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pharmacokinetics, rat

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https://www.readbyqxmd.com/read/28346885/plasma-and-brain-pharmacokinetics-of-ganoderic-acid-a-in-rats-determined-by-a-developed-uflc-ms-ms-method
#1
Fang-Rui Cao, Bing-Xin Xiao, Li-Sha Wang, Xue Tao, Ming-Zhu Yan, Rui-Le Pan, Yong-Hong Liao, Xin-Min Liu, Qi Chang
Ganoderic acid A (GAA), an active triterpenoid of the traditional Chinese herbal medicine Lingzhi, has been reported to exhibit antinociceptive, antioxidative, and anti-cancer activities. The present study aims to establish a sensitive and rapid UPLC-MS/MS method for studying the plasma and brain pharmacokinetics of GAA in rats. The analytes were separated on a C18 column eluted with a gradient mobile phase consisting of acetonitrile and 0.1% aqueous formic acid at 0.3mL/min. The eluate was monitored by a mass detector using an MRM (m/z, 515...
March 11, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28346882/determination-of-prodrug-treosulfan-and-its-biologically-active-monoepoxide-in-rat-plasma-liver-lungs-kidneys-muscle-and-brain-by-hplc-esi-ms-ms-method
#2
Michał Romański, Anna Kasprzyk, Artur Teżyk, Agnieszka Widerowska, Czesław Żaba, Franciszek Główka
A prodrug treosulfan (TREO) is currently investigated in clinical trials for conditioning prior to hematopoietic stem cell transplantation. Bioanalysis of TREO and its active derivatives, monoepoxide (S,S-EBDM) and diepoxide, in plasma and urine underlay the pharmacokinetic studies of these compounds but cannot explain an organ pharmacological action or toxicity. Recently, distribution of TREO and S,S-EBDM into brain, cerebrospinal fluid, and aqueous humor of the eye has been investigated in animal models and the obtained results presented clinical relevance...
March 18, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28346390/the-effect-and-mechanism-of-transdermal-penetration-enhancement-of-fu-s-cupping-therapy-new-physical-penetration-technology-for-transdermal-administration-with-traditional-chinese-medicine-tcm-characteristics
#3
Wei-Jie Xie, Yong-Ping Zhang, Jian Xu, Xiao-Bo Sun, Fang-Fang Yang
BACKGROUND: In this paper, a new type of physical penetration technology for transdermal administration with traditional Chinese medicine (TCM) characteristics is presented. Fu's cupping therapy (FCT), was established and studied using in vitro and in vivo experiments and the penetration effect and mechanism of FCT physical penetration technology was preliminarily discussed. METHODS: With 1-(4-chlorobenzoyl)-5-methoxy-2-methylindole-3-ylacetic acid (indomethacin, IM) as a model drug, the establishment of high, medium, and low references was completed for the chemical permeation system via in vitro transdermal tests...
March 27, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28345817/simultaneous-determination-of-multiple-active-components-in-rat-plasma-using-ultra-fast-liquid-chromatography-with-tandem-mass-spectrometry-and-application-to-a-comparative-pharmacokinetic-study-after-oral-administration-of-suan-zao-ren-decoction-and-suan-zao
#4
Yiyang Du, Bosai He, Qing Li, Jiao He, Di Wang, Kaishun Bi
Suan-Zao-Ren decoction has been used to treat insomnia for many years. In this work, a rapid and sensitive ultra-fast liquid chromatography with tandem mass spectrometry method was first developed and fully validated for the simultaneous quantification of seven main active components, spinosin, mangiferin, neomangiferin, ferulic acid, liquiritin, isoliquiritin and liquiritin apioside in rat plasma. The method was also successfully applied to compare the pharmacokinetics of these active ingredients after oral administration of Suan-Zao-Ren decoction and Suan-Zao-Ren granule...
March 27, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28344497/effect-of-nitazoxanide-on-albendazole-pharmacokinetics-in-cerebrospinal-fluid-and-plasma-in-rats
#5
María Isabel Ruiz-Olmedo, Iliana González-Hernández, Francisca Palomares-Alonso, Javier Franco-Pérez, María de Lourdes González F, Helgi Jung-Cook
Background: Although albendazole is the drug-of-choice for the treatment of neurocysticercosis, its efficacy is limited due to its low bioavailability. An alternative for optimizing pharmacological treatment is through drug combinations. In vitro studies have shown that nitazoxanide and tizoxanide (the active metabolite of nitazoxanide) exhibit cysticidal activity and that the combination of tizoxanide with albendazole sulfoxide (the active metabolite of albendazole) produced an additive effect. Objectives: (1) To assess the concentration profile of tizoxanide in plasma and in cerebrospinal fluid; and (2) to evaluate the influence of nitazoxanide on the pharmacokinetics of albendazole in plasma and in cerebrospinal fluid...
