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https://www.readbyqxmd.com/read/29145001/in-vitro-and-in-vivo-evaluation-of-10-hydroxycamptothecin-loaded-poly-n-butyl-cyanoacrylate-nanoparticles-prepared-by-miniemulsion-polymerization
#1
Xin Jin, Sajid Asghar, Xieting Zhu, Zhipeng Chen, Cihui Tian, Lining Yin, Qineng Ping, Yanyu Xiao
In this paper, 10-hydroxycamptothecin (HCPT)-loaded poly (n-butyl cyanoacrylate) nanoparticles (HCPT-PBCA-NPs) co-modified with polysorbate 80, soybean phospholipids, and polyethylene glycol (100) monostearate were successfully prepared via miniemulsion polymerization, and were characterized for particle size, morphology, zeta potential, encapsulation efficiency (EE) and drug loading capacity (DL). The chemical structure of HCPT-PBCA-NPs and the state of HCPT in the PBCA-NPs were investigated by DSC, FTIR and (1)H NMR...
November 12, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29143972/determination-of-tubuloside-b-by-lc-ms-ms-and-its-application-to-a-pharmacokinetic-study-in-rats
#2
Shenbao Yang, Ruiying Qu, Peilu Sun, Shan Xiong, Siyi Yan, Zhipeng Deng
Tubuloside B, a novel neuroprotective phenylethanoid, is a major active constituent of Cistanche tubulosa and Cistanche deserticola. A specific and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the quantification of tubuloside B in rat plasma. Sample preparation was conducted through a protein-precipitation extraction with methanol using tubuloside A as internal standard (IS). Chromatographic separation was achieved by using a Capcell Pak C18 column (2...
November 16, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29143853/sex-specific-risk-assessment-of-pfhxs-using-a-physiologically-based-pharmacokinetic-model
#3
Sook-Jin Kim, Hwajin Shin, Yong-Bok Lee, Hea-Young Cho
Perfluorohexanesulfonate (PFHxS), which belongs to the group of perfluoroalkyl and polyfluoroalkyl substances (PFASs), has been extensively used in industry and subsequently detected in the environment. Its use may be problematic, as PFHxS is known to induce neuronal cell death, and has been associated with early onset menopause in women and with attention deficit/hyperactivity disorder. Due to these impending issues, the aim of this study is to develop and evaluate a physiologically based pharmacokinetic (PBPK) model for PFHxS in male and female rats, and apply this to a human health risk assessment...
November 16, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29143757/simultaneous-determination-of-seven-anthraquinone-aglycones-of-crude-and-processed-semen-cassiae-extracts-in-rat-plasma-by-uplc-ms-ms-and-its-application-to-a-comparative-pharmacokinetic-study
#4
Rixin Guo, Hongwei Wu, Xiankuo Yu, Mengying Xu, Xiao Zhang, Liying Tang, Zhuju Wang
Semen cassiae is the ripe seed of Cassia obtusifolia L. or Cassia tora L. of the family Leguminosae. In traditional Chinese medicine, the two forms of Semen cassiae are raw Semen cassiae (R-SC) and parched Semen cassiae (P-SC). To clarify the processing mechanism of Semen cassiae, the pharmacokinetics of R-SC and P-SC extracts were examined. A simple, rapid, sensitive ultra-high-performance liquid chromatography-tandem mass spectroscopy (UPLC-MS/MS) method was developed and validated for the simultaneous determination of seven anthraquinone aglycones of Semen cassiae (aurantio-obtusin, obtusifolin, questin, 2-hydroxyemodin-1-methyl-ether, rhein, emodin, 1,2,7-trimethoxyl-6,8-dihydroxy-3-methylanthraquinone) to compare the pharmacokinetics of raw and parched Semen cassiae in rat plasma...
