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pharmacokinetics, rat

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https://www.readbyqxmd.com/read/28811130/comparative-study-on-stabilizing-ability-of-food-protein-non-ionic-surfactant-and-anionic-surfactant-on-bcs-type-ii-drug-carvedilol-loaded-nanosuspension-physicochemical-and-pharmacokinetic-investigation
#1
Tianjiao Geng, Parikshit Banerjee, Zhangdi Lu, Abdelmoumin Zoghbi, Tiantian Li, Bo Wang
Carvedilol (CAR) in its pure state has low aqueous solubility and extremely poor bioavailability which largely limit its clinical application. The aim of the study is to improve the dissolution rate and the bioavailability of CAR via preparing nanosuspensions with different stabilizers. Antisolvent precipitation-ultrasonication technique was used here. Attempts have been made to use food protein- Whey protein isolate (WPI) as a stabilizer in CAR loaded nanosuspension and also to compare its stabilizing potential with conventional nanosuspension stabilizers such as non-ionic linear copolymer-poloxamer 188 (PLX188) and anionic surfactant-sodium dodecyl sulfate (SDS)...
August 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28810527/icariin-combined-with-snailase-shows-improved-intestinal-hydrolysis-and-absorption-in-osteoporosis-rats
#2
Congyan Liu, Xia Gao, Yuping Liu, Mengmeng Huang, Ding Qu, Yan Chen
Icariin has a significant anti-osteoporotic activity, but its clinical application is limited due to a poor oral bioavailability especially under pathological conditions like osteoporosis. Based on the intestinal absorption and metabolism characteristics of icariin in the osteoporosis rats, a kind of simple enteric capsules containing icariin and snailase was designed to overcome this issue in this study. Snailase was secleted as the most efficient exogenous hydrolase of icariin and the related hydrolysis reaction parameters were optimized in the artificial intestinal liquid...
August 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28809448/improved-pharmacokinetic-and-pharmacodynamic-attributes-of-artemether-lumefantrine-loaded-solid-smedds-for-oral-administration
#3
Sameer Bhandari, Vikram Bhandari, Jatin Sood, Sunil Jaswal, Vikas Rana, Neena Bedi, Rakesh Sehgal, Ashok K Tiwary
OBJECTIVES: To evaluate the in-vivo efficacy of solid SMEDDS containing combination of artemether and lumefantrine. METHODS: Formulation development of solid SMEDDS containing combination of artemether and lumefantrine was carried out using spray drying technique. These S-SMEDDS were evaluated for reduction in parasitemia and mortality as well as subacute toxicity in mice. Haematology, biochemical parameters and histopathology were performed for evaluating safety of formulation...
August 15, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28809443/characterisation-in-vitro-and-in-vivo-evaluation-of-valproic-acid-loaded-nanoemulsion-for-improved-brain-bioavailability
#4
Suk Fei Tan, Brian P Kirby, Johnson Stanslas, Hamidon Bin Basri
OBJECTIVE: This study was aimed to investigate the potential of formulated valproic acid-encapsulated nanoemulsion (VANE) to improve the brain bioavailability of valproic acid (VPA). METHODS: Valproic acid-encapsulated nanoemulsions were formulated and physically characterised (osmolarity, viscosity, drug content, drug encapsulation efficiency). Further investigations were also conducted to estimate the drug release, cytotoxic profile, in-vitro blood-brain barrier (BBB) permeability, pharmacokinetic parameter and the concentration of VPA and VANE in blood and brain...
August 15, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28808917/development-of-a-translational-physiologically-based-pharmacokinetic-model-for-antibody-drug-conjugates-a-case-study-with-t-dm1
#5
Antari Khot, Jay Tibbitts, Dan Rock, Dhaval K Shah
Systems pharmacokinetic (PK) models that can characterize and predict whole body disposition of antibody-drug conjugates (ADCs) are needed to support (i) development of reliable exposure-response relationships for ADCs and (ii) selection of ADC targets with optimal tumor and tissue expression profiles. Towards this goal, we have developed a translational physiologically based PK (PBPK) model for ADCs, using T-DM1 as a tool compound. The preclinical PBPK model was developed using rat data. Biodistribution of DM1 in rats was used to develop the small molecule PBPK model, and the PK of conjugated trastuzumab (i...
August 14, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28808833/long-acting-ionically-paired-embonate-based-nanocrystals-of-donepezil-for-the-treatment-of-alzheimer-s-disease-a-proof-of-concept-study
#6
Naresh Mittapelly, Maharshi Thalla, Gitu Pandey, Venkatesh Teja Banala, Shweta Sharma, Abhishek Arya, Sandeep Mishra, Kalyan Mitra, Shubha Shukla, Prabhat Ranjan Mishra
PURPOSE: The aim of the present study was to prepare a patient friendly long acting donepezil (D) nanocrystals (NCs) formulation, with a high payload for i.m administration. As the native D hydrochloride salt has high aqueous solubility it is necessary to increase its hydrophobicity prior to the NCs formation. METHODS: D was ionically paired with embonic acid (E) in aqueous media and was successfully characterized using techniques like DSC, PXRD, FT-IR, NMR etc...
