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pharmacokinetics, rat

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https://www.readbyqxmd.com/read/27914534/novel-revelation-of-warfarin-resistant-mechanism-in-roof-rats-rattus-rattus-using-pharmacokinetic-pharmacodynamic-analysis
#1
Kazuki Takeda, Yoshinori Ikenaka, Tsutomu Tanikawa, Kazuyuki D Tanaka, Shouta M M Nakayama, Hazuki Mizukawa, Mayumi Ishizuka
Roof rats (Rattus rattus) live mainly in human habitats. Heavy use of rodenticides, such as warfarin, has led to the development of drug resistance, making pest control difficult. There have been many reports regarding mutations of vitamin K epoxide reductase (VKOR), the target enzyme of warfarin, in resistant rats. However, it has been suggested there are other mechanisms of warfarin resistance. To confirm these possibilities, closed colonies of warfarin-susceptible roof rats (S) and resistant rats from Tokyo (R) were established, and the pharmacokinetics/pharmacodynamics of warfarin in rats from both colonies was investigated...
November 2016: Pesticide Biochemistry and Physiology
https://www.readbyqxmd.com/read/27913821/theobromine-upregulates-osteogenesis-by-human-mesenchymal-stem-cells-in-vitro-and-accelerates-bone-development-in-rats
#2
Bret H Clough, Joni Ylostalo, Elizabeth Browder, Eoin P McNeill, Thomas J Bartosh, H Ralph Rawls, Tetsuo Nakamoto, Carl A Gregory
Theobromine (THB) is one of the major xanthine-like alkaloids found in cacao plant and a variety of other foodstuffs such as tea leaves, guarana and cola nuts. Historically, THB and its derivatives have been utilized to treat cardiac and circulatory disorders, drug-induced nephrotoxicity, proteinuria and as an immune-modulator. Our previous work demonstrated that THB has the capacity to improve the formation of hydroxyl-apatite during tooth development, suggesting that it may also enhance skeletal development...
December 2, 2016: Calcified Tissue International
https://www.readbyqxmd.com/read/27913584/nitro-fatty-acid-pharmacokinetics-in-the-adipose-tissue-compartment
#3
Marco Fazzari, Nicholas K H Khoo, Steven R Woodcock, Diane K Jorkasky, Lihua Li, Francisco J Schopfer, Bruce A Freeman
Electrophilic nitro-fatty acids (NO2-FAs) promote adaptive and anti-inflammatory cell signaling responses as a result of an electrophilic character that supports post-translational protein modifications. A unique pharmacokinetic profile is expected for NO2-FAs because of an ability to undergo reversible reactions including Michael additions with biological cysteine-containing proteins and esterification into complex lipids. Herein we report via quantitative whole-body autoradiography analysis of rats gavaged with radiolabeled 10-nitro-[14C]oleic acid, preferential accumulation in adipose tissue over two weeks...
December 2, 2016: Journal of Lipid Research
https://www.readbyqxmd.com/read/27910712/development-of-a-nanogel-formulation-for-transdermal-delivery-of-tenoxicam-a-pharmacokinetic-pharmacodynamic-modeling-approach-for-quantitative-prediction-of-skin-absorption
#4
Mohammed H Elkomy, Shahira F El Menshawe, Hussein M Eid, Ahmed M A Ali
This study investigates potentials of solid lipid nanoparticles (SLN) based gel for transdermal delivery of tenoxicam (TNX) and describes a pharmacokinetics-pharmacodynamics (PK-PD) modeling approach for predicting concentration-time profile in skin. A 2(3) factorial design was adopted to study the effect of formulation factors on SLN properties and determine the optimal formulation. SLN-gel tolerability was investigated using rabbit skin irritation test. Its anti-inflammatory activity was assessed by carrageenan induced rat paw edema test...
December 2, 2016: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/27909986/toxicity-and-pharmacokinetic-profile-for-single-dose-injection-of-aby-029-a-fluorescent-anti-egfr-synthetic-affibody-molecule-for-human-use
#5
Kimberley S Samkoe, Jason R Gunn, Kayla Marra, Sally M Hull, Karen L Moodie, Joachim Feldwisch, Theresa V Strong, Daniel R Draney, P Jack Hoopes, David W Roberts, Keith Paulsen, Brian W Pogue
PURPOSE: ABY-029, a synthetic Affibody peptide, Z03115-Cys, labeled with a near-infrared fluorophore, IRDye® 800CW, targeting epidermal growth factor receptor (EGFR) has been produced under good manufacturing practices for a US Food and Drug Administration-approved first-in-use human study during surgical resection of glioma, as well as other tumors. Here, the pharmacology, phototoxicity, receptor activity, and biodistribution studies of ABY-029 were completed in rats, prior to the intended human use...
