冰片对卡马西平在家兔体内药代动力学的影响

目的观察冰片对卡马西平(carbam azep ine,CBZ)及10,11-环氧化卡马西平(10,11-epoxide carbam azep ine,ECBZ)在家兔体内药动学过程的影响。方法CBZ和冰片灌胃给药,高效液相法检测家兔血浆和脑脊液中CBZ及ECBZ的浓度,并计算药动学参数。结果冰片和CBZ合用可使CBZ的药动学参数T12(ka)、Tpeak、AUC增大而Ka和CL减少;ECBZ的药动学参数T12(ke)和Tpeak增大而Ke减少;ECBZ的脑血比提高。结论冰片可提高CBZ的生物利用度,减慢代谢,并促进血脑屏障对ECBZ的通透性。

Studies on the effects of borneol on the pharmacokinetics of carbamazepine in rabbits

Aim To observe the effects of borneol on the pharmacokinetics of carbamazepine(CBZ) and 10,11-epoxide carbamazepine(ECBZ) in rabbits.Methods After ig administration of bornol and CBZ,the CBZ and ECBZ were determined with HPLC,then the pharmacokinetic parameters were obtained with 3P87 program on computer.Results In the CBZ-borneol combination group,the pharmacokinetic parameters of CBZ,T_(12(ka)),T_(peak) and AUC were increased,while Ka and CL were decreased.The parameters of ECBZ,T_(12(ke)) and T_(peak) were increased,while Ke was decreased.The ratio of CSF to plasma of ECBZ at the time of 0.5,1,2 hour after ig was increased.Conclusion Borneol significantly improved the bioavailability of CBZ,inhibited the metabolism of CBZ,and enhanced the ECBZ passing through blood brain barrier.