The pharmacokinetics of XXXX metabolites in healthy volunteers.

@entity1 @entity20398 @entity72740 @entity4280 @entity72741
@entity20398 is an experimental antibacterial and antiendotoxic compound whose clinical utility as an antitumor agent is being investigated in @entity1 clinical trials. @entity20398 in aqueous solution exists in equilibrium with @entity72740 . @entity72740 is subsequently transformed to @entity72741 . The pharmacokinetic profiles of these metabolites are not well established. In this study, 18 healthy volunteers were administered 5.0 g of @entity20398 in 250 mL of 5% @entity4280 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 @entity72741 , whereas that of @entity72740 was reached before completion of infusion. The @entity20398 metabolite @entity72740 demonstrated a shorter half-life and lower systemic exposure than @entity72741 . Shortening of infusion duration increased the C(max) and AUC of @entity72740 . Changes in infusion rate did not substantially change the pharmacokinetic parameters of @entity72741 .
