Planta Med 2007; 73 - P_513
DOI: 10.1055/s-2007-987293

Pharmacokinetic evaluation of phytotherapeutic drops with E. purpurea extract

P Guiotto 1, K Woelkart 2, G Grassi 3, B Campisi 4, B Perissutti 1, R Bauer 2, D Voinovich 1
  • 1Department of Pharmaceutical Science, University of Trieste, I-34127 Trieste, Italy
  • 2Institute of Pharmaceutical Sciences, Department of Pharmacognosy, Karl- Franzens- University Graz, A-8010 Graz, Austria
  • 3Department of Internal Medicine, University Hospital of Trieste, Cattinara, I- 34149 Trieste, Italy
  • 4DMRN, Via A Valerio 6, University of Trieste, I-34127 Trieste, Italy

Echinacea is a widely used herbal remedy for the prevention and treatment of respiratory upper tract infections due to their immunostimulant properties. Recently, studies on the molecular mode of action of the main lipophilic constituents, the alkamides, have been carried out [1,2]. Due to the high affinity of these components for the buccal membrane, the aim of this research was to prepare drops containing dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides, the major alkamides, in different concentrations (0.07, 0.21 and 0.9mg).

Bioavailability and the pharmacokinetic studies were carried out on these three phytotherapeutic formulations, after administration to 6 healthy volunteers of the three different dosage drops with one week washout between each other.

Liquid chromatography electronspray ionization ion-trap mass spectrometry was used to determine the content of dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides in serum. It was found that, for the 0,07mg drops, the Cmax was 0.55ng/ml and tmax was 30min; for the 0,21mg drops the Cmax was 0.88ng/ml and the tmax was again 30min. Finally, for the 0,9mg drops the Cmax was 6.53ng/ml and the tmax 20min.

An ex vivo study was performed to measure the influence on the immunological system of the three different froms of drops. All preparations gave the same effects on TNF-α pro-inflammatory cytokines and the IL-8, IL-6, IL-12p70 and IL-10 chemokines. After 24h from buccal administration a significant down-regulation of all these immune parameters was found.

References: [1] Woelkart, K., Koidl, C., et al. (2005) J. Clin. Pharmacol. 45: 683–689. [2] Woelkart, K., Marth, E., et al. (2006) Int J Clin. Pharmacol. Ther. 44: 401–408.