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作 者:吴青青[1,2] 陈彦[1] 辛然[1,2] 王晋艳[1,2] 周蕾[1,2] 袁菱[1,2] 贾晓斌[1]
机构地区:[1]江苏省中医药研究院,国家中医药管理局中药释药系统重点研究室,江苏南京210028 [2]江苏大学药学院,江苏镇江212013
出 处:《药学学报》2012年第5期657-663,共7页Acta Pharmaceutica Sinica
基 金:国家中医药管理局中医药科学技术研究专项(06-07ZP18);江苏省中医药领军人才项目(LJ200913)
摘 要:考察甘草苷、甘草酸及甘草提取物中相应成分的大鼠在体肠吸收差异。运用大鼠在体肠灌流模型,采用UPLC和HPLC法同时测定肠灌流液、胆汁和颈静脉血样中甘草苷和甘草酸浓度,并结合肠道酶共孵育实验及对两种成分表观油水分配系数的测定,多元化比较分析甘草中甘草苷、甘草酸及提取物中相应成分在大鼠体内的吸收代谢特性。结果发现,甘草苷、甘草酸及甘草提取物中相应成分在大鼠肠道的有效渗透系数Peff值均小于0.3,表明两种成分肠道吸收均较差。各成分在十二指肠、空肠、回肠和结肠中吸收均无显著性差异;各成分单体与甘草提取物中相应成分比较发现,甘草提取物中甘草酸的各肠段Peff值略有增加,但无显著性差异;甘草提取物中甘草苷在回肠段的Peff值有显著性提高(P<0.05),其余肠段均无显著性差异,提示甘草提取物中其他成分促进甘草苷的吸收,但对甘草酸无明显影响。同时收集的提取物及单体的胆汁、血浆及肠道酶共孵育样品中均未检测到甘草苷、甘草酸及代谢产物,表明提取物中其他成分对于两种成分的影响在短时间(1~3 h)内可能未能提高其吸收入血及胆汁中的含量。The aim of this study is to investigate the rat intestinal absorption behavior of two main active components,liquiritin,glycyrrhizin and the extract of Glycyrrhiza uralensis.The rat intestinal perfusion model was employed.Concentrations of the compounds of the interest in the intestinal perfusate,bile and plasma samples were determined by HPLC and UPLC.At the same time,the intestinal enzymes incubation test and the partition coefficient determination,the absorption of liquiritin and glycyrrhizin alone and the extract were multiple analyzed.The results showed that the Peff(effective permeability) of liquiritin or glycyrrhizin alone or the extract was less than 0.3,which suggested their poor absorption in the intestine.The Peff of the two main active components or the extract was not significantly different in duodenum,jejunum,colon and ileum segment.The Peff of the glycyrrhizin in the extract had no significant difference in the four intestinal segments compared with the glycyrrhizin alone.The absorption of the liquiritin displayed significant difference(P 0.05) at ileum segment compared with the liquiritin alone,while it had no markedly change in the other three segments.This phenomenon indicated that some ingredients in the extract might improve the absorption of liquiritin.Moreover,no parent compounds and their metabolites were found in the intestinal perfusate,bile and the plasma samples.The results demonstrated that the influence of the other ingredients in the extract on the two components might not increase the amount of liquiritin and glycyrrhizin in the bile and plasma within the duration of the test.
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