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https://www.readbyqxmd.com/read/28717107/human-plasma-and-urinary-metabolic-profiles-of-trimethylamine-and-trimethylamine-n-oxide-extrapolated-using-a-simple-physiologically-based-pharmacokinetic-model
#1
Makiko Shimizu, Hiroshi Yamazaki
Trimethylamine, a dietary- and medicinal carnitine-derived amine, is extensively metabolized by liver to non-malodorous trimethylamine N-oxide. Although trimethylamine and trimethylamine N-oxide under daily dietary consumption or carnitine treatment are generally regarded as nontoxic, they have been, and remain, of toxicological and clinical interest because of their potential association with atherosclerosis. The aim of the current study was to model the pharmacokinetics of trimethylamine after oral administration of trimethylamine in humans and compare the results with reported measured values...
2017: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/28716828/creation-and-preliminary-characterization-of-pregnane-x-receptor-and-constitutive-androstane-receptor-knockout-rats
#2
Kevin P Forbes, Evguenia Kouranova, Daniel Tinker, Karen Janowski, Doug Cortner, Aaron McCoy, Xiaoxia Cui
The nuclear receptors pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are closely related transcription factors that regulate the expression of Phase I (Cytochrome P450s), Phase II metabolizing enzymes and transporter genes in response to stimulation from xenobiotics, including prescription drugs. PXR and CAR are also involved in other endogenous processes, such as in inflammation, glucose homeostasis and lipid metabolism, and are thus potential drug targets themselves. PXR and CAR knockout and humanized mouse models have proven useful...
July 17, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28716728/cytochrome-p450-3a-selectively-affects-the-pharmacokinetic-interaction-between-erlotinib-and-docetaxel-in-rats
#3
Xuan Qin, Jian Lu, Peili Wang, Peipei Xu, Mingyao Liu, Xin Wang
Erlotinib as a first-line drug is used in non-small cell lung cancer (NSCLC) patients with sensitive EGFR mutations, while resistance to this drug will occur after several years of treatment. Therefore, the microtubule disturber docetaxel is introduced as combined regimen in clinical trials. This report investigated the potentials and mechanisms of drug-drug interaction (DDI) between erlotinib and docetaxel using wild type (WT) and Cyp3a1/2 knockout (KO) rats. The erlotinib O-demethylation and docetaxel hydroxylation reactions in the absence or the presence of another drug were analyzed in vitro via the assay of rat liver microsomes...
July 14, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28715789/quantification-of-idp-73152-a-novel-antibiotic-in-plasma-from-mice-rats-and-humans-using-an-ultra-high-performance-liquid-chromatography-tandem-mass-spectrometry-method-for-use-in-pharmacokinetic-studies
#4
Myongjae Lee, Dohee Kim, Jeongcheol Shin, Hee-Yeol Lee, Soobong Park, Hong-Sub Lee, Jae-Hoon Kang, Suk-Jae Chung
IDP-73152, a novel inhibitor of a bacterial peptide deformylase, was recently approved as a new, investigational drug in Korea for the clinical management of infections caused by Gram positive bacteria. The objective of this study was to develop/validate a simple and robust analytical method for the determination of IDP-73152 in plasma samples from rodents and humans, and to assess the feasibility of the assay for use in pharmacokinetic studies using animal models. Plasma samples were processed using a standard method for protein precipitation and an aliquot of the extract then injected onto an UHPLC-MS/MS system...
July 6, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28714122/a-fast-and-accurate-method-for-the-pharmacokinetic-research-of-four-coumarin-analogs-in-fructus-cnidii-using-capillary-electro-chromatography-with-a-methacrylate-ester-based-monolithic-column
#5
Zhao Chen, Aili Xu, Xiaoli Bi, Wenhui Luo, Ji Li, Guorong Fan, Dongmei Sun
In the present study, a monolithic capillary column with higher permeability was developed for the in-vivo discrimination of four coumarin analogs (bergapten, 2'-acetylangelicin, imperatorin and osthole) that typically require long separation times in HPLC. Instead of conventional methacrylate ester monolith (containing 19.5% porogen) with insufficient permeability (K = 1.52-1.66 × 10(-14) M(2) ) for plasma sample, the proposed column (20.5% porogen) had better permeability (around 3.80 × 10(-14) M(2) ) while properties such as pore distribution, stability and resolution changed slightly...
