METHOD FOR SIMULATING INHIBITION STATE OF FUNCTIONAL ACTIVITY OF GLYCOPROTEIN-P WITH DIPEPTIDYL PEPTIDASE 4 INHIBITOR Russian patent published in 2016 - IPC G09B23/28 

FIELD: medicine.

SUBSTANCE: invention relates to experimental medicine, pharmacology and aims at studying a membership of the analyzed drug preparations among efflux carrier protein of glycoprotein-P (P-gp, ABCB1 protein), as well as at using as a control of inhibiting activity of P-gp when determining substances of similar action type. That is ensured by the experimental simulating the inhibition state of functional activity of P-gp. Vildagliptin, a dipeptidyl peptidase 4 inhibitor, is used as a preparation-inhibitor which is being intragastrically administered to a rabbit in a dose of 5 mg/kg of body weight for 14 days. Fexofenadine is used as a marker substrate of P-gp, which is being intragastrically administered to the animal in a dose of 67.5 mg/kg before and after 14-day administration of vildagliptin with subsequent measurement of fexofenadine concentration in blood plasma.

EFFECT: method provides creating such a model, which ensures a selective effect on P-gp in the absence of effect on CYP3A4 without clinically significant side effects.

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