Searched for: subject%3A%22Pharmacokinetics%22
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Holmberg, A.A. (author), Weidolf, L. (author), Necander, S. (author), Bold, P. (author), Sidhu, S. (author), Pelay-Gimeno, M. (author), de Ligt, R.A.F. (author), Verheij, E.R. (author), Jauhiainen, A. (author), Psallidas, I. (author), Hamrén, U.W. (author), Prothon, S. (author)
This open-label, single-period study describes the human absorption, distribution, metabolism, excretion, and pharmacokinetics of velsecorat (AZD7594). Healthy subjects received inhaled velsecorat (non-radiolabeled; 720 mg) followed by intravenous infusion of carbon 14 (14C)-velsecorat (30 mg). Plasma, urine, and feces were collected up to 168...
article 2022
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Kentrop, J. (author), Savransky, V. (author), Klaassen, S.D. (author), van Groningen, T. (author), Bohnert, S. (author), Cornelissen, A.S. (author), Cochrane, L. (author), Barry, J. (author), Joosen, M.J.A. (author)
Nerve agent exposure is generally treated by an antidote formulation composed of a muscarinic antagonist, atropine sulfate (ATR), and a reactivator of acetylcholinesterase (AChE) such as pralidoxime, obidoxime (OBI), methoxime, trimedoxime or HI-6 and an anticonvulsant. Organophosphates (OPs) irreversibly inhibit AChE, the enzyme responsible for...
article 2021
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Gopaul, V.S. (author), Pieterman, E.J. (author), Princen, H.M.G. (author), Bergenholm, L. (author), Lundborg, E. (author), Cavallin, A. (author), Johansson, M.J. (author), Hawthorne, G. (author), Björkbom, A. (author), Hammarberg, M. (author), Li, X. (author), Jarke, A. (author), Bright, J. (author), Svensson, L. (author), Jansson-Löfmark, R. (author), Abrahamsson, B. (author), Agrawal, R. (author), Hurt-Camejo, E. (author)
We investigated the effects of mineral oil on statin pharmacokinetics and inflammatory markers in animal models. A new synthesis strategy produced regioisomers that facilitated the characterization of the main metabolite (M1) of atorvastatin, a lipophilic statin, in C57BL/6NCrl mice. The chemical structure of M1 in mice was confirmed as ortho...
article 2021
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van Berlo, D. (author), van de Steeg, E. (author), Amirabadi, H.E. (author), Masereeuw, R. (author)
The development of new medicines suffers from attrition, especially in the development pipeline. Eight out of nine drug candidates entering the clinical testing phase fail, mostly due to poor safety and efficacy. The low predictive value of animal models, used in earlier phases of drug development, for effects in humans poses a major problem. In...
article 2021
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Bohnert, S. (author), van den Berg, R.M. (author), Mikler, J. (author), Klaassen, S.D (author), Joosen, M.J.A. (author)
Organophosphorus nerve agents (NA) inhibit acetylcholinesterase (AChE) which results in the over-stimulation of both the central and peripheral nervous systems, creating a toxic syndrome that can be lethal if left untreated (Cannard, 2006). It is standard practice to treat Sarin (GB) intoxication with an oxime, an antimuscarinic such as atropine...
article 2020
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Cornelissen, A.S. (author), van Groningen, T. (author), Bohnert, S. (author), Klaassen, S.D (author), Joosen, M.J.A. (author)
Anticholinergic treatment is key for effective medical treatment of nerve agent exposure. Atropine is included at a 2 mg intramuscular dose in so-called autoinjectors designed for self- and buddy-aid. As patient cohorts are not available, predicting and evaluating the efficacy of medical countermeasures relies on animal models. The use of...
article 2020
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Stevens, L.J. (author), Donkers, J.M. (author), Dubbel, J. (author), Vaes, W.H.J. (author), van de Steeg, E. (author), Knibbe, C.A.J. (author), Alwayn, I.P.J. (author), van de Steeg, E. (author)
To predict the absorption, distribution, metabolism and excretion (ADME) profile of candidate drugs a variety of preclinical models can be applied. The ADME and toxicological behavior of newly developed drugs are often investigated prior to assessment in humans, which is associated with long time-lines and high costs. Therefore, good predictions...