October 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29138563/squarticles-as-the-nanoantidotes-to-sequester-the-overdosed-antidepressant-for-detoxification
#5
Chun-Han Chen, Tse-Hung Huang, Ahmed O Elzoghby, Pei-Wen Wang, Chia-Wen Chang, Jia-You Fang
The increasing death rate caused by drug overdose points to an urgent demand for the development of novel detoxification therapy. In an attempt to detoxify tricyclic antidepressant overdose, we prepared a lipid nanoemulsion, called squarticles, as the nanoantidote. Squalene was the major lipid matrix of the squarticles. Here, we present the animal study to investigate both the pharmacokinetic and pharmacodynamic effects of squarticles on amitriptyline intoxication. The anionic and cationic squarticles had average diameters of 97 and 122 nm, respectively...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29135439/biological-cleavage-of-the-c-p-bond-in-perfluoroalkyl-phosphinic-acids-in-male-sprague-dawley-rats-and-the-formation-of-persistent-and-reactive-metabolites
#6
Shira Joudan, Leo W Y Yeung, Scott A Mabury
BACKGROUND: Perfluoroalkyl phosphinic acids (PFPiAs) have been detected in humans, wildlife, and various environmental matrices. These compounds have been used with perfluoroalkyl phosphonic acids (PFPAs) as surfactants in consumer products and as nonfoaming additives in pesticide formulations. Unlike the structurally related perfluoroalkyl sulfonic and carboxylic acids, little is known about the biological fate of PFPiAs. OBJECTIVES: We determined the biotransformation products of PFPiAs and some pharmacokinetic parameters in a rat model...
November 3, 2017: Environmental Health Perspectives
https://www.readbyqxmd.com/read/29134775/changes-in-sensitivity-to-the-effects-of-atrazine-on-the-luteinizing-hormone-surge-in-female-sprague-dawley-rats-after-repeated-daily-doses-correlation-with-liver-enzyme-expression
#7
Charles B Breckenridge, Chad D Foradori, Pragati Sawhney Coder, James W Simpkins, Robert L Sielken, Robert J Handa
BACKGROUND: Atrazine suppression of the LH surge slowly develops over time and peaks after 4 days; sensitivity to atrazine decreases after 8 or 14 days of dosing. Adaptation of the LH response was correlated with increased phase I and phase II liver enzyme activity/expression. METHODS: The effect of atrazine on the LH surge was evaluated in female Sprague-Dawley rats administered 100 mg/kg/day atrazine by gavage for 1, 2, 3, or 4 consecutive days or 6.5, 50, or 100 mg/kg/day atrazine for 4, 8, or 14 days...
November 14, 2017: Birth defects research
https://www.readbyqxmd.com/read/29134502/the-influence-of-compatibility-of-rhubarb-and-radix-scutellariae-on-the-pharmacokinetics-of-anthraquinones-and-flavonoids-in-rat-plasma
#8
Yaqing Zhang, Zunjian Zhang, Rui Song
BACKGROUND AND OBJECTIVES: Rhubarb-Radix scutellariae is a classic herb pair, which is commonly used to clear away heat and toxin in clinic. The aim of this study was to investigate the influence of compatibility of Rhubarb and Radix scutellariae on the pharmacokinetic behaviors of anthraquinones and flavonoids in rat plasma. METHODS: Eighteen rats were randomly divided into three groups, and were orally administered Rhubarb and/or Radix scutellariae extracts. A sensitive and rapid UPLC-MS/MS method was developed and validated to determine the concentrations of baicalin, baicalein, wogonside, wogonin, rhein, and emodin in rat plasma...
November 14, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29134244/modulation-of-cyp3a-enzyme-activity-by-diosmin-and-its-consequence-on-carbamazepine-pharmacokinetics-in-rats
#9
Satish Kumar Bedada, Prasad Neerati
Diosmin is a widely used flavonoid for the treatment of varicose veins and hemorrhoids. Epileptic patients with hemorrhoids and varicose veins may use diosmin along with carbamazepine (CBZ) therapy, which leads to pharmacokinetic interaction between diosmin and CBZ. Therefore, the present study was performed to evaluate the effect of diosmin on the pharmacokinetics of CBZ in rats. Diosmin-mediated altered CYP3A enzyme activity in human and rat liver microsomes was examined using CYP3A dependent erythromycin N-demethylase assay...
November 14, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29133240/prediction-of-human-cns-pharmacokinetics-using-a-physiologically-based-pharmacokinetic-modeling-approach
#10
Yumi Yamamoto, Pyry A Välitalo, Yin Cheong Wong, Dymphy R Huntjens, Johannes H Proost, An Vermeulen, Walter Krauwinkel, Margot W Beukers, Hannu Kokki, Merja Kokki, Meindert Danhof, Johan G C van Hasselt, Elizabeth C M de Lange
Knowledge of drug concentration-time profiles at the central nervous system (CNS) target-site is critically important for rational development of CNS targeted drugs. Our aim was to translate a recently published comprehensive CNS physiologically-based pharmacokinetic (PBPK) model from rat to human, and to predict drug concentration-time profiles in multiple CNS compartments on available human data of four drugs (acetaminophen, oxycodone, morphine and phenytoin). Values of the system-specific parameters in the rat CNS PBPK model were replaced by corresponding human values...