December 1, 2016: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/27907870/immunochromatographic-determination-of-bacopaside-i-in-biological-samples
#6
Sontaya Sookying, Dumrongsak Pekthong, Sarawut Oo-Puthinan, Watoo Phrompittayarat, Waraporn Putalun, Hiroyuki Tanaka, Jie Xing, Zhaoqi Zhan, Nantaka Khorana, Nitra Nuengchamnong, Kornkanok Ingkaninan
We describe a novel immunochromatographic method for qualitative and quantitative analyses of bacopaside I, a bioactive constituent in Bacopa monnieri (L.) Wettst in biological samples. The assay was performed on polyethersulfone membrane using a polyclonal antibody raised against bacopaside I. The finalised method could quantitatively determine bacopaside I in the range of 31.3-1000.0ng and the detection and quantification limits were 1.0 and 31.3ng, respectively. The percentage recoveries of bacopaside I in blood and urine were nearly 100% indicating the accuracy of the extraction...
November 23, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/27906418/assessment-of-celecoxib-poly-lactic-co-glycolic-acid-nanoformulation-on-drug-pharmacodynamics-and-pharmacokinetics-in-rats
#7
S Harirforoosh, K O West, D E Murrell, J W Denham, P C Panus, G A Hanley
OBJECTIVE:  Celecoxib (CEL) is a nonsteroidal anti-inflammatory drug (NSAID) showing selective cycloxygenase-2 inhibition. While effective as a pain reducer, CEL exerts some negative influence on renal and gastrointestinal parameters. This study examined CEL pharmacodynamics and pharmacokinetics following drug reformulation as a poly(lactic-co-glycolic) acid nanoparticle (NP). MATERIALS AND METHODS: Rats were administered either vehicle (VEH) (methylcellulose solution), blank NP, 40 mg/kg CEL in methylcellulose, or an equivalent NP dose (CEL-NP)...
November 2016: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/27903551/analysis-of-lycobetaine-in-rat-plasma-by-lc-esi-ms-ms
#8
Tijia Chen, Wenhao Li, Ting Gong, Yao Fu, Rui Ding, Tao Gong, Zhirong Zhang
In this study, a selective and sensitive liquid chromatography-electrospray ionization-tandem mass spectrometric method was developed and validated for the determination of lycobetaine in rat plasma. Berberine was selected as the internal standard, and rat plasma samples were pretreated via protein precipitation and further separated on a diamonsil octadecyl-silylated silica column using 0.2% (v/v) aqueous formic acid and methanol as the mobile phase. Selected reaction monitoring was performed using the transitions m/z 266...
November 29, 2016: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/27899320/preparation-characterization-and-in-vivo-pharmacokinetic-study-of-pvp-modified-oleanolic-acid-liposomes
#9
Yan Liu, Xiao Luo, Xiaochao Xu, Nannan Gao, Xiaohong Liu
The primary purpose of the present study was to design and optimize a liposomal formulation of the poorly water-soluble drug oleanolic acid (OA) to improve its oral bioavailability, and prolong the duration of therapeutic drug level. Liposomes containing a soybean lecithin and cholesterol lipid bilayer, a protective hydrophilic polyvinylpyrrolidone-K30 (PVP-K30) coating, and a protective bile salt, sodium deoxycholate, were prepared by a thin-film dispersion method coupled with sonication. Several properties of the PVP-modified OA liposomes (PVPOALs), including surface morphology, particle size, zeta potential and entrapment efficiency were extensively characterized...
November 27, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27896627/n-11-c-methyl-amd3465-pet-as-a-tool-for-in-vivo-measurement-of-chemokine-receptor-4-cxcr4-occupancy-by-therapeutic-drugs
#10
S V Hartimath, M A Khayum, A van Waarde, R A J O Dierckx, E F J de Vries
PURPOSE: Chemokine receptor 4 (CXCR4) is overexpressed in many cancers and a potential drug target. We have recently developed the tracer N-[(11)C]methyl-AMD3465 for imaging of CXCR4 expression by positron emission tomography (PET). We investigated the pharmacokinetics of N-[(11)C]methyl-AMD3465 in rats bearing a C6 tumor and assessed whether the CXCR4 occupancy by the drug Plerixafor® can be measured with this PET tracer. PROCEDURE: A subcutaneous C6 tumor was grown in Wistar rats...
