Legalon 140, 140 mg capsules 60 pcs

The milk thistle fruit dry extract is standardized for the content of silymarin.

Therapeutic effects of silymarin:

Detoxifying. The anti-toxic effect of silymarin has been found in studies in various models of liver damage, such as the pale grebe toxin phalloidin and alpha-amanitin, lanthanides, carbon tetrachloride, galactosamine, thioacetamide and the hepatotoxic FV3 virus.

Cytoprotective. Silymarin inhibits the penetration into the cell of some hepatotoxic substances (pale grebes venom).

Antioxidant. Due to the ability of silymarin to bind free radicals, it has antioxidant activity. It interrupts or prevents the pathophysiological process of lipid peroxidation responsible for the destruction of cell membranes. Silymarin acts not only as an antioxidant – reducing the generation of free radicals – but also as a means of stimulating the regeneration of the glutathione system, one of the most important protective systems of the liver.

Regenerative. Membranostabilizing. Silymarin stimulates the synthesis of proteins and phospholipids. Cell membranes are stabilized. Proprietary proteins and phospholipids restore the damaged structures of the hepatocyte. Restorative capacity is improved and regeneration of liver cells is accelerated. No such effect is noted in undamaged cells.

Hypocholesterolemic. Silymarin normalizes hyperlipidemia, reduces plasma levels of cholesterol and low-density lipoproteins (LDL).

Antifibrotic. Silymarin inhibits collagenase and elastase in the liver, helping to reduce the degree of fibrosis.

Anti-inflammatory. A key feature of silymarin/silibinin is the ability to block the 5-lipoxygenase pathway and have an inhibitory effect on leukotriene formation.

Pharmacokinetics

The main component of silymarin is silybinin. When taken orally, silybinin quickly dissolves and enters the intestine, then through the portal vein system 85% of it enters the liver and is selectively distributed in hepatocytes, where it is metabolized by conjugation. Up to 80% of the active substance during the first passage through the liver is excreted with bile in combination with glucuronides and sulfates. Due to deconjugation in the intestine, up to 40% of silybinin excreted with bile is reabsorbed and enters enter enterohepatic circulation, excretion period is 6.3 h. The bioavailability of the drug Legalon® 140 is 85%.

When taking milk thistle fruit extract at therapeutic doses (140 mg silymarin 3 times daily), the level of silybinin in bile is the same after repeated doses and after taking a single dose. The results showed that silybinin does not cumulate in the body.

After repeated oral doses of silymarin at 140 mg 3 times a day, a stable level of excretion with bile is achieved.

Indications

In the complex therapy of chronic inflammatory liver diseases, liver cirrhosis and toxic liver damage (caused by substances toxic to the liver).

Pharmacological effect

Milk thistle fruit dry extract is standardized for silymarin content.
Therapeutic effect of silymarin:
Detoxifying. The antitoxic effects of silymarin have been demonstrated in studies in various models of liver injury, such as the toadstool toxin phalloidin and alpha-amanitin, lanthanides, carbon tetrachloride, galactosamine, thioacetamide, and the hepototoxic virus FV3. Cytoprotective. Silymarin inhibits the penetration of certain hepatotoxic substances (poison of the toadstool) into the cell.
Antioxidant. Due to the ability of silymarin to bind free radicals, it has antioxidant activity. The pathophysiological process of lipid peroxidation, which is responsible for the destruction of cell membranes, is interrupted or prevented. Silymarin acts not only as an antioxidant – reducing the generation of free radicals, but also as a means of stimulating the regeneration of the glutathione system, one of the most important protective systems of the liver.
Regenerative. Membrane stabilizing. Silymarin stimulates the synthesis of proteins and phospholipids. Cell membranes are stabilized. Own proteins and phospholipids restore damaged hepatocyte structures. The recovery ability is improved and the regeneration of liver cells is accelerated. This effect is not observed in undamaged cells.
Hypocholesterolemic. Silymarin normalizes hyperlipidemia, reduces the level of cholesterol and low-density lipoprotein (LDL) in the blood plasma.
Antifibrotic. Silymarin inhibits collagenase and elastase in the liver, helping to reduce the degree of fibrosis.
Anti-inflammatory. A key feature of silymarin/silibinin is the ability to block the 5-lipoxygenase pathway and have an inhibitory effect on the formation of leukotriene.

The main component of silymarin is silibinin. When taken orally, silibinin quickly dissolves and enters the intestine, then through the portal vein system, 85% of it enters the liver and is selectively distributed in hepatocytes, where it is metabolized by conjugation. Up to 80% of the active substance during the first passage through the liver is excreted in the bile in combination with glucuronides and sulfates. Due to deconjugation in the intestine, up to 40% of silibinin excreted in the bile is reabsorbed and enters the enterohepatic circulation, the elimination period is 6.3 hours. The bioavailability of the drug Legalon® 140 is 85%.
When taking milk thistle fruit extract in therapeutic doses (140 mg silymarin 3 times a day), the level of silibinin in bile is the same after taking repeated doses and after taking a single dose. The results showed that silibinin does not accumulate in the body.
After repeated oral administration of silymarin 140 mg 3 times a day, a stable level of excretion in bile is achieved.

Active ingredient

Milk thistle fruit extract

Composition

One capsule contains:

Active substance: milk thistle fruit extract dry (36-44:1) – 173.0-186.7 mg, equivalent to 140 mg silymarin (DNPH), equivalent to 108.2 mg silymarin (HPLC/German F.) calculated as silibinin.

Excipients: polysorbate 80, povidone, mannitol, sodium carboxymethyl starch (type A), magnesium stearate.

The shell is a hard gelatin capsule, size “1”, which contains: gelatin, red iron oxide dye (E172), titanium dioxide (E171), sodium lauryl sulfate, black iron oxide dye (E172).

Pregnancy

Studies have not revealed any direct or indirect toxic effects on reproductive function. As a precautionary measure, it is advisable to avoid using the drug during pregnancy and breastfeeding.

Contraindications

Hypersensitivity to the components of the drug (milk thistle fruits and/or other asteraceous plants, or to any of the excipients). Children up to 12 years of age (for this dosage form).

Side Effects

The incidence of side effects is determined as follows:
Very often: > 1/10;
Often: 1/100;
Uncommon: 1/1000;
Rare: 1/10000;
Very rare: <1/10000.
Immune system disorders: Very rarely – hypersensitivity reactions, rash.
Respiratory tract disorders: Very rarely – shortness of breath.
Gastrointestinal disorders: Rarely – gastrointestinal disorders, soft stools.

Interaction

Not studied.

Overdose

No cases of overdose have been reported.
The side effects of the drug may increase.
Treatment: in case of overdose, symptomatic therapy should be carried out.

Short product description

Pharmacotherapeutic group: hepatoprotective agent.

ATX code: A05BA03.

Storage conditions

In a place protected from light, at a temperature not exceeding 30°C
Keep out of the reach of children.

Shelf life

5 years.
Do not use after the expiration date indicated on the package.

Manufacturer

Madaus GmbH, Germany