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pharmacokinetics, rat

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https://www.readbyqxmd.com/read/28087908/-berberine-regulates-glycemia-via-local-inhibition-of-intestinal-dipeptidyl-peptidase-%C3%A2
#1
Jiesheng Wang, Guanhai Dai, Weijia Li
Objective: To investigate the effect of berberine on glycemia regulation in rats with diabetes and the related mechanisms. Methods: Diabetic-like rat model was successfully induced by intraperitoneal injection of streptozotocin in 50 out of 60 male SD rats, which were then randomly divided into 5 groups with 10 rats in each:control group (received vehicle only), positive drug control group (sitagliptin 10 mg·kg(-1)·d(-1)), low-dose berberine group (30 mg·kg(-1)·d(-1)), moderate-dose berberine group (60 mg·kg(-1)·d(-1)), and high-dose berberine group (120 mg·kg(-1)·d(-1))...
May 25, 2016: Zhejiang da Xue Xue Bao. Yi Xue Ban, Journal of Zhejiang University. Medical Sciences
https://www.readbyqxmd.com/read/28087352/engineering-hot-melt-extruded-solid-dispersion-for-controlled-release-of-hydrophilic-drugs
#2
Shuli Zhang, Xuan Meng, Zheng Wang, Aiping Fan, Guocheng Wang, Yanjun Zhao, Yu Tang
It is often challenging to precisely manipulate the release behavior of hydrophilic drugs that is believed to be crucial for a satisfactory therapeutic outcome. The aim of this work was to regulate the dissolution of hydrophilic drug from hot-melt extruded solid dispersion via rational screening of the pore-forming agents. Venlafaxine hydrochloride and Compritol® 888 ATO was selected as the model drug and carrier excipient, respectively. Hydrophilic polyethylene glycol (PEG 6000) and polyvinylpyrolidone (PVP K30) were chosen as the transient pore-forming agents...
January 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28081477/pharmacokinetic-studies-of-active-triterpenoid-saponins-and-the-total-secondary-saponin-from-anemone-raddeana-regel
#3
Dandan Zhang, Tianli Lei, Chongning Lv, Huimin Zhao, Haiyan Xu, Jincai Lu
The rhizome of Anemone raddeana Regel, a Traditional Chinese Medicine (TCM) which has a robust history treating rheumatism and neuralgia. The total secondary saponin (TSS) from it has demonstrated antitumor activity. In this study, a rapid and validated LC-MS/MS method was developed to simultaneously determine the active compounds (Hederacolchiside A1 and Eleutheroside K). Analytes were separated on a reverse-phase C18 column with acetonitrile-water (5mmol/L ammonium acetate) as the mobile phase. This assay showed acceptable linearity (r>0...
January 3, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28080060/pharmacokinetics-of-the-individual-major-components-of-polymyxin-b-and-colistin-in-rats
#4
Sivashangarie Sivanesan, Kade Roberts, Jiping Wang, Soon-Ee Chea, Philip E Thompson, Jian Li, Roger L Nation, Tony Velkov
The pharmacokinetics of polymyxin B1, polymyxin B2, colistin A, and colistin B were investigated in a rat model following intravenous administration (0.8 mg/kg) of each individual component. Plasma and urine concentrations were determined by LC-MS/MS, and plasma protein binding was measured by ultracentrifugation. Total and unbound pharmacokinetic parameters for each component were calculated using noncompartmental analysis. All of the polymyxin components had a similar clearance, volume of distribution, elimination half-life, and urinary recovery...
January 12, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28074467/systems-pharmacology-modeling-of-drug-induced-hyperbilirubinemia-differentiating-hepatotoxicity-and-inhibition-of-enzymes-transporters
#5
Kyunghee Yang, Christina Battista, Jeffrey L Woodhead, Simone H Stahl, Jerome T Mettetal, Paul B Watkins, Scott Q Siler, Brett A Howell
Elevations in serum bilirubin during drug treatment may indicate global liver dysfunction and a high risk of liver failure. However, drugs also can increase serum bilirubin in the absence of hepatic injury by inhibiting specific enzymes/transporters. We constructed a mechanistic model of bilirubin disposition based on known functional polymorphisms in bilirubin metabolism/transport. Using physiologically-based pharmacokinetic model-predicted drug exposure and enzyme/transporter inhibition constants determined in vitro, our model correctly predicted indinavir-mediated hyperbilirubinemia in humans and rats...
