Study on the Pharmacokinetics of Oleanolic Acid and Dihydrooleanolic Acid by Intragastric Administra-tion and Intravenous Injection in Rats in vivo
10.6039/j.issn.1001-0408.2017.13.14
- VernacularTitle:齐墩果酸与二氢齐墩果酸灌胃及静脉注射给药后在大鼠体内的药动学研究
- Author:
Rui CHEN
;
Wei LI
;
Yong LI
;
Yao LIU
;
Jing HUANG
;
Lei TANG
- Keywords:
Oleanolic acid;
Dihydrooleanolic acid;
Rats;
UPLC-QTOF;
Pharmacokinetics;
Bioavailability
- From:
China Pharmacy
2017;28(13):1777-1780
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To study the pharmacokinetics and absolute bioavailability of oleanolic acid and its derivative di-hydrooleanolic acid in rats in vivo. METHODS:12 SD rats were randomly divided into oleanolic acid administration group and di-hydrooleanolic acid administration group,6 in each group. All rats were intragastrically given related medicine(50 mg/kg),then in-travenously injected related medicine(2 mg/kg)in tail vein after 1 week. Sample blood 0.3 mL was taken from tail vein before ad-ministration and after administration(0.1,0.25,0.5,0.75,1,1.5,2,3,5,7,9,12 h for ig;0.05,0.15,0.25,0.5,0.75,1, 2,3,5,7,9,12 h for iv). UPLC-QTOF was conducted to determine the plasma concentration,and DAS 2.0 pharmacokinetic software was used to calculate pharmacokinetic parameters and absolute bioavailability. RESULTS:After ig and iv oleanolic acid, the AUC0-∞ were(232.10±7.17),(1203.99±19.65)ng·h/mL,t1/2 were(1.75±0.10),(1.41±0.04)h respectively;after ig,cmax was (121.3 ± 18.92) ng/mL,tmax was (0.54 ± 0.10) h,absolute bioavailability was 0.77%. After ig and iv dihydrooleanolic acid, AUC0-∞ were(382.03±23.73),(386.14±10.65)ng·h/mL,t1/2 were(2.47±0.45),(1.44±0.03)h;after ig,cmax was(124.52± 12.28)ng/mL,tmax was(0.63±0.14)h,absolute bioavailability was 3.96%. CONCLUSIONS:The absolute bioavailability of di-hydrooleanolic acid is significantly higher than oleanolic acid in rats.
