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https://www.readbyqxmd.com/read/29783787/plasma-pharmacokinetic-determination-of-canagliflozin-and-its-metabolites-in-a-type-2-diabetic-rat-model-by-uplc-ms-ms
#1
Song-Tao Dong, Hui-Min Niu, Yin Wu, Jia-Lei Jiang, Ying Li, Kun-Yu Jiang, Xin Wang, Mao-Fan Zhang, Ming-Feng Han, Sheng-Nan Meng
Canagliflozin is a novel, orally selective inhibitor of sodium-dependent glucose co-transporter-2 (SGLT2) for the treatment of patients with type 2 diabetes mellitus. In this study, a sensitive and efficient UPLC-MS/MS method for the quantification of canagliflozin and its metabolites in rat plasma was established and applied to pharmacokinetics in a type 2 diabetic rat model. We firstly investigated the pharmacokinetic changes of canagliflozin and its metabolites in type 2 diabetic rats in order to use canagliflozin more safely, reasonably and effectively...
May 20, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29782651/pharmacokinetic-and-metabolism-studies-of-bavachinin-through-ultra-high-performance-liquid-chromatography-coupled-with-electrospray-ionization-tandem-mass-spectrometry
#2
Jun Qian, Fan Xie, Yanhong Shi, Jinhang Li, Liuqiang Zhang, Yiming Li, Fujiang Guo, Rui Wang
Bavachinin (BVC), one of the main bioactive prenylated flavonoids derived from Psoralea corylifolia Linn, has a wide variety of pharmacological effects, such as antiangiogenic, antitumour, antiallergic, anti-inflammatory, and antibacterial activities, especially as a pan-peroxisome proliferator-activated receptors (PPARs) agonist. A rapid and sensitive method for quantifying BVC in rat plasma was developed and validated through ultra-high-performance liquid chromatography coupled with electrospray-ionization tandem mass spectrometry...
May 21, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29779406/inhalation-delivery-of-topotecan-is-superior-to-intravenous-exposure-for-suppressing-lung-cancer-in-a-preclinical-model
#3
Philip J Kuehl, Marcie J Grimes, Devon Dubose, Michael Burke, David A Revelli, Andrew P Gigliotti, Steven A Belinsky, Mathewos Tessema
Intravenous (IV) topotecan is approved for the treatment of various malignancies including lung cancer but its clinical use is greatly undermined by severe hematopoietic toxicity. We hypothesized that inhalation delivery of topotecan would increase local exposure and efficacy against lung cancer while reducing systemic exposure and toxicity. These hypotheses were tested in a preclinical setting using a novel inhalable formulation of topotecan against the standard IV dose. Respirable dry-powder of topotecan was manufactured through spray-drying technology and the pharmacokinetics of 0...
November 2018: Drug Delivery
https://www.readbyqxmd.com/read/29778893/synthesis-of-proline-derived-benzenesulfonamides-a-potent-anti-trypanosoma-brucei-gambiense-agent
#4
David I Ugwu, Uchechukwu C Okoro, Narendra K Mishra
Thousands of death in Africa and other developing nations are still attributed to trypanosomiasis. Excessive sleep has been associated with increased inflammation. We report herein, the synthesis, antitrypanosomal and anti-inflammatory activities of eight new carboxamide derivatives bearing substituted benzenesulfonamides. The base promoted reactions of l-proline and L-4-hydroxyproline with substituted benzenesulfonyl chlorides gave the benzenesulfonamides (11a-h) in excellent yields. Boric acid mediated amidation of the benzenesulfonamides (11a-h) and p-aminobenzoic acid (12) gave the new carboxamides (13a-h) in excellent yields...
