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pharmacokinetics, rat

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https://www.readbyqxmd.com/read/28214380/application-of-the-mechpeff-model-to-predict-passive-effective-intestinal-permeability-in-the-different-regions-of-the-rodent-small-intestine-and-colon
#1
D Pade, M Jamei, A Rostami-Hodjegan, D B Turner
A major component of Physiologically-Based Pharmacokinetic (PBPK) models is prediction of the rate and extent of absorption of orally dosed drugs for which knowledge of effective passive intestinal permeability (Peff ) is essential. Single pass intestinal perfusion (SPIP) studies are used to establish effective permeability in vivo but are difficult to perform in rodents while mechanistic models to predict drug Peff in rat and mouse have not been published. This work evaluates the predictive performance of the 'MechPeff' model to predict Peff in the rodent intestine based upon knowledge of regional gut physiology and drug-specific physicochemical parameters...
February 18, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28214059/pharmacokinetic-alterations-of-rhubarb-anthraquinones-in-experimental-colitis-induced-by-dextran-sulfate-sodium-in-the-rat
#2
Wen-Jin Wu, Ru Yan, Ting Li, Ya-Ping Li, Rui-Na Zhou, Yi-Tao Wang
ETHNOPHARMACOLOGICAL RELEVANCE: Rhubarb (Rhei Rhizoma et Radix) is used for the treatment of digestive diseases in traditional medicinal practice in China. Recent studies also support its beneficial activities in alleviating ulcerative colitis (UC). AIM OF THE STUDY: This study aimed to characterize the oral pharmacokinetics of rhubarb anthraquinones, the main bioactive components of this herb, in the experimental chronic colitis rat model induced by dextran sulfate sodium (DSS) and to identify the factors causing the pharmacokinetic alterations...
February 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28213295/determination-of-imm-h004-a-novel-neuroprotective-agent-in-rat-plasma-and-brain-tissue-by-liquid-chromatography-tandem-mass-spectrometry
#3
Ziqian Zhang, Xiangmeng Wu, Manman Zhao, Yakun Yang, Yan Wang, Jinping Hu, Baolian Wang, Li Sheng, Yan Li
A rapid and sensitive liquid chromatography-tandem mass spectrometry method for determination of IMM-H004, a novel neuroprotective agent, in rat plasma and brain was developed. Plasma and brain tissue homogenate samples containing IMM-H004 and propranolol (internal standard, IS) were prepared by using a direct protein precipitation of acetonitrile. Separation was carried out in Zorbax SB-C18 column at a flow rate of 0.3mL/min utilizing acetonitrile/water as mobile phases which contain 0.5% formic acid (v/v)...
February 6, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28211608/preclinical-characterisation-of-55p0251-a-novel-compound-that-amplifies-glucose-stimulated-insulin-secretion-and-counteracts-hyperglycaemia-in-rodents
#4
Karin Stadlbauer, Barbara Brunmair, Zsuzsanna Lehner, Immanuel Adorjan, Thomas Scherer, Anton Luger, Leonhardt Bauer, Clemens Fürnsinn
AIMS: 55P0251 is a novel compound with blood glucose lowering activity in mice, which has been developed from a molecular backbone structure found in herbal remedies. We here report its basic pharmacological attributes and initial progress in unmasking the mode of action. MATERIALS AND METHODS: Pharmacokinetic properties of 55P0251 were portrayed in several species. First efforts to elucidate the glucose lowering mechanism in rodents included numerous experimental protocols dealing with glucose tolerance, insulin secretion from isolated pancreatic islets, and comparison to established drugs...
February 17, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28210753/puerarin-7-o-glucuronide-a-water-soluble-puerarin-metabolite-prevents-angiotensin-ii-induced-cardiomyocyte-hypertrophy-by-reducing-oxidative-stress
#5
Ning Hou, Bin Cai, Cai-Wen Ou, Zhen-Hui Zhang, Xia-Wen Liu, Mu Yuan, Gan-Jian Zhao, Shi-Ming Liu, Long-Gen Xiong, Jian-Dong Luo, Cheng-Feng Luo, Min-Sheng Chen
This study aimed to investigate the anti-oxidant and anti-hypertrophic effects of puerarin-7-O-glucuronide, a water-soluble puerarin metabolite. The anti-oxidant effects of puerarin-7-O-glucuronide were assessed by measurement of intracellular superoxide levels, total superoxide dismutase (SOD) activity, total anti-oxidant capacity, and glutathione (GSH)/glutathione disulfide (GSSG) ratio in cultured neonatal rat cardiomyocytes (NRCMs) stimulated with the xanthine oxidase (XO)/xanthine (X) system or angiotensin II...
