摘要
目的：研究白芷中欧前胡素（IM）和异欧前胡素（IO）2种有效成分在大鼠小肠内的吸收特性。方法：采用大鼠在体单向灌流法，研究IM和IO在小肠不同部位、不同浓度及不同pH条件下的吸收情况，并用HPLC法同时测定IM和IO在灌流液中浓度的变化。结果：IM和IO在大鼠体内的最佳吸收部位都是结肠；在1．0—100．0μg·mL^-1浓度范围内，随着浓度增大，它们的吸收速率常数（Ka）和有效渗透系数（Peff）总体上逐渐减小，药物的吸收百分率相应降低；在酸性条件下，IM和IO的吸收受到pH的影响。结论：IM和IO在大鼠肠道内吸收良好，其吸收机制可能包括被动扩散与主动转运。
Objective： To study the intestinal absorption behaviors of two active components, imperatorin（IM） and isoimperatorin（IO）, in Radix Angelicae Dahuricae extracts in various intestinal segments of rat. Methods： In situ the rat single-pass intestinal perfusion model was used to study the intestinal absorption of IM and IO in duodenum, jejunum, ileum and colon respectively, and to investigate the effects of the different drug concentrations and different pH values of perfusion solution on the rat intestinal absorption. RP-HPLC was used to determine the concentration of two active components in the perfusion solution. Results： The best intestinal absorption site of IM and IO in rats was colon. The absorption rate constant（ Ka） and the effective permeability（Peff）of IM and IO had significant difference in four different regions of rat intestine（P 〈0.05）. Among the drug concentration ranges of 1.0 to 100.0μg·mL^-1 in perfusion solution, decreases in permeability values at the highest drug concentration studied in every intestinal segment suggested a saturable transport process. In the acid condition, the absorption of IM and IO were greatly affected by pH value of perfusion solution. Conclusion： IM and IO were absorbed perfectly in rat intestine. The intestinal absorption mechanism of IM and IO may be the passive diffusion combined with the active transport.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2007年第14期1094-1098,共5页
Chinese Journal of New Drugs
基金
江苏省自然科学基金(BK2005097)
关键词
肠吸收
单向灌流模型
白芷
欧前胡素
异欧前胡素
intestinal absorption
in situ single-pass perfusion model
Radix Angelieae Dahuricae
imperatorin
isoimperatorin