August 14, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28808600/simultaneous-determination-of-11-compounds-in-gualou-guizhi-granule-and-pharmacokinetics-study-by-uplc-ms-ms
#7
Chengtao Sun, Wen Xu, Yuqin Zhang, Lishuang Yu, Miao Ye, Kedan Chu, Wei Xu, Yu Lin
A rapid and sensitive ultrafast performance liquid chromatography-tandem mass spectrometry method (UPLC-MS/MS) was developed for the simultaneous determination of 11 compounds in Gualou Guizhi Granule (GLGZG), including liquiritin, isoliquiritin, liquirtin apioside, isoliquiritin apioside, liquiritigenin, isoliquiritigenin, glycyrrhizic acid, glycyrrhetinic acid, paeoniflorin, albiflorin, and paeoniflorin sulfonate in rat plasma. UPLC-MS/MS assay with negative ion mode was performed on a Waters CORTECS C18 (2...
2017: Journal of Analytical Methods in Chemistry
https://www.readbyqxmd.com/read/28807913/reducing-antibacterial-development-risk-for-gsk1322322-by-exploring-potential-human-dose-regimens-in-nonclinical-efficacy-studies-using-immunocompetent-rats
#8
Jennifer L Hoover, Christine M Singley, Philippa Elefante, Peter DeMarsh, Magdalena Zalacain, Stephen Rittenhouse
Directly testing proposed clinical dosing regimens in nonclinical studies can reduce risk during the development of novel antibacterial agents. Optimal dosing regimens can be identified in animal models by testing recreated human pharmacokinetic profiles. An example of this approach is presented using continuous intravenous infusions of GSK1322322 in immunocompetent rats to evaluate recreated Phase 1 human exposures in pneumonia models with Streptococcus pneumoniae and Haemophilus influenzae and an abscess model with Staphylococcus aureus GSK1322322 was administered via continuous intravenous infusion to recreate 1000 or 1500 mg oral doses every 12h in humans...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28807910/24-hour-pharmacokinetic-relationships-for-vancomycin-and-novel-urinary-biomarkers-of-acute-kidney-injury
#9
J Nicholas O'Donnell, Nathaniel J Rhodes, Thomas P Lodise, Walter C Prozialeck, Cristina M Miglis, Medha Joshi, Natarajan Venkatesan, Gwendolyn Pais, Cameron Cluff, Peter C Lamar, Seema Briyal, John Z Day, Anil Gulati, Marc H Scheetz
Introduction: Vancomycin has been associated with acute kidney injury in preclinical and clinical settings, however the precise exposure profiles associated with vancomycin induced acute kidney injury has not been defined. We sought to determine pharmacokinetic/pharmacodynamics indices associated with the development of acute kidney injury using sensitive urinary biomarkers.Methods: Male Sprague-Dawley rats received clinical grade vancomycin or normal saline as an intraperitoneal injection. Total daily doses between 0 and 400 mg/kg/day were administered as single or 2 divided doses over a 24-hour period...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28807905/pulmonary-pharmacokinetics-of-colistin-following-administration-of-dry-powder-aerosols-in-rats
#10
Yu-Wei Lin, Qi Tony Zhou, Yang Hu, Nikolas J Onufrak, Siping Sun, Jiping Wang, Alan Forrest, Hak-Kim Chan, Jian Li
Colistin has been administered via nebulization for the treatment of respiratory tract infections. Recently, dry powder inhalation (DPI) has attracted increasing attention. The current study aimed to investigate the pharmacokinetics (PK) of colistin in epithelial lining fluid (ELF) and plasma following DPI and intravenous (IV) administration in healthy Sprague-Dawley rats. Rats were given colistin as DPI intratracheally (0.66 and 1.32 mg base/kg) or IV injection (0.66 mg base/kg). Histopathological examination of lung tissue was performed at 24 h...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28805469/long-chain-triglycerides-based-self-nanoemulsifying-oily-formulations-sneofs-of-darunavir-with-improved-lymphatic-targeting-potential
#11
Babita Garg, Sarwar Beg, Ranjot Kaur, Rajendra Kumar, Om Prakash Katare, Bhupinder Singh
The current studies entail systematic development of SNEOFs containing long-chain triglycerides for improving lymphatic targeting of darunavir for complete inhibition of HIV progression. As per QbD-oriented approach for formulation development, the QTPP was defined and CQAs were earmarked. Preformulation equilibrium solubility and phase diagram studies, and risk assessment through FMEA studies identified Lauroglycol 90, Tween 80 and Transcutol HP as the lipid, emulgent and cosolvent, respectively, for formulating SNEOFs of darunavir...
