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pharmacokinetics, rat

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https://www.readbyqxmd.com/read/28640646/an-enzyme-linked-immunosorbent-assay-for-monoester-type-aconitic-alkaloids-and-its-application-in-the-pharmacokinetic-study-of-benzoylhypaconine-in-rats
#1
Can-Can Liu, Yun-Hui Xu, Shuai Yuan, Yu Xu, Mo-Li Hua
A new enzyme-linked immunosorbent assay (ELISA) method for quantitative determination of monoester-type aconitic alkaloids was developed. The antibodies derived from the immunogen of benzoylmesaconine (BM) could be electively affined to benzoylaconitine-type alkaloids with an ester bond (14-benzoyl-), especially to benzoylhypaconine (BH, 140.02% of cross-reactivity). The effective working range of BH was 1 ng/ml to 5 μg/ml; the lower limit of detection and the quantification were 0.35 and 0.97 ng/ml, respectively...
June 22, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28636885/differential-changes-in-the-pharmacokinetics-of-statins-in-collagen-induced-arthritis-rats
#2
Chun-Han Lin, Ke-Wei Hsu, Chia-Hao Chen, Yow-Shieng Uang, Chun-Jung Lin
The elevated systemic levels of cytokines in rheumatoid arthritis (RA) can change the expression of metabolic enzymes and transporters. Given that statins are lipid-lowering agents frequently used in RA patients with concurrent cardiovascular diseases, the objective of the present study was to investigate the impacts of RA on the pharmacokinetics of statins of different disposition properties in rats with collagen-induced arthritis (CIA). The expression of metabolic enzymes and transporters in tissues of CIA rats were analyzed by RT-qPCR...
June 18, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28636139/review-of-hplc-and-lc-ms-ms-assays-for-the-determination-of-various-non-steroidal-anti-androgens-nsaa-used-in-the-treatment-of-prostate-cancer
#3
REVIEW
P S Suresh, Nuggehally R Srinivas, Ramesh Mullangi
Prostate cancer is the most common cancer and one of the leading causes for cancer deaths in men. One of the commonly used approaches to treat metastatic prostate cancer was via first generation non-steroidal anti-androgens (NSAA) namely flutamide, nilutamide, bicalutamide and topilutamide. Most of the prostate cancer patients who are initially responsive develop a most aggressive form of disease called castration-resistant prostate cancer (CRPC). Second generation NSAA receptor antagonists (enzalutamide, apalutamide and darolutamide) are emerging as additional new options to treat CRPC...
June 21, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28635296/benzoxaborole-antimalarial-agents-part-5-lead-optimization-of-novel-amide-pyrazinyloxy-benzoxaboroles-and-identification-of-a-preclinical-candidate
#4
Yong-Kang Zhang, Jacob J Plattner, Eric E Easom, Robert Toms Jacobs, Denghui Guo, Yvonne R Freund, Pamela Berry, Vic Ciaravino, John C L Erve, Philip J Rosenthal, Brice Campo, Francisco-Javier Gamo, Laura M Sanz, Jianxin Cao
Carboxamide pyrazinyloxy benzoxaboroles were investigated with the goal to identify a molecule with satisfactory antimalarial activity, physicochemical properties, pharmacokinetic profile, in vivo efficacy, and safety profile. This optimization effort discovered 46, which met our target candidate profile. Compound 46 had excellent activity against cultured Plasmodium falciparum, and in vivo against P. falciparum and P. berghei in infected mice. It exhibited good PK properties in mouse, rat and dog. It was highly active against other eleven P...
June 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28633598/metabolism-of-inhaled-methylethylketone-in-rats
#5
Frédéric Cosnier, Stéphane Grossmann, Hervé Nunge, Céline Brochard, Samuel Muller, Anne-Marie Lambert-Xolin, Sylvie Sebillaud, Benoît Rieger, Aurélie Thomas, Marie-Josèphe Décret, Manuella Burgart, Laurent Gaté, Benoît Cossec, Pierre Campo
Methylethylketone (MEK) is widely used in industry, often in combination with other compounds. Although nontoxic, it can make other chemicals harmful. This study investigates the fate of MEK in rat blood, brain and urine as well as its hepatic metabolism following inhalation over 1 month (at 20, 200 or 1400 ppm). MEK did not significantly accumulate in the organism: blood concentrations were similar after six-hour or 1-month inhalation periods, and brain concentrations only increased slightly after 1 month's exposure...
