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作 者:陈新民[1] 李俊松[1] 李文[1] 韩蕾[1] 刘训红[1] 狄留庆[1] 蔡宝昌[1]
出 处:《药学学报》2010年第5期652-658,共7页Acta Pharmaceutica Sinica
基 金:江苏省"青蓝工程"科技创新团队支持计划
摘 要:考察五味子提取物中五味子醇甲、五味子甲素、五味子乙素3种主要有效成分在大鼠的肠吸收性质。本文以酚红为标示物,运用在体单向肠灌流模型并采用HPLC法测定五味子提取物中3种主要有效成分在大鼠十二指肠、空肠、回肠及结肠灌流的浓度变化。结果发现,五味子提取物中3种有效成分的每种成分在不同浓度的吸收速率常数(Ka)和有效渗透系数(Peff)均有显著性差异(P<0.05)。随着浓度的增加,其Ka、Peff值均先升高而后下降,存在高浓度饱和现象,提示其在机体内的转运可能存在主动转运或促进扩散;3种有效成分在各肠段均有较好吸收,其中十二指肠吸收最好,空肠与回肠的吸收相近无显著差异(P>0.05);3种有效成分之间在不同肠段的吸收均存在显著性差异(P<0.05),十二指肠中五味子甲素吸收最好,其他肠段的Ka、Peff大小顺序依次是五味子甲素>五味子乙素>五味子醇甲,且两两之间都存在显著性差异(P<0.05)。The aim of the study is to investigate rat intestinal absorption behavior of three main active components,schisandrol A,schisandrin A and schisandrin B in Schisandra chinensis Baill extracts in intestine of rats.With phenol red as the indicator,in situ single pass intestinal perfusion (SPIP) model was used and the concentrations of three main active components in perfusion solution of different intestinal segments (duodenum,jejunum,ileum,and colon) were determined by HPLC in combination with diode array detection.The results showed that the absorption rate constant (Ka) and effective permeability values (Peff) of three main active components in Schisandra chinensis Baill extracts had significant difference (P〈0.05) at different concentrations of perfusion solution,the Ka and Peff first increased and then decreased with the increase of drug concentration,the middle concentration was higher than those of the other two concentrations.The saturate absorption phenomena were observed,and it suggested that the transport mechanisms of three main active components in vivo were similar to active transport or facilitated diffusion.Three active components can be well absorbed in all of the intestinal segments,while duodenum is the best absorption region.The Ka and Peff of three active components in jejunum and ileum had no significant difference (P〉0.05).The absorption of the three active components displayed significant difference (P〈0.05) at different intestinal segments of rats.Schisandrin A had the best absorption in duodenum.The Ka and Peff among three active components were sequenced as follows: schisandrin A 〉schisandrin B〉 schisandrol A in other intestinal segments,and there is significant difference (P〈0.05) between them.
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