茶碱在正常及肝纤维化大鼠体内的药物动力学  

Pharmacokinetic of theophylline in normal and hepatic fibrosis rats

作　　者：张懋璠 蒋昆谕[1] 韩龙[1] 赵妍[1] 王欣[1] 孟胜男[1] 

机构地区：[1]中国医科大学药学院药剂教研室,辽宁沈阳110001

出　　处：《中国生化药物杂志》2012年第6期747-749,753,共4页Chinese Journal of Biochemical Pharmaceutics

基　　金：国家自然科学基金面上项目(编号:81173123)

摘　　要：目的比较茶碱在正常及肝纤维化大鼠体内的药物动力学。方法 SD大鼠24只,分成4组:静脉给药正常组、静脉给药模型组、口服给药正常组和口服给药模型组,每组各6只,采用尾静脉注射或灌胃方式给予茶碱5mg/kg,用HPLC法测定茶碱血药浓度,运用DAS2.1.1拟合药动学参数,并采用SPSS13.0软件进行统计分析。结果在口服和静脉给药条件下,茶碱的药动学参数AUC0-24h、AUC0-∞、CLz(或CLz/F)、MRT0-24h、MRT0-∞和t1/2z在正常鼠和肝纤维化鼠之间差异有统计学意义(P<0.05),Cmax,tmax,Vz(或Vz/F)的差异则无统计学意义。结论茶碱在大鼠体内的药动学会受肝纤维化显著影响。Purpose To compare the pharmacokinetics of theophylline in normal and hepatic fibrosis rats. Methods Twenty-four Spraque-Dawley rats were divided into four groups（normal group with intrave- nous injection, hepatic fibrosis group with intravenous injection, normal group with garage administration and hepatic fibrosis group with garage administration） of which each got six rats and they were adminis- trated with theophylline 5 mg/kg via gavage or tail intravenous injection. The concentration of theophylline in plasma was determined by HPLC method. The pharmacokinetic parameters were fitted by DAS2.1.1 software and statistically analyzed by SPSS13.0 software. Results There was significant difference be- tween normal group and hepatic fibrosis group in pharmacokinetic parameters of AUC0-24h , AUG0-∞ , CLz （ or CLz/F） , MRT0.24h, MRT0-∞ and t1/2z （P 〈 0.05） under the condition of gavage and intravenous injection. There were no significant differences between normal group and hepatic fibrosis group in pharmacokinetic parameters of C t Vz （ or VJF） （P 〉 0.05 ）. Conclusion The metabolism of theophylline in rats was significantly affected by hepatic fibrosis.

关 键 词：茶碱 肝纤维化 大鼠 药物动力学 

分 类 号：R969.1[医药卫生—药理学]