胰岛素微乳大鼠肠道给药降糖作用的研究  

Hypoglycemic effect of insulin W/O microemulsions following intestinal administration to rats

作　　者：孟博宇[1] 平其能[1] 熊净[1] 高琴[1] 

机构地区：[1]中国药科大学药剂学教研室,南京210009

出　　处：《中国药科大学学报》2006年第4期304-307,共4页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.39930200)~~

摘　　要：目的:比较两种含有不同乳化剂的W/O型微乳在大鼠不同肠段对胰岛素(INS)的促吸收作用。研究微乳以及结合促吸剂N-[8-(2-羟基苯甲酰基)氨基]辛酸钠(SNAC)对INS在大鼠十二指肠给药时的降糖作用。方法:用油水乳化法制备胰岛素W/O型微乳;用葡萄糖-氧化酶法测定大鼠经时的血糖变化;采用分肠段给药的肠襻法比较两种微乳的主要促吸收部位;用大鼠十二指肠给药的方式,研究微乳及其与促吸剂SNAC结合后对胰岛素的肠道促吸收作用。结果:与溶液剂相比,遇水性介质易转化为反相微乳的微乳A,对胰岛素的主要促吸收部位在大鼠的回肠和结肠段。而遇水性介质后形成复乳的微乳B,对胰岛素的主要促吸收部位在大鼠的十二指肠以及结肠段。大鼠十二指肠给药时,微乳A中加入低剂量的SNAC就可以显著增加其降糖作用,并延长作用时间。结论:微乳制剂对胰岛素有显著的促吸收作用,促吸剂SNAC可以协同易发生转相的W/O型微乳显著增加胰岛素在肠道中的吸收。To study the absorption enhancement in W/O microemulsions with various emulsifiers and the the different regions of the rat intestine of two kinds of insulin hypoglycemic action of rats after intraduodenal administration of the microemulsions with or without the absorption enhancer sodium N-[ 8-（2-hydroxybenzoyl） amino ] caprylate （SNAC）. Methods：The W/O microemulsions was prepared by emulsifying the oil phases and water phases. The blood glucose level was detected by the glucose-oxidase method. Intestinal loops were used to identify and compare the main segments of intestines responsible for the absorption of the two kinds of preparations, and the hypoglycemic action of the insulin microemulsions with or without SNAC after intraduodenal administration to rats was examined. Results： Compared with the insulin solution, the microemulsion, which could be converted into one sort of reversal microemulsion when exposed to water, was shown to be absorbed mainly in the regions such as ileum and colon and exert remarkable hypoglycemic action in the regions. However, significant absorption of insulin in the regions such as duodenum and colon and notable decrease in the initial blood glucose level was found after administration of another type of microemulsion, which could form the multi-emulsion when encountered into water. Moreover, intraduodenal administration to rats of the first sort of microemulsion, into which low amount of SNAC was evenly incorporated, was observed to result in significant hypoglycemic actions and longer duration. Conclusion： W/O microemulsions could have potentials in the promotion of insulin absorption. In conjunction with SNAC, the easily reversing W/O microemulsion could produce remarkable hypoglycemic effects.

关 键 词：W/O型微乳 胰岛素 降糖作用 N-[8-(2-羟基苯甲酰基)氨基]辛酸钠 肠襻法 

分 类 号：R96[医药卫生—药理学]