口服胰岛素微粒剂降血糖有效性及大鼠胃肠道有效吸收部位的研究

Studies on the effective hypoglycemia and the effective absorption site in rats after administering oral insulin microparticles(INS MP)

分别以葡萄糖氧化酶法、放射免疫分析法对服用微粒剂后的四氧嘧啶致糖尿病小鼠与狗的血糖、血清胰岛素进行测定 ,验证确有外源性胰岛素进入动物体内 ,在给药后 1h动物血清胰岛素增至最高 ,约 2h动物血糖降至最低 ,且作用强度、时间与血清胰岛素变化相对应。给药剂量在 4 0～35 0u/kg范围 ,存在量效关系 :Y(% ) =13 2 1- 1 70 7X(u/kg) ,r =0 9788。给小鼠腹腔注射葡萄糖 (2 g/kg)可见 ,微粒剂 (17u/kg)能对抗并减缓因注射外源还原性单糖引起的动物血糖升高 ,0 5h可抵抗百分率达 86 % (P <0 0 0 5 )。经四氧嘧啶糖尿病大鼠胃肠道不同部位给药发现 :给药部位不同 ,微粒剂降血糖程度有显著差别 ,其中经回肠部位给药效果最好 ,降血糖百分率达 5 6 %(P <0 0 1)。

The levels of glucose and insulin (INS) in serum were detected by the methods of glucose oxidation enzyme and radioimmunoassay for the aloxan caused diabetic mice and normal dogs to which INS MP was adminstrated. It was indicated that there was exogenous INS in above animals. The highest INS level was at 1 h after oral administering INS MP, and at 2 h for the lowest point of glucose. The action intensity and the time corresponded to the change of serum INS. There was the correlation between hypoglycemic percentage and dosage, Y(%)=13 21-1 707X(u/kg) in the dose range from 4 0 to 35 0. The INS MP could retard the increase of mice′ blood glucose caused by exogenous glucose, and the anti glucose percentage was 86% (P<0 005). It was showed through administering the INS MP to different sites in diabetic rats′ gastrointestinal tracts that the best absorption site was the ileum and the hypoglycemic strength was 56% (P<0 01).