Sunday, March 10, 2013


Silibinin  also known as silybin, is the major active constituent of silymarin, a standardized extract of the milk thistle seeds containing mixture of flavonolignans consisting of among others of silibinin, isosilibinin, silicristin, and silidianin. Silibinin itself is mixture of two diastereomers silibinin A and silybinin B in approximately equimolar ratio. Both in vitro and animal research suggest that silibinin has hepatoprotective (antihepatotoxic) properties that protect liver cells against toxins. Silibinin has also demonstrated in vitro anti-cancer effects against human prostate adenocarcinoma cells, estrogen-dependent and -independent human breast carcinoma cells, human ectocervical carcinoma cells, human colon cancer cells, and both small and nonsmall human lung carcinoma cells.
Chemically modified silibinin, silibinin dihydrogen disuccinate disodium a solution for injection, is currently being tested as a treatment of severe intoxications with hepatotoxic substances, such as death cap  poisoning. There is also clinical evidence for the use of silibinin as a supportive element in alcoholic and Child grade ‘A’ liver cirrhosis

Cholagogues, Cholelitholytics & Hepatic Protectors

Chemical Formula  -  C25-H22-O10
 Molecular Weight  -  482


Hepatic diseases
Adult: 140 mg bid/tid.
Administration-   Should be taken with food.
Contraindications-   Hypersensitivity, pregnancy, lactation
Silymarin is an active principle from the fruit of Silybum marianum, which contains a mixture of flavonolignans. It reduces the turnover of membrane phospholipids and stabilises the cell membranes of hepatocytes. It has potent antioxidant action and prevents lipid peroxidation.

Poor water solubility and bioavailability of silymarin led to the development of enhanced formulations. Silipide  a complex of silymarin and phosphatidylcholine is about 10 times more bioavailable than silymarin. It has been also reported that silymarin inclusion complex with β-cyclodextrin is much more soluble than silymarin itself.There have also been prepared glycosides of silybin, which show better water solubility and even stronger hepatoprotective effect. Silibinin has been reported to exert a neuroprotective effect in mice.
Silymarin, as other flavonoids, has been shown to inhibit P-glycoprotein-mediated cellular efflux. The modulation of P-glycoprotein activity may result in altered absorption and bioavailability of drugs that are P-glycoprotein substrates. It has been reported that silymarin inhibits cytochrome P450 enzymes and an interaction with drugs primarily cleared by P450s cannot be excluded.

The acute toxicity of silymarin and silybin were investigated by oral and intravenous route in various animal species. No mortality or any signs of adverse effects were observed after silymarin at oral doses of 20 g/kg in mice and 1 g/kg in dogs. The median lethal dose (LD50) after intravenous infusion values are 400 mg/kg in mice, 385 mg/kg in rats and 140 mg/kg in rabbits and dogs. These data demonstrate that the acute toxicity of silymarin is very low.
Similarly, its subacute and chronic toxicity are very low; the compound is also devoid of embryotoxic potential.

