盐酸小檗碱对大鼠口服地高辛药动学的影响

Effect of berberine on pharmacokinetics of digoxin after oral administration to rats

目的： 研究盐酸小檗碱（BBR）与地高辛（DIG）合用对大鼠体内DIG药动学的影响。 方法： 大鼠随机分为DIG单用组和DIG＋BBR低、中、高剂量合用组。大鼠单剂量或多剂量给予BBR后,放免法测定单次口服DIG的血药浓度。药-时数据经3P97药动学软件处理,获得各组药动学参数。 结果： 合用后,BBR在低剂量时（10 mg·kg-1）对DIG的药动学过程无显著影响;但在中、高剂量（30,100 mg·kg-1）时有显著影响,AUC0~t分别增加了33％,70％（单剂量）和27％,75％（多剂量）（P〈0.05）。 结论： 体内研究表明BBR与DIG合用时,在一定浓度范围内,可明显提高其生物利用度,其机制可能与BBR抑制肠道P-糖蛋白有关。

Objective ： To study the effects of berberine （BBR） on the pharmacokinetics of digoxin （DIG） in rats. Method： Rats were randomly assigned into DIG, low dose-BBR, middle dose-BBR and high dose-BBR group. After singe or a 2-week ig pretreatment with BBR, serum DIG concentration was determined by radioimmunoassay. Pharmacokinetic calculations were performed on each individual set of data using 3P97 practical pharmacokinetic software. Result： No significant difference was found between the control and 10 mg·kg-1BBR combined group. After pretreatment with BBR （30,100 mg·kg-1）, the pharmacokinetic parameters of ig DIG were significantly altered. The AUC0~t of DIG with BBR increased by 33% and 70%（single）, 27% and 75% （2-week）, respectively. Conclusion： BBR increases bioavailability of DIG, which may be related to its inhibition effect on intestinal P-gp.