, but also with risk of the spread of drug resistance in bacteria. Therefore, the aim of this work was to evaluate the occurrence of eight commonly used sulfonamides, sulfonamide resistance genes (sul1–3) and integrase genes...
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Imidazoacridinone antitumor agent C-1311 as a selective mechanism- based inactivator of human cytochrome P450 1A2 and 3A4 isoenzymes.
Publikacja5-Diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311), a promising antitumor agent that is also active against autoimmune diseases, was determined to be a selective inhibitor of the cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1311 might modulate the effectiveness of other drugs used in multidrug therapy. The present work aimed to identify the mechanism of the observed C-1311-mediated inactivation of CYP1A2...
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Antibiotic-Based Conjugates Containing Antimicrobial HLopt2 Peptide: Design, Synthesis, Antimicrobial and Cytotoxic Activities
PublikacjaRecent studies have shown that modified human lactoferrin 20−31 fragment, named HLopt2, possesses antibacterial and antifungal activity. Thus, we decided to synthesize and evaluate the biological activity of a series of conjugates based on this peptide and one of the antimicrobials with proven antibacterial (ciprofloxacin, CIP, and levofloxacin, LVX) or antifungal (fluconazole, FLC) activity. The drugs were covalently connected...
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Novel insights into conjugation of antitumor-active unsymmetrical bisacridine C-2028 with glutathione: characteristics of non-enzymatic and glutathione S-transferase-mediated reactions
PublikacjaUnsymmetrical bisacridines (UAs) are a novel potent class of antitumor-active therapeutics. A significant route of phase II drug metabolism is conjugation with glutathione (GSH), which can be non-enzymatic and/or catalyzed by GSH-dependent enzymes. The aim of this work was to investigate the GSH-mediated metabolic pathway of a representative UA, C 2028. GSH supplemented incubations of C-2028 with rat, but not with human, liver...
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Zastosowanie metody georadarowej do badań konstrukcji żelbetowych
PublikacjaW pracy przedstawiono zastosowanie metody georadarowej do diagnostyki konstrukcji żelbetowych. Metoda GPR (z ang. ground penetrating radar) należy do grupy badań nieniszczących NDT (z ang. nondestructive testing). Jest ona powszechnie stosowana m. in. w archeologii, geologii i budownictwie. Dzięki tej metodzie możliwa jest identyfikacja warstw geologicznych, podziemnej infrastruktury a także zbrojenia i potencjalnych uszkodzeń...
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Modeling of unsaturated water flow in highly heterogeneous soils.
PublikacjaTematem pracy jest modelowanie przepływu wody w gruntach nienasyconych o podwójnej porowatości, które charakteryzują się obecnością dwóch podobszarów porowatych o skontrastowanych parametrach hydraulicznych. Jako punkt wyjścia przyjęto, że w skali lokalnej przepływ w obu podobszarach jest opisany równaniem Richardsa. Przedstawiono wyprowadzenie dwóch modeli przepływu w skali makroskopowej przy użyciu metody homogenizacji asymptotycznej....
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Identyfikacja dynamiczna i ocena odporności sejsmicznej konstrukcji dwukolumnowego odłącznika wysokiego napięcia
PublikacjaSprawność elementów sieci energetycznej po trzęsieniu ziemi jest bardzo ważnym elementem bezpieczeństwa na obszarze objętym kataklizmem. Brak elektryczności poważnie utrudnia prowadzenie akcji ratunkowej, potęguje chaos, wzmaga panikę wśród mieszkańców. Tymczasem w przeszłości wielokrotnie obserwowano uszkodzenia elementów infrastruktury energetycznej na skutek wstrząsów sejsmicznych. Istotnym elementem systemu energetycznego są...
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Determination of impurities in pharmaceutical products using LC-MS
PublikacjaPharmaceutical products can be contaminated by residues of solvents, reagents (used for the synthesis) or degradation products. Impurities in drug may pose a risk to human health and life, therefore analysis and identification of impurities in pharmaceutical products is veryimportant and inevitable.High performance liquid chromatography coupled with mass spectrometry (MS) is very useful technique for identification impurities in...
