keyword
MENU ▼
Read by QxMD icon Read
search

pharmacokinetics, rat

keyword
https://www.readbyqxmd.com/read/28938137/synthesis-and-biological-evaluation-of-novel-6-11-dihydro-5h-benzo-e-pyrimido-5-4-b-1-4-diazepine-derivatives-as-potential-c-met-inhibitors
#1
Daowei Huang, Lei Huang, Qingwei Zhang, Jianqi Li
Over expression of c-Met tyrosine kinase is known to promote tumorigenesis and metastasis, as well as to cause therapeutic resistance. Herein a series of novel 6,11-dihydro-5H-benzo[e]pyrimido[5,4-b][1,4]diazepine derivatives were designed, synthesised and evaluated for their c-Met kinase inhibition. Compounds 17e, 17f, 18a, and 18b were further examined for their anti-proliferative activities against four typical cancer cell lines (PC-3, Panc-1, HepG2, and Caki-1). The promising compound 17f was identified as a multi-target receptor tyrosine kinase inhibitor, which also displayed favourable pharmacokinetic properties in rats, had an acceptable safety profile in preclinical studies, and significant anti-tumour activity in the Caki-1 tumour xenograft model...
September 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28937442/orally-active-epoxyeicosatrienoic-acid-analogs
#2
William B Campbell, John D Imig, James M Schmitz, John R Falck
Biologically active epoxyeicosatrienoic acid (EET) regioisomers are synthesized from arachidonic acid by cytochrome P450 epoxygenases of endothelial, myocardial, and renal tubular cells. EETs relax vascular smooth muscle and decrease inflammatory cell adhesion and cytokine release. Renal EETs promote sodium excretion and vasodilation to decrease hypertension. Cardiac EETs reduce infarct size after ischemia-reperfusion injury and decrease fibrosis and inflammation in heart failure. In diabetes, EETs improve insulin sensitivity, increase glucose tolerance, and reduce the renal injury...
September 19, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28934681/simultaneous-determination-of-gentiopicroside-and-its-two-active-metabolites-in-rat-plasma-by-lc-ms-ms-and-its-application-in-pharmacokinetic-studies
#3
Kai Xiong, Tingting Gao, Tong Zhang, Zhengtao Wang, Han Han
Gentiopicroside is a natural secoiridoid glycoside that may require metabolic activation to exert pharmacological effects. In this study, two active metabolites of gentiopicroside (M1 and M2) were isolated from rat urines and identified with our previous method. Most importantly, a fast, sensitive and selective ultra high-performance liquid chromatography-tandem mass spectrometry method was developed to simultaneously determine gentiopicroside and its two metabolites in rat plasma. The analytes and internal standard (swertiamarin) were separated on an ACQUITY UPLC(®) BEH C18 column (2...
September 14, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28933124/-analysis-on-pharmacokinetics-pharmacodynamics-correlation-of-effective-ingredients-of-qing-e-wan
#4
Ling Liu, Ze-Bin Weng, Heng Wang, Xing-Yu Zhu, Zhi-Peng Chen, Li Wu, Wei-Dong Li
To study the pharmacokinetics of three active ingredients in Qing'e wan, namely geniposidic acid, psoralen and isopsoralen, in rats, in order to investigate their correlation in the anti-osteoporotic effect. The rats were taken blood from their eye sockets at different time points after being orally administered with raw and salt-processed Qing'e wan. Geniposidic acid, psoralen and isopsoralen in rats plasma were determined by means of UHPLC-MS/MS to draw the concentration-time curve. The proliferation rate of osteoblasts was taken as the pharmacodynamic index, and determined by MTT method to draw effect-time curve...
December 2016: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28933113/-evaluation-of-pharmacokinetics-and-in-vitro-in-vivo-correlation-of-ibuprofen-with-essential-oils-as-penetration-enhancer-following-transdermal-administration
#5
Qiu-Dong Jiang, Ye-Ming Wu, Hui Zhang, Pei Liu, Jun Chen, Jin-Ao Duan
The study was carried out to investigate the pharmacokinetics and in vitro/in vivo correlation of ibuprofen with essential oils as penetration enhancers (PE) following transdermal administration. With Azone as the positive control, ibuprofen hydrogels containing Chuanxiong oil, Angelica oil or Cinnamon oil as PE were prepared and administered to the rat abdominal skin. Then the pharmacokinetics of ibuprofen following transdermal administration were investigated and compared. In comparison with negative control (no PE was added), the relative bioavailability values with the addition of Chuanxiong oil, Angelica oil, Cinnamon oil and Azone as PE were determined to be 161...
