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https://www.readbyqxmd.com/read/28524914/bioavailability-of-the-ferulic-acid-derived-phenolic-compounds-of-a-rice-bran-enzymatic-extract-and-their-activity-against-superoxide-production
#1
Cristina Perez-Ternero, Alba Macià, Maria Alvarez de Sotomayor, Juan Parrado, Maria-Jose Motilva, Maria-Dolores Herrera
Rice bran is an exceptional source of such antioxidant molecules as γ-oryzanol and ferulic acid, but their bioavailability and metabolism within this matrix remain unknown. The aims of this work were to describe the oral bioavailability and metabolic pathways of the ferulic acid-derived phenolic compounds contained in a rice bran enzymatic extract (RBEE), and to determine its effect on NADPH oxidase activity. Wistar rats were administered with RBEE and sacrificed at different times over a period of 24 h to obtain plasma...
May 19, 2017: Food & Function
https://www.readbyqxmd.com/read/28521597/determination-of-cepharanthine-in-rat-plasma-by-lc-ms-ms-and-its-application-to-a-pharmacokinetic-study
#2
Yingbin Deng, Weijun Wu, Sunzhi Ye, Wei Wang, Zhiyi Wang
CONTEXT: Cepharanthine (CPA) has been reported to possess a wide range of pharmacological activities. OBJECTIVE: This study investigates the pharmacokinetic characteristics after oral or intravenous administration of CPA by using a sensitive and rapid LC-MS/MS method. MATERIALS AND METHODS: A sensitive and rapid LC-MS/MS method was developed for the determination of CPA in Sprague-Dawley rat plasma. Twelve rats were equally randomized into two groups, including the intravenous group (1 mg/kg) and the oral group (10 mg/kg)...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28516478/determination-of-oral-bioavailability-of-curcuminoid-dispersions-and-nanoemulsions-prepared-from-curcuma-longa-linnaeus
#3
P S Lu, B S Inbaraj, B H Chen
BACKGROUND: Curcuminoid from Curcuma longa Linnaeus has been demonstrated to be effective in anti-cancer and anti-inflammation. The objectives of this study were to prepare curcuminoid dispersion and nanoemulsion from C. longa and determine their oral bioavailability in rats. RESULTS: After curcuminoid extraction using 99.5% ethanol, bisdemethoxycurcumin (BDMC), demethoxycurcumin (DMC) and curcumin were separated within 10 min by HPLC with an Eclipse XDB-C18 column and a gradient mobile phase of 0...
May 18, 2017: Journal of the Science of Food and Agriculture
https://www.readbyqxmd.com/read/28513568/using-uplc-ms-ms-for-characterization-of-active-components-in-extracts-of-yupingfeng-and-application-to-a-comparative-pharmacokinetic-study-in-rat-plasma-after-oral-administration
#4
Meng-Qi Jia, Ye-Juan Xiong, Yun Xue, Yan Wang, Chao Yan
Yupingfeng (YPF), a famous traditional Chinese medicine, which contains a large array of compounds, has been effectually used in health protection. A two-dimensional liquid chromatography (²D-LC) combined with quadrupole time-of-flight mass spectrometry (QTOF-MS) method was firstly established to separate and identify chemical components in YPF. A total of 33 compounds were identified, including 15 constituents (flavonoids and saponins) in Astragali radix; seven constituents (sesquiterpenoids and polysaccharide) in Atractylodis rhizoma; and 11 constituents (chromone and coumarins) in Saposhnikoviae radix...
May 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28511864/metabolism-and-disposition-of-14-c-methycyclosiloxanes-in-rats
#5
Jeanne Y Domoradzki, Christopher M Sushynski, Jacob M Sushynski, Debra A McNett, Cynthia Van Landingham, Kathleen P Plotzke
Octamethylcyclotetrasiloxane (D4) and decamethylcyclopentasiloxane (D5) are low molecular weight cyclic volatile methyl siloxanes (cVMSs) primarily used as intermediates or monomers in the production of high molecular weight silicone polymers. The use of D4 as a direct ingredient in personal care products has declined significantly over the past 10 years, although it may be present as a residual impurity in a variety of consumer products. D5 is still used as an intentional ingredient in cosmetics, consumer products and in dry cleaning...
