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.
1 cl, 3 tbl
Title | Year | Author | Number |
---|---|---|---|
METHOD FOR EXPERIMENTAL FINASTERIDE SIMULATION OF INDUCTION OF FUNCTIONAL ACTIVITY OF GLYCOPROTEIN-P | 2012 |
|
RU2504018C1 |
METHOD TO MODEL CONDITION OF INHIBITION OF FUNCTIONAL ACTIVITY OF GLYCOPROTEIN-P BY LYNESTRENOL IN TRIAL | 2014 |
|
RU2553362C1 |
MEANS FOR REDUCTION OF GLYCOPROTEIN-P FUNCTIONAL ACTIVITY AND EXPRESSION | 2017 |
|
RU2649134C1 |
METHOD OF DETERMINING FUNCTIONAL ACTIVITY OF GLYCOPROTEIN-P | 2015 |
|
RU2587780C1 |
METHOD OF ABCB1 PROTEIN INHIBITION IN EXPERIMENT IN VITRO | 2023 |
|
RU2811993C1 |
METHOD FOR ASSESSING THE FUNCTIONAL ACTIVITY OF GLYCOPROTEIN-P IN THE BLOOD-BRAIN BARRIER | 2018 |
|
RU2677286C1 |
HYDROLYZATE OF TANSY FLOWERS COMPLEX POLYSACCHARIDE COMPLEX AS A GLYCOPROTEIN-P TRANSPORTER PROTEIN INHIBITOR | 2019 |
|
RU2699042C1 |
METHOD FOR IMPROVING DRUG USE SAFETY IN TREATING PATIENTS WITH ALCOHOL WITHDRAWAL SYNDROME | 2018 |
|
RU2690522C1 |
METHOD FOR INHIBITION OF GLYCOPROTEIN-P IN AN IN VITRO EXPERIMENT | 2021 |
|
RU2779177C1 |
THERAPEUTIC USE OF ESLICARBAZEPINE | 2008 |
|
RU2488397C2 |
Authors
Dates
2016-11-20—Published
2015-06-29—Filed