Drug intelligence / Profile preview

Silybin-Phytosome

Development stage
Unknown
Lead developer
Indena
Modality
Drug Delivery Systems
Administration
Oral
01

Overview

Silybin-Phytosome is a patented formulation that combines silybin (also known as silibinin), a flavonoid extracted from milk thistle (Silybum marianum), with phospholipids to enhance its bioavailability and absorption. This formulation addresses the poor water solubility and limited gastrointestinal absorption of silybin. ## Pharmacokinetics Silybin-Phytosome demonstrates significantly improved bioavailability compared to regular silymarin extracts. The bioavailability of silybin from Silybin-Phytosome is approximately seven times greater than standard formulations[5]. This enhanced absorption is particularly beneficial in patients with liver conditions, as the bioavailability of silybin is higher when administered as a phytosome adduct compared to standard silymarin, and is less influenced by liver damage[1]. When administered orally, Silybin-Phytosome can achieve high blood concentrations, with peak serum levels noted at 30 or 60 minutes in most patients[10]. In clinical studies, doses as high as 13-20g daily have been used, typically divided into three doses[8]. ## Clinical Applications Silybin-Phytosome has been investigated for several therapeutic applications: **Liver Protection and Treatment** - Used for treating toxic liver damage, including Amanita mushroom poisoning[4] - Adjunctive therapy in chronic hepatitis and cirrhosis[4] - Studies show improved liver function in patients with chronic hepatitis (viral, alcohol, or drug-induced)[5] **Cancer Research** - Investigated for potential anticancer properties, particularly in prostate cancer[6][8] - In a phase I study, prostate cancer patients received 13g of silybin-phytosome daily[6] - Another study used doses ranging from 2.5 to 20g daily in three divided doses for 4 weeks in men with prostate cancer history[1] ## Safety Profile Silybin-Phytosome appears to be generally well-tolerated, even at high doses. The most common adverse effects include: - Mild diarrhea[8] - Asymptomatic hyperbilirubinemia, which is typically transient and resolves with treatment cessation[1][8] - One case of grade 3 ALT elevation was reported in clinical studies[8] - One patient developed a grade 4 post-operative thromboembolic event in a clinical trial, though causality was not established[6] At very high doses (15-20g/day), treatment may need to be discontinued due to asymptomatic hyperbilirubinemia, likely resulting from inhibition of the glucuronyl transferase UGT1A1[1]. ## Mechanism of Action Silybin-Phytosome exhibits several biological activities: - Antioxidant properties - Hepatoprotective effects - Potential anticancer activity - Anti-inflammatory effects The formulation involves a complex between silybin and phospholipids, which can be confirmed through sophisticated spectroscopic methods such as FTIR, 1H NMR, 13C NMR, and other techniques[5].

Other names
Silibinin-Phytosome
02

Targets

Cyp (Cyclophilin family)FXR (Farnesoid x-activated receptor)

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