March 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28344015/transdermal-delivery-of-atorvastatin-calcium-from-novel-nanovesicular-systems-using-polyethylene-glycol-fatty-acid-esters-ameliorated-effect-without-liver-toxicity-in-poloxamer-407-induced-hyperlipidemic-rats
#6
Mohamed O Mahmoud, Heba M Aboud, Amira H Hassan, Adel A Ali, Thomas P Johnston
CONTEXT: Atorvastatin calcium (ATV), a cholesterol-lowering agent, suffers from poor systemic availability (14%) after oral administration in addition to other side effects on the gastrointestinal tract, liver and muscle. OBJECTIVE: The goal of the present investigation was to improve ATV bioavailability and overcome complications attendant with peroral administration by developing a new nanovesicular system encapsulating ATV for its delivery via the transdermal route...
March 23, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28342981/mechanisms-of-in-vivo-release-of-triamcinolone-acetonide-from-plga-microspheres
#7
Amy C Doty, David G Weinstein, Keiji Hirota, Karl F Olsen, Rose Ackermann, Yan Wang, Stephanie Choi, Steven P Schwendeman
Little is known about the underlying effects controlling in vitro-in vivo correlations (IVIVCs) for biodegradable controlled release microspheres. Most reports of IVIVCs that exist are empirical in nature, typically based on a mathematical relationship between in vitro and in vivo drug release, with the latter often estimated by deconvolution of pharmacokinetic data. In order to improve the ability of in vitro release tests to predict microsphere behavior in vivo and develop more meaningful IVIVCs, the in vivo release mechanisms need to be characterized...
March 22, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28342304/rapid-profiling-and-pharmacokinetic-studies-of-major-compounds-in-crude-extract-from-polygonum-multiflorum-by-uhplc-q-tof-ms-and-uplc-ms-ms
#8
Linlin Wang, Mangmang Sang, Erwei Liu, Prince Osei Banahene, Yi Zhang, Tao Wang, Lifeng Han, Xiumei Gao
A reliable, rapid analytical method was established for characterization of constituents in the ethanol extract of Polygonum multiflorum by combining an ultra-high performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS). 131 constituents which including phenolic acids, stilbenes, flavones, anthraquinones, naphthalenes and their derivatives were identified or tentatively identified by using characteristic diagnostic fragment ions and references. The established method was further applied to analyze blood samples, and successfully identified 41 compounds which were absorbed through the gastrointestine in rats after administration the extract of P...
March 18, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28342292/ultra-fast-liquid-chromatography-with-tandem-mass-spectrometry-determination-of-eight-bioactive-components-of-kai-xin-san-in-rat-plasma-and-its-application-to-a-comparative-pharmacokinetic-study-in-normal-and-alzheimer-s-disease-rats
#9
Xiaotong Wang, Yue Zhang, Huibin Niu, Yajing Geng, Bing Wang, Xiaomei Yang, Pengyu Yan, Qing Li, Kaishun Bi
A method of ultra-fast liquid chromatography with tandem mass spectrometry was developed and validated for the simultaneous quantitation of eight bioactive components, including polygalaxanthone III, sibiricaxanthone B, tenuifolin, sibiricose A5, sibiricose A6, tenuifoliside A, ginsenoside Re and ginsenoside Rb1 in rat plasma after oral administration of Kai-Xin-San. The plasma samples were extracted by liquid-liquid extraction using digoxin as internal standard. Chromatographic separation was performed on a Venusil MP C18 column (100 mm × 2...
March 25, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28340950/pharmacokinetics-and-bioavailability-of-oral-single-dose-maleic-acid-in-biofluids-of-sprague-dawley-rats
#10
Charlene Wu, Hsin-Chang Chen, Yu-Syuan Luo, Su-Yin Chiang, Kuen-Yuh Wu
Maleic acid (MA) was purposefully adulterated in an array of starch-based foods in Taiwan, inciting a food safety incident. Due to limited data on the pharmacokinetics and bioavailability of ingested MA, we studied pharmacokinetic (PK) parameters in serum and urine of Sprague Dawley rats. Three groups of male and female rats were given three doses of MA by oral gavage; biofluid samples were collected accordingly. Data demonstrated that a non-compartment model best described MA's linear kinetic behavior upon ingestion...
