Search results for "Bioavailability"

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 formulas—comparison 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…

P105. New findings on vasodilator potency, tachyphylaxis, and bioavailability of organic nitrates reveal: The tolerance-devoid clinical action of pen…

2006

An approach to As(III) and As(V) bioavailability studies with Caco-2 cells

2005

Foods and drinking water are the main sources of human exposure to inorganic arsenic [As(III) and As(V)]. After oral ingestion, the intestinal epithelium is the first barrier to absorption of these species. A human intestinal cell line (Caco-2) was used to evaluate cell retention and transport of As(III) (15.6-156.0 microM) and/or As(V) (15.4-170.6 microM). Cell monolayer integrity, cell viability, membrane damage and effects on cell metabolism were evaluated. Only the highest concentrations assayed [As(III): 156.0 microM; As(V): 170.6 microM] produced a cytotoxic effect with different cellular targets: As(III) altered the permeability of tight junctions, and As(V) caused uncoupling of the …

Study of the cytotoxic activity of beauvericin and fusaproliferin and bioavailability in vitro on Caco-2 cells.

2010

Abstract Beauvericin (BEA) is a cyclohexadepsipeptide mycotoxin which has insecticidal properties and produces cytotoxic effects in mammalian cells. Fusaproliferin (FUS) is a mycotoxin that has toxic activity against brine shrimp, insect cells, and teratogenic effects on chicken embryos. The aim of this study was to determine the cytotoxicity of BEA and FUS in human epithelial colorectal adenocarcinoma HT-29 and Caco-2 cells, the transepithelial transport and the bioavailability using Caco-2 cells as a simulated in vitro gastrointestinal model of the human intestinal epithelium. The inhibitory concentration (IC 50 ) evidenced by BEA in the Caco-2 cells was 24.6 and 12.7 μM at 24 and 48 h ex…

Formulation strategy towards minimizing viscosity mediated negative food effect on disintegration and dissolution of immediate release tablets.

2017

Food induced viscosity can delay disintegration and subsequent release of API from solid dosage form which may lead to severe reduction in the bioavailability of BCS type III compounds. Formulations of such tablets need to be optimized in view of this postprandial viscosity factor. In this study, three super disintegrants, croscarmellose sodium (CCS), cross-linked polyvinylpolypyrrolidone (CPD), and sodium starch glycolate (SSG) were assessed for their efficiency under simulated fed state. Tablets containing these disintegrants were compressed at 10 and 30 KN, while taking lactose as a soluble filler. In addition to other compendial tests, disintegration force of these formulations was meas…

Activity–Bioavailability balance in Oral Drug Development for a Selected Group of 6‐Fluoroquinolones

2002

Abstract A nomogram is proposed to select the best candidate in drug development studies with quinolones and is intended to substitute other possible models. The nomogram is referred to as an activity–bioavailability balance (ABB) because it includes the following two criteria: ABB= 1 / gm MIC ( drug candidate ) 1 /gm MIC ( ciprofloxacin ) · F calc \( drug candidate \) F calc ( ciproflaxacin ) . The in vitro activity of a group of 4′ N ‐alkyl‐ciprofloxacin derivatives was determined together with that of ciprofloxacin, initially against some reference strains and subsequently against 159 clinical isolates of eight selected species. The inverse of the geometric mean of the lowest concentrati…

Does the addition of caseinophosphopeptides or milk improve zinc in vitro bioavailability in fruit beverages?

2009

Abstract The influence of caseinophosphopeptides (CPPs) added to fruit beverage versus milk based fruit beverage upon zinc retention, transport, and uptake, as well as the influence of Fe supplementation, were studied using a combined simulated gastrointestinal digestion/Caco-2 cell system. Zinc retention, transport, and uptake of milk based fruit beverage was 4- to 5-fold greater than that of fruit beverages with or without CPPs – no statistically significant differences being observed in relation to the presence or absence of CPPs. Possibly, a slow release of CPPs throughout the digestive tract, as can be expected to take place during the digestion of casein, has a more beneficial effect …