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Hplc pharmacokinetics

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https://www.readbyqxmd.com/read/27920527/pharmacokinetics-and-safety-of-dts-108-a-human-oligopeptide-bound-to-sn-38-with-an-esterase-sensitive-cross-linker-in-patients-with-advanced-malignancies-a-phase-i-study
#1
Romain Coriat, Sandrine J Faivre, Olivier Mir, Chantal Dreyer, Stanislas Ropert, Mohammed Bouattour, Robert Desjardins, François Goldwasser, Eric Raymond
BACKGROUND: DTS-108 is a hydrosoluble prodrug, where the SN-38 moiety is covalently linked to a 20-amino acid vector peptide by a specific esterase-sensitive cross-linker, releasing 7-ethyl-10-hydroxycampthotecin (SN-38) by esterase bond cleavage. METHODS: The pharmacokinetics of DTS-108, adverse events graded according to NCI-CTCv3.1, dose-limiting toxicities at cycle 1, the maximum tolerated dose (MTD), and the recommended Phase II dose (RP2D) of intravenous DTS-108 (1-2 hours) every 2 weeks were evaluated in a first-in-human Phase I study in patients with advanced/metastatic carcinomas, according to an accelerated dose escalation design...
2016: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/27913584/nitro-fatty-acid-pharmacokinetics-in-the-adipose-tissue-compartment
#2
Marco Fazzari, Nicholas K H Khoo, Steven R Woodcock, Diane K Jorkasky, Lihua Li, Francisco J Schopfer, Bruce A Freeman
Electrophilic nitro-fatty acids (NO2-FAs) promote adaptive and anti-inflammatory cell signaling responses as a result of an electrophilic character that supports post-translational protein modifications. A unique pharmacokinetic profile is expected for NO2-FAs because of an ability to undergo reversible reactions including Michael additions with biological cysteine-containing proteins and esterification into complex lipids. Herein we report via quantitative whole-body autoradiography analysis of rats gavaged with radiolabeled 10-nitro-[14C]oleic acid, preferential accumulation in adipose tissue over two weeks...
December 2, 2016: Journal of Lipid Research
https://www.readbyqxmd.com/read/27907869/is-a-deuterated-internal-standard-appropriate-for-the-reliable-determination-of-olmesartan-in-human-plasma
#3
Edyta Piórkowska, Jacek Musijowski, Katarzyna Buś-Kwaśnik, Piotr J Rudzki
A right choice of the internal standard is one of the most challenging tasks during bioanalytical method development. Surprisingly, among the HPLC-MS methods for the determination of a cardiovascular drug olmesartan in plasma only structural analogues or similar compounds were used as internal standards. We have tried to answer the question whether the stable isotope labelled (deuterated) internal standard, as recommended by regulatory agencies, can be used for the reliable determination of olmesartan in human plasma...
November 16, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/27900470/influence-of-the-selective-antagonist-of-the-nr2b-subunit-of-the-nmda-receptor-traxoprodil-on-the-antidepressant-like-activity-of-desipramine-paroxetine-milnacipran-and-bupropion-in-mice
#4
Weronika Stasiuk, Aleksandra Szopa, Anna Serefko, Elżbieta Wyska, Katarzyna Świąder, Jarosław Dudka, Piotr Wlaź, Ewa Poleszak
Pre-clinical and clinical studies indicated that a blockade of the NMDA receptor complex creates new opportunities for the treatment of affective disorders, including depression. The aim of the present study was to assess the influence of traxoprodil (10 mg/kg) on the activity of desipramine (10 mg/kg), paroxetine (0.5 mg/kg), milnacipran (1.25 mg/kg), and bupropion (10 mg/kg), each at sub-therapeutic doses. Moreover, brain levels of traxoprodil and tested agents were determined using HPLC. The obtained results were used to ascertain the nature of occurring interaction between traxoprodil and studied antidepressants...
November 29, 2016: Journal of Neural Transmission
https://www.readbyqxmd.com/read/27891231/a-pharmacokinetic-evaluation-and-metabolite-identification-of-the-ghb-receptor-antagonist-ncs-382-in-mouse-informs-novel-therapeutic-strategies-for-the-treatment-of-ghb-intoxication
#5
Garrett R Ainslie, K Michael Gibson, Kara R Vogel
Gamma-aminobutyric acid (GABA) is an endogenous inhibitory neurotransmitter and precursor of gamma-hydroxybutyric acid (GHB). NCS-382 (6,7,8,9-tetrahydro-5-hydroxy-5H-benzo-cyclohept-6-ylideneacetic acid), a known GHB receptor antagonist, has shown significant efficacy in a murine model of succinic semialdehyde dehydrogenase deficiency (SSADHD), a heritable neurological disorder featuring chronic elevation of GHB that blocks the final step of GABA degradation. NCS-382 exposures and elimination pathways remain unknown; therefore, the goal of the present work was to obtain in vivo pharmacokinetic data in a murine model and to identify the NCS-382 metabolites formed by mouse and human...