December 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28338409/self-emulsifying-preconcentrates-of-daidzein-phospholipid-complex-design-in-vitro-and-in-vivo-appraisal
#11
Yosra Sr Elnaggar, Eman Mm Shehata, Sally Galal, Ossama Y Abdallah
AIM: Self-emulsifying phospholipid-complex preconcentrates (SEPPs) were fabricated to improve oral bioavailability of daidzein (DAI), an anticancer drug with challenging amphiphobic nature and extensive presystemic metabolism. METHODS: DAI-phosphatidylcholine complex was prepared to enhance DAI lipophilicity and loading in SEPPs. The physicochemical characteristics and the pharmacokinetic behavior in rats were studied. RESULTS: Surfactant-free SEPP (plain DAI:Phosal(®) 53MCT complex) was monodisperse upon aqueous dilution with nanorange globule size (485 ± 15 nm)...
March 24, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28338324/studies-to-examine-potential-tolerability-differences-between-the-5-ht2c-receptor-selective-agonists-lorcaserin-and-cp-809101
#12
Guy A Higgins, Leonardo B Silenieks, Amy Patrick, Ines A M De Lannoy, Paul J Fletcher, Linda A Parker, Neil J MacLusky, Laura C Sullivan, Teresa A Chavera, Kelly A Berg
Lorcaserin (LOR) is a selective 5-HT2C receptor agonist that has been FDA approved as a treatment for obesity. The most frequently reported side-effects of LOR include nausea and headache, which can be dose limiting. We have previously reported that in the rat, while LOR produced unconditioned signs characteristic of nausea/malaise, the highly selective 5-HT2C agonist CP-809101 (CP) produced fewer equivalent signs. Because this may indicate a subclass of 5-HT2C agonists having better tolerability, the present studies were designed to further investigate this apparent difference...
March 24, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28336575/pharmacologic-profile-of-naloxegol-a-peripherally-acting-%C3%A2%C2%B5-opioid-receptor-antagonist-for-the-treatment-of-opioid-induced-constipation
#13
Eike Floettmann, Khanh Bui, Mark Sostek, Kemal Payza, Michael Eldon
Opioid-induced constipation (OIC) is a common side effect of opioid pharmacotherapy for the management of pain because opioid agonists bind to µ-opioid receptors in the enteric nervous system (ENS). Naloxegol, a polyethylene glycol derivative of naloxone and a peripherally acting µ-opioid receptor antagonist, targets the physiologic mechanisms that cause OIC. Pharmacologic measures of opioid activity and pharmacokinetic measures of central nervous system (CNS) penetration were employed to characterize the mechanism of action of naloxegol...
March 23, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28336491/neurobehavioral-effects-of-lithium-in-the-rat-investigation-of-the-effect-concentration-relationships-and-the-contribution-of-the-poisoning-pattern
#14
Anne-Sophie Hanak, Lucie Chevillard, Rodolphe Lebeau, Patricia Risède, Jean-Louis Laplanche, Nadia Benturquia, Bruno Mégarbane
Severity of lithium poisoning depends on the ingested dose, previous treatment duration and renal function. No animal study has investigated neurobehavioral differences in relation to the lithium poisoning pattern observed in humans, while differences in lithium pharmacokinetics have been reported in lithium-pretreated rats mimicking chronic poisonings with enhanced brain accumulation in rats with renal failure. Our objectives were: 1)-to investigate lithium-related effects in overdose on locomotor activity, anxiety-like behavior, spatial recognition memory and anhedonia in the rat; 2)-to model the relationships between lithium-induced effects on locomotion and plasma, erythrocyte, cerebrospinal fluid and brain concentrations previously obtained according to the poisoning pattern...
March 20, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28330377/enhanced-oral-bioavailability-and-sustained-delivery-of-glimepiride-via-niosomal-encapsulation-in-vitro-characterization-and-in-vivo-evaluation
#15
Amira Mohamed Mohsen, Mona Mahmoud AbouSamra, Shaimaa Ahmed ElShebiney
This study was designed to investigate the potency of niosomes, for glimepiride (GLM) encapsulation, aiming at enhancing its oral bioavailability and hypoglycemic efficacy. Niosomes containing non-ionic surfactants (NIS) were prepared by thin film hydration technique and characterized. In-vitro release study was performed using a dialysis technique. In-vivo pharmacodynamic studies, as well as pharmacokinetic evaluation were performed on alloxan induced diabetic rats. GLM niosomes exhibited high entrapment efficiency percentages (E...
