The pharmacokinetics of taurolidine metabolites in healthy volunteers.
Publication/Presentation Date
6-1-2007
Abstract
Taurolidine is an experimental antibacterial and antiendotoxic compound whose clinical utility as an antitumor agent is being investigated in human clinical trials. Taurolidine in aqueous solution exists in equilibrium with taurultam. Taurultam is subsequently transformed to taurinamide. The pharmacokinetic profiles of these metabolites are not well established. In this study, 18 healthy volunteers were administered 5.0 g of taurolidine in 250 mL of 5% polyvinylpyrrolidone in water over 2, 1, or 0.5 hours by intravenous infusion in a parallel-group design. All subjects noted discomfort at the infusion site, although there were no serious adverse events. t(max) generally occurred at the end of infusion for taurinamide, whereas that of taurultam was reached before completion of infusion. The taurolidine metabolite taurultam demonstrated a shorter half-life and lower systemic exposure than taurinamide. Shortening of infusion duration increased the C(max) and AUC of taurultam. Changes in infusion rate did not substantially change the pharmacokinetic parameters of taurinamide.
Volume
47
Issue
6
First Page
697
Last Page
703
ISSN
0091-2700
Published In/Presented At
Gong, L., Greenberg, H. E., Perhach, J. L., Waldman, S. A., & Kraft, W. K. (2007). The pharmacokinetics of taurolidine metabolites in healthy volunteers. Journal of clinical pharmacology, 47(6), 697–703. https://doi.org/10.1177/0091270007299929
Disciplines
Business Administration, Management, and Operations | Health and Medical Administration | Management Sciences and Quantitative Methods
PubMedID
17395893
Department(s)
Administration and Leadership
Document Type
Article