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The Pharmacokinetics of Taurolidine Metabolites in Healthy Volunteers
Author(s) -
Gong Li,
Greenberg Howard E.,
Perhach James L.,
Waldman Scott A.,
Kraft Walter K.
Publication year - 2007
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270007299929
Subject(s) - pharmacokinetics , medicine , pharmacology , metabolite , active metabolite , adverse effect , anesthesia
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.