摘要
目的:研究灌服磷酸川芎嗪对大鼠体内硝苯地平的药动学过程影响。方法:24只雄性Wistar大鼠随机分为4组,分别灌服纯化水,20,40,80mg.kg-1磷酸川芎嗪,连续5d灌服10mg.kg-1硝苯地平,于0,0.10,0.25,0.50,0.75,1.0,2.0,4.0,6.0,8.0,10.0h取血,采用HPLC-MS/MS法测定血浆硝苯地平浓度,采用DAS2.0计算药动学参数。结果:与单独灌服硝苯地平相比,大鼠连续5d灌服40mg.kg-1和80mg.kg-1磷酸川芎嗪,硝苯地平AUC0-10h分别增加41.8%(P<0.05)和77.3%(P<0.01),MRT0-10h延长15.3%(P<0.05)和10.4%(P<0.05),Cl降低31.5%和45.0%。结论:40mg.kg-1和80mg.kg-1磷酸川芎嗪可增加硝苯地平的生物利用度,减慢硝苯地平的体内消除。
OBJECTIVE To investigate the effect of tetramethylpyrazine phosphate (TMPP, ligustrazine) on the pharmacokinetics of nifedipine in rats. METHODS Twenty four male Wistar rats were randomly divided into four groups, pretreated with water or 20, 40, 80 mg·kg^-1 tetramethylpyrazine phosphate for five days, then 10mg·kg^-1 of nifedipine were orally given. Blood samples were collected at 0, 0. 10, 0. 25, 0. 50, 0. 75, 1.0, 2. 0, 4. 0, 6. 0, 8.0 and 10. 0 h. Nifedipine in plasma was determined by HPLC-MS/MS, and main pharmacokinetic parameters were calculated and statistically analyzed by DAS 2. 0. RESULTS AUG0-10h of nifedipine in 40 mg·kg^-1 and 80 mg·kg^-1 TMPP plus nifedipine groups, were 41.8% (P〈0. 05) and 77. 3% (P〈0. 01) , and MRT0-10hwere 15.3% (P〈0. 05) and 10. 4% (P〈0. 05) more than that of water plus nifedipine group, but Cl were 31.5% (P〈0. 05) and 45.0% (P〈0. 05) less than that of water plus nifedipine group. CONCLUSION A given dose of TMPP could increase the bioavailability of nefidipine, and decrease its elimination process.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2011年第14期1193-1196,共4页
Chinese Journal of Hospital Pharmacy