December 2016: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/27881236/deferasirox-pharmacokinetics-evaluation-in-a-woman-with-hereditary-haemochromatosis-and-heterozygous-%C3%AE-thalassaemia
#6
Sarah Allegra, Silvia De Francia, Filomena Longo, Davide Massano, Jessica Cusato, Arianna Arduino, Elisa Pirro, Antonio Piga, Antonio D'Avolio
We present the deferasirox pharmacokinetics evaluation of a female patient on iron chelation, for the interesting findings from her genetic background (hereditary haemochromatosis and heterozygous β-thalassaemia) and clinical history (ileostomy; iron overload from transfusions). Drug plasma concentrations were measured by an HPLC-UV validated method, before and after ileum resection. Area under deferasirox concentration curve over 24h (AUC) values were determined by the mixed log-linear rule, using Kinetica software...
November 20, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27879193/pharmacokinetic-comparison-of-two-formulations-of-talniflumate-370%C3%A2-mg-tablets-in-healthy-korean-volunteers%C3%A2
#7
Yun Kim, Sung- Yim, Bo-Hyung Kim, SeungHwan Lee
BACKGROUND: Talniflumate, a prodrug of niflumic acid, is a potent analgesic and anti-inflammatory drug that has been widely used for the treatment of rheumatoid diseases. OBJECTIVE: The aim of this study was to compare the pharmacokinetics and to evaluate the bioequivalence of two formulations of talniflumate 370 mg tablets (test formulation: Flumagen® 370 mg tablet; reference formulation: Somalgen® 370 mg tablet). METHODS: A randomized, open-label, single dose, two-sequence, two-period crossover clinical study was conducted...
November 23, 2016: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27872700/pharmacokinetic-study-of-furosemide-incorporated-plga-microspheres-after-oral-administration-to-rat
#8
Katayoun Derakhshandeh, Moin Karimi, Abbas Hemati Azandaryani, Gholamreza Bahrami, Kiumras Ghanbari
OBJECTIVES: The purpose of the current study was to assess the feasibility of microspheres from biocompatible polymer for oral bioavailability (BA) enhancement of potent sulfonamide- type loop diuretic- Furosemide - which used in the treatment of congestive heart failure, caused edema, cirrhosis, renal disease and as an adjunct in acute pulmonary edema. The comparatively poor and inconstant BA of furosemide, which occurs site-specifically in the stomach and upper small intestine, has been ascribed to the poor dissolution of furosemide...
October 2016: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/27867277/characterization-and-bioavailability-study-of-baicalin-mesoporous-carbon-nanopowder-solid-dispersion
#9
Li Cui, E Sune, Jie Song, Jing Wang, Xiao-Bin Jia, Zhen-Hai Zhang
BACKGROUND: Baicalin is the main bioactive constitute of the dried roots of Scutellaria baicalensis and possesses various biological activities. However, the poor water solubility and low oral bioavailability limit its efficacy. OBJECTIVE: The present study was conducted to enhance the dissolution and oral bioavailability of baicalin (BA) through a novel mesoporous carbon nanopowder (MCN) drug carrier. MATERIALS AND METHODS: Solid dispersions (SDs) of BA with MCN were prepared using a solvent evaporation method...
October 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27867275/improved-oral-bioavailability-of-total-flavonoids-of-dracocephalum-moldavica-via-composite-phospholipid-liposomes-preparation-in-vitro-drug-release-and-pharmacokinetics-in-rats
#10
Cheng Zeng, Wen Jiang, Meie Tan, Jianguo Xing, Chenghui He
BACKGROUND: Dracocephalum moldavica L is a traditional Uygur medicine for centuries, total flavonoids extracted from Dracocephalum moldavica are the major active ingredients of herbs, which possesses significant medicinal values to treat coronart disease and hypertension, due to the glycosyl group on the ring, total flavonoids of Dracocephalum moldavica has low hydrophilic and poorly absorbed after oral administration, so one way is the formulation of poorly water soluble and permeabledrugs with lipids containing formulations such as Composite phospholipid liposomes to improve the absorption profile of drug...