November 28, 2016: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/27895517/influence-of-curcumin-on-the-pharmacodynamics-and-pharmacokinetics-of-gliclazide-in-animal-models
#11
Leela Krishna Vatsavai, Eswar Kumar Kilari
PURPOSE: Patients suffering from obesity-related diseases use multiple prescription drugs to control their condition, and it is therefore essential to determine the safety and efficacy of any combination. Gliclazide is one of the most commonly used drug of choice for treatment of type 2 diabetes, and curcumin is a widely used herbal supplement to counter obesity condition. The objective of this study was to investigate the effect of oral administration of curcumin on pharmacodynamics and pharmacokinetics of gliclazide in rats and rabbits to further evaluate the safety and effectiveness of this combination...
2016: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/27895468/increased-localized-delivery-of-piroxicam-by-cationic-nanoparticles-after-intra-articular-injection
#12
Sung Rae Kim, Myoung Jin Ho, Sang Hyun Kim, Ha Ra Cho, Han Sol Kim, Yong Seok Choi, Young Wook Choi, Myung Joo Kang
Piroxicam (PRX), a potent nonsteroidal anti-inflammatory drug, is prescribed to relieve postoperative and/or chronic joint pain. However, its oral administration often results in serious gastrointestinal adverse effects including duodenal ulceration. Thus, a novel cationic nanoparticle (NP) was explored to minimize the systemic exposure and increase the retention time of PRX in the joint after intra-articular (IA) injection, by forming micrometer-sized electrostatic clusters with endogenous hyaluronic acid (HA) in the synovial cavity...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895462/effects-of-resveratrol-on-p-glycoprotein-and-cytochrome-p450-3a-in-vitro-and-on-pharmacokinetics-of-oral-saquinavir-in-rats
#13
Jiapeng Li, Yang Liu, Jingru Zhang, Xiaotong Yu, Xiaoling Wang, Libo Zhao
BACKGROUND: The intestinal cytochrome P450 3A (CYP 3A) and P-glycoprotein (P-gp) present a barrier to the oral absorption of saquinavir (SQV). Resveratrol (RESV) has been indicated to have modulatory effects on P-gp and CYP 3A. Therefore, this study was to investigate the effects of RESV on P-gp and CYP 3A activities in vitro and in vivo on oral SQV pharmacokinetics in rats. METHODS: In vitro, intestinal microsomes were used to evaluate RESV effect on CYP 3A-mediated metabolism of SQV; MDR1-expressing Madin-Darby canine kidney (MDCKII-MDR1) cells were employed to assess the impact of RESV on P-gp-mediated efflux of SQV...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895112/hepatic-dipeptidyl-peptidase-4-controls-pharmacokinetics-of-vildagliptin-in-vivo
#14
Mitsutoshi Asakura, Tatsuki Fukami, Miki Nakajima, Hideaki Fujii, Koichiro Atsuda, Tomoo Itoh, Ryoichi Fujiwara
The major metabolic pathway of vildagliptin, which is an inhibitor of dipeptidyl peptidase-4 (DPP-4), in humans is hydrolysis at the cyano group to produce a carboxylic acid metabolite M20.7. Our in vitro study previously demonstrated that DPP-4 itself greatly contributed to the hydrolysis of vildagliptin in mouse, rat, and human livers. To investigate whether hepatic DPP-4 contributes to the hydrolysis of vildagliptin in vivo, in the present study, we conducted in vivo pharmacokinetics studies of vildagliptin in mice co-administered with vildagliptin and sitagliptin, which is another DPP-4 inhibitor, and also in streptozotocin (STZ)-induced diabetic mice...
November 28, 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27894874/mark-inhibitors-declaring-a-no-go-decision-on-a-chemical-series-based-on-extensive-dmpk-experimentation
#15
Andrew M Haidle, Kaleen K Childers, Anna A Zabierek, Jason D Katz, James P Jewell, Yongquan Hou, Michael D Altman, Alexander Szewczak, Dapeng Chen, Andreas Harsch, Mansuo Hayashi, Lee Warren, Michael Hutton, Hugh Nuthall, Matt G Stanton, Ian W Davies, Ben Munoz, Alan Northrup
Attempts to optimize pharmacokinetic properties in a promising series of pyrrolopyrimidinone MARK inhibitors for the treatment of Alzheimer's disease are described. A focus on physical properties and ligand efficiency while prosecuting this series afforded key tool compounds that revealed a large discrepancy in the rat in vitro-in vivo DMPK (Drug Metabolism/Pharmacokinetics) correlation. These differences prompted an in vivo rat disposition study employing a radiolabeled representative of the series, and the results from this experiment justified the termination of any further optimization efforts...
