Planta Med 2003; 69(3): 189-192
DOI: 10.1055/s-2003-38495
Rapid Communication
© Georg Thieme Verlag Stuttgart · New York

Plasma Levels of Hypericin in Presence of Procyanidin B2 and Hyperoside: A Pharmacokinetic Study in Rats

V. Butterweck1 , U. Liefländer-Wulf2 , H. Winterhoff1 , A. Nahrstedt2
  • 1Institute of Pharmacology and Toxicology, Universitätsklinikum Münster, Germany
  • 2Institute of Pharmaceutical Biology and Phytochemistry, Westfälische Wilhelms-Universität Münster, Germany
Further Information

Publication History

Received: November 22, 2002

Accepted: January 2, 2003

Publication Date:
04 April 2003 (online)

Abstract

The biological evaluation of hypericin in various test models is hampered by its poor water solubility. In former studies we have shown that the water solubility of hypericin was remarkably enhanced in the presence of the procyanidins or flavonol glycosides of Hypericum extract. The present pharmacokinetic study was designed to find out whether the improved water solubility in the presence of procyanidin B2 or hyperoside is correlated to increased plasma levels of hypericin. Plasma levels of hypericin in rats in the presence and absence of procyanidin B2 or hyperoside were determined by reversed phase HPLC using fluorimetric detection. Both compounds increased the oral bioavailability of hypericin by ca. 58 % (B2) and 34 % (hyperoside). Procyanidin B2 and hyperoside had a different influence on the plasma kinetics of hypericin; median maximal plasma levels of hypericin were detected after 360 min (Cmax: 8.6 ng/mL) for B2, and after 150 min (Cmax: 8.8 ng/mL) for hyperoside. It can be speculated that, when administered together with these compounds, a significant accumulation of hypericin in rat plasma in the presence of both polyphenols might be responsible for the observed increased in vivo activity.

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Dr. Veronika Butterweck

Institute of Pharmacology and Toxicology

Universitätsklinikum Münster

Domagkstr. 12

48149 Münster

Germany

Email: butterv@uni-muenster.de