January 11, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28070878/effects-of-caffeic-acid-and-quercetin-on-in-vitro-permeability-metabolism-and-in-vivo-pharmacokinetics-of-melatonin-in-rats-potential-for-herb-drug-interaction
#6
Snehasis Jana, Himanshu Rastogi
BACKGROUND AND OBJECTIVES: Melatonin is a popular dietary supplement and also considered as pharmaceutical product for sleep disorders. Caffeic acid and quercetin are widely distributed in leafy vegetables, fruits, tea extract, and both are used as natural antioxidant. There is an immense concern for health researchers to study the herb/food-drug interactions of melatonin. It is mainly metabolized by CYP1A2 in human so that herbs/foods containing cytochrome P450 (CYP) inhibitors can affect pharmacokinetics of melatonin...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070711/immune-suppression-during-preclinical-drug-development-mitigates-immunogenicity-mediated-impact-on-therapeutic-exposure
#7
Jonathan Herskovitz, Josiah Ryman, Theingi Thway, Stephanie Lee, Lei Zhou, Narendra Chirmule, Bernd Meibohm, Vibha Jawa
In the clinical setting, anti-drug antibodies (ADA) against biotherapeutics can influence patient safety and interfere with product efficacy. High immunogenicity has been addressed in clinic by concomitant immune suppression, such as co-administration of methotrexate with enzyme replacement therapy (ERT) and combination tacrolimus/sirolimus treatment for prophylaxis against organ transplant rejection. This study investigates the use of such immune suppressants in mitigating ADA responses to a fully human monoclonal antibody (mAb1) in preclinical animal studies...
January 9, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28069939/real-time-measurement-of-small-molecules-directly-in-awake-ambulatory-animals
#8
Netzahualcóyotl Arroyo-Currás, Jacob Somerson, Philip A Vieira, Kyle L Ploense, Tod E Kippin, Kevin W Plaxco
The development of a technology capable of tracking the levels of drugs, metabolites, and biomarkers in the body continuously and in real time would advance our understanding of health and our ability to detect and treat disease. It would, for example, enable therapies guided by high-resolution, patient-specific pharmacokinetics (including feedback-controlled drug delivery), opening new dimensions in personalized medicine. In response, we demonstrate here the ability of electrochemical aptamer-based (E-AB) sensors to support continuous, real-time, multihour measurements when emplaced directly in the circulatory systems of living animals...
January 9, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28069868/liquid-chromatography-tandem-mass-spectrometric-analysis-of-octaethylene-glycol-monodecyl-ether-in-rat-plasma-and-its-application-to-pharmacokinetic-studies
#9
Hyeon Kim, Hyeong Jun Kim, Min Sun Choi, In Sook Kim, Myung Chan Gye, Hye Hyun Yoo
Alcohol ethoxylates (AEs) are a major class of non-ionic surfactants, which are widely used in household, institutional and industrial cleaners, and they are considered as an alternative of nonylphenol. In this study, a rapid, sensitive and reliable bioanalytical method was developed for the determination of octaethylene glycol monodecyl ether (C10E8, an AE) in rat plasma using liquid chromatography-tandem mass spectrometry (LC-MS-MS). Chromatographic separation was performed on a reversed-phase C18 column (2...
January 8, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28069721/specific-inhibition-of-the-distribution-of-lobeglitazone-to-the-liver-by-atorvastatin-in-rats-evidence-for-an-roatp1b2-mediated-interaction-in-hepatic-transport
#10
Chang-Soon Yim, Yoo-Seong Jeong, Song-Yi Lee, Wonji Pyeon, Heon-Min Ryu, Jong-Hwa Lee, Kyeong-Ryoon Lee, Han-Joo Maeng, Suk-Jae Chung
CYP enzymes and hOATP1B1 are reported to be involved in the pharmacokinetics of lobeglitazone (LB), a new PPARγ agonist. Atorvastatin (ATV), a substrate for CYP3A and hOATP1B1, is likely to be co-administered with LB in patients with the metabolic syndrome. We report herein on a study of potential interactions between LB and ATV in rats. When LB was IV-administered with ATV, the systemic clearance (CL; 2.67 ± 0.63 mL/min/kg) and volume of distribution at steady-state (Vss; 289 ± 20 mL/kg) for LB remained unchanged, compared to those of LB without ATV (CL, 2...
January 9, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28069690/development-of-solid-phase-extraction-and-hplc-method-for-simultaneous-estimation-of-ilaprazole-and-glimepiride-in-rat-plasma-application-to-pharmacokinetic-studies
#11
A P Dewani, A S Tripathi, P G Shelke, R L Bakal, D S Mohale, A V Chandewar
A novel, simple and mass spectrometry (MS) compatible high-performance liquid chromatography (HPLC) method is reported for the simultaneous estimation of ilaprazole (ILA) and glimepiride (GLM) in rat plasma. The bio-analytical procedure involves extraction of ILA, GLM and internal standard (IS) from rat plasma with a solid-phase extraction (SPE) process. The chromatographic analysis was performed on Waters-600 system using an isocratic mobile phase comprising methanol:water (80:20 % v/v) with pH of water modified to three using formic acid at a flow rate of 1...
