Academic literature on the topic '(in-vitro intrinsic) clearance'

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Journal articles on the topic "(in-vitro intrinsic) clearance"

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Fang, Ping, Jia-Yang He, Ai-Xia Han, et al. "Effects of CYP2C19 Variants on Fluoxetine Metabolism in vitro." Pharmacology 100, no. 1-2 (2017): 91–97. http://dx.doi.org/10.1159/000475598.

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Aims: CYP2C19 is an important member of the cytochrome P450 enzyme superfamily. We recently identified 31 CYP2C19 alleles in the Han Chinese population. The aim of this study was to assess the catalytic activities of these allelic isoforms and their effects on the metabolism of fluoxetine in vitro. Methods: The wild-type and 30 CYP2C19 variants were expressed in insect cells and each variant was characterized using fluoxetine as the substrate. Reactions were performed at 37°C with 20-1,000 µmol/L substrate for 30 min. By using ultra-high performance liquid chromatography-mass spectrometry to d
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Lan, Tian, Ya-Qing Ma, Ya-Min Dang, et al. "Effects of 31 recombinant CYP2C19 variants on clomipramine metabolism in vitro." Journal of Psychopharmacology 35, no. 12 (2021): 1517–22. http://dx.doi.org/10.1177/02698811211050573.

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Background: CYP2C19 is an important member of the cytochrome P450 enzyme superfamily. We recently identified 31CYP2C19 alleles in the Han Chinese population; studying the effects of CYP2C19 on drug metabolism can help reduce adverse drug reactions and therapeutic failure. Aim: The aim of this study was to assess the catalytic activities of 31 allelic isoforms and their effects on the metabolism of clomipramine in vitro. Methods: The wild-type and 30 CYP2C19 variants were expressed in insect cells, and each variant was characterized using clomipramine as the substrate. Reactions were performed
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Huang, Liyue, Loren Berry, Sindhura Ganga, et al. "Relationship between Passive Permeability, Efflux, and Predictability of Clearance from In Vitro Metabolic Intrinsic Clearance." Drug Metabolism and Disposition 38, no. 2 (2009): 223–31. http://dx.doi.org/10.1124/dmd.109.029066.

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Nagilla, Rakesh, Kelly A. Frank, Larry J. Jolivette, and Keith W. Ward. "Investigation of the utility of published in vitro intrinsic clearance data for prediction of in vivo clearance." Journal of Pharmacological and Toxicological Methods 53, no. 2 (2006): 106–16. http://dx.doi.org/10.1016/j.vascn.2005.08.005.

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KC, Gaurab, and Sujal Deshmukh. "P128 - In vitro to in vivo extrapolation (IVIVE) for low intrinsic clearance compounds." Drug Metabolism and Pharmacokinetics 35, no. 1 (2020): S61. http://dx.doi.org/10.1016/j.dmpk.2020.04.129.

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Yin, Jian, Hongxia Qiu, Jing Dai, et al. "Prediction of hepatic plasma clearance in vivo from gel-entrapped rat and human hepatocytes." Canadian Journal of Physiology and Pharmacology 91, no. 2 (2013): 178–86. http://dx.doi.org/10.1139/cjpp-2012-0334.

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This paper aimed to evaluate the applicability of gel-entrapped rat and human hepatocytes in the prediction of hepatic plasma clearance (CLh,plasma) in vivo. The in vitro intrinsic clearances (CLint,in vitro) for the selected compounds were determined from the substrate disappearance rate, and further used to predict CLh,plasma using 3 classical mathematical models (well-stirred, parallel-tube, and dispersion) and disregarding drug binding. As a result, the predicted values from gel-entrapped rat hepatocytes were mostly within 2 SE of the literature data with a high correlation coefficient (R2
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Llona-Minguez, Sabin, Artin Ghassemian, Pawel Baranczewski, et al. "Structure–metabolism-relationships in the microsomal clearance of piperazin-1-ylpyridazines." MedChemComm 8, no. 7 (2017): 1553–60. http://dx.doi.org/10.1039/c7md00230k.

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In this study, we provide insight into the metabolic profile of a series of piperazin-1-ylpyridazines suffering from rapid in vitro intrinsic clearance in a metabolic stability assay using liver microsomes.
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Porter, Sarah E. G., Richard B. Keithley, and Sarah C. Rutan. "Development of an in vitro incubation procedure for screening of CYP2D6 intrinsic clearance." Journal of Chromatography B 850, no. 1-2 (2007): 74–82. http://dx.doi.org/10.1016/j.jchromb.2006.11.006.

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Fei, Yu-xing, Tian-hong Zhang, Jing Zhao, et al. "In vitro and in vivo evaluation of hypothermia on pharmacokinetics and pharmacodynamics of nimodipine in rabbits." Journal of International Medical Research 46, no. 1 (2017): 335–47. http://dx.doi.org/10.1177/0300060517720056.

