Effects of Heishun Tablets Combined with Rheum palmatum on the Pharmacokinetics of Hypaconitine in Rats / 中国药房

ABSTRACT

OBJECTIVE:To study the effects of Heishun tablets combined with Rheum palmatum on the pharmacokinetics of hypaconitine in rats. METHODS:Rats were randomly divided into single drug group(Heishun tablets decoction)and drug combi-nation group(Heishun tablets-R. palmatum mixture decoction),with 18 rats in each group. They were given relevant drugs intragas-trically,by 10 g(medicinal materials)/kg of Heishun tablets. 0.3 ml blood samples were collected before(0 h)and 0.083,0.167, 0.333,0.5,0.75,1,1.5,2,3,4,6,8,10 h after medication with 6 rats at each time point,respectively. The blood concentra-tion of hypaconitine was determined by HPLC-MS using palmatine hydrochloride as internal standard. DAS 2.0.1 software was used to calculate pharmacokinetic parameters. RESULTS:The linear range of hypaconitine was 0.102 4-100 ng/ml (r=0.998 7),and the limit of quantification was 0.1 ng/ml. The pharmacokinetic parameters of single drug group vs. drug combination group were as follows as tmax of (0.50 ± 0.086) h vs. (0.75 ± 0.132)h;t1/2 of (9.967 ± 1.123) h vs. (3.708 ± 0.507) h;AUC0-10 h of (26.087 ± 0.672) μg·h/L vs.(6.516 ± 1.135) μg·h/L;cmax of (6.124 ± 2.312) μg/L vs. (1.592 ± 0.051) μg/L. Compared with single drug group,t1/2,AUC0-10 h and cmax of hypaconitine were decreased in drug combination group,with statistical significance (P<0.05). CONCLUSIONS:R. palmatum can inhibit the absorption of hypaconitine in rats,and speed up the elimination of it in rats.