PHOSPHOCOMPLEX. Silybin-Phosphatidylcholine Complex TITOLO PRESENTAZIONE

Transcription

1 PHOSPHOCOMPLEX Silybin-Phosphatidylcholine Complex TITOLO PRESENTAZIONE

2 Phosphocomplex is a lipid-compatible active substance Phosphocomplex is obtained from the complexation of Silybin with phospholipids. Silybin origins from silymarin, the standardized extract of milk thistle plant (Silybum marianum). Water soluble phytoconstituents of milk thistle are poorly absorbed by the intestine due to: multiple-ring large size molecules which cannot be absorbed by simple diffusion, poor miscibility with oils and other lipids, severely limiting their ability to pass across the lipid-rich outer membranes of the enterocytes of the small intestine. Phospholipid complexation of Silybin helps enhance the capacity to cross the lipid-rich biomembranes and reach circulation, resulting in enhanced bioavailability.

3 Phosphocomplex and Milk thistle components Silymarin contains approximately: 70% to 80% of silymarin flavanolignans (silymarin complex) 20% to 30% of non flavonolignans compounds, comprising mostly polymeric and oxidized polyphenolic compounds (polyphenolic fraction PP). Silybin is the main component of the Silymarin complex. Silybin is a mixture of two diastereoisomeric compounds (silybin A and silybin B) in approximately 1:1 proportion.

4 Components of Silymarin Silymarin Complex Flavonolignan Non Flavonolignan SilybinA Silybin B IsosilybinA Isosilybin B Silydianin Silychristin Flavonoids Polyphenolic Compounds Taxifolin Quercetin

5 Silymarin an ancient and well-know extract Used for more than 2000 years to treat liver and gall bladder disorders: hepatitis, cirrhosis, and jaundice, MILK THILSTLE to protect the liver against poisoning from chemical and environmental toxins (including snake bites, insect stings, mushroom poisoning, and alcohol). Liver Response - Promotes hepatocyte protein synthesis, a mechanism for liver cell regeneration Inflammatory Response - Mastocites Stimulation - Neutrofiles Inhibition - Stimulates the flow bile acid and the - Leukotrien Inhibition HEPATOPROTECTIVE EFFECT production of bile salts - PG, LP and IL Inhibition Recently, silybin/silymarin has been studied for its alternative beneficial activities such as anticancer and chemopreventive actions, as well as hypocholesterolemic, cardioprotective, neuroactive and neuroprotective activities. - Increa - Increa

6 Why Silymarin has a poor oral bioavaibility? All pharmacokinetic parameters of silymarin are referred to and standardized as, silybin. Extensive phase II metabolism Only percent of oral silymarin is absorbed by the gastrointestinal tract where it undergoes extensive enterohepatic circulation. Reasons for poor oral bioavailabilitty of silymarin Low permeability across intestinal epithelial cells Low water solubility (0,5 g/l) Rapid excretion in bile and urine Phosphocomplex has a better bioavailability and a higher antioxidant activity. (Morazzoni P., Magistretti M.J., Giachetti C., Zanolo G., Eur. J. Drug Metabol. Pharmacokinet. 17, 39 (1992).

7 PHOSPHOCOMPLEX features Phosphocomplex is obtained by hydrogen bonds between the polar head of phospholipids and the polar groups of pure Silybin ( 95%) Standardized starting material ( 29% to 37% of silybin by HPLC) Natural chemical complex specifically identifiable Enhanced absorbtion through gastro-intestinal tract Improved bioavailability Enhanced stability of the complex at physiological ph Facilitated liver targeting Synergistic effect of the phospholipid phosphatidylcholine, as hepatoprotector Suitable for different formulation such as tablets, capsules and topical dosage forms Easy handling and storage

8 Phosphatidylcholin: biological and functional roles Phospholipids used in the production of Phosphocomplex contain of a consistent quantity of phosphatidylcholine which is: Is the principal constituent of cell membrane; Is the principal molecular building block for circulating lipoproteins; Is an important emulsifier in the lungs gastrointestinal tract bile; Manages the vast majority of life processes; Acts as a carrier for both fat-miscible and water-miscible nutrient.

9 Phosphocomplex and veterinary applications Phosphocomplex preparations can be used either as feed supplement intended for improving animal health and their productivity or for therapeutic purposes in veterinary pathological processes. PET APPLICATIONS Treatment of various hepatic disorders in cats and dogs Normalization of hepatic enzymes, increasing hepatic glutathione and protecting hepatic tissue Contribution to re-generation and replacement of liver cells. Treatment of poisoning such as Amanita intoxication by blocking the absorption of toxins into liver cells. Inhibition of the formation of inflammatory substances that contribute to liver degeneration. ZOOTECHNICAL APPLICATIONS Liver support as feed supplement in cows Severity of the peripartum fatty liver in cows Support metabolic pattern of the liver enzymes during the lactation onset in cows.

10 INTELLECTUAL PROPERTY LEGISLATION AND COMPLIANCE Manufacturing Operations FDA Inspected HACCP 21CFR Part 111 CERTIFICATIONS UNI EN ISO 22000:2500

11 Finished products on the market

12 Finished products on the market