CAJ | 학술논문

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。
목적：탐토웅과산분별구복、정맥주사급합용배포소후，기약대동역학변화。방법장15지 SD 웅성대서안수궤수자표법분위3조，매조5지。구복급약조여80 mg·kg－1적웅과산관위；합용배포소조선여10 mg·kg－1배포소관위，15 min 후재관복80 mg·kg－1적웅과산；미정맥급약조여웅과산원료약（80 mg ·kg－1，선용소량적DMSO 용일하，재용생리염수희석）미부정맥주사。채용 HPLC 방법측정혈약농도，DAS 연건분석약대동역학삼수。결과여구복급약조상비교，합용배포소조급정맥급약조기각약대동역학삼수 AUC（0－t）、AUC（0－∞）급 Cmax 균현저증대（P ＜0．05）。결론구복급약후웅과산재대서체내적생물이용도교저；배포소가증가웅과산적구복생물이용도。
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.