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Molecular dynamics studies of polyurethane nanocomposite hydrogels
PublikacjaPolyurethane PEO-based hydrogels have a broad range of biomedical applicability. They are attractive for drug-controlled delivery systems, surgical implants and wound healing dressings. In this study, a PEO based polyurethane hydrogels containing Cloisite R 30B, an organically modified clay mineral, was synthesized. Structure of nanocomposite hydrogels was determined using XRD technique. Its molecular dynamics was studied by means...
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Multimateriałowe oraz wielokolorowe drukowanie wysokiej jakości części z żywic utwardzanych światłem UV w technologii PolyJet
PublikacjaMożliwość budowania multimateriałowych oraz wielokolorowych elementów stanowi ważny trend w rozwoju technologii żywicznych druku 3D. W niniejszym opracowaniu skupiono się na charakterystyce podstawowej metody przetwarzającej ciekłe fotopolimery – technologii PolyJet. Omówiono zasadę jej działania oraz najważniejsze aspekty procesu dotyczące m.in. parametrów drukarki, stosowanych struktur podporowych oraz rodzaju uzyskiwanej powierzchni...
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Optoelectronic investigation of nanodiamond interactions with human blood
PublikacjaWe present optoelectronic investigation of in vitro interactions of whole human blood with different nanodiamond biomarkers. Plasmo-chemical modifications of detonation nanodiamond particles gives the possibility for controlling their surface for biological applications. Optical investigations reveal the biological activity of nanodiamonds in blood dependent on its surface termination. We compare different types of nanodiamonds:...
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Selected Methods for the Chemical Phosphorylation and Thiophosphorylation of Phenols
PublikacjaThis Focus Review gathers together a selection of methods for the chemical phosphorylation of phenols that employ three‐ and four‐coordinate phosphorus compounds. Phosphorylated scaffolds can exhibit enhanced properties compared to their non‐phosphorylated analogues, such as increased biological activity and increased/decreased solubility; as such, phosphorus compounds have gained more and more interest in organic and medicinal...
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Urinary Tract Infections Caused by K. pneumoniae in Kidney Transplant Recipients – Epidemiology, Virulence and Antibiotic Resistance
PublikacjaUrinary tract infections are the most common complication in kidney transplant recipients, possibly resulting in the deterioration of a long-term kidney allograft function and an increased risk of recipient’s death. K. pneumoniae has emerged as one of the most prevalent etiologic agents in the context of recurrent urinary tract infections, especially with multidrug resistant strains. This paper discusses the epidemiology and risk...
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Low frequency of itraconazole resistance found among avian Aspergillus fumigatus isolates
PublikacjaAspergillus fumigatus is the most frequent etiological factor of invasive aspergillosis in human as well as animals, including birds. Aspergillosis caused by drug-resistant strains poses a significant therapeutic issue, especially if resistance pattern includes insensitivity to triazoles, i.e. drugs recommended for the primary therapy purposes. Majority of resistant isolates hold the TR34/L98H...
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Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase
PublikacjaThe antifungal activity of 5‐hydroxy‐4‐oxo‐L‐norvaline (HONV), exhibited under conditions mimicking human serum, may be improved upon incorporation of this amino acid into a dipeptide structure. Several HONV‐containing dipeptides inhibited growth of human pathogenic yeasts of the Candida genus in the RPMI‐1640 medium, with minimal inhibitory concentration values in the 32 to 64 μg mL−1 range. This activity was not affected by multidrug...
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Determination of Toxicological Parameters of Selected Bioactive Organic Chemicals Using the Ostracodtoxkit FTM
PublikacjaAssessment of the impact of pharmaceutical residues on living organisms is very complex subject. Apart from taking into account the toxicity of individual compounds also their presence in mixtures should be taken into account. In this work, attempts were made to assess the ecotoxicity of biologically active substances (with 50 % effective concentration (EC50) values growing from fluoxetine (EC50 = 4.431 nM) >> gemfibrozil ≈ 17α-ethinylestradiol...
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Voriconazole-Based Salts Are Active against Multidrug-Resistant Human Pathogenic Yeasts
PublikacjaVoriconazole (VOR) hydrochloride is unequivocally converted into VOR lactates and valinates upon reaction with silver salts of organic acids. This study found that the anticandidal in vitro activity of these compounds was comparable or slightly better than that of VOR. The Candida albicans clinical isolate overexpressing CaCDR1/CaCDR2 genes, highly resistant to VOR, was apparently more susceptible to VOR salts. On the other hand,...
