Search results for "CACO-2"
showing 10 items of 203 documents
Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Piroxicam
2014
ABSTRACT 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 piroxicam in the free acid form are reviewed. Piroxicam solubility and permeability, its therapeutic use and therapeutic index, pharmacokinetic properties, data related to the possibility of excipient interactions and reported BE/bioavailability (BA), and corresponding dissolution data are taken into consideration. The available data suggest that according to the current biopharmaceutics classification system (BCS) and all current guidances, piroxicam would be assigned to BCS Class II. The ex…
Biowaiver monograph for immediate-release solid oral dosage forms: acetylsalicylic acid.
2012
A biowaiver monograph for acetylsalicylic acid (ASA) is presented. Literature and experimental data indicate that ASA is a highly soluble and highly permeable drug, leading to assignment of this active pharmaceutical ingredient (API) to Class I of the Biopharmaceutics Classification System (BCS). Limited bioequivalence (BE) studies reported in the literature indicate that products that have been tested are bioequivalent. Most of the excipients used in products with a marketing authorization in Europe are not considered to have an impact on gastrointestinal motility or permeability. Furthermore, ASA has a wide therapeutic index. Thus, the risks to the patient that might occur if a nonbioequi…
Echovirus 1 Entry into Polarized Caco-2 Cells Depends on Dynamin, Cholesterol, and Cellular Factors Associated with Macropinocytosis
2013
ABSTRACT Enteroviruses invade their hosts by crossing the intestinal epithelium. We have examined the mechanism by which echovirus 1 (EV1) enters polarized intestinal epithelial cells (Caco-2). Virus binds to VLA-2 on the apical cell surface and moves rapidly to early endosomes. Using inhibitory drugs, dominant negative mutants, and small interfering RNAs (siRNAs) to block specific endocytic pathways, we found that virus entry requires dynamin GTPase and membrane cholesterol but is independent of both clathrin- and caveolin-mediated endocytosis. Instead, infection requires factors commonly associated with macropinocytosis, including amiloride-sensitive Na + /H + exchange, protein kinase C, …
Polymeric microcontainers improve oral bioavailability of furosemide.
2016
Microcontainers with an inner diameter of 223 μm are fabricated using the polymer SU-8, and evaluated in vitro, in situ and in vivo for their application as an advanced oral drug delivery system for the poorly water soluble drug furosemide. An amorphous sodium salt of furosemide (ASSF) is filled into the microcontainers followed by applying a lid using Eudragit L100. It is possible to control the drug release in vitro, and in vitro absorption studies show that the microcontainers are not a hindrance for absorption of ASSF. In situ perfusion studies in rats are performed with ASSF-filled microcontainers coated with Eudragit and compared to a furosemide solution. The absorption rate constant …
In-vitro antioxidant capacity and cytoprotective/cytotoxic effects upon Caco-2 cells of red tilapia (Oreochromis spp.) viscera hydrolysates.
2019
Abstract The antioxidant capacity of red tilapia viscera hydrolysates (RTVH) with different degrees of hydrolysis (DH) as well as their ultrafiltration membrane fractions, were analyzed using different chemical assays. Their protective effects against oxidative stress were evaluated using H2O2-stressed human intestinal differentiated Caco-2. The highest antioxidant capacity was obtained with a DH of 42.5% (RTVH-A) and its
Identification of P-glycoprotein substrates and inhibitors among psychoactive compounds--implications for pharmacokinetics of selected substrates.
2004
Abstract The pharmacokinetics of antipsychotic drugs has become an integral part in understanding their pharmacodynamic activity and clinical effects. In addition to metabolism aspects, carrier-mediated transport, particularly secretion by ABC transporters, has been discussed as potentially relevant for this group of therapeutics. In this study, the psychoactive compounds perphenazine, flupentixol, domperidone, desmethyl clozapine, haloperidol, fluphenazine, fluvoxamine, olanzapine, levome-promazine, perazine, desmethyl perazine, clozapine, quetiapine and amisulpride were characterized in terms of P-glycoprotein (P-gp) affinity and transport. Experimental methods involved a radioligand disp…
Lemon Juice, Sesame Paste, and Autoclaving Influence Iron Bioavailability of Hummus: Assessment by an In Vitro Digestion/Caco-2 Cell Model
2020
Hummus, an iron-containing plant-based dish mainly made from chickpea puré
Presystemic metabolism and intestinal absorption of antipsoriatic fumaric acid esters.
2003
Psoriasis is a chronic inflammatory skin disease. Its treatment is based on the inhibition of proliferation of epidermal cells and interference in the inflammatory process. A new systemic antipsoriasis drug, which consists of dimethylfumarate and ethylhydrogenfumarate in the form of their calcium, magnesium and zinc salts has been introduced in Europe with successful results. In the present study, a homologous series of mono- and diesters of fumaric acid has been studied with respect to the sites and kinetics of presystemic ester degradation using pancreas extract, intestinal perfusate, intestinal homogenate and liver S9 fraction. In addition, intestinal permeability has been determined usi…
Study of the potential toxicity of commercial crispy breads by evaluation of bioaccessibility and bioavailability of minor Fusarium mycotoxins
2011
Abstract Enniatins (ENs) are bioactive compounds produced by the secondary metabolism of several Fusarium strains and known to have several biological activities, such as acting as enzyme inhibitors, antifungal and antibacterial agents, and immunomodulatory substances. This study has investigated the ENs bioaccessibility, spiked in commercial wheat crispy bread at 1.5 and 3.0 μmol/g concentrations, their transepithelial transport and bioavailability using Caco-2 cells as a model of the human intestinal epithelium. The content (%) of the four ENs contained in the gastric fluid has resulted variable from 69% to 91%, considering the two concentrations assayed. The mean bioaccessibility data fo…
Study of the potential toxicity of enniatins A, A(1), B, B(1) by evaluation of duodenal and colonic bioavailability applying an in vitro method by Ca…
2010
Abstract The bioavailability of the minor Fusarium mycotoxins enniatins (ENs) utilizing an in vitro method which allows the simulation of the small and large intestine tracts has been studied. This method, based on the application of the Caco-2 cells grown alone or in symbiosis with several strains characteristics of the gastrointestinal tract, has permitted to simulate the duodenal and colonic intestinal compartments, respectively. The duodenal bioavailability expressed as absorption value after 4 h of exposure, ranged from 57.7 to 76.8% for EN A, from 68.8 to 70.2% for EN A1, from 65.0 to 67.0% for EN B, and from 62.2 to 65.1% for EN B1. Colonic bioavailability after 48 h of incubation ra…