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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 determine the plasma concentration of theacrine in rat plasma after gavage. Methods: Plasma samples were detected by RP-HPLC with caffeine as internal standard. The mobile phase consisted of Phenomenex Luna C18 (4.6 mm × 250 mm, 5 μm) and methanol-water (25:75) with a flow rate of 1.0 mL · min-1. The detection wavelength was 290 nm and the column temperature was 25 ℃. RESULTS: There was a good linear relationship between the concentration of Theacrine in the plasma of 0.5-100 mg.L-1 (R2 = 0.998 9) and the lowest limit of quantification was 0.5 mg.L-1. In theacrine plasma concentrations of 0.5,5.0,50 mg.L-1, the intra-day and inter-day precision were less than 15%, the recovery rates were (95.8 ± 8.6)%, (92.5 ± 5.0)%, ± 5.2)%. The main pharmacokinetic parameters were Cmax (35.45 ± 2.68) mg.L-1, tmax (0.51 ± 0.13) h and t1 / 2 (3.13 ± 1.37) h when the drug concentration was 30 mg.kg- AUC0-∞ (265.39 ± 94.71) mg.L-1.h. Conclusion: The method established by this study has high sensitivity and good reproducibility, which can provide the basis for theacrine research in vivo metabolism, and lay a foundation for exploring theacrine mechanism and pharmacodynamic evaluation.