Essentiale Forte Mechanism of Action

Liver therapeutic agent. ATC Code: A05BA.
Pharmacology: Pharmacodynamics: Among the pharmacodynamic properties were reported hepatoprotective effects found in numerous experimental models into acute liver damage, for example induced by ethanol, alkyl alcohol, carbon-tetrachloride, paracetamol and galactosamine. Moreover, in chronic models (ethanol, thioacetamide, organic solvents) was seen also the inhibition of steatosis and fibrosis. As active principle has been suggested accelerated membrane regeneration and stabilisation, inhibited lipid peroxidation and inhibited collagen synthesis. Specific investigations into human pharmacodynamics are not available.
Pharmacokinetics: Animal experiments into the pharmacokinetics showed that more than 90% of the orally applied radiolabelled soya-bean phospholipids are absorbed in the small intestine. Most of it is split by phospholipase A to 1-acyl-lyosphosphatidylcholine, 50% of which is reacylated immediately into polyunsaturated phosphatidylcholine still during the process of absorption in the intestinal mucosa. This polyunsaturated phosphatidylcholine reaches the blood via the lymph pathway and from there - mainly bound to HDL - it passes in particular to the liver.
Tests into human pharmacokinetics were performed a.o. with radioactively labeled dilinoleoyl-phosphatidylcholine (³H and ¹⁴C). The choline moiety was ³H-labeled and linoleic acid had the ¹⁴C-label.
The maximum ³H concentration was achieved after 6 to 24 hours and amounted to 19.9% of the dose. The half-life for the choline component was 66 hours.
The maximum ¹⁴C concentration was achieved after 4 to 12 hours and amounted to 27.9% of the dose. The half-life for this component was 32 hours.
In the faeces were found 2% of the ³H and 4.5% of the ¹⁴C label, in the urine 6% of the ³H and only minor amounts of the ¹⁴C label.
These results show that both isotopes are absorbed to over 90% in the intestine.