January 8, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28067090/assessment-of-formulated-amodiaquine-microparticles-in-leishmania-donovani-infected-rats
#12
Henry Nettey, Grace Lovia Allotey-Babington, Isaac Somuah, N'guessan Benoit Banga, Barima Afrane, Seth Kwabena Amponsah, Henrietta Annor, Henry Darko, Kwame Hanson, Anoa Aidoo, Marisa Nyarkoa Broni, Clement Sasu, Alexander Nyarko
The aim of this study was to formulate, characterize and evaluate the activity of Amodiaquine microparticles against Leishmania donovani. Microparticles were formulated by encapsulating the drug in bovine serum albumin using the spray-dryer method. The microparticles were evaluated for size, zeta potential, drug content, encapsulation efficiency and in vitro release profile. The size range of the microparticles formulated was between 1.9 and 10 µm with an average zeta potential of -25.5 mV. Of the expected 20% drug loading, an average of 18...
January 9, 2017: Journal of Microencapsulation
https://www.readbyqxmd.com/read/28064067/simultaneous-determination-of-imperatorin-and-its-metabolite-xanthotoxol-in-rat-plasma-and-urine-by-lc-ms-ms-and-its-application-to-pharmacokinetic-studies
#13
Lien Ngo, Phuong Tran, Seong-Ho Ham, Jung-Hee Cho, Hea-Young Cho, Yong-Bok Lee
An accurate, precise, selective, and sensitive liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) method was developed for the simultaneous determination of imperatorin (IMP) and its metabolite, xanthotoxol (XAN), in rat plasma and urine samples. The analytes, along with psoralen as an internal standard, were determined by multiple reaction monitoring (MRM) operated in the positive electrospray ionization (ESI) mode. Chromatographic separation was performed on an Acquity UPLC BEH C18 column (50mm×2...
December 28, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28060996/determination-of-a-naturally-dnmt1-inhibitor-peperomin-e-in-rat-plasma-by-uflc-ms-ms-and-method-application-in-pharmacokinetic-study
#14
Xin-Zhi Wang, Hong-Mei Wen, Chuan Chai, Wen-Ying Zhang, Ming Gao, Rui Liu, Hao Wu, Jing-Yu Liang
Peperomin E (PepE), a naturally occurring secolignan isolated from Peperomia dindygulensis, has drawn much attention recently due to its anticancer and DNA methyltransferase 1 (DNMT1) inhibitory activity. Here, a simple and sensitive ultra-fast liquid chromatography-tandem mass spectrometry method was developed and validated for the determination of PepE in rat plasma for the first time. Samples were prepared by simple protein precipitation. Separation was performed on an XBridge(TM) C18 column using a mobile phase of acetonitrile and 0...
January 6, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28057546/in-vitro-and-in-vivo-evaluation-of-a-hydrogel-based-microneedle-device-for-transdermal-electro-modulated-analgesia
#15
Sunaina Indermun, Yahya E Choonara, Pradeep Kumar, Lisa C du Toit, Girish Modi, Regina Luttge, Mershen Govender, Viness Pillay
With a significant portion of the world suffering from chronic pain, the management and treatment of this condition still requires extensive research to successfully mobilize and functionalize its sufferers. This paper details the in vitro and in vivo evaluation of a transdermal Electro-Modulated Hydrogel- Microneedle array (EMHM) device for the treatment of chronic pain. In vitro characterization of the Electro-Modulated Hydrogel was undertaken prior to the determination of the in vivo release, histopathological and pharmacokinetic profiles of the EMHM in a Sprague Dawley rat model...
January 2, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28057170/can-the-ceiba-cocktail-designed-for-human-cytochrome-p450-enzymes-be-used-in-the-rat-for-drug-interaction-studies
#16
Paulo Magalhães, Fernando De Andrés, Amílcar Falcão, Adrián LLerena, Gilberto Alves
Purpose - The CEIBA cocktail consisting of caffeine (CAF), omeprazole (OZ), dextromethorphan (DM) and losartan (LOS) was previously proposed for the clinical phenotyping of five major human cytochrome P450 (CYP) isoenzymes. This work aimed to assess the usefulness of CEIBA cocktail to study non-clinical drug interactions in the rat. Methods - Wistar rats were divided into five groups to receive a single-oral dose of each probe drug (CAF, OZ, LOS, DM), individually or in combination as a cocktail. Plasma concentrations of the probe drugs and their metabolites [paraxanthine (1,7-X), 5-hydroxyomeprazole (5-OZ), losartan carboxylic acid (E-3174), dextrorphan (DX) and 3-methoxymorphinan (3-MM)] were determined by LC-MS/MS, and the corresponding pharmacokinetic parameters were estimated by non-compartmental analysis...
