摘要
目的:研究丹皮酚(paeonol,Pae)在正常小鼠体内的药动学过程,为Pae药理作用的研究提供实验依据。方法:正常小鼠一次性按50mg.kg-1灌胃(ig)Pae后,用HPLC法检测不同时间间隔血药浓度,血药浓度-时间(C-t)数据在计算机上经DAS ver1.0程序软件拟合,进行自动房室模型的判别及药动学参数的计算。结果:正常小鼠一次性50mg.kg-1ig Pae后血清的药-时曲线为单室模型一级吸收,其主要药动学参数为:Ka=(10.7±10.9)min-1,Ke=(0.10±0.07)min-1,Vd=(3.7±1.4)L.kg-1,t1/2Ka=(0.6±0.9)min,t1/2α=(8.7±3.9)min,CL=(0.37±0.16)L.min-1,AUC0-t=(121.9±37.3)mg.L-1.min,MRT0-t=(42.4±7.0)min,tmax=5.0min,Cmax=(14.5±6.1)mg.L-1。结论:正常小鼠ig Pae后,体内药动学过程符合单室模型一级吸收,药物进入体内迅速分布,代谢消除也较快。
OBJECTIVE To study the pharmacokinetic parameters of serum in mice after intragastric(ig) administration, for the research on pharmacological activities of paeonol(Pae). METHODS The serum samples were extracted one time with chloroform for HPLC analysis. Serum samples were obtained at different time point after ig single dose of 50 mg" kg~. The serum contention-time curve and the pharmacokinetic parameters were calculated with DAS ver 1.0 practical pharmacokinetics program. RESULTS The mean serum concention-time curve of Pae after ig administrtion of a single dose(50 mg·kg^-1 ) in mice could be fitted to first order absorption one-compartment model with a weight of 1. The main pharmacokinetic parameters of Pae at single dose of 50 mg·kg^-1 in mice were: K8 = (10. 7±10. 9)min^-1 , K8 - (0. 10±0. 07)min^-1 ,Vd = (3.7 ± 1.4) L·kg^-1 , t1/2Ka = (0. 6± 0. 9) min, t1/2α = (8.7 ± 3. 9) min, CL= (0. 37 ± 0. 16)L·min^-1, AUC, , = (121.9 ±37.3)mg·L^-1·min, MRT0-t=(42.4±7. 0)min, tmax=5.0min, and Cmax= (14.5±6.1)mg·L^-1, respectively. CONCLUSION A one compartment first order absorption model could describe the pharmacokinetics of Pae in mice after ig administration, and it is distributed and eliminated quickly. The pharmacokinetics of Pae in mice would provide essential data to the pharmacological activities research of Pae.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2006年第5期543-545,共3页
Chinese Journal of Hospital Pharmacy