article 2020
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Erpelinck, S. (author), Meijers, T. (author), Ariga, K. (author)
Membrane embedded transporter proteins play an important role in the absorption, distribution and excretion of many drugs. A reliable prediction of human pharmacokinetics of (new) drugs based on PBPK modeling is highly dependent on accurate determination of the absolute protein expression levels of these transmembrane transporter proteins.
other 2017
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Luijten, M. (author), Olthof, E.D. (author), Hakkert, B.C. (author), Rorije, E. (author), van der Laan, J.-W. (author), Woutersen, R.A. (author), van Benthem, J. (author)
Assessment of genotoxic and carcinogenic potential is considered one of the basic requirements when evaluating possible human health risks associated with exposure to chemicals. Test strategies currently in place focus primarily on identifying genotoxic potential due to the strong association between the accumulation of genetic damage and cancer...
article 2016
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Garner, C.R. (author), Park, K.B. (author), French, N.S. (author), Earnshaw, C. (author), Schipani, A. (author), Selby, A.M. (author), Byrne, L. (author), Siner, S. (author), Crawley, F.P. (author), Vaes, W.H.J. (author), van Duijn, E. (author), de ligt, R. (author), Varendi, H. (author), Lass, J. (author), Grynkiewicz, G. (author), Maruszak, W. (author), Turner, M.A. (author)
Aims The aims of the study were to compare [14C]-paracetamol ([14C]-PARA) paediatric pharmacokinetics (PK) after administration mixed in a therapeutic dose or an isolated microdose and to develop further and validate accelerator mass spectrometry (AMS) bioanalysis in the 0-2 year old age group. Methods [14C]-PARA concentrations in 10-15 μl...
article 2015
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Turner, M.A. (author), Mooij, M.G. (author), Vaes, W.H.J. (author), Windhorst, A.D. (author), Hendrikse, N.H. (author), Knibbe, C.A.J. (author), Körgvee, L.T. (author), Maruszak, W. (author), Grynkiewicz, G. (author), Garner, R.C. (author), Tibbocl, D. (author), Park, B.K. (author), de Wildt, S.N. (author)
Important information gaps remain on the efficacy and safety of drugs in children. Pediatric drug development encounters several ethical, practical, and scientifîc chaflenges One barrier to the evaluation of medicines for children is a lack of Innovative methodologies that have been adapted to the needs of chiIdren This article presents our...
article 2015
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van Mierlo, G.J.D. (author), Cnubben, N.H.P. (author), Wouters, D. (author), Wolbink, G.J. (author), Hart, M.H.L. (author), Rispens, T. (author), Ganderup, N.C. (author), Kuper, C.F. (author), Aarden, L. (author), Penninks, A.H. (author)
Immunogenicity is a major issue of concern for monoclonal antibodies used in human diseases and is by default mainly determined in non-human primates (NHP), as target molecules are considered most similar in NHP compared to human. In this manuscript the predictive value of immunogenicity testing in minipigs for human safety is evaluated, as the...
article 2014
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Reus, A.A. (author), Maas, W.J.M. (author), Jansen, H.T. (author), Constant, S. (author), Staal, Y.C.M. (author), van Triel, J.J. (author), Kuper, C.F. (author)
The respiratory route is an important portal for human exposure to a large variety of substances. Consequently, there is an urgent need for realistic in vitro strategies for evaluation of the absorption of airborne substances with regard to safety and efficacy assessment. The present study investigated feasibility of a 3D human airway epithelial...
article 2014
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Bosgra, S. (author), van de Steeg, E. (author), Vlaming, M.L. (author), Verhoeckx, K.C. (author), Huisman, M.T. (author), Verwei, M. (author), Wortelboer, H.M. (author)
In contrast to primary hepatocytes, estimating carrier-mediated hepatic disposition by using a panel of single transfected cell-lines provides direct information on the contribution of the individual transporters to the net disposition. The most direct way to correct for differences in transporter abundance between cell-lines and tissue is by...
