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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 effect of combined use of berberine hydrochloride (BBR) and digoxin (DIG) on the pharmacokinetics of DIG in rats. Methods: The rats were randomly divided into DIG single group and DIG + BBR low, medium and high dose combination group. After single or multiple dose administration of BBR in rats, the plasma concentration of single oral DIG was determined by radioimmunoassay. Drug-time data by 3P97 pharmacokinetics software to obtain the pharmacokinetic parameters of each group. RESULTS: BBR had no significant effect on the pharmacokinetics of DIG at low dose (10 mg.kg-1), but significant at the middle and high dose (30,100 mg.kg-1). AUC0 ~ t were increased by 33%, 70% (single dose) and 27%, 75% (multiple dose) (P <0.05). CONCLUSIONS: In vivo studies showed that BBR and DIG could significantly increase their bioavailability within a certain concentration range. The mechanism may be related to the inhibition of intestinal P-glycoprotein by BBR.