大鼠在体单向灌流法研究莪术油磷脂复合物的肠吸收

目的研究莪术油磷脂复合物在大鼠肠内的吸收情况。方法选用大鼠在体单向灌流模型,以莪术油为对照组,采用HPLC法,以莪术油中主要活性成分呋喃二烯和牻牛儿酮为检测指标,同时测定复合物在大鼠十二指肠、空肠、回肠及结肠的吸收。结果莪术油磷脂复合物中的呋喃二烯和牻牛儿酮的有效渗透系数(Peff)分别约为6×10-5 cm.s-1和1×10-4 cm.s-1,莪术油中的呋喃二烯和牻牛儿酮的有效渗透系数分别约为1×10-5 cm.s-1和2×10-5 cm.s-1,说明莪术油磷脂复合物在大鼠肠内的吸收比莪术油提高了5倍。结论应用磷脂复合物技术可显著改善莪术油的两亲性,提高莪术油在大鼠肠内的吸收。莪术油磷脂复合物的吸收无自身浓度抑制作用,在肠黏膜的转运为被动扩散过程;呋喃二烯和牻牛儿酮均无特殊的吸收窗;在各个肠段均属于高渗透性药物。本实验为莪术油口服剂型的研究提供了有效数据。

Absorption of the phospholipid complex of zedoary turmeric oil in rats intestine using in situ single pass perfusion model

Objective To study the absorption of the phospholipid complex of the zedoary turmeric oil(ZO-PC)in the intestine of rats. Methods Using in situ single pass perfusion model,and with the zedoary turmeric oil as the control group,the concentrations of furanodiene(FDE) and germacrone in perfusate were determined by HPLC in 4 intestinal segments(duodenum,jejunum,ileum and colon). Results The Peffs of the FDE and germacrone in the ZO-PC were 6× 10-5 cm·s-1 and 1× 10-4 cm·s-1 respectively,and in the oil were 1×10-5 cm·s-1 and 2× 10-5 cm·s-1.In short,the Peffs of ZO-PC was 5 times higher than the oil. Conclusions The phospholipid complex can increase the hydrophilicity of the zedoary turmeric oil,which improves the absorption in intestine of rats significantly.The concentrations of ZO-PC have no significant effect on the Peffs,the absorption of ZO-PC is in the passive diffusion process;the two components have no special absorption window in the 4 intestinal segments;the ZO-PC is hypertonic in all the 4 intestine segments of rats.The study provides effective data for the research of the zedoary turmeric oil in peroral dosage form.