article 2014
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Kostewicz, E.S. (author), Abrahamsson, B. (author), Brewster, M. (author), Brouwers, J. (author), Butler, J. (author), Carlert, S. (author), Dickinson, P.A. (author), Dressman, J. (author), Holm, R. (author), Klein, S. (author), Mann, J. (author), McAllister, M. (author), Minekus, M. (author), Muenster, U. (author), Müllertz, A. (author), Verwei, M. (author), Vertzoni, M. (author), Weitschies, W. (author), Augustijns, P. (author)
Accurate prediction of the in vivo biopharmaceutical performance of oral drug formulations is critical to efficient drug development. Traditionally, in vitro evaluation of oral drug formulations has focused on disintegration and dissolution testing for quality control (QC) purposes. The connection with in vivo biopharmaceutical performance has...
article 2014
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Minekus, M. (author), Alminger, M. (author), Alvito, P. (author), Ballance, S. (author), Bohn, T. (author), Bourlieu, C. (author), Carrière, F. (author), Boutrou, R. (author), Corredig, M. (author), Dupont, D. (author), Dufour, C. (author), Egger, L. (author), Golding, M. (author), Karakaya, S. (author), Kirkhus, B. (author), Le Feunteun, S. (author), Lesmes, U. (author), MacIerzanka, A. (author), MacKie, A. (author), Marze, S. (author), McClements, D.J. (author), Ménard, O. (author), Recio, I. (author), Santos, C.N. (author), Singh, R.P. (author), Vegarud, G.E. (author), Wickham, M.S.J. (author), Weitschies, W. (author), Brodkorb, A. (author)
Simulated gastro-intestinal digestion is widely employed in many fields of food and nutritional sciences, as conducting human trials are often costly, resource intensive, and ethically disputable. As a consequence, in vitro alternatives that determine endpoints such as the bioaccessibility of nutrients and non-nutrients or the digestibility of...
article 2014
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Fransman, W. (author), Kager, H. (author), Meijster, T. (author), Heederik, D. (author), Kromhout, H. (author), Portengen, L. (author), Blaauboer, B.J. (author)
Several studies showed that oncology nurses are exposed to antineoplastic drugs via the skin during daily activities. Several antineoplastic drugs (including cyclophosphamide) have been classified as carcinogenic to humans. This study aims to assess the leukemia risk of occupational exposure to cyclophosphamide. Average task frequencies from the...
article 2014
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van Loo-Bouwman, C.A. (author), Naber, T.H.J. (author), Minekus, M. (author), van Breemen, R.B. (author), Hulshof, P.J.M. (author), Schaafsma, G. (author)
Since the food matrix determines β-carotene availability for intestinal absorption, food matrix effects on the bioaccessibility of β-carotene from two diets were investigated in vitro and compared with in vivo data. The "mixed diet" consisted of β-carotene-rich vegetables, and the "oil diet" contained β-carotene-low vegetables with supplemental...
article 2014
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Mooij, M.G. (author), van Duijn, E. (author), Knibbe, C.A.J. (author), Windhorst, A.D. (author), Hendrikse, N.H. (author), Vaes, W.H.J. (author), Spaans, E. (author), Fabriek, B.O. (author), Sandman, H. (author), Grossouw, D. (author), Hanff, L.M. (author), Janssen, P.J.J.M. (author), Koch, B.C.P. (author), Tibboel, D. (author), de Wildt, S.N. (author)
Results: Ten infants (aged 0.1–83.1 months) were included; one was excluded as he vomited shortly after administration. In nine patients, [14C]AAP and metabolites in blood samples were detectable at expected concentrations: median (range) maximum concentration (Cmax) [14C]AAP 1.68 (0.75–4.76) ng/L, [14C]AAP-Glu 0.88 (0.34–1.55) ng/L, and [14C...
article 2014
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Westerhout, J. (author)
In the development of drugs for the treatment of central nervous system (CNS) disorders, the prediction of human CNS drug action is a big challenge. Direct measurement of brain extracellular fluid (brainECF) concentrations is highly restricted in human. Therefore, unbound drug concentrations in human cerebrospinal fluid (CSF) are used as a...
doctoral thesis 2014
Searched for: subject%3A%22Pharmacokinetics%22
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