摘要
研究静注和灌胃给予一定量人参皂苷Rg1后,其原形和3种代谢产物的药代动力学。以Wistar大鼠为模型动物,以LC-MS/MS法测定血浆中人参皂苷Rg1及其代谢产物的浓度,并计算药代动力学参数。灌胃给药后,在血浆中检测到人参皂苷Rg1、Rh1、F1和原人参三醇4种物质。其Tmax分别为0.92、3.64、5.17和7.30h,MRT分别为2.68、5.06、6.65和5.33h,AUC0-t为2363.5、4185.5、3774.3和396.2ng·mL-1·h。静注给药后,在血浆中检测到人参皂苷Rg1、Rh1和F13种物质。其T1/2β分别为3.12、5.87和6.87h,MRT分别为1.92、5.99和7.13h,AUC0-t分别为1454.7、597.5和805.6ng·mL-1·h。结果表明灌胃给药后,大鼠体内的人参皂苷Rg1代谢产物的量超过原形药,且代谢产物的吸收和消除速率相对缓慢。静注给药后,大鼠体内的人参皂苷Rg1以原形为主,但仍有少量代谢产物存在,且代谢产物的吸收和消除速率相对缓慢。
To study the pharmacokinetics of ginsenosides Rg1 and its metabolites after iv and oral admini-stration in Wistar rats,the LC-MS/MS method was selected to determine ginsenosides Rg1 and its metabolites in plasma and their pharmacokinetic parameters were calculated.After oral administration of ginsenosides Rg1 to rats,ginsenosides Rg1,Rh1,F1 and protopanaxatriol （Ppt） could be detected in plasma.Their Tmax were 0.92,3.64,5.17,and 7.30 h,respectively;MRT were 2.68,5.06,6.65,and 5.33 h,respectively;AUC0-t were 2 363.5,4 185.5,3 774.3,and 396.2 ng·mL＇,余凌英-1·h,respectively.After iv administration of ginsenosides Rg1 to rats,ginsenosides Rg1,Rh1 and F1 could be detected in plasma.Their T1/2βs were 3.12,5.87,and 6.87 h,respectively;MRTs were 1.92,5.99,and 7.13 h,respectively;AUC0-ts were 1 454.7,597.5,and 805.6 ng·mL-1·h,respectively.So,it can be concluded that after oral administration,the amounts of metabolites were higher than the prototype in vivo,and the distribution and elimination of the metabolites were relatively slow.After iv administration,the amount of prototype were higher than that of the metabolites in vivo,and the distribution and elimination of the metabolites were relatively slow.
出处
《药学学报》
CAS
CSCD
北大核心
2010年第5期636-640,共5页
Acta Pharmaceutica Sinica
基金
四川省教育厅基金课题(07ZB019)