November 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29133176/effect-of-zonisamide-on-refractory-epilepsy-during-pregnancy-in-lamotrigine-resistant-kindled-rats
#11
Reza Narenji Sani, Keivan Keramati, Niloufar Saberi, Melika Moezifar, Ali Mahdavi
Drug-resistant epilepsy with uncontrolled severe seizures despite state-of-the-art medical treatment continues to be a major clinical problem. Pregnancy is a state where drug pharmacokinetic changes are more pronounced and more rapid than any other period of life. The current study investigated the effect of zonisamide (ZNS) on refractory epilepsy during pregnancy in lamotrigine-resistant kindled rats. Fifty-six lamotrigine (LTG)-resistant kindled Wistar rats were divided into five experimental (four pregnant and one non-pregnant) and 2 positive controls (pregnant and non-pregnant) groups and eight intact Wistar rats were put in the negative pregnant control group...
November 11, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/29131861/delivery-of-epirubicin-via-slow-infusion-as-a-strategy-to-mitigate-chemotherapy-induced-cardiotoxicity
#12
Fang Yang, Qiao Lei, Lu Li, Jian Chang He, Jiajia Zeng, Chunxiang Luo, Sai-Ching Jim Yeung, Runxiang Yang
BACKGROUND: Continuous infusion of doxorubicin has been a strategy to reduce cardiotoxicity. Epirubicin is another anthracycline in common clinical use. However, evidence is lacking regarding whether this strategy can reduce cardiotoxicity of epirubicin without compromising antineoplastic efficacy. DESIGN AND METHODS: Healthy rats were randomized into groups: epirubicin (8 mg/kg) delivered intraperitoneally via micro osmotic pumps (MOP), epirubicin (8 mg/kg) by intraperitoneal (IP) bolus injection, and placebo control...
2017: PloS One
https://www.readbyqxmd.com/read/29131518/metabolic-profile-of-kudiezi-injection-in-rats-by-uhplc-coupled-with-fourier-transform-ion-cyclotron-resonance-mass-spectrometry
#13
Jingdan Zhang, Xiaoxue Zhang, Yangyang Zhao, Aihua Song, Wei Sun, Ran Yin
In this study, a reliable and sensitive ultra high performance liquid chromatography coupled with Fourier transform ion cyclotron resonance mass spectrometry method was developed for the systematic study of the metabolic profile of Kudiezi injection in rat plasma, bile, urine and feces after intravenous administration of a single dose. The chromatographic separation was performed on an Agilent Eclipse Plus C18 column (4.6 mm × 50 mm, 1.8 μm) and the identification of prototype components and metabolites was achieved on a Bruker Solarix 7...
November 13, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/29131376/method-development-for-quantification-of-quizartinib-in-rat-plasma-by-liquid-chromatography-tandem-mass-spectrometry-for-pharmacokinetic-application
#14
Essam Ezzelddin, Muzaffar Iqbal, Gamal Mostafa, Khalid A Al-Rashood, Toqa El Nahhas
Quizartinib is a highly potent inhibitor of the fms-like tyrosine kinase receptor, which is one of the most commonly mutated genes in acute myeloid leukemia (AML). Quizartinib has shown a significant antileukemic clinical influence among relapsed/refractory acute AML patients. This study aimed at developing and validating an analytical method for the measurement of quizartinib in rat plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The method was validated according to FDA guidelines, and the results obtained in this work met the set criteria...
November 13, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29129847/effects-of-ketoconazole-on-cyclophosphamide-metabolism-evaluation-of-cyp3a4-inhibition-effect-using-the-in-vitro-and-in-vivo-models
#15
Le Yang, Chenyang Yan, Feng Zhang, Bo Jiang, Shouhong Gao, Youtian Liang, Lifeng Huang, Wansheng Chen
Cyclophosphamide (CP) is widely used in anticancer therapy regimens and 2-dechloroethylcyclophosphamide (DECP) is its side-chain dechloroethylated metabolite. N-dechloroethylation of CP mediated by the enzyme CYP3A4 yields nephrotoxic and neurotoxic chloroacetaldehyde (CAA) in equimolar amount to DECP. This study aimed to evaluate the inhibitory effect of ketoconazole (KTZ) on CP metabolism through in vitro and in vivo drug-drug interaction (DDI) research. Long-term treatment of KTZ induces hepatic injury; thus single doses of KTZ at low, middle, and high levels (10, 20, and 40 mg/kg) were investigated for pharmacokinetic DDI with CP...