February 16, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28208738/oral-administration-of-the-japanese-traditional-medicine-keishibukuryogan-ka-yokuinin-decreases-reactive-oxygen-metabolites-in-rat-plasma-identification-of-chemical-constituents-contributing-to-antioxidant-activity
#6
Yosuke Matsubara, Takashi Matsumoto, Kyoji Sekiguchi, Junichi Koseki, Atsushi Kaneko, Takuji Yamaguchi, Yumiko Kurihara, Hiroyuki Kobayashi
Insufficient detoxification and/or overproduction of reactive oxygen species (ROS) induce cellular and tissue damage, and generated reactive oxygen metabolites become exacerbating factors of dermatitis. Keishibukuryogan-ka-yokuinin (KBGY) is a traditional Japanese medicine prescribed to treat dermatitis such as acne vulgaris. Our aim was to verify the antioxidant properties of KBGY, and identify its active constituents by blood pharmacokinetic techniques. Chemical constituents were quantified in extracts of KBGY, crude components, and the plasma of rats treated with a single oral administration of KBGY...
February 8, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28205294/simultaneous-determination-of-the-bioactive-components-in-rat-plasma-by-uplc-ms-ms-and-application-in-pharmacokinetic-studies-after-oral-administration-of-radix-scutellariae-extract
#7
Jin-Hua Tao, Jun Xu, Shu Jiang, Yong Ling, Dong-Geng Wang
A highly sensitive and rapid ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) has been developed and validated for simultaneous quantification of the four main bioactive compounds, i.e., baicalin, baicalein, wogonoside and wogonin in rat plasma after oral administration of Radix scutellariae extract. Clarithromycin was used as an internal standard (IS). Plasma samples were processed by protein precipitation with methanol. The separation was performed on an Acquity BEH C18 column (100 mm × 2...
February 16, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28205290/development-and-qualification-of-an-lc-ms-ms-method-for-investigating-the-biological-implications-of-micelle-entrapped-paclitaxel-in-cell-culture-and-rats
#8
Amal Kaddoumi, Kanwaldeep K Gill, Khaled Elfakhri, Sami Nazzal
Paclitaxel is a front-line antineoplastic drug used in chemotherapeutic modalities for treatment of various types of malignancies. However, its efficacy is limited by dose related toxicities. In this study, we have explored two important biological aspects of entrapping paclitaxel in PEG2000 -DSPE micelles. First, we evaluated the impact of this micellar delivery system on P-glycoprotein (P-gp)-paclitaxel interaction, and we investigated differences in plasma pharmacokinetics of free and micelle entrapped paclitaxel...
February 15, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28199114/curcumin-loaded-blood-stable-polymeric-micelles-for-enhancing-therapeutic-effect-on-erythroleukemia
#9
Feirong Gong, Dan Chen, Xin Teng, Junhua Ge, Xianfeng Ning, Ya-Ling Shen, Jian Li, Shanfeng Wang
Curcumin has high potential in suppressing many types of cancer and overcoming multi-drug resistance in a multi-faceted manner by targeting diverse molecular targets. However, the rather low systemic bioavailability resulted from its extremely low aqueous solubility and rapid metabolism and excretion in vivo has hampered its application in cancer therapy. With the primary aim to increase the aqueous solubility of curcumin while retaining its stability in the blood circulation before it accesses the tumor site, here we report preparation of curcumin-loaded N-(tert-butoxycarbonyl)-L-phenylalanine end-capped methoxy-poly(ethylene glycol)-block-poly(ε-caprolactone) (mPEG-PCL-Phe(Boc)) micelles with high stability both in vitro and in vivo and anti-tumor efficacy...
February 15, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28195469/effect-of-a-type-linkage-on-the-pharmacokinetics-and-intestinal-metabolism-of-litchi-pericarp-oligomeric-procyanidins
#10
Shuyi Li, Yang Liu, Gang Liu, Jingren He, Xinguang Qin, Haochen Yang, Zhongze Hu, Olusola Lamikanra
The bioavailability of A-type procyanidins in vivo has been rarely investigated; as such, this study discusses the effect of A-type linkage and degree of polymerization on the metabolism of procyanidins extracted from litchi pericarp (LPOPC). Sprague-Dawley rats were gavaged with (-)-epicatechin (EC) and LPOPC and sacrificed at different time points after ingestion. A-type linkage procyanidin oligomers inhibited the absorption of EC. Analysis of urinary contents from rats administered with EC, A-type procyanidin dimer (A-2) and trimer (A-3) showed distinct native and metabolite profiles for each rat...