August 14, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/28803882/changes-in-coumarin-kinetics-and-subcellular-localization-of-cyp2e1-contribute-to-bile-duct-damage-and-reduce-hepatocellular-damage-after-repeated-administration-of-coumarin-in-rats
#12
Yasuhiro Tanaka, Wataru Fujii, Hisako Hori, Yoshinori Kitagawa, Kiyokazu Ozaki
Coumarin exhibits different hepatotoxicity in rats depending on the administration frequency. To investigate the underlying mechanisms for the differences, we administered coumarin to rats as a single dose or repeatedly for 4 weeks. We found large increases in blood levels of liver enzymes and noticeable centrilobular hepatic necrosis after a single dose of coumarin. After repeated administration, enzyme levels mildly increased, while those of γ-GTP and total bilirubin significantly increased, suggesting bile duct damage...
August 10, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28803538/pharmacokinetics-of-tafamidis-a-transthyretin-amyloidosis-drug-in-rats
#13
Kyeong-Ryoon Lee, Jong-Woo Jeong, Hun-Chan Hyun, Jang Eunseo, Sunjoo Ahn Ahn, Sungwook Choi, Sang Hoon Joo, Sung-Sub Kim, Tae-Sung Koo
1. We characterized the pharmacokinetics of tafamidis, a novel drug to treat transthyretin-related amyloidosis, in rats after intravenous and oral administration at doses of 0.3-3 mg/kg. In vitro Caco-2 cell permeability and liver microsomal stability, as well as in vivo tissue distribution and plasma protein binding were also examined. 2. After intravenous injection, systemic clearance (CL), volumes of distribution at steady state (Vss), and half-life (T½) remained unaltered as a function of dose, with values in the ranges of 6...
August 14, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28802242/an-lc-ms-ms-method-for-simultaneous-determination-of-nine-steroidal-saponins-from-paris-polyphylla-var-in-rat-plasma-and-its-application-to-pharmacokinetic-study
#14
Guangyi Yang, Wei Lu, Meng Pan, Chenning Zhang, Yuan Zhou, Pei Hu, Ming Hu, Gao Song
Paris polyphylla var is an herbal plant herb widely used in Traditional Chinese Medicine. The purpose of this study is to develop an Ultra Performance Liquid Chromatography-tandem mass spectrometer (UPLC-MS) method to quantify the major components (i.e., nine saponins) from P. polyphylla in plasma samples. A UItra BiPh column (100×2.1mm, 5μm) was used with acetonitrile/0.1% formic acid in water as mobile phases. The analytes were quantified using a Waters XEVO TQ mass spectrometer via multiple reaction monitoring (MRM) with positive scan mode...
August 1, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28802219/development-and-validation-of-a-high-performance-liquid-chromatography-tandem-mass-spectrometry-method-to-quantify-ly-354-740-in-rat-and-marmoset-plasma
#15
Fleur Gaudette, Adjia Hamadjida, Dominique Bédard, Stephen G Nuara, Francis Beaudry, Philippe Huot
LY-354,740 (eglumegad) is a selective and potent agonist of the metabotropic glutamate group II receptors (mGluR2,3) that has already entered clinical trials as a potential anti-psychotic agent and therefore has well-documented pharmacokinetic (PK), safety and tolerability profiles in human. Whereas its development as an anti-psychotic agent has not been pursued, LY-354,740 may have potential in other neuroscience-related fields, notably anxiety and neuro-protection. The common marmoset is a small primate that has long been used in neuroscience...
July 15, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28802217/comparatively-evaluating-the-pharmacokinetic-of-fifteen-constituents-in-normal-and-blood-deficiency-rats-after-oral-administration-of-xin-sheng-hua-granule-by-uplc-ms-ms
#16
Han-Qing Pang, Yu-Ping Tang, Yu-Jie Cao, Ya-Jie Tan, Yi Jin, Xu-Qin Shi, Sheng-Liang Huang, Da-Zheng Sun, Jin Sun, Zhi-Shu Tang, Jin-Ao Duan
Xin-Sheng-Hua Granule (XSHG), a famous traditional Chinese medicine prescription, are clinically applied for the treatment of postpartum disease through nourishing blood and promoting blood circulation. In this investigation, a multi-constituents (trigonelline, stachydrine hydrochloride, hydroxysafflor yellow A, chlorogenic acid, amygdalin, leonurine, liquiritin, ferulic acid, senkyunolide I, senkyunolide H, glycyrrhizic acid, senkyunolide A, ligustilide, butylidenephthalide and glycyrrhetinic acid) pharmacokinetic study of XSHG was conducted for the first time...
