P-glycoprotein involved in regulation of penetration of carbamazepine and phenytoin through blood-brain barrier / 中华神经科杂志

ABSTRACT

Objective To study the effect of P-glycoprotein (PGP) in regulation of penetration of carbamazepine and phenytoin through blood-brain barrier, as to indicating the entry of epileptic drugs into the brain restricted by PGP and deducing the multidrug resistance mechanisms of refractory epilepsy. Methods The microdialysis probe was placed into the cortex of rats, and after systemic injection of carbamazepine and phenytoin, dialysate was collected and the antiepiletic drug concentration in the extracellular fluid of the cerebral cortex was determined by high-performance liquid chromatography (HPLC). Then observing whether the concentration of drugs in extracellular fluid can be enhanced by PGP’s inhibitor verapamil. Results Verapamil significantly enhanced the concentration of carbamazepine in extracellular fluid of the cerebral cortex during 60—90 minutes after injection ((1.74?0.28)?g/ml in 60 minutes and (1.87?0.31)?g/ml in 90 minutes,P