July 17, 2017: Electrophoresis
https://www.readbyqxmd.com/read/28707762/pharmacokinetics-and-tissue-distribution-study-of-clevidipine-and-its-primary-metabolite-h152-81-in-rats
#6
Yan Wang, Lanting Zhao, Tengfei Li, Wen Yang, Qian Li, Luning Sun, Li Ding
This present study was designed to investigate the pharmacokinetic profiles and tissue distribution characteristics of clevidipine and its primary metabolite H152/81 in rats following a single intravenous administration of clevidipine butyrate injectable emulsion (CBIE). For this study, a sensitive and selective liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was established and validated for the simultaneous quantitation of clevidipine and H152/81 in rat whole blood and various tissues. A Hedera ODS-2 column with two gradient elution programs was employed for the troubleshooting of matrix effect on the detection of analytes among different biological samples...
July 14, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28706557/comparative-pharmacokinetics-and-bioavailability-of-three-ephedrines-in-rat-after-oral-administration-of-unprocessed-and-honey-fried-ephedra-extract-by-response-surface-experimental-design
#7
Yezhe Cheng, Yu Zhang, Hang Xing, Kun Qian, Longshan Zhao, Xiaohui Chen
Ephedra have been used as a common traditional Chinese medicine for thousands of years. However, the perspiration effect of the unprocessed ephedra was too strong. Clinical trials have shown that processing methods play a critical role in moderating the perspiration property of ephedra according to the needs. A LC-MS/MS method was developed and validated to compare the pharmacokinetic properties of the three ephedrines after oral administration of unprocessed and honey-fried ephedra extract. The contents of honey, frying temperature, and frying time were set at 20%, 116°C, and 7 min by the Box-Behnken response surface method, respectively...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28705918/in-vivo-quantification-of-er-%C3%AE-expression-by-pharmacokinetic-modeling-studies-with-18-f-fhnp-pet
#8
Inês F Antunes, Antoon T M Willemsen, Jurgen W A Sijbesma, Ate S Boerema, Aren van Waarde, Andor W J M Glaudemans, Rudi A Dierckx, Elisabeth G E de Vries, Geke A P Hospers, Erik F de Vries
The estrogen receptor (ER) is a target for endocrine therapy in breast cancer patients. Individual quantification of ERα and ERβ expression, rather than total ER levels, might enable better prediction of the response to treatment. We recently developed the tracer 2-(18)F-fluoro-6-(6-hydroxynaphthalen-2-yl)pyridin-3-ol ((18)F-FHNP) for assessment of ERβ levels with positron emission tomography (PET). Here we investigated several pharmacokinetic analysis methods to quantify changes in ERβ availability with (18)F-FHNP-PET...
July 13, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28705021/atorvastatin-loaded-micelles-with-bone-targeted-ligand-for-the-treatment-of-osteoporosis
#9
Yonghui Xie, Xueying Tan, Jian Huang, Hongwei Huang, Ping Zou, Jingbo Hu
Osteoporosis is a common bone disorder where the declined bone mass is far more than normal physiological status and usually associated with enhanced fracture risk, reduced bone strength and even deteriorated quality of life. Recent studies showed that statins could exert beneficial effects on bones via promoting osteoblastic activity mediated by increased expression of bone morphogenetic protein 2 and also by suppressing osteoclast proliferation. In this study, we developed atorvastatin-loaded tetracycline-poly (ethylene glycol)-poly(lactic-co-glycolic acid) (TC-PEG-PLGA/ATO) micelles for the targeted treatment of osteoporosis...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28704725/simultaneous-estimation-of-lisofylline-and-pentoxifylline-in-rat-plasma-by-high-performance-liquid-chromatography-photodiode-array-detector-and-its-application-to-pharmacokinetics-in-rat
#10
Kishan S Italiya, Saurabh Sharma, Ishit Kothari, Deepak Chitkara, Anupama Mittal
Lisofylline (LSF) is an anti-inflammatory and immunomodulatory agent with proven activity in serious infections associated with cancer chemotherapy, hyperoxia-induced acute lung injury, autoimmune disorders including type-1 diabetes (T1DM) and islet rejection after islet transplantation. It is also an active metabolite of another anti-inflammatory agent, Pentoxifylline (PTX). LSF bears immense therapeutic potential in multiple pharmacological activities and hence appropriate and accurate quantification of LSF is very important...
June 29, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28698254/mechanism-based-pharmacokinetic-pharmacodynamic-modeling-of-the-glucagon-like-peptide-1-receptor-agonist-exenatide-to-characterize-its-anti-obesity-effects-in-diet-induced-obese-mice
#11
Shinji Iwasaki, Teruki Hamada, Ikumi Chisaki, Tomohiro Andou, Noriyasu Sano, Atsutoshi Furuta, Nobuyuki Amano
Glucagon-like peptide-1 (GLP-1) analogs lower body weight in humans in addition to their potent anti-diabetic effects. Hence, agonistic targeting of the GLP-1 receptor could be a valid approach to target obesity. However, quantitative analyses of the pharmacokinetic/pharmacodynamic (PK/PD) relationship between GLP-1 analogs and their anti-obesity effect have not been reported in either animals or humans. Therefore, the present study was performed to establish a mechanism-based PK/PD model of GLP-1 receptor agonists using the GLP-1 analog, exenatide, for the development of promising new anti-obesity drugs...
