C3Medline
Eur J
Drug Metab Pharmacokinet 1990 Oct-Dec;15(4):333-8
Pharmacokinetic
studies on IdB 1016 (Siliphos®), 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.
IdB 1016
(Siliphos®) 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 (Siliphos®) and silymarin (equivalent
to 360 mg silybin) to 9 healthy volunteers. Although absorption
was rapid with both preparations, the bioavailability of IdB
1016 (Siliphos®) 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 (Siliphos®)
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
C3Medline
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