Претрага

Упит dcterms_subject_txt:fasted/fed bioavailability

7 items

  • Overcoming the Low Oral Bioavailability of Deuterated Pyrazoloquinolinone Ligand DK-I-60-3 by Nanonization: A Knowledge-Based Approach

    Jelena R. Mitrović , Branka Divović-Matović, Daniel E. Knutson, Jelena B. Ðoković, Aleksandar Kremenović, Vladimir D. Dobričić, Danijela V. Randjelović, Ivana Pantelić, James M. Cook, Miroslav M. Savić, Snežana D. Savić (2021)
    Poor water solubility of new chemical entities is considered as one of the main obstacles in drug development, as it usually leads to low bioavailability after administration. To overcome these problems, the selection of the appropriate formulation technology needs to be based on the physicochemical properties of the drug and introduced in the early stages of drug research. One example of the new potential drug substance with poor solubility is DK-I-60-3, deuterated pyrazoloquinolinone, designed for the treatment of various neuropsychiatric ...
    pyrazoloquinolinones, nanocrystals, wet media milling, fasted/fed bioavailability
    ... the developed formulations in rats, two to three-fold bioavailability enhancement was observed in plasma and investigated organs, including the brain. Keywords: pyrazoloquinolinones; nanocrystals; wet media milling; fasted/fed bioavailability 1. Introduction The emerging trends in the combinatorial ...
    ... nal affil- ‘ations bioavailability enhancement was observed in plasma and investigated organs, including the brain. Copyright: © 2021 by the authors. Licensee MDPI, Basel, Switzerland. Keywords: pyrazoloquinolinones; nanocrystals; wet media milling; fasted/fed bioavailability 1. Introduction This ...
    ... group containing 18 an- imals (three animals per time point): group I received F5 in fasted conditions, group II received F5 in fed conditions, group III received S5 in fasted conditions, and group IV received S5 in fed conditions. The test formulations were administered orally via a gastric probe in a ...

  • Freeze-dried nanocrystal dispersion of novel deuterated pyrazoloquinolinone ligand (DK-I-56-1): Process parameters and lyoprotectant selection through the stability study

    Jelena R. Mitrović, Maja Bjelošević Žiberna, Aleksandar Vukadinović, Daniel E. Knutson, Dishary Sharmin, Aleksandar Kremenović, Pegi Ahlin Grabnar, Odon Planinšek, Dominique Lunter, James M. Cook, Miroslav M. Savić, Snežana D. Savić (2023)
    Recently, nanocrystal dispersions have been considered as a promising formulation strategy to improve the bioavailability of the deuterated pyrazoloquinolinone ligand DK-I-56-1 (7‑methoxy-2-(4‑methoxy-d3-phenyl)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one). In the current study, the freeze-drying process (formulation and process parameters) was investigated to improve the storage stability of the previously developed formulation. Different combinations of lyoprotectant (sucrose or trehalose) and bulking agent (mannitol) were varied while formulations were freeze-dried under two conditions (primary drying at -10 or -45 °C). The obtained lyophilizates were characterized in terms ...
    Pharmaceutical Science
    ... stability and bioavailability, deuterated analogues, including DK-I-56-1 (7-methoxy-2-(4-methox- y-d3-phenyl1)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one), have been developed. Deuteration of a methoxy group increased the stability of DK-I-56-1 to O-demethylation, as well as bioavailability and brain ...
    ... ABSTRACT Keywords: Recently, nanocrystal dispersions have been considered as a promising formulation strategy to improve the Pyrazoloquinolinone bioavailability of the deuterated pyrazoloquinolinone ligand DK-I-56-1 (7-methoxy-2-(4-methoxy-d3-phenyl)- Nanocry“?ls 2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one) ...
    ... commonly used oils, co-solvents, and organic solvents, nanocrystal dispersion has been chosen as a formulation strategy to further improve bioavailability and enable future drug development (Mitrović et al., 2020). Nanocrystal dispersions are submicron size dispersions of drug nanoparticles stabilized ...