May 13, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28510480/dry-powder-inhaler-formulation-of-rifampicin-an-improved-targeted-delivery-system-for-alveolar-tuberculosis
#6
Tejal Rawal, Laurent Kremer, Iman Halloum, Shital Butani
BACKGROUND: The delivery of antitubercular drugs through direct lung targeting can lead to reduction in the dose as well as side effects of the drug. In the present investigation, carrier (lactose)-based dry-powder inhaler of rifampicin was prepared to achieve direct targeting of the drug into the lungs. METHODS: The dry powder inhaler formulation was prepared by simply mixing micronized rifampicin with coarse and fine lactose preblend. Preliminary blends of the drug were prepared with various lactose grades (Inhalac(®), Respitose,(®) and Lactohale(®))...
May 16, 2017: Journal of Aerosol Medicine and Pulmonary Drug Delivery
https://www.readbyqxmd.com/read/28510418/conjugation-reaction-with-8-arm-peg-markedly-improves-the-immunogenicity-of-mycobacterium-tuberculosis-cfp10-tb10-4-fusion-protein
#7
Xiaowei Sun, Weili Yu, Quanhai Pang, Tao Hu
Mycobacterium tuberculosis (Mtb) is a serious fatal pathogen responsible for tuberculosis (TB). Effective vaccination is highly desired for immunoprotection against Mtb infection. CFP10 and TB10.4 are two important immunodominant Mtb-secreted protein antigens, which suffer from poor immunogenicity. Thus, an antigen delivery system and adjuvants are needed to improve the immunogenicity of the two proteins. CFP10 and TB10.4 are two Mtb-secreted immunodominant protein antigens. A CFP10-TB10.4 fusion protein (CT) was used as the antigen...
May 16, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28510130/the-penetration-of-5-oxo-pro-arg-pro-into-the-brain-and-the-major-metabolic-pathways-of-this-peptide-in-the-rat-brain-and-blood-at-the-intranasal-and-intravenous-administration
#8
K V Shevchenko, I Yu Nagaev, V P Shevchenko, L A Andreeva, S I Shram, N F Myasoedov
It was shown that the neuroactive peptide 5-oxo-Pro-Arg-Pro (5-oxo-PRP) is detected in the brain in the time interval of 5-120 min after it was intravenously or intranasally administered to rats; the maximum concentration of labeled tripeptide in these modes of administration was observed after 30 and 10 min, respectively. A significant difference in the concentrations of 5-oxo-PRP in the blood and brain (the latter was 50 times lower) during intravenous administration indicates a relatively low permeability of the peptide across the blood-brain barrier...
March 2017: Doklady. Biochemistry and Biophysics
https://www.readbyqxmd.com/read/28507469/lungs-deposition-and-pharmacokinetic-study-of-submicron-budesonide-particles-in-wistar-rats-intended-for-immediate-effect-in-asthma
#9
Abdul Rauf, Aseem Bhatnagar, S S Sisodia, Roop K Khar, Farhan J Ahmad
The purpose of the present investigation was to study the aerosolization, lungs deposition and pharmacokinetic study of inhalable submicron particles of budesonide in male Wistar rats. Submicron particles were prepared by antisolvent nanoprecipitation method and freeze-dried to obtain free flowing powder. The freeze-drying process yielded dry powder with desirable aerodynamic properties for inhalation therapy. An in-house model inhaler was designed to deliver medicine to lungs, optimized at dose level of 10 mg for 30 sec of fluidization...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28506835/impact-of-common-clandestine-structural-modifications-on-synthetic-cathinone-bath-salt-pharmacokinetics
#10
Gregory G Grecco, David F Kisor, Joseph S Magura, Jon E Sprague
Since 2009, the synthetic cathinones ("bath salts") have risen in popularity as drugs of abuse. However, there are a paucity of studies that have determined the impact of functional group modifications in the synthetic cathinone chemical structures on plasma and central nervous system (CNS) pharmacokinetics. In the present study, we investigated the in vivo plasma and CNS pharmacokinetics of three synthetic cathinones whose structures differ by lengthening of the α-alkyl chain: methylone (-CH3), butylone (-CH2CH3), and pentylone (-CH2CH2CH3)...