October 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27867020/a-randomized-dose-escalation-study-of-intravenous-baclofen-in-healthy-volunteers-clinical-tolerance-and-pharmacokinetics
#11
Natalie S Schmitz, Linda E Krach, Lisa D Coles, Usha Mishra, Suresh K Agarwal, James C Cloyd, Robert L Kriel
BACKGROUND: Abrupt discontinuation of baclofen can result in a potentially severe withdrawal syndrome. The current treatment for baclofen withdrawal is inadequate, resulting in a critical need to develop an alternative method to prevent or treat this withdrawal syndrome. OBJECTIVE: To evaluate the safety profile and pharmacokinetics of oral (PO) and investigational intravenous (IV) baclofen formulations at clinically relevant doses. DESIGN: Randomized, open-label, dose escalation, crossover study SETTING: Contract Research Organization (CRO) METHODS: Three cohorts of 12 healthy adults received single doses of PO baclofen (10mg, 15 mg or 20 mg) and 10-minute infusions of IV baclofen (7...
November 17, 2016: PM & R: the Journal of Injury, Function, and Rehabilitation
https://www.readbyqxmd.com/read/27864843/measurement-of-caffeine-and-its-three-primary-metabolites-in-human-plasma-by-hplc-esi-ms-ms-and-clinical-application
#12
Feng Chen, Zhe-Yi Hu, Robert B Parker, S Casey Laizure
Caffeine is a mild stimulant with significant potential for abuse being consumed in larger doses with the widespread availability of energy drinks and by novel routes of administration such as inspired powder, oral sprays, and electronic cigarettes. How these recent changes in caffeine consumption affecting caffeine disposition and abuse potential is of growing concern. In the study of caffeine disposition in humans, it is common to only measure the caffeine concentration; however, caffeine's three major metabolites (paraxanthine, theobromine, and theophylline) retain central nervous system stimulant activity that may contribute to the overall pharmacological activity and toxicity...
November 18, 2016: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/27864660/effects-of-cyp2c9-genetic-polymorphisms-on-the-pharmacokinetics-of-celecoxib-and-its-carboxylic-acid-metabolite
#13
Se-Hyung Kim, Do-Hoon Kim, Ji-Yeong Byeon, Young-Hoon Kim, Dong-Hyun Kim, Hye-Jin Lim, Choong-Min Lee, Sang Sup Whang, Chang-Ik Choi, Jung-Woo Bae, Yun Jeong Lee, Choon-Gon Jang, Seok-Yong Lee
Celecoxib, a selective cyclooxygenase (COX)-2 inhibitor, is used for the treatment of rheumatoid arthritis and osteoarthritis. The predominant hepatic metabolism of celecoxib to celecoxib carboxylic acid (CCA) is mediated mainly by CYP2C9. We investigated the effects of the major CYP2C9 genetic variants in Asian populations, CYP2C9*3 and CYP2C9*13, on the pharmacokinetics of celecoxib and its carboxylic acid metabolite in healthy Korean subjects. A single 200-mg oral dose of celecoxib was given to 52 Korean subjects with different CYP2C9 genotypes: CYP2C9EM (n = 26; CYP2C9*1/*1), CYP2C9IM (n = 24; CYP2C9*1/*3 and *1/*13), and CYP2C9PM (n = 2; CYP2C9*3/*3)...
November 18, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27859251/a-randomized-two-way-crossover-bioequivalence-study-in-healthy-adult-volunteers-of-paediatric-zidovudine-lamivudine-nevirapine-fast-disintegrating-fixed-dose-combination-tablet
#14
Anjali Joshi, Daniel Gbadero, Fredrick Esseku, Olufikayo J Adesanya, Moji C Adeyeye
OBJECTIVE: The bioequivalence study was conducted to compare the developed paediatric fixed-dose combination (FDC) zidovudine/lamivudine/nevirapine (60/30/50 mg) tablet - the test formulation - with the combined mixture of single-entity innovator products (reference product). METHODS: A single-dose open-label randomized two-way crossover study was conducted in healthy adult African volunteers after an informed consent was obtained. The 24 volunteers, divided into two groups, were administered the products after an overnight fast on two treatment days with 14 days of washout period...
November 18, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27856301/sulfur-fumigation-reducing-systemic-exposure-of-ginsenosides-and-weakening-immunomodulatory-activity-of-ginseng
#15
Bin Ma, Winnie Lai Ting Kan, He Zhu, Song-Lin Li, Ge Lin
ETHNOPHARMACOLOGICAL RELEVANCE: Ginseng (Ginseng Radix et Rhizoma) is used worldwide for its miracle tonic effects, especially for its immunomodulatory activities. Sulfur fumigation, a fast and convenient method to prevent pesticidal and bacterial contamination in the food industry, has been recently employed during post-harvest processing of ginseng. Our previous studies demonstrated that sulfur fumigation significantly altered the chemical profile of the bioactive ingredients in ginseng...