December 2016: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28933097/-pharmacokinetics-and-brain-distribution-of-nmd-tmp-nanoparticles
#6
Wen-Jie He, Qian Hong, Jing Liang, Xiao-Wei He, Feng-Jia Zhu
This study aims to prepare nimodipine/tetramethylpyrazine-loaded poly(D, L-lactide-co-glycolide) dual-drug nanoparticles (NMD/TMP-NPs) and investigate pharmacokinetics and brain distribution to evaluate the possibility of enhancing the drug effect of dual-drug nanoparticles. NMD/TMP-NPs were prepared via W/O/W emulsion solvent evaporation. Entrapment efficiency and drug loading of NMD/TMP-NPs were investigated by ultracentrifugation, and drug release behavior in vitro was studied by dialysis method. The pharmacokinetic and brain distribution were studied in SD mice administered intravenously with NMD/TMP-NPs in comparison with NMD-suspension, NMD/TMP-suspension and NMD-NPs, (NMD-NPs+TMP)-suspension...
November 2016: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28931488/carboxylate-cross-linked-cyclodextrin-a-nanoporous-scaffold-for-enhancement-of-rosuvastatin-oral-bioavailability
#7
Mai Mahmoud Gabr, Sana Mohamed Mortada, Marwa Ahmed Sallam
Cyclodextrins play an important role in supramolecular chemistry acting as building blocks than can be cross-linked by various linker molecules forming nano-porous structures called nanosponges (NS). NS have the ability to enhance the stability, solubility and bioavailability of various actives. This work aimed at elaborating rosuvastatin (ROS) loaded NS to improve its oral bioavailability. Carboxylate-linked NS were synthesized by reacting β-CD with pyromellitic dianhydride (PDA) at different molar ratios under specific conditions...
September 17, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28928659/brain-pharmacokinetics-and-the-pharmacological-effects-on-striatal-neurotransmitter-levels-of-pueraria-lobata-isoflavonoids-in-rat
#8
Bingxin Xiao, Zengxian Sun, Fangrui Cao, Lisha Wang, Yonghong Liao, Xinmin Liu, Ruile Pan, Qi Chang
Isoflavonoids are putatively active components of Pueraria lobata and has been demonstrated prominent neuro-protection effect against cerebrovascular disorders, hypertension or Parkinson's disease (PD). However, the molecular basis for the beneficial effect of Pueraria lobata on nervous systems has not been well revealed. The present study aims to assess striatum exposure to main active isoflavonoids and changes of striatal extracellular neurotransmitters levels in rat brain after intravenous administration of Pueraria lobata isoflavonoids extracts (PLF), to further elucidate its' substantial bases for neuro activities...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28926562/generics-for-the-treatment-of-hepatitis-c-in-monoinfected-and-hiv-coinfected-patients-pros-and-cons
#9
Dario Cattaneo, Alessandro Fossati, Chiara Resnati, Massimo Galli, Cristina Gervasoni
The treatment of hepatitis C virus in monoinfected and HIV-coinfected patients has greatly changed over recent years as a result of the introduction of direct-acting antiviral agents (DAAs), which have revolutionized clinical outcomes and led to sustained virological response rates above 90-95%. The discovery of new molecules and the subsequent competition between pharmaceutical companies, together with the negotiated price policies pursued by many national health systems, have led to a gradual reduction in the cost of DAAs, and expand their use to an increasing number of patients, including those with mild liver damage...
September 19, 2017: AIDS Reviews
https://www.readbyqxmd.com/read/28925896/allopurinol-old-drug-new-indication-in-neonates
#10
Kim V Annink, Axel R Franz, Jan B Derks, Mario Rüdiger, Frank van Bel, Manon J N L Benders
BACKGROUND: Hypoxic-ischemic encephalopathy (HIE) is an important cause of neonatal mortality and neurological morbidity, even despite hypothermia treatment. Neuronal damage in these infants is partly caused by the production of superoxides via the xanthine-oxidase pathway and concomitant free radical formation. Allopurinol is a xanthine-oxidase inhibitor and can potentially reduce the formation of these superoxides that lead to brain damage in HIE. METHODS: The aim of this review is to provide an overview of the animal and clinical data about the neuroprotective effect of allopurinol in HIE and the relevant mechanisms leading to brain injury in HIE...