July 11, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28697305/optimizing-multi-step-delivery-of-pegylated-trail-toxin-conjugates-for-improved-antitumor-activities
#12
Xiaoyue Wei, Xiaoyue Yang, Wenbin Zhao, Yingchun Xu, Liqiang Pan, Shu Qing Chen
Although TRAIL (tumor-necrosis-factor (TNF)-related apoptosis-inducing ligand) has been considered as a promising broad-spectrum anti-tumor agent, its further application was limited by poor drug delivery and TRAIL-resistant tumors. A three-step drug delivery strategy was applied to TRAIL for solving the above two obstacles in the form of PEG-TRAIL-MMAE (Monomethyl Auristatin E). PEGylation of TRAIL in first step was to improve its in vivo pharmacokinetics, while the interaction between TRAIL conjugates with death receptors in second step was to activate TRAIL extrinsic apoptosis pathway, and the further release of MMAE from lysosome was the third step for introducing another apoptosis pathway to overcome TRAIL resistance in some tumors...
July 11, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28696229/mdr1-and-bcrp-transporter-mediated-drug-drug-interaction-between-rilpivirine-and-abacavir-effect-on-intestinal-absorption
#13
Josef Reznicek, Martina Ceckova, Zuzana Ptackova, Ondrej Martinec, Lenka Tupova, Lukas Cerveny, Frantisek Staud
Rilpivirine (TMC278) is a highly potent second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) representing an effective component of combination antiretroviral therapy (cART) in the treatment of HIV-positive patients. Many antiretroviral drugs commonly used in cART are substrates of ATP-binding cassette (ABC) and/or solute carrier (SLC) drug transporters and, therefore, prone to pharmacokinetic drug-drug interactions (DDIs). The aim of our study was to evaluate rilpivirine interactions with abacavir and lamivudine on selected ABC and SLC transporters in vitro and assess its importance for pharmacokinetics in vivoUsing accumulation assays in MDCK cells overexpressing selected ABC or SLC drug transporters we revealed rilpivirine as a potent inhibitor of MDR1 and BCRP, but not MRP2, OCT1, OCT2 or MATE1...
July 10, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28696058/early-postnatal-gentamicin-and-ceftazidime-treatment-in-normal-and-food-restricted-neonatal-wistar-rats-implications-for-kidney-development
#14
Ruud R G Bueters, Annelies Jeronimus-Klaasen, Roger J M Brüggemann, Lambertus P van den Heuvel, Michiel F Schreuder
BACKGROUND: Up to two-thirds of premature born neonates are treated for infections with aminoglycosides such as gentamicin. Although acute toxicities are well described, there is uncertainty on developmental changes after treatment of premature born neonates. We studied the effect of gentamicin and ceftazidime on kidney development in the rat. Additionally, we evaluated the modulating effect of extrauterine growth restriction. METHODS: On postnatal day (PND) 2, Wistar rats were cross-fostered into normal sized litters (12 pups) or large litters (20 pups) to create normal food (NF) or food restricted (FR) litters to simulate growth restriction and dosed daily intraperitoneally with placebo, 4 mg/kg of gentamicin or 50 mg/kg ceftazidime until PND 8...
July 11, 2017: Birth defects research
https://www.readbyqxmd.com/read/28689253/effect-of-arteether-and-pyrimethamine-coadministration-on-the-pharmacokinetic-and-pharmacodynamic-profile-of-ormeloxifene
#15
Abhisheak Sharma, Swati Jaiswal, Mahendra Shukla, Jawahar Lal
The study was intended to investigate the effect of concomitant administration of antimalarial drug (pyrimethamine or arteether) on pharmacokinetic and post coitus contraceptive efficacy of ormeloxifene in female Sprague-Dawley rats. A serial sampling technique coupled with LC-MS/MS detection was utilized for quantification of ormeloxifene in plasma samples collected from female rats treated with ormeloxifene only and ormeloxifene with pyrimethamine or arteether. Coitus-proven female rats were utilized to investigate the effect of pyrimethamine or arteether coadministration on contraceptive efficacy of ormeloxifene by investigating the presence or absence of implantations and status of corpora lutea on day 10 post coitum...