May 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29777772/improving-maraviroc-oral-bioavailability-by-formation-of-solid-drug-nanoparticles
#5
Alison C Savage, Lee M Tatham, Marco Siccardi, Trevor Scott, Manoli Vourvahis, Andrew Clark, Steve P Rannard, Andrew Owen
Oral drug administration remains the preferred approach for treatment of HIV in most patients. Maraviroc (MVC) is the first in class co-receptor antagonist, which blocks HIV entry into host cells. MVC has an oral bioavailability of approximately 33%, which is limited by poor permeability as well as affinity for CYP3A and several drug transporters. While once-daily doses are now the favoured option for HIV therapy, dose-limiting postural hypotension has been of theoretical concern when administering doses high enough to achieve this for MVC (particularly during coadministration of enzyme inhibitors)...
May 16, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29777509/improving-the-oral-bioavailability-of-tapentadol-via-a-carbamate-prodrug-approach-synthesis-bioactivation-and-pharmacokinetics
#6
Yingchao Li, Yongjun Wang, Ran Zhang, Cuiru Liu, Yue Wei, Jin Sun, Zhonggui He, Youjun Xu, Tianhong Zhang
Tapentadol suffers from rapid clearance due to extensive metabolism in vivo, which results in low oral bioavailability. In the present study, three novel prodrugs of tapentadol (WWJ01, WWJ02, and WWJ03) were synthesized to improve its metabolic stability and thereby improve its oral bioavailability. They all exhibited good stability in phosphate buffers, simulated gastrointestinal fluids, rat plasma, and intestinal and liver homogenates. Disappointingly, the N,N-diethylcarbamate prodrug of tapentadol (WWJ02) and the N,N-diisopropylcarbamate prodrug of tapentadol (WWJ03) were metabolized into inactive metabolites when incubated with liver microsomes...
May 17, 2018: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29777407/modelling-the-delay-between-pharmacokinetics-and-eeg-effects-of-morphine-in-rats-binding-kinetic-versus-effect-compartment-models
#7
Wilhelmus E A de Witte, Vivi Rottschäfer, Meindert Danhof, Piet H van der Graaf, Lambertus A Peletier, Elizabeth C M de Lange
Drug-target binding kinetics (as determined by association and dissociation rate constants, k on and k off ) can be an important determinant of the kinetics of drug action. However, the effect compartment model is used most frequently instead of a target binding model to describe hysteresis. Here we investigate when the drug-target binding model should be used in lieu of the effect compartment model. The utility of the effect compartment (EC), the target binding kinetics (TB) and the combined effect compartment-target binding kinetics (EC-TB) model were tested on either plasma (ECPL , TBPL and EC-TBPL ) or brain extracellular fluid (ECF) (ECECF , TBECF and EC-TBECF ) morphine concentrations and EEG amplitude in rats...
May 18, 2018: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/29773886/pretreatment-with-broad-spectrum-antibiotics-alters-the-pharmacokinetics-of-major-constituents-of-shaoyao-gancao-decoction-in-rats-after-oral-administration
#8
Meng Liu, Jie Yuan, Wen-Juan Hu, Chang-Qiang Ke, Yi-Fan Zhang, Yang Ye, Da-Fang Zhong, Guang-Rong Zhao, Sheng Yao, Jia Liu
The influence of broad-spectrum antibiotics on the pharmacokinetics and biotransformation of major constituents of Shaoyao-Gancao decoction (SGD) in rats was investigated. The pharmacokinetic behaviors of paeoniflorin (PF), albiflorin (AF), liquiritin (LT), isoliquiritin (ILT), liquiritin apioside (LA), isoliquiritin apioside (ILA), and glycyrrhizic acid (GL), seven major constituents of SGD, as well as glycyrrhetinic acid (GA), a major metabolite of GL, were analyzed. A 1-week pretreatment with broad-spectrum antibiotics (ampicillin, metronidazole, neomycin, 1 g L-1 ; and vancomycin, 0...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29773199/health-risk-assessment-of-arsenic-in-realgar-and-niuhuangjiedu-tablets-based-on-pharmacokinetic-study
#9
Xiao Wu, Shanhu Wu, Yuexin Liu, Rong Guan, Fangmei Liang, Min Song, Taijun Hang
NiuHuangJieDu Tablets (NHJDT), a popular realgar (As4 S4 ) containing patented traditional Chinese medicine (TCM), is widely used in the treatment of acute tonsillitis, pharyngitis, periodontitis and mouth ulcer. However, arsenic is considered as one of the most toxic elements, leading to growing concerns about the quality and safety of realgar-containing TCMs recently. In this study, health risk assessment of arsenic in realgar and NHJDT was conducted through oral administration of both substances to rats with single and multiple doses, respectively...
