C3Medline
Eur J
Drug Metab Pharmacokinet 1990 Oct-Dec;15(4):333-8
Pharmacokinetic
studies on IdB 1016 (Silybin Phytosome), a silybin- phosphatidylcholine
complex, in healthy human subjects.
Barzaghi
N, Crema F, Gatti G, Pifferi G, Perucca E
Department
of Medical Pharmacology, University of Pavia, Italy.
See
National Library of Medicine Citation
IdB
1016 (Silybin Phytosome) is a complex of silybin (the main active
component of silymarin) and phosphatidylcholine, which in
animal models shows greater oral bioavailability and therefore
greater pharmacological activity compared with pure silybin
and silymarin. In order to assess its pharmacokinetic profile
in man, plasma silybin levels were determined after administration
of single oral doses of IdB 1016 (Silybin Phytosome) and silymarin
(equivalent to 360 mg silybin) to 9 healthy volunteers. Although
absorption was rapid with both preparations, the bioavailability
of IdB 1016 (Silybin Phytosome) was much greater than that of
silymarin, as indicated by higher plasma silybin levels at
all sampling times after intake of the complex. Regardless
of the preparation used, the terminal half-life was relatively
short (generally less than 4 h).
In
a subsequent study, 9 healthy volunteers received IdB 1016
(120 mg b.i.d., expressed as silybin equivalents) for 8 consecutive
days. The plasma silybin level profiles and kinetic parameters
on day 1 were similar to those determined on day 8. Most of
the silybin present in the systemic circulation was in conjugated
form.
Less
than 3% of the administered dose was accounted for by urinary
recovery of free plus conjugated silybin, a significant proportion
of the dose probably being excreted in the bile. It is concluded
that complexation with phosphatidylcholine in IdB 1016 (Silybin Phytosome)
greatly increases the oral bioavailability of silybin, probably
by facilitating its passage across the gastrointestinal mucosa.
Publication
Types:
*
Clinical trial
*
Randomized controlled trial
PMID:
2088770, UI: 91209372
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