March 23, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28329443/analyzing-the-potential-root-causes-of-variability-of-pharmacokinetics-in-preclinical-species
#16
Pierre Daublain, Kung-I Feng, Michael D Altman, Iain Martin, Suman Mukherjee, Rebecca Nofsinger, Alan B Northrup, Richard Tschirret-Guth, Mark Cartwright, Caroline McGregor
The purpose of this research was to assess variability in pharmacokinetic profiles (PK variability) in preclinical species and identify the risk factors associated with the properties of a drug molecule that contribute to the variability. Exposure data in mouse, rat, dog and monkey for a total of 16,592 research compounds studied between 1999 and 2013 were included in the analysis. Both in vivo study parameters and in silico/experimental physicochemical properties of the molecules were analyzed. Areas under the plasma concentration vs...
March 22, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28327191/real-time-in-vivo-monitoring-of-magnetic-nanoparticles-in-the-bloodstream-by-ac-biosusceptometry
#17
André G Próspero, Caio C Quini, Andris F Bakuzis, Patrícia Fidelis-de-Oliveira, Gustavo M Moretto, Fábio P F Mello, Marcos F F Calabresi, Ronaldo V R Matos, Ednaldo A Zandoná, Nícholas Zufelato, Ricardo B Oliveira, José R A Miranda
BACKGROUND: We introduce and demonstrate that the AC biosusceptometry (ACB) technique enables real-time monitoring of magnetic nanoparticles (MNPs) in the bloodstream. We present an ACB system as a simple, portable, versatile, non-invasive, and accessible tool to study pharmacokinetic parameters of MNPs, such as circulation time, in real time. We synthesized and monitored manganese doped iron oxide nanoparticles in the bloodstream of Wistar rats using two different injection protocols...
March 21, 2017: Journal of Nanobiotechnology
https://www.readbyqxmd.com/read/28324691/comparison-of-three-different-types-of-cilostazol-loaded-solid-dispersion-physicochemical-characterization-and-pharmacokinetics-in-rats
#18
Omer Mustapha, Kyung Soo Kim, Shumaila Shafique, Dong Shik Kim, Sung Giu Jin, Youn Gee Seo, Yu Seok Youn, Kyung Taek Oh, Chul Soon Yong, Jong Oh Kim, Han-Gon Choi
The aim of this research was to compare three different types of cilostazol-loaded solid dispersion system including solvent-evaporated, solvent-wetted and surface-attached solid dispersion. The effect of polymers and surfactants on the aqueous solubility of cilostazol was investigated, leading to the selection of polyvinylpyrrolidone (PVP) and sodium lauryl sulphate (SLS). Employing a spray-drying technique, numerous surface-attached, solvent-evaporated and solvent-wetted solid dispersions were prepared with various amounts PVP and SLS using water, 90% ethanol and acetone, respectively...
March 9, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28323117/absorption-metabolism-and-excretion-of-the-glp-1-analogue-semaglutide-in-humans-and-nonclinical-species
#19
Lene Jensen, Hans Helleberg, Ad Roffel, Jan Jaap van Lier, Inga Bjørnsdottir, Palle Jacob Pedersen, Everton Rowe, Julie Derving Karsbøl, Mette Lund Pedersen
Semaglutide is a human glucagon-like peptide-1 analogue in clinical development for the treatment of type 2 diabetes. The absorption, metabolism and excretion of a single 0.5mg/450μCi [16.7MBq] subcutaneous dose of [(3)H]-radiolabelled semaglutide was investigated in healthy human subjects and compared with data from nonclinical studies. Radioactivity in blood, plasma, urine and faeces was determined in humans, rats and monkeys; radioactivity in expired air was determined in humans and rats. Metabolites in plasma, urine and faeces were quantified following profiling and radiodetection...
March 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28322896/pharmacokinetics-of-opicapone-a-third-generation-comt-inhibitor-after-single-and-multiple-oral-administration-a-comparative-study-in-the-rat
#20
Daniela Gonçalves, Gilberto Alves, Ana Fortuna, Patrício Soares-da-Silva, Amílcar Falcão
Opicapone is a novel potent, reversible and purely peripheral catechol-O-methyltransferase inhibitor that has been developed to be used as an adjunct to levodopa/aromatic L-amino acid decarboxylase inhibitor therapy for Parkinson's disease. Thus, this study aimed to compare the plasma pharmacokinetics of opicapone and its active metabolite (BIA 9-1079) after the administration of single and multiple oral doses to rats. Wistar rats (n=8 per group) were orally treated with single (30, 60 or 90mg/kg) or multiple (30mg/kg once-daily for seven consecutive days) oral doses of opicapone...
March 16, 2017: Toxicology and Applied Pharmacology
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