The pharmacokinetics of taurolidine metabolites in healthy volunteers.

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Gong L, Greenberg HE, Perhach JL, Waldman SA, Kraft WK

The pharmacokinetics of taurolidine metabolites in healthy volunteers.

J Clin Pharmacol. 2007 Jun;47(6):697-703. doi: 10.1177/0091270007299929. Epub 2007 Mar 29.

PubMed ID
17395893 [ View in PubMed
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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.

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