Essentiale Max Mechanism of Action

Hepatoprotector.
Pharmacology: Pharmacodynamics: In many experimental models of acute liver damage, such as damage from ethanol, alkyl alcohol, tetra-chloromethane, paracetamol and galactosamine, liver protective effects have been reported among the pharmacodynamic properties of the substance. In addition, inhibition of steatosis and fibrosis has also been observed in chronic models (ethanol, thioacetamide, organic solvents). The mechanism of action is assumed to be accelerated regeneration and stabilization of membranes, and inhibition of lipid peroxidation and collagen synthesis. There are no specific studies available on pharmacodynamics in man.
Pharmacokinetics: Animal experiments on pharmacokinetics have shown that orally administered radiolabeled soybean phospholipids were over 90% absorbed in the small intestine. Most of the phospholipids were cleaved by phospholipase A into 1-acyl-lysophosphatidylcholine, approximately 50% of which was reacylated immediately into polyunsaturated phosphatidylcholine during the absorption process in the mucosa of the small intestine. The phosphatidylcholine reaches the blood through the lymph pathway and then passes into the liver in particular, mostly bound to HDL. Pharmacokinetic studies in man were conducted with ³H and ¹⁴C radiolabeled dilinoleoylphosphatidylcholine, among other substances. The choline residue was labeled with ³H and the linoleic acid with ¹⁴C.
Peak ³H concentrations were reached between 6 and 24 hours and accounted for 19.9% of the dose. The half-life of the choline component was 66 hours.
Peak ¹⁴C concentrations were reached between 4 and 12 hours and were 27.9% of the dose. The half-life of this component was 32 hours. 2% of the ³H and 4.5% of the ¹⁴C markers were recovered in the feces. 6% of the ³H and only trace amounts of the ¹⁴C markers were recovered in the urine. These results therefore show that more than 90% of both isotopes were absorbed in the intestine.
Toxicology: Preclinical Safety Data: No toxicological studies are available for soybean phospholipids. The no-effect dose following 48-week oral administration of phosphatidylcholine (a constituent of soybean phospholipids) in rats was more than 3750 mg/kg BW/day. This corresponds to 100 times the daily dose of Phospholipids (Essentiale Max) 600 mg hard capsules, i.e. 1800 mg. In studies in dams, embryos and offspring, involving administration of up to 3750 mg of soybean phospholipids/kg BW, no teratogenic effects were found. However, since the studies did not fulfil current requirements and were also not complete, no final evaluation of the finding can be made with regard to embryotoxicity. In rodents, phosphatidylcholine showed no teratogenic or embryotoxic effects at therapeutic doses. The lowest teratogenic-embryotoxic daily dose following oral administration was more than 1 g/kg BW in rats and more than 0.5 g/kg BW in rabbits. Fertility studies in rats showed no effects on male or female fertility up to 3750 mg/kg. There are no data available concerning fertility in humans.
In various in vitro test systems, no mutagenic potential was demonstrated. Carcinogenicity studies are not available.