Pharmacology: Pharmacodynamics: The active ingredient of Carbotrap is acarbose, a pseudotetrasaccharide of microbial origin. Acarbose exerts its activity in the intestinal tract. The action is based on the inhibition of intestinal enzymes (α-glucosidases) involved in the degradation of disaccharides, oligosaccharides and polysaccharides. This leads to a dose-dependent delay in the digestion of these carbohydrates.
Most importantly, glucose derived from carbohydrates is released and taken up into blood more slowly. In this way acarbose postpones and reduces the postprandial rise in blood glucose. As a result of the balancing effect on the uptake of glucose from the intestine, the blood glucose fluctuations over the day are reduced and the mean blood glucose values decrease.
Pharmacokinetics: Following administration, only 1-2% of the active inhibitor was absorbed.
The pharmacokinetics of Acarbose were investigated after oral administration of the 14C-labelled substance (200 mg) to healthy volunteers. On average, 35% of the total radioactivity (sum of the inhibitory substance and any degradation products) was excreted by the kidneys within 96 h. The proportion of inhibitory substance excreted in the urine was 1.7% of the administered dose. 50% of the activity was eliminated within 96 hours in the faeces. The course of the total radioactivity concentration in plasma was comprised of two peaks. The first peak, with an average acarbose equivalent concentration of 52.2±15.7 μg/l after 1.1±0.3 h, is in agreement with corresponding data for the concentration course of the inhibitor substance (49.5±26.9 µg/l after 2.1±1.6 h). The second peak is on average 586.3±282.7 µg/L and is reached after 20.7±5.2 h. The second, higher peak is due to the absorption of bacterial degradation products from distal parts of the intestine. In contrast to the total radioactivity, the maximum plasma concentration of the inhibitory substance are lower by a factor of 10-20. The plasma elimination half-lives of the inhibitory substance are 3.7±2.7 h for the distribution phase and 9.6±4.4 h for the elimination phase.
A relative volume of distribution of 0.32 l/kg body-weight has been calculated in healthy volunteers from the concentration course in the plasma.