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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。
Objective To study the hypoglycemic effect of insulinsolution (INS SOL) after oral administration in normal rats. Methods Based on the blood glucose level, the effects of various absorption enhancers on the hypolipidemic effect of INS-SOL were investigated after oral administration of INS. The pharmacological bioavailability of INS-SOL was calculated under hypodermic conditions (pharmacological bioavailability, PA). Results Under the condition of no absorption enhancer, 10U · kg-1 INS SOL had lower bioavailability after oral administration (PA = 69%). Sodium lauryl sulfate (5%, PA = 145%), Benzyl 78 (5%, PA = 206%), sodium deoxycholate (5% 10%, PA = 138%) increased the hypoglycemic effect of INS SOL. Benson 78 (5%) maximizes PA up to 33% for INS SOL (5U · kg-1). Conclusions INS SOL has obvious hypoglycemic effect after oral administration with appropriate absorption enhancer.