Search results for "absorption."
showing 10 items of 2682 documents
Impact of nutritional status on the pharmacokinetics of erlotinib in rats
2015
Malnourishment is a complex condition in which physiopathological changes take place in multiple systems as a result of energy, protein and nutrient deficiency. The purpose of this study was to evaluate, using an experimental animal model, the impact of nutritional status on the pharmacokinetic profile of erlotinib, a reversible, highly selective, human epidermal growth factor receptor (HER1/EGFR) tyrosine kinase inhibitor. Two groups of rats -WN (well-nourished) and UN (undernourished) - were fed with different diets for 23-26 days. Rats were assigned randomly to one of three erlotinib treatments (n = 42) consisting of a single dose administered intravenously (i.v.), via oral solution or v…
Influence of Rhein on Rat Colonic Na<sup>+</sup>, K<sup>+</sup>-ATPase and Permeability in vitro
1988
Rhein, an aglucone of a laxative-acting anthraquinone, which induces net secretion in the human jejunum and colon, does not induce net secretion under open circuit current in in vitro conditions but r
Estabilidad en suero fisiológico del busulfán intravenoso en un envase de poliolefinas
2008
Introduction: Although it has been used orally, the variability in its absorption and the risk of causing vomiting has lead to a push towards the intravenous use of bulsulfan. This study looks at the stability of 60 mg of busulfan, in fixed volumes of 250 mL (0.24 mg/mL) and 500 mL (0.12 mg/mL) of serum and different conservation conditions, in a new plastic pack made from polyolefin/polyamide laminates. Material and methods: High-efficiency liquid chromatography with ultraviolet detection was used to determine the concentration of busulfan derivate with sodium diethyldithiocarbamatetrihydrate. Stability was assessed for both concentrations; refrigerated and at room temperature, using the t…
Nonlinear intestinal absorption kinetics of cefuroxime axetil in rats.
1997
Cefuroxime is commercially available for parenteral administration as a sodium salt and for oral administration as cefuroxime axetil, the 1-(acetoxy)ethyl ester of the drug. Cefuroxime axetil is a prodrug of cefuroxime and has little, if any, antibacterial activity until hydrolyzed in vivo to cefuroxime. In this study, the absorption of cefuroxime axetil in the small intestines of anesthetized rats was investigated in situ, by perfusion at four concentrations (11.8, 5, 118 and 200 microM). Oral absorption of cefuroxime axetil can apparently be described as a specialized transport mechanism which obeys Michaelis-Menten kinetics. Parameters characterizing absorption of prodrug in free solutio…
Evidence of a flip-flop phenomenon in acamprosate pharmacokinetics: an in vivo study in rats.
2006
The pharmacokinetics of acamprosate were examined in the rat after oral and intravenous administration in order to detect the possible presence of a flip-flop phenomenon. Rats received 9.3 or 73.3 mg/kg of the drug as an intravenous bolus. The same doses were orally administered via gastric intubation. Plasma samples were taken from the jugular vein for determination of acamprosate concentration by liquid scintillation counting. The drug content was also quantified in urine and faeces. The acamprosate bioavailability was close to 20%, the amount recovered in the faeces being around 80% of the administered dose. The terminal slope of the oral plasma curve was significantly lower than that ob…
A topological sub-structural approach for predicting human intestinal absorption of drugs.
2004
The human intestinal absorption (HIA) of drugs was studied using a topological sub-structural approach (TOPS-MODE). The drugs were divided into three classes according to reported cutoff values for HIA. "Poor" absorption was defined as HIAor =30%, "high" absorption as HIAor =80%, whereas "moderate" absorption was defined between these two values (30%HIA79%). Two linear discriminant analyses were carried out on a training set of 82 compounds. The percentages of correct classification, for both models, were 89.02%. The predictive power of the models were validated by three test: a leave-one-out cross validation procedure (88.9% and 87.9%), an external prediction set of 127 drugs (92.9% and 80…
Beneficial effects of l-carnitine in myoblastic C2C12 cells
2003
L-Carnitine is a key molecule in the transfer of fatty acid across mitochondrial membranes. Bioavailable L-carnitine is either provided by an endogeneous biosynthesis or after intestinal absorption of dietary items containing L-carnitine. After intestinal absorption or hepatic biosynthesis, L-carnitine is transferred to organs whose metabolism is dependent upon fatty acid oxidation, such as skeletal muscle. To cross the muscle plasma membrane, there are several transporters involved. Among those transporters, OCTN2 is actually the only one to have been clearly characterized. Zidovudine is a commonly used inhibitor of human immunodeficiency virus (HIV) replication. Zidovudine has many side e…
The Prediction of Human Intestinal Absorption Based on the Molecular Structure
2014
Human Intestinal Absorption (HIA) has been modeled many times by using classification models. However, regression models are scarce. Here, Artificial Neural Networks (ANNs) are implemented for this purpose. A dataset of structurally diverse chemicals with their respective experimental HIA were used to design robust, true predictive and widespread applicable ANN models. An input variables pool was made up of structural invariants calculated by using either Dragon or our software Desmol 1. The selection of best variables was performed following three steps using the entire dataset of molecules. Firstly, variables poorly correlated with the experimental data were eliminated. Secondly, input va…
High-pressure, high-temperature phase diagram of InSe: A comprehensive study of the electronic and structural properties of the monoclinic phase of I…
2006
We report on an investigation of the high-pressure, high-temperature phase diagram of InSe. We optically observed the phase transition from the rhombohedral polytype (InSe-I) to the monoclinic phase (InSe-II) and determined the phase boundary up to $10\phantom{\rule{0.3em}{0ex}}\mathrm{GPa}$. High-pressure resistivity measurements were performed to complement the optical measurements. Monoclinic and cubic InSe (InSe-III) were observed to be metastable around $14.5\phantom{\rule{0.3em}{0ex}}\mathrm{GPa}$ and $420\phantom{\rule{0.3em}{0ex}}\mathrm{K}$, and evidence suggesting the existence of an as yet unidentified new high-pressure and high-temperature phase was found. By means of optical ab…
Electronic structure and optical properties of CdTe rock-salt high pressure phase
2003
This paper reports on optical absorption and reflectance measurements in thin CdTe samples up to 15 GPa. All studied samples become virtually opaque at the pressure transition between the zinc-blende and rock-salt phases (3.9 GPa). As pressure increases up to 10 GPa, a relative transparency region is observed between 1.2 eV and 2.4 eV, whose high energy edge shifts to higher photon energies. Above 10 GPa the transparency region gradually shrinks and disappears at about 11 GPa. The low energy side of the absorption spectrum is attributed to free carrier absorption, as electronic structure calculations show that rock-salt CdTe is a semimetal or a low gap semiconductor. Band filling effects lo…