July 8, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28688270/simultaneous-quantitative-analysis-of-polyethylene-glycol-peg-pegylated-paclitaxel-and-paclitaxel-in-rats-by-ms-ms-all-technique-with-hybrid-quadrupole-time-of-flight-mass-spectrometry
#16
Heping Sun, Qi Zhang, Zhi Zhang, Jin Tong, Dafeng Chu, Jingkai Gu
PEGylation is practically one of most important modifications of drugs including small molecules, peptides and proteins, which has been proven to dramatically improve physicochemical properties and pharmacokinetic behavior of the PEGylated drugs. However, it is a challenge currently to quantitatively analyze PEG and PEGylated drugs by various analytical methods, even mass spectrometry because of multiple parent ion distribution of PEG caused by its polydispersity of molecular weight. Here we developed a robust method with MS/MS(ALL) technique using electrospray ionization (ESI) source coupled high resolution Quadrupole Time-of-Flight (Q-TOF) mass spectrometry for the quantification of PEG2K-Paclitaxel (PEG-PTX) and its two metabolites, PEG and Paclitaxel (PTX)...
June 23, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28687198/neu-p11-a-novel-mt1-mt2-agonist-reverses-diabetes-by-suppressing-the-hypothalamic-pituitary-adrenal-axis-in-rats
#17
Jun Zhou, Jin Zhang, XiaoHong Luo, MaoXing Li, Ying Yue, Moshe Laudon, ZhengPing Jia, RuXue Zhang
Excessive glucocorticoid (GC) in type 2 diabetes mellitus (T2DM) reduces insulin sensitivity, impairs β-cell function, increases gluconeogenesis and glycogenolysis, impairs glucose uptake and metabolism, and reduces the insulinotropic effects of glucagon-like peptide 1. Melatonin, which serves as a physiological regulator of the hypothalamic-pituitary-adrenal (HPA) axis, has been suggested to have anti-diabetic effects. The objective of the present study was to investigate the effect of the MT1/MT2 melatonin agonist Neu-P11 on glucose and lipid metabolism in T2DM rats induced by a high fat diet combined with low doses of streptozotocin...
July 4, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28685967/rapid-solid-phase-extraction-coupled-with-gc-ms-method-for-the-determination-of-venlafaxine-in-rat-plasma-application-to-the-drug-drug-pharmacokinetic-interaction-study-of-venlafaxine-combined-with-fluoxetine
#18
Lin Song, Zhen Zheng, Chen Liang, Xiujuan Chen, Runsheng Zhang, Zhanying Hong, Yifeng Chai
A rapid and sensitive gas chromatography with mass spectrometry method for the determination of venlafaxine in rat plasma has been developed and applied to a drug-drug interaction study of fluoxetine on pharmacokinetics of venlafaxine in rats. Rat plasma was spiked with 2% aqueous ammonia before subjected to preactivated C18 solid-phase extraction columns and eluted with methanol. No endogenous interferences were observed under optimal condition. The calibration curve was linear (R(2)  = 0.9994) in the range of 10-1000 ng/mL...
July 7, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28684121/discovery-of-a-biarylamide-series-of-potent-state-dependent-nav1-7-inhibitors
#19
Laurie B Schenkel, Erin F DiMauro, Hanh N Nguyen, Nagasree Chakka, Bingfan Du, Robert S Foti, Angel Guzman-Perez, Michael Jarosh, Daniel S La, Joseph Ligutti, Benjamin C Milgram, Bryan D Moyer, Emily A Peterson, John Roberts, Violeta L Yu, Matthew M Weiss
The NaV1.7 ion channel has garnered considerable attention as a target for the treatment of pain. Herein we detail the discovery and structure-activity relationships of a novel series of biaryl amides. Optimization led to the identification of several state-dependent, potent and metabolically stable inhibitors which demonstrated promising levels of selectivity over NaV1.5 and good rat pharmacokinetics. Compound 18, which demonstrated preferential inhibition of a slow inactivated state of NaV1.7, was advanced into a rat formalin study where upon reaching unbound drug levels several fold over the rat NaV1...
June 26, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28683649/in-vitro-and-in-vivo-delivery-of-artemisinin-loaded-pcl-peg-pcl-micelles-and-its-pharmacokinetic-study
#20
Hamidreza Kheiri Manjili, Hojjat Malvandi, Mir Sajjad Mousavi, Elahe Attari, Hossein Danafar
Artemisinin (ART) is a natural anti-malarial sesquiterpene lactone with anticancer properties, but its application is limited because of its low water solubility. To increase the bioavailability and water solubility of ART, we synthesized three series of poly (ɛ-caprolactone)-poly (ethylene glycol)-poly (ɛ-caprolactone) (PCL-PEG-PCL) tri-block copolymers. The structure of the copolymers was characterized by HNMR, FTIR, DSC and GPC techniques. ART was encapsulated inside micelles by a nanoprecipitation method which leading to the formation of ART/PCL-PEG-PCL micelles...
July 7, 2017: Artificial Cells, Nanomedicine, and Biotechnology
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