Ref8P22
Comparative
pharmacokinetics of silipide (Silybin Phytosome) and silymarin
in rats
P. MORAZZONI1, A. MONTALBETTI1, S. MALANDRINO1 AND G. PIFFERI2
1
Inverni della Beffa Research and Development Laboratories,
Milan Italy
2
Istituto di Chimica Farmaceutica, Univarea di Milano, Milan,
Italy
See
National Library of Medicine Citation
The
plasma level profile and the biliary excretion of silybin,
the main flavanolignan component of silymarin, were evaluated
in rats after single equimolar oral doses of the silybin-phosphatidylcholine
complex silipide (Laboratory code Idb 1016), (Silybin Phytosome),
and of silymarin.
The introduction of this study states that the standardized
extract of silymarin is widely used in Eurpoe for the treatment
of liver disorders(1-3). It goes on to state the a problem
with oral use of the main constituent of silymarin (silybin)
is the low bioavailability of the compound, as demonstrated
in studies with lab animals (4,5) and man (6).
Previous
studies in rats (7), healthy volunteers (8) and patients with
liver disease (9, 10) have shown that after oral intake of
silipide (Silybin Phytosome), plasma silybin levels are several-fold
higher than those measured after treatment with silymarin
at equal doses in terms of silybin content.
This
study showed the relative bioavailability of silipide (Silybin Phytosome)
was nearly 10-fold higher than that of silymarin. Measured
as silybin, the blood plasma peak for Silybin Phytosome was 1,004,
whereas for silymarin it was 139.
Hruby
K., Cosmos G., Fuhrmann M., Thaler H. (1983): Chemotherapy
of Amanita phalloides poisoning with intravenous silybinin.
Human Toxicol.2, 183-195.
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P., Dragosics B., Frank H., Benda L., Dittrich H., Meryn S.
(1985): Randomized controlled trial of silymarin tratment
in patinets with cirrhosis of the liver. J. Hepatol., 1, S229.
Ferenci
P., Dragosics B., Dittrich H., et al (1989): Randomized controlled
trial of silymarin treatment in patients with cirrhosis of
the liver. J Hepatol.,9, 105-113.
Morazzoni
P., Magistretti M.J., Giachetti C., Zanolo G. (1992): Compartive
bioavailability of silipide (Silybin Phytosome), a new flavanolignan
complex, in rats. Eur. J. Drug Metab. Pharmacokinet., 17,
39-44.
Arcari
M., Brambilla A., Brandt A., et al. (1992): Nuovo comlesso
di incllusione tra la silybina e la ciclodrestrina: velocita
di dissoluzione in vitro e assorbimento in vivo in confronto
a fromulazioni tradizianali. Boll. Chim Farmaceutico, 131,
205-209.
Zanolo
G., (1989): RBM Exp. N. 254, Inverni della Beffa SpA, data
on file.
Morazzoni
P., Malandrino S., Pifferi G. (1992) : Comparative bioavailability
of a silybin-phosphatidylcholine complex (Silybin Phytosome) and
silymarin in rats. In: Bres J., Panis G. (eds).
Barzaghi
N., Crema F., Gatti G., Pifferi G., Perucca E. (1990): Pharmakinetic
studies on Idb 1016, a silybin-phosphatidylcholine complex
(Silybin Phytosome), in healthy human subjects. Eur. J. Drug Metab.
Pharmacokinet., 15, 333-338.
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R., Fragasso A., Lampertico M., Marena C. (1990): Silybin
kinetics in patients with liver cirrhosis: a comparative study
of a silybin-phospatidylcholine complex (Silybin Phytosome) And
silymarin. Med. Sci Res. 18, 861-863.
Schandalik
R., Gatti G., Perucca E. (1992): Pharmacokinetics in bile
following administration of silipide (Silybin Phytosome) and silymarin
in cholecystectomy patients. Arzneimittelforsch., 42 (II),
964-968
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