摘要
目的:测定theacrine灌胃后在大鼠血浆中的血药浓度。方法:采用RP-HPLC检测血浆样品,以咖啡因为内标。色谱柱为Phenomenex Luna C18(4.6 mm×250 mm,5μm),甲醇-水(25∶75)为流动相,流速为1.0 mL.min-1,检测波长为290nm,柱温为25℃。结果:Theacrine血浆中质量浓度在0.5～100 mg.L-1线性关系良好(R2=0.998 9),最低定量限为0.5 mg.L-1。在theacrine血浆质量浓度为0.5,5.0,50 mg.L-1时,日内、日间精密度均小于15%,提取回收率分别为(95.8±8.6)%,(92.5±5.0)%,(90.3±5.2)%。当给药质量浓度为30 mg.kg-1时,主要药动学参数为Cmax(35.45±2.68)mg.L-1,tmax(0.51±0.13)h,t1/2(3.13±1.37)h,AUC0-∞(265.39±94.71)mg.L-1.h。结论:经过系统的方法学考察,该研究所建立的测定方法灵敏度较高、重复性良好,可为theacrine在体内的代谢研究提供依据,为探讨theacrine作用机制及药效学评价奠定基础。
Objective： To establish a method for the determination of theacrine in rat plasma after ig. administration of theac- fine. Method： Blood sample was taken timely from the eyes canthus of rats. Plasma was isolated and the protein was precipitated by ethyl acetate. Then the plasma concentration of theacrine was determined with RP-HPLC. Caffeine was used as the internal stand- ard. The chromatographic conditions were as follows： Phenomenex Luna Cls（4. 6 mm ×250 mm, 5 μm） at 25 ℃, a mixture of metha- nol-water （25：75） as the mobile phase, at the flow rate of 1.0 mL · min- 1 and the detection wavelength of 290 nm. Result： The line- ar range of theacrine was 0. 5-100 mg · L^-1 （R2 =0. 998 9）. The lower limit of quantification was 0. 5 mg · L^-1. The intra-day RSD was 1.49% -4. 40% and inter-day RSD was 0. 80% -10. 27%. The average extraction recoveries of theacrine were 90. 3% -95.8% at concentrations of 0. 5, 5.0, 50 mg· L^-1. The main pharmacokinetic parameters after ig. administration of theacrine at concentration of 30 mg·kg^-1were as follow： Cmax（35.45 ±2.68） mg· L^-1 tmax（0.51 ±0.13） h, t1/2（3.13 ±1.37） h, AUC0-∞ （265.39 ±94. 71 ） mg· L^-1· h. Conclusion： The method has been confirmed to be simple, stable, reproducible and with high specificity, and can be used for the pharmacokinetie study of theacrine in rats.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2013年第5期753-756,共4页
China Journal of Chinese Materia Medica
基金
国家自然科学基金项目(81274115
81102343
30901998)
北京市科技新星项目(2009A35)
教育部新世纪优秀人才项目(NCET-11-0606)
北京中医药大学自主选题中青年教师项目