August 25, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27894245/recent-advances-in-understanding-of-kinetic-interplay-between-phase-ii-metabolism-and-efflux-transport
#16
Shuai Wang, Huijie Xing, Mengjing Zhao, Danyi Lu, Zhijie Li, Dong Dong, Baojian Wu
Mechanistic understanding of the metabolism-transport interplay assumes great importance in pharmaceutical fields because the knowledge can help to interpret drug/xenobiotic metabolism and disposition studies as well as the drug-drug interactions in vivo. About 10 years ago, it started to recognize that cellular phase II metabolism is strongly influenced by the excretion (efflux transport) of generated metabolites, a kinetic phenomenon termed "phase II metabolism-transport interplay". This interplay is believed to have significant effects on the pharmacokinetics (bioavailability) of drugs/chemicals undergoing phase II metabolism...
November 28, 2016: Current Drug Metabolism
https://www.readbyqxmd.com/read/27892765/comparison-of-predictability-for-human-pharmacokinetics-parameters-among-monkeys-rats-and-chimeric-mice-with-humanised-liver
#17
Maki Miyamoto, Shinji Iwasaki, Ikumi Chisaki, Sayaka Nakagawa, Nobuyuki Amano, Hideki Hirabayashi
The aim of the present study was to evaluate the usefulness of chimeric mice with humanised liver (PXB mice) for the prediction of clearance (CLt) and volume of distribution at steady state (Vdss), in comparison with monkeys, which have been reported as a reliable model for human pharmacokinetics (PK) prediction, and with rats, as a conventional PK model. CLt and Vdss values in PXB mice, monkeys, and rats were determined following intravenous administration of 30 compounds known to be mainly eliminated in humans via the hepatic metabolism by various drug-metabolising enzymes...
November 28, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27891611/pharmacokinetics-cannot-explain-the-increased-effective-dose-requirement-for-morphine-and-midazolam-in-rats-during-their-extended-administration-alone-or-in-combination
#18
Stefan J Schaller, Saad M Alam, Jianren Mao, Yanli Zhao, Manfred Blobner, David J Greenblatt, J A Jeevendra Martyn
OBJECTIVES: Chronic administration of morphine and midazolam, alone or in combination, can induce tolerance to their effects. Data showed that co-administration of morphine and midazolam increased effective dose requirement of morphine, exceeding that observed with morphine alone. METHODS: To elucidate the pharmacokinetic component to the tolerance, we administered midazolam (2 mg/kg) and morphine (10 mg/kg) alone or their combination daily to rats for 12 days followed by a pharmacokinetic study on day 13...
November 28, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27890817/sec-butylpropylacetamide-spd-a-new-amide-derivative-of-valproic-acid-for-the-treatment-of-neuropathic-and-inflammatory-pain
#19
Dan Kaufmann, Peter J West, Misty D Smith, Boris Yagen, Meir Bialer, Marshall Devor, H Steve White, K C Brennan
Chronic pain is a multifactorial disease comprised of both inflammatory and neuropathic components that affect ∼20% of the world's population. sec-Butylpropylacetamide (SPD) is a novel amide analogue of valproic acid (VPA) previously shown to possess a broad spectrum of anticonvulsant activity. In this study we defined the pharmacokinetic parameters of SPD in rat and mouse, and then evaluated its antinociceptive potential in neuropathic and acute inflammatory pain models. In the sciatic nerve ligation (SNL) model of neuropathic pain, SPD was equipotent to gabapentin and more potent than its parent compound VPA...
November 24, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27889876/population-pharmacokinetic-pharmacodynamic-modeling-of-5-fluorouracil-for-toxicities-in-rats
#20
Shinji Kobuchi, Yukako Ito, Toshiyuki Sakaeda
BACKGROUND AND OBJECTIVES: Myelosuppression is a dose-limiting toxicity of 5-fluorouracil (5-FU). Predicting the inter- and intra-patient variability in pharmacokinetics and toxicities of 5-FU may contribute to the individualized medicine. This study aimed to establish a population pharmacokinetic-pharmacodynamic model that could evaluate the inter- and intra-individual variability in the plasma 5-FU concentration, 5-FU-induced body weight loss and myelosuppression in rats. METHOD: Plasma 5-FU concentrations, body weight loss, and blood cell counts in rats following the intravenous administration of various doses of 5-FU for 4 days were used to develop the population pharmacokinetic-pharmacodynamic model...
November 26, 2016: European Journal of Drug Metabolism and Pharmacokinetics
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