February 28, 2017: Drug and Chemical Toxicology
https://www.readbyqxmd.com/read/28631076/effects-of-glycyrrhizic-acid-on-the-pharmacokinetics-of-pristimerin-in-rats-and-its-potential-mechanism
#6
Xiufen Zhao, Yan Wu, Dongmei Wang
BACKGROUND AND OBJECTIVES: Pristimerin has been reported to possess a wide range of pharmacological activities. This study investigates the effects of glycyrrhizic acid on the pharmacokinetics of pristimerin in rats. METHODS: The pharmacokinetics of orally administered pristimerin (2 mg/kg) with or without glycyrrhizic acid pretreatment (at a dose of 100 mg/kg/day for 7 days) were investigated. The plasma concentration of pristimerin was determined using a sensitive and reliable LC-MS/MS method, and the pharmacokinetics profiles were calculated and compared...
June 19, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28630216/fractionated-dosing-improves-preclinical-therapeutic-index-of-pyrrolobenzodiazepine-containing-antibody-drug-conjugates
#7
Mary Jane Hinrichs, Pauline M Ryan, Bo Zheng, Shameen Afif-Rider, Xiang-Qing Yu, Michele Gunsior, Haihong Zhong, Jay Harper, Binyam Bezabeh, Kapil Vashisht, Marlon Rebelatto, Molly Reed, Patricia C Ryan, Shannon Breen, Neki Patel, Cui Chen, Luke A Masterson, Arnaud Tiberghien, Philip W Howard, Nazzareno Dimasi, Rakesh Dixit
                Purpose:  To use preclinical models to identify a dosing schedule that improves tolerability of highly potent pyrrolobenzodiazepine dimers (PBD) antibody drug conjugates (ADCs) without compromising anti-tumor activity.  <p>                Experimental design:   A series of dose-fractionation studies were conducted to investigate the pharmacokinetic drivers of safety and efficacy of PBD ADCs in animal models.  The exposure-activity relationship was investigated in mouse xenograft models of human prostate cancer, breast and gastric cancer by comparing anti-tumor activity after single and fractionated dosing with tumor-targeting ADCs conjugated to SG3249, a potent PBD dimer...
June 19, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28630178/efficacy-of-cefiderocol-against-carbapenem-resistant-gram-negative-bacilli-in-immunocompetent-rat-respiratory-tract-infection-models-recreating-human-plasma-pharmacokinetics
#8
Shuhei Matsumoto, Christine M Singley, Jennifer Hoover, Rio Nakamura, Roger Echols, Stephen Rittenhouse, Masakatsu Tsuji, Yoshinori Yamano
Cefiderocol (S-649266), a novel siderophore cephalosporin, shows potent activity against carbapenem-resistant Gram-negative bacilli. In this study, we evaluated the efficacy of cefiderocol against carbapenem-resistant Gram-negative bacilli (Pseudomonas aeruginosa,Acinetobacter baumannii and Klebsiella pneumoniae) in immunocompetent rat respiratory tract infection models recreating plasma pharmacokinetics (PK) profiles in healthy human subjects. A total of 6 clinical isolates (1 cephalosporin-susceptible P. aeruginosa, 1 multidrug-resistant P...
June 19, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28629804/zero-order-controlled-release-delivery-of-cholecalciferol-from-injectable-biodegradable-microsphere-in-vitro-characterization-and-in-vivo-pharmacokinetic-studies
#9
Lalit Vora, Sita V G, Pradeep Vavia
Poly(lactic-co-glycolic acid) microspheres loaded with cholecalciferol (CL), more bioactive form of vitamin D was developed as an injectable controlled drug release system and was evaluated for its feasibility of once a month delivery. The CL loaded microspheres (CL-MS) were prepared by simple oil in water (O/W) emulsion-solvent evaporation technique incorporated with a stabilizer, Tocopherol Succinate (TS). Different formulation as well as process parameters were investigated namely concentration of emulsifier, concentration of stabilizer and drug: polymer mass ratios...
June 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28628923/cremophor-el-alters-the-plasma-protein-binding-and-pharmacokinetic-profile-of-valspodar-in-rats
#10
Ziyad Binkhathlan
Cremophor EL is a nonionic surfactant widely used in pharmaceutical formulations. Nonetheless, there are several reports on the influence of this excipient on the protein binding, pharmacokinetics, and pharmacodynamics of drugs. Valspodar is an investigational non-immunosuppressive derivative of cyclosporine A, used in clinical trials for treatment of multidrug resistant tumors. The formulation of valspodar (Amdray(®)) contains cremophor EL and ethanol as solubilizing agents. The main aim of the current study was to assess the plasma protein binding (in vitro) and the pharmacokinetic profile of valspodar in the cremophor EL-based formulation in comparison to a cremophor EL-free formulation following intravenous (i...
