摘要
目的:考察冰片对卡马西平在大鼠体内药动学及脑组织分布的影响。方法:大鼠随机分为2组,分别给予溶媒、冰片灌胃7天,并于第7天灌胃20min后,给予卡马西平(120mg.kg-1,ig),在不同时间点采集血样及脑组织样品,测定血浆与脑组织中卡马西平的浓度,并用药动学统计软件DAS2.0计算药动学参数。结果:冰片组与溶媒对照组卡马西平的药动学参数为:t1/2β(h)(3.5±0.6)vs(10.1±0.4),AUC(0-8)(mg.L-1.h)(12.1±1.6)vs(5.4±0.6),AUC(0-∞)(mg.L-1.h)(17.5±3.0)vs(8.5±0.8),tmax(h)(0.38±0.035vs(0.25±0.012)、Cmax(mg.L-1)(4.07±0.19)vs(2.24±0.21),2组t1/2β、AUC(0-t)、AUC(0-∞)、Cmax间差异显著(P<0.05);冰片组与溶媒对照组相比15,120min时脑组织中卡马西平浓度显著升高(P<0.05)。结论:冰片提高了卡马西平的生物利用度,并增加了其脑组织分布。
OBJECTIVE The main purpose of this study was to doserce the effects of borneol on the pharmaeokinetics and brain tissue distribution of carbamazepine. METHODS The rats were given i.g. with solvent, borneol after 7 days, and intragastric carbamazepine（CBZ）（120 mg.kg-1, ig） after twenty minutes at last oral administrate inducer. The concentrations of CBZ on the plasma and brain tissue in rats were determined by HPLC. The pharmacokinetic parameters were computed by soft- ware program DAS 2. 0. RESULTS The pharmacokinetic parameters and the brain tissue concentration showed that the bioavailability of CBZ could be improved with borneol. There was obvious difference between the pharmacokinetic parameters of the borneol group vs control group, such as： t1/2β （h） （3. 5 ± 0. 6） vs （ 10. 1 ± 0. 4）, AUC （0-8） （mg. L- 1. h） （ 12. 1 ± 1.6） vs （5.4 ± 0.6）,AUC（0-∞）（mg.L-l.h）（17.5±-3.0） vs （8.5±0.8）,Cmax（mg.L-1）（4.07±0.19） vs （2.24±0.21） （P〈0.05）. Also the brain tissue concentration had obvious difference at 15,120 min （P〈 0. 05）. CONCLUSION The borneol has the enhancing effect on absorption and brain tissue distribution, and the improving effect on bioavailability of CBZ.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2011年第9期747-750,共4页
Chinese Journal of Hospital Pharmacy