February 14, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28194422/pharmacokinetic-properties-of-adenosine-amine-congener-in-cochlear-perilymph-after-systemic-administration
#11
Hao Chang, Ravindra S Telang, Sreevalsan Sreebhavan, Malcolm Tingle, Peter R Thorne, Srdjan M Vlajkovic
Noise-induced hearing loss (NIHL) is a global health problem affecting over 5% of the population worldwide. We have shown previously that acute noise-induced cochlear injury can be ameliorated by administration of drugs acting on adenosine receptors in the inner ear, and a selective A1 adenosine receptor agonist adenosine amine congener (ADAC) has emerged as a potentially effective treatment for cochlear injury and resulting hearing loss. This study investigated pharmacokinetic properties of ADAC in rat perilymph after systemic (intravenous) administration using a newly developed liquid chromatography-tandem mass spectrometry detection method...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28192936/generic-hybrid-ligand-binding-assay-liquid-chromatography-high-resolution-mass-spectrometry-based-workflow-for-multiplexed-human-immunoglobulin-g1-quantification-at-the-intact-protein-level-application-to-preclinical-pharmacokinetic-studies
#12
Christian Lanshoeft, Sarah Cianférani, Olivier Heudi
The quantitative analysis of human immunoglobulin G1 (hIgG1) by mass spectrometry is commonly performed using surrogate peptides after enzymatic digestion. Since some limitations are associated with this approach, a novel workflow is presented by hybridizing ligand binding assay (LBA) with liquid chromatography-high-resolution mass spectrometry (LC-HRMS) for hIgG1 quantification directly at the intact protein level. Different hIgG1s, including a [(13)C]-labeled version used as internal standard, were immuno-enriched from rat serum with a fully automated platform based on streptavidin coated tips and a biotinylated mouse anti-hIgG capture antibody targeting the fragment crystallizable region followed by overnight deglycosylation prior to LC-HRMS analysis...
February 9, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28192759/precise-simultaneous-quantification-of-methadone-and-cocaine-in-rat-serum-and-brain-tissue-samples-following-their-successive-i-p-administration
#13
David S Nakhla, Lobna A Hussein, N Magdy, Inas A Abdallah, Hazem E Hassan
A sensitive high-performance liquid chromatography (HPLC) assay with dual UV detection has been developed and validated for the simultaneous quantification of methadone and cocaine in rat serum and brain tissue samples. Liquid-liquid extraction using hexanes was applied for samples extraction with Levo-Tetrahydropalmatine (L-THP) as the internal standard. Chromatographic separation of the analytes was achieved on a reversed-phase Waters Symmetry(®) C18 column (150mm×4.6mm, 5μm). A gradient elution was employed with a mobile phase consisting of 5mM potassium phosphate containing 0...
February 7, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28188763/hiv-antiretroviral-drug-efavirenz-induces-anxiety-like-and-depression-like-behavior-in-rats-evaluation-of-neurotransmitter-alterations-in-the-striatum
#14
Giuliana Ignácio Teixeira Cavalcante, Adriano José Maia Chaves Filho, Maria Isabel Linhares, Camila Nayane de Carvalho Lima, Edith Teles Venâncio, Emiliano Ricardo Vasconcelos Rios, Francisca Cléa Florenço de Souza, Silvânia Maria Mendes Vasconcelos, Danielle Macêdo, Marta Maria de França Fonteles
Efavirenz (EFV) is an effective antiretroviral drug with a favorable pharmacokinetic profile and widely used in combination regimens to treat HIV infection. However, there are major concerns about the safety of this drug. Patients treated with EFV often experience neuropsychiatric adverse effects, which frequently lead to switching to alternative EFV-free regimens. The mechanisms involved in the central action of EFV are intrinsically unclear. Thus, this study aimed to investigate the effects of acute and subchronic (2 weeks) EFV administration in a series of behavioral tests for anxiety-like and depression-like behavior in healthy rats...
February 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28188296/effect-of-garlic-gingko-and-st-john-s-wort-extracts-on-the-pharmacokinetics-of-fexofenadine-a-mechanistic-study
#15
Jasmina Turkanovic, Jacobus P Gerber, Michael B Ward, Robert W Milne
The aim of this study was to determine the effects of garlic and ginkgo herbal extracts on the pharmacokinetics of the P-glycoprotein (P-gp)/Organic anion transporting polypeptides (Oatps) substrate fexofenadine. Male rats were dosed orally with garlic (120 mg/kg), ginkgo (17 mg/kg), St. John's wort (SJW; 1000 mg/kg; positive control) or milli Q water for 14 days. On day 15, rats were either administered fexofenadine (orally or intravenously), had their livers isolated and perfused with fexofenadine, or the small intestine divided into four segments (SI-SIV) and analysed for P-gp and Oatp1a5...