July 2018: Journal of Trace Elements in Medicine and Biology
https://www.readbyqxmd.com/read/29772297/pharmacokinetic-profile-and-oral-bioavailability-of-kaurenoic-acid-from-copaifera-spp-in-rats
#10
Dalyara Mendonça de Matos, Milainy Rocha Viana, Marcela Cristina de Oliveira Alvim, Lara Soares Aleixo de Carvalho, Laura Hora Rios Leite, Ademar Alves da Silva Filho, Jorge Willian Leandro Nascimento
Kaurenoic acid (KA) is a kaurane diterpene found in several medicinal plants that displays biological activities, such as anti-inflammatory, smooth muscle relaxant and hypotensive response. However, there are no pharmacokinetic data available about this molecule. The purpose of the study was to determine the pharmacokinetics profile and the oral bioavailability of KA in rats. Wistar rats submitted to jugular vein cannulation received 50 mg/kg of KA by intravenous or oral route. The implanted cannula allowed intravenous administration and serial blood collection along 10 h...
May 14, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29771932/a-multi-center-preclinical-study-of-gadoxetate-dce-mri-in-rats-as-a-biomarker-of-drug-induced-inhibition-of-liver-transporter-function
#11
Anastassia Karageorgis, Stephen C Lenhard, Brittany Yerby, Mikael F Forsgren, Serguei Liachenko, Edvin Johansson, Mark A Pilling, Richard A Peterson, Xi Yang, Dominic P Williams, Sharon E Ungersma, Ryan E Morgan, Kim L R Brouwer, Beat M Jucker, Paul D Hockings
Drug-induced liver injury (DILI) is a leading cause of acute liver failure and transplantation. DILI can be the result of impaired hepatobiliary transporters, with altered bile formation, flow, and subsequent cholestasis. We used gadoxetate dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI), combined with pharmacokinetic modelling, to measure hepatobiliary transporter function in vivo in rats. The sensitivity and robustness of the method was tested by evaluating the effect of a clinical dose of the antibiotic rifampicin in four different preclinical imaging centers...
2018: PloS One
https://www.readbyqxmd.com/read/29768080/effects-of-quercetin-on-the-pharmacokinetics-of-losartan-and-its-metabolite-exp3174-in-rats
#12
Qingling Zhao, Jinlan Wei, Hongying Zhang
1. This study investigates the influence of quercetin on the pharmacokinetics of losartan and its metabolite EXP3174 in rats. 2. The pharmacokinetic profiles of losartan and EXP3174 of orally administered losartan (10 mg/kg) with or without pretreatment with quercetin (20 mg/kg/day for 7 days) were investigated. Additionally, Caco-2 cell transwell model and rat liver microsome incubation experiments were also conducted to investigate its potential mechanism. 3. The results showed that when the rats were pretreated with quercetin, the Cmax (2...
