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pharmacokinetics, rat

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https://www.readbyqxmd.com/read/29351251/compatibility-with-panax-notoginseng-and-rehmannia-glutinosa-alleviates-the-hepatotoxicity-and-nephrotoxicity-of-tripterygium-wilfordii-via-modulating-the-pharmacokinetics-of-triptolide
#1
Qichun Zhang, Yiqun Li, Mengzhu Liu, Jinao Duan, Xueping Zhou, Huaxu Zhu
Tripterygium wilfordii (TW) and the representative active component triptolide show positive therapeutic effect on the autoimmune disorders and simultaneously ineluctable hepatotoxicity and nephrotoxicity. Combinational application of Panax notoginseng (PN) and Rehmannia glutinosa (RG) weakens the toxicity of TW according the clinical application of traditional Chinese medicine. This article was aimed at the mechanism of decreasing toxicity of TW by the combinational application of PN and RG. Biochemical and pathohistological analysis were utilized to assess the toxicity on liver and kidney in rats administrated with TW, TW-PN, TW-RG and TW-PN-RG for 3 and 7 days...
January 19, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29349861/validated-uplc-ms-ms-method-for-quantification-of-seven-compounds-in-rat-plasma-and-tissues-application-to-pharmacokinetic-and-tissue-distribution-studies-in-rats-after-oral-administration-of-extract-of-eclipta-prostrata-l
#2
Guangyan Du, Lingling Fu, Jun Jia, Xu Pang, Haiyang Yu, Youcai Zhang, Guanwei Fan, Xiumei Gao, Lifeng Han
A rapid, sensitive and specific ultra high performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS) method was developed to investigate the pharmacokinetics and tissue distribution of Eclipta prostrata extract. Rats were orally administrated the 70% ethanol extract of E. prostrata, and their plasma as well as various organs were collected. The concentrations of seven main compounds, including ecliptasaponin IV, ecliptasaponin A, apigenin, 3'-hydroxybiochanin A, luteolin, luteolin-7-O-glucoside, and wedelolactone, were quantified by UPLC-MS/MS through multiple reactions monitoring (MRM) method...
January 19, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29348719/effects-of-processing-method-on-the-pharmacokinetics-and-tissue-distribution-of-orally-administered-ginseng
#3
Jianbo Chen, Meijia Li, Lixue Chen, Yufang Wang, Shanshan Li, Yuwei Zhang, Lei Zhang, Mingjie Song, Chang Liu, Mei Hua, Yinshi Sun
Background: The use of different methods for the processing of ginseng can result in alterations in its medicinal properties and efficacy. White ginseng (WG), frozen ginseng (FG), and red ginseng (RG) are produced using different methods. WG, FG, and RG possess different pharmacological properties. Methods: WG, FG, and RG extracts and pure ginsenosides were administered to rats to study the pharmacokinetics and tissue distribution characteristics of the following ginsenosides-Rg1, Re, Rb1, and Rd...
January 2018: Journal of Ginseng Research
https://www.readbyqxmd.com/read/29348099/spray-dried-curcumin-nanoemulsion-a-new-road-to-improvement-of-oral-bioavailability-of-curcumin
#4
Liandong Hu, Qiaofeng Hu, Chenchen Yang
In this study a new soluble solid curcumin nanoemulsion powder was prepared using spray-drying technology to improve the solubility and bioavailability of curcumin. The liquid nanoemulsion consisted of curcumin, Capryol 90, Transcutol P, and Cremophor RH40. The solid nanoemulsion was prepared by spray-drying the liquid nanoemulsion in laboratory spray dryer, using lactose as solid carrier. The in vitro release from powder formulation was 97.6% within 15 min while the release from the curcumin crystalline was about 10%...
January 2018: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29345044/preclinical-characterisation-of-absorption-distribution-metabolism-and-excretion-properties-of-tak-063
#5
Kimio Tohyama, Miyako Sudo, Akio Morohashi, Suguru Kato, Junzo Takahashi, Yoshihiko Tagawa
TAK-063 is currently being developed to treat schizophrenia. In this study, we investigated the absorption, distribution, metabolism and excretion (ADME) properties of TAK-063 using several paradigms. Following oral administration of TAK-063 at 0.3 mg/kg, bioavailability of TAK-063 was 27.4% in rats and 49.5% in dogs with elimination half-lives of 3.1 hr in rats and 3.7 hr in dogs. TAK-063 is a highly permeable compound without P-glycoprotein (P-gp) or breast cancer resistance protein substrate liability and can be readily absorbed into systemic circulation via the intestine...