June 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28628838/validated-uplc-ms-ms-method-for-simultaneous-quantification-of-eight-saikosaponins-in-rat-plasma-application-to-a-comparative-pharmacokinetic-study-in-depression-rats-after-oral-administration-of-extracts-of-raw-and-vinegar-baked-bupleuri-radix
#11
Tianli Lei, Dandan Zhang, Kun Guo, Mingxiao Li, Chongning Lv, Jing Wang, Lingyun Jia, Jincai Lu
A sensitive and efficient UPLC-MS/MS method was developed and validated for simultaneous quantification of eight saikosaponins (SSa, SSb1, SSb2, SSb3, SSb4, SSc, SSd and SSf) in rat plasma. Furthermore, comparative pharmacokinetic profiles of these sakosaponins were investigated, following oral administration of extracts of raw and vinegar-baked Bupleuri Radix to depression rats. Biosamples were processed with liquid-liquid extraction technique using ethyl acetate. Chromatographic separation was accomplished on Waters BEH C18 UPLC column...
June 16, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28628837/the-influence-of-essential-oils-from-xiang-fu-si-wu-decoction-on-its-non-volatile-components-and-its-application-for-pharmacokinetics-in-normal-rats
#12
Ying Pan, Dawei Qian, Pei Liu, Yang Zhang, Zhenhua Zhu, Li Zhang, Jin-Ao Duan
Xiang-Fu-Si-Wu Decoction (XFSWD) has been used to treat gynecology diseases in clinical practice for hundreds of years in China, especially for primary dysmenorrheal of QiZhi Type. In previous researches, both essential oils (XEO) and non-volatile components (NXEO) extracted from XFSWD showed significant pharmacological activities, but the influence of XEO on NXEO was unclear. The purpose of this paper was to develop a validated analytical method for simultaneous determination of ten components including Vanillic acid, Ferulic acid, Caffeic acid, Gallic acid, Paeoniflorin, Albiflorin, Tetrahydropalmatine, Protopine, Berberine and Tetrahydrocolumbamine, and to compare the pharmacokinetic parameters of these components to illustrate the influences of XEO on NXEO in normal rats...
June 4, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28627167/plasma-pharmacokinetics-bioavailability-and-tissue-distribution-of-four-c-glycosyl-flavones-from-mung-bean-vigna-radiata-l-seeds-extracts-in-rat-by-uhplc-ms-ms
#13
Yan Bai, Qili Zhang, Baoyu Wang, Meiyan Zhang, Yan Xu, Shasha Li, Yunli Zhao, Zhiguo Yu
The main polyphenols in mung bean (Vigna radiata L.) seeds (MBS), an edible legume with various biological activities, are C-glycosyl flavones (vitexin, isovitexin, isovitexin-6''-O-α-L-glucoside, and dulcinoside). In our study, a validated UHPLC-MS/MS method was developed to quantitate the concentrations of four C-glycosyl flavones from MBS extracts in the plasma and various tissues of rats, and successfully applied to study their pharmacological profile and tissue distribution in vivo. Four C-glycosyl flavones were rapidly absorbed after oral administration, achieving a Cmax at around 1...
June 19, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28626996/vortex-ultrasound-assisted-dispersive-liquid-liquid-microextraction-coupled-with-gc-ms-for-the-analysis-of-volatile-bioactive-components-and-comparative-pharmacokinetic-study-of-the-herb-herb-interactions-in-guanxin-shutong-capsule
#14
Jingqing Mu, Xun Gao, Qing Li, Xiaomei Yang, Wenling Yang, Xu Sun, Kaishun Bi, Huifen Zhang
Guanxin Shutong Capsule, an effective traditional Chinese medicine, is widely used for coronary heart disease clinically. Volatile components are one of its important bioactive constituents. To better understand the material basis for the therapeutic effects, the components of Guanxin Shutong Capsule absorbed into the blood and their metabolites were identified based on gas chromatography with mass spectrometry coupled with vortex-ultrasound-assisted dispersive liquid-liquid microextraction. As a result, three prototypes and 15 metabolites were identified or tentatively characterized in rat plasma...
June 19, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28626475/stereospecific-pharmacokinetic-characterization-of-liquiritigenin-in-the-rat
#15
Samaa Alrushaid, Neal M Davies, Stephanie E Martinez, Casey L Sayre
Liquiritigenin is a chiral flavonoid present in licorice and other medicinal plants. The nature of its biological fate with respect to the individual enantiomers has not been examined. In this study, we characterize, for the first time, the stereoselective pharmacokinetics of liquiritigenin. Liquiritigenin was intravenously (20 mg/kg) and orally (50 mg/kg) administered to male Sprague-Dawley rats (n = 4 per route of administration). Concentrations in serum and urine were characterized via stereospecific reversed-phase, isocratic HPLC method with UV detection...