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Objective To investigate the effect of hypothermia on the pharmacokinetics and pharmacodynamics of nimodipine in rabbits using in vivo and in vitro methods. Methods Five healthy New Zealand rabbits received a single dose of nimodipine (0.5 mg/kg) intravenously under normothermic and hypothermic conditions. Doppler ultrasound was used to monitor cerebral blood flow, vascular resistance, and heart rate. In vitro evaluations of protein binding, hepatocyte uptake and intrinsic clearance of liver microsomes at different temperatures were also conducted. Results Plasma concentrations of nimodipine w
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Riley, Robert J., D. F. McGinnity, and R. P. Austin. "A UNIFIED MODEL FOR PREDICTING HUMAN HEPATIC, METABOLIC CLEARANCE FROM IN VITRO INTRINSIC CLEARANCE DATA IN HEPATOCYTES AND MICROSOMES." Drug Metabolism and Disposition 33, no. 9 (2005): 1304–11. http://dx.doi.org/10.1124/dmd.105.004259.

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Dissertations / Theses on the topic "(in-vitro intrinsic) clearance"

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Kimble, Benjamin. "Pharmacokinetic aspects of meloxicam in koalas: including its hepatic microsomal metabolism compared with other selected species." Thesis, The University of Sydney, 2015. http://hdl.handle.net/2123/13996.

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Prior to this research, no disposition studies of meloxicam (nor any other non steroidal anti-inflammatory drugs) had been conducted in koalas (a specialist Eucalyptus spp. foliage feeder) despite being readily administered to this species, in the field. Thus, aspects of the in-vivo pharmacokinetic profile of meloxicam in the koala and the in-vitro metabolism of meloxicam in the koala and selected species were investigated. In the first stage of the research, a simple, sensitive and improved method using high performance liquid chromatography equipped with photo diode array detection was deve
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Books on the topic "(in-vitro intrinsic) clearance"

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Test No. 319A: Determination of in vitro intrinsic clearance using cryopreserved rainbow trout hepatocytes (RT-HEP). OECD, 2018. http://dx.doi.org/10.1787/9789264303218-en.

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Test No. 319B: Determination of in vitro intrinsic clearance using rainbow trout liver S9 sub-cellular fraction (RT-S9). OECD, 2018. http://dx.doi.org/10.1787/9789264303232-en.

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Book chapters on the topic "(in-vitro intrinsic) clearance"

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"Kinetics of In Vitro Metabolism: Assimilation of Intrinsic Clearance in Hepatic Clearance." In Pharmacokinetics and Toxicokinetics. CRC Press, 2015. http://dx.doi.org/10.1201/b18133-9.

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Vamsi Krishna, Marothu, Kantamaneni Padmalatha, and Gorrepati Madhavi. "In vitro Metabolic Stability of Drugs and Applications of LC-MS in Metabolite Profiling." In Drug Metabolism. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.99762.

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Metabolic stability of a compound is an important factor to be considered during the early stages of drug discovery. If the compound has poor metabolic stability, it never becomes a drug even though it has promising pharmacological characteristics. For example, a drug is quickly metabolized in the body; it does not have sufficient in vivo exposure levels and leads to the production of toxic, non-active or active metabolites. A drug is slowly metabolized in the body it could remain longer periods in the body and lead to unwanted adverse reactions, toxicity or may cause drug interactions. Metabolic stability assay is performed to understand the susceptibility of the compound to undergo biotransformation in the body. Intrinsic clearance of the compound is measured by metabolic stability assays. Different in vitro test systems including liver microsomes, hepatocytes, S9 fractions, cytosol, recombinant expressed enzymes, and cell lines are used to investigate the metabolic stability of drugs. Metabolite profiling is a vital part of the drug discovery process and LC–MS plays a vital role. The development of high-resolution (HR) MS technologies with improved mass accuracy, in conjunction with novel data processing techniques, has significantly improved the metabolite detection and identification process. HR-MS based data acquisition (ion intensity-dependent acquisition, accurate-mass inclusion list-dependent acquisition, isotope pattern-dependent acquisition, pseudo neutral loss-dependent acquisition, and mass defect-dependent acquisition) and data mining techniques (extracted ion chromatogram, product ion filter, mass defect filter, isotope pattern filter, neutral loss filter, background subtraction, and control sample comparison) facilitate the drug metabolite identification process.
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Conference papers on the topic "(in-vitro intrinsic) clearance"

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Bussel, J. "FOR MODULATION AS A MEANS OF ELEVATING THE PLATELET COUNT IN ITP." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644761.

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ITP is an autoantibody-mediated disease which would logically be treated by decreasing the level of autoantibody. However, the most exciting developments in understanding the pathophysiology of the thrombocytopenia and its treatment involve a better understanding of the MPS FcR system and ways in which it can be modulated. This work has focussed on phagocytic paralysis or FcR blockade (FcRBl): the slowing of destruction of antibody-coated platelets despite the persistent presence of antibody on the surface of the platelet.Several areas have been explored in learning about the MPS system. Inves
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