摘要
目的 :研究胰岛素的口腔吸收及吸收促进剂、酶抑制剂对药物吸收的影响。方法 :以血糖水平为指标 ,考察各种吸收促进剂和酶抑制剂经糖尿病模型的大鼠口腔给药后对胰岛素溶液 (insulinsolution ,INS SOL)和胰岛素贴片 (insulinpatch ,INS PAT)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和INS PAT的药理生物利用度。结果 :不加吸收促进剂的条件下 ,32U·kg-1的INS SOL和10U·kg-1的INS PAT经口腔给药后的生物利用度较低 (0 .77%和 1.82 % )。 3%去氧胆酸钠和 5 %壬苯醇醚均能显著增加INS SOL和INS PAT的降血糖作用 (P <0 .0 5 )。其中 3%去氧胆酸钠作用最明显 ,INS SOL和INS PAT的生物利用度增加了近 3倍(2 .83%和 7.2 6 % )。结论 :胰岛素可通过口腔吸收 ,适当的吸收促进剂对其吸收具有显著的促进作用。
AIM: To evaluate the buccal absorption and the effects of absorption enhancers and the enzyme inhibitor on the absorption of insulin. METHODS: The hypoglycemic response was examined by buccal delivery of insulin solution (INS-SOL) and insulin patch (INS-PAT) co-administered with various absorption enhancers and the enzyme inhibitor in diabetic rats. The pharmacological bioavailability was used to evaluate the absorption enhancement of INS-SOL and INS-PAT from the buccal cavity under various conditions in comparison with subcutaneous injection. RESULTS: In the absence of enhancers, the bioavailabilities were low ( 0.77 % and 1.82 %) after buccal delivery of INS-SOL and INS-PAT. However, the concomitant administration of 3% sodium deoxycholate (SDCh) and 5% nonoxinol (NON) appeared to be more effective in increasing the hypoglycemic effect of insulin (P< 0.05 ). 3% SDCh had the optimal enhancement, and the bioavalabilities of INS-SOL and INS-PAT were increased by three times ( 2.84 % and 7.26 %). CONCLUSION: Insulin can be absorbed through the buccal mucous, and proper absorption enhancers can promote absorption function.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2003年第4期389-392,共4页
Chinese Journal of Clinical Pharmacology and Therapeutics
关键词
药理学
胰岛素
口腔吸收
吸收促进剂
口腔贴片
酶抑制剂
去氧胆酸钠
壬苯醇醚
降血糖作用
pharmacology
insulin
buccal absorption
absorption enhancers
buccal patch
the enzyme inhibitor
sodium deoxycholate
nonoxinol
hypoglycemic effect