January 17, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29343943/the-oral-bioavailability-excretion-and-cytochrome-p450-inhibition-properties-of-epiberberine-an-in-vivo-and-in-vitro-evaluation
#6
Ning Chen, Xiao-Yan Yang, Chang-E Guo, Xin-Ning Bi, Jian-Hua Chen, Hong-Ying Chen, Hong-Pin Li, Hong-Ying Lin, Yu-Jie Zhang
Epiberberine (EPI) is a novel and potentially effective therapeutic and preventive agent for diabetes and cardiovascular disease. To evaluate its potential value for drug development, a specific, sensitive and robust high-performance liquid chromatography-tandem mass spectrometry assay for the determination of EPI in rat biological samples was established. This assay was used to study the pharmacokinetics, bioavailability and excretion of EPI in rats after oral administration. In addition, a cocktail method was used to compare the inhibition characteristics of EPI on cytochrome P450 (CYP450) isoforms in human liver microsomes (HLMs) and rat liver microsomes (RLMs)...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29342955/pharmacokinetics-of-schizandrin-and-its-pharmaceutical-products-assessed-using-a-validated-lc-ms-ms-method
#7
Chi-Lin Li, Yung-Yi Cheng, Chen-Hsi Hsieh, Tung-Hu Tsai
Schisandra chinensis has been used as an important component in various prescriptions in traditional Chinese medicine and, more recently, in Western-based medicine for its anti-hepatotoxic effect. The aim of this study was to develop a selective, rapid, and sensitive ultra-performance liquid chromatography-tandem mass spectrometry method for pharmacokinetic studies of schizandrin in rats. Liquid-liquid extraction was used for plasma sample preparation. A UHPLC reverse-phase C18e column (100 mm × 2.1 mm, 2 μm) coupled with a mobile phase of methanol-0...
January 15, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29342239/hplc-estimation-ex-vivo-everted-sac-permeability-and-in-vivo-pharmacokinetic-studies-of-darunavir
#8
Vasanti M Suvarna, Preeti C Sangave
Darunavir ethanolate (DRV) is an efficient protease inhibitor (PI) used in the treatment of human immunodeficiency virus (HIV) type-1 patients. An isocratic reversed-phase HPLC method was developed to monitor concentration of darunavir in in vitro intestinal fluid samples in everted sac absorption model in the presence of bioenhancers, viz., piperine, quercetin, naringenin. The method was validated and successfully applied to everted sac and pharmacokinetic studies in rats. The absorption profiles of DRV and apparent permeability coefficients were determined...
January 12, 2018: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/29342170/determination-of-2-4-dichlorophenoxyacetic-acid-2-4-d-in-rat-serum-for-pharmacokinetic-studies-with-a-simple-hplc-method
#9
Xiao Chen, Hongling Zhang, Yanjian Wan, Xi Chen, Yuanyuan Li
2,4-Dichlorophenoxyacetic acid (2,4-D) is a chlorophenoxy herbicide used worldwide. We describe a high-performance liquid chromatography (HPLC) method with UV detection for the determination of 2,4-D in female and male rat serum. This allows to observe the change of serum 2,4-D concentration in rats with time and its pharmacokinetics characteristics with a simple, rapid, optimized and validated method. The serum samples are pretreated and introduced into the HPLC system. The analytes are separated in a XDB-C18 column with a mobile phase of acetonitrile (solvent A) and 0...
2018: PloS One
https://www.readbyqxmd.com/read/29342085/development-of-a-region-specific-physiologically-based-pharmacokinetic-brain-model-to-assess-hippocampus-and-frontal-cortex-pharmacokinetics
#10
Zaril Zakaria, Raj Badhan
Central nervous system drug discovery and development is hindered by the impermeable nature of the blood-brain barrier. Pharmacokinetic modeling can provide a novel approach to estimate CNS drug exposure; however, existing models do not predict temporal drug concentrations in distinct brain regions. A rat CNS physiologically based pharmacokinetic (PBPK) model was developed, incorporating brain compartments for the frontal cortex (FC), hippocampus (HC), "rest-of-brain" (ROB), and cerebrospinal fluid (CSF). Model predictions of FC and HC Cmax, tmax and AUC were within 2-fold of that reported for carbamazepine and phenytoin...
