Search results for "Lability"
showing 10 items of 802 documents
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…
Bioactive Polyphenols from Grapes and Wine Emphasized with Resveratrol
2013
Grape polyphenols are abundant. They play essential roles in the plant's life, particularly in defence mechanisms. Moreover, the grape, fresh or dried, is a widely consumed fruit by humans, as are its by-products, grape juice and wine. They also contain vast and highly varied quantities of polyphenols. Like other phytophenols, grape and wine resveratrol is considered a protective micronutrient. Resveratrol is a well known antioxidant, for example, a protector of low-density lipoproteins against oxidation. Its applications are therefore highly varied. Research supports the idea that wine consumed regularly, without excess, is a natural biological product possesses preventive properties, and …
Relationships betweenin vitrodrug dissolution andin vivoresponse
2012
In recent years there has been an effort to relate manufacturing variables to the performance of the dosage form from a clinical point of view (in terms of safety and efficacy). Consequently any control strategy or the establishment of meaningful specifications should take into consideration the clinical impact on the patient. Since plasma levels are considered to be one of the most useful surrogates for clinical safety (in that bioequivalent plasma levels are considered therapeutically equivalent) and dissolution is the best surrogate for bioavailability, it is a natural consequence that dissolution be used to establish the design space in which all the formulations would have similar safe…
Increased bioavailability of oral melatonin after fluvoxamine coadministration*1
2000
Background Fluvoxamine, a selective serotonin reuptake inhibitor, is known to elevate melatonin serum concentrations. It has not been clear whether these effects might be attributed to an increased melatonin production or to an decreased elimination of melatonin. The latter hypothesis was tested by this study. Methods Five healthy male volunteers (one CYP2D6 poor metabolizer) received 5 mg melatonin either with or without coadministration of 50 mg fluvoxamine. Serum concentrations of melatonin and fluvoxamine were assessed from 0 to 28 hours after melatonin intake. Results Coadministration of fluvoxamine, on average, led to an 17-fold higher (P <.05) area under concentration–time curve (AUC…
Multitechnique Analysis of the Hydration in Three Different Copper Paddle-Wheel Metal-Organic Frameworks
2019
The structural instability in a humid environment of the majority of metal-organic frameworks (MOFs) is a challenging obstacle for their industrial-scale development. Recently, two water-resistant MOFs have been synthetized, STAM-1 and STAM-17-OEt. They both contain copper paddle wheels, like the well-known water-sensitive HKUST-1, but different organic linkers. The crystal lattice of both the MOFs undergoes a phase transition upon interaction with water molecules. Their unusual flexibility allows the controlled breaking of some interpaddle wheel Cu-O interactions in the so-called crumple zones, with a mechanism called hemilability, which is considered to have a crucial role for the stabili…
Calcium, iron and zinc uptakes by Caco-2 cells from white beans and effect of cooking
2006
White beans (Phaseolus vulgaris L.) have an interesting content of essential elements, calcium, iron and zinc, but they content also phytates, oxalates, proteins, polyyphenols and complex polysaccharides that are known to interact with minerals and to affect their bioavailability. The bioavailability of calcium, iron and zinc from raw and cooked white beans was estimated using their uptake by Caco-2 cells as the criteria. Previously, the mineral fraction (soluble or dialysable) to be added to the Caco-2 cell monolayer was selected. The results obtained show that cooking increases the Caco-2 cells' uptake percentages (calcium, 18.8 versus 3.6; iron, 33.7 versus 1.7; and zinc, 17.2 versus 2.1…
Pharmacological Properties of Polyphenols: Bioavailability, Mechanisms of Action, and Biological Effects in In Vitro Studies, Animal Models, and Huma…
2021
Este artículo se encuentra disponible en la siguiente URL: https://www.mdpi.com/2227-9059/9/8/1074 Este artículo de investigación pertenece al número especial "Oxidative Stress and Inflammation: From Mechanisms to Therapeutic Approaches 2.0". Drugs are bioactive compounds originally discovered from chemical structures present in both the plant and animal kingdoms. These have the ability to interact with molecules found in our body, blocking them, activating them, or increasing or decreasing their levels. Their actions have allowed us to cure diseases and improve our state of health, which has led us to increase the longevity of our species. Among the molecules with pharmacological activity …
Effects and future trends of casein phosphopeptides on zinc bioavailability
2007
This review focuses on studies of the effects of CPPs on zinc bioavailability. It evaluates the main differences in studies performed in the last two decades, such as methodology used to measure zinc, food matrix, CPP preparation, CPP dose, CPP:Zn molar ratio and presence and concentration of zinc absorption inhibitors, such as phytate, iron and calcium. The future trends of CPPs as functional ingredients in zinc-enriched or zinc-containing foods are also discussed.
Effect of Caseinophosphopeptides from αs- and β-Casein on Iron Bioavailability in HuH7 Cells
2015
International audience; Two pools of caseinophosphopeptides (CPPs) obtained from αs- and β-casein fractions (α-CPPs and β-CPPs) were characterized. A total of 16 CPPs were identified in the α-CPPs pool, 9 of them derived from αs1-casein and 7 from αs2-casein. A total of 18 CPPs were identified in the β-CPPs pool. Four of the identified CPPs contained the characteristic phosphoseryl-glutamic acid cluster SpSpSpEE. Calcein assay was used to compare the iron-binding capacity of the α- and β-CPPs pools. At the concentration of 12.5 μM CPPs used in the iron bioavailability assays, β-CPPs pools show greater iron-binding capacity than α-CPPs pools. HuH7 human hepatoma cells show many differentiate…