Determination of lidocaine and its metabolites by HPLC to evaluate CYP3A activity of human liver microsomes / 中国药理学通报

ABSTRACT

AIMTo evaluate CYP3A activity of hum an liver microsomes by the ratio of lidocaine(LDC) to its metabolites. M ETHODSIn 1 g?L -1 microsomal protein lidocaine was incubated at 37 ℃ for 1 hour. Lidocaine, monoethylglycinexylidide(MEGX) and glycinexylidide(GX) were determined by HPLC. RESULTSThe linear regress equations fo r LDC, MEGX and GX were = 0 293 4 X- 0 005 661 (r= 0 9 99 7 )、= 0 791 3 X- 0 008 916 (r= 0 999 3 ) and = 0 679 9 X- 0 007 770 (r= 0 998 5 ). The best conditio n for the incubation test in vitro was 2 0 mg?L -1 LDC plus 1 0 g ?L -1 microsomal protein for 60 min. The mean (MEGX+GX)/LDC ratio was 3 2 8. CONCLUSIONThe (MEGX+GX)/LDC ratio can be used to evaluate C YP3A activity of human liver microsomes.