Brand Names
Alepa-forte  -   Duopharm, Germany
Bao-Gan  -  Chen Ta, Taiwan
Bilsyl  -  Anglopharma, Colombia
Carsil   -   Briz, Latvia; Corpus Medica, Lithuania; Sopharma, Bulgaria; Sopharma, Estonia; Sopharma, Georgia
Carsil Forte  -  Sopharma, Georgia
Cefasilymarin  -  Cefak, Germany
Ci Ning  -  Shanxi C&Y Pharmaceutical Co., Ltd., China
Darsil  -  Darnitsa, Georgia
Dilacan Silymarin  -  CanCap, Taiwan
Durasilymarin  -  Mylan dura, Germany; Wyeth, Taiwan
Econlin  -  Health Chemical, Taiwan
Eliamine  -  Panion & BF, Taiwan
Elianine  -  Panion & BF, Taiwan
Enpex  -  Yuan Chou, Taiwan
Flavobion  -  Nycomed, Czech Republic; Zentiva, Slovakia
Forliver  -  Root, Taiwan
Gen Bo  -  Chen Ho, Taiwan
Hanomarin   -  Han All, South Korea
Hegrimarin  -  Strathmann, Germany; Strathmann, Hungary
HepaBesch  -  Strathmann, Germany
Hepa-Loges  -  Loges, Germany
Hepanat  -  Yung Shin, Taiwan
Hepanavit  -  Keyfarm, Peru
Hepar-Pasc  -  Pascoe, Germany
Hepasil  -  Signova, India
Hepatoflam  -  Sherfarma, Peru
Hepatos  -  Hevert, Germany
Hepa-V  -  UBI, Taiwan
Hepavit  -   Littman, Philippines
Hepawell  -  Quest Vitamins, Taiwan
Heplant  -  Spitzner,           Germany
Heprin  -  Dong Kook,       Taiwan
Higaflam  -  Sherfarma,    Peru
Higanatur  -  Sherfarma,  Peru
Higaox  -  Sherfarma,       Peru
Kenbo  -  Yung Chang,     Taiwan
Kupfer Q Forte (Silibinin and Ubidecarenone)  -  BioGenet, Ecuador
Kupfer Q Recargado (Silibinin and Ubidecarenone)  -  BioGenet, Ecuador
Lagosa  -  Dragenopharm, Georgia;      Worwag, Slovakia;       Wörwag Pharma, Czech Republic;      Wörwag Pharma, Germany;         Wörwag Pharma, Poland;        Wörwag Pharma, Romania
Laragon      -  Roemmers, Argentina
Legacell  -   Dae Won, South Korea
Legalon Forte  -  Bayer, Chile
Legalon  -   Bu Kwang, South Korea;         Grünenthal, Colombia;            Madaus, Bulgaria;                Madaus, Georgia;           Madaus, Hungary;            Madaus, Luxembourg;           Madaus, Oman;            Madaus, Philippines;               Madaus, Poland;       Madaus, Slovakia;      Madaus, Thailand;             Maskati, Bahrain;    Nycomed, Mexico;     Nycomed, South Africa;    Nycomed Pharma, Brazil;     Rottapharm, China;    Rottapharm, Spain;      Rottapharm, Italy;      Rottapharm, Malta;    Rottapharm Madaus, Portugal;              Rottapharm/Madaus, Germany;          Rottapharm-Madaus, Romania;         Zuoz, Venezuela
Lemarin  -  Hans-E Lembecke, Taiwan
Leprotek  -  Zdravlje, Serbia
Levalon  -  Micro B & B, India
Leveron  -  Vesco Pharmaceutical, Thailand
Limarin  -  Serum Institute, India
Liparin  -  Guardian Pharmatama, Indonesia
Lipositol Q10 Forte (Silibinin and Ubidecarenon)  -  Kronos, Ecuador
Livercon  - Sheng Chung Tang, Taiwan
Liverman-   Dong-A, South Korea
Liveron  -  Hua Shin, Taiwan
Livorin  -  Weidar, Taiwan
Livosil Forte  -  Centaur, India
Lolian  -     Hwang's, Taiwan
Marina   -    T Man, Thailand
Miltis   -   Millimed, Thailand
Pharmarin   -   Pharmaland, Thailand
Phytohepar  -  Steigerwald, Germany
Poken   -  Meider, Taiwan
Pougenin   -   Hua Shin, Taiwan
Poulican-U    -         Sinphar, Taiwan
Procam    -      Everest, Taiwan
Prohep Forte   -      Lupin, India
Samarin    -    Berlin, Thailand
SE Mariendistel    -    Spitzner, Germany
Shui Lin Jia    -    Tasly, China
Sican    -     Astar, Taiwan
Silarine    -     Vir, Spain
Silegon    -    Teva, Hungary
Silibene   -    Merckle Recordati, Germany
Silibin    -    Hwang's, Taiwan
Silibinum    -    Arena, Romania
Silicur   -    Hexal, Germany; Hexal, Luxembourg
Siligen    -    Synmosa, Taiwan
Silima    -    Souriree, Taiwan
Silimar    -    Zydus Cadila, India
Silimarin   -    Germed Pharma, Italy
Silimarina Genfar     -      Genfar, Ecuador;       Genfar S.A., Colombia;      Genfar S.A., Costa Rica;        Genfar S.A., Guatemala;           Genfar S.A., Nicaragua;         Genfar S.A., El Salvador Silimarinã
Biofarm, Romania;    Fabiol, Romania
Silimarit    -    Bionorica, Germany
Silimax    -    Filofarm, Poland
Silimin    -    Kojar, Taiwan
Silin    -    Shun Sheng, Taiwan
Silirin   -    Chin Teng, Taiwan
Silliver   -   Chung Mei, Taiwan
Ming Ta, Taiwan
Sanum-Kehlbeck, Germany
Silybon  -   Micro Labs, India
Silycon  -  AND, Taiwan
Silygal  -  Teva, Czech Republic
Silygen   -   Siu Guan, Taiwan
Silygen-F   -Hor Chen, Taiwan
Silygen-H   -    Hor Chen, Taiwan
Silyhep    -   Kojar, Taiwan
Silyma   -    Ming Ta, Taiwan
Silyman   -   Han Mi, South Korea
Silymarin AL   -   Aliud, Czech Republic; Aliud, Germany
Silymarin Belupo   -  Belupo, Croatia (Hrvatska)
Silymarin dura   -    Mylan dura, Germany
Silymarin Stada   -  STADA, Germany
Silymarin Vramed   -   Vramed, Bulgaria
Silymarin    -    Belupo, Bosnia & Herzegowina;    Pei Li, Taiwan; Quality Pharmaceutical, Hong Kong; Sedico, Oman; Shou Chan, Taiwan; Tai Yu, Taiwan
Silymarin-CT   -    CT Arzneimittel, Germany
Silyme-V   -   Oriental, Taiwan
Silymin   -   Swiss Pharm,   Taiwan
Silyrin  -  Talent, India
Simepar Forte    -    Mepha, Estonia; Mepha, Latvia
Sison   -    Dr. Alson Labs, India
Sivylar   -    Ranbaxy, India; Ranbaxy, Thailand
Sucan  -    Yu Sheng, Taiwan
Suganlin  -  Fisherman, Taiwan
Sulican  -  Yu Sheng, Taiwan
Sylimarol  -   Herbapol Poznan, Poland
Syliverin  -  Aflofarm, Poland
Symatone  -  Patron, Taiwan
Winmarin  -  Winston, Taiwan
Legalon SIL   -  Madaus, Austria; Madaus, Belgium; Madaus, Spain; Rottapharm/Madaus, Germany; Zeller, Switzerland

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