Search results for "Availability"
showing 10 items of 510 documents
Effect of simulated gastrointestinal digestion on sialic acid and gangliosides present in human milk and infant formulas.
2011
The effects of simulated gastrointestinal digestion upon sialic acid and gangliosides in infant and follow-on formulas and human milk, as well as their bioaccessibility, have been evaluated. The gastric stage is the step that causes a greater decrease in sialic acid and ganglioside contents. The intestinal stage only decreases the total and individual contents of gangliosides. After gastrointestinal digestion, neither sialic acid nor gangliosides were found in the nonbioaccessible fraction. The highest bioaccessibility (100 × content in soluble fraction after gastrointestinal digestion/total content) of sialic acid is found in human milk (87%), followed by infant formula (77%) and follow-on…
Poloxamer/sodium cholate co-formulation for micellar encapsulation of Doxorubicin with high efficiency for intracellular delivery: an in-vitro bioava…
2020
Abstract Hypothesis Doxorubicin hydrochloride (DX) is widely used as a chemotherapeutic agent, though its severe side-effects limit its clinical use. A way to overcome these limitations is to increase DX latency through encapsulation in suitable carriers. However, DX has a high solubility in water, hindering encapsulation. The formulation of DX with sodium cholate (NaC) will reduce aqueous solubility through charge neutralization and hydrophobic interactions thus facilitating DX encapsulation into poloxamer (F127) micelles, increasing drug latency. Experiments DX/NaC/PEO-PPO-PEO triblock copolymer (F127) formulations with high DX content (DX-PMs) have been prepared and characterized by scat…
Calcium, Iron, and Zinc Uptake from Digests of Infant Formulas by Caco-2 Cells
2001
Our aim was to estimate the bioavailability of calcium, iron, and zinc from infant formulas using a model that includes in vitro digestion and a Caco-2 cell culture to estimate the uptake. The cell culture conditions were selected, and uptake assays were carried out first with calcium, iron, and zinc standard solutions, and then with the soluble fraction of enzymatic digests of an adapted milk-based and a soy-based infant formula. It was not possible to measure the uptake of calcium, iron, and zinc from standard solutions added to the cell cultures in amounts similar to those present in infant formula digests with our method. The fact that it was, however, possible in the case of enzymatic …
Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Bisoprolol Fumarate
2014
Abstract Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate-release (IR) solid oral dosage forms containing bisoprolol as the sole active pharmaceutical ingredient (API) are reviewed. Bisoprolol is classified as a Class I API according to the current Biopharmaceutics Classification System (BCS). In addition to the BCS class, its therapeutic index, pharmacokinetic properties, data related to the possibility of excipient interactions, and reported BE/bioavailability problems are taken into consideration. Qualitative compositions of IR tablet dosage forms of bisoprolol with a marketing authorization (MA) in ICH (Inter…
An automatic flow-through system for exploration of the human bioaccessibility of endocrine disrupting compounds from microplastics
2021
This article reports on the first attempt towards investigating the leaching rates in the human gastrointestinal (GI) tract of plastic-borne contaminants that can be ingested accidentally using physiologically relevant body fluids. Oral bioaccessibility under fasted and fed states was determined in dynamic mode exploiting an automatic flow setup. The flow system is able to mimic the fast uptake of the released species from the polymeric matrix by absorption in the human digestive system by the in-line removal of the leached species. Complex GI extractants based on the Unified Bioaccessibility Method (UBM, fasted state) and Versantvoort test (fed-state) were brought through a microplastic-lo…
Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Moxifloxacin Hydrochloride.
2020
Abstract In this monograph, literature data is reviewed to evaluate the feasibility of waiving in vivo bioequivalence testing and instead applying the Biopharmaceutics Classification System (BCS) based methods to the approval of immediate-release solid oral dosage forms containing moxifloxacin hydrochloride as the sole active pharmaceutical ingredient. To facilitate the feasibility decision, solubility and permeability and dissolution characteristics in the context of the BCS, therapeutic index, therapeutic use, pharmacokinetic parameters, bioequivalence/bioavailability issues, drug-excipient interactions and other relevant data were taken into consideration. Moxifloxacin is a BCS class I d…
Cluster-determinant 36 (CD36) impacts on vitamin E postprandial response
2014
International audience; Scope: A single nucleotide polymorphism in the cluster determinant 36 (CD36) gene has recently been associated with plasma alpha-tocopherol concentration, suggesting a possible role of this protein in vitamin E intestinal absorption or tissue uptake. Methods and results: To investigate the involvement of CD36 in vitamin E transport, we first evaluated the effect of CD36 on alpha- and gamma-tocopherol transmembrane uptake and efflux using transfected HEK cells. gamma-Tocopherol postprandial response was then assessed in CD36-deficient mice compared with wild-type mice, after the mice had been fully characterized for their alpha -tocopherol, vitamin A and lipid plasma,…
PHEA-graft-polymethacrylate supramolecular aggregates for protein oral delivery
2013
Abstract Salmon calcitonin (sCT) is characterized by a poor oral availability. A new copolymer, β-poly(N-2-hydroxyethyl)-graft-{N-2-ethylene[2-poly(methacrylic acid sodium salt)isobutyrate]}- d , l -aspartamide (PHEA-IB-p(MANa + )), was designed for the oral administration of sCT through the formation of supramolecular aggregates (SAs) based on electrostatic interactions. Several sCT/PHEA-IB-p(MANa + ) weight ratios were characterized by turbidimetry, DLS, zeta potential, and microscopy analysis. After the incubation of sCT/PHEA-IB-p(MANa + ) complex with digestive enzymes, 10% (w/w) of loaded sCT was released in the native form. In vitro investigation was carried out to determine the copol…
Calcium bioavailability in human milk, cow milk and infant formulasâcomparison between dialysis and solubility methods
1999
Abstract The percentages of total, soluble and dialysable calcium of human milk, cow milk and milk and soy based infant formulas were determined in order to detect possible differences in the calcium bioavailability of the samples. For this purpose an in vitro method was applied to these four calcium sources. The ranking of the analysed samples in terms of calcium bioavailability depends on the criteria applied. Calcium ranked dialysis percentage was: cow milk>human milk>soy based formula>milk based formulas. Calcium ranked solubility percentage was: human milk>cow milk>soy-based formula>milk-based formulas. Comparison of the results of the in vitro assay with the information available on i…
Calibration and Validation
2016
The aim of this chapter is to summarise the problems incurred during the phases of calibrating and validating the extortion racket models used by the GLODERS project. The chapter starts with the discussion of the data availability and summarises shortly the contents of Sect. 4.3. It continues with a discussion of what parameterisation, calibration, sensitivity analysis and validation have to do with each other and ends up with a discussion of the validity of the GLODERS models.