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目的:研究吸收促进剂对大鼠胰岛素溶液(insulin solution, INS-SOL)口腔给药的吸收促进作用。方法:以血糖水平为指标,考察在各种吸收促进剂的影响下INS-SOL经正常大鼠口腔给药后的降血糖作用,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(pharmacological bioavailability, PA)。结果:不加吸收促进剂的条件下,10 U·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=20.6%),脱氧胆酸钠(5%,PA=16.5%)和卵磷酯(10%, PA=13.8%)均显著地增加INS-SOL的降血糖作用。苄泽 78 (5%)可使INS-SOL(5 U·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经口腔给药后具有显著的降血糖效果。
OBJECTIVE: To investigate the effect of absorption enhancers on the absorption of rat oral solution of insulin solution (INS-SOL). Methods: The hypoglycemic effect of INS-SOL after oral administration of INS-SOL under the influence of various absorption accelerators was investigated by means of blood glucose level. The pharmacological agents of INS-SOL under different conditions were calculated by subcutaneous injection Pharmacological bioavailability (PA). RESULTS: INS-SOL at 10 U · kg-1 had lower bioavailability (PA = 6.9%) after oral administration without absorption enhancer. (5%, PA = 14.5%), Benzyl 78 (5%, PA = 20.6%), sodium deoxycholate (5%, PA = 16.5%) and lecithin (10% PA = 13.8%) significantly increased INS-SOL hypoglycemic effect. Bezers 78 (5%) maximizes PA up to 33% for INS-SOL (5 U · kg-1). CONCLUSIONS: INS-SOL has a significant hypoglycemic effect after oral administration of an appropriate absorption enhancer.