Cholecystokinin regulates satiation independently of the abdominal vagal nerve in a pig model of total subdiaphragmatic vagotomy

The vagal nerve and gut hormones CCK and GLP-1 play important roles in the control of food intake. However, it is not clear to what extent CCK and GLP-1 increase satiation by stimulating receptors located on abdominal vagal nerve endings or via receptors located elsewhere. This study aimed to further explore the relative contribution of the...

In vitro models for the prediction of in vivo performance of oral dosage forms

Accurate prediction of the in vivo biopharmaceutical performance of oral drug formulations is critical to efficient drug development. Traditionally, in vitro evaluation of oral drug formulations has focused on disintegration and dissolution testing for quality control (QC) purposes. The connection with in vivo biopharmaceutical performance has...

A new approach to predict human intestinal absorption using porcine intestinal tissue and biorelevant matrices

A reliable prediction of the oral bioavailability in humans is crucial and of high interest for pharmaceutical and food industry. The predictive value of currently used in silico methods, in vitro cell lines, ex vivo intestinal tissue and/or in vivo animal studies for human intestinal absorption, however, is often insufficient, especially when...

Recent methodology in the phytochemical analysis of ginseng

This review summarises the most recent developments in ginseng analysis, in particular the novel approaches in sample pre-treatment and the use of high-performance liquid-chromatography-mass spectrometry. The review also presents novel data on analysing ginseng extracts by nuclear magnetic resonance spectroscopy and high-resolution mass...

Transdermal administration of radiolabelled [14C]rotigotine by a patch formulation: A mass balance trial

Background and objective: The dopamine agonist rotigotine has been formulated in a silicone-based transdermal system for once-daily administration. The objective of the present study was to characterise the mass balance of rotigotine in humans after administration of a single transdermal patch containing radiolabelled [14C]rotigotine and to...

Dermatokinetics of didecyldimethylammonium chloride and the influence of some commercial biocidal formulations on its dermal absorption in vitro

The in vitro dermal absorption kinetics of didecyldimethylammonium chloride (DDAC) was studied after single and multiple exposure. In addition, the influence of biocidal formulations on the absorption of DDAC was investigated. Following dermal exposure to DDAC in aqueous solution, less than 0.5% of the applied dose reached the receptor fluid...

A dynamic artificial gastrointestinal system for studying the behavior of orally administered drug dosage forms under various physiological conditions

Purpose. The purpose of this study was to demonstrate the potential of a dynamic, multicompartmental in vitro system simulating the human stomach and small intestine (TIM-1) for studying the behavior of oral drug dosage forms under various physiological gastrointestinal conditions. Methods. Two model drug compounds were studied in TIM-1: a...

Percutaneous absorption of mexoryl SX® in human volunteers: Comparison with in vitro data

The potential human health risk of UV filters depends on their toxicity and the human systemic exposure which is a function of the extent of percutaneous absorption of the topically applied substance into the human organism. Using a 'mass balance' approach, a study was designed to investigate the systemically absorbed dose of [14C]-Mexoryl SX®...

Physicochemical properties and transport of steroids across Caco-2 cells

Purpose. The purpose of this work was to study the relevant physicochemical properties for the absorption of steroids. Methods. Various physicochemical properties of steroids were calculated (molecular weight, ClogP, static polar surface area [PSA], etc.). Within this series of steroids, different pharmacological groups were defined. Based on...

Intestinal absorption of different types of folate in healthy subjects with an ileostomy

Our knowledge on the absorption of folate is incomplete. The deconjugation process as a possible limiting factor in the absorption of folates was investigated. The study also attempted to validate the use of the area under the serum response curve (AUC) from food compared with folic acid as a proxy variable for food folate bioavailability....

Intravenous and inhalation toxicokinetics of sarin stereoisomers in atropinized guinea pigs

We report the first toxicokinetic studies of (±)-sarin. The toxicokinetics of the stereoisomers of this nerve agent were studied in anesthetized, atropinized, and restrained guinea pigs after intravenous bolus administration of a dose corresponding to 0.8 LD50 and after nose-only exposure to vapor concentrations yielding 0.4 and 0.8 LCt50 in an...

Safety evaluation of synthetic β-carotene

The safety of β-carotene was reassessed by evaluating the relevant literature on the beneficial and adverse effects of β-carotene on cancer and, in particular, by evaluating the results of toxicity studies. β- Carotene appeared neither genotoxic nor reprotoxic or teratogenic, and no signs of organ toxicity have been found in subacute, subchronic...

Oligofructose stimulates calcium absorption in adolescents

Background: In rats, nondigestible oligosaccharides stimulate calcium absorption. Recently, this effect was also found in human subjects. Objective: The objective of the study was to investigate whether consumption of 15 g oligofructose/d stimulates calcium absorption in male adolescents. Design: Twelve healthy, male adolescents aged 14-16 y...

A randomized three-way cross-over study in healthy pituitary-suppressed women to compare the bioavailability of human chorionic gonadotrophin (Pregnyl®) after intramuscular and subcutaneous administration

The objective of this study was to compare the bioavailability of s.c. and i.m. administration of human chorionic gonadotrophin (HCG; Pregnyl®). In a randomized, single centre, three-way cross-over study, 18 healthy pituitary-suppressed volunteers were assigned to single HCG injections of 5000 and 10000 IU i.m. and 10000 IU s.c. Rate (C(max), t...

Absorption enhancement, structural changes in tight junctions and cytotoxicity caused by palmitoyl carnitine in Caco-2 and IEC-18 cells

Palmitoyl carnitine chloride (PCC) has been shown to be an effective enhancer of intestinal transport of hydrophilic molecules. The exact mechanism by which the epithelial barrier function is decreased is not clear. In an attempt to elucidate the mechanism of action of PCC, we studied the relationship among absorption enhancement, cell viability...

Differences in uptake of adriamycin and daunomycin by normal BM cells and acute leukemia cells determined by flow cytometry

Flow cytometry was used to measure the uptake of adriamycin (AM) and daunomycin (DM) by various cell types of the haemopoietic organs and by acute myeloid leukemia (AML) cells. For this purpose, the spontaneous fluorescence of the drugs upon excitation with laser light at 488 nm was measured. The difference in the uptake of these two drugs...

On the antifungal mode of action of metalaxyl, an inhibitor of nucleic acid synthesis in Pythium splendens

Chemicals/CAS: metalaxyl, 57837-19-1; mithramycin, 18378-89-7