Comparative bioavailability of Silipide, a new flavanolignan complex, in rats.
The comparative pharmacokinetics of Silipide (IdB 1016, a silybin-phosphatidylcholine complex) and silybin were investigated by measuring unconjugated and total plasma silybin levels as well as total biliary and urinary silybin excretion in rats following administration of a single oral dose (200 mg/kg as silybin). Mean peak levels of unconjugated and total silybin after IdB 1016 were 8.17 and 74.23 micrograms/ml respectively. Mean AUC (0-6 h) values were 9.78 and 232.15 h.micrograms.ml-1 indicating that about 94% of the plasma silybin is present in a conjugated form. After administration of silybin, plasma levels of both unconjugated and total compound were under the analytical detection limit. Cumulative biliary (0-24 h) and urinary (0-72 h) excretion values after administration of IdB 1016 accounted for 3.73% and 3.26% of the administered dose, respectively. After silybin administration, the biliary and urinary excretion accounted for only 0.001% and 0.032% of the dose respectively. Our results indicate a superior bioavailability of silybin administered orally as IdB 1016. This was due mainly to an impressive increase in gastrointestinal absorption.
Morazzoni
P
P
Inverni della Beffa Research and Development Laboratories, Milan, Italy.
Magistretti
M J
MJ
Giachetti
C
C
Zanolo
G
G
D000818:Animals; D001646:Bile / Q000737:chemistry; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D008297:Male; D010713:Phosphatidylcholines / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains; D012838:Silymarin / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine
D010713:Phosphatidylcholines; D012838:Silymarin; C067772:IdB 1016