目的:探讨熊果酸分别口服、静脉注射及合用环孢素后,其药代动力学变化。方法将15只 SD 雄性大鼠按随机数字表法分为3组,每组5只。口服给药组予80 mg·kg-1的熊果酸灌胃;合用环孢素组先予10 mg·kg-1环孢素灌胃,15 min 后再灌服80 mg·kg-1的熊果酸;尾静脉给药组予熊果酸原料药(80 mg ·kg-1,先用少量的DMSO 溶一下,再用生理盐水稀释)尾部静脉注射。采用 HPLC 方法测定血药浓度,DAS 软件分析药代动力学参数。结果与口服给药组相比较,合用环孢素组及静脉给药组其各药代动力学参数 AUC(0-t)、AUC(0-∞)及 Cmax 均显著增大(P <0.05)。结论口服给药后熊果酸在大鼠体内的生物利用度较低;环孢素可增加熊果酸的口服生物利用度。
Objective To explore the changes in pharmacokinetics of ursolic acid after oral ad-ministration,intravenous injection or combined treatment with cyclosporine.Methods Fifteen male SD rats were randomly divided into three groups,with 5 rats in each group.The oral admin-istration group was intragastrically given ursolic acid 80 mg·kg -1 .The intravenous administra-tion group was injected with ursolic acid 80 mg·kg-1 via tail vein (ursolic acid was dissolved in DMSO and then diluted in normal saline).The combined treatment group was intragastrically giv-en ursolic acid 80 mg· kg-1 15 minutes after treatment with cyclosporine 10 mg· kg-1 .Blood concentrations of ursolic acid were determined by HPLC,and pharmacokinetic parameters were analyzed using DAS software.Results Compared with oral administration group,pharmacokinet-ics parameters AUC(0-t),AUC(0-∞) and Cmax increased significantly in both intravenous adminis-tration group and combined treatment group.Conclusion The bioavailability of ursolic acid is low after oral administration in rats.Cyclosporine can increase the oral bioavailability of ursolic acid.