February 10, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28187732/comparative-studies-on-the-multi-component-pharmacokinetics-of-aristolochiae-fructus-and-honey-fried-aristolochiae-fructus-extracts-after-oral-administration-in-rats
#16
Jinbin Yuan, Gang Ren, Jian Liang, Chong-Zhi Wang, Zhihong Yan, Qun Huang, Jiankang Li, Yang Chen, Yi Tang, Xiaofei Liu, Chun-Su Yuan
BACKGROUND: Aristolochiae Fructus (AF) and honey-fried Aristolochiae Fructus (HAF) have been used in China for a long time as anti-tussive and expectorant drugs. Few clinical cases have been reported to be associated with the toxicity of AF and HAF, although relatively high amounts of aristolochic acids (AAs) have been found in them. Our previous experiments have verified from the chemical changes and from traditional toxicology that honey-processing can significantly reduce the toxicity of AF...
February 10, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28187377/simultaneous-quantification-of-reparixin-and-paclitaxel-in-plasma-and-urine-using-ultra-performance-liquid-chromatography-tandem-mass-spectroscopy-uhplc-ms-ms-application-to-a-preclinical-pharmacokinetic-study-in-rats
#17
Sarandeep Malhi, Nicholas Stesco, Samaa Alrushaid, Ted M Lakowski, Neal M Davies, Xiaochen Gu
A liquid chromatography-tandem mass spectroscopy (LC-MS/MS) assay was developed and validated to simultaneously quantify anticancer drugs reparixin and paclitaxel in this study. The compounds were extracted from plasma and urine samples by protein precipitation with acetone (supplemented with 0.1% formic acid). Chromatographic separation was achieved using a C18 column, and drug molecules were ionized using dual ion source electrospray and atmospheric pressure chemical ionization (DUIS: ESI-APCI). Reparixin and paclitaxel were quantified using negative and positive multiple reaction monitoring (MRM) mode, respectively...
February 3, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28185989/enhanced-oral-bioavailability-of-docetaxel-in-rats-combined-with-myricetin-in-situ-and-in-vivo-evidences
#18
Tianyun Hao, Yunni Ling, Meijuan Wu, Yajing Shen, Yu Gao, Shujun Liang, Yuan Gao, Shuai Qian
The purpose of this study was to investigate the effect of myricetin on the pharmacokinetics of docetaxel in rats. In comparison to oral docetaxel alone (40mg/kg), the bioavailability of docetaxel could be significantly enhanced by 1.6-2.4-fold via oral co-administration with various flavonoids (apigenin, naringenin, baicalein, quercetin and myricetin) at a dosage of 10mg/kg, and myricetin showed the highest bioavailability improvement. Further pharmacokinetic studies demonstrated that the presence of myricetin (5-20mg/kg) enhanced both Cmax and AUC of docetaxel with the highest Cmax (162ng/mL, 2...
February 7, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28185720/discovery-of-phenyl-acetamides-as-potent-and-selective-gpr119-agonists
#19
Cheng Zhu, Liping Wang, Yuping Zhu, Zack Zhiqiang Guo, Ping Liu, Zhiyong Hu, Jason W Szewczyk, Ling Kang, Gary Chicchi, Anka Ehrhardt, Andrea Woods, Toru Seo, Morgan Woods, Margaret van Heek, Karen H Dingley, Jianmei Pang, Gino M Salituro, Joyce Powell, Jenna L Terebetski, Viktor Hornak, Louis-Charles Campeau, Robert K Orr, Feroze Ujjainwalla, Michael Miller, Andrew Stamford, Harold B Wood, Timothy Kowalski, Ravi P Nargund, Scott D Edmondson
The paper describes the SAR/SPR studies that led to the discovery of phenoxy cyclopropyl phenyl acetamide derivatives as potent and selective GPR119 agonists. Based on a cis cyclopropane scaffold discovered previously, phenyl acetamides such as compound 17 were found to have excellent GPR119 potency and improved physicochemical properties. Pharmacokinetic data of compound 17 in rat, dog and rhesus will be described. Compound 17 was suitable for QD dosing based on its predicted human half-life, and its projected human dose was much lower than that of the recently reported structurally-related benzyloxy compound 2...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28181835/irinotecan-encapsulated-double-reverse-thermosensitive-nanocarrier-system-for-rectal-administration
#20
Fakhar Ud Din, Ju Yeon Choi, Dong Wuk Kim, Omer Mustapha, Dong Shik Kim, Raj Kumar Thapa, Sae Kwang Ku, Yu Seok Youn, Kyung Taek Oh, Chul Soon Yong, Jong Oh Kim, Han-Gon Choi
Intravenously administered for the treatment of rectum cancer, irinotecan produces severe side effects due to very high plasma concentrations. A novel irinotecan-encapsulated double reverse thermosensitive nanocarrier system (DRTN) for rectal administration was developed as an alternative. The DRTN was fabricated by dispersing the thermosensitive irinotecan-encapsulated solid lipid nanoparticles (SLN) in the thermosensitive poloxamer solution. Its gel properties, pharmacokinetics, morphology, anticancer activity and immunohistopathology were assessed after its rectal administration to rats and tumor-bearing mice...
November 2017: Drug Delivery
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