Plasma concentrations of free and conjugated silybin after oral intake of a silybin-phosphatidylcholine complex (silipide) in healthy volunteers

G. Gatti, E. Perucca

Research output: Contribution to journalArticle

78 Citations (Scopus)

Abstract

The plasma concentrations of free (unconjugated) and conjugated silybin after intake of a single oral dose of a lipophilic silybin-phospatidylcholine complex (silipide, 80 mg expressed as silybin equivalents) were evaluated in 12 healthy volunteers by using a sensitive and specific HPLC method. Free silybin concentrations reached a peak of 141 ± 31 ng/ml (mean ± SEM) at 2.4 hours after dosing and declined thereafter with a half-life of about 2 hours, Peak concentrations of conjugated silybin were greater (255 ± 35 ng/ml) and occurred at a later time (about 3.8 hours). The elimination of conjugated drug tended to be slower than that of free drug. AUC values for conjugated sylibin were about three-fold greater than those of free drug. It is concluded that after oral intake of silipide, silybin undergoes extensive conversion to conjugated derivative(s) which are retained in the circulation at relatively large concentrations.

Original languageEnglish
Pages (from-to)614-617
Number of pages4
JournalInternational Journal of Clinical Pharmacology and Therapeutics
Volume32
Issue number11
Publication statusPublished - 1994

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IdB 1016
Healthy Volunteers
Plasmas
Pharmaceutical Preparations
Area Under Curve
Half-Life
silybin
High Pressure Liquid Chromatography

Keywords

  • Pharmacokinetics
  • Silipide
  • Silybin

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Toxicology

Cite this

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title = "Plasma concentrations of free and conjugated silybin after oral intake of a silybin-phosphatidylcholine complex (silipide) in healthy volunteers",
abstract = "The plasma concentrations of free (unconjugated) and conjugated silybin after intake of a single oral dose of a lipophilic silybin-phospatidylcholine complex (silipide, 80 mg expressed as silybin equivalents) were evaluated in 12 healthy volunteers by using a sensitive and specific HPLC method. Free silybin concentrations reached a peak of 141 ± 31 ng/ml (mean ± SEM) at 2.4 hours after dosing and declined thereafter with a half-life of about 2 hours, Peak concentrations of conjugated silybin were greater (255 ± 35 ng/ml) and occurred at a later time (about 3.8 hours). The elimination of conjugated drug tended to be slower than that of free drug. AUC values for conjugated sylibin were about three-fold greater than those of free drug. It is concluded that after oral intake of silipide, silybin undergoes extensive conversion to conjugated derivative(s) which are retained in the circulation at relatively large concentrations.",
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T1 - Plasma concentrations of free and conjugated silybin after oral intake of a silybin-phosphatidylcholine complex (silipide) in healthy volunteers

AU - Gatti, G.

AU - Perucca, E.

PY - 1994

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N2 - The plasma concentrations of free (unconjugated) and conjugated silybin after intake of a single oral dose of a lipophilic silybin-phospatidylcholine complex (silipide, 80 mg expressed as silybin equivalents) were evaluated in 12 healthy volunteers by using a sensitive and specific HPLC method. Free silybin concentrations reached a peak of 141 ± 31 ng/ml (mean ± SEM) at 2.4 hours after dosing and declined thereafter with a half-life of about 2 hours, Peak concentrations of conjugated silybin were greater (255 ± 35 ng/ml) and occurred at a later time (about 3.8 hours). The elimination of conjugated drug tended to be slower than that of free drug. AUC values for conjugated sylibin were about three-fold greater than those of free drug. It is concluded that after oral intake of silipide, silybin undergoes extensive conversion to conjugated derivative(s) which are retained in the circulation at relatively large concentrations.

AB - The plasma concentrations of free (unconjugated) and conjugated silybin after intake of a single oral dose of a lipophilic silybin-phospatidylcholine complex (silipide, 80 mg expressed as silybin equivalents) were evaluated in 12 healthy volunteers by using a sensitive and specific HPLC method. Free silybin concentrations reached a peak of 141 ± 31 ng/ml (mean ± SEM) at 2.4 hours after dosing and declined thereafter with a half-life of about 2 hours, Peak concentrations of conjugated silybin were greater (255 ± 35 ng/ml) and occurred at a later time (about 3.8 hours). The elimination of conjugated drug tended to be slower than that of free drug. AUC values for conjugated sylibin were about three-fold greater than those of free drug. It is concluded that after oral intake of silipide, silybin undergoes extensive conversion to conjugated derivative(s) which are retained in the circulation at relatively large concentrations.

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