Phosphocomplex® is the proprietary bioavailable Sylibin, in the form of a lipid-compatible active compound where the Silybin has been complexed with phospholipids. Silybin is the most abundant and potent constituent of silymarin, the most active ingredient of milk thistle plant (Silybum marianum) that has been extensively studied for its benefits in liver health. Through its antioxidant and anti-inflammatory effects, the Silybin contained in Phosphocomplex® has the capacity to protect and normalize liver functions, also promoting the production of glutathione.
Unfortunately, Silybin has a poor intestinal absorption and a low bioavailability. In Phosphocomplex®, the phospholipid complexation of Silybin occurs with phosphatidylcholine, which is an important emulsifier in the gastrointestinal tract and improves the capacity of the Silybin to cross the lipid-rich bio-membranes and reach circulation, resulting in enhanced bioavailability. The enhanced bioavailability of Phosphocomplex® has been tested in comparison with a formulation purchased from the nutraceutical market and used as reference product. Silybin (from Silybum, the generic name of the plant from which it is extracted), is the major active constituent of silymarin, a standardized extract of the milk thistle seeds, containing a mixture of flavonolignans consisting of silibinin, isosilibinin, silicristin, silidianin and others. Silybin itself is a mixture of two diastereomers, silybin A and silybin B, in approximately equimolar ratio.
Silybin has been used for centuries to address liver health, due to the recognized role in liver protection and detoxification. There are clinical evidences for the use of silybin as a supportive element in alcoholic and non alcoholic steatohepatitis (Fatty liver disease) and chronic liver disease (Cacciapuoti et al., World Journal of Hepatology, 5 (3), 109–113, 2013).
Silybin has an important role in liver protection and detoxification. It inhibits lipid peroxidation, it supports a good cell functionality and neutralizes the excess of free radicals thus reducing the oxidative stress in the liver. The effective antioxidant property of Silybin allows to conserve Glutathione (GSH) in liver cells while stabilizing the liver cells membranes against oxidative attack.
Several studies have also demonstrated that Silybin stimulates synthesis and activity of enzymes responsible for detoxification pathways in liver and also blocks the oxidative toxicities of alcohol, carbon tetrachloride and mushroom toxins. Silybin is poorly absorbed by the intestine, that limits its benefits because of :
- Multiple-ring large size molecules which cannot be absorbed by simple diffusion
- Poor miscibility with lipids, severely limiting their ability to pass across the lipid-rich outer membranes of the enterocytes of the small intestine
- Extensive phase II metabolism and rapid excretion in bile and urine, The poor water solubility and bioavailability of silybin have inspired to the development of enhanced formulations to increase its absorption. A complex of silybin and phospholipids has shown to be about 10 times more bioavailable than silybin itself (Kidd P. et al., Alternative Medicine Review: a Journal of Clinical Therapeutic 10 (3): 193–203,2005.
Biological & Functional Roles In A Healthy Liver
Phosphatidylcholine (PC) has also biological and functional roles in healthy liver. It is one of the most important support nutrients for the liver, a large biological molecule that is a universal building block for cell membranes. More than 2 decades of clinical trials indicate that PC protects the liver against damage from alcoholism, pharmaceuticals, pollutant substances, viruses, and other toxic influences, most of which operate by damaging cell membranes. Dietary supplementation with PC (a minimum 800 mg daily, with meals) significantly speeds recovery of the liver. PC is fully compatible with pharmaceuticals, and with other nutrients. PC is also highly bioavailable (about 90% of the administered amount is absorbed over 24 hours), and PC is an excellent emulsifier that enhances the bioavailability of nutrients with which it is coadministered. (Kidd PM. Phosphatidylcholine: A Superior Protectant Against Liver Damage. Alternative Med. Rev. 1996) PC’s diverse benefits and proven safety indicate that it is a premier liver nutrient:
- It is the principal molecular building block for circulating lipoproteins
- It is an important emulsifier in the lungs gastrointestinal tract bile
- It manages the vast majority of life processes
- It acts as a carrier for both fat-miscible and water-miscible nutrient
Uses and doses :
Phosphocomplex® is obtained by hydrogen bonds between the polar head of phospholipids and the polar groups of pure Silybin (≥ 95%). The standardized starting material is equal to ≥29% to ≤37% of Silybin by HPLC. The enhanced absorption through gastro-intestinal tract and the increased bioavailability facilitates liver targeting, with a synergistic effect of the phosphatidylcholine phospholipid as hepatoprotector. Supported by pharmacological and clinical data. Phosphocomplex ™ is a yellow-brownish powder suitable for different formulation such as tablets, capsules and sachets.
At the recommended dosage of 80 – 160 mg/day it may be indicated as a complement product for :
- Fatty Liver –Steatosis
- Alcoholic liver disease
- Also Non Alcoholic Fatty Liver Disease
- Chronic liver disease
- Acute viral hepatitis.
Mechanisms of working of phosphocomplex :
1. Hepatocye protection : promotes hepatocyte protein synthesis, a mechanism forliver cell regeneration
2. Anti-inflammatory effects
a) mastocytes stimulated
b) neutrophil stimulation
c) leucotrine inhibition
d) Prostaglandin, lipoprotein and lnterleucin inhibition
3. Detoxification : increases GSH, increases superoxide dismutase
4. Liver protection : stimulates the flow of bile acid and the production of bile salts, and protection of hepatic tissue.