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中国临床药理学与治疗学 ›› 2003, Vol. 8 ›› Issue (4): 389-392.

• 研究原著 • 上一篇    下一篇

不同吸收促进剂对大鼠口腔胰岛素吸收作用的影响

俞佳, 杨民锋1, 袁弘2   

  1. 浙江省人民医院药剂科,杭州 310014,浙江;
    1杭州民生药业集团有限公司,杭州 310011,浙江;
    2浙江大学药学院,杭州 310006,浙江
  • 收稿日期:2003-03-20 修回日期:2003-03-27 出版日期:2003-08-26 发布日期:2020-11-19
  • 通讯作者: 俞佳,女,硕士,药师,主要从事医院药学工作。Tel:0571-85239988-3702 E-mail:yujiazhz@hzcnc.com

Effects of the various absorption enhancers on the buccal absorption of insulin in rats

YU Jia, YANG Min-Feng1, YUAN Hong2   

  1. Department ofPharmacy,ZhejiangProvincialPeople' s Hospital,Hangzhou 310014,Zhejiang,China;
    1MinshengPharmaceutical GrouPCo .LTD,Hangzhou 310011,Zhejiang,China;
    2College ofPharmacy,Zhejiang University,Hangzhou 310006,Zhejiang,China
  • Received:2003-03-20 Revised:2003-03-27 Online:2003-08-26 Published:2020-11-19

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(insulin solution,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<0.05)。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7.26 %)。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。

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

Abstract: 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 insulinPatch(INS-PAT)co-administered with various absorption enhancers and the enzyme inhibitor in diabetic rats.ThePharmacological 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 werelow(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,andProper absorption enhancers canPromote absorption function.

Key words: pharmacology, insulin, buccal absorption, absorption enhancers, buccalPatch, the enzyme inhibitor, sodium deoxycholate, nonoxinol, hypoglycemic effect

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