EXPLORE THE NATURE AND WITHDRAWAL PERIOD OF SULFONYLUREA II GENERATION DERIVATIVE ? GLIQUIDONE ON FUNCTIONAL ACTIVITY OF THE DRUG TRANSPORTER P-GLYCOPROTEIN

In the in vivo study in rabbits the effect of gliquidone at 10 mg / kg body weight of the functional activity of the protein transporter P-glycoprotein (P-gp, ABCB1 protein) was studied. P-gp activity was evaluated by its pharmacokinetics marker substrate ? fexofenadine after a single intragastric administration. Applying gliquidonefor 14 days led to an increase in the maximum concentration of fexofenadine, its half-life, area under the concentration- time curve from zero to the last point of drawing blood, area under the concentration- time curve from zero to infinity, and the retention time of marker substrate and reduce the overall clearance and rate of absorption, indicating that the inhibition of the functional activity of the protein transporter at the level of the whole organism. On the 5- day of withdrawal period of gliquidone there was a complete or partial recovery of these pharmacokinetic parameters.