November 13, 2017: Experimental Animals
https://www.readbyqxmd.com/read/29129557/pharmacokinetic-and-behavioural-profile-of-thc-cbd-and-thc-cbd-combination-after-pulmonary-oral-and-subcutaneous-administration-in-rats-and-confirmation-of-conversion-in-vivo-of-cbd-to-thc
#16
Tomáš Hložek, Libor Uttl, Lukáš Kadeřábek, Marie Balíková, Eva Lhotková, Rachel R Horsley, Pavlína Nováková, Klára Šíchová, Kristýna Štefková, Filip Tylš, Martin Kuchař, Tomáš Páleníček
Metabolic and behavioural effects of, and interactions between Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD) are influenced by dose and administration route. Therefore we investigated, in Wistar rats, effects of pulmonary, oral and subcutaneous (sc.) THC, CBD and THC+CBD. Concentrations of THC, its metabolites 11-OH-THC and THC-COOH, and CBD in serum and brain were determined over 24h, locomotor activity (open field) and sensorimotor gating (prepulse inhibition, PPI) were also evaluated. In line with recent knowledge we expected metabolic and behavioural interactions between THC and CBD...
November 9, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29128276/simultaneous-determination-of-saikosaponin-a-paeonol-and-imperatorin-components-of-da-9805-in-rat-plasma-by-lc-ms-ms-and-application-to-a-pharmacokinetic-study
#17
Mi Hye Kwon, Jin Seok Jeong, Jayoung Ryu, Young Woong Cho, Hee Eun Kang
DA-9805 is a new botanical antiparkinson drug candidate formulated using an ethanolic extract of the root of Bupleurum falcatum, the root cortex of Paeonia suffruticosa, and the root of Angelica dahurica. In this study, a sensitive and rapid LC-MS/MS method was developed to simultaneously determine, saikosaponin a, paeonol, and imperatorin, three active/representative ingredients of DA-9805, in rat plasma. Plasma was extracted by mixture of ethyl acetate and methyl tertiary butyl ether. Chromatographic separation was carried out using a C18 column and a gradient elution of mobile phases consisting of 5mM formic acid in water and acetonitrile...
November 4, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29127904/pharmacokinetics-and-brain-uptake-study-of-novel-ampa-receptor-antagonist-perampanel-in-sd-rats-using-a-validated-uhplc-qtof-ms-method
#18
David Paul, Lingesh Allakonda, Amit Sahu, Shruti Surendran, Nanjappan Satheeshkumar
Perampanel (PER) is a novel AMPA receptor antagonist for antiepileptic therapy and is prospective for the treatment of other neurological disorders. A highly sensitive and rapid UHPLC-QTOF-MS method was developed for the quantification of PER in plasma/brain homogenate of SD rat with alogliptin as an internal standard (IS). Chromatographic separation was carried out on an Acquity UPLC HSS Cyano column (100mm×2.1mm, 1.8μm) using gradient mobile phase consisting of 0.1% formic acid and acetonitrile at a flow rate of 0...
November 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29127295/clinical-potential-of-an-enzyme-based-novel-therapy-for-cocaine-overdose
#19
Ting Zhang, Xirong Zheng, Ziyuan Zhou, Xiabin Chen, Zhenyu Jin, Jing Deng, Chang-Guo Zhan, Fang Zheng
It is a grand challenge to develop a truly effective medication for treatment of cocaine overdose. The current available, practical emergence treatment for cocaine overdose includes administration of a benzodiazepine anticonvulsant agent (e.g. diazepam) and/or physical cooling with an aim to relieve the symptoms. The inherent difficulties of antagonizing physiological effects of drugs in the central nervous system have led to exploring protein-based pharmacokinetic approaches using biologics like vaccines, monoclonal antibodies, and enzymes...
November 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29126941/glycol-chitosan-functionalized-asenapine-nanostructured-lipid-carriers-for-targeted-brain-delivery-pharmacokinetic-and-teratogenic-assessment
#20
Sanjay Kumar Singh, Mahendra Kumar Hidau, Shrikant Gautam, Kiran Gupta, Krishna Pal Singh, Shio Kumar Singh, Sanjay Singh
Blood brain barrier (BBB) is a complex, tight barrier between endothelial cells of cerebral blood vessels. It acts as a physical barrier and provides access to only those moieties which are necessary for proper brain functioning. However, this selective prudence also acts as a hindrance in therapeutic targeting of brain necessitating pharmaceutical intervention. Intranasal drug delivery is one such approach which we have exploited here for targeted brain delivery of asenapine via glycol chitosan coated nanostructured lipid carrier (GC-ANLC)...
November 7, 2017: International Journal of Biological Macromolecules
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