Search results for "Ibuprofen"
showing 10 items of 60 documents
Identification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin.
2017
A single high-affinity fatty acid binding site in the important human transport protein serum albumin (HSA) is identified and characterized using an NBD (7-nitrobenz-2-oxa-1,3-diazol-4-yl)-C12 fatty acid. This ligand exhibits a 1:1 binding stoichiometry in its HSA complex with high site-specificity. The complex dissociation constant is determined by titration experiments as well as radioactive equilibrium dialysis. Competition experiments with the known HSA-binding drugs warfarin and ibuprofen confirm the new binding site to be different from Sudlow-sites I and II. These binding studies are extended to other albumin binders and fatty acid derivatives. Furthermore an X-ray crystal structure …
Effects of ibuprofen and carbamazepine on the ion transport system and fatty acid metabolism of temperature conditioned juveniles of Solea senegalens…
2018
The increasing presence of pharmaceuticals in aquatic environments in the last decades, derived from human and veterinary use, has become an important environmental problem. Previous studies have shown that ibuprofen (IB) and carbamazepine (CBZ) modify physiological and biochemical processes in Senegalese sole (Solea senegalensis) in a temperature-dependent manner. In other vertebrates, there is evidence that both of these pharmaceuticals interfere with the ‘arachidonic acid (AA) cascade’, which is responsible for the biosynthesis of numerous enzymes that are involved in the osmoregulatory process. The present work aims to study the temperature-dependent effects of these two pharmaceuticals…
A Comprehensive Spectroscopic Analysis of the Ibuprofen Binding with Human Serum Albumin, Part I
2020
Human serum albumin (HSA) plays a fundamental role in the human body. It takes part in the transport of exogenic and endogenic substances, especially drugs. Ibuprofen (IBU) is one of the most commonly used non-steroidal anti-inflammatory drugs, used for pain relief, fever relief, and for anti-inflammatory purposes. The binding of ligands with HSA is a significant factor which determines the toxicity and the therapeutic dosages of these substances. The aim of this study was to compare the degree of ibuprofen binding with human serum albumin at various temperatures and protein solution pH values. In order to evaluate conformational changes in HSA caused by interaction with ibuprofen, spectrop…
Efectos de la hiperamonemia y la encefalopatía hepática sobre la conectividad neuronal en cerebro de pacientes cirróticos y modelos animales. Implica…
2018
La encefalopatía hepática (HE) es un complejo síndrome neuropsiquiátrico producido por la alteración en la función del sistema nervioso central asociada a la cirrosis hepática. Entre un 33-55% de los pacientes cirróticos sin síntomas clínicos evidentes de EH padecen encefalopatía hepática mínima (EHM) con deterioro cognitivo leve que empeora su calidad y esperanza de vida. Los pacientes cirróticos con EHM presentan alteraciones en la generación del potencial MMN (Mismatch Negativity), concretamente una disminución del área bajo la curva del potencial, que se correlaciona con los déficits de atención. En esta tesis hemos demostrado que las ratas con hiperamonemia crónica reproducen las alter…
A novel technique for intraduodenal administration of drug suspensions/solutions with concurrent pH monitoring applied to ibuprofen formulations
2019
Characterization of dissolution of solid suspended drug particles in vivo is important for developing biopredictive in vitro tests. Therefore, methods to gain deeper insights into particle dissolution in vivo are needed. The soft Bioperm intubation method, a well established tool for investigation of permeability, absorption, metabolism, and drug interactions at predefined locations in the gastroinstinal tract, was modified. The novel intubation method involved pump-controlled infusion of pharmaceutical suspensions as well as simultaneous pH monitoring. This technique was used in a proof of concept study in healthy humans. Plasma sampling and non-compartmental analysis allowed comparison of…
Endogenous opioid peptide responses to opioid and anti-inflammatory medications following eccentric exercise-induced muscle damage.
2009
To determine the effects of Vicoprofen, Ibuprofen, and a placebo on the responses of endogenous opioid peptides following eccentric exercise-induced muscle damage 36 healthy men (age: 22.8 years; height: 178.8+/-6.2cm; body mass: 78.9+/-13.7kg; body fat: 15.8+/-6.5%) volunteered to participate in the study. Each participant was evaluated for pain 24h post and randomly assigned to an experimental group: VIC (Vicoprofen), IBU (Ibuprofen), or P (placebo). Medication was given four times daily (i.e., VIC (hydrocodone bitartrate 7.5mg with Ibuprofen 200mg) and IBU 200mg). Blood was obtained at rest and at 0, 24, 48, 72, 96 and 120h following the eccentric exercise damage protocol. No significant…
Factors associated with efficacy of an ibuprofen/pseudoephedrine combination drug in pharmacy customers with common cold symptoms
2016
SummaryAim The aim of this study was to explore factors affecting efficacy of treatment of common cold symptoms with an over-the-counter ibuprofen/pseudoephedrine combination product. Methods Data from an anonymous survey among 1770 pharmacy customers purchasing the combination product for treatment of own common cold symptoms underwent post-hoc descriptive analysis. Scores of symptoms typically responsive to ibuprofen (headache, pharyngeal pain, joint pain and fever), typically responsive to pseudoephedrine (congested nose, congested sinus and runny nose), considered non-specific (sneezing, fatigue, dry cough, cough with expectoration) and comprising all 11 symptoms were analysed. Multiple…
Resolving Binding Events on the Multifunctional Human Serum Albumin
2020
Abstract Physiological processes rely on initial recognition events between cellular components and other molecules or modalities. Biomolecules can have multiple sites or mode of interaction with other molecular entities, so that a resolution of the individual binding events in terms of spatial localization as well as association and dissociation kinetics is required for a meaningful description. Here we describe a trichromatic fluorescent binding‐ and displacement assay for simultaneous monitoring of three individual binding sites in the important transporter and binding protein human serum albumin. Independent investigations of binding events by X‐ray crystallography and time‐resolved dyn…
In vitro prediction of in vivo absorption of ibuprofen from suspensions through rational choice of dissolution conditions
2020
Two ibuprofen suspension formulations were investigated for their dissolution in various bicarbonate, phosphate and acetate buffers. Phosphate and acetate gave faster release than bicarbonate at comparable molarities. Nevertheless, mass transport modelling using the reversible non-equilibrium (RNE) approach enabled the calculation of phosphate molarities that gave good matches to physiological bicarbonate in terms of ibuprofen dissolution. This shows that developing surrogate buffers for bicarbonate that are devoid of the technical difficulties associated with the bicarbonate-CO2 systems is possible. In addition, the intestinal dissolution kinetics of the tested suspensions were determined …
Comparison of different removal techniques for selected pharmaceuticals
2015
[EN] Recently, there is an emergence of endocrine-disrupting compounds, pharmaceuticals, and personal care products (EDC/PPCPs) as important pollutants to remove from drinking water and reclaimed wastewater. In this work, the efficiency of removing pharmaceuticals (PCs) from model aqueous solutions and raw wastewater with ultrafiltration (UF), nanofiltration (NF), activated carbon adsorption (AC), biological methods (SBR) and oxidation with ClO2 was investigated. Some treatments have also been used as combined processes: UF + NF, UF +AC, SBR + ClO2. Ibuprofen, Acetaminophen, Diclofenac, Sulfamethoxazole, Clonazepam, and Diazepam were selected as model compounds. In order to evaluate their r…