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Application of bioassays in studies on the impact of pharmaceuticals on the environment
PublikacjaDrug interactions are often desirable particularly in medicine, when treatment of a patient requires using a mixture of drugs in specific doses to produce the adequate therapeutic effect. Unfortunately, interactions between drugs in the environment are not as desirable, despite the fact that drugs are present in the environment at low concentration levels [1]. Pharmaceuticals are present in the environment in a mixture of compounds,...
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Modulation of CYP3A4 activity and induction of apoptosis, necrosis and senescence by the antitumor imidazoacridinone C-1311 in human hepatoma cells
PublikacjaThere is increasing evidence that the expression level of drug metabolic enzymes affects the final cellular response following drug treatment. Moreover, anti-tumour agents may modulate enzymatic activity and/or cellular expression of metabolic enzymes in tumour cells. We investigated the influence of CYP3A4 overexpression on the cellular response induced by the anti-tumour agent C-1311 in hepatoma cells. C-1311-mediated CYP3A4...
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Glucosamine-6-phosphate synthase with an oligoHis insert
PublikacjaGlucosamine-6-phosphate (GlcN-6-P) synthase known also as L-Glutamine: D-fructose-6-phosphate aminotransferase (EC 2.6.1.16), catalyzes the first committed step in the amino sugar biosynthetic pathway in prokaryotic and eukaryotic organisms. The final product of this pathway is an activated precursor of numerous macromolecules containing amino sugars, including chitin and mannproteins in fungi, peptydoglican and lipopolysaccharides...
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Development and evaluation of RADA-PDGF2 self-assembling peptide hydrogel for enhanced skin wound healing
PublikacjaBackground: Wound healing complications affect numerous patients each year, creating significant economic and medical challenges. Currently, available methods are not fully effective in the treatment of chronic or complicated wounds; thus, new methods are constantly sought. Our previous studies showed that a peptide designated as PDGF2 derived from PDGF-BB could be a promising drug candidate for wound treatment and that RADA16-I...
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Application of the near-infrared spectroscopy in the pharmaceutical technology
PublikacjaNear-infrared (NIR) spectroscopy is currently the fastest-growing and the most versatile analytical method not only in the pharmaceutical sciences but also in the industry. This review focuses on recent NIR applications in the pharmaceutical technology. This article covers monitoring, by NIR, of many manufacturing processes, such as granulation, mixing or drying, in order to determine the end-point of these processes. In this...
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Detection of some volatile degradation products released during photoexposition of ranitidine in a solid state
PublikacjaRanitidine (RAN) is on top of the list of prescribed drugs, due to its popularity as a selective H2-receptor antagonist, which efficiently decreases the amount of acid produced in the stomach. RAN is not stable both in a solid state and in a solution, which creates manufacturing problems, requires appropriate storage conditions, and results in a short drug shelf-life. The aim of this work was to study the emission of volatile...
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Application of vibrational spectroscopy, thermal analyses and X-Ray diffraction in the rapid evaluation of the stability in solid-state of ranitidine, famotidine and cimetidine
PublikacjaThis paper reports the study on applicability of Fourier transform infrared (FTIR), near-infrared (NIR) and Raman spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) for the estimation of the chemical stability and photostability of histamine H2-receptor antagonist substances. Ranitidine hydrochloride (RAN), famotidine (FAM) and cimetidine (CIM) were tested and differences in sensitivity were measured...
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VUV photofragmentation of the six-membered heterocyclic molecules containing oxygen
PublikacjaCancer is a significant public health concern worldwide, which results in millions of deaths each year. The standard cure routine for cancer is surgery, and nowadays, radiotherapy or a hadrontherapy. Depending on the type of cancer, patients may undergo additional treatment, including targeted therapy. A combination of radio- or hadron-therapy with proper drug treatment can inhibit the proliferation of cancer cells and thus can...
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Monosubstituted hydrazone β-cyclodextrin derivatives for pH-sensitive complex formation with aromatic drugs
PublikacjaA new and convenient synthetic pathway was developed to produce monosubstituted cyclodextrins with high yields. Each of the β-cyclodextrin derivatives described in this work has an aromatic substituent connected with cyclodextrin core by a pH-sensitive hydrazone linker and a carbon chain. Carbon chains differ in lengths having one or three carbon atoms. The correlation between water solubility and linker length was determined using...
