木姜叶柯总黄酮大鼠口服吸收研究

Study on the oral absorption of total flavonoids from Lithocarpus litseifoliusin rats

目的研究大鼠灌胃木姜叶柯总黄酮,总黄酮中根皮苷的吸收利用及三叶苷含量对根皮苷生物利用度的影响。方法取3组大鼠,分别灌胃木姜叶柯总黄酮(含根皮苷质量分数75%、三叶苷质量分数5%),配方A(含根皮苷质量分数75%、三叶苷质量分数10%),配方B(含根皮苷质量分数75%、三叶苷质量分数20%),剂量80mg·kg-1(相当于根皮苷60mg·kg-1);另取1组大鼠静脉注射根皮苷60mg·kg-1,于给药后不同时间测定血浆根皮苷质量浓度。做血药质量浓度-时间曲线;分别以灌胃给药组血药曲线下面积(AUC)除以静脉注射给药组血药曲线下面积,计算各药根皮苷的生物利用度。结果大鼠灌胃木姜叶柯总黄酮,血浆根皮苷质量浓度最低,生物利用度只有7.8%。随着灌胃药液中的三叶苷含量增加,灌胃给药动物血浆根皮苷质量浓度和AUC明显提高。结论三叶苷可以提高木姜叶柯总黄酮中的根皮苷生物利用度。

Objective To study the absorption of phlorizin, and to observe the effect of tritobatin in total flavonoids from Lithocarpus litseifolius on phlorizin bioavailability after oral administration of total flavonoids of Lithocarpus litseifolius in rats. Methods Three groups of rats received oral administration of total flavonoids from Lithocarpus litseifolius （containing phlorizin 75 %, trilobatin 5 % ）, formula A （containing phlorizin 75 %, trilobatin 10 % ）, formula B （containing phlorizin 7 5 %, trilobatin 20 % ） at a dose of 80 mg·kg^-1 （equivalent to 60 mg·kg^-1 of phlorizin） ,respectively. Another group of rats received intravenous administration of phlorizin at a dose of 60 mg·kg^-1. Plasma phlorizin concentration was determined by HPLC after administration at different time, and concentration-time curve was then established. The bioavailability of phlorizin in total flavonoids from Lithocarpus litse- ifolius, formula A,and formula B was calculated by dividing their area under curve （AUCs） by the AUC of intravenous adminis tration of phlorizin,respectively. Results The lowest concentration of plasma phlorizin was found in total flavonoids from Litho- carpus litseifolius group with bioavailability only 7.8o//00 . The plasma concentration of phlorizin and AUCs in the groups of oral administration increased significantly with the increase of trilobatin content in the total flavonoids from Lithocarpus litseifolius, formula A and formula B. Conclusion Trilobatin can increase the bioavailability of phlorizin in the total flavonoids from Lithocarpus litseifolius.