运用单向灌流模型研究抗糖尿病创新药物西格列松大鼠在体肠的吸收

目的研究西格列松大鼠在体各肠段的吸收情况。方法运用单向灌流模型、采用高效液相色谱法对药物的质量浓度进行检测来研究药物在不同质量浓度、不同pH值下的吸收。结果西格列松在各肠段的表观吸收系数有显著性差异(P<0.05);不同质量浓度药物的表观吸收系数无显著性差异(P>0.05);不同pH值条件下药物的表观吸收系数有显著性差异(P<0.05)。结论西格列松的吸收不受药物质量浓度的影响,药物在较大质量浓度下(100 mg.L-1)也无饱和现象,在肠黏膜的转运为被动扩散过程;药物吸收有pH值依赖性,pH值越低吸收越好。

Absorption of chiglison in rat intestine using in situ single pass perfusion model

Objective To study the absorption of chiglison in rat.Methods Single pass perfusion model was used to study the absorption of chiglison at different concentrations and various pH respectively;concentration of chiglison was determined by HPLC.Results The P_(app) of chiglison showed significant difference(P<0.05)in four different regions of rat intestine;no difference(P>0.05)in P_(app) was observed when tested at different concentrations;significant difference(P<0.05)in P_(app) was observed in different pH mediums.Conclusions The absorption of chiglison is reduced in the order of duodenum,jejunum,ileum,and colon;the increase of concentration of chiglison has no effect on absorption kinetics,the absorption of chiglison is a passive diffusion process;the absorptions of the drug are pH-dependent,the lower pH value in drug solution can increase the absorption of chiglison.