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目的 建立测定胡黄连苷 I血浆浓度的RP HPLC法 ,并研究比较大鼠和犬体注射胡黄连苷 I(HD I)后体内药代动力学特征。方法 采用乙腈 -水 (2 0∶80 )为流动相 ,AgilentXDBC18柱 (2 5 0mm× 4 .6mm ,5 μm)为固定相 ,紫外检测波长 2 77nm ,内标法测定。大鼠和Beagle犬分别ivHD I 7、2 .5mg·kg-1,采用RP -HPLC法测定药后血浆药物浓度 ,用 3p97药动学软件对血药浓度 -时间数据进行拟合。结果 最低定量限为 0 .1μg·ml-1,方法回收率大于 90 % ,日内日间RSD均小于 5 %。大鼠和Beagle犬单次ivHD I后 ,血药浓度 -时间曲线均呈二室开放模型 ,半衰期 (T1/ 2 β )、清除速率 (CLs)、平均滞留时间 (MRT)等主要药动学参数无显著性差异。结论 HD I在大鼠和犬体内代谢较快 ,分布较广 ,清除较快。在大鼠和犬体内药动学行为无显著性差异。
Objective To establish a RP HPLC method for determination of plasma concentration of berberine I and study the in vivo pharmacokinetic characteristics of rat and dog injected with berberine I (HD I). Methods Acetonitrile-water (20:80) was used as the mobile phase. Agilent XDBC18 column (250mm×4.6mm, 5μm) was used as the stationary phase. UV detection wavelength was 2 77nm. The internal standard method was used for the determination. The rats and Beagle dogs had ivHD I of 7 and 2.5 mg·kg -1 , respectively. Plasma drug concentration was measured by RP-HPLC. The plasma concentration-time data were fitted by 3p97 pharmacokinetic software. Results The minimum limit of quantitation was 0.1 μg·ml-1. The recovery of the method was greater than 90%. The intra-day RSD was less than 5%. After one-time iv HD I in rats and Beagle dogs, the plasma concentration-time curve showed a two-compartment open model, and the main pharmacokinetic parameters such as half-life (T1/ 2 β ), clearance rate (CLs), mean residence time (MRT), etc. No significant difference. Conclusions HD I is metabolized rapidly in rats and dogs, with a wide distribution and rapid clearance. There was no significant difference in pharmacokinetic behavior between rats and dogs.