  • Curcumin nanonization using an alternative small-scale production unit: selection of proper stabilizer applying basic physicochemical consideration and biological activity assessment of nanocrystals

    Ines Nikolić, Jelena Antić-Stanković, Dragana Božić, Danijela Ranđelović, Bojan Marković, Dominique Jasmin Lunter, Aleksandar Kremenović, Miroslav Savić, Snežana Savić (2020)
    As the number of poorly soluble drugs is increasing, nanocrystals have become very interesting due to wide range of application possibilities. Curcumin was used as a model active ingredient in this work. Even though it has many proven positive effects, due to its physicochemical issues, its possibilities have not been fully exploited. The goal of this work was to select optimal conditions for a top-down method for curcumin nanosuspension production, and to perform their comprehensive characterization applying complementary methodologies: ...
    nanocrystal, curcumin, top-down method, wetball milling

  • The influence of Al<sup>3+</sup>ion on porcine pepsin activity<i>in vitro</i>

    Vesna M. Pavelkić, Kristina R. Gopcević, Danijela Z. Krstić, Marija A. Ilić (2008)
    The in vitro effect of Al3þ ions in the concentration range 1.7·1026M–8.7·1023M on pepsin activity at pH 2, via kinetic parameters and its electrophoretic mobility was evaluated. Kinetic study demonstrated the existence of an activation effect of Al3þ at pH 2 on pepsin molecule. Kinetic analysis with respect to concentrations of haemoglobin showed that Al3þ ions increase the maximal velocity (Vmax) and kcat values rather than apparent affinity for substrate (KS) implying the non-competitive nature of activation which indicated ...
    Пепсин, алуминијум, кинетика, активација, електрофоретска мобилност
    ... Pavelhic et al. [34] precipitation assay to complex samples: Aluminium binding capacity of human gastrointestinal fluids. Chem Spec Bioavailability 2004;16:7—104. OCottrell JT, Harris LJ., Tanaka T, Yada RY. The sole lysine residue in porcine pepsin works as a key residue for catalysis ...

  • Mikroelementi u uljnim šejlovima Aleksinca i njihov uticaj na životnu sredinu

    Nikoleta Aleksić (2021)
    ... for bioavailability of pyrene. Water Science and Technology 77, 439–447. 31. Spasojević, J.M., Maletić, S.P., Rončević, S.D., Radnović, D. V., Čučak, D.I., Tričković, J.S., Dalmacija, B.D., 2015. Using chemical desorption of PAHs from sediment to model biodegradation during bioavailability assessment ...
    ... major and trace element bioavailability in vineyard soil applying different single extraction procedures and pseudo-total digestion. Chemosphere 171, 284–293. [3] Milićević, T., Aničić Urošević, M., Relić, D., Vuković, G., Škrivanj, S., Popović, A. (2018a). Bioavailability of PTE in soil-grapevine ...
    ... amendment with activated carbon, Journal of Contaminant Hydrology 129–130, 25–37. 13. Beckingham, B., Ghosh, U. 2011. Field-scale reduction of PCB bioavailability with activated carbon amendment to river sediments. Environmental Science & Technology 45, 10567–10574. 14. Cornelissen, G., Krusa, M.E., Breedveld ...

  • A survey of greenhouse gases production in central European lignites

    Anna Pytlak, Anna Szafranek-Nakonieczna, Weronika Goraj, Izabela Śnieżyńska, Aleksandra Krążała, Artur Banach, Ivica Ristović, Mirosław Słowakiewicz, Zofia Stępniewska (2021)
    Lignit, Gasovi sa efektom staklene bašte, Ugljen dioksid, Metan, Azotni oksid
    ... desorption (e.g., Kholod et al., 2020). In the case of hard coals, which are resistant to biodegradation, these calcu- lations are justified. However, bioavailability of the organic matter for microbial processes increases with decreasing thermal maturity (Robbins et al., 2016) and in the case of brown coal, ...

  • Mineral Resources of Serbia: Environmental, Societal and Economic Challenges

    Vladimir Simić, Rade Jelenković, Dragana Životić (2019)
    ... pollution of the freshwater systems (river, lake and groundwater), soil and sediments by heavy metals, through the study of their mobility, the bioavailability Environmental risk assessment Complimentary Contributor Copy In: Serbia ISBN: 978-1-53614-897-8 Editor: Igor Janev O 2019 Nova Science ...
    ... Journal of Environmental Research 12(2):135-146. Alloway, B.J. 2013. Heavy Metals in Soils. Trace Metals and Metalloids in Soils and their Bioavailability. Environmental Pollution (22). Third Edition. Springer Dordrecht Heidelberg New York London. Complimentary Contributor Copy 350 Slađana ...
    ... 80 9.56 Countries USA 2855 -1.21 4.15 Brazil 2854 1.01 7.49 Argentina 2436 4.01 16.28 China 821 3.95 6.57 India 177 -0.73 14.61 Russian Fed. 304 3.85 9.60 Ukraine 819 4.68 11.52 Serbia 2479 -5.97 21.11 Italy 3322 -2.07 9.54 Mexico 507 0.53 20.73 Romania 932 -0.85 21.05 Iran 2367 ...