January 17, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29341909/nanogel-dfo-conjugates-as-a-model-to-investigate-pharmacokinetics-biodistribution-and-iron-chelation-in-vivo
#11
Yan Wang, Zhi Liu, Tien-Min Lin, Shaurya Chanana, May P Xiong
Deferoxamine (DFO) to treat iron overload (IO) has been limited by toxicity issues and short circulation times and it would be desirable to prolong circulation to improve non-transferrin bound iron (NTBI) chelation. In addition, DFO is currently unable to efficiently target the large pool of iron in the liver and spleen. Nanogel-Deferoxamine conjugates (NG-DFO) can prove useful as a model to investigate the pharmacokinetic (PK) properties and biodistribution (BD) behavior of iron-chelating macromolecules and their overall effect on serum ferritin levels...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29339225/metabolism-and-pharmacokinetics-of-a-potent-n-acylindole-antagonist-of-the-oxe-receptor-for-the-eosinophil-chemoattractant-5-oxo-6-8-11-14-eicosatetraenoic-acid-5-oxo-ete-in-rats-and-monkeys
#12
Chintam Nagendra Reddy, Hussam Alhamza, Shishir Chourey, Qiuji Ye, Vivek Gore, Chantal Cossette, Sylvie Gravel, Irina Slobodchikova, Dajana Vuckovic, Joshua Rokach, William S Powell
We previously identified the indole 264 as a potent in vitro antagonist of the human OXE receptor that mediates the actions of the powerful eosinophil chemoattractant 5-oxo-ETE. No antagonists of this receptor are currently commercially available or are being tested in clinical studies. The lack of a rodent ortholog of the OXE receptor has hampered progress in this area because of the unavailability of commonly used mouse or rat animal models. In the present study, we examined the feasibility of using the cynomolgus monkey as an animal model to investigate the efficacy of orally administered 264 in future in vivo studies...
January 12, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29338533/enhanced-solubility-oral-bioavailability-and-anti-osteoporotic-effects-of-raloxifene-hcl-in-ovariectomized-rats-by-igepal-co-890-nanomicelles
#13
Jaleh Varshosaz, Vahab Ziaei, Mohsen Minaiyan, Ali Jahanian, Leila Seyed Tabatabaei
The purpose of the present study was to enhance the bioavailability and anti-osteoporotic effects of raloxifene HCl (RH) by increasing its solubility and inhibition of the p-glycoprotein-pump using surfactant micelles of Igepal CO-890. The micelles were prepared by the direct method and their critical micellar concentration, drug dissolution rate, saturated solubility, drug loading and surface morphology were defined. The cytotoxicity of Igepal CO-890 and its ability to inhibit the p-glycoprotein pump were studied on Caco-2 cells...
January 16, 2018: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/29338251/delivery-of-oxytocin-to-the-brain-for-the-treatment-of-autism-spectrum-disorder-by-nasal-application
#14
Akiko Tanaka, Tomoyuki Furubayashi, Mari Arai, Daisuke Inoue, Shunsuke Kimura, Akiko Kiriyama, Kosuke Kusamori, Hidemasa Katsumi, Reiko Yutani, Toshiyasu Sakane, Akira Yamamoto
Oxytocin (OXT) is a cyclic nonapeptide, two amino acids of which are cysteine, forming an intramolecular disulfide bond. OXT is produced in the hypothalamus and is secreted into the blood stream from the posterior pituitary. As recent studies have suggested that OXT is a neurotransmitter exhibiting central effects important for social deficits, it has drawn much attention as a drug candidate for the treatment of autism. Although human-stage clinical trials of the nasal spray of OXT for the treatment of autism have already begun, few studies have examined the pharmacokinetics and brain distribution of OXT after nasal application...
January 16, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29337578/physiologically-based-pharmacokinetic-modeling-in-lead-optimization-i-evaluation-and-adaptation-of-gastroplus-to-predict-bioavailability-of-medchem-series
#15
Pankaj R Daga, Michael B Bolger, Ian S Haworth, Robert Daniel Clark, Eric J Martin
When medicinal chemists need to improve bioavailability (%F) within a chemical series during lead optimization, they synthesize new series members with systematically modified properties mainly by following experience and general rules of thumb. More quantitative models that predict %F of proposed compounds from chemical structure alone have proven elusive. Global empirical %F quantitative structure-property (QSPR) models perform poorly and projects have too little data to train local %F QSPR models. Mechanistic oral absorption and physiologically-based pharmacokinetic (PBPK) models simulate the dissolution, absorption, systemic distribution, and clearance of a drug in preclinical species and humans...
January 16, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29337342/polysaccharides-reduce-absorption-and-mutagenicity-of-3-amino-1-4-dimethyl-5h-pyrido-4-3-b-indole-in-vitro-and-in-vivo
#16
Lingying Luo, Yun Bai, Guanghong Zhou
3-Amino-1,4-dimethyl-5H-pyrido[4,3-b]indole (Trp-P-1) is a group 2B carcinogen characterized by the International Agency for Research on Cancer (IARC) and great efforts have been taken to reduce Trp-P-1 mutagenicity to humans. In this study, the effect of a reduction of Trp-P-1 on intestinal absorption as a promising strategy was investigated. The data showed that when 20 mM Trp-P-1 cotransported with 10 mM of sodium carboxymethyl cellulose (CMC), xanthan gum, or carrageenan, the absorption rate of Trp-P-1 was reduced by 31...
