摘要
目的:建立基于肠吸收技术快速发现龙胆中吸收成分群的方法,为龙胆质量控制指标的选择提供依据。方法:采用大鼠外翻肠囊模型,分别收集3个质量浓度龙胆提取物给药后不同时间点的肠囊液样品,并以龙胆苦苷、马钱苷酸、当药苦苷、当药苷为代表成分,采用HPLC对4种成分进行检测,分别计算其累计吸收量。结果:龙胆中6种主要成分可进入肠囊,在90 min后均能检测到;不同质量浓度的龙胆提取物中龙胆苦苷、马钱苷酸、当药苦苷、当药苷在各肠段均为线性吸收,R2均大于0.9,符合零级吸收;龙胆苦苷和当药苦苷在空肠中的吸收速率常数(Ka)随着剂量增加而增加(P<0.05),符合被动吸收,而在回肠中大、中剂量的Ka无显著差异,且均高于小剂量,符合主动吸收;当药苷在空、回肠中大、中剂量的Ka无显著差异,且均高于小剂量,符合主动吸收;马钱苷酸在回肠与空肠中的Ka随着剂量增加而增加(P<0.05),符合被动吸收。结论:基于肠吸收的质量评价指标选择方法可以用于龙胆吸收成分群的研究,药物在不同肠段中的吸收具有选择性。
Objective： To establish a method for quickly investigating the absorption ingredients which could be used as the index of quality control of Gentianae Radix et Rhizoma.Method： The absorption ingredients of Gentianae Radix et Rhizoma were investigated by using the model of in vitro everted intestinal sac（VEIS）.The intestinal sac liquors of jejunum and ileum were collected at 6 intervals（15,30,45,60,90,120 min） and gentiopicroside,loganin acid,swertiamarin and sweroside were detected by HPLC as the representative marker.The accumulative absorption quantity of gentiopicroside,loganin acid,swertiamarin and sweroside were calculated,respectively.Result： Six components could be detected in intestinal sac.In different concentrations of Gentianae Radix et Rhizoma,gentiopicroside and swertiamarin in various intestinal sections were the linear absorption（R20.9）,conformed to zero order absorption rate.In jejunum the constant of absorption rate（Ka） of gentiopicroside and swertiamarin increased with the raised dosage of Gentianae Radix et Rhizoma（P0.05）,which indicated a passive absorption manner,and the value of Ka of high and middle dosage of those in ileum were higher than that of low dosage,and the difference of Ka between high and middle dosage were not significant,which indicated a positive absorption manner.The Ka of high and middle dosage of sweroside in ileum and jejunum were higher than that of low dosage（P0.05）,and the difference of Ka between high and middle dosage were not significant,which indicated a positive absorption manner.The Ka of loganin acid in jejunum and ileum increased along with the raised dosage of Gentianae Radix et Rhizoma（P0.05）,which indicated a passive absorption manner.Conclusion： SEMAC could be used as a tool to investigate the absorption ingredients of Gentianae Radix et Rhizoma.Drug in intestine sac was selective,and the absorption part of intestine was also different.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2012年第7期969-973,共5页
China Journal of Chinese Materia Medica
基金
国家"重大新药创制"科技重大专项(2009ZX09308-003
2009ZX09301-005
2009ZX09052-021)
中医药行业科技专项(200707009)
关键词
龙胆
肠外翻模型
HPLC
吸收成分检测
Gentianae Radix et Rhizoma
in vitro everted intestinal sac
HPLC
absorption ingredients detecting