September 18, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28925166/-comparison-of-pharmacokinetics-of-curcumin-in-rats-administered-with-two-kinds-of-polymeric-micelles
#11
Di Zhang, Qian Xu, Ke Liu, Hui Xu
To investigate the effect of end-capped modification of mPEG-PLA with Boc-phenylalanine(BP) on pharmacokinetic characteristics of curcumin(CUR) loaded micelles, and then provide experimental evidence for prescription optimization. Healthy male SD rats were randomly divided into three groups and they were intravenously administered with a single injection of CUR-mPEG-PLA micelles, CUR-mPEG-PLA-BP micelles and reference formulations DMSO solution(n=6). The doses were 20 mg•kg⁻¹ in term of CUR. Blood samples were collected before and after administration, and the concentration of curcumin in blood plasma was determined by HPLC to draw time-concentration curve...
October 2016: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28925165/-effects-of-sanguisorba-tannins-and-saponins-compatibility-on-pharmacokinetic-parameters-of-catechin-epicatechin-and-ziyuglycoside-%C3%A2-in-rats
#12
Yong-Ai Xiong, Ming Yang
To study the effects of sanguisorba tannins and saponins compatibility at different proportions [tannins-saponins (1∶1) and tannins-saponins(8∶1)] after intragastric administration (50 mg•kg⁻¹) on pharmacokinetic parameters of catechin, epicatechin and ziyuglycoside Ⅰ in rats by using pharmacokinetic techniques and methods. Kinetica 5.0 software was used to calculate the pharmacokinetic parameters. The results showed that the specificity, linearity, recovery rate, precision and stability of the established detection method were in line with the test requirements...
October 2016: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28925046/in-vivo-pharmacodynamic-and-pharmacokinetic-interactions-of-hibiscus-sabdariffa-calyces-extracts-with-simvastatin
#13
S J Showande, O M Adegbolagun, S I Igbinoba, T O Fakeye
WHAT IS KNOWN AND OBJECTIVES: Increasing number of patients use herbs with their medications. Such practice may result in beneficial or harmful herb-drug interactions. A recent survey reported that some participants co-administered Hibiscus sabdariffa, a widely used beverage, or tea, with their antihyperlipidaemic medications. This study therefore evaluated the effect of concomitant administration of Hibiscus sabdariffa calyces' extracts with simvastatin on hyperlipidaemia and pharmacokinetics of the drug in vivo...
September 18, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28923868/gelofusine-ameliorates-colistin-induced-nephrotoxicity
#14
Sivashangarie Sivanesan, Mohammad A K Azad, Elena K Schneider, Maizbha U Ahmed, Jiayuan Huang, Jiping Wang, Jian Li, Roger L Nation, Tony Velkov
Colistin therapy is used as the last-line of defence against life-threatening Gram-negative infections. Nephrotoxicity is the major dose-limiting side-effect that impedes optimal dosing of patients. This study aims to examine the nephroprotective effect of the plasma volume expander gelofusine against colistin-induced nephrotoxicity. Renal protection was assessed in mice that were subcutaneously injected with colistin sulphate (14 mg/kg x 6 doses every 2 h; accumulated dose 84 mg/kg) and simultaneously injected in the intraperitoneal region with gelofusine (75, 150, 300 or 600 mg/kg x 6)...
September 18, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28923568/a-method-for-determining-polysaccharide-content-in-biological-samples
#15
Duoduo Xu, Wei Zheng, Yanqiu Zhang, Qipin Gao, Mingxing Wang, Yang Gao
Difficulties in the determination of polysaccharide content in biological samples has been one of the bottlenecks limiting the development of polysaccharides pharmacokinetics, greatly due to the complicated chemical structure of these compounds. In this study, we established a simple, reproducible and reliable method for the determination of polysaccharide content in biological samples. Polysaccharides were replaced by fluorescein isothiocyanate (FITC) and iodine to generate a complex. The iodine content in the complex was measured by inductively coupled plasma-mass spectrometry (ICP-MS) to indirectly reflect polysaccharide content...
September 15, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28923421/avoidance-of-food-effect-on-oral-absorption-profile-of-itraconazole-by-self-micellizing-solid-dispersion-approach
#16
Yoshiki Kojo, Kanako Kobayashi, Saori Matsunaga, Hiroki Suzuki, Yoshiki Seto, Hideyuki Sato, Satomi Onoue
The present study was aimed to avoid pharmacokinetic transitions of itraconazole (ITZ) evoked by high-fat meal intake by employing a self-micellizing solid dispersion (SMSD) approach. The dissolution behavior of SMSD/ITZ was assessed in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). To evaluate the food effect on the oral absorption profile of ITZ, a pharmacokinetic study was conducted on orally-dosed ITZ samples in fasted and high-fat meal-fed rats. Crystalline ITZ showed a 9.0-fold higher dissolution amount of ITZ in fed-state SGF (FeSSGF) than in fasted-state SGF (FaSSGF), whereas there was no significant difference in the dissolution amount of ITZ in SMSD/ITZ between FeSSGF and FaSSGF...