October 2016: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28056947/triptolide-induces-hepatotoxicity-via-inhibition-of-cyp450s-in-rat-liver-microsomes
#17
Yan Lu, Tong Xie, Yajie Zhang, Fuqiong Zhou, Jie Ruan, Weina Zhu, Huaxu Zhu, Zhe Feng, Xueping Zhou
BACKGROUND: Triptolide (TP), an active constituent of Tripterygium wilfordii, possesses numerous pharmacological activities. However, its effects on cytochrome P450 enzymes (CYP450s) in rats remain unexplored. METHODS: In this study, the effects of triptolide on the six main CYP450 isoforms (1A2, 2C9, 2C19, 2D6, 2E1, and 3A) were investigated both in vivo and in vitro. We monitored the body weight, survival proportions, liver index, changes in pathology, and biochemical index upon TP administration, in vivo...
January 5, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28056427/sensitive-analysis-and-simultaneous-assessment-of-pharmacokinetic-properties-of-crocin-and-crocetin-after-oral-administration-in-rats
#18
Yue Zhang, Fei Fei, Le Zhen, Xuanxuan Zhu, Jiankun Wang, Sijia Li, Jianliang Geng, Runbin Sun, Xiaoyi Yu, Tingting Chen, Siqi Feng, Pei Wang, Na Yang, Yejin Zhu, Jingqiu Huang, Yuqing Zhao, Jiye Aa, Guangji Wang
Crocin and crocetin in rat plasma were simultaneously analysed using ultra-performance liquid chromatography tandem mass spectroscopy (UPLC-MS/MS), and method was fully validated. For the first time, levels of both crocin and crocetin in plasma were profiled after oral administration of crocin, and this UPLC-MS/MS approach was applied to evaluate pharmacokinetics and relative bioavailability of crocin and crocetin in rats. It was shown that crocin transformed into crocetin quickly in the gastrointestinal tract, and crocetin was 56-81 fold higher exposed in rat plasma than crocin after oral administration of crocin...
December 15, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28055308/binding-to-ocular-albumin-as-a-half-life-extension-principle-for-intravitreally-injected-drugs-evidence-from-mechanistic-rat-and-rabbit-studies
#19
Holger Fuchs, Frederik Igney
PURPOSE: The ocular half-life of intravitreally (IVT) injected drugs is of major relevance for the suitability of a drug intended for chronic intraocular treatment, as the half-life determines the dosing frequency. Thus, half-life extension principles are very attractive as they can reduce the IVT dosing frequency. In this study, we investigated the ocular pharmacokinetics (PK) of the IVT injected Nanobody(®) BI-X and whether the noncovalent binding of BI-X to vitreous albumin could increase its ocular half-life...
January 5, 2017: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28055204/design-synthesis-of-novel-potent-selective-orally-bio-available-adenosine-a2a-receptor-antagonists-and-their-biological-evaluation
#20
Sujay Basu, Dinesh A Barawkar, Sachin Thorat, Yogesh D Shejul, Meena Patel, Minakshi Naykodi, Vaibhav Jain, Yogesh Salve, Vandna Prasad, Sumit Chaudhary, Indraneel Ghosh, Ganesh Bhat, Azfar Quraishi, Harish Patil, Shariq Ansari, Suraj Menon, Vishal Unadkat, Rhishikesh Thakare, Madhav S Seervi, Ashwinkumar V Meru, Siddhartha De, Ravi K Bhamidipati, Sreekanth Rouduri, Venkata P Palle, Anita Chug, Kasim A Mookhtiar
Our initial structure-activity relationship studies on 7-methoxy-4-morpholino-benzothiazole derivatives featured by aryloxy-2-methylpropanamide moieties at the 2-position lead to identification of compound 25 as a potent and selective A2A adenosine receptor (A2AAdoR) antagonist with reasonable ADME and pharmacokinetic properties. However, poor intrinsic solubility and low to moderate oral bioavailability made this series unsuitable for further development. Further optimization using structure-based drug design approach resulted in discovery of potent and selective adenosine A2A receptor antagonists bearing substituted 1-methylcyclohexyl-carboxamide groups at position 2 of the benzothiazole scaffold and endowed with better solubility and oral bioavailability...
January 5, 2017: Journal of Medicinal Chemistry
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