Application of column-switching HPLC method in evaluating pharmacokinetic parameters of zaltoprofen and its salt

Abstract

The objective of this study was to compare the pharmacokinetic parameters of zaltoprofen and those of its sodium salt in rats. Zaltoprofen, a potent non-steroidal anti-inflammatory agent, was virtually insoluble in water, but its sodium salt had excellent water solubility. To investigate the effect of aqueous solubility differences upon their pharmacokinetic parameters, minicapsules containing the drug powders were administrated orally to rats, and blood samples were taken via the common carotid artery. A column-switching high-performance liquid chromatographic analytical procedure was developed and validated for the quantitation of zaltoprofen in rat plasma samples. Our study demonstrated that the time required to reach maximum plasma concentration (Tmax) of zaltoprofen sodium was significantly reduced and its maximum plasma concentration (Cmax) was increased 1.5-fold, relative to the values for zaltoprofen. It is anticipated that the sodium salt of zaltoprofen will allow the rapid onset of the drug's action in the treatment of inflammatory diseases. Copyright © 2008 John Wiley & Sons, Ltd.