菊花黄酮及其水解产物效应成分在家兔体内动力学研究

Phannacokinetics of active component of Chrysanthemum morifolium extracts and its acid hydrolysate in rabbits

目的 比较家兔口服菊花提取物(CME)及其酸水解产物后,其效应成分(木犀草素和芹菜素)的动力学参数,阐明菊花黄 酮给药形式对其生物利用度的影响。方法 健康家兔单剂量(200mg·k-1)灌胃CME及其酸水解产物,以RP-HPLC测定给药 后不同时间点木犀草素和芹菜素血浆药物浓度。使用3P87软件拟合药动学参数,Microsoft Excel软件进行数据统计分析。结 果 家兔灌胃CME或其酸水解产物,血浆中木犀草素浓度较高,其药动学过程符合一室模型,血浆中芹菜素浓度在定量限以 下。两种形式给予家兔灌胃后,所得木犀草素药动学参数表明,与CME给药比较,以水解CME给家兔灌胃,木犀草素在其体 内的血药浓度达峰时间tmax滞后,最高血药浓度ρmax降低,而平均滞留时间MRT延长。结论 经Microsoft Excel软件统计分析, 以原型CME或水解CME给健康家兔灌胃,即CME中黄酮类化合物以苷或苷元的形式给药,在家兔体内的生物利用度无显著 性差异(P>0．05)。

OBJECTIVE To characterize and compare the metabolic pharmacokinetics of the active components （ luteolin and apigenin） in rabbit after an oral administration of acid hydrolysate of Chrysanthemum morifolittm extracts （CME） or intact CME, and clarify whether the bioavailability of flavoloids from Chrysanthemum morifolium Ramat. would be modified due to the preparation of flavonoids forms. METHODS The concentrations of luteolin and apigenin in plasma were determined by HPLC method after a single oral dose of 200 mg·kg^-1 of intact CME and hydrolysate of CME was administered to rabbits. The pharmacokinetic parameters were calculated by software 31987 and statistical analysis was performed by software Microsoft Excel. RESULTS The plasma concentration of luteolin was determined accurately and the pharmacokinetic profile was discribed by an one-compartment model. However, the present study showed that the concentration of apigenin was too low to be measured accurately. There were some differences in pharmacokinetic parameters for active component （luteolin） between the hydrolysate of CME and intact CME apparently. Furthermore, the oral hydrolysate of CME resulted in a delayed tmax, lower ρmax and longer MRT （mean residence time） for luteolin than those after an oral dose of intact CME. CONCLUSION By statistical analysis, the bioavailability of luteolin reveals no significant difference （ P 〉 0.05） after an oral administration of acid hydrolysate of CME or intact CME to rabbit.