November 15, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27854438/preparation-and-evaluation-of-indomethacin-loaded-alginate-microspheres
#16
Penjuri Subhash Chandra Bose, Ravouru Nagaraju, Damineni Saritha, Budumuru Padmasri, Poreddy Srikanth Reddy
Indomethacin-loaded alginate microspheres were prepared by the ionic cross linking technique using calcium chloride. The effect of calcium chloride concentration was evaluated with respect to the size, entrapment efficiency and shape (sphericity) of the particles. The entrapment efficiency and in vitro release profiles were found to be altered by changing various formulation parameters. The desired indomethacin in vitro release profile (as per USP specifications for extended release formulations) was obtained from microspheres prepared from gel containing 2% of sodium alginate and 2% of methyl cellulose hardened in 3% calcium chloride solution...
2016: Ceská a Slovenská Farmacie
https://www.readbyqxmd.com/read/27854256/natural-deep-eutectic-solvents-nades-as-a-tool-for-bioavailability-improvement-pharmacokinetics-of-rutin-dissolved-in-proline-glycine-after-oral-administration-in-rats-possible-application-in-nutraceuticals
#17
Marta Faggian, Stefania Sut, Beatrice Perissutti, Valeria Baldan, Iztok Grabnar, Stefano Dall'Acqua
There is a need for innovation in plant-derived pharmaceuticals, food supplements and nutraceutical products regarding the use of more eco-sustainable solvents for their extraction. Furthermore, the poor oral bioavailability of several phytochemicals with health promoting effects stimulates the research in the field of pharmaceutical formulations. Natural Deep Eutectic Solvents (NADES) are formed by natural compounds, and can be considered as future solvents being especially useful for the preparation of nutraceuticals and food-grade extracts...
November 14, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27847337/herb-drug-interaction-of-andrographis-paniculata-nees-extract-and-andrographolide-on-pharmacokinetic-and-pharmacodynamic-of-naproxen-in-rats
#18
Aishwarya Balap, Sathiyanarayanan Lohidasan, Arulmozhi Sinnathambi, Kakasaheb Mahadik
ETHNOPHARMACOLOGICAL RELEVANCE: Andrographis paniculata Nees (Acanthacae) have broad range of pharmacological effects such as hepatoprotective, antifertility, antimalarial, antidiabetic, suppression of various cancer cells and anti-inflammatory properties and is widely used medicinal plant in the traditional Unani and Ayurvedic medicinal systems. Andrographolide (AN) is one of the active constituent of the A. paniculata Nees extract (APE). They have been found in many traditional herbal formulations in India and proven to be effective as anti-inflammatory drug...
November 12, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27846855/changes-in-ceftriaxone-pharmacokinetics-pharmacodynamics-during-the-early-phase-of-sepsis-a-prospective-experimental-study-in-the-rat
#19
Valentina Selmi, Beatrice Loriga, Luca Vitali, Martina Carlucci, Alessandro Di Filippo, Giulio Carta, Eleonora Sgambati, Lorenzo Tofani, Angelo Raffaele De Gaudio, Andrea Novelli, Chiara Adembri
BACKGROUND: Sepsis is characterized by the loss of the perm-selectivity properties of the glomerular filtration barrier (GFB) with consequent albuminuria. We examined whether the pharmacokinetics-pharmacodynamics (PK/PD) of ceftriaxone (CTX), an extensively protein-bound 3rd generation cephalosporin, is altered during early sepsis and whether an increase in urinary loss of bound-CTX, due to GFB alteration, can occur in this condition. METHODS: A prospective, experimental, randomized study was carried out in adult male Sprague-Dawley rats...
November 15, 2016: Journal of Translational Medicine
https://www.readbyqxmd.com/read/27835937/fractional-laser-assisted-topical-delivery-leads-to-enhanced-accelerated-and-deeper-cutaneous-5-fluorouracil-uptake
#20
Emily Wenande, Uffe H Olesen, Mette M B Nielsen, Christian Janfelt, Steen Honoré Hansen, Rox Anderson, Merete Haedersdal
BACKGROUND: Topical 5-Fluorouracil (5-FU) exhibits suboptimal efficacy for non-melanoma skin cancer, attributed to insufficient intracutaneous penetration. This study investigates the impact of ablative fractional laser (AFXL) at different laser-channel depths on cutaneous 5-FU pharmacokinetics and biodistribution. METHODS: In vitro porcine skin underwent AFXL-exposure using a fractional 10,600nm CO2-laser, generating microscopic ablation zones (MAZ) reaching the dermoepidermal junction (MAZ-ED), superficial-(MAZ-DS), or mid-dermis(MAZ-DM)...
November 11, 2016: Expert Opinion on Drug Delivery
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