May 16, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29765372/is-iqg-607-a-potential-metallodrug-or-metallopro-drug-with-a-defined-molecular-target-in-mycobacterium-tuberculosis
#13
REVIEW
Bruno L Abbadi, Valnês da Silva Rodrigues-Junior, Adilio da Silva Dadda, Kenia Pissinate, Anne D Villela, Maria M Campos, Luiz G de França Lopes, Cristiano V Bizarro, Pablo Machado, Eduardo H S Sousa, Luiz A Basso
The emergence of strains of Mycobacterium tuberculosis resistant to isoniazid (INH) has underscored the need for the development of new anti-tuberculosis agents. INH is activated by the mycobacterial katG -encoded catalase-peroxidase, forming an acylpyridine fragment that is covalently attached to the C4 of NADH. This isonicotinyl-NAD adduct inhibits the activity of 2- trans -enoyl-ACP(CoA) reductase (InhA), which plays a role in mycolic acid biosynthesis. A metal-based INH analog, Na3 [FeII (CN)5 (INH)]·4H2 O, IQG-607, was designed to have an electronic redistribution on INH moiety that would lead to an intramolecular electron transfer to bypass KatG activation...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29759726/n-aryl-piperidine-4-carboxamides-as-a-novel-class-of-potent-inhibitors-of-malt1-proteolytic-activity
#14
Achim Schlapbach, Laszlo Revesz, Carole Pissot Soldermann, Thomas Zoller, Catherine H Régnier, Frédéric Bornancin, Thomas Radimerski, Jutta Blank, Ansgar Schuffenhauer, Martin Renatus, Paulus Erbel, Samu Melkko, Richard Heng, Oliver Simic, Ralf Endres, Markus Wartmann, Jean Quancard
Starting from a weak screening hit, potent and selective inhibitors of the MALT1 protease function were elaborated. Advanced compounds displayed high potency in biochemical and cellular assays. Compounds showed activity in a mechanistic Jurkat T cell activation assay as well as in the B-cell lymphoma line OCI-Ly3, which suggests potential use of MALT1 inhibitors in the treatment of autoimmune diseases as well as B-cell lymphomas with a dysregulated NF-κB pathway. Initially, rat pharmacokinetic properties of this compound series were dominated by very high clearance which could be linked to amide cleavage...
May 9, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29759252/simultaneous-determination-of-quercetin-and-its-metabolites-in-rat-plasma-by-using-ultra-high-performance-liquid-chromatography-tandem-mass-spectrometry
#15
Veronika Pilařová, Kateřina Plachká, Lucia Chrenková, Iveta Najmanová, Přemysl Mladěnka, František Švec, Ondřej Novák, Lucie Nováková
Fast, selective, and sensitive ultra-high performance liquid chromatography method with tandem mass spectrometry detection for the determination of quercetin and its metabolites with various physico-chemical properties such as molecular weight, lipophilicity, and acid-base properties has been developed. These compounds included small hydrophilic phenolic acids and more lipophilic metabolites with preserved flavonoid structure in small amount of rat plasma. The developed method enables selective separation of phenolic acids and a pair of isomers tamarixetin and isorhamnetin with satisfactory peak shapes and a high sensitivity using mass spectrometry detection...
August 1, 2018: Talanta
https://www.readbyqxmd.com/read/29756294/determination-of-brompheniramine-enantiomers-in-rat-plasma-by-cation-selective-exhaustive-injection-and-sweeping-cyclodextrin-modified-electrokinetic-chromatography-method
#16
Yaqi Yao, Yu Zhao, Xue Zhang, Jia Yu, Xingjie Guo
A method consisting of cation-selective exhaustive injection and sweeping (CSEI-sweeping) as online preconcentration followed by a cyclodextrin modified electrokinetic chromatography (CDEKC) enantioseparation has been developed for the simultaneous determination of two brompheniramine enantiomers in rat plasma. In this method, analytes were electrokinetically injected at a voltage of 8 kV for 80 s in a fused-silica capillary. Prior to the injection, the capillary was rinsed with 50 mM phosphate buffer pH 3...