June 15, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28918355/gallium-iii-chelates-of-mixed-phosphonate-carboxylate-triazamacrocyclic-ligands-relevant-to-nuclear-medicine-structural-stability-and-in-vivo-studies
#17
Maria I M Prata, João P André, Zoltán Kovács, Anett I Takács, Gyula Tircsó, Imre Tóth, Carlos F G C Geraldes
Three triaza macrocyclic ligands, H6NOTP (1,4,7-triazacyclononane-N,N',N″-trimethylene phosphonic acid), H4NO2AP (1,4,7-triazacyclononane-N-methylenephosphonic acid-N',N″-dimethylenecarboxylic acid), and H5NOA2P (1,4,7-triazacyclononane-N,N'-bis(methylenephosphonic acid)-N″-methylene carboxylic acid), and their gallium(III) chelates were studied in view of their potential interest as scintigraphic and PET (Positron Emission Tomography) imaging agents. A (1)H, (31)P and (71)Ga multinuclear NMR study gave an insight on the structure, internal dynamics and stability of the chelates in aqueous solution...
September 1, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28918324/simultaneous-determination-and-pharmacokinetic-study-of-twelve-bioactive-compounds-in-rat-plasma-after-intravenous-administration-of-xuebijing-injection-by-uhplc-q-orbitrap-hrms
#18
Lihua Zuo, Qiuyue Zhong, Zhenhui Wang, Zhi Sun, Lin Zhou, Zhuolun Li, Tanye Xu, Yingying Shi, Jinfa Tang, Shuzhang Du, Xiaojian Zhang
Xuebijing injection (XBJ) is a traditional Chinese herbal prescription widely used in the treatment of sepsis. Extensive studies revealed that the major bioactive constituents of XBJ injection, including phenolic acids, flavonoids, monoterpene glycosides, lactones and organic acids, play an important role in the treatment. In this study, a rapid, sensitive and accurate ultra high performance liquid chromatography - Q Exactive hybrid quadrupole - orbitrap high-resolution accurate mass spectrometry (UHPLC-Q-Orbitrap HRMS) method was developed for simultaneous determination of twelve bioactive compounds in rat plasma after intravenous administration of XBJ injection...
September 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28917081/evaluation-of-the-ecstasy-influence-on-tramadol-and-its-main-metabolite-plasma-concentration-in-rats
#19
Bardia Jamali, Behjat Sheikholeslami, Yalda Hosseinzadeh Ardakani, Hoda Lavasani, Mohammad-Reza Rouini
BACKGROUND: Tramadol is prone to be abused alone, or in combination with 3,4-methylenedioxymethamphetamine (MDMA, Ecstasy). It was reported that 95% of people with a history of substance abuse in the United States used tramadol in 2004. According to the WHO report in 2016, there was a growing number of tramadol abusers alone or in combination with psychoactive substances such as MDMA in particular in some Middle East countries. Higher concentrations of tramadol in plasma may lead to adverse drug reactions or lethal intoxication...
September 16, 2017: Drug Metabolism and Personalized Therapy
https://www.readbyqxmd.com/read/28916980/pharmacokinetics-of-panax-notoginseng-saponins-in-adhesive-and-normal-preparation-of-fufang-danshen
#20
Xiao-Nan Chen, Dan-Qi Li, Meng-di Zhao, Gang-Yan Yu, Shou-Ying Du, Yang Lu, Jie Bai, Peng-Yue Li, Ya-Li Wu, Zhi-Hao Tian, Yan-Ying Zeng
BACKGROUND AND OBJECTIVE: Fufang Danshen formula, a famous Chinese patent medicine containing Salvia miltiorrhiza, Panax notoginseng and borneol, has been widely used in the treatment of coronary heart disease. The application is restricted by low bioavailability partly due to Panax notoginseng saponins (PNS) instability and low in vivo absorption. Thus, adhesive pellets were developed to improve bioavailability. The objectives of the present study were to evaluate the adhesive preparation by describing PNS's plasma pharmacokinetics in vivo and compare adhesive micro pills with normal preparation...
September 15, 2017: European Journal of Drug Metabolism and Pharmacokinetics
keyword
keyword
96131
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"