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State of the art and prospects of methods for determination of lipophilicity of chemical compounds
PublikacjaLipophilicity of the compounds is useful to (i) explain their distribution in biological systems, which is different in plant and in animal organisms, (ii) predict the possible pathways of pollutant transport in the environment, and (iii) support drug discovery process and select optimal composition in terms of bioactivity and bioavailability. The lipophilic properties can be determined by two main approaches, experimental, which...
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Optical Magnetometry Based on Nanodiamonds with Nitrogen-Vacancy Color Centers
PublikacjaNitrogen-vacancy color centers in diamond are a very promising medium for many sensing applications such as magnetometry and thermometry. In this work, we study nanodiamonds deposited from a suspension onto glass substrates. Fluorescence and optically detected magnetic resonance spectra recorded with the dried-out nanodiamond ensembles are presented and a suitable scheme for tracking the magnetic-field value using a continuous...
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Zdalne rozpoznawanie twarzy w poprawie bezpieczeństwa osobistego interweniującego funkcjonariusza Policji
PublikacjaStreszczenie: W 2017 r. ruszył w Polsce pilotażowy program zakładania kamer cyfrowych na mundurach policyjnych. Z perspektywy dnia dzisiejszego wiadomo, że kamery będące indywidualnym wyposażeniem policjanta, rejestrując czas, datę i przebieg interwencji, niejednokrotnie stanowią istotny dowód w sprawach spornych, zwłaszcza w sytuacjach pomawiania policjantów o przekroczenie uprawnień podczas interwencji. W dobie nieustannie...
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Metody redukcji rzędu modelu w analizie elektromagnetycznej metodą elementów skończonych
PublikacjaSymulacje numeryczne są wykorzystywane w wielu gałęziach inżynierii, jako podstawowe narzędzie do modelowania zjawisk fizycznych. W trzech ostatnich dekadach zdobyły one szczególną popularność w odniesieniu do pól elektromagnetycznych, w ramach tzw. elektrodynamiki obliczeniowej. Są one niezastąpionym narzędziem w procesie projektowania i optymalizacji urządzeń i systemów mikrofalowych. Jedną z najczęściej wykorzystywanych technik...
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Experimental and theoretical solubility advantage screening of bi-component solid curcumin formulations
PublikacjaA comprehensive experimental and theoretical screening was performed for identification of curcumin solubilizers. Experimental data led to formulation of a non-linear QSPR model correlating molecular descriptors with measured solubilities. The majority of synthesized binary systems exhibited a moderate enhancement of curcumin solubility, which was found to be the highest in the case of curcumin cocrystallized with pyrogallol. New...
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Beyond clinical care: the pharmacoeconomic and research roles of pharmacists in Poland
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Experimental and theoretical studies on the Sulfamethazine-Urea and Sulfamethizole-Urea solid-liquid equilibria
PublikacjaThe miscibility of active pharmaceutical ingredients with excipients is an important aspect in pharmaceutical technology protocols. In this study, the differential scanning calorimetry (DSC) was used for Sulfamethazine-Urea (SI–U) and Sulfamethizole-Urea (SO–U) solid-liquid phase diagrams determination. Both sulfonamides form simple binary eutectics with Urea. The lack of new co-crystal phase formation was confirmed by inspection...
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Neuroprotective Effects of Cannabidiol in Hypoxic Ischemic Insult. The Therapeutic Window in Newborn Mice
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ASSESSMENT OF SAFETY OF PAIN CONTROL BY NON-OPIOID OVER-THE COUNTER MEDICATIONS
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THE USE OF OTC HERBAL SEDATIVES BY PHARMACY PATIENTS – A QUESTIONNAIRES-BASED SURVEY STUDY
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In vitro dissolution test of ketoprofene: development and evaluation of release from soft and hard gelatine capsules
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In vivo evaluation of the antipsoriatic effect of hydrogel with lavandin essential oil and its main components after topical application
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Acetylcholinesterase inhibitors: structure-activity relationship and kinetic studies on selected flavonoids
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NK1 receptor binding of a few low molecular weight 3,5-bistrifluoromethylbenzene derivatives
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Quantitative chirality in the binding of androgens to their receptor
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