Search results for "solubility"
showing 10 items of 681 documents
Improving Dissolution Behavior and Oral Absorption of Drugs with pH-Dependent Solubility Using pH Modifiers: A Physiologically Realistic Mass Transpo…
2021
Orally dosed drugs must dissolve in the gastrointestinal (GI) tract before being absorbed through the epithelial cell membrane. In vivo drug dissolution depends on the GI tract's physiological conditions such as pH, residence time, luminal buffers, intestinal motility, and transit and drug properties under fed and fasting conditions (Paixao, P. et al. Mol. Pharm. 2018 and Bermejo, et al. M. Mol. Pharm. 2018). The dissolution of an ionizable drug may benefit from manipulating in vivo variables such as the environmental pH using pH-modifying agents incorporated into the dosage form. A successful example is the use of such agents for dissolution enhancement of BCS class IIb (high-permeability,…
Bioaccessibility of calcium, iron and zinc from three legume samples
2004
Legumes can be a source of mineral elements but also of antinutritional factors which can affect their absorption. An in vitro method including gastrointestinal digestion was used to estimate mineral bioavailability. Soluble (bioaccessible) and insoluble calcium, iron and zinc from white beans, chickpeas and lentils were determined after gastrointestinal digestion. The influence of the original sample weight on the soluble mineral fraction was also estimated. The results obtained show that white beans are the legumes with the highest bioaccessible calcium and iron contents. Lentils have a high iron content but its bioaccessibility is much lower than that of iron from white beans and chickpe…
Viscosity-mediated negative food effect on oral absorption of poorly-permeable drugs with an absorption window in the proximal intestine: In vitro ex…
2014
Concomitant food intake can diminish oral absorption of drugs with limited permeability and an absorption window in the proximal intestine, due to viscosity-mediated decrease in dosage form disintegration time and drug dissolution rate. Three poorly-permeable drugs (atenolol, metformin hydrochloride, and furosemide) exhibiting negative food effect, and one highly-soluble and highly-permeable (metoprolol tartrate), serving as a negative control, were selected for the study. In vitro and in silico tools were used to evaluate the influence of media viscosity on drug bioperformance under fasted and fed conditions. The obtained results demonstrated that increased medium viscosity in the presence…
Effect of simulated gastrointestinal digestion on plant sterols and their oxides in enriched beverages
2013
Abstract This study evaluates the bioaccessibility (percentage of soluble compound available for absorption) of plant sterols (PS) and their oxides (phytosterol oxidation products, POPs) after simulated gastrointestinal digestion in fruit (Fb), milk (M) and fruit-based milk beverages with (FbM a ) or without (FbM b ) tangerine juice. In beverages and their bioaccessible fraction (BF), campesterol, campestanol, stigmasterol, β-sitosterol and sitostanol were detected. Bioaccessibility of total PS ranged between 2.62 and 6.48%, FbM b yielding the highest value, followed by FbM a > Fb > M. Campesterol/campestanol were the most bioaccessible PS. Only oxides of β-sitosterol were detected in beve…
Development and Characterization of an Amorphous Solid Dispersion of Furosemide in the Form of a Sublingual Bioadhesive Film to Enhance Bioavailabili…
2017
Administered by an oral route, Furosemide (FUR), a diuretic used in several edematous states and hypertension, presents bioavailability problems, reported as a consequence of an erratic gastrointestinal absorption due to various existing polymorphic forms and low and pH-dependent solubility. A mucoadhesive sublingual fast-dissolving FUR based film has been developed and evaluated in order to optimize the bioavailability of FUR by increasing solubility and guaranteeing a good dissolution reproducibility. The Differential Scanning Calorimetry (DSC) analyses confirmed that the film prepared using the solvent casting method entrapped FUR in the amorphous state. As a solid dispersion, FUR increa…
Synthesis of polymeric derivatives of isoniazid: characterization and in vitro release from a water-soluble adduct with polysuccinimide.
1989
Coupling of isoniazid with polysuccinimide afforded a water-insoluble polymeric pro-drug; by reaction with ethanolamine it was chemically transformed in a water-soluble adduct. The in vitro release of isoniazid from the drug-polymer adduct was studied by using an artificial stomach wall lipid membrane. The transfer rate constant from simulated gastric juice to simulated plasma was defined and compared with that of an equivalent dose of pure drug.
Investigation of water sorption and aluminum releases from high viscosity and resin modified glass ionomer.
2019
Background High viscosity glass ionomer cement (HVGIC) and resin-modified glass ionomer cement (RMGIC) have recently been clinically preferred thanks to their numerous advantages. However, initial moisture contamination has a negative effect on the mechanical and physical properties of these cements. The aim of this study was in vitro of HVGICs and RMGICs, with and without surface protection, on water sorption, solubility and release of aluminum. Material and Methods In this study, as HVGICs; Equia Forte, IonoStar Plus, Riva Self Cure; as RMCIS, Ionolux and Riva Light Cure; and as control, Z250 universal composite was used. Equia coat, Voco varnish and Riva coat were chosen as surface prote…
Estimation of Arsenic Bioaccessibility in Edible Seaweed by an in Vitro Digestion Method
2003
The aim of this study was to examine the bioaccessibility (maximum soluble concentration in gastrointestinal medium) of total (AsT) and inorganic (AsI) arsenic contents and the effect on them of cooking edible seaweed, a food of great interest because of its high As content. An in vitro gastrointestinal digestion (pepsin, pH 2, and pancreatin−bile extract, pH 7) was applied to obtain the mineral soluble fraction of three seaweeds (Hizikia fusiforme, Porphyra sp., and Enteromorpha sp.). AsT was determined by dry-ashing flow injection hydride generation atomic absorption spectrometry. AsI was determined by acid digestion, solvent extraction, and flow injection hydride generation atomic absorp…
Darstellung und polymerisation von diestern aus 2,2′-methylendiphenolen und acryl-, methacryl- bzw. Crotonsäure
1984
Several mono- and diesters of four selected 2,2′-methylenediphenols with acrylic, methacrylic, and crotonic acid were synthesized for the first time. Special emphasis was paid to the preparation of diesters with two different acyl groups which could be obtained via the corresponding monoesters. The radical polymerization of these esters with AIBN (mainly in benzene) gave insoluble (crosslinked) products from dimethacrylates and soluble (linear) polymers from mixed diesters with methacrylic and crotonic acid, while the dicrotonates are not reactive.
Polymerizable and polymeric zwitterionic surfactants: 2. Surface activity and aggregation behaviour in aqueous systems
1991
Abstract The surfactant properties of a series of permanently zwitterionic monomers and polymers were studied with respect to structural variations. A strong influence of the molecular geometry on solubility and aggregation behaviour was observed, in particular for the polymers. Whereas all monomers were water-soluble and true surfactants, the water solubility of the polymers was restricted to selected geometries. Water-soluble polymers showed the properties of classical polysoaps, i.e. low surface activity and solubilization power for hydrophobic solutes. In contrast, water-insoluble polymers formed stable monolayers at the air-water interface and could be deposited onto solid substrates b…