Search results for "Intestinal Absorption"

Pharmacology of Acamprosate: An Overview

2003

In the last years important advances have been made in the development of drugs for the treatment of alcohol addiction. Acamprosate (calcium bis‐acetylhomotaurine) is one of the better established drugs in this field on the European market. This review focuses first on the pharmacokinetics of acamprosate. The published data and the recent advances in our knowledge on the mechanisms involved in the intestinal absorption and elimination of this drug are summarized. The importance of pharmacokinetics for the proper clinical use of acamprosate is highlighted. The anti‐relapse as well as the well‐known effects of acamprosate on ethanol intake are discussed. The recent experiments in animal model…

The Biopharmaceutics Classification System: Subclasses for in vivo predictive dissolution (IPD) methodology and IVIVC

2013

The Biopharmaceutics Classification System (BCS) has found widespread utility in drug discovery, product development and drug product regulatory sciences. The classification scheme captures the two most significant factors influencing oral drug absorption; solubility and intestinal permeability and it has proven to be a very useful and a widely accepted starting point for drug product development and drug product regulation. The mechanistic base of the BCS approach has, no doubt, contributed to its wide spread acceptance and utility. Nevertheless, underneath the simplicity of BCS are many detailed complexities, both in vitro and in vivo which must be evaluated and investigated for any given…

Unraveling the behavior of oral drug products inside the human gastrointestinal tract using the aspiration technique: History, methodology and applic…

2020

Fluid sampling from the gastrointestinal (GI) tract has been applied as a valuable tool to gain more insight into the fluids present in the human GI tract and to explore the dynamic interplay of drug release, dissolution, precipitation and absorption after drug product administration to healthy subjects. In the last twenty years, collaborative initiatives have led to a plethora of clinical aspiration studies that aimed to unravel the luminal drug behavior of an orally administered drug product. The obtained drug concentration-time profiles from different segments in the GI tract were a valuable source of information to optimize and/or validate predictive in vitro and in silico tools, freque…

Ion-pair approach coupled with nanoparticle formation to increase bioavailability of a low permeability charged drug.

2018

Abstract Atenolol is a drug widely used for the treatment of hypertension. However, the great drawback it presents is a low bioavailability after oral administration. To obtain formulations that allow to improve the bioavailability of this drug is a challenge for the pharmaceutical technology. The objective of this work was to increase the rate and extent of intestinal absorption of atenolol as model of a low permeability drug, developing a double technology strategy. To increase atenolol permeability an ion pair with brilliant blue was designed and the sustained release achieved through encapsulation in polymeric nanoparticles (NPs). The in vitro release studies showed a pH-dependent relea…

Does uremic enterocolitis exist?

1981

In rats a severe but compensated chronic renal insufficiency was induced by stepwise 9/10 nephrectomy. Despite this severe chronic renal insufficiency we observed no relevant pathological changes in the intestinal mucosa. In particular, we found no evidence of mucosal erosions, ulceration or pseudomembranous colitis, findings which are traditionally thought to be characteristic of the uremic state. This was also true of those animals dying prematurely from uremia. Thus serious doubts arise about the existence of “uremic enterocolitis”, doubts which also proved justified after a critical review of the literature on human pathology.

Bioavailability and metabolism.

2002

Mind the gap—deficits in our knowledge of aspects impacting the bioavailability of phytochemicals and their metabolites—a position paper focusing on …

2015

This is an open access article under the terms of the Creative Commons Attribution-Non-Commercial-NoDerivs Licence.-- et al.

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 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…

Possible links between intestinal permeablity and food processing: a potential therapeutic niche for glutamine

2010

Increased intestinal permeability is a likely cause of various pathologies, such as allergies and metabolic or even cardiovascular disturbances. Intestinal permeability is found in many severe clinical situations and in common disorders such as irritable bowel syndrome. In these conditions, substances that are normally unable to cross the epithelial barrier gain access to the systemic circulation. To illustrate the potential harmfulness of leaky gut, we present an argument based on examples linked to protein or lipid glycation induced by modern food processing. Increased intestinal permeability should be largely improved by dietary addition of compounds, such as glutamine or curcumin, which…