June 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28623874/lansoprazole-sulphide-pharmacokinetics-of-this-promising-anti-tuberculous-agent
#16
Sipho Mdanda, Sooraj Baijnath, Adeola Shobo, Sanil D Singh, Glenn E M Maguire, Hendrik G Kruger, Per I Arvidsson, Tricia Naicker, Thavendran Govender
Lansoprazole (LPZ) is a commercially available proton-pump inhibitor (PPI) whose primary metabolite, lansoprazole sulphide (LPZS) was recently reported to have in vitro and in vivo activity against M. tb. It was also reported that a 300 mg kg(-1) oral administration of LPZS was necessary to reach therapeutic levels in the lung, with the equivalent human dose being unrealistic. A validated liquid chromatography-tandem mass spectrometric method (LC-MS/MS) for the simultaneous quantification LPZ and LPZS in rat plasma and lung homogenates, was developed...
June 17, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28623851/quantification-of-%C3%AE-eudesmol-in-rat-plasma-using-lc-ms-ms-and-its-application-to-a-pharmacokinetic-study
#17
Ligang Jiang, Chunyang Zhang, Haiping Li
A sensitive and specific LC-MS/MS assay for determination of β-eudesmol in rat plasma was developed and validated. After liquid-liquid extraction with ethyl ether, the analyte and IS were separated on a Capcell Pak C18 column (50 × 2.0 mm, 5 μm) by isocratic elution with acetonitrile-water-formic acid (77.5:22.5:0.1, v/v/v) as the mobile phase at a flow rate of 0.4 mL/min. An ESI source was applied and operated in positive ion mode; selected reaction monitoring (SRM) scan was used for quantification by monitoring the precursor-product ion transitions of m/z 245...
June 17, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28623364/distribution-and-kinetics-of-the-kv1-3-blocking-peptide-hstx1-r14a-in-experimental-rats
#18
Ralf Bergmann, Manja Kubeil, Kristof Zarschler, Sandeep Chhabra, Rajeev B Tajhya, Christine Beeton, Michael W Pennington, Michael Bachmann, Raymond S Norton, Holger Stephan
The peptide HsTX1[R14A] is a potent and selective blocker of the voltage-gated potassium channel Kv1.3, which is a highly promising target for the treatment of autoimmune diseases and other conditions. In order to assess the biodistribution of this peptide, it was conjugated with NOTA and radiolabelled with copper-64. [(64)Cu]Cu-NOTA-HsTX1[R14A] was synthesised in high radiochemical purity and yield. The radiotracer was evaluated in vitro and in vivo. The biodistribution and PET studies after intravenous and subcutaneous injections showed similar patterns and kinetics...
June 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28623171/broad-analgesic-activity-of-a-novel-selective-m1-agonist
#19
Michael W Wood, Giovanni Martino, Martin Coupal, Mattias Lindberg, Patricia Schroeder, S Santhakumar, Manon Valiquette, Johan Sandin, Daniel Widzowski, Jennifer Laird
Although the muscarinic receptor family has long been a source of potentially compelling targets for small molecule drug discovery, it was difficult to achieve agonist selectivity within the family. A new class of M1 muscarinic agonists has emerged, and these compounds have been characterized as agonists that activate the receptor at an allosteric site. Members of this class of M1 agonists have been shown to be selective across the muscarinic receptors. However, upon introduction of a novel pharmacologic mechanism, it is prudent to ensure that no new off-target activities have arisen, particularly within the context of in vivo experiments...
June 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28622708/pharmacokinetic-comparison-of-two-phenolic-acids-after-oral-administration-of-typhae-pollen-to-normal-rats-and-rats-with-acute-cold-blood-stasis
#20
Yingni Pan, Wenjie Zhang, Wei Zhang, Xuewei Bai, Shumeng Ren, Jiang Zheng, Dongmei Wang, Xiaoqiu Liu
Typhae Pollen (TP), dried pollen of Typha angustifolia L., Typha orientalis Presl or other plants of the same genus (Typhaeceae), has effect of activating the circulation to cure blood stasis in traditional Chinese Medicine (TCM). The purpose of this study was to set up an ultra-high performance liquid chromatography method that could determine p-hydroxybenzoic acid and vanillic acid simultaneously in rat plasma, and to compare their pharmacokinetics in normal rats and rats with acute cold blood stasis, and further to investigate the influence of different dosages of oral administration...
June 16, 2017: Biomedical Chromatography: BMC
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