Search results for "Bioavailability"
showing 10 items of 301 documents
Antihypertensive effect of a bovine lactoferrin pepsin hydrolysate: Identification of novel active peptides
2012
et al.
Toxicity of binary mixtures of Cu, Cr and As to the earthworm Eisenia andrei
2020
AbstractChromated copper arsenate (CCA) mixtures were used in the past for wood preservation, leading to large scale soil contamination. This study aimed at contributing to the risk assessment of CCA-contaminated soils by assessing the toxicity of binary mixtures of copper, chromium and arsenic to the earthworm Eisenia andrei in OECD artificial soil. Mixture effects were related to reference models of Concentration Addition (CA) and Independent Action (IA) using the MIXTOX model, with effects being related to total and available (H2O and 0.01 M CaCl2 extractable) concentrations in the soil. Since only in mixtures with arsenic dose-related mortality occurred (LC50 92.5 mg/kg dry soil), it wa…
An uptake and elimination kinetics approach to assess the bioavailability of chromium, copper, and arsenic to earthworms (Eisenia andrei) in contamin…
2019
The aim of this study was to determine the bioavailability of metals in field soils contaminated with chromated copper arsenate (CCA) mixtures. The uptake and elimination kinetics of chromium, copper, and arsenic were assessed in the earthworm Eisenia andrei exposed to soils from a gradient of CCA wood preservative contamination near Hartola, Finland. In soils contaminated with 1480–1590 mg Cr/kg dry soil, 642–791 mg Cu/kg dry soil, and 850–2810 mg Ag/kg dry soil, uptake and elimination kinetics patterns were similar for Cr and Cu. Both metals were rapidly taken up and rapidly excreted by Eisenia andrei with equilibrium reached within 1 day. The metalloid As, however, showed very slow uptak…
Permeability and toxicological profile estimation of organochlorine compounds by biopartitioning micellar chromatography
2008
This paper points out the usefulness of biopartitioning micellar chromatography (BMC) as a high-throughput primary screening tool providing key information about the oral absorption, skin permeability (Kp), brain–blood distribution coefficient (BB) and ecotoxicological parameters such as median lethal concentration (LC50) and bioconcentration factors of 15 organochloride compounds. The retention data of compounds in BMC conditions were interpolated in previously developed quantitative–retention activity relationships by our research group. Results show that the compounds studied readily cross the intestinal barrier (oral absorption >ercnt;) and the blood–brain barrier (log BB >p;0.4). In ad…
ADME Prediction with KNIME: Development and Validation of a Publicly Available Workflow for the Prediction of Human Oral Bioavailability.
2020
In silico prediction of human oral bioavailability is a relevant tool for the selection of potential drug candidates and for the rejection of those molecules with less probability of success during the early stages of drug discovery and development. However, the high variability and complexity of oral bioavailability and the limited experimental data in the public domain have mainly restricted the development of reliable in silico models to predict this property from the chemical structure. In this study we present a KNIME automated workflow to predict human oral bioavailability of new drug and drug-like molecules based on five machine learning approaches combined into an ensemble model. Th…
In vitro digestion of two age-tailored dairy products in the aging gastrointestinal tract
2023
For older adults (> 65 years old), undernutrition is a severe health problem that can impact the quality of life, induce or aggravate the development of diseases, and reduce life expectancy. Undernutrition can be defined as an inadequate intake of dietary energy and proteins combined with a low muscle mass. Diet-induced muscle mass and strength loss in older adults may be due to insufficient protein intake. Therefore, older adults need to increase the amount of high-quality ingested proteins, particularly foods rich in leucine, to promote muscle health. However, it is still unclear if changes in protein digestibility and absorption kinetics in old age may affect the anabolic effect of high-…
IMI – Oral biopharmaceutics tools project – Evaluation of bottom-up PBPK prediction success part 4: Prediction accuracy and software comparisons with…
2020
Oral drug absorption is a complex process depending on many factors, including the physicochemical properties of the drug, formulation characteristics and their interplay with gastrointestinal physiology and biology. Physiological-based pharmacokinetic (PBPK) models integrate all available information on gastro-intestinal system with drug and formulation data to predict oral drug absorption. The latter together with in vitro-in vivo extrapolation and other preclinical data on drug disposition can be used to predict plasma concentration-time profiles in silico. Despite recent successes of PBPK in many areas of drug development, an improvement in their utility for evaluating oral absorption i…
Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Codeine Phosphate
2014
The present monograph reviews data relevant to applying the biowaiver procedure for the approval of immediate-release multisource solid dosage forms containing codeine phosphate. Both biopharmaceutical and clinical data of codeine were assessed. Solubility studies revealed that codeine meets the "highly soluble" criteria according to World Health Organization (WHO), the European Medicines Agency (EMA), and the United States Food and Drug Administration (US FDA). Codeine's fraction of dose absorbed in humans was reported to be high (>90%) based on cumulative urinary excretion of drug and drug-related material following oral administration. The permeability of codeine was also assessed to be …
Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Sitagliptin Phosphate Monohydrate
2021
Sitagliptin is an antihyperglycemic drug used in adults for the treatment of diabetes Type 2. Literature data and in-house experiments were applied in this monograph to assess whether methods based on the Biopharmaceutics Classification System (BCS) could be used to assess the bioequivalence of solid immediate-release (IR) oral dosage forms containing sitagliptin phosphate monohydrate, as an alternative to a pharmacokinetic study in human volunteers. The solubility and permeability characteristics of sitagliptin were reviewed according to the BCS, along with dissolution, therapeutic index, therapeutic applications, pharmacokinetics, pharmacodynamic characteristics, reports of bioequivalence…
Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Ketoprofen
2012
Literature and experimental 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 ketoprofen are reviewed. Ketoprofen's solubility and permeability, its therapeutic use and therapeutic index, pharmacokinetic properties, data related to the possibility of excipient interactions, and reported BE/bioavailability (BA)/dissolution data were taken into consideration. The available data suggest that according to the current Biopharmaceutics Classification System (BCS) and all current guidances, ketoprofen is a weak acid that would be assigned to BCS Class II. The extent of ketoprofen abso…