July 30, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28801971/pharmacokinetics-and-metabolism-of-olerciamide-a-from-portulaca-oleracea-l-in-rats-by-uhplc-uv-and-uhplc-esi-q-tof-ms
#17
Zheming Ying, Cuiyu Li, Mingzhe Gao, Xixiang Ying, Guanlin Yang
The aim of this study was to elucidate the pharmacokinetics of olerciamide A in rats after oral and intravenous administration of P. oleracea L. extract (POE) by a simple and rapid ultra high-performance liquid chromatography (UHPLC) method with bergapten as internal standard (IS). The pharmacokinetic results indicated that olerciamide A was rapidly distributed with Tmax of 30 min after oral administration and presented a low oral absolute bioavailability to be 4.57 %. The metabolism of olerciamide A in rats was also investigated using ultra-high performance liquid chromatography electrospray coupled with quadrupole-time of flight mass spectrometry (UHPLC-ESI-Q-TOF/MS) to elucidate the reason of the low absolute bioavailability of olerciamide A and 7 metabolites of oleraciamide A were found in rat plasma and urine...
August 12, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28800523/quantification-of-cyclocreatine-in-mouse-and-rat-plasma-using-hydrophilic-interaction-ultra-performance-liquid-chromatography-tandem-mass-spectrometry
#18
Amy Q Wang, Emma Hughes, Wenwei Huang, Edward H Kerns, Xin Xu
An accurate, rapid and selective method was developed to quantify cyclocreatine in mouse and rat plasma using hydrophilic interaction (HILIC) ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). The plasma samples were prepared by protein precipitation with acetonitrile:methanol (70:30). Chromatographic separation was performed on a HILIC BEH amide column (2.1mm×50mm, 1.7μm) with a 3min gradient elution at a flow rate of 0.5mL/min. For mass spectrometric detection, selected reaction monitoring (SRM) was used; the SRM transitions were m/z 144→98 and m/z 144→56 for cyclocreatine and m/z 148→102 for the internal standard (D4-cyclocreatine) in the positive ionization mode...
July 31, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28799733/supercritical-fluid-chromatography-coupled-with-tandem-mass-spectrometry-a-high-efficiency-detection-technique-to-quantify-taxane-drugs-in-whole-blood-samples
#19
Chan Jin, Jibin Guan, Dong Zhang, Bing Li, Hongzhuo Liu, Zhonggui He
We present a technique to rapid determine taxane in blood samples by supercritical fluid chromatography together with mass spectrometry. The aim of this study was to develop a supercritical fluid chromatography with mass spectrometry method for the analysis of paclitaxel, cabazitaxel and docetaxel in whole-blood samples of rats. Liquid-dry matrix spot extraction was selected in sample preparation procedure. Supercritical fluid chromatography separation of paclitaxel, cabazitaxel, docetaxel and glyburide (internal standard) was accomplished within 3 min by using the gradient mobile phase consisted of methanol as the compensation solvent and carbon dioxide at a flow rate of 1...
August 11, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28796496/discovery-of-clinical-candidate-n-1s-1-3-fluoro-4-trifluoromethoxy-phenyl-2-methoxyethyl-7-methoxy-2-oxo-2-3-dihydropyrido-2-3-b-pyrazine-4-1h-carboxamide-tak-915-a-highly-potent-selective-and-brain-penetrating-phosphodiesterase-2a-inhibitor-for-the-treatment
#20
Satoshi Mikami, Shinji Nakamura, Tomoko Ashizawa, Izumi Nomura, Masanori Kawasaki, Shigekazu Sasaki, Hideyuki Oki, Hironori Kokubo, Isaac D Hoffman, Hua Zou, Noriko Uchiyama, Kosuke Nakashima, Naomi Kamiguchi, Haruka Imada, Noriko Suzuki, Hiroki Iwashita, Takahiko Taniguchi
Phosphodiesterase (PDE) 2A inhibitors have emerged as a novel mechanism with potential therapeutic option to ameliorate cognitive dysfunction in schizophrenia or Alzheimer's disease through upregulation of cyclic nucleotides in the brain, and thereby achieve potentiation of cyclic nucleotide signaling pathways. This article details the expedited optimization of our recently disclosed pyrazolo[1,5-a]pyrimidine lead compound 4b, leading to the discovery of clinical candidate 36 (TAK-915), which demonstrates an appropriate combination of potency, PDE selectivity, and favorable pharmacokinetic (PK) properties, including brain penetration...
August 10, 2017: Journal of Medicinal Chemistry
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