May 13, 2018: Electrophoresis
https://www.readbyqxmd.com/read/29755544/physicochemical-stress-degradation-evaluation-and-pharmacokinetic-study-of-azgh101-a-new-synthesized-cox2-inhibitor-after-i-v-and-oral-administration-in-male-and-female-rats
#17
Hoda Bahmanof, Simin Dadashzadeh, Afshin Zarghi, Alireza Shafaati, Seyed Mohsen Foroutan
Nonsteroidal anti-inflammatory drugs (NSAIDs) act mainly via inhibition of prostaglandins synthesis by inhibition of cyclooxygenase (COX) isoenzymes (COX-1 and COX-2). Selective COX-2 inhibitors which are also known as coxibs provide the main therapeutic effects of NSAIDs. Zarghi et al . reported 6-benzoyl-2-(4-(methylsulfonyl) phenyl) quinoline-4-carboxylic acid (AZGH101) as a novel derivative of ketoprofen with improved selectivity index (COX-1/COX-2 inhibitory potency) in comparison with ketoprofen. In this study, the log P and stability of AZGH101 were evaluated and the pharmacokinetic characteristics of this compound were investigated following intravenous (10 mg/kg), and oral administration (20 mg/kg), to Wistar rats...
2018: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29754833/discovery-of-benzimidazole-derivatives-as-orally-active-renin-inhibitors-optimization-of-3-5-disubstituted-piperidine-to-improve-pharmacokinetic-profile
#18
Hidekazu Tokuhara, Yasuhiro Imaeda, Yoshiyuki Fukase, Koichi Iwanaga, Naohiro Taya, Koji Watanabe, Ray Kanagawa, Keisuke Matsuda, Yumiko Kajimoto, Keiji Kusumoto, Mitsuyo Kondo, Gyorgy Snell, Craig A Behnke, Takanobu Kuroita
We previously identified 2-tert-butyl-4-[(3-methoxypropyl)amino]-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]pyrimidine-5-carboxamide 3 as a potent renin inhibitor. Since 3 showed unacceptably low bioavailability (BA) in rats, structural modification, using SBDD and focused on physicochemical properties was conducted to improve its PK profile while maintaining renin inhibitory activity. Conversion of the amino group attached at the 4-position of pyrimidine to methylene group improved PK profile and decreased renin inhibitory activity...
April 27, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29754485/supersaturable-self-emulsifying-drug-delivery-system-of-krill-oil-with-improved-oral-absorption-and-hypotriglyceridemic-function
#19
Yoshiki Seto, Chikara Morizane, Kodai Ueno, Hideyuki Sato, Satomi Onoue
This study aimed to develop a supersaturable self-emulsifying drug delivery system (S-SEDDS) of krill oil (KO), a rich source of docosahexaenoic acid and eicosapentaenoic acid (EPA), to improve its hypotriglyceridemic function. S-SEDDS of KO (KO/S-SEDDS) was prepared by the addition of lysolecithin, glycerin, and hydroxypropyl methylcellulose (HPMC). SEDDS of KO (KO/SEDDS) and KO with HPMC (KO/HPMC) were also prepared for comparison purposes. The physicochemical and pharmacokinetic properties of KO samples were characterized, and the hypotriglyceridemic function of KO/S-SEDDS was evaluated...
May 14, 2018: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29753956/smart-gated-magnetic-silica-mesoporous-particles-for-targeted-colon-drug-delivery-new-approaches-for-inflammatory-bowel-diseases-treatment
#20
Adrián H Teruel, Édgar Pérez-Esteve, Isabel González-Álvarez, Marta González-Álvarez, Ana M Costero, Daniel Ferri, Margarita Parra, Pablo Gaviña, Virginia Merino, Ramón Martínez-Mañez, Félix Sancenón
Magnetic mesoporous silica microparticles were loaded with safranin O (S1) and with hydrocortisone (S2) and the outer surface functionalized with a bulky azo derivative bearing urea moieties. Aqueous suspensions of both solids at pH 7.4 showed negligible payload release whereas a marked delivery was observed in the presence of sodium dithionite due to the rupture of the azo bonds. Besides, a moderate cargo release was observed at acidic pH due to the hydrolysis of the urea bonds that linked the azo derivative onto the external surface of the inorganic scaffolds...
May 10, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
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