胰岛素经口腔给药对正常大鼠的降血糖作用

目的　研究胰岛素溶液 (insulinsolution ,INS SOL)经正常大鼠口腔给药后的降血糖作用。方法　以血糖水平为指标 ,考察各种吸收促进剂经正常大鼠口腔给药后对INS SOL降血糖作用的影响 ,以皮下注射为对照 ,计算不同条件下INS SOL的药理生物利用度 (pharmacologicalbioavailability ,PA)。 结果　不加吸收促进剂的条件下 ,10U·kg-1的INS SOL经口腔给药后的生物利用较低 (PA =6 9% )。十二烷基硫酸钠 (5 % ,PA =14 5 % ) ,苄泽 78(5 % ,PA =2 0 6 % ) ,脱氧胆酸钠 (5 % ,PA =16 5 % )和卵磷脂(10 % ,PA =13 8% )均增加INS SOL的降血糖作用。苄泽78(5 % )可使INS SOL(5U·kg-1)的PA最高达到 33%。结论　在适当的吸收促进剂的作用下INS SOL经口腔给药后具有明显的降血糖效果。

Hypoglycaemic effect of insulin by buccal delivery in normal rats

AIM To investigate the hypoglycemic effect of buccally delivered insulin solution (INS SOL) in normal rats. METHODS The hypoglycemic response was examined after buccal delivery of INS SOL co administered with various absorption enhancers. The pharmacological bioavailability (PA) was used to evaluate the absorption enhancement of INS SOL from the buccal cavity under various conditions compared with subcutaneous injection. RESULTS In the absence of enhancers, the PA was low(6 8%) after buccal delivery of INS SOL. However, the concomitant administration of sodium lauryl phosphate, sodium deoxycholate, Brij78 as well as lecithin appeared to be more effective in increasing the hypoglycemic effects of insulin. INS SOL (5 μ·kg -1 ) containing 5% Brij 78 had the highest PA of 33%. CONCLUSION The use of proper absorption enhancers is useful for improving the buccal absorption of insulin.