January 16, 2018: Journal of Food Science
https://www.readbyqxmd.com/read/29335861/alterations-of-gefitinib-pharmacokinetics-by-co-administration-of-herbal-medications-in-rats
#17
Kwon-Yeon Weon, Min Gi Kim, Soyoung Shin, Tae Hwan Kim, Sang Hoon Joo, Eunsook Ma, Seok Won Jeong, Sun Dong Yoo, Yu Seok Youn, Beom Soo Shin
OBJECTIVE: To evaluate the potential pharmacokinetic interactions of the anticancer agent gefifitinib (Iressa®) and the oriental medications Guipi Decoction (, GPD, Guibi-tang in Korean) and Bawu Decoction (, BWD, Palmul-tang in Korean). METHODS: Methylcellulose (MC, control), GPD (1,200 mg/kg), or BWD (6,000 mg/kg) was orally administered to rats either as a single dose or multiple doses prior to gefitinib administration. To examine the effects of a single dose of the herbal medicines, gefifitinib (10 mg/kg) was orally administered after 5 min or 1 h of MC or the herbal medicine pretreatments...
January 15, 2018: Chinese Journal of Integrative Medicine
https://www.readbyqxmd.com/read/29334816/anti-colchicine-fab-fragments-prevent-lethal-colchicine-toxicity-in-a-porcine-model-a-pharmacokinetic-and-clinical-study
#18
Michael Eddleston, Nicolas Fabresse, Adrian Thompson, Ibrahim Al Abdulla, Rachael Gregson, Tim King, Alain Astier, Frederic J Baud, R Eddie Clutton, Jean-Claude Alvarez
BACKGROUND: Colchicine poisoning is commonly lethal. Colchicine-specific Fab fragments increase rat urinary colchicine clearance and have been associated with a good outcome in one patient. We aimed to develop a porcine model of colchicine toxicity to study the pharmacokinetics and efficacy of ovine Fab. METHODS: A Göttingen minipig critical care model was established and serial blood samples taken for colchicine and Fab pharmacokinetics, clinical chemistry, and haematology...
January 15, 2018: Clinical Toxicology
https://www.readbyqxmd.com/read/29334814/dual-ligand-modified-liposomes-provide-effective-local-targeted-delivery-of-lung-cancer-drug-by-antibody-and-tumor-lineage-homing-cell-penetrating-peptide
#19
Congcong Lin, Xue Zhang, Hubiao Chen, Zhaoxiang Bian, Ge Zhang, Muhammad Kashif Riaz, Deependra Tyagi, Ge Lin, Yanbo Zhang, Jinjin Wang, Aiping Lu, Zhijun Yang
The abilities of a drug delivery system to target and penetrate tumor masses are key factors in determining the system's chemotherapeutic efficacy. Here, we explored the utility of an anti-carbonic anhydrase IX (anti-CA IX) antibody and CPP33 dual-ligand modified triptolide-loaded liposomes (dl-TPL-lip) to simultaneously enhance the tumor-specific targeting and increase tumor cell penetration of TPL. In vitro, the dl-TPL-lip increased the cytotoxicity of TPL in CA IX-positive lung cancer cells, which showed tunable size (137...
November 2018: Drug Delivery
https://www.readbyqxmd.com/read/29334326/predicting-the-dopamine-d2-receptor-occupancy-of-ropinirole-in-rats-using-positron-emission-tomography-and-pharmacokinetic-pharmacodynamic-modeling
#20
Chenrong Huang, Ziteng Wang, Linsheng Liu, Xiaoxue Liu, Ji Dong, Qingqing Xu, Bin Zhang, Liyan Miao
The purpose of this study was to measure dopamine D2/3 receptor occupancy (RO) as a marker of the clinical efficacy of ropinirole in rats via positron emission tomography (PET) using 18F-fallypride as the radiotracer and to explore the relationship between dopamine RO and the plasma concentration of ropinirole via pharmacokinetic-pharmacodynamic modeling. Plasma was collected from 16 rats treated with one of four doses of ropinirole. For the time-dependent study, the data of 16 rats in the 15 mg/kg dose group at four time points were averaged, and another 24 rats were divided into three dose groups (5 mg/kg, 30 mg/kg and 60 mg/kg) for the dose-dependent study; the animals were assessed via 18F-fallypride PET scans...
January 15, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
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