The use of wireless capsule enteroscopy in a preclinical study: a novel diagnostic tool for indomethacin-induced gastrointestinal injury in experimental pigs.

Objectives: The aim was the utilization of capsule microscopy and other diagnostic techniques for prospective pre-clinical research of absorption and biotransformation mechanisms of xenobiotics in the intestinal wall after induction of gastrointestinal dysfunction. Consequently, there is a demonstration of the extrems of gastrointestinal lesions development induced with indomethacin as a representative of non-steroidal anti-inflammatory drug.

Methods: The experimental animal species were small adult pigs (n=10; body weight 30-35 kg; 4-5 months old) used for their relative physiological and metabolic resemblance to man.

Gliclazide: pharmacokinetic-pharmacodynamic relationships in rats.

The relationship between the pharmacokinetics of gliclazide and its antidiabetic efficacy were evaluated on the basis of experimental determination of changes with time in the plasma levels of this antidiabetic agent and those of glucose. The experiment included rats with both initial normal glycaemia and alloxan-induced hyperglycaemia (glycaemia increased by a minimum of 30%). Pharmacokinetic and pharmacodynamic parameters were examined in the interval of 30 to 180 min after p.

Effect of galantamine on acetylcholinesterase and butyrylcholinesterase activities in the presence of L-carnitine in rat selected brain and peripheral tissues.

Objectives: The alkaloid galantamine (GAL), which exhibits a combined anticholinesterase and direct parasympathomimetic mechanism of action, is employed in conjunction with therapeutic interventions in the stimulation of central cholinergic transfer in cognitive diseases. We attempted to achieve pharmacologically-induced enhancement of the parasympathomimetic activity of GAL in the key areas of rat brain, using an interactive combination of the alkaloid with the transmembrane enhancer L-carnitine (CAR).

Methods: We investigated activities of acetylcholinesterase (AChE) in brain areas (frontal cortex, basal ganglia, septum and hippocampus) and the hypophysis, and that of butyrylcholinesterase (BuChE) in plasma and liver.

Galantamine antiacetylcholinesterase activity in rat brain influenced by L-carnitine.

Galantamine (GAL) is a selective, competitive and reversible acetylcholinesterase (AChE) inhibitor, which increases the activity of the cholinergic system and hence gives rise to an improvement of cognitive functions in patients suffering from dementia of Alzheimer type. L-Carnitine (CAR) is a natural component of the mammalian tissue and is known to increase penetration of some chemical compounds/groups across biological membranes. The aim of this study was to evaluate the influence of pretreatment with CAR on AChE inhibition caused by GAL in selected brain parts in rat (basal ganglia, septum, frontal cortex, hippocampus) and in hypophysis, which does not lay beyond the blood-brain-barrier.