May 12, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28503995/preparation-and-characterization-of-surface-modified-plga-polymeric-nanoparticles-used-to-target-treatment-of-intestinal-cancer
#11
Niyaz Ahmad, Md Aftab Alam, Rizwan Ahmad, Atta Abbas Naqvi, Farhan Jalees Ahmad
Docetaxel (DTX), a cytotoxic taxane, is a poor water-soluble drug and exhibits less oral bioavailability. Current research investigates the effective transport, for DTX-loaded chitosan (CS)-coated-poly-lactide-co-glycolide (PLGA)-nanoparticles (NPs) (DTX-CS-PLGA-NPs) and DTX-PLGA-NPs as well as a novel third-generation P-gp inhibitor i.e. GF120918 (Elacridar), across intestinal epithelium with its successive uptake by the tumour cells in an in vitro model. The prepared NPs showed a spherical shape particle size i...
May 14, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28502673/glucosamine-modulates-propranolol-pharmacokinetics-via-intestinal-permeability-in-rats
#12
Hanadi A Al Shaker, Nidal A Qinna, Mujtaba Badr, Mahmoud M H Al Omari, Nasir Idkaidek, Khalid Z Matalka, Adnan A Badwan
Propranolol (PROP) undergoes extensive first-pass metabolism by the liver resulting in a relatively low bioavailability (13-23%); thus, multiple oral doses are required to achieve therapeutic effect. Since some studies have reported that glucosamine (GlcN) can increase the bioavailability of some drugs, therefore, it is aimed to study whether GlcN can change the pharmacokinetic parameters of PROP, thus modulating its bioavailability. When PROP was orally co-administered with GlcN (200mg/kg) to rats, PROP area under curve (AUC) and maximum concentration (Cmax) were significantly decreased by 43% (p<0...
May 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28500645/development-and-validation-of-an-lc-esi-ms-ms-approach-to-determinate-a-highly-hydrophobic-drug-norcantharidin-palmitate-and-apply-to-a-preliminary-pharmacokinetic-study-in-rats
#13
Xiaolin Liu, Xiaoguang Tao, Qi Zheng, Hang Xu, Yu Zhang, Tian Lei, Tian Yin, Haibing He, Xing Tang
In order to investigate the pharmacokinetics of norcantharidin palmitate (NCTD-PAL) in rats, we developed and validated an LC-ESI-MS/MS method. The NCTD-PAL and internal standard (Triamcinoloneacetonide palmitate, TAP) were separated on a Phenomenex Kinetex®XB C18 column, and the mobile phase was composed of tetrahydrofuran (THF)-acetonitrile (20/80, v/v) and an aqueous phase containing 0.2% ammonium hydroxide at a flow rate of 0.3 mL/min. The ESI interface operated in positive mode was used to acquire the mass spectrometric data, and the transition ions were m/z 635...
May 12, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28499643/pharmacokinetic-profile-of-bilberry-anthocyanins-in-rats-and-the-role-of-glucose-transporters-lc-ms-ms-and-computational-studies
#14
G Baron, A Altomare, L Regazzoni, V Redaelli, S Grandi, A Riva, P Morazzoni, A Mazzolari, M Carini, G Vistoli, G Aldini
The aim of the present investigation was to better understand the pharmacokinetic profile of bilberry (Vaccinium Myrtillus) anthocyanins and the role of glucose transporters (sGLT1 and GLUT2) on their absorption. In particular, the absorption of 15 different anthocyanins contained in a standardized bilberry extract (Mirtoselect(®)) was measured in rats by a validated LC-ESI-MS/MS approach. The plasma concentration peak (Cmax) of 11.1ng/mL was reached after 30min and fasting condition significantly increased the bioavailability of anthocyanins by more than 7 fold in respect to fed rats...
April 27, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28497570/-laps-insulin115-a-novel-ultra-long-acting-basal-insulin-with-a-unique-action-profile
#15
Nina Wronkowitz, Thorsten Hartmann, Sven Görgens, Daniela Dietze-Schroeder, Ira Indrakusuma, In Young Choi, Sung Hee Park, Young-Mi Lee, Se Chang Kwon, Yeonjoo Kang, Marcus Hompesch, Juergen Eckel
AIMS: Developing a safe, while more convenient long-acting basal insulin for diabetic patients is still an unmet medical need. Thus, we conducted a comprehensive pre-clinical study of the novel ultra-long acting insulin analogue (LAPS) Insulin115. METHODS: Pharmacokinetic/pharmacodynamic studies comparing (LAPS) Insulin115 with other basal insulins were conducted in (db/db) mice. Insulin signaling in the major target organs was analysed by Western blot after single subcutaneous injection in wildtype male Wistar rats...
