Pharmacokinetic Equivalence of Taxotere and SID530, a Novel Docetaxel Formulation Containing Hydroxypropyl-beta-cyclodextrin in Monkeys

Abstract

SID530 is a new parenteral formulation of docetaxel containing hydroxypropyl-beta-cyclodextrin (HP-beta-CD). In this study, a comparative pharmacokinetic study of 2 docetaxel parenteral solutions, SID530 and Taxotere, was carried out. In a crossover experimental design, 6 male cynomolgus monkeys received each formulation by intravenous infusion of a single dose. The concentration of docetaxel in whole blood and plasma was determined using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The 2 formulations showed similar pharmacokinetic parameters in both whole blood and plasma, and displayed comparable values for maximum serum concentration (C-max), time to peak concentration (T-max), and area under the concentration-time curve (AUC). The 90% confidence intervals for the ratios of C-max and AUC values for SID530 to Taxotere were within the acceptable range of 0.80-1.20 in both plasma and whole blood. These findings indicate that SID530 and Taxotere are comparable in terms of their distribution in the blood and their plasma profile; consequently, these drugs are bioequivalent in the monkey.