大鼠体内生地黄吸收成分分析及其药动学研究  

Absorption and pharmacokinetics of Radix Rehmanniae in rats

作　　者：钟杰[1] 谭朝丹[1] 王天明[1] 石荣[1] 马越鸣[1] 

机构地区：[1]上海中医药大学中药学院,上海201203

出　　处：《药学学报》2013年第9期1464-1470,共7页Acta Pharmaceutica Sinica

基　　金：国家重大新药创制资助项目(2012ZX09303009-001);上海高校青年教师培养资助计划(ZZszy12010);上海高校创新团队建设项目(2009)

摘　　要：本文采用液质联用方法,通过比较标准品、生地黄水提物、空白血浆和生地黄给药后不同时间的大鼠血浆样品的紫外、正负离子全扫描图、提取离子流图及选择性反应监测图,发现梓醇和筋骨草醇是生地黄主要吸收成分,桃叶珊瑚苷、二氢梓醇、地黄苷A(或地黄苷B、密力特苷)和地黄苷D亦有吸收。建立了大鼠血浆梓醇和桃叶珊瑚苷的定量分析方法及其他吸收成分的半定量分析方法。大鼠灌胃给予生地黄水提物6 g·kg 1后,梓醇和筋骨草醇Cmax、t1/2和AUC0-∞分别为(2 349.05±1 438.34)和(104.25±82.05)ng·mL-1、(0.86±0.32)和(0.96±0.37)h,(4 407.58±2 734.89)和(226.66±188.38)ng·h·mL-1,tmax均为1.00 h。梓醇和筋骨草醇的吸收和消除均很快。In this paper, absorption and pharmacokinetic study of Radix Rehmanniae was studied by liquid chromatography coupled with mass spectrometry method after oral administration to rats. By comparing the chromatograms of ultraviolet, full scan, extracted ion and selective reaction monitoring （SRM） of standard solution, Radix Rehmanniae, blank＇ plasma and rat plasma post drug administration, catalpol and ajugol were found to be the main compounds absorbed from Radix Rehmanniae. Plasma concentrations of aucubin, dihydrocatalpol, rehmannioside A （or rehmannioside B/ melittoside） and rehmannioside D were very low. Quantitative method for catalpol and aucubin and semi-quantitative method for other compounds in rat plasma were established. The pharmacokinetic study of those absorbed components was conducted after oral administration of 6 g·kg ^-1 Radix Rehmanniae water extract to rats. C max,t1/2 and AUC0-∞ ofcatalpol and ajugol were （2 349.05± 1 438.34） and （104.25±82.05） ng·mL^-1, （0.86±0.32） and （0.96±0.37） h, （4 407.58±2 734.89） and （226.66±188.38） ng·h·mL^-1, respectively, tmax was at 1.00 h for catalpol and ajugol. Both catalpol and ajugol were absorbed and excreted rapidly.

关 键 词：生地黄 梓醇 筋骨草醇 药动学 

分 类 号：R969[医药卫生—药理学]