May 12, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28496463/antibacterial-loaded-spray-dried-chitosan-polyelectrolyte-complexes-as-dry-powder-aerosol-for-the-treatment-of-lung-infections
#16
Brahmeshwar Mishra, Madhusmita Mishra, Sarita Kumari Yadav
Inhalation delivery of aerosolized antibacterials is preferred over conventional methods of delivery for targeting lung infection. The present study is concerned with the development and characterization of a novel, spray dried, aerosolized, chitosan polyelectrolyte complex (PEC) based microparticles containing antibacterials for the treatment of lung infections. Chitosan polyelectrolyte complex microparticles were formulated by spray drying process. Prepared spray dried chitosan PEC microparticles were studied for surface morphology, drug encapsulation efficiency, moisture content, Carr's index, solid state interaction by XRD, aerosolization behaviour and in-vitro drug release...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/28495902/regio-and-stereo-selective-oxidation-of-a-cardiovascular-drug-metoprolol-mediated-by-cytochrome-p450-2d-and-3a-enzymes-in-marmoset-livers
#17
Shotaro Uehahara, Sakura Ishii, Yasuhiro Uno, Takashi Inoue, Erika Sasaki, Hiroshi Yamazaki
A β-blocker metoprolol is one of the in vivo probes for human cytochrome P450 (P450) 2D6. Investigation of non-human primate P450 enzymes helps improve accuracy of the extrapolation of pharmacokinetic data from animals into humans. Common marmosets (Callithrix jacchus) are a potential primate model for preclinical research, but detailed roles of marmoset P450 enzymes in metoprolol oxidations remained unknown. In this study, regio- and stereo-selectivity of metoprolol oxidations by a variety of P450 enzymes in marmoset and human livers were investigated in vitro...
May 11, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28495566/the-constraints-construction-and-verification-of-a-strain-specific-physiologically-based-pharmacokinetic-rat-model
#18
H Musther, M D Harwood, J Yang, D B Turner, A Rostami-Hodjegan, M Jamei
The use of in vitro-in vivo extrapolation (IVIVE) techniques, mechanistically incorporated within Physiologically-Based Pharmacokinetic (PBPK) models, can harness in vitro drug data and enhance understanding of in vivo pharmacokinetics. This study's objective was to develop a user-friendly rat (250g, male Sprague-Dawley) IVIVE linked PBPK model. A 13-compartment PBPK model including mechanistic absorption models was developed, with required system data (anatomical, physiological and relevant IVIVE scaling factors) collated from literature and analysed...
May 8, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28494732/pharmacokinetics-of-botanical-drugs-and-plant-extracts
#19
Gina Paola Domínguez Moré, Paola Andrea Cárdenas, Geison M Costa, Cláudia M O Simões, Diana Marcela Aragón
Botanical drugs contain plant extracts, which are complex mixtures of compounds. As with conventional drugs, it is necessary to validate their efficacy and safety through preclinical and clinical studies. However, pharmacokinetic studies for active constituents or characteristic markers in botanical drugs are rare. The objective of this review was to investigate the global state of the art in pharmacokinetic studies of active ingredients present in plant extracts and botanical drugs. A review of pharmacokinetics studies of chemical constituents of plant extracts and botanical drugs was performed, with a total of 135 studies published between January 2004 and February 2015 available in recognized scientific databases...
May 9, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28494337/quantification-of-apigenin-trimethyl-ether-in-rat-plasma-by-liquid-chromatography-tandem-mass-spectrometry-application-to-a-pre-clinical-pharmacokinetic-study
#20
Mai Gamal Elhennawy, Hai-Shu Lin
Apigenin trimethyl ether (5,7,4'-trimethoxyflavone, ATE) is a naturally occurring polymethoxyflavone with a wide range of health-promoting activities. In this study, a sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantification of ATE in rat plasma. Protein precipitation was applied as plasma clean-up procedure; the electrospray ionization was operated in its positive ion mode while ATE and formononetin (internal standard) were measured by multiple reactions monitoring (ATE: m/z 313...
April 22, 2017: Journal of Pharmaceutical and Biomedical Analysis
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